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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 559 journals)
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Journal Cover Saudi Pharmaceutical Journal
  [SJR: 0.417]   [H-I: 14]   [0 followers]  Follow
    
  This is an Open Access Journal Open Access journal
   ISSN (Print) 1319-0164
   Published by Elsevier Homepage  [2970 journals]
  • The Genetic Profiles of CYP1A1, -A2 and -2E1 Enzymes as Susceptibility
           Factor in Xenobiotic Toxicity in Turkish Population

    • Abstract: Publication date: Available online 16 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): ARICI Merve, ÖZHAN Gül
      Evaluation and sequencing of heritable alterations in the human genome and the large-scale identification of gene polymorphism for understanding the genetic background of individuals in response to potential toxicants are provided by toxicogenetics. Cytochrome P450 (CYP) enzymes play role not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds. CYP1A1, CYP1A2 and CYP2E1 enzymes, which are in phase I enzymes, are responsible for metabolic activation and detoxification of several chemical compounds. In the present study, it was determined the genotype and allele frequency of CYP1A1∗2A, CYP1A2∗1C, CYP1A2∗1F, CYP2E1 and CYP2E1∗6, very common and functional single-nucleotide polymorphisms (SNPs), in Turkish healthy volunteers. It is believed that the determination of polymorphisms in the enzymes may be beneficial to prevent and reduce and adverse effects and death in response to drugs. The allele frequencies of these genes were 24, 9, 33, 42, and 12%, respectively. In the present study, the genotype profile of Turkish population was determined about critical enzymes for xenobiotic metabolism. It is suggested that obtained results might be beneficial in order to dose adjustment of drugs and prevention of adverse reactions, and further investigation about mentioned enzymes and their polymorphisms.


      PubDate: 2016-06-18T15:56:39Z
       
  • Neonatal parenteral nutrition: Review of the pharmacist role as a
           prescriber

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Mohamed H. Ragab, Mohammed Y. Al-Hindi, Meshari M. Alrayees
      Introduction In the context of the continuous quest to improve the care of the neonates especially the critically ill premature infants, the extended role of pharmacists in the process of parenteral nutrition order writing and effective participation in decision-making especially in the neonatal population is increasingly important. This review aims to present results from the literature review of available evidence on the pharmacist role in neonatal parenteral nutrition therapy. Material and methods Key medical, clinical, and review databases were searched; relevant articles were retrieved and evaluated. Results and discussion A total of 19 papers out of 7127 searched papers met the criteria for inclusion, discussing the review topic. The main focus of the selected papers was on parenteral nutrition practice as related to the pharmacy practice. The overall quality of studies was mixed. Conclusion Overall, the review presents the up-to-date status of the most recent analysis being undertaken on the topic of pharmacist involvement in the parenteral nutrition order writing practices and more specific in the neonatal population over the period from 1979 to 2013. The overall impression is that the practice of pharmacist writing neonatal parenteral nutrition orders already exists, but still limited if compared with the practice of pharmacist writing adult parenteral nutrition orders which is much more established in many countries. There was no single clinical study evaluating this practice, as we were able to retrieve only two surveys, which make it difficult to evaluate the pharmacist role in this area. Nevertheless, despite the wide variation in literature types, characteristics and quality, there are consistent patterns across all the reviewed literatures that competencies of the pharmacist in this field are well represented, which make it very important to carry out good quality clinical studies in this field. Finally, we are currently conducting a prospective clinical study to evaluate the impact of clinical pharmacist as a neonatal PN prescriber, this impact will be judged through the study outcomes as reducing the metabolic and electrolyte complications and increasing the mean daily weight gain during PN therapy and reducing the average number of days of PN till enteral feeding is achieved.


      PubDate: 2016-06-11T09:45:41Z
       
  • Prolonged Exposure of Colon Cancer Cells to 5-Fluorouracil Nanoparticles
           Improves its Anticancer Activity

    • Abstract: Publication date: Available online 6 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Essam Tawfik, Maqusood Ahamed, Abdulaziz Almalik, Mohammad Alfaqeeh, Aws Alshamsan
      In this study, we aimed to improve the anticancer effect of 5-FU on human colon cancer cell lines by incorporating in poly(D,L lactic-co-glycolic acid) (PLGA) nanoparticles (NPs). The 5-FU-PLGA NPs were prepared by nanoprecipitation technique. Prepared NPs were moderately dispersed with an average diameter of 133±25.19 nm. Scanning Electron Microscope (SEM) images revealed spherical structures with subtle surface irregularity. Free 5-FU dose-response curves were constructed (12.5-2000 μM) using MTT assay on HCT 116 and HT-29 cell lines for 1, 3, and 5 days. The calculated IC50 on HCT 116 were 185 μM after 1 day, 11.3 μM after 3 days, and 1.48 μM after 5 days. On HT-29, IC50 was only reached after 5 days of 5-FU treatment (11.25 μM). The HCT 116 viability following treatment with 100 μM 5-FU in free or NPs forms for 3 days was 38.8% and 18.6%, respectively. Similarly, when 250 μM was applied, HCT 116 viability was 17.03% and 14.6% after treatment with free and NPs forms of 5-FU, respectively. Moreover, HT-29 cell viability after 250 μM 5-FU treatment in free or NPs forms was 55.45% and 34.01%, respectively. We also noticed that HCT 116 cells were more sensitive to 5-FU-PLGA NPs as compared to HT-29 cells. Overall, our data indicate that 5-FU activity is time dependent and the prolonged effects created by PLGA NPs may contributed, at least in part, to the noticed enhancement of the anticancer activity of 5-FU drug.


      PubDate: 2016-06-11T09:45:41Z
       
  • Drug safety: The concept, inception and its importance in patients’
           health

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Thamir M. Alshammari
      Background Drug safety is one of the hottest topics in daily medical practice, particularly with regard to approving new medication or questioning the possibility of withdrawing a drug from the market. Aim The aim of this review is to highlight the importance of the drug safety concept and its impact on patients’ health. Methods A literature search was conducted using Pubmed®, EMBASE®, EBSCO and Medline in the period between 1980 and 2013. The terms used in the search included “Drug Safety”, “Medication Safety”, “Patient Safety”, “Drug Interaction”, “Drug Pharmacokinetic”, and “Adverse Drug Reaction”. All retrieved abstracts were evaluated within the context of the review objectives. The full texts of the selected articles were included in this review. Studies in non-English language were excluded in this review. Results Since the early days of the past century, many acts, laws, or amendments have been created to make sure that approved drugs are first safe and then effective. Furthermore, these regulations are continuing to change to make sure that these drugs have a positive benefit–risk balance. Personalized medicine should be considered when medications are given to patients because the pharmacokinetic process inside the body varies from patient to patient and from one specific disease state to another. However, adverse drug reactions can be minimized if more precautions are taken by healthcare professionals, especially including the patient as one pillar of the therapeutic plan and providing more patient counseling, which will improve drug safety. Conclusion The drug safety concept has earned a lot of attention during the past decade due to the fact it plays a major role in patients’ health. Recent laws stress this concept should be included in the process of new medications’ approval and continued conduct of post-marketing drug evaluations. Benefit–risk assessment should be considered by all health care professionals when they need to give specific drugs to specific groups of patients. Therefore, more care should be given to some patients, such as pregnant women, children and the elderly, since they are considered vulnerable populations.


      PubDate: 2016-06-11T09:45:41Z
       
  • Biosynthesis of metallic nanoparticles using plant derivatives and their
           new avenues in pharmacological applications – An updated report

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Palaniselvam Kuppusamy, Mashitah M. Yusoff, Gaanty Pragas Maniam, Natanamurugaraj Govindan
      The field of nanotechnology mainly encompasses with biology, physics, chemistry and material sciences and it develops novel therapeutic nanosized materials for biomedical and pharmaceutical applications. The biological syntheses of nanoparticles are being carried out by different macro–microscopic organisms such as plant, bacteria, fungi, seaweeds and microalgae. The biosynthesized nanomaterials have been effectively controlling the various endemic diseases with less adverse effect. Plant contains abundant natural compounds such as alkaloids, flavonoids, saponins, steroids, tannins and other nutritional compounds. These natural products are derived from various parts of plant such as leaves, stems, roots shoots, flowers, barks, and seeds. Recently, many studies have proved that the plant extracts act as a potential precursor for the synthesis of nanomaterial in non-hazardous ways. Since the plant extract contains various secondary metabolites, it acts as reducing and stabilizing agents for the bioreduction reaction to synthesized novel metallic nanoparticles. The non-biological methods (chemical and physical) are used in the synthesis of nanoparticles, which has a serious hazardous and high toxicity for living organisms. In addition, the biological synthesis of metallic nanoparticles is inexpensive, single step and eco-friendly methods. The plants are used successfully in the synthesis of various greener nanoparticles such as cobalt, copper, silver, gold, palladium, platinum, zinc oxide and magnetite. Also, the plant mediated nanoparticles are potential remedy for various diseases such as malaria, cancer, HIV, hepatitis and other acute diseases.


