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Formulation, characterization and evaluation to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation 阿替洛尔胃滞留粘附剂剂量在人体内的生物利用度的配方、表征和评估
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.22034/IJPS.2020.105389.1540
K. Kumar, Gurunath Surampalli, Y. Rao, M. Ajitha
Objective: This study was planned to formulate, characterize and evaluate to establish the bioavailability of gastroretentive mucoadhesive dosage of atenolol in human subjects with possible in-vitro-in-vivo correlation. Method: In this investigation gastroretentive mucoadhesive dosage of Atenolol was formulated using HPMCK4M, chitosan and Isabgul husk by wet granulation technique. The prepared tablets were subjected to physical evaluation, in-vitro drug release and in-vivo X-ray studies, followed by the pharmacokinetic study in human volunteers. Results: All the prepared tablets showed physicochemical properties within the limits and good in-vitro mucoadhesion. Formulation F2 was selected based on the in-vitro characteristics and in-vivo radiographic studies by replacing part of the drug by adding barium sulphate. From the radiographic studies it was found that the F2 could be successfully retained in stomach for more than 6 hours. Pharmacokinetic studies showed a significant improvement in AUC0-14; 6414.93 ± 58.221 ng.h/mL (p < 0.05) when compared to reference AUC0-14; 4752.18 ± 76.759 ng.h/mL in healthy human volunteers with good invitro-invivo correlation. Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, F2 was selected as optimized gastroretentive mucoadhesive dosage form with improved bioavailability for better patient compliance and disease management.
目的:本研究拟制定、表征和评价胃保留黏附剂阿替洛尔在人体中的生物利用度,并可能存在体内外相关性。方法:以HPMCK4M、壳聚糖和蚕豆壳为原料,采用湿法制备阿替洛尔胃保留黏附剂。对制备的片剂进行了物理评价、体外释药和体内x线研究,并在人体志愿者体内进行了药代动力学研究。结果:所制片剂理化性质均在限定范围内,体外黏附良好。配方F2是根据体外特性和体内放射学研究选择的,通过添加硫酸钡代替部分药物。放射学研究发现,F2可在胃中成功滞留6小时以上。药代动力学研究显示AUC0-14显著改善;6414.93±58.221 ng.h/mL (p < 0.05);4752.18±76.759 ng.h/mL,具有良好的体内外相关性。结论:基于体外特性和体内放射学研究,F2是最佳的胃保留黏附剂剂型,具有更好的生物利用度,可提高患者的依从性和疾病管理。
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引用次数: 0
Antibacterial Properties and Flavonoids Content of Some Mosses Common in Armenia 亚美尼亚常见藓类植物的抗菌性能及类黄酮含量
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.22034/IJPS.2020.121318.1639
I. Semerjyan, G. Semerjyan, H. Semerjyan, A. Trchounian
The present study was aimed to evaluate the antibacterial potential of ethanol, methanol, acetone and aqueous extracts of some bryophytes common in Armenia (Mnium spinosum (Voit) Schwaegr, Brachythecium salebrosum (Web. et Mohr) B.S.G., Thuidiumrecognitum (Hedw) Lindb and Dicranum scoparium (Hedw). Antibacterial activity was determined using agar-well diffusion method against five bacterial species (Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Salmonella enterica and S. typhimirium). The results showed that the bryophytes D. scoparium and B. salebrosum possessed high antibacterial activity in methanol extracts, whereas M. spinosum - in acetone extract. Antibacterial activity against S. aureus was comparably weaker. Ethanol extract of T. recognitum had greater antibacterial activity than the extract of M. spinosum. Of all those tested for antibacterial activity bryophytes in vitro extracts of D. scoparium have yielded the most promising results. Antibacterial activity might be caused by a high content of flavonoids in bryophytes determined. Thus, the studied bryophytes might be used to develop new antibacterial agents.
