CN: 32-1845/R
ISSN: 2095-6975
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WANG Shao-Chi, YANG Yun, LIU Jing, JIANG Ai-Dou, CHU Zhao-Xing, CHEN Si-Ying, GONG Guo-Qing, HE Guang-Wei, XU Yun-Gen, ZHU Qi-Hua. Discovery of novel limonin derivatives as potent anti-inflammatory and analgesic agents[J]. Chinese Journal of Natural Medicines, 2018, 16(3): 231-240

Discovery of novel limonin derivatives as potent anti-inflammatory and analgesic agents

WANG Shao-Chi1,2, YANG Yun2, LIU Jing1,2, JIANG Ai-Dou3, CHU Zhao-Xing4, CHEN Si-Ying3, GONG Guo-Qing3, HE Guang-Wei4, XU Yun-Gen1,2, ZHU Qi-Hua1,2
1 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China;
2 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
3 Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China;
4 Hefei YiGong Pharmaceutical Co., Ltd., Hefei 230088, China
Abstract:
Novel series of limonin derivatives (V-A-1-V-A-8, V-B-1-V-B-8) were synthesized by adding various tertiary amines onto the C (7)-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.
Key words:    Limonin derivatives    Analgesic    Anti-inflammatory   
Received: 2017-06-20   Revised:
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Articles by WANG Shao-Chi
Articles by YANG Yun
Articles by LIU Jing
Articles by JIANG Ai-Dou
Articles by CHU Zhao-Xing
Articles by CHEN Si-Ying
Articles by GONG Guo-Qing
Articles by HE Guang-Wei
Articles by XU Yun-Gen
Articles by ZHU Qi-Hua
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