      PubDate: 2016-06-11T09:45:41Z
       
  • Dilemmas of the causality assessment tools in the diagnosis of adverse
           drug reactions

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Lateef M. Khan, Sameer E. Al-Harthi, Abdel-Moneim M. Osman, Mai A. Alim A. Sattar, Ahmed S. Ali
      Importance: Basic essence of Pharmacovigilance is prevention of ADRs and its precise diagnosis is crucially a primary step, which still remains a challenge among clinicians. Objective: This study is undertaken with the objective to scrutinize and offer a notion of commonly used as well as recently developed methods of causality assessment tools for the diagnosis of adverse drug reactions and discuss their pros and cons. Evidence review: Overall 49 studies were recognized for all assessment methods with five major decisive factors of causality evaluation, all the information regarding reasons allocating causality, the advantages and limitations of the appraisal methods were extracted and scrutinized. Findings: From epidemiological information a past prospect is designed and subsequent possibility merged this background information with a clue in the individual case to crop up with an approximation of causation. Expert judgment is typically based on the decisive factor on which algorithms are based, nevertheless in imprecise manner. The probabilistic methods use the similar principle; however connect probabilities to each measure. Such approaches are quite skeptical and liable to generate cloudy causation results. Causation is quite intricate to ascertain than correlation in Pharmacovigilance due to numerous inherent shortcomings in causality assessment tools. Conclusions and relevance: We suggest that there is a need to develop a high quality assessment tool which can meticulously establish suitable diagnostic criteria for ADRs with universal acceptance to improvise the fundamental aspect of drug safety and evade the impending ADRs with the motive to convert Pharmacovigilance into a state of art.


      PubDate: 2016-06-11T09:45:41Z
       
  • Hyperphosphatemia Management in Patients with Chronic Kidney Disease

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Ahmed M. Shaman, Stefan R. Kowalski
      Hyperphosphatemia in chronic kidney disease (CKD) patients is a potentially life altering condition that can lead to cardiovascular calcification, metabolic bone disease (renal osteodystrophy) and the development of secondary hyperparathyroidism (SHPT). It is also associated with increased prevalence of cardiovascular diseases and mortality rates. To effectively manage hyperphosphatemia in CKD patients it is important to not only consider pharmacological and nonpharmacological treatment options but also to understand the underlying physiologic pathways involved in phosphorus homoeostasis. This review will therefore provide both a background into phosphorus homoeostasis and the management of hyperphosphatemia in CKD patients. In addition, it will cover some of the most important reasons for failure to control hyperphosphatemia with emphasis on the effect of the gastric pH on phosphate binders efficiency.


      PubDate: 2016-06-11T09:45:41Z
       
  • A review on the strategies for oral delivery of proteins and peptides and
           their clinical perspectives

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Abdul Muheem, Faiyaz Shakeel, Mohammad Asadullah Jahangir, Mohammed Anwar, Neha Mallick, Gaurav Kumar Jain, Musarrat Husain Warsi, Farhan Jalees Ahmad
      In the modern world, a number of therapeutic proteins such as vaccines, antigens, and hormones are being developed utilizing different sophisticated biotechnological techniques like recombinant DNA technology and protein purification. However, the major glitches in the optimal utilization of therapeutic proteins and peptides by the oral route are their extensive hepatic first-pass metabolism, degradation in the gastrointestinal tract (presence of enzymes and pH-dependent factors), large molecular size and poor permeation. These problems can be overcome by adopting techniques such as chemical transformation of protein structures, enzyme inhibitors, mucoadhesive polymers and permeation enhancers. Being invasive, parenteral route is inconvenient for the administration of protein and peptides, several research endeavors have been undertaken to formulate a better delivery system for proteins and peptides with major emphasis on non-invasive routes such as oral, transdermal, vaginal, rectal, pulmonary and intrauterine. This review article emphasizes on the recent advancements made in the delivery of protein and peptides by a non-invasive (peroral) route into the body.


      PubDate: 2016-06-11T09:45:41Z
       
  • Microemulgel: an overwhelming approach to improve therapeutic action of
           drug moiety

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Kalpesh C. Ashara, Jalpa S. Paun, M.M. Soniwala, J.R. Chavda, Vishal P. Mendapara, Nitin M. Mori
      As compared to gel and other topical preparations microemulgel has been prepared by screening of oils, emulsifier, and co-emulsifier on bases of solubility of an API in it. An API has high solubility and oil may also have more or less pharmacological property, so it may assist the therapeutic action of API. Due to presence of oil portion, it leads to more penetration of API in the skin. Oil Micelle Size was less than 500nm which provides more area for absorption of API in the skin so more penetration and more effective than macro-emulsion. Microemulgel has an advantage of emulgel that has dual benefits of micro-emulsion and gel and several other desirable properties like good consistency, thyrotrophic, greaseless, easily spreadable as well as removable, emollient, non-staining, water soluble, longer shelf-life, bio-friendly, transparent, pleasant appearance, ability of patients for self-medication, termination of medications will be easy, etc.


      PubDate: 2016-06-11T09:45:41Z
       
  • Microparticles as controlled drug delivery carrier for the treatment of
           ulcerative colitis: A brief review

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Nidhi, Muzamil Rashid, Veerpal Kaur, Supandeep Singh Hallan, Saurabh Sharma, Neeraj Mishra
      Ulcerative colitis is the chronic relapsing multifactorial gastrointestinal inflammatory bowel disease, which is characterized by bloody or mucus diarrhea, tenesmus, bowel dystension, anemia. The annual incidence of ulcerative colitis in Asia, North America and Europe was found to be 6.3, 19.2 and 24.3 per 100,000person-years. The major challenge in the treatment of ulcerative colitis is appropriate local targeting and drug related side-effects. To overcome these challenges, microparticulate systems seem to be a promising approach for controlled and sustained drug release after oral administration. The main goal of this article is to explore the role of microparticles in ulcerative colitis for the appropriate targeting of drugs to colon. There are different approaches which have been studied over the last decade, including prodrugs, polymeric approach, time released system, pH sensitive system, which show the site specific drug delivery to colon. Among these approaches, microparticulate drug delivery system has been gaining an immense importance for local targeting of drug to colon at a controlled and sustained rate. Combined approaches such as pH dependent and time dependent system provide the maximum release of drug into colon via oral route. This article embraces briefly about pathophysiology, challenges and polymeric approaches mainly multiparticulate systems for site specific drug delivery to colon in sustained and controlled manner so that drug related side-effects by reducing dosage frequency can be minimized.


      PubDate: 2016-06-11T09:45:41Z
       
  • Editorial Board

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4




      PubDate: 2016-06-11T09:45:41Z
       
  • Pain and anxiety management for pediatric dental procedures using various
           combinations of sedative drugs: A review

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Giath Gazal, Wamiq Musheer Fareed, Muhammad Sohail Zafar, Khalid H. Al-Samadani
      For fearful and uncooperative children behavioral management techniques are used. In order to control the pain and anxiety in pedodontic patients, pharmacologic sedation, anesthesia and analgesia are commonly used. Midazolam is commonly used as an oral sedation agent in children; it has several features such as safety of use, quick onset and certain degree of amnesia that makes it a desirable sedation agent in children. This review paper discusses various aspects of oral midazolam, ketamine and their combinations in conscious sedation including, advantages of oral route of sedation, pharmacokinetics, range of oral doses, and antagonists for clinical dental treatment procedures.


