Euphane and Tirucallane Triterpenes with Trypanocidal Activity from .

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.

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Publication Details

Journal
Open Access CRIS of the University of Bern
Published
2024-09-27
DOI
https://doi.org/10.48620/76140
Primary Topic
Genomic variations and chromosomal abnormalities
Type
article
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article

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from .

Open Access CRIS of the University of Bern
Genomic variations and chromosomal abnormalities
article

Euphane and Tirucallane Triterpenes with Trypanocidal Activity from .

article en

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.

Open Access CRIS of the University of Bern
Institute of Molecular Medicine (IN)
Openalex Percentile: Top 60%
Genomic variations and chromosomal abnormalities
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