Photoreactivity of some light-sensitive estrogen derivatives. Use of an exchange assay to determine their photointeraction with the rat uterine estrogen binding protein.
Photoreactivity of some light-sensitive estrogen derivatives. Use of an exchange assay to determine their photointeraction with the rat uterine estrogen binding protein.
复制标题
一些光敏雌激素衍生物的光反应性。
作者：
J. Katzenellenbogen;H. J. Johnson;K. Carlson;H. N. Myers
本文用大鼠子宫胞浆交换法测定了20种雌激素衍生物（4种叠氮化合物、4种重氮化合物、4种三芳基乙烯化合物和8种其它化合物）的光反应性。将光敏衍生物与含有或不含有雌二醇的大鼠子宫上清液部分在4 ℃下孵育1-2小时。然后在2 ℃下用254 nm或315 nm光照射。同时取出样品用于测定氚化雌激素结合位点。计算了光解消耗的反应效率或雌激素结合能力的百分比。叠氮化物和重氮化合物的反应效率为0%-21%，三芳基乙烯的反应效率为20%-51%。苯偶酰、邻碘苯酚、邻硝基苯酚、α-肟酮、二苯乙烯和苯乙烯发色团不反应。反应的动力学通常是双相的，由于光敏部分的光解和解释为雌激素结合蛋白的直接光解降解的较慢的速率，具有快速的初始速率。6-氧代雌二醇具有一级反应。
The photoreactivity of 20 estrogen derivatives (4 azides 4 diazos 4 triarylethylenes and 8 miscellaneous) was analyzed by a rat uterus cytosol exchange assay. The photosensitive derivative was incubated with rat uterus supernatant fraction with or without estradiol for 1-2 hours at 4 degrees C. then irradiated with 254 nm or 315 nm light at 2 degrees C. while samples were removed for assay of tritiated estrogen-binding sites. The reaction efficiency or percent of estrogen-binding capacity consumed by photolysis was computed. The reaction efficiency of azides and diazos ranged from 0%-21% and of triarylethylenes 20%-51%. Benzil o-iodophenol o-nitrophenol alpha-oximo ketone stilbene and styrene chromophores were unreactive. The kinetics of reaction was usually biphasic with a rapid initial rate due to photolysis of the photosensitive moiety and a slower rate interpreted as direct photolytic degradation of the estrogen-binding protein. 6-oxoestradiol had a first order reaction.