环孢霉素A对人单个核白细胞糖皮质激素受体和雌激素受体的影响及意义

Effects of Cyclosporine A on Glucocorticoid and Estradial Receptors of Human Mononuclear Leukocytes and Its Significance

用放射配体结合分析，体外实验观察了环孢霉素Ａ（ＣｓＡ）、环磷酰胺（ＣＴＸ）及甲基强的松龙对人单个核白细胞（ＭＮＬ）的糖皮质激素受体（ＧＲ）和雌激素受体（ＥＲ）结合容量的影响，以阐明ＣｓＡ免疫抑制作用的机制，并为联合用药提供理论依据。当ＣｓＡ浓度为１００ｎｇ／ｍｌ时，ＧＲ和ＥＲ的结合容量无改变；５００和１０００ｎｇ／ｍｌ时，ＧＲ结合容量升高３０％左右，ＥＲ的降低３０％左右；２０００和１００００ｎｇ／ｍｌ时，ＧＲ和ＥＲ结合容量均降低５０％左右。ＣＴＸ和甲强龙均使ＧＲ和ＥＲ结合容量降低。当ＣｓＡ与ＣＴＸ和甲强龙合用时，可以逆转ＣＴＸ和甲强龙对ＧＲ的抑制作用，故可充分发挥免疫抑制作用。

Effects of cyelosporine A (CsA),cyclophosphamide (CTX) and medrol on glucocorticoid receptor (GR) and estradial receptor (ER) of human peripheral mononuclear leukocytes (MNL) were studied in vitro by radioligand binding assay. The binding capacity of GR and ER was not changed at a concentration of 100 ng/ml of CsA. When the concentration of CsA was 500 and 1000 ng/ml,the binding capacity of GR was raised by 30%,while ER was reduced by 30%. At a concentration of 2000 and 10000 ng/ml,the bindng capacity of both GR and ER was lowered by 50%. Both CTX and medrol decreased the binding capacity of GR and ER. Combined administration of CsA ,CTX and medrol increased by 15% the binding capacity of GR which was significantly higher than that of controls (P<0. 05). The findings suggest that CsA may reverse the inhibition of CTX and medrol on GR and explain the better therapeutic effect of CsA compared to CTX and medrol.