本研究旨在评价亚美尼亚常见苔藓植物(um spinosum (Voit) Schwaegr, Brachythecium salebrosum (Web.), Brachythecium salebrosum)的乙醇、甲醇、丙酮和水提取物的抑菌潜力。等Mohr) B.S.G, Thuidiumrecognitum (Hedw) Lindb和Dicranum scoparium (Hedw)。采用琼脂孔扩散法测定对大肠杆菌、枯草芽孢杆菌、金黄色葡萄球菌、肠炎沙门氏菌和鼠伤寒沙门氏菌5种细菌的抑菌活性。结果表明,在甲醇提取物中,苔藓植物东莨菪和龙葵具有较高的抑菌活性,而在丙酮提取物中,棘草具有较高的抑菌活性。对金黄色葡萄球菌的抑菌活性相对较弱。金针菇乙醇提取物的抑菌活性高于棘毛菌提取物。在所有对苔藓植物抑菌活性进行的测试中,东莨菪提取物获得了最有希望的结果。苔藓植物中黄酮类化合物的高含量可能是其抗菌活性的主要原因。因此,所研究的苔藓植物可用于开发新的抗菌药物。
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引用次数: 2
Persicoimidate isolated from Allium ampeloprasum Subsp. Persicum with Apoptotic effects against Breast cancer cell lines 从香蒜亚种中分离得到桃霉酰咪酯。仙子对乳腺癌细胞凋亡的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.22034/IJPS.2020.122139.1644
Seyed Reza Naji Esfahani, Masoud Sadeghi-Dinani, F. Moazen, F. Shafiee
Breast cancer is the most common malignancy among American women and the second leading cause of cancer death after the lung cancer. For this reason, trying to find new drugs for the treatment of this disease is essential. The aim of the present study was to evaluate the cytotoxic effects of three cinnamic acid derivatives isolated from Allium ampeloprasum var. Persicum including Caffeoyl tyramine, Feruloyl tyramine, and Persicoimidate on two breast cancer cell lines, MCF-7 and BT-474. Evaluation the cytotoxic effects of mentioned purified compounds against MCF-7 and BT-474 cells was performed using MTT assay and their IC50 was determined. Finally, flow cytometery analysis on MCF-7 cells was performed and used to determine the cell death mechanism of investigated compounds. The results exhibited that the cytotoxic effects of all three compounds against breast cancer cell lines was concentration-dependent. The IC50 of Caffeoyl tyramine, Feruloyl tyramine, and Persicoimidate was determined to be as 73, 56, and 40 μg/ml for MCF-7 and 100, 54, and 37 μg/ml for BT-474 cells, respectively. So, Perscicoimidate showed the most potent cytotoxic effects against two breast cancer cells. Finally, flow cytometery analysis showed that Persicoimidate caused approximately 48% of apoptosis in concentration of 40 μg/ml. According to the tyrosine kinase inhibitory activity of cinnamic acid derivatives, these compounds has the potential of being cancer drug candidates for complementary studies on breast tumors with highly expression of EGF receptor. However, evaluation of anti-cancer effects of these compounds against other breast cancer cell lines is suggested.
癌症是美国女性最常见的恶性肿瘤,也是癌症死亡的第二大原因,仅次于癌症。因此,寻找治疗这种疾病的新药至关重要。本研究的目的是评估从大葱中分离的三种肉桂酸衍生物,包括咖啡酰酪胺、Feruloyl酪胺和Persicoimide对两种乳腺癌症细胞系MCF-7和BT-474的细胞毒性作用。使用MTT测定法评价上述纯化的化合物对MCF-7和BT-474细胞的细胞毒性作用,并测定它们的IC50。最后,对MCF-7细胞进行流式细胞术分析,并用于确定所研究化合物的细胞死亡机制。结果表明,三种化合物对癌症细胞系的细胞毒性作用均呈浓度依赖性。MCF-7细胞的咖啡酰酪胺、铁酰酪胺和Persicoimide的IC50分别为73、56和40μg/ml,BT-474细胞的IC50为100、54和37μg/ml。因此,泛昔胺对两种癌症细胞显示出最有效的细胞毒性作用。最后,流式细胞仪分析显示,在40μg/ml的浓度下,Persicomidate可引起约48%的细胞凋亡。根据肉桂酸衍生物对酪氨酸激酶的抑制活性,这些化合物有可能成为癌症药物的候选物,用于EGF受体高表达的乳腺肿瘤的补充研究。然而,建议评估这些化合物对其他乳腺癌症细胞系的抗癌效果。
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引用次数: 0
Cytotoxic effect of Tilia dasystyla and Polygonatum orientale Desf extracts on AGS and SKOV-3 cancer cell lines 硬叶椴和黄精提取物对AGS和SKOV-3癌细胞的细胞毒作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.22034/IJPS.2020.111775.1591
Roshanak Zarringhalami, P. Hanachi, Reihaneh Ramezani Tamijani
