Document Type
Article
Publication Date
1-31-2014
Abstract
A phytochemical investigation of the methanolic extract of the bark of Endiandra kingiana led to the isolation of seven new tetracyclic endiandric acid analogues, kingianic acids A–G (1–7), together with endiandric acid M (8), tsangibeilin B (9) and endiandric acid (10). Their structures were determined by 1D- and 2D-NMR analysis in combination with HRMS experiments. The structure of compounds 9 and 10 were confirmed by single-crystal X-ray diffraction analysis. These compounds were screened for Bcl-xL and Mcl-1 binding affinities and cytotoxic activity on various cancer cell lines. Compound 5 showed moderate cytotoxic activity against human colorectal adeno-carcinoma (HT-29) and lung adenocarcinoma epithelial (A549) cell lines, with IC50 values in the range 15–17 µM, and compounds 3, 6 and 9 exhibited weak binding affinity for the anti-apoptotic protein Mcl-1.
Keywords
Endiandra kingiana, lauraceae, endiandric acids, kingianic acids, anti-apoptotic proteins, Bcl-xL, Mcl-1
Divisions
fac_med
Funders
University of Malaya (PV050/2012A, RP001-2012B and RP001A-13BIO),Agence National de la Recherche (ANR), contract number ANR-2010-JCJC-702-1 and ICSN, CNRS for financial support
Publication Title
Molecules Online
Volume
19
Issue
2
Publisher
Springer Verlag (Germany)