期刊
MOLECULES
卷 19, 期 2, 页码 1732-1747出版社
MDPI AG
DOI: 10.3390/molecules19021732
关键词
Endiandra kingiana; lauraceae; endiandric acids; kingianic acids; anti-apoptotic proteins; Bcl-xL; Mcl-1
资金
- Bright Spark Unit
- University of Malaya, Malaysia
- French Embassy in Malaysia
- University of Malaya [PV050/2012A, RP001-2012B, RP001A-13BIO]
- Agence National de la Recherche (ANR) [ANR-2010-JCJC-702-1]
- ICSN, CNRS
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 mu M, and compounds 3, 6 and 9 exhibited weak binding affinity for the anti-apoptotic protein Mcl-1.
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