Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
Jatrorrhizine hydrochloride suppresses C8161 cell proliferation in a dose-dependent manner, with a half-maximal inhibitory concentration of 47.4±1.6 μmol/l. however, it does not induce significant cellular apoptosis at doses up to 320 μmol/l. Mechanistic studies show that JH-induced C8161 cell cycle arrest at the G0/G1 transition, which is accompanied by overexpression of the cell cycle-suppressive genes p21 and p27 at higher doses[2].
JH reduces metastatic melanoma cell-mediated neovascularization[2]. JH ameliorates hyperlipidemia via the suppression of lipogenesis and the enhancement of lipid oxidation in the liver[3].
[1] Xiaofei Jiang, et al. Journal of Chemistry. 2017. [2] Liu R, et al. Anticancer Drugs. 2013, 24(7):667-76. [3] Yang W, et al. Mol Med Rep. 2016, 14(4):3277-84.