AI Article Synopsis
- The crude extract of Brucea javanica demonstrated strong inhibitory effects against Trypanosoma evansi, a parasite responsible for certain diseases.
- Bruceines A, C, and bruceantinol were identified as the most effective compounds among isolated quassinoids.
- Structural analysis showed that the free hydroxyl groups at specific positions (C-3, C-11, C-12) are crucial for their antitrypanosomal activity, with C-11 and C-12 being more critical than C-3, while C-4' does not significantly influence the activity.
Article Abstract
The crude extract of Brucea javanica showed strong in vitro inhibitory activity against Trypanosoma evansi. Among the isolated quassinoids, bruceines A, C, and bruceantinol were found to be the most potent compounds against T. evansi. To gain a deeper understanding of the relationship between the free hydroxyl groups and the activity, several O-acetylated derivatives of bruceines A and C were synthesized and their in vitro antitrypanosomal activities against trypomastigotes of T. evansi were examined and compared with those of the original compounds. The following structure-activity relationships were observed: (1) the free hydroxyl groups at positions C-3, C-11, and C-12 are essential for antitrypanosomal activity; (2) the C-11 and C-12 hydroxyl groups are more important for the activity than the enolic hydroxyl group at C-3, and; (3) the free hydroxyl group at C-4' of bruceine C does not have any significant effect on the activity.
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| http://dx.doi.org/10.1007/s11418-011-0571-5 | DOI Listing |
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