Radhika P, Cabeza M, Bratoeff E, García G
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.
Steroids. 2004 Jul;69(7):439-44. doi: 10.1016/j.steroids.2004.04.001.
The aim of this study is to determine the 5alpha-reductase inhibitory activity of several new steroidal compounds PR-01-PR-07 by measuring the conversion of [3H]T to[3H]DHT in Penicillium crustosum broths. These compounds were obtained from marine soft corals collected on the coasts of Andaman and Nicobar at Hori, Natkal and Kalipur (Diglipur) Islands and identified as Sinularia grandilobata Verseveldt, Sinularia crassa Tixier- Durivault, Sinularia gravis Tixier- Durivault, Sinularia sp., Lobophytum sp., Lobophytum crassum and Cladiella sp. PR-01-PR-04 significantly inhibited the conversion of [3H]T to [3H]DHT (P < 0.05) whereas PR-05 and PR-06 did not show an appreciable difference (P > 0.05) in this model. On the other hand PR-07 stimulated (P < 0.05) the enzymatic reaction.
本研究的目的是通过测量在 crustosum 青霉肉汤中[3H]睾酮([3H]T)向[3H]双氢睾酮([3H]DHT)的转化,来确定几种新的甾体化合物 PR - 01 - PR - 07 的 5α - 还原酶抑制活性。这些化合物是从在安达曼和尼科巴群岛海岸的 Hori、Natkal 和 Kalipur(迪格利普尔)岛采集的海洋软珊瑚中获得的,经鉴定为大裂片刺柳珊瑚 Sinularia grandilobata Verseveldt、厚刺柳珊瑚 Sinularia crassa Tixier - Durivault、重刺柳珊瑚 Sinularia gravis Tixier - Durivault、刺柳珊瑚属 Sinularia sp.、肉芝软珊瑚属 Lobophytum sp.、厚肉芝软珊瑚 Lobophytum crassum 和 Cladiella sp.。在该模型中,PR - 01 - PR - 04 显著抑制了[3H]T 向[3H]DHT 的转化(P < 0.05),而 PR - 05 和 PR - 06 没有表现出明显差异(P > 0.05)。另一方面,PR - 07 刺激了(P < 0.05)酶促反应。