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Comparative Analysis of Histamine in Fresh and Processed Fish Sold in Jordanian Market 约旦市场上销售的新鲜鱼和加工鱼中组胺的比较分析
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.35516/jjps.v17i1.1809
Alaa Sirhan, Yazan Alrashdan, Yousef Al-Ebini, L. Hassouneh, Tamara Ghrear, L. Abdulra’uf
Food poisoning from histamine, a biogenic amine formed due to the decarboxylation of histidine by bacteria in fish and fish products, has become a pivotal concern in food safety. This study measured the concentration of histamine in various fish products available in the Jordanian market, but manufactured in multiple countries, utilizing an Enzyme-Linked Immunosorbent Assay (ELISA). The ELISA kit and the protocol were provided by Veratox for histamine. Approximately 93.69% of the samples tested positive for the presence of histamine, with levels ranging between 0.317 and 230.41 mg/kg. Solely 0.9% of the samples exceeded the maximum permissible level established by the European Union (EU) and only 4.5% of the fish samples were free of histamine. The Principal Component Analysis (PCA) revealed that the type of fish was the most significant source of variability in histamine concentration, explaining 31.2% of the variability. Conversely, the sample weight accounted for the least variability (only 20.2%), implying that it has little or no effect on the concentration of histamine in the fish samples.
组胺是鱼类和鱼类产品中的组氨酸在细菌作用下脱羧而形成的一种生物胺,组胺引起的食物中毒已成为食品安全的一个重要问题。这项研究利用酶联免疫吸附测定法(ELISA)测定了约旦市场上销售的、由多个国家生产的各种鱼类产品中的组胺浓度。ELISA试剂盒和方案由Veratox公司提供。约 93.69% 的样本检测结果呈阳性,组胺含量在 0.317 至 230.41 mg/kg 之间。只有 0.9% 的样本超过了欧盟(EU)规定的最高允许含量,只有 4.5% 的鱼类样本不含组胺。主成分分析(PCA)显示,鱼的种类是造成组胺浓度变化的最主要原因,占31.2%。相反,样本重量的变化最小(仅占 20.2%),这意味着样本重量对鱼样本中组胺浓度的影响很小或没有影响。
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引用次数: 0
Optimizing Drug Delivery Vehicle with Multi-Criteria Decision Making (MCDM) - Based Excipient Selection 基于多标准决策(MCDM)的辅料选择优化给药载体
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.35516/jjps.v17i1.1692
I. Omoyayi, Süleyman Aşır, Abdullahi U. Ibrahim
Excipients are used in drug delivery systems as a means of effectively delivering drugs to their target site. Multi-criteria decision-making (MCDM) methods are tools for decision-making that consider multidimensional factors. Such methods are a comparative technology used in medicine that combines individual criteria into the total assessment of selected alternatives. This study aims to enhance the solubility and bioavailability of drugs through the application of MCDM-based excipient selection. By incorporating the Preference Ranking Organization Method for Enrichment Evaluations (PROMETHEE), various excipients can be evaluated and ranked based on their suitability for specific applications, considering parameters related to drug solubility and bioavailability. The results highlight the potential of cyclodextrins (net flow: 0.0023) and Eudragit polymers (net flow: 0.0016) as preferred options for drug carriers, while Poloxamer 188 (P188) (net flow: -0.0030) is identified as the least preferred option. This study demonstrates the effectiveness of the PROMETHEE method in improving the performance of poorly soluble and bioavailable drugs, ultimately contributing to the development of new drug delivery systems. The findings have significant implications for therapeutic outcomes in the treatment of diseases.
