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- NANOCRYSTALLIZATION OF DAPSONE; A NOVEL APPROACH TO BOOST SOLUBILITY,
DISSOLUTION, AND IN-VITRO ...
Abstract: The low aqueous solubility of dapsone (DPS), a widely used anti-acne drug, greatly limits its biological efficacy, especially the anti-inflammatory effect. This article has applied the nanocrystallization technique to increase the surface area which consequently improves the solubility, dissolution, and anti-inflammatory effect of dapsone. Span-stabilized dapsone nanocrystals (DPS-NCs) have been prepared using solvent-antisolvent crystallization technique. The obtained nanocrystals (NCs) were characterized by FTIR, DSC, and X-ray. The morphology, particles surface, sizes, and surface charge of DPS-NCs were examined by TEM, SEM, and zetasizer, respectively. Additionally, the in vitro solubility, dissolution, and anti-inflammatory of the DPS-NCs were investigated. DPS-NCs were spherical in shape with smooth surfaces and had a hydrodynamic particle size of about 149±4.73 nm. The saturated aqueous solubility of DPS-NCs was 1.8 ± 0.05 mg/mL which was about 6 fold higher than that of a pure drug and showed improved in vitro dissolution. The used excipients did not interact chemically with the drug as indicated by DSC and FTIR. X-ray diffraction and TEM imaging confirmed that the produced nanocrystals (NCs) still have a certain degree of crystallinity and did not completely convert to the amorphous state. The in vitro anti-inflammatory of DPS-NCs greatly improved compared to pure drug. DSP-NCs could be considered a novel, promising, and effective therapeutic option for the treatment of acne as well as for relieving the accompanying inflammation.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- NOVEL APPLICATION OF SPIRULINA PLATENSIS EXTRACT AS AN ALTERNATIVE TO THE
EXPENSIVE PLANT ...
Abstract: Capparis cartilaginea is an important medicinal and industrial plant with various bioactivities compound, C. cartilaginea which is difficult to propagate in normal conditions. For establishment and multiplication, MS mediumtreated with crude extract of Spirulina platensis as a source of phytohormones was achieved. Growth parameters of calli revealed that the greatest shoot length (4.08 ± 0.86) and leaf number per shootlet (8.40 ± 1.14) on MS medium supplemented with 4mg/L of algal extract. The phenolic content was measured by the Folin–Ciocalteau method. Results of this study showed that application of crude extract Spirulina platensis at 4mg/L significantly increased the content of phenolic compounds in C. cartilaginea (1.01 mg/g dry mass).HPLC analysis of phytohormones of methanol extract of S. platensis recorded the contents of gibberellins, kinetin and adenine as 241.6, 150.2 and 140.6 ppm respectively.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- PHYTOCHEMICAL CONSTITUENTS AND GAS CHROMATOGRAPHY WITH MASS SPECTROSCOPY
ANALYSIS OF EUPHORBIA ...
Abstract: Alkaloids, phenolics, tannins, glycosides, saponins, sterols, and flavonoids among other bioactive secondary metabolites were found in phytochemical analysis. It was found that cardiac glycosides were absent in leaves of the investigated plant whereas anthraquinones were not found in both leaves and stems of the plant. This study identified the plant's total (alkaloids, flavonoids, tannins, saponins and phenolic acids) percentage. The non-polar components of Euphorbia heterophylla L. were studied. GC-MS analysis of chloroform extracts and crude hexane, as well as other chromatographic separation procedures, were used to identify and characterise eight known chemicals (using MASS). These compounds: Hotrienol, 1,7-Octadiene-3,6-diol, 2,6-dimethyl, 1,7-Octadiene-3,6-diol, 2,6-dimethyl, Coumarin, Caryophyllene oxide, 2H-1-Benzopyran-2-one, 7-methoxy, Longifolenaldehyde, Hexadecanoic acid and ethyl ester.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- RECENT ADVANCES IN DRUGS TARGETING PROTEIN KINASES FOR CANCER THERAPY.
