3',4'-Dimethoxyflavone demonstrates a diverse range of bioactivities affecting multiple biological pathways and cellular processes. It notably exhibits bioactivity against Staphylococcus aureus, inhibiting its growth with a minimum inhibitory concentration (MIC) of 6.3 ug/mL in combination with subinhibitory levels of Berberine. Additionally, it shows antihistaminic activity in rat RBL2H3 cells, with an IC50 value greater than 500,000 nM for the inhibition of DNP-BSA-induced beta-hexosaminidase release.
The compound also demonstrates significant bioactivity in various assays, including inhibition of enzymes and proteins such as HSD17B4, JMJD2E, Fructose-1,6-bisphosphate Aldolase, and several others associated with different pathways. It modulates activities like Enhancers of SMN2 Splice Variant Expression, Cytochrome P450 3A4 activation, and USP1/UAF1 inhibition. In AML-2/D100 cells, it shows drug resistance against vincristine with an IC50 of 1200.0 nM.
Moreover, 3',4'-Dimethoxyflavone possesses antioxidant activity in rat liver microsomes (IC50 = 40.0 ug/mL), inhibits the growth of human MOLT4, MCF7, and HepG2 cells at 100 uM (though with less than 50% growth inhibition), and inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells.
Cytotoxic effects are observed against mouse RAW264.7 cells (IC50 = 39680.0 nM), along with anti-inflammatory activity, inhibiting NO and PGE2 production with IC50 values of 34540.0 nM and 6460.0 nM, respectively. It also inhibits NO production by 33.31% in LPS-stimulated RAW264.7 cells and shows inhibition of CYP450 in human liver microsomes, affecting the formation of 20-HETE and EpETrE with a selectivity index of 0.08 at 10 uM concentration..
Note: Summary generated by AI. Data source: ChEMBL 