药物输送系统中使用的辅料是将药物有效输送到目标部位的一种手段。多标准决策(MCDM)方法是考虑多维因素的决策工具。这种方法是一种用于医药领域的比较技术,它将单个标准与对所选替代品的总体评估相结合。本研究旨在通过应用基于 MCDM 的辅料选择来提高药物的溶解度和生物利用度。通过采用 "富集评价偏好排序组织法"(PROMETHEE),可以根据各种辅料在特定应用中的适用性对其进行评估和排序,同时考虑与药物溶解度和生物利用度相关的参数。结果表明,环糊精(净流量:0.0023)和 Eudragit 聚合物(净流量:0.0016)具有作为药物载体首选的潜力,而 Poloxamer 188 (P188)(净流量:-0.0030)被认为是最不可取的选择。这项研究证明了 PROMETHEE 方法在改善溶解性差、生物利用度低的药物性能方面的有效性,最终有助于新型药物输送系统的开发。研究结果对治疗疾病的疗效具有重要意义。
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引用次数: 0
Evaluation of Anti-Inflammatory, Antioxidant Activities and Molecular Docking Analysis of Rubus idaeus Leaf Extract 茜草叶提取物的抗炎、抗氧化活性评估和分子对接分析
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.35516/jjps.v17i1.1808
O. Maslov, M. Komisarenko, S. Kolisnyk, Lyudmyla Derymedvid
The study aimed to identify the most abundant compounds in raspberry leaf extract via HPLC analysis, conduct theoretical and practical assessments of antioxidant and anti-inflammatory activities both in silico, in vitro, and in vivo, and evaluate the correlation between antioxidant and anti-inflammatory activities. Polyphenols were quantified using HPLC; molecular docking was carried out using AutoDockTools 1.5.6; antioxidant activity was ascertained via the potentiometric method; and anti-inflammatory activity was examined based on the carrageenan edema method. The extract was found to be rich in epicatechin (0.417%), (+)-catechin (0.501%), and ellagitannins (0.401%). The free energy of (+)-catechin and epicatechin was -8.40 and -7.20 respectively for the active sites of cyclooxygenase-2 (COX-2), and -6.60 and -7.11 for nicotinamide adenine dinucleotide phosphate oxidase (NADPH oxidase). Notably, the antioxidant activity of the raspberry leaf extract was 1.43%, 1.04%, and 10.62% higher than that of green tea leaf extract for doses of 4.00, 2.00, 0.20 mg/mL, respectively. Treatment with the raspberry leaf extract at a dose of 13.0 mg/kg resulted in a significant decrease in edema after 1, 2, and 3 hours by 38.8%, 41.8%, and 48.8%, respectively, compared to the control group. The study demonstrated a correspondence between experimental and theoretical results in evaluating antioxidant and anti-inflammatory activities. Correlation analysis further substantiated that the anti-inflammatory action is dependent on antioxidant activity.
该研究旨在通过高效液相色谱分析确定覆盆子叶提取物中含量最高的化合物,对抗氧化和抗炎活性进行理论和实践评估,包括硅学、体外和体内评估,以及评估抗氧化和抗炎活性之间的相关性。采用高效液相色谱法对多酚类化合物进行了定量;使用 AutoDockTools 1.5.6 进行了分子对接;通过电位法确定了抗氧化活性;根据卡拉胶水肿法检测了抗炎活性。结果发现,该提取物富含表儿茶素(0.417%)、(+)-儿茶素(0.501%)和鞣花丹宁酸(0.401%)。(+)-儿茶素和表儿茶素在环氧化酶-2(COX-2)活性位点的自由能分别为-8.40和-7.20,在烟酰胺腺嘌呤二核苷酸磷酸氧化酶(NADPH氧化酶)活性位点的自由能分别为-6.60和-7.11。值得注意的是,在剂量为 4.00、2.00 和 0.20 毫克/毫升时,覆盆子叶提取物的抗氧化活性分别比绿茶叶提取物高 1.43%、1.04% 和 10.62%。覆盆子叶提取物的剂量为 13.0 毫克/千克,与对照组相比,水肿在 1、2 和 3 小时后分别显著减少了 38.8%、41.8% 和 48.8%。该研究表明,在评估抗氧化和抗炎活性方面,实验结果与理论结果是一致的。相关分析进一步证实,抗炎作用取决于抗氧化活性。
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引用次数: 0
MMP-1 and MMP-7 Expression is Influenced by Ginsenosides in Mice Exposed to Aflatoxin B1: in vivo Study 人参皂苷影响暴露于黄曲霉毒素 B1 的小鼠体内 MMP-1 和 MMP-7 的表达:体内研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.35516/jjps.v17i2.1989
Safa M Abdulateef, S. Ibraheem, Humam S Hussein, B. Dheeb, B. M. Khashman, Dunya Muayed Ahmed, Khaled H Abu-Elteen, L. Abu-Qatouseh
Panax ginseng (PG), one of the most widely used herbal medicines, has demonstrated various beneficial effects such as anti-inflammatory, antioxidant, and anticancer impacts. Naturally occurring ginsenosides in the ginseng plant inhibit cell proliferation and significantly reduce liver damage induced by certain chemicals. Aflatoxin B1 (AFB1) is a primary mycotoxin due to its hepatotoxic, immunotoxic, and oncogenic effects in animal models and humans. In this study, we examined the effects of assorted doses of PG aqueous crude extract on the expression of matrix metalloproteinase 1 and 7 (MMP-1 and