Fu Jing, Shen Zhong-Hua, Cheng Fei-Xiong, Liu Gui-Xia, Li Wei-Hua, Tang Yun
School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Yao Xue Xue Bao. 2012 Jan;47(1):18-28.
Aromatase is a key enzyme responsible for in vivo estrogen biosynthesis. Inhibition of the activity of the aromatase has become an alterative way for treatment of breast cancer. In this review, the structure and catalytic mechanism of the aromatase is briefly introduced followed by thorough review of the progress in the study of the steroidal and non-steroidal aromatase inhibitors. This review is focused on the natural compounds that exhibit the aromatase inhibition, which include flavonoids, xanthones, coumarins, and sesquiterpenes. The structure-activity relationship of these compounds is also discussed.
芳香化酶是负责体内雌激素生物合成的关键酶。抑制芳香化酶的活性已成为治疗乳腺癌的一种替代方法。在本综述中，简要介绍了芳香化酶的结构和催化机制，随后全面综述了甾体和非甾体芳香化酶抑制剂的研究进展。本综述重点关注具有芳香化酶抑制作用的天然化合物，包括黄酮类、呫吨酮类、香豆素类和倍半萜类。还讨论了这些化合物的构效关系。
