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Egyptian Pharmaceutical Journal
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  This is an Open Access Journal Open Access journal
ISSN (Print) 1687-4315 - ISSN (Online) 2090-9853
Published by Medknow Publishers Homepage  [448 journals]
  • Antibacterial and phytochemical evaluations of Alternanthera repens (L.)
           and honey on Pseudomonas aeruginosa of clinical origin

    • Authors: Olorunjuwon O Bello, Faith O Lebi, Temitope K Bello, Yinka D Oluwafemi
      Pages: 273 - 281
      Abstract: Olorunjuwon O Bello, Faith O Lebi, Temitope K Bello, Yinka D Oluwafemi
      Egyptian Pharmaceutical Journal 2022 21(3):273-281
      Context Medicinal plants have long been used as a source of therapeutic agents worldwide, and herbal medicines have increasingly been employed in the treatment of diseases. Alternanthera repens is one of the underexploited plant species for its antimicrobial potentials.Aims This study aimed at investigating the antibacterial efficacy of the leaf and stem ethanolic extracts of A. repens and honey against Pseudomonas aeruginosa.Materials and methods The phytochemical analyses were performed on ethanolic plant extracts using the universal laboratory techniques for qualitative and quantitative determination. The agar-well diffusion method was used for the in-vitro antibacterial bioassay. The antibacterial activities of the honeys, ethanolic leaf and stem extracts, and antibiotics were compared. The minimum inhibitory concentrations and minimum bactericidal concentrations of the honeys and extracts were determined.Statistical analysis used The students' t-test was employed to determine the significant differences between the phytochemical constituents in the extracts and also the antibacterial activities of the ethanolic leaf and stem extracts against P. aeruginosa.Results Phytochemical screening showed the presence of total phenols, saponins, tannins, total flavonoids, alkaloids, cyanogenic glycosides, phytate, and terpenoids in the plant extracts. The extracts and honeys were able to inhibit the growth of the P. aeruginosa at varying concentrations (25, 50, 75, and 100%). The combinations of the honeys and ethanolic extracts of the plant parts exerted significantly higher antibacterial effects on P. aeruginosa.Conclusion The ethanolic extracts of A. repens possessed antibacterial properties against P. aeruginosa, which was more pronounced in combination with honey. The presence of various phytochemicals in the plant indicated its high potential for possible drug production.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):273-281
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_10_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Isolation of asparaginase-producing microorganisms and evaluation of the
           enzymatic antitumor activity

    • Authors: Walid Bakeer, Mohamed Amer, Walaa G Hozayen, Nahla S Kotb, Marwa H.A Hassan
      Pages: 282 - 292
      Abstract: Walid Bakeer, Mohamed Amer, Walaa G Hozayen, Nahla S Kotb, Marwa H.A Hassan
      Egyptian Pharmaceutical Journal 2022 21(3):282-292
      Background L-asparaginase is an enzyme with very high biological activity owing to its activity on several tumor cells. It is mainly used to treat acute lymphoblastic leukemia. The complicated immunogenic adverse effects of present microbial sources present a need for switching to natural novel sources that have no immunogenic effect and better activity of L-asparaginase, so screening for other sources of L-asparaginase, like marine bacteria, may result in an enzyme having fewer adverse effects.Objective To screen and identify marine eco-friendly and potent L-asparaginase-producing bacteria, having a novel immunological property that possibly will avoid hypersensitivity.Materials and methods In the present study, bacterial strains were screened for extracellular L-asparaginase production from marine isolates, identified by 16 s rDNA technology, and L-asparaginase productivity was assessed using semiquantitative and quantitative enzymatic assays. The antiproliferative effect of the partially purified enzyme on different tumor human cell lines [HepG-2 (human hepatocellular carcinoma cell line), MCF-7 (breast cancer cell line), and PC-3 (prostate carcinoma cell line)] was assessed by the mitochondrial-dependent reduction of yellow MTT.Results and conclusion Bacillus safensis was established as the bacterial strain (Gene Bank accession number: MK541039). The extracellular enzyme-yielding capacity of the isolate B. safensis (518 IU/ml) was found to be 4.18 times higher than Bacillus pumilus (157.03 IU/ml) and higher than Bacillus circulans species (85 IU/ml). The marine isolate is environmentally friendly and can be used to produce significant quantities of extracellular L-asparaginase for the treatment of a variety of tumors and preparation of acrylamide-free fry food.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):282-292
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_11_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • The spray-dried mucoadhesive microparticles of rizatriptan with chitosan
           and carbopol in migraine

