Screening the bioactive compounds in aqueous extract of Coptidis rhizoma which specifically bind to rabbit lung tissues β2-adrenoceptor using an affinity chromatographic selection method

Zhao, Xinfeng; Yang, Nan; Xiao, Chaoni; Zheng, Jianbin; Zheng, Xiaohui; Wei, Yinmao; Zhang, Youyi

doi:10.1016/j.jchromb.2010.05.040

Cited by 24 publications

(15 citation statements)

References 43 publications

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“…The assay proves to be an alternative for investigating the interaction between drug and receptor and screening bioactive compounds from complex system such as traditional Chinese medicine [23,24]. This study was designed to develop another stationary phase attaching a 1 -AR for exploring the interaction between prazosin hydrochloride and the receptor.…”

Section: Introductionmentioning

confidence: 99%

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Zhao

Huang

et al. 2012

Chromatographia

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Binding interaction between ligand and G-protein coupled receptor plays an important role in the several steps of exertion of therapeutic effect by a drug and has become increasingly interesting to pharmacists, chemists, biologists and companies. a 1 -Adrenoceptor (a 1 -AR) was purified from cell line which stably expressed a 1 -AR and evenly immobilized on the surface of macroporous silica gel to prepare a novel stationary phase for investigating the interaction between drug and receptor. Control drugs of a 1 -AR including phentolamine, terazosin and urapidil were used to characterize the retention properties of the stationary phase containing the receptor. Further work was performed to calculate the binding sites and association constant of prazosin binding to the immobilized receptor. The results presented a value of 4.55 9 10 -7 M -1 for binding sites and of 2.2 9 10 4 M for the association constant during the interaction between prazosin and a 1 -AR. The proposed affinity method was stable at least in seven consecutive days, as well as had the primary bioactivities of recognizing and binding the ligand, providing an alternative for representing the interaction between drug and functional protein.

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Section: Introductionmentioning

confidence: 99%

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Zhao

Huang

et al. 2012

Chromatographia

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“…Zhao et al. have screened and identified four bioactive compounds from aqueous extract of Coptidis rhizome by β 2 ‐AR chromatography. An et al.…”

Section: Resultsmentioning

confidence: 99%

“…Superior to serum albumin, GPCRs have proved to be the targets of almost 50% of approved drugs due to high-specific binding interaction between the receptors and their ligands. Zhao et al [40] have screened and identified four bioactive compounds from aqueous extract of Coptidis rhizome by β 2 -AR chromatography. An et al [41] screened sinapine as the bioactive compounds specifically binding to β 2 -AR from Semen sinapis.…”

Section: Comparison With Other Screening Methodsmentioning

confidence: 99%

Bioactive compounds of Shuang-Huang-Lian prescription and an insight into its binding mechanism by β₂-adrenoceptor chromatography coupled with site-directed molecular docking

Wang

Li²,

Zeng

et al. 2017

J. Sep. Sci.

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Owing to the promising clinical efficacy and relatively simple composition, Shuang-Huang-Lian prescription is widely prescribed for the treatment of acute upper respiratory tract infection and acute bronchitis in practice. This necessitates the understanding of the bioactive compounds of the prescription and their binding mechanism to β -adrenoceptor, which mediates the aforementioned ailments. In this work, a column containing immobilized β -adrenoceptor was prepared using a diazonium salt reaction. The bioactive compound collected from the β -adrenoceptor column was identified as chlorogenic acid by using high-performance liquid chromatography coupled with ion trap mass spectrometry. Using an injection amount dependent method, chlorogenic acid proved the binding to β -adrenoceptor through two kinds of sites. The numbers of the sites were (1.42 ± 0.03) × 10 and (9.06 ± 0.49) × 10 M. The association constants were (2.72 ± 0.01) × 10 and (2.80 ± 0.01) × 10 M , respectively. Molecular docking analysis of the interaction between chlorogenic acid and β -adrenoceptor indicated that the binding mainly occurred on Ser , Ser , and Phe of β -adrenoceptor. These results paved the way to screen bioactive compounds of other traditional medicines by receptor chromatography.

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“…The major issue of these researches is the relative lack of specificity. Receptors, the main target for drugs, are also immobilized on silica gel to construct more specific receptor-based stationary phase for screening bioactive compounds from traditional medicines [42][43][44]. Although the specificity improved greatly, the receptor-based stationary phase has limitations because it is difficult to maintain the natural conformation of the receptor without a bilayer membrane system.…”

Section: Comparison With Other Hpac Screening Methodsmentioning

confidence: 99%

Screening bioactive compounds from Ligusticum chuanxiong by high density immobilized human umbilical vein endothelial cells

Wang

Liu

et al. 2015

Anal Bioanal Chem

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High throughput screening methodologies play a very important role in screening bioactive compounds from complex media. In this work, a new strategy for attaching cells onto amino microspheres using human umbilical vein endothelial cells (HUVECs) as a probe was developed. The immobilization depended on the specific affinity between integrin on the cells and the RGD peptide, which was coated on poly[oligo (ethylene glycol) methacrylate] by atom transfer radical polymerization. Validated application of the stationary phase was performed in the analysis of Ligusticum chuanxiong extraction by high performance affinity chromatography-mass spectrometry. Three compounds were screened as the bioactive compounds of Ligusticum chuanxiong. Two of them were identified as 3-butyl-hexahydroisobenzofuran-1(3H)-one and tetramethylpyrazine (TMP), whereas the other one remains indistinct. The association constant of vascular endothelial growth factor (VEGF) and TMP binding to VEGF receptor (VEGFR) on HUVECs were calculated to be (1.04 ± 0.08) × 10(11) M(-1) and (9.84 ± 1.11) × 10(8) M(-1) by zonal elution. Molecular docking showed that one hydrogen bond was formed between N atom of TMP and 3-N atom of imidazole group in histidine(223) of VEGFR. Both zonal elution and molecular docking indicated that TMP and VEGF bind to the same site of VEGFR on HUVECs. It is possible to become a promising tool for high throughput screening of the bioactive compounds binding to HUVECs through broad application of the stationary phase.

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Screening the bioactive compounds in aqueous extract of Coptidis rhizoma which specifically bind to rabbit lung tissues β2-adrenoceptor using an affinity chromatographic selection method

Cited by 24 publications

References 43 publications

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Bioactive compounds of Shuang-Huang-Lian prescription and an insight into its binding mechanism by β₂-adrenoceptor chromatography coupled with site-directed molecular docking

Screening bioactive compounds from Ligusticum chuanxiong by high density immobilized human umbilical vein endothelial cells

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Screening the bioactive compounds in aqueous extract of Coptidis rhizoma which specifically bind to rabbit lung tissues β2-adrenoceptor using an affinity chromatographic selection method

Cited by 24 publications

References 43 publications

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Binding Interaction Between Prazosin and Immobilized Receptor by Frontal Analysis

Bioactive compounds of Shuang-Huang-Lian prescription and an insight into its binding mechanism by β2-adrenoceptor chromatography coupled with site-directed molecular docking

Screening bioactive compounds from Ligusticum chuanxiong by high density immobilized human umbilical vein endothelial cells

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Bioactive compounds of Shuang-Huang-Lian prescription and an insight into its binding mechanism by β₂-adrenoceptor chromatography coupled with site-directed molecular docking