3',4'-Dihydroxyflavone is a synthetic flavonoid that has diverse biological activities.1,2,3,4 It inhibits tankyrase 1 (TNKS1) and TNKS2 (IC50s = 0.23 and 0.17 ?M for the human enzymes, respectively).1 3',4'-Dihydroxyflavone is active against L. donovani, T. brucei, and T. cruzi with IC50 values of 2, 1.1, and 10.1 ?g/ml, respectively.2 It induces apoptosis in and inhibits migration of GL15 glioblastoma cells when used at a concentration of 50 ?M.3 3',4'-Dihydroxyflavone (5 mg/kg) prevents LPS-induced increases in brain levels of COX-2 and inducible nitric oxide synthase (iNOS) in a mouse model of neuroinflammation.4
1.Narwal, M., Koivunen, J., Haikarainen, T., et al.Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivityJ. Med. Chem.56(20)7880-7889(2013) 2.Tasdemir, D., Kaiser, M., Brun, R., et al.Antitrypanosomal and antileishmanial activities of flavonoids and their analogues: In vitro, in vivo, structure-activity relationship, and quantitative structure-activity relationship studiesAntimicrob. Agents Chemother.50(4)1352-1364(2006) 3.Santos, B.L., Oliveira, M.N., Coelho, P.L.C., et al.Flavonoids suppress human glioblastoma cell growth by inhibiting cell metabolism, migration, and by regulating extracellular matrix proteins and metalloproteinases expressionChem. Biol. Interact.242123-138(2015) 4.Kim, N., Yoo, H.-S., Ju, Y.-J., et al.Synthetic 3',4'-dihydroxyflavone exerts anti-neuroinflammatory effects in BV2 microglia and a mouse modelBiomol. Ther. (Seoul)26(2)210-217(2018)