    • Authors: Sachin Jadhav, Sagar Mishra
      Pages: 293 - 301
      Abstract: Sachin Jadhav, Sagar Mishra
      Egyptian Pharmaceutical Journal 2022 21(3):293-301
      Background The traditional oral formulation for migraine treatment has the drawbacks of first-pass metabolism, plasma-protein binding, and poor blood–brain-barrier penetration. This study was conducted to establish the nasal route of administration for rizatriptan formulations in migraine.Materials and methods Rizatriptan mucoadhesive microparticles were synthesized by spray-drying and evaluated for infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. The ex vivo study was done with Franz’s diffusion cell using goat nasal mucosa. The in vivo study was performed on the Albino rat’s nasal route for determining drug concentration by high-performance liquid chromatography analysis in brain tissue at single-point evaluation.Result The microparticles were of optimum size with no drug–polymer interaction in infrared spectroscopy and differential scanning calorimetry. Scanning electron microscopy exhibited the morphology of spherical or ellipsoid microparticles with efficient drug entrapment. The percentage of drug permeability for chitosan microparticles was 76.53–91.09 and for carbopol microparticles was 78.49–92.25 in the ex vivo permeability study. In vivo studies showed that drug concentrations of 126.46–148.50% for chitosan batches and 152.83–165.04% for carbopol batches were superior to controls.Conclusion Ex vivo permeability study revealed drug-permeation patterns as high as 91.09±0.03% for RCH3 formulation and 92.25±0.2% for RC3 formulation. In in vivo study formulation, RCH3 displayed a drug concentration of 132.22±8.32% and RC3 showed 159.46±4.05% over the control batch, which is conclusive for improved drug delivery of rizatriptan through mucoadhesive microparticles for the nose-to-brain targeting in migraine.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):293-301
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_37_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Isolation, screening, and molecular identification of pectinase producers
           from fruits, vegetables, and soil samples

    • Authors: Abd-El-Aal S Kh, A.G. Attallah, Nagwa M Abdel-Aziz, Bigad E Khalil
      Pages: 302 - 311
      Abstract: Abd-El-Aal S Kh, A.G. Attallah, Nagwa M Abdel-Aziz, Bigad E Khalil
      Egyptian Pharmaceutical Journal 2022 21(3):302-311
      Background and objective In this work, isolation, identification (morphological and chemical), and molecular characterization were done of local isolates of some pectinase-producing microorganisms such as bacteria, actinomycetes, fungi, and yeast.Materials and methods A total of 22 local bacterial isolates were obtained from various sources and were assayed for pectinolytic activity after optimization of conditions for pectinase production. Isolate no. 19 showed the highest pectinase-specific activity (6.73 U/ml) on glucose-supplemented medium, whereas isolate no. 5 gave the lowest pectinase productivity (3.21 U/ml). The identification of isolate no. 19 revealed that it belonged to the genus Bacillus based on morphological and biochemical characteristics. Based on molecular identification (16 S rRNA technique), isolate no. 19 was named Bacillus sp. strain NRBANKI-4 (with 99% similarity), with Gene Bank accession number OM540351.Results and conclusion A total of 14 local actinomycete isolates were obtained from soil samples. Isolate no. 13 showed the highest pectinase-specific activity (6.48 U/ml), whereas sample no. 10 gave the lowest pectinase-specific activity (3.07 U/ml). Based on molecular identification (16 S rRNA technique), isolate no. 13 was named Streptomyces sp. KP 12 (90.63% similarity), with Gene Bank accession number OM403596. A total of 10 fungal isolates were obtained from crop waste soil. Isolate no. 2 gave the highest pectinase productivity (21.20 U/ml). Based on molecular identification (internal transcribed spacer-PCR technique), isolate no. 2 was named Aspergillus niger F8121 (99.47% similarity), with Gene Bank accession number OM392061. Following the same trend, 10 yeast isolates were isolated from crop waste soil. The isolate that gave the highest pectinase productivity was no. 7, which gave 22.03 U/ml. The isolate that gave the lowest was no. 9 (20.74 U/ml). Isolate no. 7 was named Pichia barkeri Y1 (90.91% similarity), with Gene Bank accession number OM392066.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):302-311
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_39_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • In-vivo antidiabetic and antidyslipidemic effects of methanolic leaf
           extract of Combretum indicum in the streptozotocin-induced diabetic rats

