Journal of Advanced Pharmacy Research最新文献

{"title":"Pyrimidines as Anticancer and Antiviral: Synthesis & Reactions (A Review)","authors":"S. Fatahala, M. Mohamed, M. Khodair, Rania H. Abd El-hameed","doi":"10.21608/aprh.2022.144745.1180","DOIUrl":"https://doi.org/10.21608/aprh.2022.144745.1180","url":null,"abstract":"Background: The interest of many medicinal and organic chemists has been attracted to the synthesis of pyrimidines and their analogues due to their highly biological and medicinal properties. Objectives& Methodology: Based on these activities, this review discusses the various recent methods for the synthesis of these heterocyclic compounds during the period of 2017 to 2021 with certain two main medicinal actions. Conclusion: Pyrimidine moiety bearing compounds, are synthesized, and reacted either through one-pot synthesis or multi-step synthesis pathways, in catalytic and solvent free condition or using catalysts and solvent.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74694140","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phenylimidazoles Scaffolds as Potent Anticancer Agents (Part I)","authors":"A. Hassan, M. Sarg, A. Bayoumi, Fatma Abdul Rahman","doi":"10.21608/aprh.2022.145308.1183","DOIUrl":"https://doi.org/10.21608/aprh.2022.145308.1183","url":null,"abstract":"Objective: Novel anticancer agents were designed to be synthesized comprising the essential features for anticancer activity considering Leucettamine B as a lead compound. Method: 3-Phenyl-2-thioxoimidazolidin-4-one 1 has been utilized for synthesis of various fused pyrrolo[1,2-e]imidazole 4, 8a,b, 11, 14, 16, 18, 20, 21, 23, 25 analogues through different chemical reactions. Results : Structures of these compounds were confirmed by spectral and elemental analyses Thirteen of the newly synthesized compounds were selected by the NCI – Maryland-U.S.A. and were tested for their anticancer activity in an initial single high dose in the full NCI 60 cell line panel. Conclusion: 5-amino-2,3,7,7a-tetrahydro-7-(4-methoxyphenyl)-1-oxo-2-phenyl-3-thioxo-1H-pyrrolo[1,2-e]imidazole-6-carbonitrile; 4 , 1-(7-(4-chlorophenyl)-3,7-dihydro-1,5-dihydroxy-2-phenyl-3-thioxo-2H-pyrrolo[1,2-e]imidazol-6yl) ethenone; 21 , were found to possess very selective potent anticancer activity against certain cancer cell lines.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79198593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Insight into the Pathophysiology of Myocardial Infarction","authors":"Basant Al-Botaty, Abeer El-Khoely, Elsayed Elsayed, A. Eissa","doi":"10.21608/aprh.2022.155725.1188","DOIUrl":"https://doi.org/10.21608/aprh.2022.155725.1188","url":null,"abstract":"as a of non-atherosclerotic Consequent effects of ischemia are primarily due to which is the main precursor of cell death. Myocardial cell death is triggered through intrinsic or extrinsic pathways. In both pathways, apoptosis has been clearly explained through different studies but recently, necroptosis was determined to be involved. The heart has negligible ability for regeneration, thus infarcted regions are by replacing dead cells with scar formation. Infarct healing is triggered through an inflammatory cascade, induced by alarmins released from dying cells. Clearance of dead cells by immune cells is followed with the activation of fibroblasts to promote deposition of extracellular matrix proteins. This discusses the events involved following ischemia including the mechanistic signalling during injury, inflammation, and repair of the infarcted heart. Moreover, the possible complications are mentioned along with the established treatment strategies and some new therapeutic approaches for myocardial infarction.