Saudi Pharmaceutical Journal最新文献

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Preparing a novel baicalin-loaded microemulsion-based gel for transdermal delivery and testing its anti-gout effect 制备新型黄芩苷微乳液透皮给药凝胶并测试其抗痛风效果
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-14 DOI: 10.1016/j.jsps.2024.102100
Yingzhou Wang , Mingxue Liu , Junjie Li , Peipei Jiang , Di Han , Hongling Zhang , Lingyun Xu , Yinsheng Qiu
{"title":"Preparing a novel baicalin-loaded microemulsion-based gel for transdermal delivery and testing its anti-gout effect","authors":"Yingzhou Wang ,&nbsp;Mingxue Liu ,&nbsp;Junjie Li ,&nbsp;Peipei Jiang ,&nbsp;Di Han ,&nbsp;Hongling Zhang ,&nbsp;Lingyun Xu ,&nbsp;Yinsheng Qiu","doi":"10.1016/j.jsps.2024.102100","DOIUrl":"10.1016/j.jsps.2024.102100","url":null,"abstract":"<div><p>We previously demonstrated that baicalin had efficacy against gouty arthritis (GA) by oral administration. In this paper, a novel baicalin-loaded microemulsion-based gel (B-MEG) was prepared and assessed for the transdermal delivery of baicalin against GA. The preparation method and transdermal capability of B-MEG was screened and optimized using the central composite design, Franz diffusion cell experiments, and the split-split plot design. Skin irritation tests were performed in guinea pigs. The anti-gout effects were evaluated using mice. The optimized B-MEG comprised of 50 % pH 7.4 phosphate buffered saline, 4.48 % ethyl oleate, 31.64 % tween 80, 13.88 % glycerin, 2 % borneol, 0.5 % clove oil and 0.5 % xanthan gum, with a baicalin content of (10.42 ± 0.08) mg/g and particle size of (15.71 ± 0.41) nm. After 12 h, the cumulative amount of baicalin permeated from B-MEG was (672.14 ± 44.11) μg·cm<sup>−2</sup>. No significant skin irritation was observed following B-MEG application. Compared to the model group, B-MEG groups significantly decreased the rate of auricular swelling (<em>P</em> &lt; 0.01) and number of twists observed in mice (<em>P</em> &lt; 0.01); and also reduced the rate of paw swelling (<em>P</em> &lt; 0.01) and inflammatory cell infiltration in a mouse model of GA. In conclusion, B-MEG represents a promising transdermal carrier for baicalin delivery and can be used as a potential therapy for GA.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102100"},"PeriodicalIF":4.1,"publicationDate":"2024-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001506/pdfft?md5=a6369a3ce9998124973d81376eeaf652&pid=1-s2.0-S1319016424001506-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141042788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Streptomyces isolate SOM013, a potential agent against microbial resistance and gastric ulcers 链霉菌分离物 SOM013--抗微生物耐药性和胃溃疡的潜在药物
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-13 DOI: 10.1016/j.jsps.2024.102101
Kizito Eneye Bello , Ahmad Adebayo Irekeola , Ahmad A. Alshehri
{"title":"Streptomyces isolate SOM013, a potential agent against microbial resistance and gastric ulcers","authors":"Kizito Eneye Bello ,&nbsp;Ahmad Adebayo Irekeola ,&nbsp;Ahmad A. Alshehri","doi":"10.1016/j.jsps.2024.102101","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102101","url":null,"abstract":"<div><p>The menace of microbial resistance and re-emerging disease is still a problem for healthcare givers globally, and the need for newer sources of potent antibiotics has become paramount. This study investigated the antimicrobial and antiulcer activities of Streptomyces isolate SOM013. Streptomyces isolates were cultivated and purified following standard microbiological protocols. Secondary metabolites were recovered and characterized from Streptomyces isolate SOM013 via broth fermentation and extraction. Varying concentrations (0.5 mg/mL, 0.025 mg/mL and 0.0125 mg/mL) of the SOM013 extract were used for antimicrobial screening against resistant bacteria and medically important fungi (methicillin-resistant <em>Escherichia coli</em>, Oxacillin resistant <em>Helicobacter pylori</em>, <em>Shigella spp</em>, extended broad-spectrum resistant <em>Pseudomonas aeruginosa</em>, <em>Streptococcus spp, Campylobacter spp, Candida albicans, Aspergillus