Ganguly M, Cheo K L, Brodie H J
Biochim Biophys Acta. 1976 May 27;431(2):326-34. doi: 10.1016/0005-2760(76)90153-3.
(1) In order to study the relationship between aromatization (estrogen biosynthesis) and 1beta-hydroxylation, the effects of a variety of factors on these processes were evaluated. (2) Using the C18 substrate, 4-estrene-3,17-dione, it was found that carbon monoxide, SU-4885, amphenone B, potassium cyanide, 4-androstene-3,17-dione and 1,4-androstadiene-3,17-dione inhibited the above transformations significantly and to varying degrees. However, within a given experiment the inhibition of each process was similar. (3) SKF-525A did not inhibit either transformation. In addition, phosphate, Tris and barbital buffers, as well as pH changes from 6.9 to 7.7, had no stimulatory or inhibitory effect on the production of estrogen and 1beta-hydroxy compounds. (4) In contrast, several inhibitors affected the aromatization of C19 and C18 steroids differently. These include carbon monoxide, SU-4885 and amphenone B. (5) When a mixture of 4-[7beta-3Hi1estrene-3,17-dione and 19-[4-14C]nortestosterone were incubated together the former was preferentially converted to estrogen. This preference for the 17-keto steroidal form mimics results observed for C19 substrates. (6) We conclude that while estrogen biosynthesis and 1beta-hydroxylation appear to be mediated by the same enzyme system, the same conclusion cannot be drawn for the aromatization of C19 and C18 substrates.
(1)为了研究芳香化作用（雌激素生物合成）与1β-羟基化作用之间的关系，评估了多种因素对这些过程的影响。(2)使用C18底物4-雌甾烯-3,17-二酮，发现一氧化碳、SU-4885、氨苯酮B、氰化钾、4-雄甾烯-3,17-二酮和1,4-雄二烯-3,17-二酮均能不同程度地显著抑制上述转化。然而，在给定的实验中，每个过程的抑制作用相似。(3)SKF-525A对两种转化均无抑制作用。此外，磷酸盐、Tris和巴比妥缓冲液以及pH值从6.9到7.7的变化对雌激素和1β-羟基化合物的产生没有刺激或抑制作用。(4)相比之下，几种抑制剂对C19和C18类固醇的芳香化作用影响不同。这些抑制剂包括一氧化碳、SU-4885和氨苯酮B。(5)当将4-[7β-3H]雌甾烯-3,17-二酮和19-[4-14C]去甲睾酮的混合物一起孵育时，前者优先转化为雌激素。这种对17-酮甾体形式的偏好与C19底物的观察结果相似。(6)我们得出结论，虽然雌激素生物合成和1β-羟基化作用似乎由同一酶系统介导，但对于C19和C18底物的芳香化作用不能得出相同结论。
