Kingianic Acids A–G, Endiandric Acid Analogues from Endiandra kingiana

Molecules

Mohamad Nurul Azmi³  Charlotte Gény¹  Aurélie Leverrier¹  Marc Litaudon¹  Vincent Dumontet¹  Nicolas Birlirakis¹  Françoise Guéritte¹  Kok Hoong Leong²  Siti Nadiah Abd. Halim³  Khalit Mohamad² 

[1] Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles (ICSN), CNRS, Labex LERMIT, Gif-sur-Yvette Cedex 91198, France; E-Mails:;Department of Pharmacy, Faculty of Medicine, University Malaya, Kuala Lumpur 50603, Malaysia; E-Mails:;Department of Chemistry, Faculty of Science, University Malaya, Kuala Lumpur 50603, Malaysia; E-Mails:

关键词: Endiandra kingiana;    lauraceae;    endiandric acids;    kingianic acids;    anti-apoptotic proteins;    Bcl-xL;    Mcl-1;   

DOI  :  10.3390/molecules19021732

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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