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DEVELOPING THE ROLE OF THE ROMANIAN COMMUNITY PHARMACY IN ENVIRONMENTAL PROTECTION 发展罗马尼亚社区药房在环境保护中的作用
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.25
ALEXANDRA  TOMA
Environmental pollution with medicines is a major problem against which the best solutions are sought, in the context of a risk of contamination present in all activities relating to medicines, including those specific to the community pharmacy. The objective of the paper was to identify the best ways for developing the role of the Romanian community pharmacy in environmental protection. We performed documentary research on the websites of professional associations and pharmacies in Romania to find relevant documents, which we submitted to a thematic analysis. The community pharmacy can contribute to the protection of the environment in many ways, from reducing the waste of medicines, by promoting rational use practices and providing appropriate services for patient adherence to treatment, to collecting waste medicines from the population. In Romania, the community pharmacy is too little involved in environmental protection, therefore proper regulation of its role is necessary, combined with the will of pharmacy owners and professional associations to develop it. The most accessible ways to involve the Romanian community pharmacy include adopting institutional green policies and providing information to the population regarding the best practices for environmental protection. Rezumat
在所有与药品有关的活动(包括社区药房特有的活动)都存在污染风险的背景下,药品造成的环境污染是一个需要寻求最佳解决方案的重大问题。本文旨在确定发展罗马尼亚社区药房在环境保护方面作用的最佳途径。我们在罗马尼亚专业协会和药房的网站上进行了文献研究,以查找相关文件,并对这些文件进行了专题分析。社区药房可以通过多种方式为环境保护做出贡献,包括通过促进合理用药、为患者坚持治疗提供适当的服务来减少药品浪费,以及从居民中收集废弃药品。在罗马尼亚,社区药房参与环境保护的程度太低,因此有必要对其作用进行适当规范,同时药房业主和专业协会也有意愿发展社区药房。让罗马尼亚社区药房参与其中的最便捷方法包括采取机构绿色政策,并向居民提供有关环境保护最佳实践的信息。网站
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引用次数: 0
QUANTITATIVE ANALYSIS OF SORAFENIB AND NILOTINIB IN HUMAN PLASMA BY SPE-LC-MS 利用SPE-LC-MS对人体血浆中的索拉非尼和尼洛替尼进行定量分析
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.17
Monica Denisa Elena POPESCU
Sorafenib and nilotinib are two tyrosine kinase inhibitors (TKIs) used in the treatment of cancer. Plasmatic levels of the drugs show an important variability, so determining plasma concentration of the drugs, benefits in cancer treatment can be improved. Most papers published so far in the literature use protein precipitation followed by liquid chromatography - tandem mass-spectrometry (LC-MS/MS) as separation and detection method. With this work, we propose an alternative method for the analysis of both TKIs in human plasma. Solid phase extraction (SPE) involving Oasis PRiME HLB ® cartridges was our choice for plasma “clean-up” procedure. Extraction recoveries were at least 85%. Chromatography was performed by an ultra-high-performance liquid chromatographic system (UHPLC), using a C18 (4.6 x 50 mm) column and a mobile phase consisting of ammonium acetate/acetic acid-acetonitrile gradient elution. Detector was a simple mass spectrometer (MS) in Single Ion Recording (SIR) mode. Intra-and inter-day precision data for both TKIs were 3.8 - 7.6% and 4.5 - 8.8% for sorafenib and nilotinib, respectively. Sorafenib and nilotinib calibration curves were linear between 500 and 20000 ng/mL and 5 and 5000 ng/mL respectively, with correlation coefficients higher than 0.998. Analytes were determined in a 15 min run-time. The validated LC-MS method was applied in real human plasma routine analysis. This method may improve dose adjustment of the drugs in patients involved in cancer therapy