MMP-7) in the kidney, spleen, and liver of experimental AFB1-exposed mice, using immunohistochemistry (IHC). Mice were orally administered 6 mg/kg body weight (bw) of refined AFB1 (isolated and extracted from Aspergillus flavus, conc. 0.05 ppm) twice weekly for two weeks. We then compared the effects of three different doses (50, 100, and 150 mg/kg bw) of crude ginseng. We estimated the expression of MMP-1 and 7 in organs using IHC. We used the 6 mg/kg of purified AFB1, representing a 60% concentration, as a control group. IHC analysis showed that MMP (1 and 7) expression in the spleen, liver, and kidney of mice decreased after treatment with ginseng crude extract. MMP-1 expression was reduced in the liver by approximately 2.6 times, while the effectiveness in the MMP-1 reduction reached 9 and 8 times, respectively, in the spleen and kidney when treated with a higher dose of PG compared to the control. MMP-7 expression was reduced in the liver by approximately 13 times, while the reduction effectiveness fell to 2.3 and 5.6 times in the spleen and kidney when treated with a higher dose of PG compared to the control. The reduction in MMPs expression due to the effect of PG aqueous crude extract was observed to act against the effect of AFB1 on various living organs involved in AFB1 metabolism. IHC analysis indicated a more significant reduction efficiency observed in the expression of MMP-7 compared to both studied markers in the mice's liver.
人参(PG)是应用最广泛的草药之一,具有抗炎、抗氧化和抗癌等多种有益作用。人参植物中天然存在的人参皂苷能够抑制细胞增殖,并显著减轻某些化学物质对肝脏造成的损伤。黄曲霉毒素 B1(AFB1)是一种主要的霉菌毒素,在动物模型和人体中具有肝毒性、免疫毒性和致癌作用。在这项研究中,我们采用免疫组织化学方法(IHC),研究了各种剂量的 PG 水提取物对基质金属蛋白酶 1 和 7(MMP-1 和 MMP-7)在暴露于 AFB1 的小鼠肾脏、脾脏和肝脏中表达的影响。给小鼠口服 6 毫克/千克体重(bw)的精制 AFB1(从黄曲霉中分离提取,浓度为 0.05 ppm),每周两次,连续两周。然后,我们比较了三种不同剂量(50、100 和 150 毫克/千克体重)粗人参的效果。我们使用 IHC 评估了器官中 MMP-1 和 7 的表达。我们使用 6 毫克/千克纯化的 AFB1(浓度为 60%)作为对照组。IHC 分析表明,使用人参粗提取物治疗后,小鼠脾脏、肝脏和肾脏中的 MMP(1 和 7)表达量减少。肝脏中的 MMP-1 表达量减少了约 2.6 倍,而与对照组相比,用较高剂量的 PG 处理脾脏和肾脏时,MMP-1 的减少效果分别达到了 9 倍和 8 倍。与对照组相比,当使用较高剂量的 PG 时,肝脏中 MMP-7 的表达量减少了约 13 倍,而脾脏和肾脏中 MMP-7 的减少效果则分别下降到 2.3 倍和 5.6 倍。据观察,PG 水提取物可减少 MMPs 的表达,从而抵消 AFB1 对参与 AFB1 代谢的各种活体器官的影响。IHC 分析表明,与所研究的两种标记物相比,小鼠肝脏中 MMP-7 的表达明显减少。
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引用次数: 0
Potential Drug-Drug Interactions and their Associated Factors at the University Children's Hospital in Syria: A Cross-Sectional Study 叙利亚大学儿童医院潜在的药物相互作用及其相关因素:横断面研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-03-19 DOI: 10.35516/jjps.v17i1.1606
Linda Hsien, Samir Srour
Objective: Polypharmacy among pediatric inpatients is common and exposes children to the risk of drug-drug interactions (DDIs). This study aimed to characterize potential DDIs (pDDIs) and their associated risk factors among pediatric inpatients.Methods: A cross-sectional study was conducted over six months at the University Children's Hospital in Damascus. A total of 575 children taking two drugs or more participated. pDDIs were checked using Lexi-Interact® software. pDDIs within risk category B (No action needed), C (Monitor therapy), D (Modify regimen), and X (Avoid combination) were included. Logistic regression was used to identify factors associated with pDDIs.Results: At least one pDDI was detected in 49.7% of children. Overall, 744 pDDIs were identified. The majority of pDDIs were within risk category C (71.6%), followed by D (14%), B (12.8%), and X (1.6%). The most common pDDIs were: aminoglycosides - penicillins (n=56), aminoglycosides - cephalosporins (n=27), and vitamin D analogs - calcium salts (n=23). The number of prescribed drugs and nervous system drugs were significantly associated with the presence of pDDIs.Conclusion: pDDIs among pediatric inpatients were prevalent. The majority of the pDDIs were within risk category C, which necessitates therapy monitoring and necessary action to avoid adverse consequences.
