Dihydromethysticin

Dihydromethysticin is an orally active natural active ingredient. Dihydromethysticin can be extracted from Piper methysticum. Dihydromethysticin inhibits carboxylesterase 1 (K_i = 68.2 μM) and CYP2A5. Dihydromethysticin upregulates NLRC3 and induces Apoptosis. Dihydromethysticin exhibits anticancer activity against colorectal cancer and lung adenoma^{[1][2][3][4][5]}. In Vitro: Dihydromethysticin (0-400 μM; 24-48 h) inhibits proliferation, migration, invasion, promotes apoptosis and G0/G1 arrest in colorectal cancer cells via the NLRC3/PI3K pathway^[1].
Dihydromethysticin (0-208.46 μM) inhibits carboxylesterase 1 with mixed competitive-noncompetitive type inhibition (K_i = 68.2 μM)^[2].
Dihydromethysticin (10-100 μM) inhibits coumarin 7-hydroxylation (CYP2A5) activity in mouse liver microsomes^[3].
In Vivo: Dihydromethysticin (10 mg/kg; i.p.; daily for 4 weeks) suppresses tumor growth and angiogenesis in BALB/c nude mice with subcutaneous CRC via NLRC3/PI3K pathway, without toxicity^[1].
Dihydromethysticin (0.8 mg/mouse; p.o.; before NNK injection) completely inhibits lung adenoma formation in A/J mice by reducing DNA adducts and enhancing NNAL detoxification^[4].