Probucol

Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases^{[1][2][3][4][5][6][7][8][9][10][11][12][13]}. IC50 & Target:Probucol (DH-581) is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. Probucol (DH-581) inhibited cholesterol efflux up to 80% in J774 macrophages expressing ABCA1. Probucol (DH-581) is an effective inhibitor of ABCA1-mediated cholesterol efflux without influencing scavenger receptor class B type I-mediated efflux. The inhibition of ABCA1 translocation to the plasma membrane may in part explain the reported in vivo high-density lipoprotein-lowering action of probucol^[1]. In Vitro:Probucol (10 μM, 2 h) inhibits ABCA1-mediated cholesterol efflux by affecting the ABCA1 translocation to the plasma membrane, the membrane cholesterol pool, and the ¹²⁵I-apo-AI binding in J774 macrophages expressing ABCA1^[3].
Probucol (10 μM, 24 h) promotes high glucose-induced proliferation and inhibits apoptosis by reducing reactive oxygen species generation in Müller cells^[5].
Probucol (0.01-0.1 mL of a 50 mg probucol/mlacetone solution, 60 min) inhibits peroxidation of microsomal membrane lipids and DNA damage induced by Fe-NTA plus H₂O₂^[6].
Probucol (3-10 μM) protects neuroblastoma cells from peroxide-induced damage by activating glutathione peroxidase (GPx)^[7].
Probucol (10 μM) promotes osteoblasts differentiation of MC3TE-E1 cells through reducing oxidative stress^[11].
In Vivo:Probucol (48 mg/day, diet, 12 weeks) alleviates atherosclerosis by accelerating the process of reverse cholesterol transport, improving the anti-inflammatory and anti-oxidant functions in rabbits^[4].
Probucol (60 mg/kg, i.p., 2 weeks) promotes endogenous antioxidants and provides protection against adriamycin-induced cardiomyopathy in Sprague-Dawley rats^[8].
Probucol (cumulative dose, 120 mg/kg, i.p., 4 weeks) provide complete protection against adriamycin cardiomyopathy without interfering with its antitumor effect in Sprague-Dawley rats^[9].
Probucol (500 mg/kg, intracavernosal injection, daily) enhances the therapeutic efficiency of mesenchymal stem cells in the treatment of erectile dysfunction in diabetic SD rats by prolonging their survival time via Nrf2 pathway^[10].
Probucol (1-3.5 mg/kg, p.o., 12 weeks) promotes prevents osteoporosis development through reducing oxidative stress in hormone-deficiency-induced postmenopausal osteoporosis SD rats^[11].
Probucol (61 mg/kg, p.o., 80 days) exerts multiple beneficial morphological effects that result in better left ventricular remodeling and function, reduced neurohumoral activation, and preserved renal function in the rats^[12].
Probucol (500-1000 mg/kg, p.o., once a day for 15 days) recovers pathological damage of myocardial tissue through improvement of myocardium-related proteins Caspase-3 and Caspase-9 in viral myocarditis rats^[13].