索拉非尼和尼洛替尼是两种用于治疗癌症的酪氨酸激酶抑制剂(TKIs)。这两种药物的血浆浓度存在很大差异,因此确定药物的血浆浓度可以提高癌症治疗的效益。迄今为止,发表在文献中的大多数论文都使用蛋白质沉淀后的液相色谱-串联质谱(LC-MS/MS)作为分离和检测方法。通过这项工作,我们提出了分析人体血浆中这两种 TKIs 的替代方法。在血浆 "净化 "过程中,我们选择了使用 Oasis PRiME HLB ® 滤芯的固相萃取 (SPE)。萃取回收率至少为 85%。色谱采用超高效液相色谱系统(UHPLC),使用 C18(4.6 x 50 毫米)色谱柱和乙酸铵/乙酸-乙腈梯度洗脱流动相。检测器为简单质谱仪(MS),采用单离子记录(SIR)模式。索拉非尼和尼洛替尼两种 TKIs 的日内和日间精密度数据分别为 3.8 - 7.6% 和 4.5 - 8.8%。索拉非尼和尼洛替尼的校准曲线分别在500-20000纳克/毫升和5-5000纳克/毫升之间呈线性关系,相关系数高于0.998。分析物的测定只需 15 分钟的运行时间。经过验证的液相色谱-质谱方法被应用于实际人体血浆的常规分析。该方法可改善癌症治疗患者的药物剂量调整
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引用次数: 0
INCISION-WOUND HEALING ACTIVITY OF SUNFLOWER SEED OIL (HELIANTHUS ANNUUS L.: IN VIVO AND IN SILICO STUDY 向日葵籽油的切口愈合活性:体内和硅学研究
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.15
Rita MALIZA
Sunflower seed oil (SFO) ( Helianthus annuus L.) is rich in oleic acid and unsaturated fatty acids and can potentially treat various ailments. To validate the ethno-therapeutic claims of the SFO in skin diseases, the incision wound healing activity was studied. The objectives of this study were to evaluate the chemical content and incision wound-healing activities of SFO. Twenty-seven adult male Wistar rats were used, and a 2 cm length and 2 mm depth incision was made on the back of the rat. The rats were administered SFO, povidone iodine (PI), or were left untreated as a control group. Histological evaluations were conducted on postoperative wound tissue biopsies on days 0, 5 and 10. The SFO compounds were assessed using GC/MS analysis, and a subsequent in silico investigation was conducted based on the GC/MS findings. The binding affinity of these compounds to TNF-α, VEGFR1, IGFR1 and TGF-β1 was evaluated. On day 10, sunflower seed oil topical application accelerated wound healing by decreasing wound area and increasing wound contraction compared to untreated and PI-treated wounds. Moreover, granulation tissue expanded more, and the epidermis fully recovered. Twenty-four active compounds were detected using GC/MS, and six are responsible for lipid metabolism regulation and anti-inflammatory activity. The in silico study showed that 9,10-Secocholesta-5,7,10(19)-triene-3,24,25-triol (3ß,5Z,7E) had a high affinity of - 8.5 kcal/mol for TNF-α. The conclusion of this study shows that SFO has incision wound healing activity in vivo and in silico by controlling the inflammatory phase and proangiogenic factors with a high affinity to bind to TNF-α in the skin tissue
向日葵籽油(Helianthus annuus L.)富含油酸和不饱和脂肪酸,可治疗多种疾病。为了验证葵花籽油对皮肤病的民族治疗功效,我们对其切口伤口愈合活性进行了研究。本研究的目的是评估 SFO 的化学成分和切口伤口愈合活性。研究人员使用 27 只成年雄性 Wistar 大鼠,在大鼠背部切开一个长 2 厘米、深 2 毫米的切口。给大鼠注射 SFO、聚维酮碘(PI)或不作处理作为对照组。对术后第 0、5 和 10 天的伤口组织活检进行组织学评估。通过 GC/MS 分析对 SFO 化合物进行了评估,随后根据 GC/MS 分析结果进行了硅学研究。评估了这些化合物与 TNF-α、VEGFR1、IGFR1 和 TGF-β1 的结合亲和力。第 10 天,与未经处理的伤口和 PI 处理的伤口相比,葵花籽油局部涂抹可通过减少伤口面积和增加伤口收缩加速伤口愈合。此外,肉芽组织扩张更多,表皮完全恢复。利用气相色谱/质谱仪检测到了 24 种活性化合物,其中 6 种具有调节脂质代谢和抗炎活性。硅学研究表明,9,10-Secocholesta-5,7,10(19)-triene-3,24,25-triol (3ß,5Z,7E)与 TNF-α 的亲和力高达 - 8.5 kcal/mol。这项研究的结论表明,SFO 通过控制炎症阶段和促血管生成因子与皮肤组织中的 TNF-α 高亲和力结合,在体内和硅学中具有切口伤口愈合活性。
