Rapid screening of bioactive compound in Sanzi Yangqin Decoction and investigating of binding mechanism by immobilized β-adrenogic receptor chromatography coupled with molecular docking.

Screening bioactive compounds from traditional Chinese medicines plays pivotal role in preventing and curing diseases. Sanzi Yangqin Decoction (SYD) is a commonly used prescription for the treatment of cough, asthma and some other respiratory diseases for hundreds of years in practice. This reminds us that there may exist some bioactive compounds strongly binding with the recognized receptors mediating these diseases like β-adrenegic receptor (β-AR).

Curcumin suppresses colorectal tumorigenesis via the Wnt/β-catenin signaling pathway by downregulating Axin2.

Colorectal cancer (CRC) is the third most common cancer worldwide, with high incidence and mortality rates. Conventional therapies, including surgery, chemotherapy and radiation, are extensively used for the treatment of CRC. However, patients present with adverse effects, such as toxicity, hepatic injury and drug resistance.

G protein-coupled receptor-in-paper, a versatile chromatographic platform to study receptor-drug interaction.

High-performance affinity chromatography is limited by its high cost and high pressure. Paper is made up of porous fiber networks and has the properties of low cost, ease of fabrication, and biodegradable. Due to these advantages, herein, we immobilized beta2-adrenoceptor (β-AR) onto the surface of the polytetrafluoroethylene membrane, a paper-based material, and constructed a G protein-coupled receptor (GPCR)-in-paper chromatographic platform.

Reversible and site-specific immobilization of β-adrenergic receptor by aptamer-directed method for receptor-drug interaction analysis.

Immobilized protein makes a profound impact on the development of assays for drug discovery, diagnosis and in vivo biological interaction analysis. Traditional methods are enormously challenged by the G-protein coupled receptor ascribed to the loss of receptor functions. We introduced a β-adrenergic receptor (β-AR) aptamer into the immobilization of the receptor.

Screening Bioactive Compounds of Siraitia grosvenorii by Immobilized β-Adrenergic Receptor Chromatography and Druggability Evaluation.

As the first and key step of traditional Chinese medicine (TCM)-guided drug development, lead discovery necessitates continuous exploration of new methodology for screening bioactive compounds from TCM. This work intends to establish a strategy for rapidly recognizing β-adrenergic receptor (β-AR) target compounds from the fruit of (LHG). The method involved immobilization of β-AR onto amino-microsphere to synthesize the receptor column, the combination of the column to high-performance liquid chromatography (HPLC) to screen bioactive compounds of LHG, the identification of the compounds by HPLC coupled with mass spectrometry (MS), and the evaluation of druggability through pharmacokinetic examination by HPLC-MS/MS.