Flavokawain C

Flavokawain C is a chalcone that has been found in kava and has enzyme inhibitory and anticancer activities.^1,2,3 It inhibits collagenase and elastase in cell-free assays (IC₅₀s = 62.05 and 17.6 µM, respectively).¹ It is cytotoxic to HCT116, HT-29, MCF-7, A549, and Ca Ski cancer cells (IC₅₀s = 12.75, 39, 47.63, 40.28, and 39.88 µM, respectively).² Flavokawain C (20, 40, and 60 µM) induces apoptosis and cell cycle arrest at the G₁ phase in HCT116 cells. In vivo, flavokawain C (1 and 3 mg/kg) reduces tumor volume and induces intratumoral necrosis and apoptosis in an HCT116 mouse xenograft model.³

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1. Wei, L., Liao, Z., Ma, H., et al. Antioxidant properties, anti- SARS-CoV-2 study, collagenase and elastase inhibition effects, anti-human lung cancer potential of some phenolic compounds. J. Indian Chem. Soc. 99(4), 100416 (2022).

2. Phang, C.-W., Karsani, S.A., Sethi, G., et al. Flavokawain C inhibits cell cycle and promotes apoptosis, associated with endoplasmic reticulum stress and regulation of MAPKs and Akt signaling pathways in HCT 116 human colon carcinoma cells. PLoS One 11(2), e0148775 (2016).

3. Phang, C.-W., Malek, S.N.A., and Karsani, S.A. Flavokawain C exhibits anti-tumor effects on in vivo HCT 116 xenograft and identification of its apoptosis-linked serum biomarkers via proteomic analysis. Biomed. Pharmacother. 137, 110846 (2021).