首页 > 最新文献

Saudi Pharmaceutical Journal最新文献

英文 中文
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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

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.

使用 "一刀切 "模式生产药品的传统方法,由于无法生产出符合个人需求的定制药品,正成为制药商面临的一大问题。三维(3D)打印技术是一项全新的颠覆性技术,它彻底改变了药品的研发和生产方式,为制药业带来了诸多益处。三维打印技术可按需生产具有定制剂量、形状和释放特性的个性化药品。尽管缺乏明确的监管指导,但人们对在大规模药品生产中采用 3D 打印技术兴趣浓厚。本综述旨在评估中东和北非(MENA)地区的 3D 打印技术研究工作,尤其侧重于医药研发。我们的分析表明,3D 打印技术的整体研究活动激增,但在制药研发方面进展有限。虽然中东和北非地区仍然落后,但有证据表明,该地区对扩大 3D 打印技术在制药等不同领域的应用很感兴趣。在中东和北非地区,3D 打印技术为制药业的发展带来了巨大的希望,其发展需要学术研究人员和行业合作伙伴之间的紧密合作,同时监管机构也要起草详细的指导方针。
{"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":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

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. In-vitro 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.

本研究的目的是通过采用各种主动和被动负载方法,探索人血浆衍生外泌体作为多功能载体用于药物递送的潜力。研究人员采用差速离心和超滤方法从人血浆中分离出外泌体。采用超声和冻融方法实现了药物负载,从而促进了药物在外泌体中的有效包封和输送。对每种方法的有效性、装载效率和保持膜稳定性的能力进行了检验。使用粒度分析、透射电子显微镜和药物负载能力等多种技术对外泌体进行了表征,将甲氨蝶呤(MTX)这种弱酸性模型药物以 2.2 µM 的浓度载入外泌体。人血浆衍生外泌体的平均粒径为 162.15 ± 28.21 nm,zeta 电位为 -30.6 ± 0.71 mV。这些外泌体成功载入了 MTX,冻融法的药物包封率为 64.538 ± 1.54%,而超声法为 55.515 ± 1.907%。体外药物释放显示,冻融法在 72 小时内释放了 60% 的药物,与超声法在 72 小时内释放了 99% 的药物有显著差异(p 值为 0.0045)。此外,冻融法负载外泌体的细胞存活率明显高于超声法(p 值 0.0091),表明超声法存在膜破坏。总之,本研究为冻融法负载人血浆衍生外泌体提供了有价值的见解,表明这种载体具有改善药物负载和保持外泌体膜完整性的潜力。
{"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":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

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. The 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.

氧化应激累积是糖尿病神经病变(DN)的一个病理生理因素,会激活 TRPV-1。可可荚果皮中的白藜芦醇具有抗氧化活性,可能对糖尿病神经病变有益。本研究探讨了可可荚果壳乙醇提取物(EECPH)如何通过靶向 TRPV-1 影响小鼠的 DN。可可荚果皮是用 96% 的乙醇再曝气提取的。使用 DPPH 测量抗氧化活性。第 14 天,将小鼠随机分为七组:正常组、糖尿病组、加巴喷丁 100 毫克/千克体重组、二甲双胍 250 毫克/千克体重组和 EECPH 组(剂量为 250、500 和 750 毫克/千克体重组)。每天口服一次,连续治疗 14 天。第 7、14、21 和 28 天测量潜伏时间和血糖水平。第 29 天,小鼠被处死,并取出血液、胰腺和脊髓。检查丙二醛、胆固醇和血清谷草转氨酶/丙酮转氨酶(SGOT/PT)。使用苏木精和伊红染色法确定脊髓和胰腺的形态。TRPV-1的表达采用免疫组化法进行评估。750 毫克/千克体重的 EECPH 剂量对降低小鼠的痛觉减退、血糖、胆固醇和 SGOT/PT 的效果最好。该剂量还能通过改变 TRPV-1 的表达来改善胰腺和脊髓的组织学。由此可以得出结论,EECPH 可以降低 TRPV-1 在小鼠胰腺和脊髓中的表达。这种活性可减轻 DN 小鼠的痛觉减退。
{"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":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

Background

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.

Methods

Computational techniques such as structure-based virtual screening and molecular dyncamic simulation were employed to predict potential AG inhibitors from compounds of Oroxylum indicum. Finally, in silico results were validated by in vitro analysis using n-butanol fraction of crude methanol extracts.

