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14-DÉSOXY-11,12-DÉHYDRO-8,12-ÉPOXY OU 7,8-ÈNE-ANDROGRAPHOLIDE, DÉRIVÉS SUBSTITUÉS EN POSITION 15 ET LEUR UTILISATION
专利权人:
ZHENGZHOU UNIVERSITY;郑州大学
发明人:
DAI, Guifu,戴桂馥,YAN, Guangming,闫光明,WU, Di,吴笛,XU, Haiwei,徐海伟,ZHU, Jiazhen,朱家贞,FU, Zibo,伏自波,GUAN, Zhenzhen,关珍贞,ZHANG, Xiaopei,张晓沛,SHANG, Ning,尚宁,ZHANG, Shuqiu,张淑秋
申请号:
CNCN2019/076608
公开号:
WO2019/166003A1
申请日:
2019.03.01
申请国别(地区):
CN
年份:
2019
代理人:
摘要:
The present invention belongs to the technical field of medicine, and discloses use of 14-deoxy-11,12-dehydro-8,12-epoxy-andrographolide and derivatives thereof and 14-deoxy-11,12-dehydro-7,8-ene andrographolide and 15-substituted derivatives thereof in the preparation of medicaments for preventing and treating diseases having fibrotic pathological processes. It has been proved by experiments that such compounds significantly inhibit the migration and activation of hepatic stellate cells, significantly inhibit TGF-β1-induced mesenchymal transition in human alveolar type II epithelial cells A549; significantly inhibit TGF-β1-induced mesenchymal transition in epithelial cells HK-2 in human renal cortex proximal convoluted tubules; and inhibit angiotensin II (AngII)-induced migration of primary human cardiac fibroblasts HCFB. In a mouse common bile duct ligation model, a silica-induced mouse pulmonary fibrosis model and a mouse unilateral ureteral ligation model, the compounds in this study all exhibit good anti-fibrotic activities in vivo. Such compounds are used as active ingredients in the preparation of anti-fibrotic medicaments, and have high efficiency and low toxicity, thus having good prospects for being developed into medicaments resistant to multiple fibrosis.La présente invention se rapporte au domaine technique de la médecine et concerne l'utilisation de 14-désoxy-11,12-déhydro-8,12-époxy-andrographolide et de ses dérivés et de 14-désoxy-11,12-déhydro-7,8-ène andrographolide et des dérivés substitués en position 15 de ceux-ci dans la préparation de médicaments pour la prévention et le traitement de maladies ayant des processus pathologiques fibrotiques. Il a été démontré par des expériences que de tels composés inhibent de manière significative la migration et l'activation de cellules stellaires hépatiques, inhibent de manière significative la transition mésenchymateuse induite par TGF-β1 dans des cellules épithéliales A549 de type II alvéolaires humaines ;
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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