      PubDate: 2016-06-11T09:45:41Z
       
  • Drug nanocrystals: A way toward scale-up

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Kale Mohana Raghava Srivalli, Brahmeshwar Mishra
      Drug nanocrystals comprise unique drug delivery platforms playing a significantly important and distinctive role in drug delivery and as such, the industry and academia are spending a lot of their time and money in developing the nanocrystal products. The current research works in this field depict a vivid shift from lab scale optimization studies to scale up focused studies. In this emerging scenario of nanocrystal technology, a review on some exemplary and progressing research studies with either scalability as their objective or upscaling as their future scope may smoothen the future upscaling attempts in this field. Hence, this paper reviews the efforts of such research works as case studies since an analysis of such research studies may input certain beneficial knowledge to carry out more scale up based research works on nanocrystals.


      PubDate: 2016-06-11T09:45:41Z
       
  • An evolving role of clinical pharmacists in managing diabetes: Evidence
           from the literature

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Samia Alhabib, Maha Aldraimly, Ali Alfarhan
      Background Diabetes mellitus is a rapidly growing disease world-wide that is estimated to be present in 6.6% of the international population and projected to be increased by 7.8% in 2030. Treating diabetic patients is multifaceted in all aspects and they require objectives and optimum information in order to obtain the maximum benefits of their treatment and avoid complications. Pharmacists are increasingly considered as a part of the health care system. Hence, the aim of this review is to address and summarize the effectiveness of clinical pharmacists in managing diabetic patients. Method This is a narrative review of the evidence from the literature in order to answer the present question of what is the evidence of the role of clinical pharmacists in managing diabetic patients. We searched five databases including: the Cochrane library, MEDLINE, EMBASE, TRIP, and Science Direct. We will also try to look for other potentially eligible trials or ancillary publications by searching the reference lists of retrieved included trials, (systematic) reviews, meta-analyses and health technology assessment reports. Outcomes included short-term and long-term measures. Results Final search revealed nine studies. They were heterogeneous in terms of interventions, participants, settings and outcomes. Studies varied in their quality and/or reporting of their findings conducted in several settings. Majority of the studies were conducted in Western countries, one in Hong Kong and one in South India. In majority of the studies, pharmacists’ role was mainly to specify all drug-related problems including poor drug compliance and side effects and communicating these to the physician. We found that those who received the pharmacist care had a statistically significant reduction in coronary heart disease, blood pressure, HA1c, quality of life and lipid profile. Conclusion Our review demonstrated the important role of clinical pharmacists in managing diabetic patients at diverse settings worldwide. There is an urgent need to recognize and change regulations to allow shared practice agreements among physicians, pharmacists, and other allied health professionals. These mutual agreements would allow more streamlined provision of health care delivery from non-physician health professionals to participants with common health conditions.


      PubDate: 2016-06-11T09:45:41Z
       
  • Evidence-based pharmaceutical care: The next chapter in pharmacy practice

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Osama Mohammad Al-Quteimat, Amer Mostafa Amer
      Introduction Pharmacy is a very dynamic profession and the role of the pharmacist is improving with the expansion of the scope of services and the introduction of new subspecialties over time. Moving from being medication dispensers to outcome-oriented and patient-focused care providers; pharmacists will carry more responsibility and commitment to improve their knowledge and practice. Being updated and evidence-based is a key tool to achieve effective pharmaceutical care services. The primary purpose of this article is to highlight the concept of “evidence based pharmaceutical care” as professional practice to improve the quality of pharmaceutical care. Methods Literature for relevant evidence was searched by Medline (through PubMed), Cochrane library using the keywords: pharmaceutical care, evidence-based and pharmacy practice. Also a manual search through major journals for articles referenced in those located through PubMed was done. Results and discussion There is strong data showing that pharmaceutical care lead to improvement in health outcomes and cost-effective therapy. More efforts, policies and qualified staff are needed to establish the “evidence-based pharmaceutical care” as new daily professional practice. Evidence to support pharmacists in their emerging role as care providers is available to improve the efficacy and quality of pharmaceutical care. Education and specialized training practicing evidence based approach are vital to prepare pharmacists to provide high quality pharmaceutical care. Conclusion As care providers, pharmacists are effective in providing high quality patient care and being members in multidisciplinary clinical teams is needed to give them the opportunity. Evidence based pharmaceutical care is a natural and logical emerging concept in the modern pharmacy practice to achieve high quality and more effective pharmaceutical care but still more efforts and resources are needed to promote new attitude toward more professional career.


      PubDate: 2016-06-11T09:45:41Z
       
  • Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin
           derivatives

    • Abstract: Publication date: Available online 3 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yana Garazd, Myroslav Garazd, Roman Lesyk
      A series of novel 6-pyrazolinylcoumarins has been synthesized via multi-step protocol. The synthetic procedure was based on the acetylation of hydroxycoumarins; Fries rearrangement, and Claisen–Schmidt condensation; the target 6-[5-aryl-4,5-dihydropyrazol-3-yl]-5-hydroxy-7-methylcoumarins (33-49) were obtained under reactions of hydrazine and 2-aryl-5-methyl-2,3-dihydropyrano[2,3-f]chromen-4,8-diones as the last phase of the protocol. Anticancer activity screening in NCI60-cell lines assay allowed identification of compound 47 with the highest level of antimitotic activity with mean GI50 value of 10.20 μM and certain sensitivity profile towards the Leukemia cell lines CCRF-CEM and MOLT-4 (GI50 / TGI values 1.88 / 5.06 μM and 1.92 / 4.04 μM respectively).


      PubDate: 2016-06-05T08:35:48Z
       
  • Prevalence of UDP-glucuronosyltransferase Polymorphisms (UGT1A6∗2,
           1A7∗12, 1A8∗3, 1A9∗3, 2B7∗2, and 2B15∗2) in
           a Saudi Population

    • Abstract: Publication date: Available online 2 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Khalid M. Alkharfy, Basit L. Jan, Sibtain Afzal, Fahad I. Al-Jenoobi, Abdullah M. Al-Mohizea, Saleh Al-Muhsen, Rabih Halwani, Mohammad K. Parvez, Mohammed S. Al-Dosari
      Glucuronidation is an important phase II pathway responsible for many endogenous substances and drugs metabolism. The present work evaluated allele frequencies of certain UDP-glucuronosyl-transferases (UGT 1A6∗2, A7∗12, A8∗3, A9∗3, 2B7∗2, and 2B15∗2) in Saudi Arabians that could provide essential ethnic information. Blood samples from 192 healthy unrelated Saudi males of various geographic regions were collected. Genomic DNA was isolated and genotyping of various UGTs was carried out using polymerase chain reaction (PCR) followed by direct sequencing. For UGT1A6∗2 A/G genotype, the most common variant was the homozygous repeat (AA) and the most common allele was (A) with a frequency of 46.5% and 67.3%, respectively. Similarly, the most common variant for UGT1A7∗12 T/C genotype was the heterozygous repeat (TC) with a frequency of 78.7% while the mutant allele (C) was present in 60.6% of the study population. Both UGT1A8∗3 (G/A) and UGT1A9∗3 (T/C) showed only a wild homozygous pattern in all screened subjects. For UGT2B7∗2, the heterozygous repeat (TC) was found with a frequency of 57.3% and the alleles (A) showed a frequency of 50.8%. In contrast, for UGT2B15∗2 (G253T), the heterozygous repeat (TG) presented 62.3% of the subjects where the most common allele (G) was with a frequency of 66.2%. In conclusion, our data indicates that Saudis harbor some important UGT mutations known to affect enzyme activity. Additional studies are therefore, warranted to assess the clinical implications of these gene polymorphisms in this ethnic group. .


      PubDate: 2016-06-05T08:35:48Z
       
  • Development and Validation of Bioanalytical UHPLC-UV Method for
           Simultaneous Analysis of Unchanged Fenofibrate and Its Metabolite
           Fenofibric Acid in Rat Plasma: Application to Pharmacokinetics

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Rayan G. Alamri, Kazi Mohsin, Ajaz Ahmad, Mohammad Raish, Fars K. Alanazi
      A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been developed and validated for the simultaneous determination of a lipid regulating agent fenofibrate and its metabolite fenofibric acid in rat plasma. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol-water (65:35, v/v) as the mobile phase. The isocratic flow was 0.3 ml/min with rapid run time of 2.5 min and UV detection was at 284 nm. The method was validated over a concentration range of 100-10000 ng/mL (r2 = >0.9993). The selectivity, specificity, recovery, accuracy and precision were validated for determination of fenofibrate/fenofibric acid in rat plasma. The lower limits of detection and quantitation of the method were 30 and 90 ng/mL for fenofibrate and 40 and 100 ng/mL for fenofibric acid, respectively. The within and between-day coefficients of variation were less than 5%. The validated method has been successfully applied to measure the plasma concentrations in pharmacokinetics study of fenofibrate in an animal model to illustrate the scope and application of the method.


