Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities
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来自昆虫 Blaps japanensis 的具有 COX-1 和 COX-2 抑制活性的化合物
DOI：
10.1016/j.bmcl.2015.04.085
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发表时间：
2015-06-15
影响因子：
2.7
通讯作者：
Cheng, Yong-Xian
中科院分区：
文献类型：
--
作者：
Yan, Yong-Ming;Li, Li-Ji;Cheng, Yong-Xian
Blapsols A-D (1-4) 是从 Blaps japanensis 中分离出来的四种具有 2,3-二氢苯并[b][1,4]二恶英基团的新化合物，以及五种已知的 N-乙酰多巴胺二聚体 (5-9)。通过光谱和X射线晶体学方法测定了它们的结构，包括(+)-1的绝对构型。使用手性 HPLC 分离化合物 1-4 的 (-)- 和 (+)-对映异构体，这些化合物是从该昆虫中作为外消旋混合物分离出来的。所有化合物均对 COX-2 具有抑制作用，IC50 值在 1.3-17.8 muM 范围内。 (C) 2015 Elsevier Ltd. 保留所有权利。
Blapsols A-D (1-4), four new compounds possessing a 2,3-dihydrobenzo[b][1,4]dioxin group, together with five known N-acetyldopamine dimers (5-9), were isolated from Blaps japanensis. Their structures including the absolute configuration of (+)-1 were determined by means of spectroscopic and X-ray crystallographic methods. Chiral HPLC was used to separate (-)- and (+)-enantiomers of compounds 1-4, which were isolated from this insect as racemic mixtures. All the compounds were found to have inhibitory effects towards COX-2 with IC50 values in the range of 1.3-17.8 mu M. (C) 2015 Elsevier Ltd. All rights reserved.