Donnelly J G, Russell R L, Palaszynski E W, Copeland K R, Yatscoff R W, Chan M M, Soldin S J
Department of Laboratory Medicine, Children's National Medical Center, Washington, DC 20010.
Clin Biochem. 1991 Feb;24(1):71-4. doi: 10.1016/0009-9120(91)90273-h.
Seven purified cyclosporine (CsA) metabolites were analyzed for binding to cyclophilin and to a 50 kDa protein purified from a JURKAT cell line. In addition, the potency of the seven metabolites, relative to CsA, was obtained using a primary mixed lymphocyte culture (MLC) suppression assay. CsA, M1, 17, and 21 were found to be immunosuppressive in the concentration range used (0-500 ng/mL). These results were then compared to protein binding. CsA and metabolite 17 (M17) bound to both proteins. Conversely, M1, 13, 21, and 26 bound only to cyclophilin, while M8 and M18 bound only to the 50 kDa protein.
对七种纯化的环孢素(CsA)代谢物进行分析,以检测它们与亲环蛋白以及从JURKAT细胞系中纯化的一种50 kDa蛋白的结合情况。此外,使用原代混合淋巴细胞培养(MLC)抑制试验获得了这七种代谢物相对于CsA的效力。发现在所用浓度范围(0 - 500 ng/mL)内,CsA、M1、17和21具有免疫抑制作用。然后将这些结果与蛋白结合情况进行比较。CsA和代谢物17(M17)与两种蛋白都结合。相反,M1、13、21和26仅与亲环蛋白结合,而M8和M18仅与50 kDa蛋白结合。