niger,</em> and <em>Aspergillus flavus</em>). The antiulcer activity of the SOM013 was also examined in a methanol-induced gastric ulcer animal model. A total of 23 Streptomyces spp were recovered from the study. Methanolic extract of the SOM013 isolates was more potent across the clinical test microorganisms compared to water extract. The antimicrobial activity was dose dependent, with methanolic extract at 0.05 g/mL displaying the highest zone of inhibition (18.8 ± 0.3 mm) when tested against extended broad-spectrum resistant <em>Pseudomonas aeruginosa</em>. Further, the extract's ulcer index and protection efficacy were significant as the concentration increased (P &lt; 0.01). SOM013 isolate has a moderate antimicrobial and high antiulcer activity worthy of pharmacological exploration.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102101"},"PeriodicalIF":4.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001518/pdfft?md5=12163f73e28a396205e3ccf7f54cdb00&pid=1-s2.0-S1319016424001518-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140952260","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The concomitant use of ultra short beta-blockers with vasopressors and inotropes in critically ill patients with septic shock: A systematic review and meta-analysis of randomized controlled trials 在脓毒性休克重症患者中同时使用β受体阻滞剂和血管加压/肌注药物:系统综述和荟萃分析
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-11 DOI: 10.1016/j.jsps.2024.102094
Khalid Al Sulaiman , Hadeel A. Alkofide , Mashael E. AlFaifi , Sarah S. Aljohani , Abdullah F. Al Harthi , Rahaf A. Alqahtani , Ashwaq M. Alanazi , Lama H. Nazer , Abdulrahman I. Al Shaya , Ohoud Aljuhani
{"title":"The concomitant use of ultra short beta-blockers with vasopressors and inotropes in critically ill patients with septic shock: A systematic review and meta-analysis of randomized controlled trials","authors":"Khalid Al Sulaiman ,&nbsp;Hadeel A. Alkofide ,&nbsp;Mashael E. AlFaifi ,&nbsp;Sarah S. Aljohani ,&nbsp;Abdullah F. Al Harthi ,&nbsp;Rahaf A. Alqahtani ,&nbsp;Ashwaq M. Alanazi ,&nbsp;Lama H. Nazer ,&nbsp;Abdulrahman I. Al Shaya ,&nbsp;Ohoud Aljuhani","doi":"10.1016/j.jsps.2024.102094","DOIUrl":"10.1016/j.jsps.2024.102094","url":null,"abstract":"<div><h3>Background</h3><p>Septic shock is associated with systemic inflammatory response, hemodynamic instability, impaired sympathetic control, and the development of multiorgan dysfunction that requires vasopressor or inotropic support. The regulation of immune function in sepsis is complex and varies over time. However, activating Beta-2 receptors and blocking Beta-1 receptors reduces the proinflammatory response by influencing cytokine production. Evidence that supports the concomitant use of ultra short beta-blockers with inotropes and vasopressors in patients with septic shock is still limited. This study aimed to evaluate the use of ultra short beta-blockers and its impact on the ICU related outcomes such as mortality, length of stay, heart rate control, shock resolution, and vasopressors/inotropes requirements.</p></div><div><h3>Methods</h3><p>A systematic review and meta-analysis of randomized controlled trials including critically ill patients with septic shock who received inotropes and vasopressors. Patients who received either epinephrine or norepinephrine without beta-blockers “control group” were compared to patients who received ultra short beta-blockers concomitantly with either epinephrine or norepinephrine “Intervention group”. MEDLINE and Embase databases were utilized to systematically search for studies investigating the use of ultra short beta-blockers in critically ill patients on either epinephrine or norepinephrine from inception to October 10, 2023. The primary outcome was the 28-day mortality. While, length of stay, heart rate control, and inotropes/ vasopressors requirements were considered secondary outcomes.</p></div><div><h3>Results</h3><p>Among 47 potentially relevant studies, nine were included in the analysis. The 28-day mortality risk was lower in patients with septic shock who used ultra short beta-blockers concomitantly with either epinephrine or norepinephrine compared with the control group (RR (95%CI): 0.69 (0.53, 0.89),<!