Results

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 n-butanol fraction of the extract. The IC50 value for AG inhibition by n-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.

Conclusion

In summary, the study provides promising insights into the use of natural compounds derived from O. indicum 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.

背景据国际糖尿病联合会预测,到 2030 年,全球将有 5.78 亿人患有糖尿病,到 2045 年将达到 7 亿人。α-葡萄糖苷酶(AG)是抗击糖尿病的有望药物靶点之一,其抑制剂可通过减少复杂碳水化合物分解为单糖来控制糖尿病。本研究旨在从天然资源中鉴定和验证潜在的 AG 抑制剂,以防治糖尿病。方法采用基于结构的虚拟筛选和分子动力学模拟等计算技术,从 Oroxylum indicum 的化合物中预测潜在的 AG 抑制剂。最后,利用甲醇粗提取物的正丁醇馏分进行体外分析,验证硅学结果。结果OI_13、OI_66、OI_16、OI_44、OI_43、OI_20、OI_78和阿卡波糖的XP滑翔得分分别为-14.261、-13.475、-13.074、-13.045、-12.978、-12.659、-12.354和-12.296 kcal/mol。这些化合物与 AG 的结合亲和力极佳,超过了已知的 AG 抑制剂阿卡波糖。OI_13、OI_66和阿卡波糖的MM-GBSA dG结合能分别为-69.093、-62.950和-53.055 kcal/mol。命中率最高的大部分是苷类化合物,表明活性化合物存在于提取物的正丁醇馏分中。正丁醇馏分抑制 AG 的 IC50 值为 248.1 μg/ml,纯阿卡波糖的 IC50 值为 89.16 μg/ml。与阿卡波糖一样,前七种化合物的预测人体口服吸收率较低,这有利于这些化合物在小肠中作为抗糖尿病药物使用。然而,在临床使用之前,有必要开展进一步的研究,包括临床试验和药理学研究,以验证其有效性和安全性。
{"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":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

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 Paeonia tenuifolia L., Paeonia peregrina Mill., and Paeonia officinalis 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 P. officinalis, 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).

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 Pseudomonas aeruginosa and Salmonella 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 P. tenuifolia 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 Paeonia 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.

为了进一步了解各种萃取技术(浸渍、微波和超声辅助萃取)如何影响芍药(Paeonia tenuifolia L.)、芍药(Paeonia peregrina Mill.)和芍药(Paeonia officinalis L.)叶提取物的化学特征和生物活性,本研究进行了萃取。利用超高效液相色谱-线性阱质谱仪 OrbiTrap 仪器技术对提取物进行了有针对性的化学表征,并利用傅立叶变换红外光谱法研究了受检叶提取物的结构特性。乙醇提取物表现出中等程度的抗氧化活性,DPPH(2,2-二苯基-1-苦基肼)和磷钼测试对此进行了评估。通过超声波辅助萃取和浸渍(德利布拉托沙和 Bogovo gumno)产生的叶提取物的 MIC 值为 0.125 mg/mL,对绿脓杆菌和鼠伤寒沙门氏菌具有最佳抗菌活性。事实证明,超声辅助提取能产生最有效的抗菌剂。在酶抑制试验和分子对接模拟中评估了对葡萄糖苷酶、淀粉酶、胆碱酯酶和酪氨酸酶的抑制潜力。结果表明,通过超声辅助萃取法获得的 P. tenuifolia L. 叶子对乙酰胆碱酯酶和丁酰胆碱酯酶的抑制活性最高。也就是说,多酚结构的复杂性、萃取方法、使用地点以及叶提取物中的生物活性物质与其他成分(自由基、微生物和酶)之间的不同反应机制是影响抗氧化试验结果以及提取物的抗菌和酶抑制活性的主要因素。羟甲基-苯基戊糖基-己糖苷和乙酰基-羟苯基-己糖苷是首次在芍药叶提取物中发现。由于芍药叶提取物已被证实具有生物活性,并存在生物活性化合物,因此可用于食品、功能性食品和药品中。
{"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":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

Background

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.

Material and methods

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.

Results

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 (p = 0.003), as well as among Saudi pharmacists when compared to non-Saudi pharmacists (p = 0.002). Lack of relevant CE activities (p = 0.05), lack of quality activities (p = 0.002), lack of recognition (p = 0.013) and lack of internet access (p = 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.

Conclusion

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.