Abstract: Cancer has continued to be utmost challenging and life-threatening diseases to treat. Worldwide, cancer has been proven to be a major cause of death after cardiovascular diseases. The development of new drugs that can be able to inhibit the proliferation of cancerous cells only with minimum or without any side effects on healthy cells is a quite challenging task. Protein kinases are enzymes located in the cytoplasm that phosphorylate proteins. Protein kinases mediate most of the signal transduction in eukaryotic cells and also control many other cellular processes, including metabolism, transcription, cell cycle progression, cytoskeletal rearrangement and cell movement, development, the immune response, nervous system function, apoptosis, and differentiation. Normally, the activity protein kinases are stringently regulated. However, under pathological conditions, deregulation of protein kinases can lead to altered kinase expression and functions, and the initiation and survival of tumors. Therefore, protein kinases are a very attractive target class for therapeutic interventions in many disease states such as cancer. Kinase inhibitors now account for a quarter of all current drug discovery research and development efforts. Therefore, researchers around the globe are involved in the development of more efficient and safer targeted kinase inhibitors. Objectives To complement the published literature on clinical kinase inhibitors, we have prepared a review that recaps this large data set into an accessible format for the medicinal chemistry community. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein for cancer therapy. Results In summary, the potential for developing novel types of kinase inhibitor is huge, and we confidently predict that this will continue to be a major growth area over the next 20 years,
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- DESIGN AND SYNTHESIS OF NOVEL TERREMIDE DERIVATIVES FOR PHARMACOLOGICAL
EVALUATION
Abstract: clinicians and chemists are directed in those days toward the biologically active compounds to reduce the mortality and morbidity. Quinazolines were reported previously as a scaffold that possesses antitumor and antimicrobial activities. Close inspection of the structure-activity-relationships (SAR) of quinazolines revealed important structural features necessary for their antimicrobial activity: a nitrogenous ring and a side chain. Using quinazoline heterocyclic compound to try to synthesize compounds similar to terremide to enhance the activity. In the present work, advantageous moieties have been combined together to generate new hybrid scaffolds of quinazoline with the objective of synthesizing new moieties enhancing the antimicrobial biological activityand drug-like properties.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- AN OVERVIEW OF IMIDES AND THEIR ANALOGUES AS ANTICANCER AGENTS
Abstract: In this review article, we highlight the history of cancer immunotherapy; different types of cancer diseases, different stage of cancers, gene mutations are involved in cancer pathogenesis as well as additional information has been obtained that can be useful for early diagnosis and proper treatment. We also highlight the current pitfalls and limitations of cancer checkpoint immunotherapy and how novel research in the fields of personalized cancer vaccines, autoimmunity, the microbiome, the tumour microenvironment, and metabolomics is aiming to solve those challenges. This review also gives an overview of the many discoveries and the progression of the use of some thalidomide analogues especially naphthalimides as anticancer agents and their applications to date; focusing mainly on mono-, bis-naphthalimide based structures, and their various derivatives (e.g. amines, amino acids, heterocyclic systems).
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- DESIGN AND SYNTHESIS OF NOVEL TERREMIDE AND SULFONAIDES DERIVATIVES FOR
PHARMACOLOGICAL EVALUATION
Abstract: Bacterial infections were first recorded back at 3000 B.C.E. Since then, there have been an enormous number of pandemics that hit the world. Countless doctors and researchers have been working on a definitive solution to exterminate all bacterial infections of all kinds. Marine microorganisms have been widely used as a valid source for pharmacologically active components, and recently the amount of metabolites produced by marine-derived fungi have been increased magnificently, which provided not only wide spectrum of highly active compounds but also gave an enormous number of opportunities for chemists to modify theses incredible entities into more effective and less harmful compounds that can be used as cytotoxic, antiviral, antibacterial and antifungal agents.(He et al., 2013) Quinazolines have been spotted as a new group of agents of decent promising and potential chemotherapeutic and antimicrobial activities.(Raghavendra, Gurubasavarajaswamy, Nagaranavile, & Parameshwaran, 2009) The structure activity relationship of quinazolines has shown it has a very weak antimicrobial activity,(Alafeefy, 2009) Close inspection of the structure-activity-relationships (SAR) of quinazolines revealed important structural features necessary for their antimicrobial activity: a nitrogenous ring and a side chain. Quinazoline heterocyclic compounds have been used to synthesize compounds like terremide B to enhance the activity. Currently, advantageous moieties have been combined to generate new hybrid scaffolds of quinazoline with the objective of synthesizing new moieties enhancing the biological activity and drug-like properties.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- SIMULTANEOUS DETERMINATION OF LEVAMISOLE AND OXYCLOZANIDE IN THE
PHARMACEUTICAL PREPARATION BY ...
