Racemic xanthine and dihydroxydopamine conjugates from Cyclopelta parva and their COX-2 inhibitory activity

Racemic xanthine and dihydroxydopamine conjugates from Cyclopelta parva and their COX-2 inhibitory activity
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Cyclopelta parva 的外消旋黄嘌呤和二羟基多巴胺缀合物及其 COX-2 抑制活性

DOI:
10.1016/j.fitote.2020.104534
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发表时间:
2020-04-01
期刊:
影响因子:
3.4
通讯作者:
Cheng, Yong-Xian
Cheng, Yong-Xian
中科院分区:
医学3区
文献类型:
--
作者:
Li, Juan;Li, Yan-Peng;Cheng, Yong-Xian

文献摘要

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Seven new compounds including three pairs of enantiomeric xanthine analogues (1-3), a pair of enantiomeric hypoxanthine analogue (4), and three pairs of enantiomeric N-acetyldopamine dimers (6-8), together with a known one (5) were isolated from the insect Cyclopelta parva. Their structures including absolute configurations were assigned by using spectroscopic and computational methods. Chiral HPLC was used to separate racemic 1-8. Biological evaluation found that 6b and 7a are potent COX-2 inhibitory agents with IC50 values at 385.2 nM and 868.8 nM respectively.