Flavokawain A

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer^{[1][2][3][4][5]}. In Vitro:Flavokawain A (0.05-25 μg/mL; 4-48 h) can inhibit the proliferation of multiple bladder cancer cells, cause the loss of mitochondrial membrane potential and the release of cytochrome c in T24 cells. The mechanism involves the activation of Bax and the inhibition of Bcl-x/L^[1].
Flavokawain A (5-30 μg/mL; 4-24 h) induces apoptosis in T24 cells through the caspase pathway and by inhibiting XIAP and survivin^[1].
Flavokawain A (20-40 μM; 24 h) can inhibit IL-1β-induced inflammation, the expression of senescence-related genes, apoptosis, and the phosphorylation of genes related to the MAPK and PI3K pathways in mouse chondrocytes^[2]. In Vivo:Flavokawain A (30 mg/kg; peritumoral injection; once every 3 days; 24 days) exhibits anti-tumor activity in a mouse model of bladder cancer^[3].
Flavokawain A (50 mg/kg; oral administration; 28 days) shows no toxicity and has certain immunomodulatory effects in Balb/c mice^[4].