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

Molecules

Beatrice N. Irungu¹  Jennifer A. Orwa¹  Amra Gruhonjic⁵  Paul A. Fitzpatrick⁵  Göran Landberg⁵  Francis Kimani³  Jacob Midiwo²  Máté Erdélyi⁴ 

[1] Kenya Medical Research Institute, Centre for Traditional Medicine and Drug Research, P.O. Box 54840-00200, Nairobi 00200, Kenya; E-Mails:;Department of Chemistry, University of Nairobi, P.O. Box 30197-00100, Nairobi 00100, Kenya; E-Mail:;Kenya Medical Research Institute, Centre for Biotechnology Research and Development, P.O. Box 54840-00200, Nairobi 00200, Kenya; E-Mail:;Department of Chemistry and Molecular Biology, University of Gothenburg, Gothenburg SE-412 96, Sweden;Sahlgrenska Cancer Centre, University of Gothenburg, Gothenburg SE-405 30, Sweden; E-Mails:

关键词: Ekebergia capensis;    tritepenoid;    antiplasmodial;    cytotoxicity;    Vero;    4T1;    HEp2;    MDA-MB-231;    3-oxo-12β-hydroxy-oleanan-28;    13β-olide;   

DOI  :  10.3390/molecules190914235

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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