Batra S, Iosif C S
Department of Obstetrics and Gynecology, University of Lund, Sweden.
Anticancer Res. 2000 Jan-Feb;20(1A):463-6.
Since elevated concentrations of peripheral benzodiazepine (PBZr) have been reported in some tumors it was of interest to study the distribution PBZr in the endometrium and endometrial carcinoma. A specific ligand or PK 11195 was used to measure PBZr in the mitochondria (m-fraction) and the microsomal fraction (p-fraction). Density of binding sites and binding affinity (KD) was computed from Scatchard analysis. Binding in both m- and p-fractions from endometrium and endometrial carcinoma were saturable and of high affinity. The PBZr density in p-fraction from endometrium was slightly higher than in m-fraction, whereas the binding in m-fraction in endometrial carcinoma was more than 2-fold higher than in p-fraction. The difference between the densities in m-fraction from endometrial cancer and endometrium was highly significant (p < 0.005). There was no significant difference in the binding affinities (KD values) for PK 11195 in the various fractions. The selective increase in the density of PBZr in mitochondria of tumors suggests an association with energy demand and utilization and could be of diagnostic and/or therapeutic value in endometrial cancer. The role of a relatively high density of PBZr in microsomal fractions remains to be elucidated.
由于在一些肿瘤中已报道外周苯二氮䓬（PBZr）浓度升高，因此研究PBZr在子宫内膜和子宫内膜癌中的分布很有意义。使用一种特异性配体或PK 11195来测量线粒体（m组分）和微粒体组分（p组分）中的PBZr。结合位点密度和结合亲和力（KD）通过Scatchard分析计算得出。来自子宫内膜和子宫内膜癌的m组分和p组分中的结合均具有饱和性且亲和力高。子宫内膜p组分中的PBZr密度略高于m组分，而子宫内膜癌m组分中的结合比p组分高2倍以上。子宫内膜癌和子宫内膜m组分密度之间的差异非常显著（p < 0.005）。各组分中PK 11195的结合亲和力（KD值）没有显著差异。肿瘤线粒体中PBZr密度的选择性增加表明其与能量需求和利用有关，可能对子宫内膜癌具有诊断和/或治疗价值。微粒体组分中相对较高密度的PBZr的作用仍有待阐明。
