原发性肝癌及癌周组织雄激素受体与^3H—R1881的特异性结合

Study on Specific Binding of Androgen Receptor with ￣3H-R1881 in Human Hepatocellular Carcinoma and Surrounding Liver Tissue

本文通过受体的放射配体结合分析，显示人原发性肝癌及癌周组织的细胞胞浆、胞核内存在能与３Ｈ－Ｒ１８８１特异结合的雄激素受体（ＡＲ），其３Ｈ－Ｒ１８８１的饱和浓度分别为３．５０ｎｍｏｌ／Ｌ、４．７５ｎｍｏｌ／Ｌ；癌及癌周组织中胞浆ＡＲ与标记配体结合的亲和力基本相同（Ｐ＞０．０５），而癌组织胞核ＡＲ的亲和力则明显降低；癌组织胞浆、胞核ＡＲ的最大结合容量（Ｂｍａｘ）均分别高于癌周组织（Ｐ＜０．０１）；以双氢睾酮、甲基睾丸素和丙酸睾丸素作竞争抑制剂，其抑制常数Ｋｉ分别为５．９３±０．６０×１０（－７）、１．６７±０．２１×１０（－３）、１．３±０．１０×１０（－２）ｍｏｌ／Ｌ。

The specific binding of androgen receptor(AR) with 3H-R1881 in the cytosol and nuclei of human hepatocellular carcinoma and surrounding liver tissue was determined by the radioligand binding assay of receptor(RBA).The saturated concentration of 3H-R1881 was 3.50 nmol/L in the cytosol and 4.75 nmol/L in the nuclei.Similar affinity for AR in the cytosol was found both in the tumor and normal tissue,but there was significant difference in the nuclei.The hepatocellular carcinoma had a significantly higher Bmax values of AR both in the cytosol and nuclei than did the surrounding liver tissue.Using dihydrotestosterone,methyltestosterone and propionate testosterone as competitors,the inhibition constants(ki) were 5.93±0.60×10(-7)、1.67±0.21×10(-3)and 1.30±0.10×10(-2)mol/L,respectively.