Chelerythrine

Chelerythrine is a natural alkaloid, acts as a potent and selective Ca²⁺/phospholopid-dependent PKC antagonist, with an IC₅₀ of 0.7 μM^[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity^[2]. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC₅₀ of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy^[3][4]. In Vitro:Chelerythrine (48 h) inhibits the growth of L-1210 cells (IC₅₀: 0.53 uM )^[1].
Chelerythrine (0-20 μM, 24 h) inhibits cell viability, induces apoptosis and autophagy in A549 and NCI-H1299 cells^[4].
Chelerythrine (0-5 μM, 24 or 48 h) induces apoptosis in BclXL-overexpressing SH-SY5Y cells^[3].
Chelerythrine (2.5-10 μM, 16 h) induces mitochondrial depolarization (decrease in mitochondrial potential) in SH-SY5Y cells, and stimulates release of CytC from isolated mitochondria^[4].
Chelerythrine (0-100 ng/mL, 24 h) reduces the LPS induced production of NO and TNF-α in primary macrophages^[5].
Chelerythrine (MIC: 0.156 mg/mL) shows antibacterial activities against Gram-positive bacteria, Staphylococcus aureus (SA), MRSA, and extended spectrum β-lactamase S. aureus (ESBLs-SA)^[6].
In Vivo:Chelerythrine (5 mg/kg, i.p., daily) attenuates partial unilateral ureteral obstruction (UUO) induced kidney injury, and restores renal function in neonatal rats^[2].
Chelerythrine (1-10 mg/kg, i.p., at 24 and 1 h before injection of 100 μg/kg LPS) shows anti-inflammatory effects (increased survival rate, decreased serum nitrite and TNF-α level) in LPS induced mice endotoxic shock model^[5].