HSU, LI WEI,CHANG, SU CHEN,CHUANG, KUO SHENG,SHEN, CHEN HSIANG
申请号：
TW93137633
公开号：
TWI355933B
申请日:
2004.12.06
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
The present invention relates to andrographolide and its derivatives of the general formula (I), as well as the stereoisomers and salts of andrographolide and the derivatives.Andrographolide and its derivatives represented by general formula (I) defined above are useful as TNFα (tumor necrosis factor alpha) antagonists or inhibitors which have inhibitory effect on the binding of TNFα to TNF-R1. Andrographolide exhibited inhibitor activity with IC50 values 60 μM on L929 cell proliferation/cytotoxicity assay without cell cytotoxicity. In addition, in the animal model test of collagen-induced arthritis, andrographolide exhibited 50% paw edema. Andrographolide and its derivatives are promising sources with high TNFα-inhibiting or antagonizing activity.
