title: RXRα transcriptional inhibitors from the stems of Calophyllum membranaceum.
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.
authors.affiliation: 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.
authors.forename: Meng
authors.initials: M
authors.lastname: Ming
authors.affiliation: 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. Electronic address: syzxalice@163.com.
authors.forename: Xue
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, PR China.
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Chen
authors.affiliation: 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.
authors.forename: Ling-Juan
authors.initials: LJ
authors.lastname: Zhu
authors.affiliation: School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, PR China.
authors.forename: De-Quan
authors.initials: DQ
authors.lastname: Zeng
authors.affiliation: 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.
authors.forename: Jian
authors.initials: J
authors.lastname: Yang
authors.affiliation: 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.
authors.forename: Guang-Xun
authors.initials: GX
authors.lastname: Wu
authors.affiliation: 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.
authors.forename: Yu-Zhuo
authors.initials: YZ
authors.lastname: Wu
authors.affiliation: 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; Institute of Traditional Chinese Medicine & Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China. Electronic address: tyaoxs@jnu.edu.cn.
authors.forename: Xin-Sheng
authors.initials: XS
authors.lastname: Yao
mesh_terms: D029759:Calophyllum / Q000737:chemistry*; D002867:Chromones / Q000737:chemistry / Q000302:isolation & purification; D006027:Glycosides; D057809:HEK293 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D009005:Monosaccharides / Q000737:chemistry / Q000302:isolation & purification; D010936:Plant Extracts / Q000737:chemistry*; D018547:Plant Stems / Q000737:chemistry*; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors*; D000072482:Retinoic Acid Receptor alpha; D044004:Xanthones / Q000737:chemistry / Q000302:isolation & purification
chemical_list: C438934:C-glycoside; D002867:Chromones; D006027:Glycosides; D009005:Monosaccharides; D010936:Plant Extracts; C000607071:RARA protein, human; D018168:Receptors, Retinoic Acid; D000072482:Retinoic Acid Receptor alpha; D044004:Xanthones
keywords: C-glycoside; Calophyllum membranaceum; Chromanones; RXRα transcriptional inhibitory activity; Xanthones