Characterization of aromatase binding agents from the dichloromethane extract of Corydalis yanhusuo using ultrafiltration and liquid chromatography tandem mass spectrometry.
Aromatase represents an important target for the treatment of hormone-dependent breast cancer. In the present study, nine alkaloids from the dichloromethane extract of Corydalis yanhusuo were identified by liquid chromatography tandem mass spectrometry (LC-MS/MS) and tested for their aromatase binding activities using an ultrafiltration LC-MS method by investigating the differences of peak areas of compounds before and after incubations with aromatase. It was demonstrated that the quaternary protoberberine alkaloids and the tertiary protoberberine alkaloids exhibited potent aromatase binding activities. The quaternary ammonium group and the methyl group at C-13 position of tertiary protoberberine alkaloids might be necessary for the activity. The findings should provide guidance for the discovery of potential aromatase inhibitors from natural products.
Shi
Jing
J
Department of Pharmacy, Zhejiang Medical College, No.481 Binwen Rd., Hangzhou 310053, China. shij136@hotmail.com
Zhang
Xiaoyu
X
Ma
Zhongjun
Z
Zhang
Min
M
Sun
Fang
F
D001141:Aromatase / Q000378:metabolism*; D002853:Chromatography, Liquid; D031311:Corydalis / Q000737:chemistry*; D008752:Methylene Chloride; D010936:Plant Extracts / Q000737:chemistry*; D011485:Protein Binding; D053719:Tandem Mass Spectrometry; D014462:Ultrafiltration
D010936:Plant Extracts; D008752:Methylene Chloride; D001141:Aromatase