    • Authors: Senjuti Majumder, Hossain Md Abu Hanif, Israt Jahan Bulbul, Zebunnesa Ahmed, Md. Rajdoula Rafe
      Pages: 312 - 317
      Abstract: Senjuti Majumder, Hossain Md Abu Hanif, Israt Jahan Bulbul, Zebunnesa Ahmed, Md. Rajdoula Rafe
      Egyptian Pharmaceutical Journal 2022 21(3):312-317
      Background Combretum indicum (locally known as Basantilata) is a notable medicinal plant belonging to the family Combretaceae. Extracts collected from leaves of this plant have activities including antibacterial, antipyretic, and antidiarrheal activities.Objective This study was designed to evaluate the crude methanolic leaf extract of C. indicum (MLCI) to evaluate its activities in hyperglycemic and dyslipidemic rats.Materials and methods In-vivo antidiabetic and antidyslipidemic activities of the extract were studied in streptozotocin-induced diabetic rat models following the standard protocol established earlier. The rats were randomly divided into groups I–V as normal control, diabetic control, metformin, MLCI 250 mg/kg, and MLCI 500 mg/kg body weight, respectively.Results and conclusion The in-vivo studies indicated concentration-dependent and significant (P<0.05, 0.01, 0.001) reductions of elevated blood glucose, total cholesterol, triglyceride, and low-density lipoprotein-cholesterol levels in the treatment groups compared with diabetes-induced control group. Simultaneously, a significant (P<0.001) rise in high-density lipoprotein-cholesterol level was also observed in the study. The results revealed the advantageous roles of the MLCI in the management of diabetes mellitus.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):312-317
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_16_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Aphicidal and biochemical effects of emulsifiable concentrate and
           nanoemulsion of two selected essential oils against black bean aphid,
           Aphis fabae (Scop.)