<
背景继续教育(CE)是药学专业人员的一项基本要求,以跟上实践中不断发展的知识和技能,并满足监管要求。本研究旨在评估影响沙特阿拉伯药剂师和药学技术人员对继续教育实践满意度的因素。调查问卷包括三个部分:参与者的人口统计学特征、过去一年中有关 CE 活动的数据和总体满意度,以及参与 CE 活动的障碍(14 个项目)和促进因素(12 个项目)的陈述(以 5 分制李克特量表(5 = 总是,1 = 从不)计分)。该调查通过沙特卫生专业委员会和沙特药学会(SPS)进行试点,然后在 2018 年 1 月至 2019 年 2 月期间以链接的形式分发。结果 398 名药剂师和 40 名药剂师的数据(完成率为 55%)。大部分参与者为执业药师,男性,在医院工作,有五年以上的执业经验。半数参与者来自中部地区,约三分之一为非沙特人。只有四分之一的参与者对沙特阿拉伯目前的行政长官实践表示满意/非常满意。工作限制(62.7%)、费用(55.9%)、继续教育活动时间安排(55.4%)、缺乏继续教育机会信息(53%)和职业倦怠(49.7%)是最大的障碍。与药剂师相比,药剂技术人员的不满意度较高(p = 0.003);与非沙特籍药剂师相比,沙特籍药剂师的不满意度也较高(p = 0.002)。与药剂师相比,缺乏相关的 CE 活动(p = 0.05)、缺乏高质量的活动(p = 0.002)、缺乏认可(p = 0.013)和缺乏互联网接入(p = 0.006)是药剂师面临的更大障碍。参与 CE 活动的最大促进因素是个人的学习愿望(78.4%)、保持专业执照的要求(73.8%)、学习带来的放松(58.5%)和交流机会(53.4%)。大多数参与者更倾向于参加会议或互动研讨会、半天或更短时间的短期职业教育,以及疾病管理/药物治疗主题。研究还强调了在设计继续教育项目时满足药剂师的偏好并使这些活动与药剂师的实践相一致的重要性。
{"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":"<div><h3>Background</h3><p>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.</p></div><div><h3>Material and methods</h3><p>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.</p></div><div><h3>Results</h3><p>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 (<em>p</em> = 0.003), as well as among Saudi pharmacists when compared to non-Saudi pharmacists (<em>p</em> = 0.002). Lack of relevant CE activities (<em>p</em> = 0.05), lack of quality activities (<em>p</em> = 0.002), lack of recognition (<em>p</em> = 0.013) and lack of internet access (<em>p</em> = 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.</p></div><div><h3>Conclusion</h3><p>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.</p><","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":null,"pages":null},"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 Q1 Pharmacology, Toxicology and Pharmaceutics 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

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 in vitro, demonstrating dose-dependent cytotoxicity against Ehrlich ascites carcinoma (EAC) cancer cells while sparing normal cells from compound 5, with an IC50 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 (C6H5SO2-) had synergistic effects on the bacteria and fungi that were examined. Molecular docking was performed against the Escherichia coli (6KZV) and Candida albicans (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.

碳水化合物类似物是一类重要的、成熟的临床实用药剂,具有强大的抗菌活性。因此,我们探索了甲基α-D-吡喃甘露糖苷(MαDM)类似物的各种治疗潜力,包括合成和评估其抗菌、抗真菌和抗癌特性的能力;此外,还进行了分子对接、分子动力学模拟和 ADMET 分析。通过光谱技术以及理化和元素分析,确定了合成的 MαDM 类似物的结构。体外抗菌活性评估显示了显著的抑制作用,尤其是对革兰氏阴性细菌的抑制作用,并预测了物质的活性谱(PASS)。同时,MαDM 类似物在抗真菌病原体方面表现出良好的效果,并在体外表现出良好的抗癌效果,对艾氏腹水癌(EAC)癌细胞表现出剂量依赖性细胞毒性,而化合物 5 则对正常细胞没有毒性,根据 MTT 比色法,IC50 为 4511.65 µg/mL。结构-活性关系(SAR)研究表明,己糖与癸酰基(C-10)和苯磺酰基(C6H5SO2-)酰基链结合在一起,对所研究的细菌和真菌具有协同作用。针对大肠杆菌(6KZV)和白色念珠菌(1EAG)的蛋白质进行了分子对接,以深入了解观察到的生物活性背后的分子相互作用。对接结果还得到了 100 ns 分子动力学模拟的进一步支持,这些模拟提供了 MαDM 及其靶标复合物稳定性和灵活性的动态视图。此外,还利用 ADMET 分析评估了毒理学和药代动力学特征。由于这些 MαDM 类似物具有良好的类药物特性,因此有望成为未来开发的候选治疗药物。
{"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":null,"pages":null},"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
Intra-peritoneal lavage of Zingiber officinale rhizome and its active constituent gingerol impede inflammation, angiogenesis, and fibrosis following post-operative peritoneal adhesion in male rats 雄性大鼠术后腹膜粘连后腹腔内灌洗姜科植物姜的根茎及其活性成分姜酚能抑制炎症、血管生成和纤维化
IF 4.1 3区 医学 Q1 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-30 DOI: 10.1016/j.jsps.2024.102092
Roghayeh Yahyazadeh , Vafa Baradaran Rahimi , Seyed Ahmad Mohajeri , Milad Iranshahy , Maede Hasanpour , Vahid Reza Askari