Nowadays medicinal plants have been considered as the complementary medicine in cancer treatment by researchers. Some plants possess chemical compounds which are able to inhibit the growth of cancer cells or even eliminate them through apoptosis or necrosis. In current study anticancer effect of Tilia dasystyla and Polygonatum orientale Desf extracts on AGS and SKOV-3 cancer cell lines were investigated. The cytotoxic effect of Tilia dasystyla and Polygonatum orientale Desf extracts on AGS and SKOV-3 has not been reported so far. Cancer cell lines were treated with different concentrations (100-5000 µg/ml) of T. dasystyla and P. orientale Desf methanol extracts for 24, 48, 72 hours. Cell viability of AGS and SKOV-3 cancer cells were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) method. Results of the study indicate that, extracts of T. dasystyla and P. orientale Desf showed cytotoxic effect on AGS and SKOV-3 cancer cell lines. The lowest IC50 value of AGS and SKOV-3 cell lines was about 1.02 ± 0.01 mg /ml and 1.14 ± 0.17 mg / ml respectively. T. dasystyla and P. orientale Desf extracts showed cytotoxic effect on AGS and SKOV-3 cancer cell lines in time- and dose-dependent manner. Full potential of the extracts, as an option for cancer treatment, is yet to be determined by further studies on animal models and subsequent trials.
目前,药用植物已被研究人员视为治疗癌症的补充药物。有些植物含有能够抑制癌细胞生长甚至通过细胞凋亡或坏死来消灭癌细胞的化合物。本研究主要研究了硬叶椴和黄精提取物对AGS和SKOV-3癌细胞的抗癌作用。迄今为止,尚没有关于硬叶椴和黄精提取物对AGS和SKOV-3细胞毒作用的报道。用不同浓度(100-5000µg/ml)的冬花草和东方花草甲醇提取物处理癌细胞24、48、72小时。采用MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四氮唑)法评价AGS和SKOV-3癌细胞的细胞活力。研究结果表明,水杨花和东方花提取物对AGS和SKOV-3癌细胞具有细胞毒作用。AGS和SKOV-3细胞株的最低IC50值分别为1.02±0.01 mg /ml和1.14±0.17 mg /ml。毛茛和东方花提取物对AGS和SKOV-3癌细胞的细胞毒作用呈时间和剂量依赖性。作为癌症治疗的一种选择,这种提取物的全部潜力还有待于进一步的动物模型研究和随后的试验来确定。
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引用次数: 2
Evaluation of drug-drug interactions in chronic kidney disease patients: A single-center experience 慢性肾脏疾病患者药物-药物相互作用的评价:单中心经验
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2020.109154.1567
M. Farnoud, M. Mehrpooya, Mohammad Mehdi Mahboobian, Y. Mohammadi, M. Mohammadi
Drug-drug interactions (DDIs) result from the simultaneous consumption of two or more drugs that alter the patient’s response to the initial drug. The treatment regimen in patients with kidney disease is very diverse and may be associated with several diseases that increases the risk of DDIs. This study was carried out to investigate the DDIs incidence in patients with chronic kidney disease (CKD) in the nephrology ward. This descriptive-analytical study was performed in a 4-month period in 2017. The patients’ information such as age, sex, list of drugs during hospitalization, and kidney disease stage were recorded from patients’ medical records. Drug-drug interactions were extracted using LexiComp Online. In this study 48.55% of patients were male, 51.45% were female and 53.2% of patients were in stage 5 of kidney disease. There was a significant correlation between the incidence of drug-drug interactions with stage 5 of disease (P=0.02). The highest number of interactions was categorized as type C and interaction between atorvastatin and pantoprazole was the most frequent interaction. The maximum range of prescription drugs was between 6 and 10 items by 49.7% of patients. There was a significant correlation between the incidence of drug-drug interactions and the number of prescribed drugs (P=0.03). Drug-drug interactions are common in patients with chronic kidney disease. Based on the results, the number of prescribed drugs and the stage of the disease is effective in drug-drug interactions incidence. It is possible to reduce drug complications and increase the life span of patients by recognizing drug-drug interactions.