    • Authors: Hala M Metwally, Samar S Ibrahim, Elham A Sammour
      Pages: 318 - 327
      Abstract: Hala M Metwally, Samar S Ibrahim, Elham A Sammour
      Egyptian Pharmaceutical Journal 2022 21(3):318-327
      Background and objectives Aphids are cosmopolitan pests that feed on a wide range of host plants from different botanical families. Aphids have developed resistance to several groups of synthetic insecticides. Because of their antimicrobial, antiviral, and insect-repellent properties, essential oils extracted from medicinal plants are excellent sources of various bioactive compounds. Formulation of essential oils as emulsifiable concentrate (EC) and nanoemulsion (NE) could help to enhance their bioavailability.Materials and methods The insecticidal activity of essential oils derived from two medicinal plants, namely, Proserpinaca palustris L. and Terminalia chebula Retz., was evaluated against black bean aphid, Aphis fabae (Scop.), under laboratory and semifield conditions. The essential oils from both plants were synthesized as EC and NE formulations to enhance their insecticidal efficacy. The stability of ECs and droplet size of NEs were assessed. The toxicity of ECs in comparison with NEs was evaluated against A. fabae adults. Moreover, the biochemical efficacy of the two essential oils on the activity of acetylcholinesterase and glutathione S-transferase enzymes of A. fabae was studied.Results and conclusion In laboratory bioassay, both ECs and NEs of selected oils displayed significant toxicity in controlling A. fabae, with lethal concentration values (LC50) for P. palustris EC and NE being 0.59 and 0.50%, respectively. Moreover, LC50 for T. chebula EC and NE was 0.65 and 0.78%, respectively. The bulk essential oils showed less toxic activity against A. fabae adults, with LC50 of 0.68 and 1.16% for P. palustris and T. chebula bulk forms, respectively. Under semifield conditions, EC of P. palustris and T. chebula at LC90 and LC90x3 exhibited greatly lethal effects for aphid adults compared with NE formulations. Both formulations (ECs and NEs) significantly increased the reduction percent of acetylcholinesterase and glutathione S-transferase enzymes of the treated aphid adults. Our results suggest that EC and NE formulations from P. palustris and T. chebula enhanced the insecticidal toxicity of the selected oils and could be used to effectively control A. fabae adults.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):318-327
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_40_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Anticancer redox action of gallium nanoparticles combined with a low
           dosage of γ-radiation against hepatocellular carcinoma in male rats

    • Authors: Mohga S Abdalla, El-Sayed M El-Mahdy, Somaya Z Mansour, Sawsan M Elsonbaty, Menna A Hussien
      Pages: 328 - 337
      Abstract: Mohga S Abdalla, El-Sayed M El-Mahdy, Somaya Z Mansour, Sawsan M Elsonbaty, Menna A Hussien
      Egyptian Pharmaceutical Journal 2022 21(3):328-337
      Background and objective Nanotechnology affords a new valuable field for the preparation of intrinsic nano anticancer drugs through green synthesis of plant active extracts supported with gallium nanoparticles (GaNPs) to provide us with a new Ga form of treatment with lower toxicity risk. The current study aimed at evaluation of a new GaNP form with grape seed extract as an anticancer agent against hepatocellular carcinoma (HCC) in rats. Moreover, the effect of the exposure to a low dose of γ-radiation on the treatment and prevention of tumor was studied.Materials and methods The cytotoxic effect was measured against the HepG2 tumor cell line. An experimental design was optimized using 80 Wistar male rats (120−150 g) divided into eight groups, with 10 rats each. The animals are administered with diethylnitrosamine to induce HCC and then orally administered with a dose of 38.5 mg/kg from the GaNPs in combination with the exposure of the total body to a low dose of γ-radiation (0.5 Gy).Result and conclusion The combination of GaNPs/γ-radiation demonstrated significant cytotoxicity against HepG2 cell line with an IC50 of 388.8 µg/ml. Moreover, the results indicated normal structures in the liver architecture, and the conventional biochemical assays showed significant depletion in lipid peroxide, alanine aminotransferase, and aspartate aminotransferase activities and creatinine levels. Additionally, there was a significant increase for the antioxidant state parameter in the form of a pronounced reduction of glutathione level. The ameliorative effect of the treatment was well appreciated by the histopathological alteration results. Therefore, it can be concluded that GaNPs/γ-radiation can serve as a good therapeutic agent for the treatment of HCC that ought to attract more studies.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):328-337
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_65_21
      Issue No: Vol. 21, No. 3 (2022)
       
  • Isolation and molecular identification of lignin peroxidase-producing
           bacterial isolates from Jeddah City