--> <em>I</em>2=26%;<em> <!-->P</em>=0.24). In addition, heart rate was statistically significantly lower with a standardized mean difference (SMD) of -22.39 (95% CI: -24.71, –20.06) among the beta-blockers group than the control group. The SMD for hospital length of stay and the inotropes requirement were not statistically different between the two groups (SMD (95%CI): -0.57 (-2.77, 1.64), and SMD (95%CI): 0.08 (-0.02, 0.19), respectively).</p></div><div><h3>Conclusion</h3><p>The use of ultra short beta-blockers concomitantly with either epinephrine or norepinephrine in critically ill patients with septic shock was associated with better heart rate control and survival benefits without increment in the inotropes and vasopressors requirement.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102094"},"PeriodicalIF":4.1,"publicationDate":"2024-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001440/pdfft?md5=6a714149a42972bd56eb64361902c5c4&pid=1-s2.0-S1319016424001440-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141038882","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Trend of pharmaceuticals 3D printing in the Middle East and North Africa (MENA) region: An overview, regulatory perspective and future outlook 中东和北非 (MENA) 地区的制药 3D 打印趋势:概述、监管视角和未来展望
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-10 DOI: 10.1016/j.jsps.2024.102098
Riyad F. Alzhrani , Mohammed Y. Alyahya , Mohammed S. Algahtani , Rawan A. Fitaihi , Essam A. Tawfik
{"title":"Trend of pharmaceuticals 3D printing in the Middle East and North Africa (MENA) region: An overview, regulatory perspective and future outlook","authors":"Riyad F. Alzhrani ,&nbsp;Mohammed Y. Alyahya ,&nbsp;Mohammed S. Algahtani ,&nbsp;Rawan A. Fitaihi ,&nbsp;Essam A. Tawfik","doi":"10.1016/j.jsps.2024.102098","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102098","url":null,"abstract":"<div><p>The traditional method of producing medicine using the “one-size fits all” model is becoming a major issue for pharmaceutical manufacturers due to its inability to produce customizable medicines for individuals’ needs. Three-dimensional (3D) printing is a new disruptive technology that offers many benefits to the pharmaceutical industry by revolutionizing the way pharmaceuticals are developed and manufactured. 3D printing technology enables the on-demand production of personalized medicine with tailored dosage, shape and release characteristics. Despite the lack of clear regulatory guidance, there is substantial interest in adopting 3D printing technology in the large-scale manufacturing of medicine. This review aims to evaluate the research efforts of 3D printing technology in the Middle East and North Africa (MENA) region, with a particular emphasis on pharmaceutical research and development. Our analysis indicates an upsurge in the overall research activity of 3D printing technology but there is limited progress in pharmaceuticals research and development. While the MENA region still lags, there is evidence of the regional interest in expanding the 3D printing technology applications in different sectors including pharmaceuticals. 3D printing holds great promise for pharmaceutical development within the MENA region and its advancement will require a strong collaboration between academic researchers and industry partners in parallel with drafting detailed guidelines from regulatory authorities.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102098"},"PeriodicalIF":4.1,"publicationDate":"2024-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001488/pdfft?md5=b1d4fcf27739d26f5357d0e6cc5d7373&pid=1-s2.0-S1319016424001488-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140910473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Human plasma derived exosomes: Impact of active and passive drug loading approaches on drug delivery 人血浆外泌体:主动和被动载药方法对药物输送的影响
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-06 DOI: 10.1016/j.jsps.2024.102096