目的:儿科住院病人使用多种药物的情况很普遍,这使儿童面临药物间相互作用(DDI)的风险。本研究旨在描述儿科住院患者中潜在的 DDIs(pDDIs)及其相关风险因素:在大马士革大学儿童医院进行了为期六个月的横断面研究。使用 Lexi-Interact® 软件对 pDDIs 进行了检查。风险类别 B(无需采取行动)、C(监控治疗)、D(修改治疗方案)和 X(避免联合用药)中的 pDDIs 均包括在内。采用逻辑回归法确定与 pDDIs 相关的因素:结果:49.7%的儿童至少发现了一种 pDDI。总共发现了 744 个 pDDI。大多数 pDDI 属于风险类别 C(71.6%),其次是 D(14%)、B(12.8%)和 X(1.6%)。最常见的 pDDIs 是:氨基糖苷类-青霉素类(n=56)、氨基糖苷类-头孢菌素类(n=27)和维生素 D 类似物-钙盐(n=23)。处方药和神经系统药物的数量与 pDDIs 的存在有显著关联。大多数 pDDIs 属于 C 风险类别,需要对治疗进行监测并采取必要行动以避免不良后果。
{"title":"Potential Drug-Drug Interactions and their Associated Factors at the University Children's Hospital in Syria: A Cross-Sectional Study","authors":"Linda Hsien, Samir Srour","doi":"10.35516/jjps.v17i1.1606","DOIUrl":"https://doi.org/10.35516/jjps.v17i1.1606","url":null,"abstract":"Objective: Polypharmacy among pediatric inpatients is common and exposes children to the risk of drug-drug interactions (DDIs). This study aimed to characterize potential DDIs (pDDIs) and their associated risk factors among pediatric inpatients.\u0000Methods: A cross-sectional study was conducted over six months at the University Children's Hospital in Damascus. A total of 575 children taking two drugs or more participated. pDDIs were checked using Lexi-Interact® software. pDDIs within risk category B (No action needed), C (Monitor therapy), D (Modify regimen), and X (Avoid combination) were included. Logistic regression was used to identify factors associated with pDDIs.\u0000Results: At least one pDDI was detected in 49.7% of children. Overall, 744 pDDIs were identified. The majority of pDDIs were within risk category C (71.6%), followed by D (14%), B (12.8%), and X (1.6%). The most common pDDIs were: aminoglycosides - penicillins (n=56), aminoglycosides - cephalosporins (n=27), and vitamin D analogs - calcium salts (n=23). The number of prescribed drugs and nervous system drugs were significantly associated with the presence of pDDIs.\u0000Conclusion: pDDIs among pediatric inpatients were prevalent. The majority of the pDDIs were within risk category C, which necessitates therapy monitoring and necessary action to avoid adverse consequences.","PeriodicalId":14719,"journal":{"name":"Jordan Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140229962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Physicians' Knowledge of Theophylline Use: A Cross-Sectional Study from Jordan 医生对茶碱使用的了解:约旦的一项横断面研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.35516/jjps.v16i4.1789
Tasneem Basheer Ali, Huda Yousef Almomani, F. Al-Tarawneh, M. Alwadi, Ahmad Shaher Suliman
Objective: This cross-sectional study aims to assess physicians' knowledge regarding theophylline drug and other related characteristics in Jordan. Materials and Method: The study was conducted prospectively among physicians in Jordan. Physicians were interviewed using an online questionnaire consisting of two sections. The first section included demographics and other relevant characteristics, while the second section comprised questions about theophylline drug. Results: A total of 385 participants completed the questionnaire. The majority of participants knew that theophylline is used in clinical practice as a bronchodilator (75.6%). Nearly 39% of participants knew that theophylline can be administered orally and intravenously. The largest share of participants (76.1%) did not know that theophylline dosage is calculated based on ideal body weight. Sixty percent of participants knew that theophylline use was not contraindicated during pregnancy. On the other hand, only 27.3% knew that theophylline use was not contraindicated during breastfeeding. The majority of participants (76.1%) had an overall intermediate knowledge of theophylline. Conclusions: It was noted that physicians had an overall intermediate knowledge of theophylline. Physicians demonstrated unsatisfactory knowledge about theophylline’s indications, clinical use, administration, adverse effects, and other related aspects. These findings highlight the need for educational interventions and training programs to improve physicians’ knowledge of theophylline and enhance its effective and safe use in clinical practice.
