3,8’-Biapigenin is a polyketide synthase-derived biflavonoid that has been found in Hypericum and has diverse biological activities.1,2,3,4,5 It inhibits protein tyrosine phosphatase 1B (PTP1B; IC50 = 4.5 µM) and stimulates glucose uptake in 3T3-L1 adipocyte cells when used at concentrations of 5 and 10 µM.2 3,8’-Biapigenin inhibits the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, and CYP1A2 (Kis = 0.038, 0.32, and 0.95 µM, respectively).3 It reverses cell death induced by kainate and NMDA in isolated rat embryonic hippocampal neurons when used at a concentration of 10 µM.4 3,8’-Biapigenin (8 mg/kg) decreases carrageenan-induced paw edema and protects against gastric lesions induced by indomethacin in rats.5
1.Weng, J.-K., and Noel, J.P.Chemodiversity in Selaginella: A reference system for parallel and convergent metabolic evolution in terrestrial plantsFront. Plant Sci.4119(2013) 2.Nguyen, P.-H., Ji, D.-J., Han, Y.-R., et al.Selaginellin and biflavonoids as protein tyrosine phosphatase 1B inhibitors from Selaginella tamariscina and their glucose uptake stimulatory effectsBioorg. Med. Chem.23(13)3730-3737(2015) 3.Obach, R.S.Inhibition of human cytochrome P450 enzymes by constituents of St. John’s wort, an herbal preparation used in the treatment of depressionJ. Pharmacol. Exp. Ther.294(1)88-95(2000) 4.Silva, B., Oliveira, P.J., Dias, A.S., et al.Quercetin, kaempferol and biapigenin from Hypericum perforatum are neuroprotective against excitotoxic insultsNeurotox. Res.13(3-4)265-279(2008) 5.Zduni?, G., Go?evac, D., Milenkovi?, M., et al.Evaluation of Hypericum perforatum oil extracts for an antiinflammatory and gastroprotective activity in ratsPhytother. Res.23(11)1559-1564(2009)