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新型柠檬苦素衍生物作为具有高水溶性的抗炎和镇痛剂的合成及药理学评价

Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility.

作者信息

Yang Yun, Wang Xinhui, Zhu Qihua, Gong Guoqing, Luo Danmeng, Jiang Aidou, Yang Liyan, Xu Yungen

机构信息

Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, Jiangsu 21009, China.

Department of Pharmacology, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.

出版信息

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1851-5. doi: 10.1016/j.bmcl.2014.02.003. Epub 2014 Feb 10.

DOI:10.1016/j.bmcl.2014.02.003
PMID:24569111
Abstract

A novel series of water-soluble derivatives of limonin were synthesized by introducing various tertiary amines onto the C (7)-position of limonin. Ten target compounds were characterized and screened for their anti-inflammatory and analgesic activity in vivo. Compound 3c exhibited the strongest analgesic and anti-inflammatory activity among the limonin and its derivatives tested; its analgesic activity is more potent than that of aspirin and its anti-inflammatory activity is stronger than that of naproxen.

摘要

通过将各种叔胺引入到柠檬苦素的C（7）位，合成了一系列新型的柠檬苦素水溶性衍生物。对10种目标化合物进行了表征，并对其体内抗炎和镇痛活性进行了筛选。在测试的柠檬苦素及其衍生物中，化合物3c表现出最强的镇痛和抗炎活性；其镇痛活性比阿司匹林更强，抗炎活性比萘普生更强。

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