研究目的本横断面研究旨在评估约旦医生对茶碱类药物及其他相关特征的了解程度。材料与方法:本研究对约旦的医生进行了前瞻性调查。医生们接受了由两部分组成的在线问卷调查。第一部分包括人口统计学和其他相关特征,第二部分包括有关茶碱类药物的问题。结果:共有 385 名参与者完成了问卷调查。大多数参与者知道茶碱在临床上被用作支气管扩张剂(75.6%)。近39%的参与者知道茶碱可以口服和静脉注射。大部分参与者(76.1%)不知道茶碱的剂量是根据理想体重计算的。60%的參加者知道在懷孕期間並不禁忌使用茶鹼。另一方面,只有27.3%的參加者知道在餵哺母乳期間並不禁忌使用茶鹼。大多数参与者(76.1%)对茶碱的总体了解处于中等水平。结论医生对茶碱的总体认识处于中等水平。医生对茶碱的适应症、临床使用、用药、不良反应和其他相关方面的知识并不满意。这些发现凸显了教育干预和培训计划的必要性,以提高医生对茶碱的认识,并加强其在临床实践中的有效和安全使用。
{"title":"Physicians' Knowledge of Theophylline Use: A Cross-Sectional Study from Jordan","authors":"Tasneem Basheer Ali, Huda Yousef Almomani, F. Al-Tarawneh, M. Alwadi, Ahmad Shaher Suliman","doi":"10.35516/jjps.v16i4.1789","DOIUrl":"https://doi.org/10.35516/jjps.v16i4.1789","url":null,"abstract":"Objective: This cross-sectional study aims to assess physicians' knowledge regarding theophylline drug and other related characteristics in Jordan. Materials and Method: The study was conducted prospectively among physicians in Jordan. Physicians were interviewed using an online questionnaire consisting of two sections. The first section included demographics and other relevant characteristics, while the second section comprised questions about theophylline drug. Results: A total of 385 participants completed the questionnaire. The majority of participants knew that theophylline is used in clinical practice as a bronchodilator (75.6%). Nearly 39% of participants knew that theophylline can be administered orally and intravenously. The largest share of participants (76.1%) did not know that theophylline dosage is calculated based on ideal body weight. Sixty percent of participants knew that theophylline use was not contraindicated during pregnancy. On the other hand, only 27.3% knew that theophylline use was not contraindicated during breastfeeding. The majority of participants (76.1%) had an overall intermediate knowledge of theophylline. Conclusions: It was noted that physicians had an overall intermediate knowledge of theophylline. Physicians demonstrated unsatisfactory knowledge about theophylline’s indications, clinical use, administration, adverse effects, and other related aspects. These findings highlight the need for educational interventions and training programs to improve physicians’ knowledge of theophylline and enhance its effective and safe use in clinical practice.","PeriodicalId":14719,"journal":{"name":"Jordan Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139157721","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Methanol Leaves Extract of Zingiber officinale (Roscoe) exhibited Anti-Obesity Effect in Wistar Rats Fed with a High Fat Diet 高脂饲料喂养的 Wistar 大鼠体内 Zingiber officinale(Roscoe)的甲醇叶提取物具有抗肥胖作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.35516/jjps.v16i4.1128
O. Ibukun, E. Uhunmwangho, Iyanuoluwa Ademola, Nisi-Dominus Olokor, Oluwasina Akinnaso
This study evaluated the anti-obesity properties of the methanol extract of Zingiber officinale leaves in Wistar rats. Thirty male rats were distributed into five groups, with six rats in each group, and different groups were treated with a normal fat diet (NFD), high-fat diet (HFD), HFD + orlistat (20 mg/kg) p.o, HFD + Zingiber officinale (200 mg/kg) p.o, and HFD + Zingiber officinale (400 mg/kg) p.o for fifty-six days. After all administrations, the animals were sacrificed by cervical dislocation, and various biochemical analyses were carried out. Results showed that there was a significant decrease (p < 0.05) in body weight and adiposity in the Zingiber officinale, NFD, and orlistat groups compared to the HFD control. However, there was no significant difference in the body weights of rats in the Zingiber officinale groups compared to the NFD control and orlistat groups. Furthermore, rats in the Zingiber officinale groups had normal lipid concentrations, antioxidant status, adipokines, cytokines, liver, kidney, and cardiac function parameters that were comparable to orlistat and normal control but in contrast with the HFD control. Findings from the study suggest that Zingiber officinale leaves have significant anti-obesity, antioxidant, and anti-inflammatory properties.
