Center of Scientific Research, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
The Gynecology and Obstetrics Department, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
Biomed Res Int. 2017;2017:8284097. doi: 10.1155/2017/8284097. Epub 2017 Dec 10.
Human aromatase (CYP19A1) is an important enzyme, which produces estrogen from androgen for maintaining the female reproductive function and pregnancy. Triclocarban and triclosan are antimicrobial chemicals added to personal care, household, and industrial products. They could be endocrine disruptors and may disrupt human CYP19A1 activity. In the present study, we investigated the effects of triclocarban and triclosan on estradiol production and human CYP19A1 activity in JEG-3 cells. Triclocarban and triclosan reduced estradiol production in JEG-3 cells. Triclocarban and triclosan inhibited human CYP19A1 with IC values of 15.81 and 6.26 M, respectively. Triclosan competitively inhibited CYP19A1, while triclocarban noncompetitively inhibited this enzyme. Docking study showed that triclosan bound to the steroid-binding pocket of CYP19A1, while triclocarban was off this target, suggesting a different mechanism. In conclusion, triclocarban and triclosan are inhibitors of human CYP19A1.
人类芳香酶（CYP19A1）是一种重要的酶，它可以将雄激素转化为雌激素，从而维持女性生殖功能和妊娠。三氯卡班和三氯生是添加到个人护理、家庭和工业产品中的抗菌化学品。它们可能是内分泌干扰物，可能会干扰人类 CYP19A1 的活性。在本研究中，我们研究了三氯卡班和三氯生对 JEG-3 细胞中雌二醇产生和人 CYP19A1 活性的影响。三氯卡班和三氯生降低了 JEG-3 细胞中的雌二醇产生。三氯卡班和三氯生对人 CYP19A1 的抑制 IC50 值分别为 15.81 和 6.26 μM。三氯生竞争性抑制 CYP19A1，而三氯卡班非竞争性抑制该酶。对接研究表明，三氯生结合到 CYP19A1 的甾体结合口袋，而三氯卡班则不在这个靶点上，提示其作用机制不同。总之，三氯卡班和三氯生是人类 CYP19A1 的抑制剂。