Post-operative peritoneal adhesions (PA) are a common and important clinical problem. In this study, we focused on the ameliorative efficacy of ginger and gingerol compounds on surgical-induced peritoneal adhesion, and their strategies that disrupted the PA formation pathways to suppress their incidence. First, liquid chromatography-mass spectrometry (LC-MS) was established to separate and identify several chemical groups of ginger rhizome extract. In the next steps, male Wistar albino rats were randomly selected and divided into various groups, namely sham, control, ginger extract (0.6, 1.8, 5 %w/v), and gingerol (0.05, 0.1, 0.3, and 1 %w/v). Finally, we investigated the macroscopic parameters such as wound healing, body weight as well as spleen height and weight. In addition, visual peritoneal adhesion assessment was performed via Nair et al and Adhesion Scoring Scheme. Moreover, the microscopic parameters and biological assessment was performed via and immunoassays. The present findings revealed significant improvement in wound healing and reduction of the adhesion range, as Nair et al. and Adhesion Scoring Scheme scoring, in both the ginger and gingerol groups compared to the PA group (P < 0.05). Whereas, gingerol (0.3 % w/v) was able to increase the body weight in rats (P < 0.0001) at end stage of experiment. Also, inflammation, angiogenesis, and fibrosis were significantly decreased due to the downregulation of interleukin (IL)-6, tumor necrosis factor (TNF)-α, transforming growth factor (TGF)-β1, vascular endothelial growth factor (VEGF), respectively, in the ginger and gingerol groups compared to the PA group (P < 0.05). In contrast, the levels of IL-10 were increased in the ginger and gingerol groups compared to the control group (P < 0.01). Our results proved that ginger rhizome and gingerol, as novel therapeutic compounds, could be used to prevent PA for their beneficial anti-inflammatory as well as anti-fibrosis properties in clinical trials. However, further clinical studies are required to approve the effectiveness of ginger and gingerol.

