Stachydrine

Stachydrine inhibits cell proliferation and induces primary apoptosis and ROS production in T47D and MCF-7 cells in time- and dose-dependent manner. Its treatment induces caspase-3 activation and decreases the expression of the anti-apoptotic protein Bcl-2. Stachydrine simultaneously inhibits the phosphorylation of Akt and ERK proteins^[1]. Stachydrine ameliorates the detrimental effect of high-glucose on EC (endothelial cells) and that its beneficial effect occurs through the modulation of cell senescence signaling and SIRT1 expression^[2]. Stachydrine inhibits AngII-induced excessive autophagy within H9c2 cells. Stachydrine blocks the over phosphorylation of the p47phox subunit, decreases the translocation of p47phox and p67phox to the membrane, inhibits the activity of NOX2, and reduces the generation of ROS^[3].

The cell proliferation is determined by XTT after treatment with high-glucose (30 mM) in the presence or absence of stachydrine (0.1 mM) up to 72 h. Briefly, Endothelial cells (EC) are seeded in 96-well at a density of 4000 cells/well and incubated for 12, 24, 48, and 72h at 37 ºC with high-glucose alone or with high-glucose in the presence of stachydrine (0.1 mM). Control cells received normal glucose concentration or stachydrine (0.1 mM) alone. At the end of incubations, XTT assay is performed. The absorbance was measured at 492 nm in a spectrophotometer.

Stachydrine ameliorates transverse aortic constriction (TAC)-induced cardiac hypertrophy, dysfunction and excessive autophagy in vivo^[3]. It shows significantly pharmacological properties including low toxicity, anti-inflammatory activities by improving the cellular membrane permeability, decreasing the levels of inflammatory factors and reducing the lipid peroxidation, and anti-oxidant activities by reducing plasma LDH activity and MDA levels, and protection against myocardial ischemia reperfusion injury in rats. The mean pharmacokinetic parameters of stachydrine after oral administration of Herba Leonuri extract: Tmax=0.75 h, t1/2z=1.64 h^[4].