Kingianins O-Q: Pentacyclic polyketides from Endiandra kingiana as inhibitor of Mcl-1/Bid interaction

Azmi, M.N. and Péresse, T. and Remeur, C. and Chan, G. and Roussi, F. and Litaudon, M. and Awang, Khalijah (2016) Kingianins O-Q: Pentacyclic polyketides from Endiandra kingiana as inhibitor of Mcl-1/Bid interaction. Fitoterapia, 109. pp. 190-195. ISSN 0367-326X

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Official URL: https://doi.org/10.1016/j.fitote.2016.01.004

Abstract

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-Q were assayed for Mcl-1 binding affinity. Kingianins G and H were found to be potent inhibitors of Mcl-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.

Item Type: Article
Uncontrolled Keywords: Endiandra kingiana; Kingianins; Lauraceae; Anti-apoptotic protein; Mcl-1/Bid
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
Divisions: Faculty of Science > Dept of Chemistry
Depositing User: Ms. Juhaida Abd Rahim
Date Deposited: 04 Dec 2017 04:35
Last Modified: 01 Mar 2019 09:13
URI: http://eprints.um.edu.my/id/eprint/18418

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