Pedalitin

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^{[1][2][3][4][5][6][7][8][9][10][11]}. In Vitro:Pedalitin (20-80 μM; 24 h) significantly reduced intracellular triglyceride (TG) levels and decreased cytoplasmic lipid droplet accumulation in FFA-induced LO2 cells^[1].
Pedalitin (20 μM; 24 h) significantly downregulated the FFA-induced upregulation of inflammatory factors (IL-17, TNF-α), fatty acid metabolism factors (CPT2, HADH), and FOXO signaling pathway genes (EGFR, IRS-1, AKT-1, FOXO1) in LO2 cells^[1].
Pedalitin (4 mg/L; 0.5-48 h) exhibits significant antifungal and time-dependent fungicidal activity in Cryptococcus neoformans strain cultures, with an MIC of 3.9 mg/L^[10].
Pedalitin (1 mg/L; 30 min-2 h) combined with Amphotericin B (HY-B0221) significantly reduces Cryptococcus neoformans infection in U87-MG cells and MRC-5 cells^[10].
Pedalitin (20-80 μM; 24 h) did not substantially reduce FFA-induced LO2 cell viability, maintaining cell viability at approximately 80%^[1].
Pedalitin exhibited potent MPO inhibitory activity, ABTS radical scavenging activity, and DPPH radical scavenging activity, with IC₅₀ values of 3.8 nM, 1.4 μM, and 5.2 μM, respectively^[3].
Pedalitin significantly inhibits urease activity in the enzymatic reaction solution extracted from Proteus mirabilis^[5].
Pedalitin (0.12-62.5 mg/L; 24 h) exhibited low cytotoxicity in HepG2, MRC-5, NOK, and U87-MG cell lines, with IC₅₀ values of 131.7, 191.7, 119, and 175 mg/L, respectively^[10].

Pedalitin (0.01-0.4 mM; pre-incubation for 2-5 min) significantly inhibited tyrosinase and α-glucosidase activities, with IC₅₀ values of 0.28 mM and 0.29 mM, respectively^[11]. In Vivo:Pedalitin (40 mg/kg; intraperitoneal injection; once daily; 40 days) significantly prolonged the survival of BALB/c mice infected with C. neoformans and reduced the fungal burden in the lung and brain^[10].
Pedalitin (10 mg/kg; intraperitoneal injection; once daily; 40 days) combined with Amphotericin B has a synergistic effect, improving the survival rate, fungal burden, and histopathology of BALB/c mice infected with C. neoformans^[8].
Pedalitin (1-10 mg/kg; intraperitoneal injection; single administration; 30 min) exhibited significant dose-dependent analgesic activity in the acetic acid-induced writhing test in mice^[9].