Cholesteryl Hemisuccinate is an acidic cholesterol ester with hepatoprotective and anticancer activities[1, 2]. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase and promotes DNA replication and repair[3]. Cholesteryl Hemisuccinate is a detergent widely used in protein crystallography, protein biochemistry research and pharmacology[4]. Cholesteryl Hemisuccinate can inhibit the attachment and spreading of epithelial cells[5].
In vivo, Cholesteryl Hemisuccinate (100mg/kg) pre-treated ICR mice treated with acetaminophen (AAP) by intraperitoneal injection inhibited AAP-induced liver injury and suppressed hepatocyte necrosis and apoptosis[6].
References:
[1] Fariss M W, Fortuna M B, Everett C K, et al. The selective antiproliferative effects of α-tocopheryl hemisuccinate and cholesteryl hemisuccinate on murine leukemia cells result from the action of the intact compounds[J]. Cancer Research, 1994, 54(13): 3346-3351.
[2] Shah H, Madni A, Khan M M, et al. pH-responsive liposomes of dioleoyl phosphatidylethanolamine and cholesteryl hemisuccinate for the enhanced anticancer efficacy of cisplatin[J]. Pharmaceutics, 2022, 14(1): 129.
[3] Varshosaz J, Taymouri S, Hassanzadeh F, et al. Folated Synperonic‐Cholesteryl Hemisuccinate Polymeric Micelles for the Targeted Delivery of Docetaxel in Melanoma[J]. BioMed research international, 2015, 2015(1): 746093.
[4] Kulig W, Jurkiewicz P, Olżyńska A, et al. Experimental determination and computational interpretation of biophysical properties of lipid bilayers enriched by cholesteryl hemisuccinate[J]. Biochimica et Biophysica Acta (BBA)-Biomembranes, 2015, 1848(2): 422-432.
[5] Sauk J J, Krumwiede M, Cooking‐Johnson D, et al. Alterations in lipid fluidity induced by cholesterol and cholesterol hemisuccinate modulate the organization of microtubule skeletons in epithelial cells[J]. Journal of Oral Pathology & Medicine, 1987, 16(2): 69-74.
[6] Ray S D, Mumaw V R, Raje R R, et al. Protection of acetaminophen-induced hepatocellular apoptosis and necrosis by cholesteryl hemisuccinate[J]. Journal of Pharmacology and Experimental Therapeutics, 1996, 279: 1470-1483.
Cholesteryl Hemisuccinate是一种酸性胆固醇酯，具有肝保护和抗癌活性[1, 2]。Cholesteryl Hemisuccinate 抑制DNA聚合酶和DNA拓扑异构酶，促进DNA复制和修复[3]。Cholesteryl Hemisuccinate是一种去垢剂，广泛应用于蛋白质晶体学、蛋白质生化研究和药理学[4]。Cholesteryl Hemisuccinate能够抑制上皮细胞的附着和扩散[5]。
在体内，Cholesteryl Hemisuccinate（100mg/kg）通过腹腔注射预处理接受乙酰氨基酚（AAP）治疗的ICR小鼠，抑制了AAP诱导的肝损伤，抑制了肝细胞坏死和凋亡[6]。