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Novel matrine derivative MD-1 attenuates hepatic fibrosis by inhibiting EGFR activation of hepatic stellate cells

Protein & Cell 2016年第9期7卷 662-672页

作者： Yi Feng Hai-yan Ying Ying Qu Xiao-bo Cai Ming-yi Xu Lun-gen Lu Department of Gastroenterology Shanghai General Hospital Nanjing Medical University Shanghai 200080 China

matrine （MT）, the effective component of Sophora fla- vescens Air, has been shown to have anti-inflammation, immune-suppressive, anti-tumor, and anti-hepatic fibrosis activities. However, the pharmacological effects of MT still need to be strengthened due to its relatively low efficacy and short half-life. In the present study, we report a more effective thio derivative of MT, MD-1, and its inhibitory effects on the activation of hepatic stellate cells （HSCs） in both cell culture and animal models. Cytological experiments showed that MD-1 can inhibit the proliferation of HSC-T6 cells with a half-maximal inhibitory concentration （ICs0） of 62 pmollL. In addition, MD-1 more strongly inhibits the migration of HSC-T6 cells compared to MT and can more effectively induce G0/G1 arrest and apoptosis. Investigating the biological mechanisms underlying anti-hepatic fibrosis in the presence of MD-I, we found that MD-I can bind the epidermal growth factor receptor （EGFR） on the surface of HSC-T6 cells, which can further inhibit the phospho- rylaUon of EGFR and its downstream protein kinase B （Akt）, resulting in decreased expression of cyclin D1 and eventual inhibition of the activation of HSC-T6 cells. Furthermore, in rats with dimethylnitrosamine （DMN）- induced hepatic fibrosis, MD-1 slowed the development and progression of hepatic fibrosis, protecting hepatic parenchymal cells and improving hepatic functions. Therefore, MD-1 is a potential drug for anti-hepatic fibrosis.

关键词： matrine derivative hepatic stellate cellhepatic fibrosis epidermal growth factor receptor signaltransduction pathway

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Semisynthesis,characterization of some new matrine derivatives as insecticidal agents

Semisynthesis,characterization of some new matrine derivativ...

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第十一届全国化学生物学学术会议

作者： Huiqing He Xuhong Jiang Fangyun Dong Jingmin Ye Hanhui,Zhang Xingan Cheng Institute of Natural Product Chemistry College of Chemistry and Chemical EngineeringZhongkai University of Agriculture and Engineering

In order to discover new potential natural-product-based crop protection agents,we synthesized three new matrine derivatives,13-cyclohexylaminomatrine(M-Cyc-Mat),13-cyclohexylaminothiocarbonylthiomatrine(S-Cyc-Mat),13-(4’-methyl)cyclohexyla minothiocarbonylthiomatrine(S-M-Cyc-Mat),by introducing different active groups to C-13 position of matrine,a biorenewable quinolizidine alkaloid isolated from Sophora *** structural configuration was characterized by IR,MS,H NMR,C NMR and X-ray crystal *** pure yields of M-Cyc-Mat,S-Cyc-Mat,S-M-Cyc-Mat were 42%,65% and 71%,***,the insecticidal activity of compounds were carried out against six typically crop-threatening agricultural insect pests,Plutella xylostella,Spodoptera exigua,Spodoptera litura,Helicoverpa armigera Hubner,Ostrinia nubilalis and Lipaphis *** compared with matrine(mortality rates 60%),the M-Cyc-Mat and S-M-Cyc-Mat exhibited potent pesticidal activities against Lipaphis erysimi,whose mortality rates reached 83.3% and 89.7%,***,Cyc-Mat and S-Cyc-Mat showed sharply lower toxicity than matrine against Lipaphis erysimi,suggesting that the introduction of methyl can increase the insecticide activity of *** work provides valuable information for obtaining new natural-product-based candidate compounds for exploring novel pesticides.

关键词： matrine derivative structural modification structural characterization Insecticidal activity

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