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引用次数: 0
A PILOT STUDY ON FORMALDEHYDE EXPOSURE RISKS OF BAKERY WORKERS 面包房工人接触甲醛风险的试点研究
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.4
ANA-MARIA VLĂSCEANU
This study is intended to explore the impacts of formaldehyde (FA) on human health, the use and sources of FA exposure, and the regulations governing acceptable levels of FA in various products across various regions globally. The objective of this pilot study is to evaluate the risk of human FA exposure in traditional bakery units. The study group consisted of 46 subjects working in various areas: the production area (leavening, baking area, storage area), the area where bakery products are sold to customers and the delivery area to stores. The control group consists of 8 non-exposed, non-smokers subjects. Demographic, medical and anthropometric data were collected based on a questionary and the urinary levels of FA were evaluated as a biomarker of exposure. No statistically significant differences regarding the anthropometric and medical parameters of exposed workers and control group were obtained. The highest levels of FA were recorded in smokers working in the fermentation area. The results indicate statistically significant differences of FA levels between the workers in the
本研究旨在探讨甲醛 (FA) 对人体健康的影响、FA 暴露的使用和来源,以及全球不同地区对各种产品中可接受 FA 含量的规定。这项试点研究的目的是评估传统烘焙单位中人体接触 FA 的风险。研究组由 46 名受试者组成,他们分别在不同的区域工作:生产区(发酵区、烘焙区、储存区)、向客户销售烘焙产品的区域以及向商店发货的区域。对照组由 8 名非接触者和非吸烟者组成。通过问卷调查收集了受试者的人口统计学、医学和人体测量数据,并将尿液中的脂肪酸水平作为暴露的生物标志物进行了评估。在人体测量和医疗参数方面,暴露工人与对照组没有明显的统计学差异。在发酵区工作的吸烟者体内的脂肪酸含量最高。结果表明,在发酵区工作的工人与对照组工人的 FA 含量在统计学上有显著差异。
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引用次数: 0
ANTIVIRAL ACTIVITY OF ORIGINAL FLAVONOIDS-CONTAINING PHYTOPREPARATION AGAINST HUMAN ALPHAHERPESVIRUS 2, HEPATITIS C SURROGATE VIRUS AND TRANSMISSIBLE GASTROENTERITIS CORONAVIRUS 含黄酮类化合物的原始植物制剂对人类阿尔法疱疹病毒 2、代丙型肝炎病毒和传染性胃肠炎冠状病毒的抗病毒活性
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.14
Alexander GALKIN
This study evaluates the antiviral activity of a complex phytopreparation consisting of alcohol tinctures of Filipendula vulgaris , Petroselinum crispum , Apium graveolens radices, Galium verum , Linaria vulgaris herbs and Calendula officinalis flowers. The phytopreparation was tested on in vitro models of human alphaherpesvirus 2 (HHV-2), hepatitis C surrogate virus (bovine viral diarrhoea virus, BVDV) and transmissible gastroenteritis virus (TGEV). The phytopreparation solution demonstrated antiviral activity against all three viruses. The phytopreparation solution is an active inhibitor of HHV-2, BVDV and coronavirus (TGEV) replication with a selectivity index of 80, 320 and 160, respectively. Animal studies showed that the phytopreparation solution (1:100 dilution), when used as a combined treatment regimen ( per os + application), delayed the onset of guinea pig genital herpes first symptoms and reduced the time of disease in vivo . The phytopreparation solution had an antiherpetic therapeutic action similar to that of acyclovir (a reference antiherpetic drug). The induction of αIFN and inhibition of RNA and DNA synthesis were suggested mechanisms of the antiviral action of the phytopreparation complex.
