New flavonoids and methylchromone isolated from the aerial parts of Baeckea frutescens and their inhibitory activities against cyclooxygenases-1 and -2  

作　　者：ZHOU Jun-Neng YAN Ming GAO Peng HOU Ji-Qin PHAM Thi-Anh WANG Hao 

机构地区：[1]State Key Laboratory of Natural Medicines,Department of Natural Medicinal Chemistry,China Pharmaceutical University [2]Jiangsu Key Laboratory of Drug Screening,China Pharmaceutical University

出　　处：《Chinese Journal of Natural Medicines》2018年第8期615-620,共6页中国天然药物（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.81573309)

摘　　要：In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-O-galloyl)-α-L-arabinofuranoside(1),6-methylquercetin 7-O-β-D-glucopyranoside(2),one new methylchromone glycoside,7-O-(4',6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone(3),together with three known compounds(4-6).The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^(-1) and ranging from 1.01 to 2.27 μmol·L^(-1),respectively.In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-（5＇-O-galloyl）-α-L-arabinofuranoside（1）,6-methylquercetin 7-O-β-D-glucopyranoside（2）,one new methylchromone glycoside,7-O-（4＇,6＇-digalloyl）-β-D-glucopyranosyl-5-hydroxy-2-methylchromone（3）,together with three known compounds（4-6）.The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^（-1） and ranging from 1.01 to 2.27 μmol·L^（-1）,respectively.

关 键 词：Baeckea frutescens Flavonoid Methylchromone CYCLOOXYGENASE-1 CYCLOOXYGENASE-2 

分 类 号：R284.1[医药卫生—中药学]