Euphane and Tirucallane Triterpenes with Trypanocidal Activity from Euphorbia desmondii

大戟科植物大戟中的具有锥虫活性的三萜和蒂鲁卡拉烯

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作者:Muhammad Bello Saidu, Gordana Krstić, Anita Barta, Attila Hunyadi, Róbert Berkecz, Umar Shehu Gallah, Kaushavi Cholke, Jürg Gertsch, Dóra Rédei, Judit Hohmann

Abstract

The phytochemical investigation of Euphorbia desmondii 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 Trypanosoma cruzi were evaluated. Desmondiins A, C, D, F, H, and M exhibited IC50 values in the range of 3-5 μM, and selectivity indices between 5-9, against T. cruzi epimastigotes over the host cell (RAW264.7 macrophages). Furthermore, desmondiin A efficiently inhibited amastigote replication in host cells (IC50 = 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.

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