期刊论文

Inhibitory Activities of Flavonoids towards AKR1C3

中文

今日药学

1674-229X

2018

28

8

505-509

10.12048/j.issn.1674-229X.2018.08.001

81602968:国家自然科学基金 2016A030313589:广东省自然科学基金 A2016201:广东省医学科学技术研究项目 201707010049:广州市科技计划

本校为其他机构

目的研究黄酮类化合物对去势抵抗性前列腺癌靶标AKR1C3的抑制活性及构效关系。方法以9,10-菲醌为反应底物,采用多功能微孔板检测仪检测化合物对辅酶NADPH消耗速率的影响。结果 3＇、4＇、5、7位含酚羟基的木犀草素、槲皮素和杨梅素对AKR1C3有显著的抑制活性,其IC（50）值分别为2.08μmol·L~（-1）,3.36μmol·L~（-1）及4.90μmol·L~（-1）。3＇、4＇、7位含酚羟基的漆黄素和2＇、4＇、5、7位含酚羟基的桑色素的抑制活性次之,IC（50）值分别为5.38μmol·L~（-1）及13.37μmol·L~（-1）,4＇、5、7位含酚羟基的高黄芩素、染料木素和4＇、7位含酚羟基的大豆苷元的抑制活性最低。结论首次发现杨...

OBJECTIVE To study the inhibitory activities and structure-activity relationship of flavonoids towards AKR1 C3, which now represents a promising therapeutic target for castration-resistant prostate cancer. METHODS The inhibitory activities of flavonoids on AKR1 C3 were determined by using multifunction microplate detector to monitor the consumption of co-enzyme NADPH with9, 10-phenanthrenequinone as substrate. RESULTS Luteolin, quercetin and myricetin containing 3'-, 4'-, 5-, and 7-hydroxyl substituents displayed significant inhibitory activiti...