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 in-gredients were collected,enriched,and identified as paeoniflorin and paeonol.Next,the affinity con-stants 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 in-gredients 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 eluci-dation of the pharmacological mechanism of TCM and facilitate its modernization.

Diya Lv;Jin Xu;Minyu Qi;Dongyao Wang;Weiheng Xu;Lei Qiu;Yinghua Li;Yan Cao

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

药物分析学报（英文）

[1]Diya Lv;Jin Xu;Minyu Qi;Dongyao Wang;Weiheng Xu;Lei Qiu;Yinghua Li;Yan Cao-.A strategy of screening and binding analysis of bioactive components from traditional Chinese medicine based on surface plasmon resonance biosensor)[J].药物分析学报（英文）,2022(03):500-508

gredients

strategy,screening,binding,analysis,bioactive,components,from,traditional,Chinese,medicine,surface,plasmon,resonance,biosensor,Elucidating,TCM,essential,understanding,mechanisms,promote,its,rational,well,derived,drug,development,Recent,studies,have,shown,that,SPR,technology,promising,this,field,In,present,study,propose,integrated,major,We,used,Radix,Paeoniae,Alba,RPA,example,identify,compounds,can,account,anti,inflammatory,via,tumor,necrosis,receptor,type,R1,First,extraction,was,analyzed,using,system,potential,were,collected,enriched,identified,paeoniflorin,paeonol,Next,affinity,con,stants,determined,respectively,Then,competition,assays,molecular,docking,performed,two,could,compete,while,subdomain,site,Finally,biological,suppressed,cytotoxicity,apoptosis,induced,by,L929,cell,line,These,findings,prove,useful,tool,determining,level,be,various,aspects,reliable,feasible,will,shed,light,eluci,dation,pharmacological,facilitate,modernization

0.545633