      PubDate: 2016-05-30T07:55:03Z
       
  • Chitosan treatment abrogates hypercholesterolemia-induced
           erythrocyte’s arginase activation

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Gamaleldin I. Harisa, Sabry M. Attia, Khairy MA Zoheir, Fars K. Alanazi
      This study was aimed to evaluate the protective effect of chitosan (CS) against hypercholesterolemia (HC) induced arginase activation and disruption of nitric oxide (NO) biosynthesis using erythrocytes as cellular model. Human erythrocytes were isolated and classified into eight groups. Next, cells were treated with L-arginine (L-ARG), Nω-nitro- L-arginine methyl ester (L-NAME), CS or CS + L-ARG in presence of normal plasma or cholesterol enriches plasma. Then, erythrocytes were incubated at 37 °C for 24 h. The present results revealed that, HC induced significant increase of cholesterol inclusion into erythrocytes membrane compared to control. Moreover, HC caused significant decrease in nitric oxide synthase (NOS) activity similar to L-NAME; however, arginase activity and arginase/NOS ratio significantly increased compared to control. On contrast, treatment of HC with, L-arginine, CS or CS plus L-arginine prevent HC induced cholesterol loading into erythrocytes membrane, NOS inhibition and arginase activation. This study suggested that CS could be protective agent against HC induced disruption of erythrocyte’s oxidative status and arginase activation.


      PubDate: 2016-05-30T07:55:03Z
       
  • High-performance thin layer chromatography based assay and stress study of
           a rare steroidal alkaloid solanopubamine in six species of Solanum grown
           in Saudi Arabia

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Nasir A. Siddiqui, Mohammad K. Parvez, Adnan J. Al-Rehaily, Mohammed S. Al Dosari, Perwez Alam, Faiyaz Shakeel, Hattan A. Al Harbi



      PubDate: 2016-05-30T07:55:03Z
       
  • New acyclic secondary metabolites from the biologically active fraction of
           Albizia lebbeck Flowers

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shaza M. Al-Massarani, Ali A. El Gamal, Mohamed Farag, Mansour S. Al-Said, Maged S. Abdel-Kader, Omer A. Basudan, Saleh I. Alqasoumi
      The total extract of Albizia lebbeck flowers was examined in vivo for its possible hepatoprotective activity in comparison with the standard drug silymarin at two doses. The higher dose expressed promising activity especially in reducing the levels of AST, ALT and bilirubin. Fractionation via liquid- liquid partition and reexamination of the fractions revealed that the n-butanol fraction was the best in improving liver biochemical parameters followed by the n-hexane fraction. However, serum lipid parameters were best improved with CHCl3 fraction. The promising biological activity results initiated an intensive chromatographic purification of Albizia lebbeck flowers fractions. Two compounds, identified from natural source for the first time, the acyclic farnesyl sesquiterpene glycoside1-O-[6-O-α-L- arabinopyranosyl-β-D-glucopyranoside]–(2E,6E-) -farnesol (6) and the squalene derivative2,3-dihydroxy-2,3-dihydrosqualene (9), in addition to eight compounds reported here for the first time from the genus Albizia; two benzyl glycosides, benzyl 1-O-β-D- glucopyranoside (1) and benzyl 6-O-α-L-arabinopyranosyl β-D-glucopyranoside (2); three acyclic monoterpene glycosides, linalyl β- D- glucopyranoside (3) and linalyl 6-O-α-L-arabinopyranosyl -β-D-glucopyranoside (4); 2E)-3,7-dimethylocta-2,6-dienoate-6-O-α-L arabinopyranosyl-β-D-glucopyranoside (5), two oligoglycosides, n- hexyl-α-L arabinopyranosyl-(1→6)-β-D-glucopyranoside (creoside) (7) and n-octyl α-L- arabinopyranosyl-(1→6)-β-D-glucopyranoside (rhodiooctanoside) (8); and ethyl fructofuranoside (10). The structures of the isolated compounds were elucidated based on extensive examination of their spectroscopic 1D and 2D-NMR, MS, UV, and IR data. It is worth mentioning that, some of the isolated linalol glycoside derivatives were reported as aroma precursors.


      PubDate: 2016-05-25T07:14:48Z
       
  • Editorial Board

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3




      PubDate: 2016-05-25T07:14:48Z
       
  • Bioactivity and chemical characterization of Acalypha fruticosa Forssk.
           growing in Saudi Arabia

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ghada Ahmed Fawzy, Areej Mohammad Al-Taweel, Shagufta Perveen, Shabana Iqrar Khan, Fatma Abdulaziz Al-Omary
      Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely; 2-methyl-5,7-dihydroxychromone 5-O-β-D-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect.


      PubDate: 2016-05-25T07:14:48Z
       
  • Acute toxicity profiling of the ethyl acetate fraction of Swietenia
           macrophylla seeds and in-vitro neuroprotection studies

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Mustak Sayyad, Tiang Ning, Yatinesh Kumari, Goh Beh Hing, Yogini Jaiswal, Rozita Rosli, Leonard Williams, Mohd. Farooq Shaikh
      Swietenia macrophylla (SM) is a medicinally important plant found in tropical and subtropical regions of the world. The ethyl acetate fraction of the seeds of Swietenia macrophylla (SMEAF) is reported to exhibit potent anticancer, antitumor, anti-inflammatory and antifeedant activities. Till date, there have been no studies reported on the acute oral toxicity profile of the ethyl acetate fraction of the seeds of SM. The objective of the present study was to determine the acute toxicity of SMEAF and evaluate the in-vitro neuroprotective activity of SMEAF using primary neuronal cell cultures. In acute oral toxicity study, the SMEAF did not produce any lethal signs of morbidity and mortality. Histo-pathological findings, support the safety of SMEAF, as there were no significant changes observed in any of the parameters studied. Based on the results obtained in MTT assay, we infer that SMEAF has a significant neuroprotective effect, as it increased the cell viability and exhibited protection to the neuronal cells against TBHP induced oxidative stress. Thus, SMEAF can be suggested for use in the development of herbal drug formulations with neuroprotective potential.


      PubDate: 2016-05-13T13:43:32Z
       
  • Compatibility study of paracetamol, chlorpheniramine maleate and
           phenylephrine hydrochloride in physical mixtures

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): G.G.G. de Oliveira, A. Feitosa, K. Loureiro, A.R. Fernandes, E.B. Souto, P. Severino
      Paracetamol (PAR), phenylephrine hydrochloride (PHE) and chlorpheniramine maleate (CPM) are commonly used in clinical practice as antipyretic and analgesic drugs to ameliorate pain and fever in cold and flu conditions. The present work describes the use of thermal analysis for the characterization of the physicochemical compatibility between drugs and excipients during the development of solid dosage forms. Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC) were used to study the thermal stability of the drug and of the physical mixture (drug/excipients) in solid binary mixtures (1:1). DSC thermograms demonstrated reproducible melting event of the prepared physical mixture. Starch, mannitol, lactose and magnesium stearate influence thermal parameters. Information recorded from the derivative thermogravimetric (DTG) and TGA curves demonstrated the decomposition of drugs in well-defined thermal events, translating the suitability of these techniques for the characterization of the drug/excipients interactions.