药物-药物相互作用(ddi)是由于同时服用两种或两种以上药物而改变患者对初始药物的反应。肾病患者的治疗方案非常多样化,可能与几种增加ddi风险的疾病有关。本研究旨在探讨慢性肾脏病(CKD)患者ddi的发生率。该描述性分析研究于2017年进行,为期4个月。从患者病历中记录患者的年龄、性别、住院期间用药清单、肾脏疾病分期等信息。使用LexiComp Online提取药物-药物相互作用。在本研究中,48.55%的患者为男性,51.45%为女性,53.2%的患者处于肾脏疾病的第5期。药物-药物相互作用的发生率与疾病的第5期有显著的相关性(P=0.02)。最多的相互作用被归类为C型,阿托伐他汀和泮托拉唑的相互作用是最常见的相互作用。49.7%的患者处方药品最大使用范围在6 ~ 10种之间。药物相互作用发生率与处方药物数量有显著相关(P=0.03)。药物-药物相互作用在慢性肾脏疾病患者中很常见。根据结果,处方药物的数量和疾病的分期是影响药物相互作用发生率的重要因素。通过认识药物-药物相互作用,有可能减少药物并发症并延长患者的寿命。
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引用次数: 0
Hypotensive effect of Centella asiatica L. extract in acute Angiotensin II-induced hypertension 积雪草提取物对急性血管紧张素ii型高血压的降压作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2020.121635.1642
R. Mohebbati, Y. Kamkar-Del, F. Kazemi, H. Rakhshandeh, M. Shafei
Centella asiatica L. (C.asiatica) is a plant with a hypotensive effect. Since this effect has several mechanism(s), therefore in the current study we investigated the effects of hydroalcoholic extract of C.asiatica on cardiovascular parameters in acute hypertensive rats. Animals were divided into four groups; 1) control, 2) Angiotensin II (AngII) that received (50 ng/kg) intravenously (i.v.), 3 and 4) two groups of C.asiatica extract (CA100, and CA200 mg/kg). In treated groups, 30 min after injection of the extract, AngII was injected. Cardiovascular parameters were recorded by the power lab system after the cannulation of the femoral artery. The maximum changes (∆) of systolic blood pressure (SBP), mean arterial pressure (MAP) and heart rate (HR) were calculated and used for statistical analysis. In the AngII group, ΔSBP and ΔMAP significantly increased compared to the control group. The HR also decreased compared to the control group but it was not significant. In CA100+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The use of these doses of CA with AngІІ compared to AngІІ alone had a significant effect on the HR. In CA200+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The change of HR in this dose was not significant to the AngII. In a recent study, we concluded that C.asiatica decreased the cardiovascular responses in hypertensive rats received AngII. Also between two doses of C.asiatica did not observe any significant difference. Therefore, one of the most important hypotensive mechanism(s) of the considered plant can be the effect on Renin-angiotensin system.