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78701102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads","authors":"Aliaa Ismail, Eman M. Raafat, W. Sakran","doi":"10.21608/aprh.2022.158576.1189","DOIUrl":"https://doi.org/10.21608/aprh.2022.158576.1189","url":null,"abstract":"Objectives: A gastroretentive drug delivery system is one of many oral drug delivery systems developed to improve drug bioavailability and control drug release. It allows prolongation of drug gastric residence period for several hours. Verapamil Hydrochloride (VerHCl) is a good candidate for gastro retention because it has narrow absorption window and short half life. The goal of this study was formulation and evaluation of optimized VerHCl loaded gastroretentive alginate beads for increasing drug bioavailability and decreasing its dosing frequency. Methods: VerHCl loaded alginate beads were prepared according to 2 3 full factorial design using ionotropic emulsion gelation method. The effect of three formulation variables; oil concentration (%w/v) (X 1 ), polymer concentration (%w/v) (X 2 ) and drug to polymer ratio (X 3 ) was investigated on mean diameter (Y 1 ), drug loading % (Y 2 ), entrapment efficiency (EE%) (Y 3 ), % drug released at 1 (Y 4 ), 5 (Y 5 ) and 8 hr (Y 6 ). The optimized formula was further assessed in terms of in vitro floating, in-vitro drug release, in vivo gastro retention in rats and flowability. Results : Design-Expert® numerical optimization revealed that optimum formulation levels for VerHCl loaded alginate gastroretentive beads were; oil concentration (X 1 ) = 17.2 %w/v, polymer concentration (X 2 ) = 4.34 %w/v and drug to polymer ratio=1.2. The optimized formula exhibited yield% (85.63± 2.65%), Drug loading% (13.60±0.89%), EE% (60.11± 2.52%), prolonged floatability with no initial lag time, sustained in vitro drug release over 8 hr, gastroretention in rats over 8 hr and good flowability. Conclusion: The optimized formula of VerHCl loaded alginate beads could be promising for retaining VerHCl in stomach for a prolonged time which could possibly be advantageous in terms of bioavailability and patient compliance.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"88 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76407889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Prevalence of Metallo-β-Lactamase-Producing Pseudomonas aeruginosa in Egypt: A Systematic Review and Meta-Analysis","authors":"Ahmed B Azzam, Heba Khaled, Marwan Hesham","doi":"10.21608/aprh.2022.142365.1177","DOIUrl":"https://doi.org/10.21608/aprh.2022.142365.1177","url":null,"abstract":"Background: Metallo- beta -lactamase (MBL)-producing Pseudomonas aeruginosa represents a serious hazard to humanity because of its high mortality rate, ability to hydrolyze all beta-lactam antibiotics, including carbapenem, and absence of a clinically approved inhibitor. There are several studies conducted in Egypt that report a heterogeneous incidence of MBL among Pseudomonas aeruginosa clinical isolates. Methods: We performed a systematic search in MEDLINE [PubMed], Scopus, Google scholar, and Web of Science. Out of 1882 records, 20 studies agreed with the inclusion and exclusion criteria and are included in our review. Results: Our investigation revealed a high incidence of MBL-producing Pseudomonas aeruginosa of about 33.7% (95% CI: 19.3-48) and MBL-mediated Imipenem resistance among P. aeruginosa of about 74.1% (95% CI: 63.5-84.6). Furthermore, based on the included studies and other molecular studies conducted in Egypt, among MBL-encoding genes, bla VIM appeared to be the most prevalent MBL gene in clinically isolated Pseudomonas aeruginosa in Egypt. Conclusion: This high disseminating rate raises the alarm to support both antimicrobial stewardship activities and infection control programs to prevent further increases.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"118 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73901198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel therapeutic approaches of Sildenafil against rhabdomyolysis-associated acute kidney injury","authors":"Ghada S. El-Tanbouly, Rania M Khalil","doi":"10.21608/aprh.2022.136558.1174","DOIUrl":"https://doi.org/10.21608/aprh.2022.136558.1174","url":null,"abstract":"","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"518 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77178586","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigation and Physicochemical Characterization of Binary Febuxostat- Sulfobutyl Ether β -Cyclodextrin Inclusion Complexes","authors":"W. Sakran, Rania Safa, Mai Abdel-Hakim, Mohamed Salah","doi":"10.21608/aprh.2022.144204.1178","DOIUrl":"https://doi.org/10.21608/aprh.2022.144204.1178","url":null,"abstract":"","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"4021 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86710933","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phytochemical