期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 1, 页码 166-174出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.10.022
关键词
Xanthine oxidase; Urate transporter 1; Anti-hyperuricemic; Uricosuric; Curcumin derivatives
资金
- National Natural Science Foundation of China [81202573]
- Suzhou Science & Technology Foundation [SYS201665]
- PAPD (Priority Academic Program Development of Jiangsu Higher Education Institutions)
A series of curcumin derivatives as potent dual inhibitors of xanthine oxidase (XOD) and urate transporter 1 (URAT1) was discovered as anti-hyperuricemic agents. These compounds proved efficient effects on anti-hyperuricemic activity and uricosuric activity in vivo. More importantly, some of them exhibited proved efficient effects on inhibiting XOD activity and suppressing uptake of uric acid via URAT1 in vitro. Especially, the treatment of 4d was demonstrated to improve uric acid over-production and under-excretion in oxonate-induced hyperuricemic mice through regulating XOD activity and URAT1 expression. Docking study was performed to elucidate the potent XOD inhibition of 4d. Compound 4d may serve as a tool compound for further design of anti-hyperuricemic drugs targeting both XOD and URAT1. (C) 2016 Elsevier Ltd. All rights reserved.
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