积雪草(Centella asiatica L.)是一种具有降血压作用的植物。由于这种作用有多种机制,因此在本研究中,我们研究了积雪草水醇提取物对急性高血压大鼠心血管参数的影响。动物被分成四组;1)对照组,2)血管紧张素II (AngII)组静脉注射(50 ng/kg), 3、4)两组积血藤提取物(CA100、CA200 mg/kg)。治疗组在注射提取物30 min后注射AngII。股动脉插管后用动力实验室系统记录心血管参数。计算收缩压(SBP)、平均动脉压(MAP)、心率(HR)的最大变化∆,并进行统计分析。在AngII组中,ΔSBP和ΔMAP与对照组相比显著增加。与对照组相比,HR也有所下降,但差异不显著。CA100+AngII组ΔSBP和ΔMAP与AngII组相比显著降低。与单独使用AngІІ相比,将这些剂量的CA与AngІІ一起使用对HR有显著影响。CA200+AngII组ΔSBP和ΔMAP与AngII组相比显著降低。该剂量组HR变化对AngII无明显影响。在最近的一项研究中,我们得出结论,马齿苋可以降低高血压大鼠接受AngII的心血管反应。两剂量间无显著性差异。因此,该植物最重要的降压机制之一可能是对肾素-血管紧张素系统的影响。
{"title":"Hypotensive effect of Centella asiatica L. extract in acute Angiotensin II-induced hypertension","authors":"R. Mohebbati, Y. Kamkar-Del, F. Kazemi, H. Rakhshandeh, M. Shafei","doi":"10.22034/IJPS.2020.121635.1642","DOIUrl":"https://doi.org/10.22034/IJPS.2020.121635.1642","url":null,"abstract":"Centella asiatica L. (C.asiatica) is a plant with a hypotensive effect. Since this effect has several mechanism(s), therefore in the current study we investigated the effects of hydroalcoholic extract of C.asiatica on cardiovascular parameters in acute hypertensive rats. Animals were divided into four groups; 1) control, 2) Angiotensin II (AngII) that received (50 ng/kg) intravenously (i.v.), 3 and 4) two groups of C.asiatica extract (CA100, and CA200 mg/kg). In treated groups, 30 min after injection of the extract, AngII was injected. Cardiovascular parameters were recorded by the power lab system after the cannulation of the femoral artery. The maximum changes (∆) of systolic blood pressure (SBP), mean arterial pressure (MAP) and heart rate (HR) were calculated and used for statistical analysis. In the AngII group, ΔSBP and ΔMAP significantly increased compared to the control group. The HR also decreased compared to the control group but it was not significant. In CA100+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The use of these doses of CA with AngІІ compared to AngІІ alone had a significant effect on the HR. In CA200+AngII group ΔSBP and ΔMAP significantly decreased compared to the AngII. The change of HR in this dose was not significant to the AngII. In a recent study, we concluded that C.asiatica decreased the cardiovascular responses in hypertensive rats received AngII. Also between two doses of C.asiatica did not observe any significant difference. Therefore, one of the most important hypotensive mechanism(s) of the considered plant can be the effect on Renin-angiotensin system.","PeriodicalId":14582,"journal":{"name":"Iranian Journal of Pharmaceutical Sciences","volume":"16 1","pages":"71-80"},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68028228","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: 1
The Determination of Antioxidant Activity of Ethanol Extracts of Gynostemma Pentaphyllum 绞股蓝乙醇提取物抗氧化活性的测定
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2021.522481.1779
Alfina Ansafovna Nizamova, E. Galiakhmetova, K. Mochalov, D. Bokov, Golrokh Farnam, N. Kudashkina
Inflammatory reactions of active radicals play a primary role in many vital circumstances, and if they are not neutralized and persist in the body, many diseases will occur. Antioxidants are the very critical resources available in the body to eliminate these free radicals. Medicinal herbs have been used extensively in the treatment of diseases for centuries. Gynostemma Pentaphyllum is grown in many different locations of Europe and Asia is an adaptogenic plant that is rich in antioxidants. During this study, the antioxidant effects of Gynostemma Pentaphyllum extract are evaluated using two different methods of adrenaline autooxidation and Chemiluminescence, both patented in Russia. Our results show that the organic solvent is more suitable for the extraction of these antioxidants with the ratio of 70% ethanolic extract being yield in more extraction. This preliminary work might open a new door for future studies on the antioxidant effects of this herb grown in Russia for the treatment of inflammations and other diseases with such pathology.
