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来自. 的具有杀变形虫活性的 euphane 和 tirucallane 三萜

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from .

机构信息

Department of Pharmacognosy, University of Szeged, Eötvös u. 6, 6720 Szeged, Hungary.

University of Belgrade, Faculty of Chemistry, Studentski trg 12-16, 11158 Belgrade, Serbia.

出版信息

J Nat Prod. 2024 Sep 27;87(9):2281-2291. doi: 10.1021/acs.jnatprod.4c00730. Epub 2024 Sep 14.

Abstract

The phytochemical investigation of resulted in the isolation of 15 previously undescribed triterpenoids (desmondiins A, C-P) and 8 already described compounds. The structures of the isolated compounds were determined by extensive spectroscopic analyses. The compounds were identified as tirucallane and euphane triterpenes based on 7-keto-8-ene, 11-keto-8-ene, or 7,11-diketo-8-ene skeletons. Additionally, the selective trypanocidal activities of these compounds against were evaluated. Desmondiins A, C, D, F, H, and M exhibited IC values in the range of 3-5 μM, and selectivity indices between 5-9, against epimastigotes over the host cell (RAW264.7 macrophages). Furthermore, desmondiin A efficiently inhibited amastigote replication in host cells (IC = 2.5 ± 0.3 μM), which was comparable to that of the positive control, benznidazole (3.6 ± 0.4 μM). Overall, the isolated euphane and tirucallane triterpenoids could act as antichagasic lead scaffolds.

摘要

对 进行的植物化学研究导致分离出 15 种以前未描述的三萜类化合物(desmondiins A、C-P)和 8 种已描述的化合物。通过广泛的光谱分析确定了分离化合物的结构。这些化合物基于 7-酮-8-烯、11-酮-8-烯或 7,11-二酮-8-烯骨架被鉴定为三萜烷和 euphane 三萜类。此外,还评估了这些化合物对 的选择性抗锥虫活性。Desmondiins A、C、D、F、H 和 M 对 滋养体的 IC 值在 3-5 μM 范围内,对宿主细胞(RAW264.7 巨噬细胞)的选择性指数在 5-9 之间。此外,desmondiin A 有效地抑制了宿主细胞中的无鞭毛体复制(IC = 2.5 ± 0.3 μM),与阳性对照苯并咪唑(3.6 ± 0.4 μM)相当。总体而言,分离出的 euphane 和三萜烷三萜类化合物可能作为抗恰加斯病的先导支架。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e5f/11443485/46e17a9ce078/np4c00730_0001.jpg

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