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Sidan uppdaterades: 2012-09-11 15:12
| Författare |
Stephen S. Nyandoro Gasper Maeda J. J. E. Munissi Amra Gruhonjic Paul A. Fitzpatrick S. Lindblad S. Duffy J. Pelletier F. F. Pan R. Puttreddy V. M. Avery Mate Erdelyi |
|---|---|
| Publicerad i | Molecules |
| Volym | 24 |
| Nummer/häfte | 15 |
| Publiceringsår | 2019 |
| Publicerad vid |
Sahlgrenska Cancer Center Institutionen för kemi och molekylärbiologi |
| Språk | en |
| Länkar |
dx.doi.org/10.3390/molecules2415274... |
| Ämnesord | Cleistochlamys kirkii, Annonaceae, benzopyranyl sesquiterpene, cleistonol, antiplasmodial activity, malaria, cytotoxicity, cadinane-type sesquiterpenes, absolute-configuration, circular-dichroism, uvaria, constituents, flavonoids, roots, Biochemistry & Molecular Biology, Chemistry |
| Ämneskategorier | Biokemi och molekylärbiologi |
Phytochemical investigations of ethanol root bark and stem bark extracts of Cleistochlamys kirkii (Benth.) Oliv. (Annonaceae) yielded a new benzopyranyl cadinane-type sesquiterpene (cleistonol, 1) alongside 12 known compounds (2-13). The structures of the isolated compounds were established from NMR spectroscopic and mass spectrometric analyses. Structures of compounds 5 and 10 were further confirmed by single crystal X-ray crystallographic analyses, which also established their absolute stereochemical configuration. The ethanolic crude extract of C. kirkii root bark gave 72% inhibition against the chloroquine-sensitive 3D7-strain malaria parasite Plasmodium falciparum at 0.01 mu g/mL. The isolated metabolites dichamanetin, (E)-acetylmelodorinol, and cleistenolide showed IC50 = 9.3, 7.6 and 15.2 mu M, respectively, against P. falciparum 3D7. Both the crude extract and the isolated compounds exhibited cytotoxicity against the triple-negative, aggressive breast cancer cell line, MDA-MB-231, with IC50 = 42.0 mu g/mL (crude extract) and 9.6-30.7 mu M (isolated compounds). Our findings demonstrate the potential applicability of C. kirkii as a source of antimalarial and anticancer agents.
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