Sadeg N, Pham-Huy C, Martin C, Warnet J M, Claude J R
Laboratoire de Toxicologie (EA 207), Faculté de Pharmacie, Paris, France.
Drug Chem Toxicol. 1994;17(2):93-111. doi: 10.3109/01480549409014304.
The potential nephrotoxicity of cyclosporine A (CsA), its three main metabolites: M1, M17 and M21, and its two analogues: cyclosporines C and D (CsC, CsD) was evaluated in vitro in suspensions of freshly isolated rabbit renal proximal tubular cells. This assessment involved the measure of enzyme release in the incubation media and the determination of Na+/K(+)-ATPase activity and glutathione content directly in the tubular cells. In vitro nephrotoxicity results of the six compounds tested could be respectively schematized as: CsA > CsD > CsC > M21 > M17, M1 It would be interesting to promote the study of promising CsC because of its low nephrotoxicity and its high immunosuppressive potency as previously reported.
在新鲜分离的兔肾近端小管细胞悬液中对环孢素A（CsA）及其三种主要代谢物：M1、M17和M21，以及其两种类似物：环孢素C和D（CsC、CsD）的潜在肾毒性进行了体外评估。该评估包括测定孵育培养基中的酶释放以及直接测定肾小管细胞中的Na+/K(+)-ATP酶活性和谷胱甘肽含量。所测试的六种化合物的体外肾毒性结果可分别概括为：CsA > CsD > CsC > M21 > M17，M1 由于先前报道的低肾毒性和高免疫抑制效力，促进对有前景的CsC的研究将是很有意思的。