本研究评估了一种复方植物制剂的抗病毒活性,该制剂由菰、芹菜、芹菜根、高丽参、扁桃草和金盏花的酒精酊剂组成。该植物制剂在人类阿尔法疱疹病毒 2(HHV-2)、丙型肝炎代用病毒(牛病毒性腹泻病毒,BVDV)和传染性胃肠炎病毒(TGEV)的体外模型上进行了测试。植物制剂溶液对这三种病毒都具有抗病毒活性。植物制剂溶液是 HHV-2、BVDV 和冠状病毒(TGEV)复制的活性抑制剂,其选择性指数分别为 80、320 和 160。动物实验表明,植物制剂溶液(1:100 稀释)作为联合治疗方案(口服 + 涂抹)可延缓豚鼠生殖器疱疹首发症状的出现,并缩短体内发病时间。植物制剂溶液的抗疱疹治疗作用与阿昔洛韦(一种抗疱疹参考药物)相似。αIFN的诱导以及RNA和DNA合成的抑制是植物制剂复合物抗病毒作用的机制。
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引用次数: 0
PERCEPTIONS OF PEOPLES TOWARDS HEALTH CARE SEEKING BEHAVIOUR FROM HEALTH CARE PROFESSIONALS – FINDINGS FROM SAUDI COMMUNITY PERSPECTIVE 人们对医护人员提供的医疗服务的看法--从沙特社区的角度得出的结论
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.24
Adel S. BASHATAH
The purpose of this study was to analyse the individuals' attitudes about seeking medical care from healthcare professionals in the Riyadh Region of Saudi Arabia (SA). Between November 2022 and January 2023, a cross-sectional, web-based study was performed among residents of Riyadh in SA. In this study, 19-items questionnaires with three sections were employed. IBM Statistic SPSS was used to evaluate the data, and the level of statistical significance was set at p < 0.05. Among the participants, 77.7% (n = 411) agreed that Saudi rules prohibit pharmacists from prescribing drugs without a prescription, while 45% (n = 193) had an unsatisfactory event with a medical doctor. The most common reason for people seeking pharmacist consultation was a common cold 79% (n = 343) followed by cough 64.5% (n = 280), headache 57.1% (n = 248), diarrhoea 38.5% (n = 176), constipation 34.6% (n = 150), fever 45.9% (n = 199). As the insurance status increased, there was a significant decrease in the unsatisfactory event associated with a medical doctor (B = ­0.138; t = -2.901; p = 0.004), respectively. A multiple regression predictor analysis revealed that education and health insurance statistically
本研究旨在分析沙特阿拉伯利雅得地区(SA)个人对向医疗保健专业人员寻求医疗护理的态度。在 2022 年 11 月至 2023 年 1 月期间,对沙特阿拉伯利雅得地区的居民进行了一项基于网络的横断面研究。本研究采用了包含三个部分的 19 个项目的调查问卷。使用 IBM 统计软件 SPSS 对数据进行评估,统计显著性水平设定为 P <0.05。在参与者中,77.7%(n = 411)的人同意沙特的规定禁止药剂师在没有处方的情况下开药,45%(n = 193)的人与医生有过不愉快的经历。人们向药剂师咨询的最常见原因是普通感冒 79%(n = 343),其次是咳嗽 64.5%(n = 280)、头痛 57.1%(n = 248)、腹泻 38.5%(n = 176)、便秘 34.6%(n = 150)、发烧 45.9%(n = 199)。随着保险状况的增加,与医生相关的不满意事件分别显著减少(B = 0.138;t = -2.901;p = 0.004)。多元回归预测分析表明,教育程度和医疗保险在统计学上
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引用次数: 0
SMOKING CESSATION – WHAT’S NEW? 戒烟--有什么新变化?
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.1
ANCUȚA-ALINA CONSTANTIN
Tobacco cessation represents a multifaceted approach involving patients who often don't neatly fit into classic prototypes. Researchers found that current smokers experience a more than 10-year reduction in life expectancy compared to non-smokers, and more than half make an attempt each year, but less than 10% manage to stay smoke-free for at least 6 months. Therefore, it's recommended to employ a combination of methods and strategies, ranging from questionnaires to established medications. The role of the medical staff is and remains vital in this context. Nicotine is a potent drug due to its rapid absorption and swift diffusion into the central nervous system, and quitting nicotine leads to important consequences, such as craving, drug-seeking behaviour and withdrawal symptoms. Negative affective states also emerge, characterized by symptoms like depressed mood, anxiety, irritability and insomnia. Hierarchical multiple regression models have revealed that extraversion, neuroticism, conscientiousness and age are among the predictors of daily cigarette consumption. The authors discuss both traditional and innovative opportunities to expedite this process, while analysing the potential to enhance the compliance of healthcare providers and patients. Smoking cessation, the process of quitting smoking, can be approached through both pharmacological (medication-based) and non-pharmacological (behavioural and supportive) methods. The choice of approach or combination of approaches depends on individual preferences and needs. Rezumat