活性自由基的炎症反应在许多重要情况下起着主要作用,如果它们不被中和并在体内持续存在,就会发生许多疾病。抗氧化剂是体内消除这些自由基的关键资源。几个世纪以来,草药被广泛用于治疗疾病。绞股蓝生长在欧洲和亚洲的许多不同地区,是一种富含抗氧化剂的适应性植物。在本研究中,采用肾上腺素自氧化和化学发光两种不同的方法评估绞股蓝提取物的抗氧化作用,这两种方法均在俄罗斯获得专利。结果表明,有机溶剂更适合提取这些抗氧化剂,乙醇提取物的提取率为70%。这项初步工作可能为未来研究俄罗斯种植的这种草药治疗炎症和其他具有这种病理的疾病的抗氧化作用打开了新的大门。
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引用次数: 2
Systematic mining of gene co-expression network suggests a new drug repositioning for the effective treatment of Duchenne Muscular Dystrophy 系统挖掘基因共表达网络,为有效治疗杜氏肌营养不良症提供新的药物重新定位
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2020.119862.1630
A. Derakhshani, M. Moosavi, S. Nasseri, E. Miri-Moghaddam, H. Safarpour, B. Baradaran
DMD is the prototype of muscular dystrophy in childhood. As there is currently no absolute treatment, the present study aimed to propose a new drug repositioning for DMD therapy. A microarray dataset of 16 DMD and 6 control samples were analyzed and 208 differentially expressed genes were screened. Weighted gene co-expression network analysis (WGCNA) algorithm, applied to obtain co-expressed gene networks for the establishment of transcriptional modules related to clinical and demographic data of DMD patients. Results indicated that a maximum of 11 co-expression modules is present in datasets with a varying number of genes. Turquoise module with 3334 genes was strongly correlated with collagen fibril organization as a positive regulator in DMD pathogenesis (r=0.98, p-value=2/00E-15) through which other DMD related hub-genes were identified as COL1A1, FZD10, COL1A2, CRISPLD1, FMO1, COL5A1, COL3A1, COL5A2, TP53I3, PLAGL1, RIPK2, SBF1, MLXIP, CFAP46, and TYRP1. Drug repositioning of the turquoise module identified some candidate drugs which are not presently approved for the treatment of DMD. The targets in the turquoise module indicate some drugs can greatly affect DMD's structure and function as COL1A1 with 42 fold changes was the most up-regulated gene. Furthermore, drug repositioning introduced Zoledronic acid as a potent antagonist for COL1A1.
DMD是儿童时期肌肉萎缩症的原型。由于目前没有绝对的治疗方法,本研究旨在提出一种新的药物重新定位治疗DMD。分析了16个DMD样本和6个对照样本的微阵列数据集,筛选了208个差异表达基因。采用加权基因共表达网络分析(Weighted gene co-expression network analysis, WGCNA)算法,获取共表达基因网络,建立与DMD患者临床及人口学数据相关的转录模块。结果表明,在不同数量基因的数据集中,最多存在11个共表达模块。含有3334个基因的绿松脂模块在DMD发病机制中与胶原纤维组织密切相关(r=0.98, p值=2/00E-15),通过该模块鉴定出其他DMD相关中心基因为COL1A1、FZD10、COL1A2、CRISPLD1、FMO1、COL5A1、COL3A1、COL5A2、TP53I3、PLAGL1、RIPK2、SBF1、MLXIP、CFAP46和TYRP1。绿松石模块的药物重新定位确定了一些目前尚未批准用于治疗DMD的候选药物。绿松石模块中的靶点表明,一些药物可以极大地影响DMD的结构和功能,其中COL1A1基因上调幅度最大,改变了42倍。此外,药物重新定位引入了唑来膦酸作为COL1A1的有效拮抗剂。
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引用次数: 0
Assessment of the Skin and Heart Tissue Damage Following Inhalation of Carbon Nanotubes in Wistar Rats Using Isolated Mitochondria 使用分离线粒体评估吸入碳纳米管对Wistar大鼠皮肤和心脏组织的损伤
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2020.130501.1685
F. Samiei, Enayatollah Seydi, Faezeh Dousti, A. Hayati, F. Shirazi, Jalal Pourahmad Jaktaji
The unique properties of carbon nanotubes (CNTs) have led to their use in various fields. But, the toxicity of CNTs has been reported in biological and environmental systems. The aim of this research is to study the effect of multi-wall carbon nanotubes (MWCNTs) through inhalation chamber on the mitochondrial damage and oxidative stress using the mitochondria obtained from the skin and heart. Rats were exposed to 5 mg/m3 of MWCNTs (10 nm) aerosol for 5 hours /day, 5 days/week for 2 weeks in a whole-body exposure chamber. After 2-weeks exposure, Heart and skin mitochondria were evaluated for evaluation of toxicity parameters. The results showed that nanoparticles significantly decreased mitochondrial succinate dehydrogenase (SDH) activity and increased the level of reactive oxygen species (ROS), collapse in mitochondria membrane potential (MMP), swelling in mitochondria, and cytochrome release. In conclusion, we suggested that 5 mg/m3 of MWCNTs (10 nm) induce ROS mediated cytotoxicity by directly targeting mitochondria in both skin and heart tissue.
