Flavokawain B

Flavokawain B is a natural chalcone first isolated from extracts of kava roots. It induces apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC₅₀s = 32, 48, 6.2, and 3.9 µM for LAPC4, LNCaP, PC-3, and DU145 cells, respectively, treated for 48 hours), with increased expression of the proapoptotic protein Bim.¹ Flavokawain B increases Bim expression and inhibits growth of DU145 xenografts in mice.¹ It also increases Bim expression, promotes apoptosis, and induces cell cycle arrest in uterine leiomyosarcoma cells.² However, flavokawain B is hepatotoxic, triggering oxidative stress, inhibiting NF-κB signaling, and activating MAPK pathways, culminating in HepG2 and L-02 cell death (LD₅₀s = 15 and 32 µM, respectively).³

WARNING This product is not for human or veterinary use.

1. Tang, Y., Xuesen, L., Zhongbo, L., et al. Flavokawain B, a kava chalcone, exhibits robust apoptotic mechanisms on androgen receptor-negative, hormone-refractory prostate cancer cell lines and reduces tumor growth in a preclinical model. Int. J. Cancer 127(8), 1758-1768 (2010).

2. Eskander, R.N., Randall, L.M., Sakai, T., et al. Flavokawain B, a novel, naturally occurring chalcone, exhibits robust apoptotic effects and induces G₂/M arrest of a uterine leiomyosarcoma cell line. J. Obstet. Gynaecol. Res. 38(8), 1086-1094 (2012).

3. Zhou, P., Gross, S., Liu, J.H., et al. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-κB and MAPK signaling pathways. FASEB J. 24(12), 4722-4732 (2010).