本研究评估了刺五加叶甲醇提取物在 Wistar 大鼠体内的抗肥胖特性。将 30 只雄性大鼠分为 5 组,每组 6 只,分别给予正常脂肪饮食(NFD)、高脂肪饮食(HFD)、HFD + 奥利司他(20 毫克/千克)(局部)、HFD + 细辛(200 毫克/千克)(局部)和 HFD + 细辛(400 毫克/千克)(局部)治疗,为期 56 天。给药后,动物颈椎脱臼处死,并进行各种生化分析。结果显示,与高纤维食物对照组相比,银杏叶组、NFD组和奥利司他组的体重和脂肪含量均有显著下降(p < 0.05)。然而,与 NFD 对照组和奥利司他组相比,细辛组大鼠的体重没有明显差异。此外,细辛组大鼠的血脂浓度、抗氧化状态、脂肪因子、细胞因子、肝脏、肾脏和心脏功能参数均正常,与奥利司他和正常对照组相当,但与高氟日粮对照组不同。研究结果表明,香叶具有显著的抗肥胖、抗氧化和抗炎特性。
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引用次数: 0
Discovery of Potential Prolyl-tRNA Synthetase Allosteric Inhibitor Through Virtual Screening and In Vitro Assay against Plasmodium falciparum 通过虚拟筛选和针对恶性疟原虫的体外检测发现潜在的脯氨酰-tRNA 合成酶异位抑制剂
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.35516/jjps.v16i4.1027
Tegar Achsendo, T. A. Yuniarta, Gede Ari Sumartha, T. M. Fakih, Rosita Handayani, Dwi Syah, Fitra Ramadhan
Objectives: This study aimed to identify novel antimalarial compounds based on allosteric inhibitor of prolyl-tRNA synthetase using hierarchical virtual screening. Materials and Methods: Pharmacophore model was designed initially, based on the structure-activity relationships data between several pyrazole-urea analogues and their IC50 enzymatic value. The model obtained was applied to screen ZINC15 database, after which followed by drug-likeness, toxicophore, and PAINS filter. The hit compounds were docked against P. falciparum prolyl-tRNA synthetase enzyme, using validated docking method. The resulting docking poses were ranked based on the docking score and re-evaluated based on the pharmacophore criteria. Top five compounds were obtained from this step and then evaluated using molecular dynamics simulation to verify its stability and hydrogen bond dynamics over 50 nanoseconds. MM-PBSA analysis was also performed to estimate their binding free energy. Ultimately, their potential bioactivity as antimalarial candidates have been verified against 3D7 strain. Results: The results showed that all five compounds obtained from virtual screening possess micromolar potency in vitro. Two compounds (ZINC 1029449 and ZINC1029453), yield high antimalarial activity (0.44 and 0.72 μM, respectively) Conclusions: Overall, the virtual screening approach has successfully produced lead compounds which can be further optimized to be antimalarial agents.