戒烟是一种多层面的方法,涉及的患者往往并不完全符合经典的戒烟模式。研究人员发现,与不吸烟者相比,目前吸烟者的预期寿命会缩短 10 年以上,每年有一半以上的人尝试戒烟,但只有不到 10%的人能够坚持至少 6 个月不吸烟。因此,建议综合采用各种方法和策略,从问卷调查到既定的药物治疗。在这方面,医务人员的作用至关重要。尼古丁是一种强效药物,能迅速被人体吸收并迅速扩散到中枢神经系统,戒除尼古丁会导致一些重要的后果,如渴求、寻求毒品的行为和戒断症状。消极情绪状态也会出现,表现为情绪低落、焦虑、易怒和失眠等症状。层次多元回归模型显示,外向性、神经质、自觉性和年龄是预测每日吸烟量的因素。作者讨论了加快这一过程的传统和创新机会,同时分析了提高医疗服务提供者和患者依从性的潜力。戒烟,即戒烟的过程,可以通过药物(基于药物)和非药物(行为和支持)两种方法来实现。选择哪种方法或方法的组合取决于个人的偏好和需求。Rezumat
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引用次数: 0
STUDY OF THE CHEMICAL COMPOSITION, ANTIBACTERIAL AND ANTIOXIDANT ACTIVITY OF VARIOUS EXTRACTS OF THE AERIAL PART OF LEONURUS CARDIACA 研究蝎尾草气生部分各种提取物的化学成分、抗菌和抗氧化活性
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.21
L. Stepanyan
The effect of various solvents (hexane, diethyl ether, ethyl acetate, isopropyl alcohol) on extraction of phytocomponents of Leonurus cardiaca leaf was studied a long with the antioxidant and antibacterial activity of the obtained extracts. The chemical composition of the obtained extracts was studied by the chemical and spectrophotometric methods. The results showed the presence of various phytocompounds in the extracts. It was found that the non-polar solvent hexane extracted a large amount of esters compared to all selected solvents. It was also established that the most polar solvent, isopropanol, extracted large amounts of fatty acids. More extractives (8.5% yield) were extracted with isopropanol and this extract contained the highest amounts of phenolic compounds (68.8 mg GAE/g) and flavonoids (22.7 mg RE/g). The analysis of the antioxidant activity showed that the isopropanol extract had the best result. The antibacterial analysis showed that all investigated conditionally pathogenic bacteria ( E. Coli , B. subtilis and Salmonella tуphimurium ) were sensitive to all extracts. Rezumat
研究了各种溶剂(正己烷、二乙醚、乙酸乙酯、异丙醇)对萃取心叶植物成分的影响,以及所获萃取物的抗氧化和抗菌活性。采用化学和分光光度法研究了所获提取物的化学成分。结果表明,提取物中含有多种植物化合物。结果发现,与所有选定的溶剂相比,非极性溶剂正己烷萃取出了大量的酯。同时还发现,极性最强的溶剂异丙醇萃取了大量脂肪酸。用异丙醇萃取的提取物较多(8.5%),酚类化合物(68.8 毫克 GAE/克)和黄酮类化合物(22.7 毫克 RE/克)的含量最高。抗氧化活性分析表明,异丙醇提取物的抗氧化效果最好。抗菌分析表明,所有调查的条件致病菌(大肠杆菌、枯草杆菌和沙门氏菌)对所有提取物都很敏感。热苏马特
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引用次数: 0
THE PHARMACIST’S ROLE IN PROMOTING FOOD SUPPLEMENTS: CONSUMPTION OF MAGNESIUM SUPPLEMENTS IN WESTERN ROMANIA 药剂师在促进食品补充剂方面的作用:罗马尼亚西部的镁补充剂消费情况
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.23
Corina MOISA
Considering the significant role of Mg in the optimal functioning of the entire organism and the widespread consumption of Mg supplements, this study aim was to identify the main factors that influence the choice of Mg supplements by the population, how the consumption of Mg supplements evolved in the post-COVID-19 period compared to the COVID-19 period, but also the pharmacist’s role in advising citizens and promoting Mg supplements. A comparative analysis regarding their consumption over two years, one during and one after the COVID-19 pandemic, was also carried out. For higher relevance of the study, pharmacies with higher consumption of Mg supplements from different county areas were chosen. Considering that most consumers purchase food supplements from pharmacies, the pharmacist's role is decisive in choosing these supplements; depending on the desired effect for each patient, the pharmacist indicated fast-acting or delayed-acting supplements. In this regard, the in vitro release of Mg at