    • Authors: Reem S.M Batayyib, Nada H Al-Twaty, Ola I.M El-Hamshary
      Pages: 338 - 346
      Abstract: Reem S.M Batayyib, Nada H Al-Twaty, Ola I.M El-Hamshary
      Egyptian Pharmaceutical Journal 2022 21(3):338-346
      Background The identification of naturally occurring bacteria with lignin-oxidizing enzymes would be significant. Several species of filamentous bacteria belonging to the genus Streptomyces (Actinomycetes) have been identified as degraders of lignin. Such species play the most important role in biodegradation of lignin.Objective This study aimed to isolate and discover promising isolates and ideal conditions for lignin peroxidase (LiP) production as well as 16S-rRNA identification of the ligninolytic bacterial strains.Materials and methods Lignin was isolated and purified from black wood liquor. The ligninolytic bacterial colonies were isolated from three types of soil farms (F1, F2, and F3) from Jeddah, KSA. Fermentation medium (FM) was used for screening of lignin-degrading bacteria after dilution of the soil sample using lignin (0.1% v/v). The FM medium was supplemented with 50 mg/l of Azure B and toluidine dyes and 100 mg/l of tannic acid. FM was used without any supplements and agar for isolation of lignin-degrading bacteria after dilution of the soil samples. Different concentrations of lignin (0.1–0.9%) were applied to optimize LiP production by the selected strains under different temperatures (30, 35, 40, and 45°C); different pH values (7, 7.5, 8.0, and 8.5); eight different carbon sources (0.1%, w/v), such as glucose, fructose, xylose, lactose, sucrose, carboxymethyl cellulose, and xylan; and four organic sources (0.1%, w/v), such as peptone, meat extract, sodium nitrate, and potassium nitrate. The enzyme productivity was evaluated in the culture supernatant. The bacterial strain genomic DNA was extracted from pure culture isolated from soil and subjected to amplification and sequencing of 16 S ribosomal RNA gene.Results and discussion Nine ligninolytic bacterial colonies that excrete peroxidases based on the use of lignin (as sole carbon source) were isolated from three types of soil farms (F1, F2, and F3) from Jeddah, KSA, and the promising isolates and the optimum conditions for LiP production using FM under three incubation periods were evaluated. Two most active isolates for production of LiP belonging to Actinomycetes and Bacilli designated (R-St-1 and R-B-1) were identified using 16S-rRNA. Results showed that the highest LiP producer was Streptomyces R-St-1 isolate (3.8 U/ml) followed by Bacilli R-B-1 isolate (2.4 U/ml) after 3 days of fermentation. Different concentrations of lignin (0.1–0.9%) were tested for their effect on LiP production by Streptomyces R-St-1. As lignin concentration increased, LiP production increased, and the maximum productivity of 4.9 U.mL−1 was observed at 0.5% lignin after which the LiP production was decreased. At the ideal temperature recorded of 35°C and at the optimum pH of 7.5, the production of LiP rose significantly (4.6 U.mL-1 and 4.0 U.mL-1).Various carbon sources were examined for LiP production, and glucose was shown to be the best option for producing a high yield of LiP by Streptomyces R-St-1, followed by lactose (4.6 and 4.0 U/ml, respectively). However, neither organic nor inorganic nitrogen sources were shown to be suited for high LiP output. As lignin concentration increased, LiP production increased, and the maximum productivity of 4.4 U/ml from Bacilli R-B-1 isolate was observed at 0.7% lignin, after which LiP production was decreased. The optimum temperature was 40°C, where LiP production showed a significant increase (4.5 U/ml), whereas the optimum pH was 8.0, and sucrose was found to be more suitable for high yield of LiP production followed by glucose (4.3 and 3.3 U/ml, respectively). The identified bacterial DNA sequences were conserved in the GenBank under two accession numbers OL697233.1 (Streptomyces lavendulae R-St-1) and Priestia aryabhattai R-B-1(OL697234.1) (formerly known as Bacillus aryabhattai).
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):338-346
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_49_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Lactic acid bacteria: economic propagation, chitinases activity, and
           enhancing viability by gel encapsulation

