4-Hydroxychalcone

4-Hydroxychalcone is an orally active flavonoid precursor. 4-Hydroxychalcone inhibits VEGF- and bFGF-induced phosphorylation of ERK1/2 and Akt. 4-Hydroxychalcone suppresses resistant hypertension by alleviating hyperaldosteronism, inflammation and renal injury in cryptochrome gene knockout mice. 4-Hydroxychalcone possesses anti-angiogenic activity^[1][2]. IC50 & Target:NF-κB^[2] In Vitro:4-hydroxychalcone (22 µg/mL; 6 days) potently inhibits VEGF/TNF-α- and bFGF/TNF-α-induced capillary-like tube formation of hMVEC in 3D fibrin matrices, with no cytotoxicity to endothelial monolayers^[1].
4-hydroxychalcone (0.22-22 µg/mL; 24-144 h) exhibits no cytotoxicity toward confluent HUVEC and hMVEC monolayers^[1].
4-hydroxychalcone (0.22-22 µg/mL; 48-72 h) exerts a cytostatic effect on the proliferation of HUVEC, but shows no cytostatic effect on HeLa, MCF-7 or A549 tumor cell lines even at a concentration as high as 22 µg/mL with a 72 h treatment^[1]. In Vivo:4-Hydroxychalcone (5.6 µg/mL; topical application) significantly inhibits bFGF-induced angiogenesis in the chick chorioallantoic membrane assay, without impairing basal vascular formation or embryonic survival^[1].
4-Hydroxychalcone (10-40 mg/kg; p.o.; twice daily; for consecutive 35 days) exerts dose-dependent protective effects against refractory hypertension, hyperaldosteronism, inflammation and renal injury in cryptochrome-knockout mice treated with high salt^[2].