Abstract: A sensitive, precise and accurate capillary electrophoresis method was developed for simultaneous determination of levamisole and oxyclozanide in pure sample and pharmaceutical preparation. Capillary electrophoresis was presented as a simple separation analytical method for the simultaneous analysis of the deliberated drugs within a shorter analytical run time. In this study, separation was achieved on fused silica capillary (30 cm - 50 µm internal diameter); background electrolyte solution consisted of phosphate buffer (40 mM, pH 7.9) and UV detection at 227 nm. The method showed to be linear (r2 > 0.9998), precise (RSD <0.193%), accurate (recovery of 99.95% for levamisole and 100.12% for oxyclozanide), specific and robust. LOD and LOQ values were 0.099 µg mL-1 and 0.299 µg mL-1 respectively for levamisole and 0.075 µg mL-1 and 0.228 µg mL-1 respectively for oxyclozanide. The proposed method obtained well separation and had a perfect accuracy. The method was validated according to ICH guidelines and carried out for determination of the cited drugs in their pharmaceutical preparation.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- THREE DIFFERENT CHEMOMETRIC APPROACHES COUPLED WITH UV SPECTROSCOPY FOR
ANALYSIS OF AMLODIPINE ...
Abstract: Amlodipine and olmesartan are two different antihypertensive drugs used in combination in the management of mild to severe hypertension. Degradation of the drug is one of the fatal processes. The potency and efficiency decrease in the presence of degradation products. The univariate spectrophotometric methods cannot provide adequate information for assessment of the presence of the degradation products. In this paper, three different multivariate models were utilized for the assessment of amlodipine and olmesartan in the presence of their degradation products. These methods are principal component regression (PCR), partial least square (PLS), and classical least square (CLS). The linearity range of these methods were 2-10 µg/ml for both drugs. The limits of detection of these methods were from 0.466 to 0.637 µg/ml for amlodipine, and from 0.435 to 0.561 µg/ml for olmesartan while the limits of quantification were from 1.413 to 1.931 µg/ml for amlodipine, and from 1.318 to 1.709 µg/ml for olmesartan.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- MORINGA OLEIFERA CRUDE EXTRACT AND THE REFERENCE M2-CHANNEL BLOCKER
AMANTADINE AS ANTIVIRALS ...
Abstract: Despite that great effort is currently running in the direction of vaccine and drug development, limited number of therapeutics are currently approved against seasonal influenza virus. To limit the spread of the transmission of highly pathogenic influenza (HPAI) viruses including HPAI H5N8 to mammals, it is recommended to control them in their natural and intermediate reservoirs, namely domestic poultry. Herein we aim to test both Moringa oleifera extract against the reference M2-channel blocker amantadine as antivirals against the Egyptian H5N8 isolate, specifically influenza A/chicken/Egypt/Q16684C/2019 (H5N8) virus. Interestingly, beside its high safety on MDCK cells (CC50= 15.42 mg/ml), the extract shows a promising and potent antiviral activity (IC50 = 0.665 µg/ml) against HPAI H5N8, while the 50% inhibitory concentration (IC50) of the amantadine was 56.81 µM. Moringa oleifera extract has shown a very promising effect as an anti-influenza, which makes it worthy of further studies.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- MOLECULAR CHARACTERIZATION OF KEY VIRULENCE TRAITS AMONG
MULTIDRUG-RESISTANT ...
