Russell D H, Larson D F, Cardon S B, Copeland J G
Mol Cell Endocrinol. 1984 May;35(2-3):159-66. doi: 10.1016/0303-7207(84)90012-1.
Cyclosporine (CyA), formerly cyclosporin A, significantly inhibited the ability of prolactin (PRL) to elevate ornithine decarboxylase (ODC) activity in a variety of rat tissues. Administration of PRL to hypophysectomized rats also resulted in an induction of ODC activity which was inhibited markedly in all tissues studied in the presence of CyA. Transglutaminase ( TGase ) activity was not affected in any significant manner by PRL or CyA in most tissues studied. However, it was elevated in the adrenal by 10(-8) M PRL. Bromocryptine, which selectively antagonizes pituitary PRL release, decreased the kidney ODC basal levels to 30% of vehicle control and serum PRL level to 4.3 +/- 1.4 compared to 28 +/- 10 in controls, suggestive of PRL maintenance of steady-state ODC activity in the kidney. CyA administration did not affect the action of glucagon, a known cyclic AMP-mediated hormone, or 8-bromo-cyclic AMP on kidney ODC activity. The elevation of rat kidney ODC activity by dexamethasone and triiodothyronine (T3), compounds which elevated serum prolactin levels in all cases, was also blocked by administration of CyA. Epidermal growth factor (EGF), which did not induce rat kidney ODC activity by itself, was capable of producing a small increment in ODC activity in the presence of CyA. The marked effect of CyA to selectively block ODC induction by PRL may be due to the ability of CyA to interact with receptor-required phospholipids in membranes and thus to antagonize hormone-receptor interaction.
环孢素（CyA），以前称为环孢菌素A，能显著抑制催乳素（PRL）在多种大鼠组织中提高鸟氨酸脱羧酶（ODC）活性的能力。给垂体切除的大鼠注射PRL也会导致ODC活性的诱导，而在存在CyA的情况下，所有研究的组织中这种诱导均受到明显抑制。在大多数研究的组织中，转谷氨酰胺酶（TGase）活性未受到PRL或CyA的任何显著影响。然而，在肾上腺中，10(-8)M的PRL使其活性升高。选择性拮抗垂体PRL释放的溴隐亭，使肾脏ODC基础水平降至载体对照的30%，血清PRL水平降至4.3±1.4，而对照组为28±10，这表明PRL维持了肾脏中ODC活性的稳态。给予CyA不影响胰高血糖素（一种已知的由环磷酸腺苷介导的激素）或8-溴环磷酸腺苷对肾脏ODC活性的作用。地塞米松和三碘甲状腺原氨酸（T3）可提高大鼠肾脏ODC活性，在所有情况下这两种化合物都会提高血清催乳素水平，给予CyA也会阻断这种作用。表皮生长因子（EGF）本身不会诱导大鼠肾脏ODC活性，但在存在CyA的情况下能够使ODC活性产生小幅增加。CyA选择性阻断PRL诱导ODC的显著作用可能是由于CyA能够与膜中受体所需的磷脂相互作用，从而拮抗激素-受体相互作用。