术后腹膜粘连(PA)是一个常见且重要的临床问题。在这项研究中,我们重点研究了生姜和姜酚化合物对手术引起的腹膜粘连的改善作用,以及它们破坏 PA 形成途径以抑制其发生的策略。首先,通过液相色谱-质谱联用技术(LC-MS)分离鉴定了生姜根茎提取物中的多个化学组。随后,随机选取雄性 Wistar 白化大鼠,将其分为假组、对照组、生姜提取物组(0.6%、1.8%、5%w/v)和姜酚组(0.05%、0.1%、0.3%、1%w/v)。最后,我们研究了伤口愈合、体重、脾脏高度和重量等宏观参数。此外,我们还通过 Nair 等人和粘附评分计划对腹膜粘附进行了目测评估。此外,还通过免疫测定进行了显微参数和生物评估。本研究结果显示,与 PA 组相比(P < 0.05),生姜组和姜酚组的伤口愈合情况均有明显改善,粘附范围也有所减少(Nair et al.而姜酚(0.3 % w/v)在实验结束阶段能够增加大鼠的体重(P < 0.0001)。此外,与 PA 组相比,生姜组和姜酚组的白细胞介素(IL)-6、肿瘤坏死因子(TNF)-α、转化生长因子(TGF)-β1、血管内皮生长因子(VEGF)分别下调,因此炎症、血管生成和纤维化明显减轻(P < 0.05)。相反,与对照组相比,生姜组和姜辣素组的 IL-10 水平升高(P < 0.01)。我们的研究结果证明,生姜根茎和姜辣素作为新型治疗化合物,具有抗炎和抗纤维化的功效,可用于临床试验预防 PA。然而,生姜和姜酚的有效性还需要进一步的临床研究来验证。
{"title":"Intra-peritoneal lavage of Zingiber officinale rhizome and its active constituent gingerol impede inflammation, angiogenesis, and fibrosis following post-operative peritoneal adhesion in male rats","authors":"Roghayeh Yahyazadeh ,&nbsp;Vafa Baradaran Rahimi ,&nbsp;Seyed Ahmad Mohajeri ,&nbsp;Milad Iranshahy ,&nbsp;Maede Hasanpour ,&nbsp;Vahid Reza Askari","doi":"10.1016/j.jsps.2024.102092","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102092","url":null,"abstract":"<div><p>Post-operative peritoneal adhesions (PA) are a common and important clinical problem. In this study, we focused on the ameliorative efficacy of ginger and gingerol compounds on surgical-induced peritoneal adhesion, and their strategies that disrupted the PA formation pathways to suppress their incidence. First, liquid chromatography-mass spectrometry (LC-MS) was established to separate and identify several chemical groups of ginger rhizome extract. In the next steps, male Wistar albino rats were randomly selected and divided into various groups, namely sham, control, ginger extract (0.6, 1.8, 5 %w/v), and gingerol (0.05, 0.1, 0.3, and 1 %w/v). Finally, we investigated the macroscopic parameters such as wound healing, body weight as well as spleen height and weight. In addition, visual peritoneal adhesion assessment was performed via Nair et al and Adhesion Scoring Scheme. Moreover, the microscopic parameters and biological assessment was performed via and immunoassays. The present findings revealed significant improvement in wound healing and reduction of the adhesion range, as Nair et al. and Adhesion Scoring Scheme scoring, in both the ginger and gingerol groups compared to the PA group (<em>P &lt; 0.05</em>). Whereas, gingerol (0.3 % w/v) was able to increase the body weight in rats (<em>P &lt; 0.0001</em>) at end stage of experiment. Also, inflammation, angiogenesis, and fibrosis were significantly decreased due to the downregulation of interleukin (IL)-6, tumor necrosis factor (TNF)-α, transforming growth factor (TGF)-β1, vascular endothelial growth factor (VEGF), respectively, in the ginger and gingerol groups compared to the PA group (<em>P &lt; 0.05</em>). In contrast, the levels of IL-10 were increased in the ginger and gingerol groups compared to the control group (<em>P &lt; 0.01</em>). Our results proved that ginger rhizome and gingerol, as novel therapeutic compounds, could be used to prevent PA for their beneficial anti-inflammatory as well as anti-fibrosis properties in clinical trials. However, further clinical studies are required to approve the effectiveness of ginger and gingerol.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001427/pdfft?md5=8c7c4914515ef9aaadd50d5df44af799&pid=1-s2.0-S1319016424001427-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140842752","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
Apixaban and clopidogrel in a fixed-dose combination: Formulation and in vitro evaluation 阿哌沙班和氯吡格雷的固定剂量复方制剂:配方和体外评估
IF 4.1 3区 医学 Q1 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-29 DOI: 10.1016/j.jsps.2024.102089
Ni'meh Al-Shami, Hani Naseef, Feras Kanaze

Fixed-dose combination (FDC) products represent a novel, safe, and cost-effective formulation. Combined use of anticoagulant and antiplatelet medications is common among comorbid cardiovascular patients. This study aimed to formulate FDC tablets for Apixaban and Clopidogrel, as prophylaxis and treatment of thrombo-embolic events. FDC tablets were developed by combining small tablets of Immediate-Release Clopidogrel 75 mg and Extend-Release Apixaban 5 mg through direct compression and wet granulation. Particularly, Apixaban tablets were developed using design expert software, and various types and concentrations of polymers were entered. For Clopidogrel tablets, various diluents were used to develop the formulation. Then, the dissolution profile for each formula was studied. Finally, the optimized formulations were encapsulated within hard gelatin capsules. Apixaban formulation followed zero-order with super case Ⅱ transport mechanism as the dominant mechanism of drug release. The Apixaban drug release rate was affected by the type and concentration of the polymers in the formulation (P < 0.05). As the HPMC concentration was increased, Apixaban release was retarded. For, Clopidogrel, the formulated tablets with spray-dried lactose filler and sodium stearyl fumarate lubricant were found to be stable with good properties. In conclusion, the optimum formulation yielded Clopidogrel and extended-release Apixaban for 24 h with the desired in vitro drug dissolution.