Abstract: Methicillin-resistant Staphylococcus aureus (MRSA) is an evolving cause of illness and death worldwide. MRSA strains can express a wide range of virulence factors that are implicated in their pathogenicity. The present study aimed to investigate the prevalence of crucial virulence traits encoding genes among MRSA isolates from Egyptian hospitals. A total of 170 S. aureus isolates were identified in this study from two Egyptian hospitals. These isolates were recovered from different clinical samples, during the period from September 2017 to December 2018. Of the 170 isolates, 138 (81.2%) were identified as MRSA by conventional microbiological methods and the identification was confirmed by the detection of methicillin resistance encoding gene mecA. Antimicrobial susceptibility was determined for MRSA isolates using the Kirby-Bauer disk diffusion method against 16 different antimicrobial agents representing diverse antimicrobial classes. Out of 109/138 (79%) Multidrug-resistant (MDR)-MRSA, fifty MDR-MRSA isolates were selected for further analysis of virulence encoding genes. MRSA isolates were resistant to different classes of antimicrobial agents including ꞵ-lactams, aminoglycosides, tetracyclines, macrolides and lincosamides. The antimicrobial resistance patterns among the selected 50 MDR-MRSA isolates revealed that the highest resistance rate was 100% to each of cefoxitin and penicillin, followed by doxycycline (80%), tetracycline (76%), gentamicin (74%), erythromycin (68%), clindamycin (60%) and azithromycin (50%). While the highest susceptibility rate was 88% to linezolid, followed by teicoplanin (66%), and amikacin (60%). Among the selected MDR-MRSA isolates, 52% were strong biofilm producers and 48% were moderate biofilm producers. The 50 MDR-MRSA isolates were screened for the presence of the virulence genes (icaA, icaD, cna, hla, geh, tsst-1 and LukE/D)that areimplicated in their pathogenicity. The highest frequency of virulence genes in the selected MDR-MRSA isolates was 100% to each of icaD and geh, followed by hla (98%), icaA (96%), cna (92%), LukE/D (68%), and tsst-1 (56%). This study indicates that MRSA infection remains a significant problem in hospitals in Egypt. In addition, this study has verified a high prevalence of virulence factors among MRSA isolates from diverse clinical sources. Therefore, future studies on MRSA should aim to elucidate MRSA epidemiology, study antimicrobial susceptibility profiles, and investigate their virulence factors for effective control measures and better health management.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- HIGHLY EFFICIENTLY INACTIVATION OF MICROBIAL PATHOGENS USING ADVANCED
OZONE GENERATOR UNIT AS ...
Abstract: Searching for an alternative disinfection and sanitization strategy to control and prevent the contamination and diseases caused by microbial pathogens represents one of the critical challenges for all world governments. So that the antimicrobial efficiency of ozone gas as a terminal disinfectant was estimated at a relatively small level (1.2 mg/l/h) using a unit that was generated as a local unit assembled at the faculty of science against six reference strains including Staphylococcus aureus (ATCC 6538), Bacillus subtilis (ATCC 9372), Bacillus spizizenii (ATCC 6633), Escherichia coli (ATCC 8739), Pseudomonas aeroginosa (ATCC 9027), and Candida albicans (ATCC 10231) for 10, 20, 30 and 40 minutes under laboratory conditions. After 10 min of ozone treatment, the log reduction of cell viability was 97.15%, 59.25%, 24.20%, 24.09%, 14.50 %, 13.47%, and 0.46% for P. aeroginosa, strains combination, E. coli, C. albicans, B. spizizenii, B. subtilis, and S. aureus, respectively. The twenty-minute exposure to ozone resulted in a reduction in microbial viability percent 98.17%, 82.88%, 69.63%, 62.79%, 49.43%, 29.57%, and 28.08%, for P. aeroginosa, strains combination, B. subtilis, and E. coli, C. albicans, S. aureus, and B. spizizenii, respectively. The efficacy of ozone for P. aeroginosa, E. coli, and strains combination increased by more than 98% after 30 min of ozone treatment followed by 90.41%, 86.76%, 52.63%, and 36.64% for B. subtilis, C. albicans, B. spizizenii, and S. aureus, respectively. The maximum ozone efficacy reached 100% for all reference stains except B. spizizenii (62.10%) after 40 min of ozone treatment making this strategy a candidate tool recommended for the management and control of the pathogenic microorganisms.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- PREVALENCE OF VANCOMYCIN RESISTANT STAPHYLOCOCCUS AUREUS (VRSA) IN SOME
