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曼尼吲哚,一种来源于 和 的吲哚衍生物,具有抗血吸虫和酶活性。

Manniindole, an indole derivative from the roots of and combined antischistosomal and enzymatic activities.

机构信息

Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, Yaoundé, Cameroon.

Laboratoire de Chimie Bio-Fonctionnelle, UMR 7199 CNRS, Faculty of Pharmacy, University of Strasbourg, Illkirch Cedex, France.

出版信息

Nat Prod Res. 2021 Dec;35(24):5665-5673. doi: 10.1080/14786419.2020.1824227. Epub 2020 Sep 28.

DOI:10.1080/14786419.2020.1824227
PMID:32985247
Abstract

A new alkaloid, manniindole , together with four known compounds: aristolactam AII , aristolactam BII , piperolactam D and polycarpol were isolated from the crude extract EtOH-HO (8:2) of the roots of by chromatographic separation. The structure elucidation was performed on the basis of a spectroscopic analysis (IR, HRESI MS, 1D and 2D NMR) as well as a comparison of their spectral data with those reported in the literature. For the first time, the crude extract and those isolated compounds were evaluated for their anti-schistosomal activity against and for cytotoxicity activity against Huh7 and A549 cells. Furthermore, they were also tested on the recent characterized NAD catabolizing enzyme (NACE) for their impact on this enzyme which is localized on the outer surface of the adult parasite. Compound displayed quite good worm killing capability, while showed significant inhibition of NACE.

摘要

从曼陀罗根的粗提物 EtOH-HO(8:2)中,通过色谱分离,分离得到了一种新的生物碱曼尼吲哚,以及四种已知化合物:aristolactam AII、aristolactam BII、piperolactam D 和 polycarpol。结构鉴定是基于光谱分析(IR、HRESI MS、1D 和 2D NMR)以及与文献报道的光谱数据的比较。首次评估了粗提物和分离得到的化合物对 和 Huh7 和 A549 细胞的抗血吸虫活性以及细胞毒性活性。此外,还在最近表征的 NAD 分解代谢酶(NACE)上测试了它们对这种酶的影响,该酶位于成虫寄生虫的外表面。化合物 显示出相当好的杀蠕虫能力,而 对 NACE 显示出显著的抑制作用。

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