来自膜叶红厚壳茎的视黄酸X受体α转录抑制剂。

RXRα transcriptional inhibitors from the stems of Calophyllum membranaceum.

作者信息

Ming Meng, Zhang Xue, Chen Hai-Feng, Zhu Ling-Juan, Zeng De-Quan, Yang Jian, Wu Guang-Xun, Wu Yu-Zhuo, Yao Xin-Sheng

机构信息

College of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

出版信息

Fitoterapia. 2016 Jan;108:66-72. doi: 10.1016/j.fitote.2015.11.001. Epub 2015 Nov 11.

DOI:10.1016/j.fitote.2015.11.001

PMID:26569353

Abstract

Bioassay-guided fractionation of the 60% ethanol extract of the stems of Calophyllum membranaceum using the RXRα transcription activation assay led to the isolation of two new chromanones, calopolyanic acid methyl ester (1) and isopinetoric acid methyl ester (2), two new xanthones, calophylixanthones A-B (3-4), and one new C-glycoside, calophymembranside C (5), along with 13 known compounds. Their structures were elucidated on the basis of extensive spectroscopic data. Compounds 5, 11 and 18 showed transcriptional inhibitory activity of RXRα with 50% inhibitory concentration (IC50) values of 29.95 ± 1.08, 31.06 ± 9.02, and 25.88 ± 1.62 μM, respectively.

摘要

使用视黄酸X受体α（RXRα）转录激活试验对薄叶红厚壳茎的60%乙醇提取物进行生物测定导向的分级分离，得到了两种新的色原酮，即红厚壳聚原酸甲酯（1）和异松脂酸甲酯（2），两种新的呫吨酮，即红厚壳呫吨酮A - B（3 - 4），以及一种新的C - 糖苷，即薄叶红厚壳苷C（5），同时还有13种已知化合物。基于广泛的光谱数据阐明了它们的结构。化合物5、11和18对RXRα表现出转录抑制活性，其50%抑制浓度（IC50）值分别为29.95±1.08、31.06±9.02和25.88±1.62μM。