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

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.

Orwa, Jennifer A. (författare)
Gruhonjic, AmraGothenburg University,Göteborgs universitet,Sahlgrenska Cancer Center (författare)
Fitzpatrick, Paul A.Gothenburg University,Göteborgs universitet,Sahlgrenska Cancer Center(Swepub:gu)xfitpa (författare)
Landberg, Göran,1963Gothenburg University,Göteborgs universitet,Sahlgrenska Cancer Center(Swepub:gu)xlgora (författare)
Kimani, Francis (författare)
Midiwo, Jacob (författare)
Erdelyi, Mate,1975Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Svenskt NMR-centrum vid Göteborgs universitet,Department of Chemistry and Molecular Biology,Swedish NMR Centre at Göteborg University,organisk kemi(Swepub:uu)mateerde (författare)
Yenesew, Abiy (författare)
Göteborgs universitetSahlgrenska Cancer Center (creator_code:org_t)

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