Rabia Gul , Hamid Bashir , Muhammad Sarfraz , Ahson Jabbar Shaikh , Yousef A. Bin Jardan , Zahid Hussain , Muhammad Hassham Hassan Bin Asad , Faisal Gulzar , Bo Guan , Imran Nazir , Muhammad Imran Amirzada
{"title":"Human plasma derived exosomes: Impact of active and passive drug loading approaches on drug delivery","authors":"Rabia Gul ,&nbsp;Hamid Bashir ,&nbsp;Muhammad Sarfraz ,&nbsp;Ahson Jabbar Shaikh ,&nbsp;Yousef A. Bin Jardan ,&nbsp;Zahid Hussain ,&nbsp;Muhammad Hassham Hassan Bin Asad ,&nbsp;Faisal Gulzar ,&nbsp;Bo Guan ,&nbsp;Imran Nazir ,&nbsp;Muhammad Imran Amirzada","doi":"10.1016/j.jsps.2024.102096","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102096","url":null,"abstract":"<div><p>The aim of the current study was to explore the potential of human plasma-derived exosomes as versatile carriers for drug delivery by employing various active and passive loading methods. Exosomes were isolated from human plasma using differential centrifugation and ultrafiltration method. Drug loading was achieved by employing sonication and freeze thaw methods, facilitating effective drug encapsulation within exosomes for delivery. Each approach was examined for its effectiveness, loading efficiency and ability to preserve membrane stability. Methotrexate (MTX), a weak acid model drug was loaded at a concentration of 2.2 µM to exosomes underwent characterization using various techniques such as particle size analysis, transmission electron microscopy and drug loading capacity. Human plasma derived exosomes showed a mean size of 162.15 ± 28.21 nm and zeta potential of −30.6 ± 0.71 mV. These exosomes were successfully loaded with MTX demonstrated a better drug encapsulation of 64.538 ± 1.54 % by freeze thaw method in comparison 55.515 ± 1.907 % by sonication. <em>In-vitro</em> drug release displayed 60 % loaded drug released within 72 h by freeze thaw method that was significantly different from that by sonication method i.e., 99 % within 72 h (p value 0.0045). Moreover, cell viability of exosomes loaded by freeze thaw method was significantly higher than that by sonication method (p value 0.0091) suggested that there was membrane disruption by sonication method. In conclusion, this study offers valuable insights into the potential of human plasma-derived exosomes loaded by freeze thaw method suggest as a promising carrier for improved drug loading and maintenance of exosomal membrane integrity.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102096"},"PeriodicalIF":4.1,"publicationDate":"2024-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001464/pdfft?md5=d135d79d069020d3bc15cea9d5615606&pid=1-s2.0-S1319016424001464-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140905354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The ethanol extract of cocoa pod husk minimizes hyperalgesia and blood glucose levels in diabetic neuropathy model through transient receptor protein vanilloid (TRPV)-1 可可荚果壳乙醇提取物通过瞬时受体蛋白香草素(TRPV)-1 降低糖尿病神经病变模型的痛觉减退和血糖水平
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-06 DOI: 10.1016/j.jsps.2024.102097
Fifteen Aprila Fajrin , Diana Holidah , Heni Nurhidayah , Putri Suci Wulansari , Didik Pudji Restanto , Lailatul Azkiyah , Yuli Witono , Ari Satia Nugraha
{"title":"The ethanol extract of cocoa pod husk minimizes hyperalgesia and blood glucose levels in diabetic neuropathy model through transient receptor protein vanilloid (TRPV)-1","authors":"Fifteen Aprila Fajrin ,&nbsp;Diana Holidah ,&nbsp;Heni Nurhidayah ,&nbsp;Putri Suci Wulansari ,&nbsp;Didik Pudji Restanto ,&nbsp;Lailatul Azkiyah ,&nbsp;Yuli Witono ,&nbsp;Ari Satia Nugraha","doi":"10.1016/j.jsps.2024.102097","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102097","url":null,"abstract":"<div><p>Oxidative stress accumulation becomes a pathophysiological factor in diabetic neuropathy (DN), activating TRPV-1. Resveratrol in cocoa pod husk exhibits antioxidant activity that could be beneficial in DN. This study examined how the ethanol extract of cocoa pod husk (EECPH) affects DN in mice by targeting TRPV-1. Cocoa pod husk was extracted using 96 % ethanol with remaceration. The antioxidant activity was measured using DPPH. Mice were