A strategy of screening and binding analysis of bioactive components from traditional Chinese medicine based on surface plasmon resonance biosensor

• Published in: Journal of pharmaceutical analysis Vol. 12; no. 3; pp. 500 - 508
• Main Authors: Lv, Diya, Xu, Jin, Qi, Minyu, Wang, Dongyao, Xu, Weiheng, Qiu, Lei, Li, Yinghua, Cao, Yan
• Format: Journal Article
• Language: English
• Published: Xi'an Elsevier B.V 01.06.2022; Xi'an Jiaotong University, Journal of Pharmaceutical Analysis; Center for Instrumental Analysis,School of Pharmacy,Second Military Medical University,Shanghai,200433,China%Department of Neurology,Changzheng Hospital,Second Military Medical University,Shanghai,200003,China%Department of Biochemical Pharmacy,School of Pharmacy,Second Military Medical University,Shanghai,200433,China%Department of Pharmaceutical Analysis,School of Pharmacy,Second Military Medical University,Shanghai,200433,China%Institute of Translational Medicine,Shanghai University,Shanghai,200444,China; Xi'an Jiaotong University; Elsevier
• Subjects: Apoptosis; Binding analysis; Bioactive components; Biosensors; Chinese medicine; Chromatography; Competition; Cytokines; Cytotoxicity; Drug development; Inflammation; Ingredients; Mass spectrometry; Modernization; Original; Proteins; Radix Paeoniae Alba; Scientific imaging; Screening; Sensors; Signal transduction; Surface plasmon resonance; Traditional Chinese medicine; Tumor necrosis factor-TNF; Tumor necrosis factor-α; United States > US; Sweden; China; Screening; Surface plasmon resonance; Bioactive components; Binding analysis; Radix Paeoniae Alba
• ISSN: 2095-1779; 2214-0883
• DOI: 10.1016/j.jpha.2021.11.006

Elucidating the active components of traditional Chinese medicine (TCM) is essential for understanding the mechanisms of TCM and promote its rational use as well as TCM-derived drug development. Recent studies have shown that surface plasmon resonance (SPR) technology is promising in this field. In the present study, we propose an SPR-based integrated strategy to screen and analyze the major active components of TCM. We used Radix Paeoniae Alba (RPA) as an example to identify the compounds that can account for its anti-inflammatory mechanism via tumor necrosis factor receptor type 1 (TNF-R1). First, RPA extraction was analyzed using an SPR-based screening system, and the potential active ingredients were collected, enriched, and identified as paeoniflorin and paeonol. Next, the affinity constants of paeoniflorin and paeonol were determined as 4.9 and 11.8 μM, respectively. Then, SPR-based competition assays and molecular docking were performed to show that the two compounds could compete with tumor necrosis factor-α (TNF-α) while binding to the subdomain 1 site of TNF-R1. Finally, in biological assays, the two compounds suppressed cytotoxicity and apoptosis induced by TNF-α in the L929 cell line. These findings prove that SPR technology is a useful tool for determining the active ingredients of TCM at the molecular level and can be used in various aspects of drug development. The SPR-based integrated strategy is reliable and feasible in TCM studies and will shed light on the elucidation of the pharmacological mechanism of TCM and facilitate its modernization. [Display omitted] •A surface plasmon resonance-based integrated strategy was established to analyze traditional Chinese medicine.•Surface plasmon resonance technology can be used for ligand screening, affinity detection, and binding site confirmation.•Paeoniflorin and paeonol were identified as TNF-R1-bound ingredients in RPA.