EGYPTIAN HOSPITALS
Abstract: A long time ago, we found that increase in the prevalence of antibiotic resistant pathogens and strains in serious infections, the reason of distribution of these strains is because of the miss use of antibiotics to treat humans against different microorganisms,one of the most important infectious etiological agent is Staphylococcus aureus.Staphylococcus aureus strains were recovered from approximately 514 clinical samples were collected from patients admitted to Beni-Suef Public Hospitals,Assuit University and Beni-Suef University Hospital,Demerdash Hospital,S. Galal Hospital.Vancomycin resistance was determined by broth dilution method. Resistance against different antibiotics were determined by disc diffusion method. Screening for virulence genes were performed by PCR method.we found that From 514 clinical samples we found that staphylococcus strain were 308 strains (59.9%),and we found that staphylococcus aureus strain were 296 strains (96.1 %). Methicillin resistant staphylococcus aureus (MRSA) strain were 215 (72.6 %). Collected MRSA strains were distributed as 184 VSSA (85.5%),19VISA (8.8 %), and12 VRSA strains (5.5 %).The incidences of VRSA in hospitalized sample equal to non-hospitalized sample.The resistant genes detected from 31 strain (VISA and VRSA) were Mec A in 15 isolates (48.3 %),Van A in 12 isolates (38.7%), Panton valentine lucocidine toxin (lucotoxin) in 16 isolates (51.6 %), Enterotoxin type A in 18 isolates (58 %) followed by TSST in 14 isolates (45.1 %), and the lower incidences observed in genes of Exfoliative toxin type A in 5 isolates (16.1 %) and Exfoliative toxin type B in 1 isolate (3.22 %).The results of study provide that the high prevalence of VRSA in Egypt, andthe necessity for new and effective drugs against VRSA.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- MOLECULAR STUDY ON CLADOSPORIUM SPECIES ISOLATED FROM AIR OF CAIRO, USING
UNIVERSALLY ...
Abstract: Universally Primed-PCR (UP-PCR) and Internal Transcribed Spacer-PCR (ITS-PCR) based genomic fingerprinting techniques are considered a good methods that rely on specifically targeted primers. These techniques, which analyse the rDNA, have been shown to be relatively robust and discriminatory. This study was designed to investigate and characterize the molecular variation among Cladosporium strains collected at different sites in Cairo by using two different fingerprinting methods, Universally Primed- PCR (UP- PCR) and Internal Transcribed Spacer (UP- PCR) technique. The Cladosporium isolates investigated were isolated from air of Cairo by settle plate method. The samples were then purified and identified by using culture based techniques, microscopical methods, and biochemical reactions followed by confirmation in the regional center for mycology and biotechnology (RCMB). Molecular fingerprinting, and genetic similarities among Cladosporium species populations depending onmicrosatellites-polymerase chain reaction (ITS-PCR). Primers used are ITS4, and ITS5. PCR products were digested with 3 restriction enzymes and separated by agarose electrophoresis. Restriction patterns generated by CfoI, Msp < /em>I and RsaI. In addition, we have applied the Universally Primed PCR (UP-PCR) technique using two primers L21 and Fok1.The current work showed prominent discriminatory power given by amplification of internal transcribes spacers PCR regions followed by restriction with CfoI enzyme than other endonucleases. moreover, Fok1 primer revealed minor variability among Cladosporium strains using UP-PCR genotyping technique.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- SILYMARIN AMELIORATES DIETHYLNITROSAMINE-INDUCED LIVER FIBROSIS IN WISTAR