    • Authors: Nagwa A Atwa, Marwa I Wahba, Dina A Maany, Hassan M Awad, Mohamed I Abo-Alkasem, Hossam M El-Masry, Mai N Amer, Ahmed I El-Diwany
      Pages: 347 - 359
      Abstract: Nagwa A Atwa, Marwa I Wahba, Dina A Maany, Hassan M Awad, Mohamed I Abo-Alkasem, Hossam M El-Masry, Mai N Amer, Ahmed I El-Diwany
      Egyptian Pharmaceutical Journal 2022 21(3):347-359
      Background In a previous study, a lactic acid bacterium, Enterococcus faecium, was locally isolated from Egyptian soil and its ability to inhibit the growth of a test phytopathogen was proven.Objective The study was performed to assess the ability of the tested strain to grow on different media. The produced antifungal agent was investigated. Finally, the strain was encapsulated within different biopolymers to increase its viability.Materials and methods Several byproducts were tested and compared with the standard De Man-Rogosa-Sharpe medium. The antifungal activity was tested using the poisoned food technique. Chromatographic analysis of the fermentation medium was performed using high-performance liquid chromatography. Production of chitinase was confirmed by cultivating the test strain on chitin and estimating the amount of reducing sugars using the Somogyi method. The E. faecium cells were also encapsulated within soy protein isolate-alginate beads, gellan gum discs, and carboxymethyl cellulose beads.Results and conclusion The strain was able to grow on all of the tested byproducts and exerted a potent antifungal activity against Fusarium solani, especially when a very economic medium, mainly composed of whey, was used. High-performance liquid chromatography results confirmed the production of a number of organic acids that contributed in the inhibition of the fungal growth. The study also proved the production of chitinase enzymes, which apparently altered the chitinous layer present in the cell wall of F. solani, causing disintegration of the fungal cells. It was also shown that encapsulation of E. faecium increased its viability in soil as compared with the free uncapsulated strain.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):347-359
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_50_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Synthesis, biological activity, and in silico studies of
           thieno[2,3-d]pyrimidine and thieno[2,3-d]triazine derivatives

    • Authors: Fatma A.A El-Hag, Ahmed A Elrashedy, Ayman M.K Sweed, Ewies F Ewies, Mansoura A Abd-El-Maksoud, Magdy S Aly, Sanaa M.Sh Atta
      Pages: 360 - 375
      Abstract: Fatma A.A El-Hag, Ahmed A Elrashedy, Ayman M.K Sweed, Ewies F Ewies, Mansoura A Abd-El-Maksoud, Magdy S Aly, Sanaa M.Sh Atta
      Egyptian Pharmaceutical Journal 2022 21(3):360-375
      Background The chemistry of condensed heterocyclic compounds has emerged in numerous reports for their diverse biological properties and drug discovery. Pyrimidine and triazine scaffolds have been utilized as therapeutic agents in many medicinal applications. Many research groups have designed and synthesized pyrimidine moieties as they are incorporated in nucleic acid bases.Objective In this report, we have designed and synthesized a variety of 2-mercaptothieno pyrimidine and thienotriazine derivatives and 2-mercaptothienopyrimidines conjugated with sugar moiety. The newly synthesized compounds were tested for their biological activity against breast (MCF-7), liver (HepG-2), and prostate (PC-3) cancer cell lines as well as a normal cell line (human normal melanocyte, HFB4) and were also analyzed for in silico studies to determine their potential.Materials and methods A variety of 2-mercaptothienopyrimidine and thienotriazine derivatives were prepared via cyclization of ethyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1) and 2-amino-N-phenyl-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (9). Two derivatives of 2-mercaptothienopyrimidines conjugated with sugar moiety were also prepared. The products were screened for their biological activity against breast (MCF-7), liver (HepG-2), and prostate (PC-3) cancer cell lines as well as the normal cell line (human normal melanocyte, HFB4) in comparison with the known anticancer drug 5-fluorouracil using the MTT assay.Results and conclusion The results indicated that most of the tested compounds exhibited no activity against the growth of HFB4. Compounds 5, 8, 10, 12, and 14 revealed effective antiproliferative activity against MCF-7 cell lines with IC50 of 4.6, 6.2, 5.4, 7, and 3.25 µg/ml, respectively, compared with 5-fluorouracil (IC50 of 3.97 µg/ml). In the same sense, the evaluation of cytotoxic effect of the tested compounds against human liver HepG-2 cancer cell lines revealed that compounds 5, 8, 10, 12, and 14 showed cytotoxic activity close to that of the standard drug (IC50 values of 5.77±0.99, 7.23±0.98, 4.42±1.32, 7.9±0.90, and 5.1±11.28 µg/ml, respectively, vs. 4.27±0.58 µg/ml for 5-fluorouracil). Free binding energy was estimated by docking and MM-GBSA calculation. Molecular dynamics simulation followed by MM-GBSA calculation was correlated to the cytotoxic effect. Compound 14 illustrated the highest MM-GBSA value (−20.38) and the best cytotoxic effect.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):360-375
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_54_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Physiological, molecular, and immune responses to milk thistle extract
           administration in goats during peripartum period

