Pedalitin is a tyrosinase and α-glucosidase inhibitor with IC50 values of 0.28 mM and 0.29 mM, respectively, and can be isolated and extracted from Rabdosia serra. Pedalitin is a xanthine oxidase (Xanthine Oxidase) (IC50 = 3.7 µM) and myeloperoxidase (MPO) (IC50 = 3.8 nM) inhibitor. Pedalitin ameliorates NAFLD by downregulating the EGFR/IRS1/AKT1/FOXO1 signaling pathway and related inflammatory and lipid metabolism factors. Pedalitin reduces the risk of urinary tract infection and stones by inhibiting the expression of the urease UreC gene in Proteus mirabilis. Pedalitin also exhibits antifungal activity, with a MIC of 3.9 mg/L against Cryptococcus neoformans. Pedalitin can be used for research on non-alcoholic fatty liver disease, chronic kidney disease, kidney stones, cryptococcosis, and abdominal pain .