研究目的本研究旨在利用分层虚拟筛选技术,鉴定基于脯氨酰-tRNA 合成酶异构抑制剂的新型抗疟化合物。材料与方法:根据几种吡唑-脲类似物的结构-活性关系数据及其 IC50 酶切值,初步设计了药效学模型。将得到的模型应用于筛选 ZINC15 数据库,然后进行药物相似性、毒性和 PAINS 筛选。采用有效的对接方法,将命中的化合物与恶性疟原虫脯氨酰-tRNA合成酶进行对接。根据对接得分对得到的对接姿势进行排序,并根据药效标准重新评估。从这一步骤中获得前五个化合物,然后用分子动力学模拟进行评估,以验证其在 50 纳秒内的稳定性和氢键动力学。此外,还进行了 MM-PBSA 分析,以估算其结合自由能。最后,验证了它们作为抗疟候选药物对 3D7 菌株的潜在生物活性。结果结果表明,虚拟筛选得到的所有五个化合物在体外都具有微摩尔效力。两个化合物(ZINC 1029449 和 ZINC1029453)具有较高的抗疟活性(分别为 0.44 和 0.72 μM):总之,虚拟筛选方法成功地产生了先导化合物,这些化合物可以进一步优化成为抗疟药物。
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引用次数: 0
Cytotoxicity, Antioxidant Activities, GC-MS and HPLC Fingerprint Analyses of Different Extracts of Desmodium tortuosum (Sw.) DC Desmodium tortuosum (Sw.) DC 不同提取物的细胞毒性、抗氧化活性、GC-MS 和 HPLC 指纹分析
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.35516/jjps.v16i4.930
Maha Elshazly, Fatma A Hamada, L. Refahy
The family Fabaceae is the third-largest flowering plant family, and the genus Desmodium has exhibited a wide range of biological activities and a variety of chemical constituents. In the present study, different extracts of Desmodium tortuosum were evaluated for their cytotoxic and antioxidant activities, as well as their total phenolic content (TPC). The antioxidant activities were estimated using the 1,1'-diphenyl-2-picraylhydrazyl free radical (DPPH), while the cytotoxic activity was evaluated via the brine shrimp lethality test (BSLT). The antioxidant activity results revealed that the DPPH radical scavenging activity (SC50) ranged from 1.12 to 61.22 µg/ml with respect to ascorbic acid (SC50 = 7.45 µg/ml). Among all tested fractions, 90% methanol was the most active. On the other hand, the cytotoxic activities were arranged as follows: n-BuOH (LC50 = 310), EtOAc (LC50 = 350), and 70% methanol (LC50 = 380). High-Performance Liquid Chromatography-Fingerprint analyses were used to determine the chemical composition and relative proportions of phenolic compounds. GC-MS analysis indicated the presence of fatty acids and other compounds. The major identified compounds were Benzene (1-butyloctyl) (11.88%) and Himachalene (11.08%) for the ethyl acetate extract and 10-Undecenoic acid, methyl ester (25.50%) for unsaponifiable matter.
豆科(Fabaceae)是第三大开花植物科,Desmodium 属具有广泛的生物活性和多种化学成分。在本研究中,研究人员对 Desmodium tortuosum 的不同提取物的细胞毒性、抗氧化活性及其总酚含量(TPC)进行了评估。抗氧化活性采用 1,1'-二苯基-2-苦肼自由基(DPPH)进行评估,而细胞毒性活性则通过盐水虾致死试验(BSLT)进行评估。抗氧化活性结果显示,与抗坏血酸(SC50 = 7.45 µg/ml)相比,DPPH 自由基清除活性(SC50)介于 1.12 至 61.22 µg/ml 之间。在所有测试馏分中,90% 甲醇的活性最高。另一方面,细胞毒性活性排列如下:正丁醇(LC50 = 310)、乙醇(EtOAc)(LC50 = 350)和 70% 甲醇(LC50 = 380)。高效液相色谱-指纹图谱分析用于确定酚类化合物的化学成分和相对比例。气相色谱-质谱分析表明了脂肪酸和其他化合物的存在。经鉴定的主要化合物是乙酸乙酯提取物中的苯(1-丁辛基)(11.88%)和绯红烯(11.08%),以及不皂化物中的 10-十一碳烯酸甲酯(25.50%)。
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引用次数: 0
الاصْطنَاع الخارج خلوي لجسيمات أوكسيد المغنيزيوم في المستوى النّانويّ والمايكروني باستخدام نبات الصّبار كمعمل حيويّ: وفعاليّتها المضادة لفطور المبيضات البيض والرشاشية السّوداء الاصْطنَاع الخارج خلوي لجسيمات أوكسيد المغنيزيوم في المستوى النّانويّ والمايكروني باستخدام نبات الصّبار كمعمل حيويّ: وفعاليّتها المضادة لفطور المبيضات البيض والرشاشية السّوداء