固定剂量复方制剂(FDC)产品是一种新型、安全且具有成本效益的制剂。在合并心血管疾病的患者中,联合使用抗凝药物和抗血小板药物很常见。本研究旨在配制阿哌沙班和氯吡格雷的 FDC 片剂,作为血栓栓塞事件的预防和治疗药物。通过直接压片和湿法制粒,将75毫克速释氯吡格雷和5毫克缓释阿哌沙班的小片组合在一起,开发出了FDC片剂。其中,阿哌沙班片剂的开发使用了设计专家软件,并输入了不同类型和浓度的聚合物。至于氯吡格雷片剂,则使用了各种稀释剂来开发制剂。然后,研究了每个配方的溶出曲线。最后,将优化配方封装在硬明胶胶囊中。阿哌沙班制剂的药物释放机制为零阶超Ⅱ型转运机制。阿哌沙班的药物释放率受制剂中聚合物类型和浓度的影响(P < 0.05)。随着 HPMC 浓度的增加,阿哌沙班的释放速度减慢。至于氯吡格雷,使用喷雾干燥乳糖填充剂和硬脂富马酸钠润滑剂配制的片剂性能稳定。总之,最佳配方可使氯吡格雷和阿哌沙班缓释片在 24 小时内达到理想的体外药物溶出度。
{"title":"Apixaban and clopidogrel in a fixed-dose combination: Formulation and in vitro evaluation","authors":"Ni'meh Al-Shami,&nbsp;Hani Naseef,&nbsp;Feras Kanaze","doi":"10.1016/j.jsps.2024.102089","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102089","url":null,"abstract":"<div><p>Fixed-dose combination (FDC) products represent a novel, safe, and cost-effective formulation. Combined use of anticoagulant and antiplatelet medications is common among comorbid cardiovascular patients. This study aimed to formulate FDC tablets for Apixaban and Clopidogrel, as prophylaxis and treatment of thrombo-embolic events. FDC tablets were developed by combining small tablets of Immediate-Release Clopidogrel 75 mg and Extend-Release Apixaban 5 mg through direct compression and wet granulation. Particularly, Apixaban tablets were developed using design expert software, and various types and concentrations of polymers were entered. For Clopidogrel tablets, various diluents were used to develop the formulation. Then, the dissolution profile for each formula was studied. Finally, the optimized formulations were encapsulated within hard gelatin capsules. Apixaban formulation followed zero-order with super case Ⅱ transport mechanism as the dominant mechanism of drug release. The Apixaban drug release rate was affected by the type and concentration of the polymers in the formulation (P &lt; 0.05). As the HPMC concentration was increased, Apixaban release was retarded. For, Clopidogrel, the formulated tablets with spray-dried lactose filler and sodium stearyl fumarate lubricant were found to be stable with good properties. In conclusion, the optimum formulation yielded Clopidogrel and extended-release Apixaban for 24 h with the desired in vitro drug dissolution.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001397/pdfft?md5=f7860717baadd2805582ea1da96ed824&pid=1-s2.0-S1319016424001397-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140816148","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
Patient Satisfaction with Private Community Pharmacies versus Pharmacies in Primary Health Care Centers in Saudi Arabia 沙特阿拉伯私立社区药房与初级保健中心药房的患者满意度比较
IF 4.1 3区 医学 Q1 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-04-29 DOI: 10.1016/j.jsps.2024.102091
Ali M. Alzahrani , Abdulrhman A. Alzhrani , Holly C. Felix , Khulud K. Alharbi , Muhammad Waseem Shahzad , Turky J. Arbaein , Sarah S. Monshi

Introduction

Saudi Arabia has begun reforming its government-run health care system to increase efficiency and reduce costs. One effort is the adoption of an electronic prescribing system (Wasfaty) and outsourcing pharmaceutical services from government-run clinics to community pharmacies (CP). This study aims to compare satisfaction with pharmaceutical services offered in the two systems.

Materials and methods

This cross-sectional observational study used existing survey data collected from patients (≥15 years of age) visiting government primary health care centers from January 2022 to June 2022. Satisfaction with three pharmaceutical services (availability of medications, pharmacist’s explanation of the prescription, and waiting time to get medications) were the main outcomes.

