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.
Authors
- Kaushavi Cholke
- Anita Barta
- Jürg Gertsch (ORCID: https://orcid.org/0000-0003-0978-1555)
- Attila Hunyadi (ORCID: https://orcid.org/0000-0003-0074-3472)
- Gordana Krstić (ORCID: https://orcid.org/0000-0001-6945-6178)
- Umar Shehu Gallah
- Róbert Berkecz (ORCID: https://orcid.org/0000-0002-9076-2177)
- Judit Hohmann (ORCID: https://orcid.org/0000-0002-2887-6392)
- Dóra Rédei (ORCID: https://orcid.org/0000-0002-5013-247X)
- Muhammad Bello Saidu (ORCID: https://orcid.org/0000-0002-4482-1834)
Institutions
- University of Bern (CH)
- University of Szeged (HU)
- University of Belgrade (RS)
- National Institute for Pharmaceutical Research and Development (NG)
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
Funders
- Nemzeti Kutatási Fejlesztési és Innovációs Hivatal
- National Research, Development and Innovation Office