Euphane and Tirucallane Triterpenes with Trypanocidal Activity from Euphorbia desmondii

Saidu, Muhammad Bello and Krstić, Gordana and Barta, Anita and Hunyadi, Attila and Berkecz, Róbert and Gallah, Umar Shehu and Cholke, Kaushavi and Gertsch, Jürg and Rédei, Dóra and Hohmann, Judit (2024) Euphane and Tirucallane Triterpenes with Trypanocidal Activity from Euphorbia desmondii. JOURNAL OF NATURAL PRODUCTS, 87 (9). ISSN 0163-3864

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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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