Results

The study comprised 91,317 participants, 74.06 % of them were CP/Wasfaty users. CP/Wasfaty patients had lower odds of satisfaction with the three pharmaceutical services: availability of medications (OR = 0.49, 95 % CI = 0.47–0.51), pharmacists’ explanation of prescription (OR = 0.55, 95 % CI = 0.53–0.58), and waiting time to get medications (OR = 0.81, 95 % CI = 0.75–0.88). Additional findings showed variations in satisfaction levels based on demographic factors and clinic types.

Conclusions

The significant differences observed in satisfaction levels based on demographic characteristics and type of clinics visited emphasize the importance of tailoring pharmaceutical services to meet the specific needs and expectations of different patient populations.

导言沙特阿拉伯已开始改革其政府运营的医疗保健系统,以提高效率和降低成本。其中一项措施是采用电子处方系统(Wasfaty),并将政府开办的诊所的药品服务外包给社区药房(CP)。这项横断面观察性研究使用了现有的调查数据,这些数据来自 2022 年 1 月至 2022 年 6 月在政府初级卫生保健中心就诊的患者(年龄≥15 岁)。研究的主要结果是对三项医药服务(药品供应、药剂师对处方的解释和取药等待时间)的满意度。 结果研究共有 91,317 名参与者,其中 74.06% 为 CP/Wasfaty 使用者。CP/Wasfaty患者对以下三项医药服务的满意度较低:药品供应(OR = 0.49,95 % CI = 0.47-0.51)、药剂师对处方的解释(OR = 0.55,95 % CI = 0.53-0.58)和取药等待时间(OR = 0.81,95 % CI = 0.75-0.88)。结论 根据人口统计学特征和就诊诊所类型观察到的满意度的显著差异强调了定制医药服务以满足不同患者群体的特定需求和期望的重要性。
{"title":"Patient Satisfaction with Private Community Pharmacies versus Pharmacies in Primary Health Care Centers in Saudi Arabia","authors":"Ali M. Alzahrani ,&nbsp;Abdulrhman A. Alzhrani ,&nbsp;Holly C. Felix ,&nbsp;Khulud K. Alharbi ,&nbsp;Muhammad Waseem Shahzad ,&nbsp;Turky J. Arbaein ,&nbsp;Sarah S. Monshi","doi":"10.1016/j.jsps.2024.102091","DOIUrl":"https://doi.org/10.1016/j.jsps.2024.102091","url":null,"abstract":"<div><h3>Introduction</h3><p>Saudi Arabia has begun reforming its government-run health care system to increase efficiency and reduce costs. One effort is the adoption of an electronic prescribing system (Wasfaty) and outsourcing pharmaceutical services from government-run clinics to community pharmacies (CP). This study aims to compare satisfaction with pharmaceutical services offered in the two systems.</p></div><div><h3>Materials and methods</h3><p>This cross-sectional observational study used existing survey data collected from patients (≥15 years of age) visiting government primary health care centers from January 2022 to June 2022. Satisfaction with three pharmaceutical services (availability of medications, pharmacist’s explanation of the prescription, and waiting time to get medications) were the main outcomes.</p></div><div><h3>Results</h3><p>The study comprised 91,317 participants, 74.06 % of them were CP/Wasfaty users. CP/Wasfaty patients had lower odds of satisfaction with the three pharmaceutical services: availability of medications (OR = 0.49, 95 % CI = 0.47–0.51), pharmacists’ explanation of prescription (OR = 0.55, 95 % CI = 0.53–0.58), and waiting time to get medications (OR = 0.81, 95 % CI = 0.75–0.88). Additional findings showed variations in satisfaction levels based on demographic factors and clinic types.</p></div><div><h3>Conclusions</h3><p>The significant differences observed in satisfaction levels based on demographic characteristics and type of clinics visited emphasize the importance of tailoring pharmaceutical services to meet the specific needs and expectations of different patient populations.</p></div>","PeriodicalId":49257,"journal":{"name":"Saudi Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":4.1,"publicationDate":"2024-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S1319016424001415/pdfft?md5=d0dd46c1c0a93f4f5776820e3431f3a8&pid=1-s2.0-S1319016424001415-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140901089","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
期刊
Saudi Pharmaceutical Journal
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1