Euphane and Tirucallane Triterpenes with Trypanocidal Activity from <i>Euphorbia desmondii</i>

The phytochemical investigation of <i>Euphorbia desmondii</i> 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 <i>Trypanosoma cruzi</i> were evaluated. Desmondiins A, C, D, F, H, and M exhibited IC<sub>50</sub> values in the range of 3-5 μM, and selectivity indices between 5-9, against <i>T. cruzi</i> epimastigotes over the host cell (RAW264.7 macrophages). Furthermore, desmondiin A efficiently inhibited amastigote replication in host cells (IC<sub>50</sub> = 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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Publication Details

Journal
Journal of Natural Products
Published
2024-09-14
DOI
https://doi.org/10.1021/acs.jnatprod.4c00730
Citations
1
Primary Topic
Bioactive Natural Diterpenoids Research
Type
article
Field-Weighted Citation Impact
0.23

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article

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from Euphorbia desmondii

Kaushavi Cholke, Anita Barta, Jürg Gertsch, Attila Hunyadi et al.
1 citations
Journal of Natural Products
Bioactive Natural Diterpenoids Research
0.23
article

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from Euphorbia desmondii

Kaushavi Cholke, Anita Barta, Jürg Gertsch, Attila Hunyadi, Gordana Krstić, Umar Shehu Gallah, Róbert Berkecz, Judit Hohmann, Dóra Rédei, Muhammad Bello Saidu
article en
1 citations

Abstract

The phytochemical investigation of <i>Euphorbia desmondii</i> 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 <i>Trypanosoma cruzi</i> were evaluated. Desmondiins A, C, D, F, H, and M exhibited IC<sub>50</sub> values in the range of 3-5 μM, and selectivity indices between 5-9, against <i>T. cruzi</i> epimastigotes over the host cell (RAW264.7 macrophages). Furthermore, desmondiin A efficiently inhibited amastigote replication in host cells (IC<sub>50</sub> = 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.

Journal of Natural ProductsVol. 87(9)
University of Bern (CH), University of Szeged (HU), University of Belgrade (RS), National Institute for Pharmaceutical Research and Development (NG)
Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, National Research, Development and Innovation Office
Openalex Percentile: Top 43%
Bioactive Natural Diterpenoids Research
0.23
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