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对闹羊花碱(1)、小檗碱(2)和泽漆碱(3)这三种季铵类异喹啉生物碱进行了抑制可溶性环氧化物水解酶(sEH)活性的评价。它们表现出相似的抑制活性,IC50值分别为29.6 ± 0.5、33.4 ± 0.8和27.3 ± 0.4 μM。通过酶动力学测定的各自Ki值分别为26.9、46.8和44.5 μM,表明它们通过与sEH非竞争性结合抑制催化反应。计算化学对体外结果的应用揭示了配体可能结合的受体位点。因此,三种生物碱被确定为具有适合开发sEH抑制剂先导化合物的基骨架。
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Jang Hoon Kim
Chong Woon Cho
Mok Hur
SHILAP Revista de lepidopterología
Current Issues in Molecular Biology
Chungnam National University
Rural Development Administration
Korea Institute of Oriental Medicine
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Kim 等人(周五,)研究了这个问题。
www.synapsesocial.com/papers/69d78bead84d071b73f3073b — DOI: https://doi.org/10.3390/cimb44090294
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