Rapid screening and identification of bioactive compounds specifically binding to beta 2-adrenoceptor from San-ao decoction using affinity magnetic fine particles coupled with high-performance liquid chromatography-mass spectrometry.

Abstract

BACKGROUND:

San-ao decoction (SAD) has been widely used in Chinese medicine against respiratory diseases, such as asthma and rhinallergosis. The bioactive compounds for such pharmacological action remain unknown.

METHODS:

We developed a methodology to isolate the bioactive compounds of SAD. The assay involved the immobilization of beta 2-adrenoceptor (β 2-AR) onto magnetic fine particles, the capture of target compounds by the immobilized receptor, the identification of the receptor bound compounds by reversed-phase high-performance liquid chromatography coupled with tandem mass spectrometry.

RESULTS:

Vicenin, shaftoside, isoshaftoside, liquiritin apioside and isoliquiritin apioside were identified as β 2-AR ligands in SAD extract. The binding of these compounds to β 2-AR occurred on serine169, serine170 and phenylalanine256 of the receptor.

CONCLUSIONS:

The developed methodology has high stability and specificity for recognizing and isolating target compounds. It is an alternative method for rapidly screening bioactive compounds of immobilized receptor from Chinese prescriptions.

• Authors: Fuhuan Fei, Huanmei Sun, Xixi Cheng, Jiajun Liu, Jing Wang, Qian Li, Yajun Zhang
• Journal: Chinese medicine (Chin Med) Vol. 13 Pg. 49 ( 2018) ISSN: 1749-8546 [Print] England
• PMID: 30258489 (Publication Type: Journal Article)