期刊
FITOTERAPIA
卷 109, 期 -, 页码 190-195出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2016.01.004
关键词
Endiandra kingiana; Kingianins; Lauraceae; Anti-apoptotic protein; Mcl-1/Bid
资金
- CNRS-UM
- Associated International Laboratory (LIA) under International French Malaysian Natural Product Laboratory (IFM-NatProLab)
- Bright Spark Unit, University of Malaya, Malaysia
- French Embassy in Malaysia
- University of Malaya [PV050/2012A, SF018-2013, RP001-2012A, RP001-2012B]
- Agence National de la Recherche (ANR)
- [ANR-2010-JCJC-702-1]
- [ANR-10-LABEX-25-01]
A phytochemical study of the EtOAc-soluble part of the methanolic extract of the bark of Endiandra kingiana led to the isolation of three new pentacyclic kingianins as racemic mixtures, kingianins O-Q (1-3), together with the known kingianins A, F, K, L, M and N (4-9), respectively. The structures of the new kingianins 1-3 were determined by 1D and 2D NMR analysis in combination with HRESIMS experiments. Kingianins A-Qwere assayed for Mcl-1 binding affinity. Kingianins G and H were found to be potent inhibitors of Mc1-1/Bid interaction. A structure-activity relationship study showed that potency is very sensitive to the substitution pattern on the pentacyclic core. In addition, in contrast with the binding affinity for Bcl-xL, the levorotatory enantiomers of kingianins G, 'H and J exhibited similar binding affinities for Mcl-1 than their dextrorotatory counterparts, indicating that the two anti-apoptotic proteins have slightly different binding profiles. (C) 2016 Elsevier B.V. All rights reserved.
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