    • Authors: Nasser Ghanem, Hoda B Mabrok, Sameh M Shedeed, Walaa M Abd El-Wahab, Waleid M.E Shakweer, Mamdouh I Mohamed, Eman H ElSabaawy
      Pages: 376 - 384
      Abstract: Nasser Ghanem, Hoda B Mabrok, Sameh M Shedeed, Walaa M Abd El-Wahab, Waleid M.E Shakweer, Mamdouh I Mohamed, Eman H ElSabaawy
      Egyptian Pharmaceutical Journal 2022 21(3):376-384
      Background Using natural compounds as additives in livestock nutrition could be a new goal in livestock production. Milk thistle extract is rich in bioactive compounds such as silymarin, which act as a strong antioxidant agent.Objective The current study aimed to investigate the metabolic profile, oxidative statue, and immune response after milk thistle extract administration in goats during the peripartum period.Materials and methods Multiparous pregnant Egyptian Nubian goats (n=16) were allocated into four experimental groups. The first group was kept as the control group. The second group was administrated milk thistle extract (10 g/day), whereas third and fourth groups were administrated 20 and 30 g/day for 4 months, respectively. Blood biochemical parameters were measured using colorimetric and enzyme-linked immunosorbent assay. Gene expressions of antioxidant genes [catalase (CAT), superoxide dismutase (SOD1, SOD2), glutathione peroxidase (GPX1), and peroxiredoxin 2] and transcription factor (nuclear factor erythroid 2 related factor 2) were evaluated using quantitative real-time PCR.Results and conclusion Biochemical parameters (total protein, glucose, total lipids, total cholesterol, triglycerides, high-density lipoprotein, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, urea, creatinine, triiodothyronine, and thyroxine) in plasma of groups administrated with milk thistle extract did not significantly differ compared with the control group. Milk thistle extract at high levels (20 and 30 g/day) significantly increased the level of activity of antioxidant enzymes (SOD, CAT, and GPX), total antioxidant capacity, and total immunoglobulin in cases compared with the control group. Moreover, milk thistle extract (20 or 30 g/day) significantly decreased the level of malondialdehyde (lipid peroxidation biomarker) and tumor necrosis factor alpha (inflammatory biomarker) in cases compared with the control group. The results indicated a significant increase in transcript abundance of CAT, GPX1, and SOD1 mRNA in the three groups administrated with milk thistle extract compared with the control group. However, mRNA expressions of SOD2, peroxiredoxin 2, and nuclear factor erythroid 2 related factor 2 were significantly up-regulated after administration with milk thistle extract at high levels (20 and 30 g/day). Milk thistle extract exerts antioxidant, anti-inflammatory, and immune-modulator effects during pregnancy and lactation in goat and maintained normal physiological functions.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):376-384
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_55_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Investigation of chitosan, its depolymerized products, and nanoformulation
           as novel anticonvulsants