考虑到镁在优化整个机体功能方面的重要作用以及镁补充剂的广泛消费,本研究旨在确定影响人们选择镁补充剂的主要因素、COVID-19 后与 COVID-19 期间相比镁补充剂消费的演变情况,以及药剂师在向公民提供建议和推广镁补充剂方面的作用。此外,还对药剂师在 COVID-19 大流行期间和之后两年的消费情况进行了比较分析。为了提高研究的相关性,我们选择了不同县区中镁补充剂消费量较高的药店。考虑到大多数消费者都是从药店购买保健品,药剂师在选择保健品时起着决定性作用;根据每位患者所需的效果,药剂师会推荐速效或缓效保健品。在这方面,镁的体外释放在
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引用次数: 0
ASSESSMENT OF THE ANTI-ARTHRITIC AND IMMUNOSUPPRESSIVE POTENTIAL OF ENALAPRIL BY USING NETWORK PHARMACOLOGY, MOLECULAR DOCKING AND EXPERIMENTAL PHARMACOLOGY APPROACHES 利用网络药理学、分子对接和实验药理学方法评估依那普利的抗关节炎和免疫抑制潜力
IF 1.6 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-26 DOI: 10.31925/farmacia.2023.5.16
SUMERA  QASIM
The present study validates the anti-arthritic and immunosuppressive attributes of enalapril, an angiotensin-converting enzyme inhibitor (ACEI) with a potential role in major inflammatory pathways. A network pharmacology-based prediction approach was utilised to reveal the possible target genes that can be targeted by enalapril for managing arthritis. In vitro anti-arthritic efficacy of enalapril was assessed using an assay that measures the denaturation of proteins in bovine serum albumin (BSA), egg albumin and the stability of the human red blood cell (HRBC) membrane at a dosage ranging from 100 to 6400 µg/mL. In vivo anti-arthritic efficacy of enalapril at doses of 2, 4 and 8 mg/kg bw was assessed in formaldehyde-induced arthritis model. Dinitrochlorobenzene (DNCB)-provoked delayed type hypersensitivity (DTH) and cyclophosphamide-provoked myelosuppression were employed to assess the immunosuppressant capacity of enalapril. Network pharmacology outcomes revealed that the anti-arthritic effects of enalapril targets include tumour necrosis factor (TNF), matrix metalloproteinase 9 (MMP-9) and caspase 3 (CASP3). Molecular docking of enalapril with these three targets also validates the strong interaction between them. Enalapril markedly inhibited protein denaturation in egg albumin and bovine serum albumin (BSA) assays and stabilised RBC haemolysis exposed to hypotonic media. Likewise, enalapril demonstrated a dose-dependent inhibition of paw oedema provoked by formaldehyde. In the DTH assay, enalapril significantly reduced skin thickness compared to the negative control group and exhibited potent immunosuppressant potential in cyclophosphamide-induced myelosuppression. Based on the outcomes of the current study, it can be predicted that enalapril has anti-arthritic attributes that might be due to its immunosuppressive potential
依那普利是一种血管紧张素转换酶抑制剂(ACEI),在主要炎症通路中具有潜在作用,本研究验证了依那普利的抗关节炎和免疫抑制特性。利用基于网络药理学的预测方法,揭示了依那普利可用于治疗关节炎的靶基因。依那普利的体外抗关节炎疗效是通过一种测定牛血清白蛋白(BSA)、鸡蛋白蛋白中蛋白质变性以及人红血球(HRBC)膜稳定性的试验来评估的,其剂量范围为 100 至 6400 微克/毫升。在甲醛诱导的关节炎模型中,以 2、4 和 8 毫克/千克体重的剂量评估了依那普利的体内抗关节炎功效。采用二硝基氯苯(DNCB)诱发的迟发型超敏反应(DTH)和环磷酰胺诱发的骨髓抑制来评估依那普利的免疫抑制能力。网络药理学结果显示,依那普利的抗关节炎作用靶点包括肿瘤坏死因子(TNF)、基质金属蛋白酶 9(MMP-9)和卡巴酶 3(CASP3)。依那普利与这三个靶点的分子对接也验证了它们之间的强相互作用。依那普利明显抑制了鸡蛋白蛋白和牛血清白蛋白(BSA)测定中的蛋白质变性,并稳定了暴露在低渗介质中的红细胞溶血。同样,依那普利对甲醛引起的爪水肿也有剂量依赖性抑制作用。在 DTH 试验中,与阴性对照组相比,依那普利能显著减少皮肤厚度,并在环磷酰胺诱导的骨髓抑制中表现出强大的免疫抑制潜力。根据目前的研究结果,可以预测依那普利具有抗关节炎的特性,这可能是由于它具有免疫抑制潜能。
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引用次数: 0
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