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Heterodimeric Diterpenoids Isolated from Euphorbia ebracteolata Roots and Their Inhibitory Effects on α-Glucosidase
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-11-17 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00595 Yunlong Wei 1, 2 , Chao Wang 1 , Zhongbin Cheng 3 , Xiangge Tian 1 , Jingming Jia 2 , Yonglei Cui 1 , Lei Feng 1 , Chengpeng Sun 1 , Baojing Zhang 1 , Xiaochi Ma 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-11-17 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00595 Yunlong Wei 1, 2 , Chao Wang 1 , Zhongbin Cheng 3 , Xiangge Tian 1 , Jingming Jia 2 , Yonglei Cui 1 , Lei Feng 1 , Chengpeng Sun 1 , Baojing Zhang 1 , Xiaochi Ma 1
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Two heterodimeric diterpenoids (1 and 2) comprising abietane lactone and nor-rosane constituent units were isolated from Euphorbia ebracteolata roots. Compound 1 exhibited a moderate inhibitory effect on α-glucosidase (IC50 = 7.94 μM), with a Ki value of 10.8 μM. In silico molecular docking has been performed to investigate the inhibition mechanism. Compound 2 inhibited the acetyl transfer activity of Mycobacterium tuberculosis GlmU (IC50 = 41.85 μM), which is a novel tuberculosis treatment target.
中文翻译：
从大戟根中分离的异二聚二萜及其对α-葡萄糖苷酶的抑制作用
从大戟（Euphorbia ebracteolata）根中分离出两个包含二氢枞酸内酯和正戊烷组成单元的异二聚二萜（1和2）。化合物1对α-葡萄糖苷酶表现出中等抑制作用（IC 50 = 7.94μM），K i值为10.8μM。在计算机上已经进行了分子对接以研究抑制机理。化合物2抑制了结核分枝杆菌GlmU的乙酰转移活性（IC 50 = 41.85μM），这是一种新型的结核病治疗靶标。
更新日期：2017-11-17
中文翻译：
从大戟根中分离的异二聚二萜及其对α-葡萄糖苷酶的抑制作用
从大戟（Euphorbia ebracteolata）根中分离出两个包含二氢枞酸内酯和正戊烷组成单元的异二聚二萜（1和2）。化合物1对α-葡萄糖苷酶表现出中等抑制作用（IC 50 = 7.94μM），K i值为10.8μM。在计算机上已经进行了分子对接以研究抑制机理。化合物2抑制了结核分枝杆菌GlmU的乙酰转移活性（IC 50 = 41.85μM），这是一种新型的结核病治疗靶标。
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