Osthenol

Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC₅₀=0.74 μM, K_i=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer^[1][2][3][4]. In Vitro:Osthenol (0.74 μM; enzyme activity assay) exhibits potent, selective and reversible competitive inhibitory activity against recombinant hMAO-A with IC₅₀=0.74 μM, SI >81.1^[1].
Osthenol (25-100 μM; 24-48 h) significantly inhibits cell proliferation, induces apoptosis, arrests the cell cycle at the G1 phase and inhibits cell migration in HCT116 human colon cancer cells assay^[2].
Osthenol has antifungal activity with MICs of 125 μg/mL against Fusarium solani and 250 μg/mL against Candida albicans and Aspergillus fumigatus^[3].
Osthenol is effective against Gram-positive bacteria with MICs of 125-62.5 μg/mL^[4].
In Vivo:Osthenol (5 mg/kg; intravenous injection; single dose) has a rapid distribution characteristic in male ICR mice, with initial blood concentration C₀=14.3 μg/mL, T_1/2=47.0 min, AUC_last=211.5 μg·min/mL, MRT_last=22.5 min^[5].
Osthenol (5 mg/kg, 20 mg/kg; oral gavage; single dose) has extremely low bioavailability in male ICR mice (0.43% and 0.02%, respectively), and is rapidly metabolized to sulfonylated (M1) and glucuronidated (M2) conjugates after oral administration^[5].