induced using alloxan 210 mg/kg BW i.p. At day 14, mice were randomized into seven groups: normal, diabetic, gabapentin 100 mg/kg BW, metformin 250 mg/kg BW, and EECPH (doses 250, 500, and 750 mg/kg BW). Treatments were administered orally, once daily for 14 days. The latency time and blood glucose levels were measured on days 7, 14, 21, and 28. On day 29, mice were sacrificed, and the blood, pancreas, and spinal cord were removed. Malondialdehyde, cholesterol, and serum glutamic oxaloacetic/pyruvic transaminase (SGOT/PT) were examined. Morphology of the spinal cord and pancreas was determined using hematoxylin and eosin staining. The expression of TRPV-1 was assessed using immunohistochemistry. <strong>T</strong>he EECPH dose of 750 mg/kg BW showed the greatest effect in lowering hyperalgesia and blood glucose as well as cholesterol and SGOT/PT in mice. That dose also improved the histology of the pancreas and spinal cord by altering the expression of TRPV-1. It can be concluded that EECPH may lower the expression of TRPV-1 in the pancreas and spinal cord of mice. This activity was responsible of reducing hyperalgesia in DN mice.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102097"},"PeriodicalIF":4.1,"publicationDate":"2024-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001476/pdfft?md5=0cbac3ed15b712c5c99b12555667e1af&pid=1-s2.0-S1319016424001476-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140893940","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
α-Glucosidase inhibitory potential of Oroxylum indicum using molecular docking, molecular dynamics, and in vitro evaluation 利用分子对接、分子动力学和体外评估研究 Oroxylum indicum 的α-葡萄糖苷酶抑制潜力
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-03 DOI: 10.1016/j.jsps.2024.102095
Samhita Bhaumik , Alekhya Sarkar , Sudhan Debnath , Bimal Debnath , Rajat Ghosh , Magdi E.A. Zaki , Sami A. Al-Hussain
{"title":"α-Glucosidase inhibitory potential of Oroxylum indicum using molecular docking, molecular dynamics, and in vitro evaluation","authors":"Samhita Bhaumik ,&nbsp;Alekhya Sarkar ,&nbsp;Sudhan Debnath ,&nbsp;Bimal Debnath ,&nbsp;Rajat Ghosh ,&nbsp;Magdi E.A. Zaki ,&nbsp;Sami A. Al-Hussain","doi":"10.1016/j.jsps.2024.102095","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102095","url":null,"abstract":"<div><h3>Background</h3><p>According to the International Diabetes Federation, there will be 578 million individuals worldwide with diabetes by 2030 and 700 million by 2045. One of the promising drug targets to fight diabetes is α-glucosidase (AG), and its inhibitors may be used to manage diabetes by reducing the breakdown of complex carbohydrates into simple sugars. The study aims to identify and validate potential AG inhibitors in natural sources to combat diabetes.</p></div><div><h3>Methods</h3><p>Computational techniques such as structure-based virtual screening and molecular dyncamic simulation were employed to predict potential AG inhibitors from compounds of <em>Oroxylum indicum</em>. Finally, in silico results were validated by <em>in vitro</em> analysis using <em>n</em>-butanol fraction of crude methanol extracts.</p></div><div><h3>Results</h3><p>The XP glide scores of top seven hits OI_13, OI_66, OI_16, OI_44, OI_43, OI_20, OI_78 and acarbose were –14.261, –13.475, –13.074, –13.045, –12.978, –12.659, –12.354 and –12.296 kcal/mol, respectively. These hits demonstrated excellent binding affinity towards AG, surpassing the known AG inhibitor acarbose. The MM-GBSA dG binding energies of OI_13, OI_66, and acarbose were −69.093, −62.950, and −53.055 kcal/mol, respectively. Most of the top hits were glycosides, indicating that active compounds lie in the <em>n</em>-butanol fraction of the extract. The IC<sub>50</sub> value for AG inhibition by <em>n</em>-butanol fraction was 248.1 μg/ml, and for that of pure acarbose it was 89.16 μg/ml. The predicted oral absorption rate in humans for the top seven hits was low like acarbose, which favors the use of these compounds as anti-diabetes in the small intestine.