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Two New Thymol Derivatives from the Roots of Ageratina adenophora

2018-11-23 本站

题目:Two New Thymol Derivatives from the Roots of Ageratina adenophora

期刊:Molecules

作者:Li-Mei Dong 1,2,3, Mei Zhang 1,5,Qiao-Lin Xu4, Qiang Zhang 1,3, Bi Luo1,3, Qing-Wen Luo1,3, Wen-Bin Liu 1,3, Jian-Wen Tan 1

单位:1.Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou 510650, China ; 2.State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources/Guangdong Key Laboratory for Innovative Development and Utilization of Forest Plant Germplasm, College of Forestry and Landscape Architecture, South China Agricultural University, Guangzhou 510642, China;3.College of Life Sciences, University of Chinese Academy of Sciences, Beijing 100049, China;  4.Guangdong Provincial Key Laboratory of Bio-Control for the Forest Disease and Pest, Guangdong Academy of Forestry, Guangzhou 510520, China Presently work at Beijing Center for Physical and Chemical Analysis, Beijing Key Laboratory of Organic Materials Testing Technology & Quality Evaluation, Beijing 100089, China.  5.Presently work at Beijing Center for Physical and Chemical Analysis, Beijing Key Laboratory of Organic Materials Testing Technology & Quality Evaluation, Beijing 100089, China.

摘要: Two new thymol derivatives, 7,9-diisobutyryloxy-8-ethoxythymol (1) and 7-acetoxy-8-methoxy-9-isobutyryloxythymol (2), were isolated from fresh roots of Ageratina adenophora, together with four known compounds, 7,9-di-isobutyryloxy-8-methoxythymol (3), 9-oxoageraphorone (4), (−)-isochaminic acid (5) and (1α,6α)-10-hydroxycar-3-ene-2-one (6). Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the roots of A. adenophora for the first time. All the compounds were tested for their in vitro antibacterial activity toward three Gram-positive and two Gram-negative bacterial strains. Thymol derivatives 1–3 only selectively showed slight in vitro bacteriostatic activity toward three Gram-positive bacteria. The two known carene-type monoterpenes 5 and 6 were found to show moderate in vitro antibacterial activity against all five tested bacterial strains, with MIC values from 15.6 to 62.5 μg/mL. In addition, compounds 5 and 6 were further revealed to show in vitro cytotoxicity against human tumor A549, HeLa and HepG2 cell lines, with IC50 values ranging from 18.36 to 41.87 μM. However, their cytotoxic activities were inferior to those of reference compound adriamycin.

关键词:Ageratina adenophora,thymol derivatives,monoterpenes, antibacterial,cytotoxicity