      PubDate: 2016-05-13T13:43:32Z
       
  • Preparation and evaluation of rotigotine-loaded implant for the treatment
           of Parkinson’s disease and its evolution study

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Aiping Wang, Yanxiang Liu, Rongcai Liang, Xuemei Zhang, Kaoxiang Sun, Zimei Wu, Wanhui Liu
      Purpose To develop rotigotine-loaded implants (RI) to achieve continuous release of rotigotine for long duration for the treatment of Parkinson’s disease (PD). Methods RI was prepared by hot-melt extrusion method using poly (lactide-co-glycoside) (PLGA) as the matrix. In vitro drug release was optimized by drug loading, melting temperature during preparing process and additives. The surface and internal morphology of RI was imaged by SEM. The in vivo release profile of RI was investigated on rat. Results RI prepared with PLGA 8515 4A showed sustained release of 40 days while suffering a lag phase, which was significantly shortened by blending 5050 2A and mannitol in the matrix. RI prepared by 8515 4A/5050 2A/mannitol = 55:10:5 (rotigotine 30%) showed a 40-day sustained release in vivo with no lag phase. The drug release from RI was also affected by drug loading and melting temperature probably due to the drug state existed in the implant. The evolution of implants during release process was correlated well with the drug release kinetics. Conclusion RI could achieve sustained drug release for 40 days which could supply an alternative of continuous dopamindergic stimulation (CDS) for the treatment of PD.


      PubDate: 2016-05-08T12:54:51Z
       
  • Natural cures for breast cancer treatment: A review

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Munazza Shareef, Muhammad Aqeel Ashraf, Maliha Sarfraz
      For centuries, herbs and plants have been used for medicinal purposes and as food as well. This review concern about different types of plants that retain the immune stimulating and anti-tumor properties. Large variety of active phytochemicals like carotenoids, flavonoids, ligands, polyphenolics, terpenoids, sulfides, lignans and plant sterols have been identified in different types of herbs. These phytochemicals have different mechanisms of action. They either stimulate the protective enzyme like glutathione transferase or prevent the cell proliferation. This review has centered on the biochemical properties of Allium sativum, Echinacea, Curcuma longa, Arctium lappa, Camellia sinensis, Panax ginseng and Flax seed. Extracts and juices of Withania somnifera, Amoora rohituka, Dysoxylum binectariferum and Vaccinium macrocarpon, respectively also used as anti-breast cancer. The volatile oils and extracts of these herbs and plants inhibit the synthesis of mevalonate that lessen the tumor growth and cholesterol synthesis.


      PubDate: 2016-05-08T12:54:51Z
       
  • Histatin peptides: Pharmacological functions and its applications in
           dentistry

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Zohaib Khurshid, Shariq Najeeb, Maria Mali, Syed Faraz Moin, Syed Qasim Raza, Sana Zohaib, Farshid Sefat, Muhammad Sohail Zafar
      There are many human oral antimicrobial peptides responsible for playing important roles including maintenance, repairing of oral tissues (hard or soft) and defense against oral microbes. In this review we have highlighted the biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human. The significance of these peptides includes; capability for ionic binding that can kill fungal Candida albicans. They have histidine rich amino acids sequences (7-12 family members; corresponding to residues 12-24, 13-24, 12-25, 13-25, 5-11, and 5-12, respectively) for Histatin-3. However, Histatin-3 can be synthesised proteolytically from histatin 5 or 6. Due to their fungicidal response and high biocompatibility (little or no toxicity), these peptides can be considered as therapeutic agents with most probable applications for example, artificial saliva for denture wearers and salivary gland dysfunction conditions. The objectives of current article are to explore the human histatin peptides for its types, chemical and biological aspects. In addition, the potential for therapeutic bio-dental applications has been elaborated.


      PubDate: 2016-05-08T12:54:51Z
       
  • The Transport Mechanism of Monocarboxylate Transporter on Spinosin in
           Caco-2 Cells

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Xiang Le Meng, Yan Li Guo, Hai Yinghuang
      Objectives The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4 °C) SPI uptake increased 20% than that of 37 °C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax=5.364 μg/mg protein, Km=657.0 μg/mL]. Conclusion The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid.


      PubDate: 2016-05-08T12:54:51Z
       
  • Structure characteristics of self-bonding boards during hot press for
           leukemia inhibition

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Jiang Zhang, Zhi Lin
      The 80% leukemia were caused by indoor formaldehyde pollution. And the results shown that the absorbances of many connectionbonds (such as C-O-C, C-OOC, and so on) increased. It could be inferred that a lot of bonds were produced and played the role of molecularcrosslinking. After hot press, the content of lignin in Eucalyptus wood fiber were all lower than ones of self-bonding boards. And the change of content of lignin was closely related to time and temperature of hot press.


      PubDate: 2016-05-08T12:54:51Z
       
  • Biomechanical analysis of press-extension technique on degenerative lumbar
           with disc herniation and staggered facet joint

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Hong-gen Du, Sheng-hui Liao, Zhong Jiang, Huan-ming Huang, Xi-tao Ning, Neng-yi Jiang, Jian-wei Pei, Qin Huang, Hui Wei
      This study investigate the effect of a new Chinese massage technique named “press-extension” on degenerative lumbar with disc herniation and facet joint dislocation, and provide a biomechanical explanation of this massage technique. Self-developed biomechanical software used to establish a normal L1-S1 lumbar 3D FE model, which integrated the spine CT and MRI data-based anatomical structure. Then utilize graphics technique to build a degenerative lumbar FE model with disc herniation and facet joint dislocation. According to the actual press-extension experiments, mechanics parameters are collected to set boundary condition for FE analysis. The result demonstrated that press-extension techniques bring the annuli fibrosi obvious induction effect, make the central nucleus pulposus forward close, increasing the pressure in front part. Study conclude that finite element modeling for lumbar spine is suitable for the analysis of press-extension technique impact on lumbar intervertebral disc biomechanics, to provide the basis for the disease mechanism of intervertebral disc herniation using press-extension technique.


      PubDate: 2016-05-08T12:54:51Z
       
  • Treatment on Patients with Nueroglioma by Teniposide and Semustine and Its
           Influence on Twist and E-cadherin Expression

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yongbo Zhang, Guoyi Liu, Meiling Lang, Jing Zhang, Jia Geng
      This study focus on curative effects of teniposide combining with semustine on patients with neuroglioma and the influences on the expression of Twist and E-cadherin in tissue. Sixty eight patients with neuroglioma taking operation in our hospital were divided into two groups randomly. Single radiotherapy was given to 34 patients in group A, and teniposide (VM-26) and semustine (Me-CCUN) were added to radiotherapy for 34 patients in group B. Then, curative effects, survival rate, living quality and adverse reaction rate after operation were compared between two groups. Moreover, the difference in positive expression rate of Twist and E-cadherin before and after treatment between two groups was analyzed by immunohistochemistry. Results: In group B, the effective rate of treatment was 88.2%, and the disease control rate was 70.6%, higher than 52.9% and 32.4% in group A with statistical significance (P<0.05). Moreover, the survival rate in three years of group B was 44.1%, and the score of living quality was 67.11±4.32, also higher than 23.5% and 63.79±4.53 in group A with statistical significance (P<0.05). However, the difference between two groups in adverse reaction rate has no statistical significance (P>0.05). In addition, the difference in positive expression rate of Twist and E-cadherin between group A and group B has no statistical significance before treatment (P>0.05). After treatment, however, the positive rate of Twist in group B is lower than that in group A, while the positive rate of E-cadherin is higher. Both differences have statistical significance (P<0.05). Chemotherapy of VM-26 combining with Me-CCNU can inhibit Twist expression and improve the expression rate of E-cadherin to help improving the curative effects and living quality and increasing survival rate.


      PubDate: 2016-05-08T12:54:51Z
       
  • Protective effect of Astragaloside IV against sepsis-induced acute lung
           injury in rats

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ruiqin Huang, Min LI, Min Li
      The study aimed to explore the protective effects of AS-IV against sepsis-induced ALI. Sepsis was induced by cecal ligation and puncture (CLP) method in Sprageue Dawley rats. Rats were randomly assigned into five groups: animals undergoing a sham CLP (sham group); animals undergoing CLP (CLP group); animals undergoing CLP and treated with AS-IV at 2.5mg/kg.bw (low-dose AS-IV [L-AS] group), at 5mg/kg.bw (mid-dose AS-IV [M-AS] group), and at 10mg/kg.bw (high-dose AS-IV [H-AS] group). At 6 h, 12 h and 24 h post-CLP surgery, six rats were respectively sacrificed to collect blood and lung tissue samples. The levels of arterial blood gas index, lung water content, protein level and leukocyte counts (total amount, neutrophils and lymphotes) in bronchoalveolar lavage fluid (BALF) and cytokines such as TNF-α and IL-6 in BALF were measured at each time point in different groups. HE-staining and optical microscopy were performed to examine the pathologic changes in lungs. The 72 h-survival rate of each group was also recorded. PaO2 was decreased significantly, while the lung water content, BALF protein level, cell numbers, BALF cytokine TNF-α and IL-6 levels were increased significantly for CLP group as compared with sham group. Moreover, pathological injury was observed in lung tissue indicating the successful sepsis-induced ALI model. Speaking of the effect of AS-IV, we founded that, compared with the CLP group, the AS-IV treatment groups could significantly alleviate all the abovenegative changes exited in the CLP group in a dose-dependent manner. What’s more, the pathological injury was also gradually improved by AS-IV treatment compared with the CLP rats. AS-IV exerts its protective effect against sepsis-induced ALI in rats via improving pulmonary ventilation function, decreasing the permeability of alveolar epithelium and capillary as well as repressing lung inflammation.