</p></div><div><h3>Conclusion</h3><p>In summary, the study provides promising insights into the use of natural compounds derived from <em>O. indicum</em> as potential AG inhibitors to manage diabetes. However, further research, including clinical trials and pharmacological studies, would be necessary to validate their efficacy and safety before clinical use.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102095"},"PeriodicalIF":4.1,"publicationDate":"2024-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001452/pdfft?md5=5ad10387fcd25e2e345afed6e9c307e6&pid=1-s2.0-S1319016424001452-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140893941","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A novel source of biologically active compounds – The leaves of Serbian herbaceous peonies 生物活性化合物的新来源--塞尔维亚草本牡丹的叶子
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-03 DOI: 10.1016/j.jsps.2024.102090
Petar Batinić , Aleksandra Jovanović , Dejan Stojković , Natalija Čutović , Ilija Cvijetić , Uroš Gašić , Tamara Carević , Gökhan Zengin , Aleksandar Marinković , Tatjana Marković
{"title":"A novel source of biologically active compounds – The leaves of Serbian herbaceous peonies","authors":"Petar Batinić ,&nbsp;Aleksandra Jovanović ,&nbsp;Dejan Stojković ,&nbsp;Natalija Čutović ,&nbsp;Ilija Cvijetić ,&nbsp;Uroš Gašić ,&nbsp;Tamara Carević ,&nbsp;Gökhan Zengin ,&nbsp;Aleksandar Marinković ,&nbsp;Tatjana Marković","doi":"10.1016/j.jsps.2024.102090","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102090","url":null,"abstract":"<div><p>In order to gain further insight into how various extraction techniques (maceration, microwave-, and ultrasound-assisted extractions) affect the chemical profile and biological activities of leaf extracts from <em>Paeonia tenuifolia</em> L., <em>Paeonia peregrina</em> Mill., and <em>Paeonia officinalis</em> L., this research was performed. The targeted chemical characterization of the extracts was achieved using the Ultra-High-Performance-Liquid-Chromatography-Linear-Trap-Mass-Spectrometry OrbiTrap instrumental technique, while Fourier Transform Infrared Spectroscopy was conducted to investigate the structural properties of the examined leaf extracts. According to the results, the species <em>P. officinalis,</em> Božurna locality as the origin of the plant material, and microwave-assisted extraction produced the maximum polyphenol yield, (491.9 ± 2.7 mg gallic acid equivalent (GAE)/mL).</p><p>The ethanolic extracts exhibited moderate antioxidant activity as evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl) and phosphomolybdenum tests. With MIC values of 0.125 mg/mL, the leaf extracts produced by ultrasound-assisted extraction and maceration (Deliblato sands and Bogovo gumno) had the best antibacterial activity against <em>Pseudomonas aeruginosa</em> and <em>Salmonella</em> Typhimurium. Ultrasound-assisted extraction has proven to produce the most effective antimicrobial agents. Inhibitory potential towards glucosidase, amylase, cholinesterases, and tyrosinase was evaluated in enzyme inhibition assays and molecular docking simulations. Results show that leaves of <em>P. tenuifolia</em> L. obtained by ultrasound-assisted extraction had the highest acetylcholinesterase and butyrylcholinesterase inhibitory activity. Namely, the complexity of the polyphenol structures, the extraction method, the used locality, and the different mechanisms of the reactions between bioactives from leaf extracts and other components (free radicals, microorganisms, and enzymes) are the main factors that influence the results of the antioxidant tests, as well as the antibacterial and enzyme-inhibitory activities of the extracts. Hydroxymethyl-phenyl pentosyl-hexoside and acetyl-hydroxyphenyl-hexoside were the first time identified in the leaf extract of the <em>Paeonia</em> species. Due to their proven biological activities and the confirmed existence of bioactive compounds, leaf extracts may find use in foodstuffs, functional foods, and pharmaceutical products.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102090"},"PeriodicalIF":4.1,"publicationDate":"2024-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001403/pdfft?md5=efd482de6df188299636ef97f7cd8946&pid=1-s2.0-S1319016424001403-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140893942","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of factors affecting pharmacists and pharmacy technicians' satisfaction towards practicing CE activities in Saudi Arabia 评估影响沙特阿拉伯药剂师和药学技术人员对开展 CE 活动满意度的因素
