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专利概况
专利名称 15-IDENE-14-DEOXY-11, 12-DEHYDROANDROGRAPHOLIDE DERIVATIVE AND APPLICATION THEREOF IN PREPARING ANTI-FIBROSIS DRUGS
申请号 EP18777705 申请日
公开(公告)号 EP3608313A1 公开(公告)日
申请(专利权)人 Zhengzhou University 发明人 DAI Guifu; XU Haiwei; GUAN Zhenzhen; WANG Yake; WU Di; SHEN Pengpeng; SHANG Ning; WU Fengjuan; ZHAO Jin; ZHANG Xiaopei
专利来源 国家知识产权局 转化方式
摘要

The present invention relates to the technical field of medicine, and relates to a 15-idene-14-deoxy-11, 12-dehydroandrographolide derivative and a use thereof in anti-fibrosis. Experiments show that this compound can significantly inhibit metastasis and activation of hepatic stellate cells LX-2, significantly reduce the fibrosis level of hepatic tissues of rats infected with hepatic fibrosis, reduce contents of extracellular matrix protein (ECM) related components, effectively inhibit immune inflammation, inhibit activation of hepatic stellate cells in hepatic tissues, promote collagen degradation, significantly inhibit TGF-1-induced epithelial-mesenchymal transition (E MT) of human alveolar type II cells A549 and kidney epithelial cells HK-2, significantly reduce the bleomycin-induced pulmonary fibrosis degree in mice and the unilateral ureteral obstruction-induced renal fibrosis degree in rats, and significantly inhibit angiotensin II (Ang II)-induced proliferation of human cardiac fibroblasts (HCFB). This compound can be used as an active ingredient for preparing anti-fibrosis drugs, which are efficient and have low toxicity, thus providing a novel medicine route for treatment and prevention of diseases related with fibrosis, and expanding the optional range of clinical medication. The compound has good application and development prospects.

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