      PubDate: 2016-05-08T12:54:51Z
       
  • New discovery of cryptorchidism: Decreased retinoic acid in testicle

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Jinpu Peng, Lianju Shen, Jinjun Chen, Xining Cao, Yue Zhou, Huali Weng, Chunlan Long, Deying Zhang, Shengfen Tu, Yan Zhang, Dawei He, Tao Lin, Guanghui Wei
      This study focus on investigatation of cryptorchidism induced by flutamide (Flu) and its histopathological damage, and detect retinoic acid concentration in testicle tissue, in order to find a new method for clinical treatment to infertility caused by cryptorchidism. Twenty SD (Sprague Dawley) pregnant rats were randomly divided into Flu cryptorchidism group (n=10) and normal control group (n=10). HE stained for observing morphological difference. TEM(transmission electron microscope) was used for observing the tight junction structure between Sertoli cells. Epididymal caudal sperms were counted and observed in morphology. The expression of stimulated by retinoic acid gene 8 (Stra8) was detected using immunohistochemistry, western blot, and Q-PCR. High performance liquid chromatography (HPLC) analysis was made on retinoic acid content. Sperm count and morphology observation confirmed cryptorchidism group was lower than normal group in sperm quantity and quality. The observation by TEM showed a loose structure of tight junctions between Sertoli cells. Immunohistochemistry, western blot, and Q-PCR showed that cryptorchidism group was significantly lower than normal group in the expression of Stra8. HPLC showed that retinoic acid content was significantly lower in cryptorchid testis than normal testis. In the cryptorchidism model, retinoic acid content in testicular tissue has a significant reduction; testicles have significant pathological changes; damage exists in the structure of tight junctions between Sertoli cells; Stra8 expression has a significant reduction, perhaps mainly contributing to spermatogenesis disorder.


      PubDate: 2016-05-08T12:54:51Z
       
  • Identification and characterization of Endophytic filamentous fungi from a
           Catharanthus roseus

    • Abstract: Publication date: Available online 29 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Farah Wahida Ayob, Khanom Simarani
      This paper reported on the various filamentaous fungi strains that were isolated from a wild grown Catharanthus roseus. Based on the morphological characteristics and molecular technique through a Polymerase Chain Reaction and DNA sequencing method using internal transcribed spacer (ITS), these fungi had been identified as a Colletotrichum sp, Macrophomina phaseolina, Nigrospora sphaerica and Fusarium solani. The ultrastructures of spores and hyphae were observed under a Scanning Electron Microscope. The hydrolytic enzyme test showed that all strains were positive in secreting cellulase. Colletotrichum sp and Fusarium solani strains also gave a positive result for amylase while only Fusarium solani capable to secrete protease. These fungi were putatively classified as endophytic fungi since they produced extracellular enzymes that allow them to penetrate plants cell walls and colonized with symbiotic properties.


      PubDate: 2016-05-04T13:40:02Z
       
  • The standard aqueous stem bark extract of Mangifera indica L. inhibits
           toxic PLA2 – NN-XIb-PLA2 of Indian cobra venom

    • Abstract: Publication date: Available online 30 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Bhadrapura Lakkappa Dhananjaya, Shivalingaiah Sudarshan, Yashad Dongol, Sunil S. More
      The aqueous extract of Mangifera indica is known to possess diverse medicinal properties, which also includes anti-snake venom activities. However, its inhibitory potency and mechanism of action on multi-toxic snake venom Phospholipases A2s is still unknown. Therefore, the objective of this study was to evaluate the modulatory effect of standard aqueous bark extract of M. indica on NN-XIb-PLA2 of Indian cobra venom. The in vitro sPLA2, in situ hemolytic and in vivo edema inhibition effect were carried out as described. Also the effect of substrate and calcium concentration was carried out. M. indica extract dose dependently inhibited the GIA sPLA2 (NN-XIb-PLA2) activity with an IC50 value of 7.6 μg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ∼40 μg/ml concentration. Further, M. indica extract (0-50 μg/ml) inhibited the edema formed in a dose dependent manner. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect of M. indica extract on the NN-XIb-PLA2. Further, the inhibition was irreversible as evident from binding studies. The in vitro inhibition is well correlated with in situ and in vivo edema inhibiting activities of M. indica. As the inhibition is independent of substrate and calcium and was irreversible, it can be concluded that M. indica extracts mode of inhibition could be due to direct interaction of components present in the extract with the PLA2 enzyme. The aqueous extract of M. indica effectively inhibits svPLA2 enzymatic and its associated toxic activities, which substantiate their anti-snake venom properties. Further in-depth studies on the role and mechanism of the principal constituents present in the extract, responsible for the anti-PLA2 activity will be interesting to develop them into potent antisnake component and also as an anti-inflammatory agent.


      PubDate: 2016-05-04T13:40:02Z
       
  • The effect of chitooligosaccharides on oleic acid-induced lipid
           accumulation in HepG2 cells

    • Abstract: Publication date: Available online 29 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Peiqiu Cao, Guidong Huang, Qingyun Yang, Jiao Guo, Zhengquan Su
      This experiment aimed to evaluate the capacities of two types of chitooligosaccharides (COS) with different molecular weights for the ability to eliminate lipid accumulation in hepatocytes. We have established a lipid accumulation model in HepG2 cells for these studies in vitro, which was established by induction with oleic acid. The capacity of COS to eliminate lipid accumulation were evaluated using three metrics: the thiazolyl blue dye absorbance (MTT value), the morphology of intracellular lipid droplets and the triglyceride level (TG). Two types of COS with different molecular weights (1000Da and 3000Da) can significantly reduce intracellular lipid accumulation and decrease TG content in HepG2 cells, in a dose-dependent fashion. We found that low molecular weight COS is more efficacious than high molecular weight COS. Two types of COS can eliminate lipid accumulation induced by oleic acid in HepG2 cells, leading to an obvious hypolipidemic effect in vitro. These results suggest that COS may be effective preventive agents in fatty liver disease.


      PubDate: 2016-04-29T13:15:42Z
       
  • Diagnosis of Genus Helicobacter through A hemi-nested PCR assay of 16S
           rRNA

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Heping Qin, Guodu Tang, Ping Yi, Xinyi Pan, Huali Huang, Renjie Chang, Zhe Shi, Muhammad Aqeel Ashraf
      The present study aimed to establish a genus-specific PCR-based assay to detect helicobacters using 16S rRNA gene as the target template. We designed the hemi-nested primers based on sequences of 16S rRNA gene of 34 types of Helicobacter species. The inclusivity, sensitivity, and specificity of the PCR assay using these primers were examined in three different models, comprising feces simulated samples, BLAB/c mice infection model and clinic patients samples. The detection sensitivity of H.pylori, H.hepaticus and H.bilis strains from feces simulated samples was all 102 CFU/ml. We successfully detected H.hepaticus and H.bilis in the liver, caecum and feces of experimentally infected mice. H.pylori was successfully detected in the feces samples from 3 patients infected with H.pylori while not in the feces samples from 3 healthy human. However, the C97/C05-C97/C98 PCR assay detected H.pylori in the 2 positive samples. Due to the PCR assay’s excellent inclusivity, high sensitivity and specificity it may be used to detect the presence of Helicobacters.


