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Journal of Zhejiang University SCIENCE B 2009 Vol.10 No.4 P.243-250

http://doi.org/10.1631/jzus.B0820340


A system for screening agonists targeting β2-adrenoceptor from Chinese medicinal herbs


Author(s):  Hui WANG, Shi-you LI, Chuan-ke ZHAO, Xin ZENG

Affiliation(s):  Graduate School of the Chinese Academy of Sciences, Beijing 100039, China; more

Corresponding email(s):   lishiyou@big.ac.cn

Key Words:  &beta, 2-adrenoceptor, Enhanced green fluorescent protein (EGFP), Chinese medicinal herbs, Screening


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Hui WANG, Shi-you LI, Chuan-ke ZHAO, Xin ZENG. A system for screening agonists targeting β2-adrenoceptor from Chinese medicinal herbs[J]. Journal of Zhejiang University Science B, 2009, 10(4): 243-250.

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%A Shi-you LI
%A Chuan-ke ZHAO
%A Xin ZENG
%J Journal of Zhejiang University SCIENCE B
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%I Zhejiang University Press & Springer
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T1 - A system for screening agonists targeting β2-adrenoceptor from Chinese medicinal herbs
A1 - Hui WANG
A1 - Shi-you LI
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A1 - Xin ZENG
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VL - 10
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SP - 243
EP - 250
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PB - Zhejiang University Press & Springer
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DOI - 10.1631/jzus.B0820340


Abstract: 
In order to develop a model for screening the agonists of human &beta;2-adrenoceptor from chinese medicinal herbs extracts, we used a cell-based functional assay based on a common G protein-coupled receptor (GPCR) regulation mechanism and destabilized enhanced green fluorescent protein (d2EGFP) reporter gene technique. The positive cell clone was confirmed by real-time polymerase chain reaction (PCR) and imaging analysis. To assess the value of this model, we screened over 2000 high performance liquid chromatography (HPLC)-fractionated samples from the ethanol extracts of chinese medicinal herbs. Six fractions (isolated from Panax japonicus, Veratrum nigrum, Phellodendron amurense, Fructus Aurantii Immaturus, Chaenomeles speciosa, and Dictamnus dasycarpus) showed significant effects on active reporter gene expression, three of which (isolated from Phellodendron amurense, Fructus Aurantii Immaturus, and Chaenomeles speciosa) were selected for further concentration response analysis and the half maximal effective concentration (EC1/2 max) values were 4.2, 2.7, and 4.8 µg/ml, respectively. Therefore, this reporter gene assay was suitable for screening &beta;2-adrenoceptor agonists. The results suggest that the six herbal extracts are the possible agonists of &beta;2-adrenoceptor.

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