Hydrastine

Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC₅₀=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC₅₀=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage^[1][2]. In Vitro:Hydrastine (50-750 μM; 24-48 h) reduces the cell viability of PC12 cells in a concentration- and time-dependent manner, and significantly induces cytotoxicity at 500-750 μM^[1].
Hydrastine (750 μM; 48 h) induces apoptosis in PC12 cells, and combined with L-DOPA (50 μM) significantly aggravates apoptosis^[1]. In Vivo:Hydrastine (46 mg/kg; oral gavage; single dose) has no significant effect on the pharmacokinetics of metformin (10 mg/kg; oral) in the male FVB mouse model, with no changes in C_max, AUC_0-12h and elimination half-life^[2].