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Constituents of the Roots and Leaves of Ekebergia capensis and Their Potential Antiplasmodial and Cytotoxic Activities

Artikel i vetenskaplig tidskrift
Författare Beatrice N. Irungu
Jennifer A. Orwa
Amra Gruhonjic
Paul A. Fitzpatrick
Göran Landberg
Francis Kimani
Jacob Midiwo
Mate Erdelyi
Abiy Yenesew
Publicerad i Molecules
Volym 19
Nummer/häfte 9
Sidor 14235-14246
ISSN 1420-3049
Publiceringsår 2014
Publicerad vid Sahlgrenska Cancer Center
Svenskt NMR-centrum vid Göteborgs universitet
Institutionen för kemi och molekylärbiologi
Sidor 14235-14246
Språk en
Länkar http://dx.doi.org/10.3390/molecule...
Ämnesord Ekebergia capensis; tritepenoid; antiplasmodial; cytotoxicity; Vero; 4T1; HEp2; MDA-MB-231; 3-oxo-12β-hydroxy-oleanan-28,13β-olide
Ämneskategorier Organisk kemi, Läkemedelskemi, Farmaceutisk kemi

Sammanfattning

A new triterpenoid, 3-oxo-12β-hydroxy-oleanan-28,13β-olide (1), and six known triterpenoids 2–7 were isolated from the root bark of Ekebergia capensis, an African medicinal plant. A limonoid 8 and two glycoflavonoids 9–10 were found in its leaves. The metabolites were identified by NMR and MS analyses, and their cytotoxicity was evaluated against the mammalian African monkey kidney (vero), mouse breast cancer (4T1), human larynx carcinoma (HEp2) and human breast cancer (MDA-MB-231) cell lines. Out of the isolates, oleanonic acid (2) showed the highest cytotoxicity, i.e., IC50’s of 1.4 and 13.3 µM against the HEp2 and 4T1 cells, respectively. Motivated by the higher cytotoxicity of the crude bark extract as compared to the isolates, the interactions of oleanonic acid (2) with five triterpenoids 3–7 were evaluated on vero cells. In an antiplasmodial assay, seven of the metabolites were observed to possess moderate activity against the D6 and W2 strains of P. falciparum (IC50 27.1–97.1 µM), however with a low selectivity index (IC50(vero)/IC50(P. falciparum-D6) < 10). The observed moderate antiplasmodial activity may be due to general cytotoxicity of the isolated triterpenoids.

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