Chemical onstituents and mechanism of Corydalis Rhizoma based on HPLC-QTOF/MS and G protein-coupled receptor analysis
10.16438/j.0513-4870.2016-0195
- VernacularTitle:基于HPLC-QTOF/MS及G蛋白偶联受体分析的延胡索物质基础及作用机制研究
- Author:
Yan-qi HAN
1
;
Jun XU
1
;
Su-xiao GONG
1
;
Tie-jun ZHANG
1
;
Chang-xiao LIU
2
Author Information
1. Tianjin Engineering Laboratory of Quality Control Technology of Traditional Chinese Medicine, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
2. Tianjin Center for New Drug Evaluation and Research, State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
Corydalis Rhizoma;
G protein-coupled receptor;
chemical constituent;
mechanism
- From:
Acta Pharmaceutica Sinica
2016;51(8):1302-
- CountryChina
- Language:Chinese
-
Abstract:
The chemical constituents of Corydalis Rhizoma were identified in the 60% ethanol extract using high performance liquid chromatography/electrospray ionization quadruple time-of-flight mass spectrometry (HPLC-QTOF/MS). The stimulation and inhibition effects of Corydalis Rhizoma and its representative compounds (protopine, palmatine, tetrahydropalmatine) on G protein-coupled receptor (GPCR), including 5-hydroxytryptamine 1A receptor (5-HT1A), μ opioid receptor (OPRM1), β2 adrenergic receptor (ADRB2), dopamine receptor (D2), acetylcholine receptor (M2) and thromboxane-prostaglandin receptor (TP) were explored using the fluorescence assay of intracellular calcium ion. As a result, 31 compounds were obtained and 28 alkaloid compounds were identified. The results of GPCR experiments showed that Corydalis Rhizoma could activate 5-HT1A, OPRM1, ADRB2 receptors and block D2 receptor. Protopine showed antagonism on D2 and M2 receptors, tetrahydropalmatine could agitate ADRB2 receptor and antagonize D2 and TP receptors, while palmatine showed no significant biological activity on the 6 GPCRs. In conclusion, Corydalis Rhizoma may exert biological activity by multi-components acting on multi-targets.
