BCRP Activator

Xanthine oxidase-IN-23 (Compound BPF) is an orally active, reversible, mixed-type Xanthine oxidase inhibitor with an IC₅₀ of 3.33 μM. Xanthine oxidase-IN-23 directly binds to XOD in a reversible mixed-type manner to inhibit its catalytic activity. Xanthine oxidase-IN-23 upregulates ABCG2 and downregulates GLUT9 to promote renal urate excretion. Xanthine oxidase-IN-23 reduces serum urate levels and improves renal function in hyperuricemic mice. Xanthine oxidase-IN-23 can be used in the research of hyperuricemia.

11β,13-Dihydrolactucopicrin is a sesquiterpene lactone and the main bitter component of chicory root. 11β,13-Dihydrolactucopicrin inhibits yeast α-glucosidase activity (IC₅₀ = 27.49 μM) and inhibits Crz1 activation and nuclear accumulation. 1β,13-Dihydrolactucopicrin possesses blood-brain barrier penetration capacity in an in vitro HBMEC blood-brain barrier model and can generate cysteine-conjugated metabolites within brain microvascular endothelial cells. 11β,13-Dihydrolactucopicrin can regulate the lncRNA H19/miR-21-3p signaling axis; it upregulates the expression of ABCG2 and lncRNA H19, downregulates miR-21-3p, inhibits the release of IL-6, TNF-α, and hs-CRP pro-inflammatory mediators, and alleviates urate-induced inflammatory injury in renal epithelial cells. 11β,13-Dihydrolactucopicrin can be used in research on diabetes and renal urate deposition.