      PubDate: 2016-04-29T13:15:42Z
       
  • Serum TNF-α, GTH and MDA of High-Fat Diet-Induced Obesity and Obesity
           Resistant Rats

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Peixian Wu, Fan Zhang, Yali Dai, Lingchuan Han, Shuo Chen
      Objective Mechanism of high fat diet-induced obesity is analyzed and serum tumor necrosis factor, malondialdehyde and glutathione levels of obesity resistant rats are effectively analyzed. Methods 120 male SD rats were grouped into obesity group and control group, each group with 60 rats. Obese rats were fed with high fat diet, while control rats were fed with ordinary fodder. After six months of feeding, observe growth degree of two groups of rats, and divide the rats into obesity group and obesity resistant group based on extent of growth. Then detect glutathione, tumor necrosis factor-α and MDA content in bat serum with enzyme-linked immunosorbent assay. Results The content of tumor necrosis factor α in obese rats and obesity resistant rats is far higher than that in control group (P <0.05), there exists no statistical significance (P> 0.05) in tumor necrosis factor α in obesity group and obesity resistant group, glutathione level of obesity group rats and obesity resistant group rats are significantly increased (P <0.05) compared with that of control group, also serum MDA level of the two groups have significant statistical significance compared with that of normal control group, (P <0.05). Conclusion Among rats fed with high fat diet, in comparison of weight of obesity resistant rats and control group rats, there is no statistically significant difference, (P> 0.05). However, high fat diet will impact mechanisms in vivo in rats, which then induces oxidative stress response and inflammatory response in rats.


      PubDate: 2016-04-29T13:15:42Z
       
  • Forgotten Topological Index of Chemical Structure in Drugs

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Wei Gao, Muhammad Kamran Siddiqui, Muhammad Imran, Muhammad Kamran Jamil, Mohammad Reza Farahani
      A massive of early drug tests implys that there exist strong inner relationships between the bio-medical and pharmacology characteristics of drugs and their molecular structures. The forgotten topological index was defined to be used in the analysis of drug molecular structures, which is quite helpful for pharmaceutical and medical scientists to grasp the biological and chemical characteristics of new drugs. Such tricks are popularly employed in developing countries where enough money is lacked to afford the relevant chemical reagents and equipment. In our article, by means of drug molecular structure analysis and edge dividing technology, we present the forgotten topological index of several widely used chemical structures which often appear in drug molecular graphs.


      PubDate: 2016-04-29T13:15:42Z
       
  • Release property study on the novel divalproex sodium enteric-coated
           capsules

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shuoye Yang, Xin Wang, Jiangsong Jia, Pengyuan Li
      In present study, a novel divalproex sodium (DS) enteric-coated capsule was prepared, high performance liquid chromatography (HPLC) assay method for DS was developed. Their uniformity, release curve and release characteristics in different solvents were examined. The release studies were performed using marketed sample as a reference and data were analyzed in terms of cumulative release amounts as a function of time. It was demonstrated by the results that assay developed was specific, rapid and reliable, which can be used to determine DS in vitro accurately, our developed samples was similar to reference preparation in in vitro release characteristics. The release characteristics of different batches of samples were quite similar with each other, the total release percents of DS from enteric-coated capsule were within 0-10 % in HCl, and reached close to 100 % in phosphate buffer. Similarity factors (f2) of three batches between two preparations were all higher than 50. The developed enteric-coated capsule may be a promising alternative dosage form for treatment of related diseases.


      PubDate: 2016-04-29T13:15:42Z
       
  • Treatment with Glial derived neurotropic factor (GDNF) attenuates
           oxidative damages of spinal injury in rat model

    • Abstract: Publication date: Available online 25 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Tao Li, Qi Li, Hui Gong, Zhuo-fu Chen, Xia-wu Peng
      Spinal cord injury (SCI) is a serious and debilitating issue being suffered by wide population worldwide. Extensive treatment approaches have been tested and being verified for their efficacy. Owing to the nature of central nervous system (CNS), the resident stem cells would be triggered in response to any sort of trauma with nerve factors as their communication signals. Apart from physical injuries, damages due to oxidative stress also needs to be addressed while CNS repair mechanism takes place. This study looks at the potential of glial derived nerve factor (GDNF) in addressing the SCI in regards to oxidative damages. A total of 60 Wistar rats were clustered into five groups and GDNF at various concentration were tested in each group. Assessments in terms of oxidative stress parameters were noted and analyzed accordingly. It was noted that GDNF had reduced oxidative damages and increased the levels of anti-oxidants in dose-dependent manner (p<0.05). Though treatment with 10mg/mL and 20mg/mL showed significant changes as compared to control group, these treatment modalities remained insignificant among each other. In conclusion, we demonstrated that GDNF exerted a neuro-protective effect on CNS by inducing anti-oxidants and reducing the levels of oxidative stress in SCI induced rat models.


      PubDate: 2016-04-29T13:15:42Z
       
  • Research on AIDS Patients’ Survival Time after Highly Active
           Antiretroviral Therapy, Treatment Effect and Treatment Modes

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Riying Lv, Guojian Li, jizhou Wu, Yujia Zhu, XiongLin Qin, Shixiong Li
      To fully define clinical efficacy of highly active antiretroviral therapy for AIDS, analyze patients’ survival time and treatment mode after receiving treatment, and provide scientific theory to guide improvement of antiviral therapy, this paper selected 3100 cases of patients diagnosed with AIDS during April 2006 and April 2014 as object of this study. All patients were treated with highly active antiretroviral therapy. The main analysis contents of this study include CD4 + T lymphocyte count, viral load changes, incidence of opportunistic infections, specific cause of death and the like. The results show that patients’ CD4 +, T lymphocyte levels are significantly increased 3,18,24 months after treatment, difference between the situation after and before receiving treatment, P <0.05, with statistically significant difference. Analyzed from effective inhibition of virus, effective inhibition rate is 72.58.0% (2250/3100). Main causes of death in patients is usually respiratory failure. It thus can be concluded that highly active antiretroviral therapy for AIDS is with good clinical effect, which can effectively improve survival time of patients. So it enjoys application value of being widely used in clinical treatment of AIDS.


      PubDate: 2016-04-29T13:15:42Z
       
  • Analgesic effect and possible mechanism of SCH772984 intrathecal injection
           on rats with bone cancer pain

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Bian Juhua, Zhu Shanshan, Ma Wenwen, Li Chunwei, Muhammad Aqeel Ashraf
      This study is to establish a model of rat tibial osteocarcinoma pain, intrathecally inject specific ERK1/2 inhibitors SCH772984, observe the analgesic effect, and discuss the influence of ERK-P90RSK-Fos signal path in bone cancer pain. Forty female SD rats were randomly divided into 5 groups. Establish a bone cancer pain model after putting the intrathecal tube 5d, determine the rats’ mechanical withdrawal threshold(MWT) after tube 5d 40 SD rats with intrathecal tube back 5d were randomly divided into 5 groups. Sham Group receives no medication, the other four respectively receives 5% DMSO 10 μl, SCH 0.1, 1.0, 10 μ g (SCH dissolved in 10 μl 5% DMSO) intrathecally. Determine the rats’ mechanical withdrawal threshold(MWT) before and after giving medication 1, 3, 6, 9, 12, 15, 18, 24h, and 2min spontaneous paw withdrawal. Western Blot and immuno-fluorescence determine the expression condition of spinal cord dorsal horn of p-ERK, p-p90RSK and Fos protein. Intrathecal injection of SCH772984 has analgesic effects on rats with bone cancer pain, and the effects enhance with increasing dose; intrathecal injection of SCH772984 10 μg could greatly reduce the expression of spinal dorsal horn Fos protein. Injecting walker 256 tumor cells into rats’ tibia could cause behavior changes, such as idiopathic pain sensitivity and pain; the intrathecal tube almost has no effect on motor function of rats; ERK1/2 is involved in bone cancer pain, intrathecal injection of ERK1/2 specific inhibitors SCH772984 10 μg may effectively relieve bone cancer pain.


