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利用尼罗罗非鱼(Oreochromis niloticus)肝脏微粒体研究抗芳香化酶活性。

Investigation of antiaromatase activity using hepatic microsomes of Nile tilapia (Oreochromis niloticus).

作者信息

Sassa-Deepaeng Tanongsak, Chaisri Wasana, Pikulkaew Surachai, Okonogi Siriporn

机构信息

Nanoscience and Nanotechnology Program, the Graduate School, Chiang Mai University.

Department of Food Animal Clinic, Faculty of Veterinary Medicine, Chiang Mai University.

出版信息

Drug Discov Ther. 2017 May 30;11(2):84-90. doi: 10.5582/ddt.2017.01006. Epub 2017 Mar 19.

Abstract

Microsomal aromatase enzymes of humans and rats have been used in antiaromatase assays, but enzyme activity is species-specific. The current study extracted hepatic microsomes of Nile tilapia (Oreochromis niloticus) to investigate and compare the antiaromatase activity of chrysin, quercetin, and quercitrin. This activity was evaluated using a dibenzylfluorescein (DBF) assay. Results revealed that the age and body weight of Nile tilapia affected the yield of extracted microsomes. Extraction of hepatic microsomes of Nile tilapia was most effective when using a reaction medium with a pH of 8.0. A DBF assay using Nile tilapia microsomes revealed significant differences in levels of antiaromatase activity for chrysin, quercetin, and quercitrin. Chrysin was the most potent aromatase inhibitor, with an IC50 of 0.25 mg/mL. In addition, chrysin is an aromatase inhibitor that also inhibits the proliferation of cancer cells. Hepatic microsomes of Nile tilapia can be used to investigate and compare the antiaromatase activity of different compounds.

摘要

人类和大鼠的微粒体芳香化酶已用于抗芳香化酶测定,但酶活性具有物种特异性。当前研究提取尼罗罗非鱼(Oreochromis niloticus)的肝脏微粒体,以研究和比较白杨素、槲皮素和芦丁的抗芳香化酶活性。使用二苄基荧光素(DBF)测定法评估该活性。结果显示,尼罗罗非鱼的年龄和体重影响提取的微粒体产量。使用pH为8.0的反应介质时,尼罗罗非鱼肝脏微粒体的提取最为有效。使用尼罗罗非鱼微粒体的DBF测定法显示,白杨素、槲皮素和芦丁的抗芳香化酶活性水平存在显著差异。白杨素是最有效的芳香化酶抑制剂,IC50为0.25 mg/mL。此外,白杨素是一种芳香化酶抑制剂,还能抑制癌细胞的增殖。尼罗罗非鱼的肝脏微粒体可用于研究和比较不同化合物的抗芳香化酶活性。

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