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牛角瓜乳胶对改善发热生化特征的体内疗效及可能机制

In Vivo Efficacy of Latex from Calotropis procera in Ameliorating Fever-Biochemical Characteristics and Plausible Mechanism.

作者信息

Kumar Vijay L, Guruprasad B, Fatmi Syed Meraj A, Chaudhary Priyanka, Alencar Nylane Maria Nunes, Lima-Filho José Vitor Moreira, Ramos Márcio Viana

机构信息

Department of Pharmacology, All India Institute of Medical Sciences, Ansari Nagar, New Delhi, 110 029, India.

Departamento de Fisiologia e Farmacologia, Universidade Federal do Ceará, Campus do Porangabu, Fortaleza, CE, CEP 60430-270, Brazil.

出版信息

Appl Biochem Biotechnol. 2017 Jul;182(3):1229-1239. doi: 10.1007/s12010-016-2395-y. Epub 2017 Jan 11.

Abstract

Calotropis procera latex fractions possessing anti-inflammatory property were characterized for their biochemical properties, compared for their efficacy in ameliorating fever in rats and their mechanism of action was elucidated. Aqueous fraction and methanol extract (AqDL and MeDL) were derived from the dried latex (DL) and proteins were separated from the fresh latex (LP). Polyacrylamide gel electrophoresis carried out under denaturing conditions showed the presence of proteins with some similarity in LP and AqDL and both of these fractions exhibited proteinase activity by gelatin zymography. A further analysis revealed that only the LP fraction possesses cysteine proteinase activity. Oral administration of both AqDL and MeDL produced a dose-dependent reduction in body temperature in rats where fever was induced by yeast and their effect was comparable to that of standard drug paracetamol while intravenous administration of LP was not so effective. Both AqDL and MeDL produced a significant reduction in the levels of TNF-α, PGE, and immunoreactivity of COX-2 in the hypothalamus as compared to yeast control group. This study shows that both AqDL and MeDL, the orally effective anti-inflammatory fractions of latex, have therapeutic potential in treating various febrile conditions.

摘要

对具有抗炎特性的牛角瓜乳胶组分进行了生化特性表征,比较了它们在减轻大鼠发热方面的功效,并阐明了其作用机制。水相组分和甲醇提取物(AqDL和MeDL)源自干燥乳胶(DL),蛋白质从新鲜乳胶(LP)中分离出来。在变性条件下进行的聚丙烯酰胺凝胶电泳显示,LP和AqDL中存在一些相似的蛋白质,并且这两种组分通过明胶酶谱法均表现出蛋白酶活性。进一步分析表明,只有LP组分具有半胱氨酸蛋白酶活性。口服AqDL和MeDL均可使酵母诱导发热的大鼠体温呈剂量依赖性降低,其效果与标准药物对乙酰氨基酚相当,而静脉注射LP则效果不佳。与酵母对照组相比,AqDL和MeDL均使下丘脑TNF-α、PGE水平以及COX-2免疫反应性显著降低。本研究表明,AqDL和MeDL这两种乳胶的口服有效抗炎组分在治疗各种发热病症方面具有治疗潜力。

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