    • Authors: Mona E Aboutabl, Bahgat Fayed, Shaymaa A Ismail
      Pages: 385 - 394
      Abstract: Mona E Aboutabl, Bahgat Fayed, Shaymaa A Ismail
      Egyptian Pharmaceutical Journal 2022 21(3):385-394
      Objectives Chitosan is a natural biopolymer that possesses various biological activities. The aim of the current study was to evaluate the potentiality of chitosan and its enzymatically depolymerized products as anticonvulsants.Materials and methods In the current study, chitosan enzymatic depolymerization was carried out using Bacillus cereus chitosanase followed by fractionation of the produced chitooligosaccharides. Phase I anticonvulsant activity of chitosan as well as its enzymatically depolymerized products was evaluated using pentylenetetrazole-induced seizures, maximal electric shock, and neurotoxicity tests. In phase II, median effective dose, median toxic dose, and protective index were determined. In addition, γ-aminobutyric acid brain level and acute toxicity were evaluated.Results and conclusion The results indicated that the fraction with the lower degree of acetylation and longer chains of glucosamine (COSH) possessed rapid onset of action with the highest protection (75%) at 0.5 h and long-acting effect for 4 h. In addition, the median effective dose of COSH was 12.7-fold more potent than the reference ethosuximide, whereas in the maximal electric shock test, COSH showed lower potency than phenytoin. The median toxic dose was 1.4-fold and 7.9-fold higher than ethosuximide and phenytoin, respectively. The protective index was 18.1-fold and 3.98-fold higher than ethosuximide and phenytoin, respectively, with a significant increase in γ-aminobutyric acid neurotransmitter brain level. In an attempt to prolong the anticonvulsant effect of COSH, a nano-formulation was carried out in which the particle size was estimated as 188.7±0.26 nm. After that, an equivalent dose of a combined treatment of COSH and the nanoformula (each 15 mg/kg) was evaluated in which a prolonged effect was achieved up to 24 h.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):385-394
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_58_22
      Issue No: Vol. 21, No. 3 (2022)
       
  • Bullous fixed drug eruptions consequent to NSAID usage &#8722; a
           case series

    • Authors: Naga V Kandra, Anjaly M Varghese, Praveen K Uppala, Yakaiah Vangoori, Upendra R Uttaravelli, S. Venkata Saibaba, Butti Lavanya
      Pages: 395 - 400
      Abstract: Naga V Kandra, Anjaly M Varghese, Praveen K Uppala, Yakaiah Vangoori, Upendra R Uttaravelli, S. Venkata Saibaba, Butti Lavanya
      Egyptian Pharmaceutical Journal 2022 21(3):395-400
      Fixed drug eruption (FDE) is a distinct, delayed type-IV hypersensitivity manifesting as recurring cutaneous reaction (on skin or mucosa) in the same locations on re-exposure to the offending drug. This is most commonly due to oral medications, antimicrobials and NSAIDs being the most common culprits. Herein, we discuss six cases of bullous FDE due to diverse NSAIDs. The first case was Naproxen-induced bullous fixed drug eruption (BFDE), the second case was due to Etoricoxib, the third patient had Mefenamic acid-induced BFDE, the fourth was Ibuprofen-induced FDE, the fifth one was Diclofenac-induced BFDE, the sixth was Aceclofenac-induced BFDE, and the seventh was a case of paracetamol-induced BFDE. All these patients noticed skin reactions that were clinically diagnosed by the dermatologist as NSAID-induced BFDE. The mainstay of treatment adopted was to avoid the culprit drug. All the seven patients were treated with oral steroids, followed by antihistaminics for reducing FDE-associated pruritus, ointment soframycin, and topical steroids for hyperpigmented lesions. Prompt diagnosis of BFDE and drug withdrawal at the clinician side may help in rapid resolution of the reaction within days to delayed recovery within few weeks, thus preventing rise in morbidity and mortality.
      Citation: Egyptian Pharmaceutical Journal 2022 21(3):395-400
      PubDate: Wed,21 Sep 2022
      DOI: 10.4103/epj.epj_25_22
      Issue No: Vol. 21, No. 3 (2022)
       
 
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