      PubDate: 2016-04-29T13:15:42Z
       
  • Pathogen Distribution and Drug Resistance of Nephrology Patients with
           Urinary Tract Infections

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yunqian Wang, Huicong Li, Baoping Chen
      Objective Pathogen distribution characteristics of nephrology patients with urinary tract infections are studied, and drug resistance of nephrology and urinary tract infections disease are analyzed, so as to provide sufficient evidence for treatment of patients. Methods: Conduct randomized control study of 3,500 cases of nephrology patients with urinary tract infections treated in different hospitals from December 2013 to December 2015, isolate pathogens in patients’ urine samples, perform identification and drug sensitive test and then conduct detailed analysis of drug resistance of pathogens. Results: Through isolation of pathogens, it can be found that all pathogens include Escherichia coli, Gram-positive cocci, gram-negative bacteria, fungi, Acinetobacter baumannii, Enterococcus faecalis, urinary Enterococcus. Among them, proportion of Escherichia coli is the largest. Patients have relatively high drug resistance to ceftriaxone, gentamicin, ciprofloxacin and cotrimoxazole. Conclusion: For nephrology patients with urinary tract infection, the main pathogen is escherichia coli, which has had some drug resistance. Drug resistance detection of pathogen should be strengthened in clinics, so as to provide strong guidance for clinical treatment and promote effective treatment of patients.


      PubDate: 2016-04-25T12:38:27Z
       
  • Effect of Cynomorium Flavonoids on morphology of Perimenopausal Depression
           mice model

    • Abstract: Publication date: Available online 24 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Tan Wang, Mingsan Miao, Yan Li, Min Li, Ying Zhang, Shuo Tian
      Objective In this report, the effects of cynomorium flavonoids on mouse model of perimenopausal depression were investigated. Method 60 ovariectomized female mice were randomly divided into 6 groups evenly: high, medium and low doses of cynomorium flavonoids groups (400mg·kg-1, 200mg·kg-1, 100mg·kg-1), Gengnian’an capsule group (675mg·kg-1), soy isoflavones soft capsule group (250mg·kg-1), and model group. Give the corresponding drug fifth days after surgery for once a day, consecutive thirty days. The model group and control group given the water of same volume. The model related groups were applied with different stress for consecutive eighteen days. Kill the mice and remove the thymus, spleen, uterus and one hand of brain when it is 2 hours after the last administration in mice of each group. Observe the histological changes of each group under light microscope. Results By observing the pathological section. Compared with model group, the pathological changes of the uterus and hypothalamus of mice were significantly improved. The thymic cortex markedly thickened, volume of splenic nodule also significantly increases, the number of lymphocytes significantly increased (P < 0.01). Simulation results that the high dose of cynomorium flavonoids group has the best effective. Conclusion Cynomorium flavonoids on mouse uterus, hypothalamus, thymus and spleen lesions have a significant role in the improvement. Cynomorium flavonoids have a good therapeutic effect on mice with perimenopausal depression


      PubDate: 2016-04-25T12:38:27Z
       
  • Study on Fluorouracil - Chitosan Nanoparticle Preparation and its
           Antitumor Effect

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Gaimin Chen, Rudong Gong
      To successfully prepare fluorouracil - chitosan nanoparticles, and further analyze its anti-tumor activity mechanism, this paper makes a comprehensive study of existing preparation prescription and makes a detailed analysis of fluorouracil - chitosan in vitro release and pharmacodynamic behavior of animals. Two-step synthesis method is adopted to prepare 5-FU-CS-mPEG prodrugs, and infrared, 1H-NMR and differential thermal analysis are adopted to analyze characterization synthetic products of prepared drugs. To ensure clinical efficacy of prepared drugs, UV spectrophotometry is adopted for determination of drug loading capacity of prepared drugs, transmission electron microscopy is adopted to observe the appearance, dynamic dialysis method is used to observe in vitro drug release of prepared drugs and fitting of various release models is done. Anti-tumor effect is studied via level of animal pharmacodynamics. After the end of the experiment, tumor inhibition rate, spleen index and thymus index of drugs are calculated. Experimental results show that the prepared drugs are qualified in terms of regular shape, dispersion, drug content, etc.. Animal pharmacodynamics experiments have shown that concentration level of drug loading capacity of prepared drugs has a direct impact on anti-tumor rate. The higher concentration, the higher anti-tumor rate. Results of pathological tissue sections of mice show that the prepared drugs cause varying degrees of damage to receptor cells, resulting in cell necrosis or apoptosis problem. It can thus be concluded that ion gel method is an effective method to prepare drug-loading nanoparticles, with prepared nanoparticles evenly distributed in regular shape which demonstrate good slow-release characteristics in receptor vitro and vivo. At the same time, after completion of drug preparation, relatively strong anti-tumor activity can be generated for the receptor, so this mode of preparation enjoys broad prospects for development.


      PubDate: 2016-04-25T12:38:27Z
       
  • Ablation Effects of Noninvasive Radiofrequency Field -Induced Hyperthermia
           on Liver Cancer Cells

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Kaiyun Chen, Shuguang Zhu, Guoan Xiang, Xiaopeng Duan, Jiwen He, Guihua Chen
      To have in-depth analysis of clinical ablation effect of noninvasive radiofrequency field- induced hyperthermia on liver cancer cells, this paper collected liver cancer patients’ treatment information from10 hospitals during January 2010 and December 2011, from which 1050 cases of patients were randomly selected as study object of observation group who underwent noninvasive radiofrequency field- induced hyperthermia treatment; in addition, 500 cases of liver cancer patients were randomly selected as study object of control group who underwent clinical surgical treatment. After treatment was completed, three years of return visit was done, survival rates of the two groups of patients after 1 year, 2 years, 3 years were compared, and clinical effects of radiofrequency ablation of liver cancer was evaluated. Zoom results show that the two groups are similar in terms of survival rate, and the difference is without statistical significance. 125 patients in observation group had varying degrees of adverse reactions, while 253 patients in control group had adverse reactions. Difference between groups P<0.05, with significant statistical significance. It can be concluded that radiofrequency ablation of liver cancer is more secure. Therefore, the results of this study fully demonstrate that liver cancer treatment with noninvasive radiofrequency field-induced hyperthermia is with safety effect and satisfactory survival rate, thus with relatively high clinical value in clinical practice.


      PubDate: 2016-04-25T12:38:27Z
       
  • Preparation and Application of Functionalized Nano Drug Carriers

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Rudong Gong, Gaimin Chen
      Objective Targeting at category memory characteristics and preparation methods of functionalized nano drugs, preparation technology of functionalized nano drug carriers are studied, and then important role of functionalized nano drug carrier in preparation of medicine is studied. Methods Carry out the relevant literature search with computer, change limited language in the paper to Chinese and necessarily remove repetitive studies. Results After first review of 1260 retrieved literature, it can be found that nano drug is with accurate quantity, relatively good targeting, specificity and absorbency. Necessary research of nano drug carriers can prevent and treat disease to a certain extent. Conclusion Preparation of functionalized nanocarrier is simple and convenient, which can improve frequency of use of nano preparation technology and provide better development space for medical use. Therefore, nanocarriers should be combined with drugs with relatively strong specificity in clinics, in order to be able to conduct effective research on nanometer intelligent drug, effectively promote long-term development of nano biotechnology, and then provide favorable, reliable basis for clinical diagnosis and treatment.


      PubDate: 2016-04-25T12:38:27Z
       
  • Separation and Purification and in Vitro Anti-Proliferative Activity of
           Leukemia Cell K562 of Galium Aparine L. Petroleum Ether Phase

    • Abstract: Publication date: Available online 24 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Guoqing Shi, Jiang Liu, Wen’en Zhao, Yanqi Liu, Xinfeng Tian
      To explore material basis of in vitro anti-proliferative activity of leukemia cell K562 of petroleum ether phase of product resulting from galium aparine L. 60% ethanol extraction, the experiment adopts column chromatography combined with thin layer preparation, isolates and purifies petroleum ether, conducts structural identification of obtained single compound and applies MTT method for viability assay of in vitro anti-proliferative activity of leukemia cell K562. Experimental results show that galium aparine L. petroleum ether contains mainly β- sitosterol, daucosterol and dibutyl phthalate and other substances. Under experimental conditions, the three could inhibit the proliferation of leukemia cell K562 with dose-effect and time-effect relationship, of which dibutyl phthalate has strongest activity. Dibutyl phthalate with excellent activity, β- sitosterol with rich content and moderate effect should be the main contributor to its biological activity.


      PubDate: 2016-04-25T12:38:27Z
       
 
 
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