Endiandric Acid Analogues from Beilschmiedia ferruginea as Dual Inhibitors of Bcl-xL/Bak and Mcl-1/Bid Interactions
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- 作者：C茅cile Apel ; Charlotte G茅ny ; Vincent Dumontet ; Nicolas Birlirakis ; Fanny Roussi ; Van Cuong Pham ; Huong Doan Thi Mai ; Van Hung Nguyen ; Van Minh Chau ; Marc Litaudon
- 刊名：Journal of Natural Products
- 出版年：2014
- 出版时间：June 27, 2014
- 年：2014
- 卷：77
- 期：6
- 页码：1430-1437
- 全文大小：356K
- ISSN：1520-6025
文摘
A rapid screening by 1H and 1H鈥?sup>13C HSQC NMR spectroscopy of EtOAc extracts of Endiandra and Beilschmiedia species allowed the selection of Beilschmiedia ferruginea leaves and flowers extract for a chemical investigation, leading to the isolation of 11 new tetracyclic endiandric acid analogues, named ferrugineic acids A鈥揔 (1鈥?b>11). Their structures were determined by 1D and 2D NMR spectroscopic analysis in combination with HRMS data. These compounds were assayed for Bcl-xL and Mcl-1 binding affinities. Ferrugineic acids B, C, and J (2, 3, and 10) exhibited significant binding affinity for both antiapoptotic proteins Bcl-xL (Ki = 19.2, 12.6, and 19.4 渭M, respectively) and Mcl-1 (Ki = 14.0, 13.0, and 5.2 渭M, respectively), and ferrugineic acid D (4) showed only significant inhibiting activity for Mcl-1 (Ki = 5.9 渭M).