and Pharmacological Values of Two Major Constituents of Asparagus Species and their Nano formulations: A Review","authors":"Yasmin Sobhy, M. Mady, S. Mina, Y. Abo-Zeid","doi":"10.21608/aprh.2022.141715.1176","DOIUrl":"https://doi.org/10.21608/aprh.2022.141715.1176","url":null,"abstract":"","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"9 33","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91508043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Silico Studies of Bioactive Compounds Selected from Four African Plants with Inhibitory Activity Against Plasmodium falciparum Dihydrofolate Reductase-Thymidylate Synthase (pfDHFR-TS)","authors":"Ishola Akinwumi, A. Faleti, Adefolarin Owojuyigbe, Faridat Raji, Michael Alaka","doi":"10.21608/aprh.2022.139794.1175","DOIUrl":"https://doi.org/10.21608/aprh.2022.139794.1175","url":null,"abstract":"Objective: This present study aims to assess in silico inhibitory potentials of bioactive compounds present in Vernonia amygdalina (Bitter leaf), Cymbopogon citratus (Lemongrass), Azadirachta indica (Neem leaf), and Carica papaya (Pawpaw leaf) against Plasmodium falciparum Dihydrofolate reductase-thymidylate synthase ( pf DHFR-TS) via binding at their active sites. Methods : In silico methods were used in this study. Twenty (20) bioactive compounds were selected from Vernonia amygdalina , Cymbopogon citratus , Azadirachta indica , and Carica papaya. Artemether and Lumefantrine were used as the control drugs. The PubChem identification number (PID), the 3D structure in structure data format (SDF), and the canonical SMILES of the bioactive compounds and the control drugs were obtained using the PubChem online server. The crystal structure of pf DHFR-TS was retrieved from the protein data bank. Drug-likeness of the selected bioactive compounds was assessed using the SwissADME online server. The successful compounds were docked into the protein's active site using AutoDock Vina docking software. The docked complexes were analyzed using proteins plus and protein-ligand interaction profiler web server. The bioactivity of the ligands was determined using the Molinspiration online server. ADMETlab online tool was used to determine the ligands' absorption, distribution, metabolism, excretion, and toxicity (ADMET) characteristics. Results: The drug-likeness screening indicated that eleven (11) out of the twenty bioactive compounds violated two or more of the five rules (Lipinski's, Ghose's, Veber's, Egan's, and Muegge's rules). The control drug Artemether didn't violate any rule, while Lumefantrine violated four out of the five rules. The molecular docking revealed that Nimbolide, Vernomygdin, Luteolin, and Emetine from Azadirachta indica (Neem leaf), Vernonia amygdalina (Bitter leaf), and Carica papaya (Pawpaw leaf) have binding energies of -10.1 kcal/mol, -9.2 kcal/mol, -8.6 kcal/mol, and -9.2 kcal/mol respectively, which are better than the binding energies of Artemether and Lumefantrine (-8.2 kcal/mol, and -7.6 kcal/mol). Thus, these bioactive compounds' binding energies indicate the binding affinity with pf DHFR-TS protein, suggesting that four ligands, Nimbolide, Vernomygdin, Luteolin, and Emetine, also showed excellent ADMET properties. Conclusion: Conclusively, the in silico analysis proposes that Nimbolide, Vernomygdin, Luteolin, and Emetine from Azadirachta indica (Neem leaf), Vernonia amygdalina (Bitter leaf), and Carica papaya (Pawpaw leaf) prove to be probable antimalarial drugs, and show better docking with the target protein compared to Artemether and Lumefantrine. To validate this study, an in-vitro and in vivo study is recommended to further this study for validation of the hit compounds, as in silico methods only predict the activity of these bioactive compounds.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89845535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of Formulation Variables and Bile Salts Addition on Entrapment Efficiency of Curcumin Loaded Niosomes","authors":"F. Hashim, Dalia G Elkhateeb, Marwa F. Ali, R. Abdel-Rashid","doi":"10.21608/aprh.2022.133710.1172","DOIUrl":"https://doi.org/10.21608/aprh.2022.133710.1172","url":null,"abstract":"","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86873914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}