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-05-01 DOI: 10.1016/j.jsps.2024.102083
Raniah Aljadeed , Rana Aljadeed , Wasmeah Alsamti , Hadeel Alharbi , Rand Alturki , Haya Almalag , Lobna Aljuffali , Jawza Alsabhan , Noha AlAloola , Hadeel Alkofide , Rihaf Alfaraj , Njoud Altuwaijri , Nora Alkhudair , Lamya Alnaim , Ghada Bawazeer
{"title":"Evaluation of factors affecting pharmacists and pharmacy technicians' satisfaction towards practicing CE activities in Saudi Arabia","authors":"Raniah Aljadeed ,&nbsp;Rana Aljadeed ,&nbsp;Wasmeah Alsamti ,&nbsp;Hadeel Alharbi ,&nbsp;Rand Alturki ,&nbsp;Haya Almalag ,&nbsp;Lobna Aljuffali ,&nbsp;Jawza Alsabhan ,&nbsp;Noha AlAloola ,&nbsp;Hadeel Alkofide ,&nbsp;Rihaf Alfaraj ,&nbsp;Njoud Altuwaijri ,&nbsp;Nora Alkhudair ,&nbsp;Lamya Alnaim ,&nbsp;Ghada Bawazeer","doi":"10.1016/j.jsps.2024.102083","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102083","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Background&lt;/h3&gt;&lt;p&gt;Continuing education (CE) is an essential requirement for pharmacy professionals to stay abreast with the evolving knowledge and skills of the practice and meet the regulatory mandate. The purpose of this research is to assess factors affecting the satisfaction of pharmacists and pharmacy technicians towards CE practices in Saudi Arabia.&lt;/p&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Material and methods&lt;/h3&gt;&lt;p&gt;A self-administered survey instrument was developed following an extensive literature search. The questionnaire consisted of three sections: participants’ demographics, data on CE activities over the past year and overall satisfaction, and statements of barriers (14 items) and facilitators (12 items) for participation in CE activities (scored on a 5-point Likert scale (5 = always, 1 = never)). The survey was piloted and then distributed as a link through the Saudi Commission for Health Specialties and Saudi Pharmaceutical Society (SPS) between Jan 2018 and Feb 2019.&lt;/p&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;p&gt;Data was available on 398 pharmacists and 40 pharmacy technicians (completion rate was 55 %). The majority were practitioners, male, working in a hospital setting and had more than five years of practice experience. Half of the participants were from the Central Region and about one-third were non-Saudi. Only a quarter of the participants were satisfied/very satisfied with the current CE practices in Saudi Arabia. Job constraints (62.7 %), cost (55.9 %), schedule of CE activities (55.4 %), lack of information on CE opportunities (53 %) and professional burnout (49.7 %) were the top barriers. There was a significant level of dissatisfaction among pharmacy technicians when compared to pharmacists (&lt;em&gt;p&lt;/em&gt; = 0.003), as well as among Saudi pharmacists when compared to non-Saudi pharmacists (&lt;em&gt;p&lt;/em&gt; = 0.002). Lack of relevant CE activities (&lt;em&gt;p&lt;/em&gt; = 0.05), lack of quality activities (&lt;em&gt;p&lt;/em&gt; = 0.002), lack of recognition (&lt;em&gt;p&lt;/em&gt; = 0.013) and lack of internet access (&lt;em&gt;p&lt;/em&gt; = 0.006) were significantly more barriers for pharmacy technicians compared to pharmacists. The most identified facilitators to engage in CE activities were a personal desire to learn (78.4 %), the requirement to maintain a professional license (73.8 %) and relaxation provided by learning (58.5 %) and networking opportunities (53.4 %). The majority of the participants preferred conferences or interactive workshops, short CE over half a day or less, and the topic of disease management/drug therapy.