摘要
以熊果酸、对羟基苯乙酮和芳醛为原料,合成了一系列熊果酸衍生物-查耳酮缀合物,均未见文献报道,其结构均通过IR、~1H NMR、^(13)C NMR和HR-MS进行确认。通过建立二甲苯致小鼠耳廓肿胀和角叉菜胶大鼠足跖肿胀炎症模型,探讨了熊果酸衍生物-查耳酮缀合物的体内抗炎作用。结果表明,熊果酸衍生物-查耳酮缀合物皆有抗炎活性,部分化合物的活性与熊果酸相比均有提高。其中,1-烯-3-氧代熊果酸-查耳酮缀合物(6a^6g)的抗炎活性强于3-氧代熊果酸-查耳酮(5a^5g)和3-烯熊果酸-查耳酮(7a^7g)缀合物。
A series of novel conjugates with ursolic acid core and different chalcone ligands were synthesized via ursolic acid, 4-hydroxyacetophenone and aromatic aldehydes. All of the conjugates were confirmed by the application of IR, ~1H NMR, ^（13）C NMR and HR-MS. The anti-inflammatory effect was observed for the target compounds in xylene-induced mouse ear edema and carrageenan-induced paw edema in rats. The preliminary bioassay test demonstrated that these compounds had potent anti-inflammatory activities, and their activities were better than that of the parent ursolic acid. Among them, 1-en-3-oxoursolic acid-chalcone conjugates（6a-6g） exhibited higher activities than analogues 5a-5g and 7a-7g.
出处
《药学学报》
CAS
CSCD
北大核心
2016年第6期938-946,共9页
Acta Pharmaceutica Sinica
关键词
熊果酸衍生物-查耳酮缀合物
衍生物
抗炎
ursolic acid derivative-chalcone conjugate
derivative
anti-inflammatory
