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抗阿米巴原虫和抗贾第鞭毛虫活性的来自用于治疗腹泻的墨西哥鼠尾草属植物的 clerodane 二萜

Antiamoebic and Antigiardial Activity of Clerodane Diterpenes from Mexican Salvia Species Used for the Treatment of Diarrhea.

机构信息

Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORCE, Centro Médico Nacional Siglo XXI, México D. F., México.

Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, México D. F., México.

出版信息

Phytother Res. 2015 Oct;29(10):1600-4. doi: 10.1002/ptr.5421. Epub 2015 Jul 16.

Abstract

Terpenoids from Salvia species have been identified to possess biological properties as antiprotozoal agents. Here, we evaluated the antiamoebic and antigiardial activities of 14 known clerodane and modified clerodane-type diterpenes isolated from five Mexican Salvia species against Entamoeba histolytica and Giardia lamblia, and analyzed the effects of the functionalities in decalin ring or in the whole clerodane framework to visualize the structural requirements necessary to produce an antiprotozoal activity. Among these, linearolactone was the most active clerodane diterpene against both protozoa with IC50 values of 22.9 μM for E. histolytica and of 28.2 μM in the case of G. lamblia. In this context it may be a lead compound for the development of novel therapeutic agent for the treatment of diarrhea and dysentery. The remaining diterpenes assayed showed moderate to weak activity against both protozoa. These findings give support to the use of Salvia species in the traditional medicine from México for the treatment of diarrhea.

摘要

从鼠尾草属植物中分离得到的萜类化合物具有抗原虫作用。本研究评价了从 5 种墨西哥鼠尾草属植物中分离得到的 14 种已知的克罗烷型和修饰型二萜的抗阿米巴原虫和抗贾第鞭毛虫活性,并分析了十氢萘环或整个克罗烷骨架中的官能团对产生抗原虫活性的结构要求的影响。其中,线性内酯是对两种原生动物最具活性的克罗烷二萜,对溶组织内阿米巴的 IC50 值为 22.9 μM,对蓝氏贾第鞭毛虫的 IC50 值为 28.2 μM。在这种情况下,它可能是开发新型治疗腹泻和痢疾药物的先导化合物。其余测定的二萜对两种原生动物均表现出中等至弱的活性。这些发现为墨西哥传统医学中使用鼠尾草属植物治疗腹泻提供了支持。

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