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Identifying the mechanism of eriosematin E from Eriosema chinense Vogel. For its antidiarrhoeal potential against Shigella flexneri-induced diarrhoea using in vitro, in vivo and in silico models
Microbial Pathogenesis ( IF 3.3 ) Pub Date : 2020-10-18 , DOI: 10.1016/j.micpath.2020.104582
Komal M Parmar 1 , Saurabh K Sinha 2 , Rupali S Prasad 1 , Mohit S Jogi 1 , Damiki Laloo 3 , Mahaveer Dhobi 4 , Shailendra S Gurav 5 , Satyendra K Prasad 1
Affiliation  

The main objective of the present investigation was to mechanistically evaluate the potency of the root extract (EEC), its bioactive chloroform fraction (CEC) and eriosematin E (ECM) isolated from Eriosema chinense against Shigella flexneri-induced sub-chronic model of infectious diarrhoea using in vitro, in vivo, and in silico methods. The in vitro antibacterial activity against pathogenic strain of S. flexneri demonstrated maximum effect of ECM followed by CEC and EEC in inhibiting growth of bacteria. Further, for in vivo evaluation, was carried out by inducing diarrhoea to the rats by administering oral suspension of S. flexneri to the animals, which was followed by treatment for a period of 6 days. EEC at 200, CEC at 100 and ECM at 10 mg/kg, p.o. showed promising effect, where EEC and ECM were found to be more effective showing maximum % protection on 6th day. Results also demonstrated a significant restoration of altered antioxidants, pro-inflammatory cytokines (IL-1β and TNF-α) expression, electrolyte balance, Na+/K+–ATPase activity and was also supported by histopathological examinations. Molecular docking study revealed that, eriosematin E inactivated the protease activity of SepA, a protein secreted by Shigella, which is responsible for disruption of epithelial barrier integrity. Thus, the overall observation confirmed the role of eriosematin E from E. chinense in treatment of Shigella flexneri-induced infectious diarrhoea.



中文翻译:

识别eriosematin电子商务从机制雀脷珠属楸沃格尔。使用体外体内计算机模拟模型对弗氏志贺氏菌引起的腹泻具有止泻作用

本研究的主要目的是机械地评价根提取物(EEC),其生物活性氯仿级分(CEC)和分离自eriosematin E(ECM)的效力雀脷珠属楸针对志贺氏菌flexneri-诱导感染性腹泻的亚慢性模型使用体外体内计算机模拟方法。在体外对抗的致病菌株的抗菌活性弗氏志贺菌表现出随后CEC和EEC在抑制细菌生长的ECM最大效果。另外,为了进行体内评价,通过给予口服混悬液诱导腹泻。将弗氏链球菌感染动物,然后进行6天的治疗。200的EEC,100的CEC和10 mg / kg的ECM表现出良好的效果,其中EEC和ECM在第6天显示出最大的保护百分比,被认为更有效。结果还表明,抗氧化剂,促炎性细胞因子(IL-1β和TNF-α)表达,电解质平衡,Na + / K + -ATPase活性显着恢复,并且得到组织病理学检查的支持。分子对接研究表明,芥子素E灭活了志贺氏菌分泌的蛋白SepA的蛋白酶活性,该酶负责破坏上皮屏障的完整性。因此,总体观察结果证实了中华肠杆菌治疗弗氏志贺氏菌引起的感染性腹泻。

更新日期:2020-10-19
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