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.35516/jjps.v16i4.864
Taif AlHoly, Walid Khaddam
صُنعت جسيمات أوكسيد المغنيزيوم النّانويّة والمايكرونية بواسطة صبار التين الشوكي وتم تقييم فعاليتها المضادة للفطور المسببة للأمراض الهامة عند البشر كمبيضات البيض والرشاشيات السّوداء. وتم توصيف الجسيمات الناتجة بـِ UV–Vis، FTIR، DLS، EDX،  .FESEMأظهر تحليل مطيافية الأشعة المرئية وفوق البنفسجية قمة عند 300 نانومتر، وبيّن اختبار الأشعة تحت الحمراء أن المستقلبات الحيوية في النبات تلعب دورًا مهمًا في إرجاع أيونات المعدن ثم نموها لتعطي في النهاية جسيماتٍ نانويّة، كما يبين التحليل قمة قريبة من 400  تعود للرابطة Mg-O-Mg. يؤكد تحليل الـ EDX وجود جسيمات أوكسيد المغنيزيوم. تراوحت أبعاد جسيمات أوكسيد المغنيزيوم النّانويّة ذات الشكل الكروي بين 15.5 و78.01 نانومتر (بمتوسط 42.28 نانومتر)، أما أبعاد الجسيمات المايكرونية الكروية تراوحت بين 105.2 و 1313.9 نانومتر (بمتوسط 356.09 نانومتر) وذلك باستخدام المجهر الإلكتروني الماسح عالي النفاذية FESEM. بينما كان متوسط الأبعاد المحسوب بطريقة التشتت الضوء الديناميكي DLS مساوياً لـِ  46.04 و 377 نانومتر. اختبار الفعالية المضادة للفطور في المختبر In vitro للجسيمات الناتجة تمت دراسته بواسطة طريقيتين مايكروبيولوجيتين هما الانتشار في الآبار وتمديد المرق الدقيق في كلتا الطريقتين كانت للجسيمات النّانوية تأثير أكبر من الجسيمات بالحجم الأكبرضد الفطور، وكان التركيز المثبط الأدنى الـ  MIC لجسيمات أوكسيد المغنيزيوم النّانويّة مساوياً لـِ  1.5 ، 6.25 ملغ / مل لكل من المبيضات البيض والراشاشيات السوداء على التوالي.
صُنعت جسيمات أوكسيد المغنيزيوم النّانويّة والمايكرونية بواسطة صبار التين الشوكي وتم تقييم فعاليتها المضادة للفطور المسببة لأمراض الهامة عند البشر كمبيضات البيض والرشاشيات السّوداء.وتم توصيف الجسيمات الناتجة بـِ UV-Vis ، FTIR ، DLS ، EDX ، .fesemأظهر تحليل مطيافية الأشعة المرئية وفوق البنفسجية قمة عند 300 نانومتر، وبيّن اختبار الأشعة تحت الحمراء أن المستقلبات الحيوية في النباتتلعب دورًا مهمًا في إرجاع أيونات المعدن ثم نموها لتعطي في النهاية جسيماتٍ نانويّة، كما يبين التحليل قمة قريبة من 400 تعود للرابطة Mg-O-Mg.يؤكد تحليل الـ edx وجود جسيمات أوكسيد المغنيزيوم.تراوحت أبعاد جسيمات أوكسيد المغنيزيوم النّانويّة ذات الشكل الكروي بين 15.5 و78.01 نانومتر (بمتوسط 42.28 نانومتر)، أما أبعاد الجسيمات المايكرونية الكروية تراوحت بين 105.2 و 1313.9 نانومتر (بمتوسط 356.09 نانومتر) وذلك باستخدام المجهر الإلكتروني الماسح عالي النفاذية fesem.بينما كان متوسط الأبعاد المحسوب بطريقة التشتت الضوء الديناميكي dls مساوياً لـِ 46.04 و 377 نانومتر.اختبار الفعالية المضادة لفطور في المختبر 体外 لجسيمات الناتجة تمت دراسته بواسطة طريقيتين مايكروبيولوجيتين هما الانتشار في الآبار وتمديد المرق الدقيق في كلتاالطريقتين كانت لجسيمات النّانوية تأثير أكبر من الجسيمات بالحجم الأكبرضد الفطور، وكان التركيز المثبط الأدنى ال micـ لجسيمات أوكسيد المغنيزيوم النّانويّة مساوياً لـِ 1.5 ، 6.25 ملغ / مل لكل من المبيضات البيض والراشاشيات السوداء على التوالي.
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Jordan Journal of Pharmaceutical Sciences
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