天然和合成聚癸二醛衍生物对无鞭毛体、动基体和滋养体的活性。
Activity of natural and synthetic polygodial derivatives against amastigotes, trypomastigotes and epimastigotes.
机构信息
Department of Biology, New Mexico Tech, Socorro, New Mexico, USA.
School of Natural Sciences - Chemistry, University of Tasmania, Hobart, Tasmania, Australia.
出版信息
Nat Prod Res. 2021 Mar;35(5):792-795. doi: 10.1080/14786419.2019.1597350. Epub 2019 Apr 28.
Abstract
Our laboratories have been investigating biological effects of a sesquiterpenoid polygodial and its natural and synthetic analogues. Herein, we report the evaluation of these compounds against the three forms of amastigotes, trypomastigotes and epimastigotes. Although polygodial was found to be poorly active, its natural congener epipolygodial and synthetic Wittig-derived analogues showed low micromolar potency against all three forms of the parasite. Synthetic α,β-unsaturated phosphonate compared favorably with clinically approved drugs benznidazole and nifurtimox, and was effective against trypomastigotes, toward which benznidazole showed no activity.[Formula: see text].
摘要
我们的实验室一直在研究倍半萜聚戈醛及其天然和合成类似物的生物学效应。在此，我们报告了这些化合物对三种形式的无鞭毛体、鞭毛体和滋养体的评估。虽然聚戈醛的活性较差，但它的天然同系物表聚戈醛和合成的威蒂希衍生类似物对寄生虫的三种形式均显示出低微摩尔的效力。合成的α，β-不饱和膦酸酯与临床批准的药物苯并咪唑和硝呋替莫相当，对鞭毛体有效，而苯并咪唑对鞭毛体没有活性。
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