来自日本扁谷盗的具有COX - 1和COX - 2抑制活性的化合物。
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities.
作者信息
Yan Yong-Ming, Li Li-Ji, Qin Xiao-Chu, Lu Qing, Tu Zheng-Chao, Cheng Yong-Xian
机构信息
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China; University of Chinese Academy of Sciences, Yuquan Road 19, Beijing 100049, People's Republic of China.
Kunming Institute of Medical Sciences, Kunming 650011, People's Republic of China.
出版信息
Bioorg Med Chem Lett. 2015 Jun 15;25(12):2469-72. doi: 10.1016/j.bmcl.2015.04.085. Epub 2015 Apr 30.
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 1.3-17.8μM.
从日本扁甲中分离出了布拉普索 A - D（1 - 4）这四种具有 2,3 - 二氢苯并[b][1,4]二噁英基团的新化合物，以及五种已知的 N - 乙酰多巴胺二聚体（5 - 9）。通过光谱和 X 射线晶体学方法确定了它们的结构，包括(+)-1 的绝对构型。采用手性高效液相色谱法分离了化合物 1 - 4 的(-)-和(+)-对映体，这些化合物最初是以外消旋混合物形式从这种昆虫中分离得到的。发现所有化合物对 COX - 2 均有抑制作用，IC50 值在 1.3 - 17.8μM 范围内。
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