依托红霉素会损害线粒体和微粒体的钙稳态：与肝毒性的相关性。

Erythromycin estolate impairs the mitochondrial and microsomal calcium homeostasis: correlation with hepatotoxicity.

作者信息

Richelmi P, Baldi C, Manzo L, Berte F, Martino A P, Mirabelli F, Bellomo G

出版信息

Arch Toxicol Suppl. 1984;7:298-302. doi: 10.1007/978-3-642-69132-4_49.

Abstract

The effects of erythromycin estolate, a well known hepatotoxic macrolide antibiotic, on isolated rat hepatocyte viability and on subcellular Ca2+ transport have been investigated. Erythromycin estolate (0.5 mM), but not erythromycin base and erythromycin ethylsuccinate, induced 100% cell death after 60 min incubation, and caused maximal inhibition of mitochondrial and microsomal Ca2+ sequestration activities at 0.1 mM concentration. Sodium lauryl sulphate, which is the surfactant moiety of the erythromycin estolate molecule, caused effects similar to those exhibited by erythromycin estolate. Disorders of the intracellular calcium homeostasis seem to play a role in the lauryl sulphate-mediated hepatotoxic action of erythromycin estolate.

摘要

已对一种著名的具有肝毒性的大环内酯类抗生素依托红霉素对离体大鼠肝细胞活力及亚细胞Ca2+转运的影响进行了研究。依托红霉素（0.5 mM），而非红霉素碱和琥乙红霉素，在孵育60分钟后诱导100%细胞死亡，并在0.1 mM浓度时对线粒体和微粒体Ca2+螯合活性产生最大抑制。月桂基硫酸钠是依托红霉素分子的表面活性剂部分，其产生的作用与依托红霉素类似。细胞内钙稳态紊乱似乎在月桂基硫酸钠介导的依托红霉素肝毒性作用中发挥作用。