Bilobetin is a biflavonoid that has been found in G. biloba and has diverse biological activities.1,2,3 It is cytotoxic to HeLa, NCI-H460, Daudi, K562, SKOV3, MIA PaCa-2, and MCF-7 cells in vitro (IC50s = 14.79-97.28 μM).1 Bilobetin halts the cell cycle at the G2/M phase in HeLa cells in a concentration-dependent manner and induces apoptosis in HeLa cells when used at a concentration of 20 μM. It selectively inhibits matrix metalloproteinase-9 (MMP-9; IC50 = 10.33 μM) over MMP-2 and MMP-3 (IC50s = >100 μM).2 Bilobetin also inhibits aggregation of amyloid-β (1-40) peptide in vitro with an IC50 value of 4.7 μM.3
1.Li, M., Li, B., Xia, Z.-M., et al.Anticancer effects of five biflavonoids from Ginkgo Biloba L. male flowers in vitroMolecules24(8)E1496(2019) 2.Wang, C.G., Yao, W.N., Ahang, B., et al.Lung cancer and matrix metalloproteinases inhibitors of polyphenols from Selaginella tamariscina with suppression activity of migrationBioorg. Med. Chem. Lett.28(14)2413-2417(2018) 3.Sirimangkalakitti, N., Juliawaty, L.D., Hakim, E.H., et al.Naturally occurring biflavonoids with amyloid β aggregation inhibitory activity for development of anti-Alzheimer agentBioorg. Med. Chem. Lett.29(15)1994-1997(2019)