碳纳米管(carbon nanotubes, CNTs)的独特性能使其在各个领域得到了广泛的应用。但是,碳纳米管在生物和环境系统中的毒性已被报道。本研究的目的是利用从皮肤和心脏获得的线粒体,研究多壁碳纳米管(MWCNTs)通过吸入室对线粒体损伤和氧化应激的影响。在全身暴露室中,将大鼠暴露于5mg /m3的MWCNTs (10 nm)气溶胶中5小时/天、5天/周,共2周。暴露2周后,对心脏和皮肤线粒体进行毒性参数评价。结果表明,纳米颗粒显著降低线粒体琥珀酸脱氢酶(SDH)活性,增加活性氧(ROS)水平,线粒体膜电位(MMP)崩溃,线粒体肿胀,细胞色素释放。总之,我们建议5mg /m3的MWCNTs (10 nm)通过直接靶向皮肤和心脏组织中的线粒体诱导ROS介导的细胞毒性。
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引用次数: 0
Profile of TLC-densitometry Annona squamosa and Persea americana as Antihyperlipidemic Medicinal Raw Material 抗高脂血症药用原料番荔枝和美洲槐的tlc -密度谱
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 DOI: 10.22034/IJPS.2020.121834.1643
Siti Rofida
Natural medicine products usually consist of two to five kinds of plants that have synergistic biological activity. The responsible constituents for the therapeutic activity in plants often involve diverse chemical components. The combination of ethanol extracts of Annona squamosa L. (EEAS) and Persea americana M. (EEPA) has been shown to have antihyperlipidemic activity. To ensure the correctness and consistency of the EEAS and EEPAs combination as the antihyperlipidemic treatments, it is necessary to characterize the plant’s secondary metabolites. This study aimed to obtain the profiles of the secondary metabolites of Annona squamosa L. and Persea americana M. using the TLC-densitometry technique. Extract samples were applied to TLC plates and screened using densitometry at 254 nm. The obtained chromatogram peak was measured at the wavelength range of 200–700 nm to obtain the maximum wavelength of each peak. The results showed that EEAS had 5 peaks with rf values of 0.00, 0.61, 0.67, 0.73, and 0.87. The TLC-densitometry analysis results of EEPA showed eight peaks with rf values of 0.00, 0.11, 0.19, 0.49, 0.56, 0.71, 0.77, and 0.90. The extract chromatograms spectra showed that 2–3 peaks at the wavelength range of 300-350 nm. Chromatogram TLC-densitometry profile data on EEAS and EEPA can be used as the indicators in the raw material combinations standardization process of EEAS and EEPA as natural medicine products to treat antihyperlipidemic.
天然药物产品通常由两到五种具有协同生物活性的植物组成。植物中起治疗作用的成分通常包括多种化学成分。研究表明,番荔枝(Annona squamosa L., EEAS)和美洲波斯(Persea americana M., EEPA)乙醇提取物联合使用具有抗高脂血症的作用。为了确保EEAS和EEPAs联合作为抗高脂血症处理的正确性和一致性,有必要对该植物的次生代谢物进行表征。本研究旨在利用薄层色谱密度测定技术获得番荔枝和美洲波斯次生代谢产物的谱图。提取样品应用于TLC板,在254 nm处进行密度测定筛选。在200 ~ 700 nm波长范围内测量得到的色谱峰,得到各峰的最大波长。结果表明,EEAS有5个峰,rf值分别为0.00、0.61、0.67、0.73和0.87。EEPA的tlc -密度分析结果显示8个峰,rf值分别为0.00、0.11、0.19、0.49、0.56、0.71、0.77和0.90。在300 ~ 350 nm波长范围内有2 ~ 3个峰。EEAS和EEPA的色谱- tlc -密度谱数据可作为EEAS和EEPA作为天然药物产品治疗高脂血症的原料组合标准化过程中的指标。
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Iranian Journal of Pharmaceutical Sciences
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