&lt;/p&gt;&lt;/div&gt;&lt;div&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;p&gt;The findings of the study highlight the need for a partnership strategy that includes various stakeholders to improve CE program quality and accessibility that supports and promotes the professional development of pharmacists and pharmacy technicians in Saudi Arabia. It also underscores the importance of meeting the preferences of pharmacy practitioners when designing CE programs and aligning such activities with their practices.&lt;/p&gt;&lt;","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102083"},"PeriodicalIF":4.1,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001336/pdfft?md5=6f37d36336cbec793e0391e29fe7dcf2&pid=1-s2.0-S1319016424001336-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140952205","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
In vitro antimicrobial, anticancer evaluation, and in silico studies of mannopyranoside analogs against bacterial and fungal proteins: Acylation leads to improved antimicrobial activity 针对细菌和真菌蛋白的甘露吡喃糖苷类似物的体外抗菌、抗癌评估和硅学研究:酰化可提高抗菌活性
IF 4.1 3区 医学
Saudi Pharmaceutical Journal Pub Date : 2024-04-30 DOI: 10.1016/j.jsps.2024.102093
Md. Ahad Hossain , Shahin Sultana , Mohammed M. Alanazi , Hanine Hadni , Ajmal R. Bhat , Imtiaj Hasan , Sarkar M.A. Kawsar
{"title":"In vitro antimicrobial, anticancer evaluation, and in silico studies of mannopyranoside analogs against bacterial and fungal proteins: Acylation leads to improved antimicrobial activity","authors":"Md. Ahad Hossain ,&nbsp;Shahin Sultana ,&nbsp;Mohammed M. Alanazi ,&nbsp;Hanine Hadni ,&nbsp;Ajmal R. Bhat ,&nbsp;Imtiaj Hasan ,&nbsp;Sarkar M.A. Kawsar","doi":"10.1016/j.jsps.2024.102093","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102093","url":null,"abstract":"<div><p>Carbohydrate analogs are an important, well-established class of clinically useful medicinal agents that exhibit potent antimicrobial activity. Thus, we explored the various therapeutic potential of methyl α-D-mannopyranoside (MαDM) analogs, including their ability to synthesize and assess their antibacterial, antifungal, and anticancer properties; additionally, molecular docking, molecular dynamics simulation, and ADMET analysis were performed. The structure of the synthesized MαDM analogs was ascertained by spectroscopic techniques and physicochemical and elemental analysis. In vitro antimicrobial activity was assessed and revealed significant inhibitory effects, particularly against gram-negative bacteria along with the prediction of activity spectra for substances (PASS). Concurrently, MαDM analogs showed good results against antifungal pathogens and exhibited promising anticancer effects <em>in vitro</em>, demonstrating dose-dependent cytotoxicity against Ehrlich ascites carcinoma (EAC) cancer cells while sparing normal cells from compound <strong>5</strong>, with an IC<sub>50</sub> of 4511.65 µg/mL according to the MTT colorimetric assay. A structure–activity relationship (SAR) study revealed that hexose combined with the acyl chains of decanoyl (C-10) and benzenesulfonyl (C<sub>6</sub>H<sub>5</sub>SO<sub>2</sub>-) had synergistic effects on the bacteria and fungi that were examined. Molecular docking was performed against the <em>Escherichia coli</em> (6KZV) and <em>Candida albicans</em> (1EAG) proteins to acquire insights into the molecular interactions underlying the observed biological activities. The docking results were further supported by 100 ns molecular dynamics simulations, which provided a dynamic view of the stability and flexibility of complexes involving MαDM and its targets. In addition, ADMET analysis was used to evaluate the toxicological and pharmacokinetic profiles. Owing to their promising drug-like properties, these MαDM analogs exhibit potential as prospective therapeutic candidates for future development.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":"32 6","pages":"Article 102093"},"PeriodicalIF":4.1,"publicationDate":"2024-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001439/pdfft?md5=180573288ac434629d1e5635cf6b8485&pid=1-s2.0-S1319016424001439-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140842855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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