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一种来自蓝刺头根部的新型联噻吩。

A New Bithiophene from the Root of Echinops grijsii.

作者信息

Chang Fang-Pin, Chen Chien-Chih, Huang Hui-Chi, Wang Sheng-Yang, Chen Jih-Jung, Yang Chang-Syun, Ou Chung-Yi, Wu Jin-Bin, Huang Guan-Jhong, Kuo Yueh-Hsiung

出版信息

Nat Prod Commun. 2015 Dec;10(12):2147-9.

Abstract

A new bithiophene, 5-(4-hydroxy-3-methoxy-1-butyny)-2,2'-bithiophene (1), and sixteen known thiophenes: 2-(3,4-dihydroxybut-1-ynyl)-5-(penta-1,3-diynyl)thiophene (2), α-terthienyl (3), 5-(3,4-dihydroxybut-1-ynyl)-2,2'-bithiophene (4), 5-acetyl-2,2'-bithiophene (5), 5-formyl-2,2'-bithiophene (6), methyl 2,2'-bithiophene-5-carboxylate (7), 5-(but-3-en-1-ynyl)-2,2'-bithiophene (8), 5-(4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (9), cardopatine (10), isocardopatine (11), 5-(3-hydroxy-4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (12), 5-(3-hydroxymethyl-3-isovaleroyloxyprop-1-ynyl)-2,2'-bithiophene (13), 5-(4-hydroxy-1-butynyl)-2,2'-bithiophene (14), 5-(4-acetoxy-1-butynl)-2,2'-bithiophene (15), 2,2'-bithiophene-5-carboxylic acid (16) and 2-(4-hydroxybut-1-ynyl)-5-(penta-1,3-diynyl)thiophene (17) were isolated from the roots of Echinops grjisii Hance. Among them, compounds 6, 7 and 16 were isolated from a natural source for the first time. Compounds 2, 4 and 14 exhibited significant anti-inflammatory activity against nitrite of LPS-stimulated production in the RAW 264.7 cell line.

摘要

从蓝刺头(Echinops grjisii Hance)的根部分离得到了一种新的联噻吩,即5-(4-羟基-3-甲氧基-1-丁炔基)-2,2'-联噻吩(1),以及十六种已知的噻吩:2-(3,4-二羟基丁-1-炔基)-5-(戊-1,3-二炔基)噻吩(2)、α-三联噻吩(3)、5-(3,4-二羟基丁-1-炔基)-2,2'-联噻吩(4)、5-乙酰基-2,2'-联噻吩(5)、5-甲酰基-2,2'-联噻吩(6)、2,2'-联噻吩-5-羧酸甲酯(7)、5-(丁-3-烯-1-炔基)-2,2'-联噻吩(8)、5-(4-异戊酰氧基丁-1-炔基)-2,2'-联噻吩(9)、卡多帕汀(10)、异卡多帕汀(11)、5-(3-羟基-4-异戊酰氧基丁-1-炔基)-2,2'-联噻吩(12)、5-(3-羟甲基-3-异戊酰氧基丙-1-炔基)-2,2'-联噻吩(13)、5-(4-羟基-1-丁炔基)-2,2'-联噻吩(14)、5-(4-乙酰氧基-1-丁炔基)-2,2'-联噻吩(15)、2,2'-联噻吩-5-羧酸(16)以及2-(4-羟基丁-1-炔基)-5-(戊-1,3-二炔基)噻吩(17)。其中,化合物6、7和16首次从天然来源中分离得到。化合物2、4和14对RAW 264.7细胞系中脂多糖刺激产生的亚硝酸盐具有显著的抗炎活性。

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