RATS
Abstract: Aim: the aim of this study was to compare the impact of silymarin on the liver fibrosis induced by diethylnitrosamine (DEN) between both sexes of Wistar rats and proposing possible mechanisms.Main Methods: twenty-four Wistar male and twenty-four Wistar female rats were randomly assigned into 8 groups according to their sex (n=6) for administration of vehicle, DEN, silymarin or both DEN and silymarin for 8 weeks. At the end of the experiment, the traditional rat body and liver weight parameters, liver injury biomarkers (serum ALT, AST, ALP, and total bilirubin) were measured. Furthermore, hematological parameters, lipid profiles (TC, LDL-C, HDL-C, and TG) and oxidative stress biomarkers (TBARS, SOD, CAT, and GSH) were determined. Also, the inflammatory biomarkers in liver tissue homogenate (TNF-α, TGF-β) were evaluated. Histopathological subjective scoring system graded the damage markers of liver tissue. Expression of NF-kB was measured immunohistochemically.Results: Markedly diminished DEN induced liver fibrosis markers in female groups while worsened in male groups. Silymarin regimen improved liver functions and fibrosis markers. Additionally, it counteracted DEN-induced oxidative stress, lipid peroxidation and inflammations, silymarin provided these ameliorative effects either in males or females rats.Conclusion: Silymarin plays an ameliorative role of DEN-induced liver fibrosis in male and female rats via reducing oxidative stress and inflammations.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- ESTROGEN ATTENUATES DIMETHYLHYDRAZINE-INDUCED COLON INJURY IN FEMALE RATS
VIA ABROGATION OF ...
Abstract: The involvement of estrogen, the female sex hormone, in a variety of gastrointestinal conditions has been documented. We studied the effect of endogenous and exogenous estrogen (estradiol benzoate, 30μg/kg/day S.C) for 8 weeks on early preneoplastic markers induced by the intraperitoneal injection of 1,2-dimethylhydrazine (20 mg/kg) in female rats. Either in sham rats or estradiol benzoate administered animals, estrogen abrogated tumor markers (CA 19.9 and CEA), decreased damage and inflammatory cells infiltration in colon tissue, attenuated oxidative stress markers (MDA, SOD, CAT, and GSH) and inflammatory mediators (IL-6 and IL-10). In conclusion, the estrogen protects against colon injury by reducing precancerous colonic lesions and oxidative stress. The research sheds new light on the therapeutic benefits of estrogen against colon injury in rats.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
- SIMULTANEOUS DETERMINATION OF LEVAMISOLE AND OXYCLOZANIDE IN THE
PHARMACEUTICAL PREPARATION BY GC-MS
Abstract: A sensitive, precise, and accurate gas chromatography-mass spectrometry method was developed for the simultaneous determination of levamisole and oxyclozanide in pure samples and pharmaceutical preparation. Gas chromatography was presented as a simple separation analytical method for the simultaneous analysis of the deliberated drugs within a shorter analytical run time. In this study, separation was achieved using a ZB5 column with (30 m ×0.53 mm, 1.50 µm), and helium as a carrier gas. The proposed method showed well separation between the drugs and each other and had good accuracy. The method showed to be linear (r2 = 0.9998), precise (RSD < 0.496%), accurate (recovery of 99.37% for levamisole and 100.14% for oxyclozanide), specific and robust. LOD and LOQ values were 0.935 ng mL-1 and 3.085 ng mL-1 respectively for levamisole and 0.884 ng mL-1 and 2.917 ng mL-1 respectively for oxyclozanide. The proposed method obtained well separation and had perfect accuracy. The method was validated according to ICH guidelines and carried out to determine the cited drugs in their pharmaceutical preparation.
PubDate: Wed, 31 Aug 2022 22:00:00 +010
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