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Identification of a ligand for tumor necrosis factor receptor from Chinese herbs by combination of surface plasmon resonance biosensor and UPLC-MS

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Abstract

Identification of bioactive compounds directly from complex herbal extracts is a key issue in the study of Chinese herbs. The present study describes the establishment and application of a sensitive, efficient, and convenient method based on surface plasmon resonance (SPR) biosensors for screening active ingredients targeting tumor necrosis factor receptor type 1 (TNF-R1) from Chinese herbs. Concentration-adjusted herbal extracts were subjected to SPR binding assay, and a remarkable response signal was observed in Rheum officinale extract. Then, the TNF-R1-bound ingredients were recovered, enriched, and analyzed by UPLC-QTOF/MS. As a result, physcion-8-O-β-d-monoglucoside (PMG) was identified as a bioactive compound, and the affinity constant of PMG to TNF-R1 was determined by SPR affinity analysis (K D  = 376 nM). Pharmacological assays revealed that PMG inhibited TNF-α-induced cytotoxicity and apoptosis in L929 cells via TNF-R1. Although PMG was a trace component in the chemical constituents of the R. officinale extract, it had considerable anti-inflammatory activities. It was found for the first time that PMG was a ligand for TNF receptor from herbal medicines. The proposed SPR-based screening method may prove to be an effective solution to analyzing bioactive components of Chinese herbs and other complex drug systems.

Scheme of the method based on SPR biosensor for screening and recovering active ingredients from complex herbal extracts and UPLC-MS for identifying them. Scheme of the method based on SPR biosensor for screening and recovering active ingredients from complex herbal extracts and UPLC-MS for identifying them

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Abbreviations

AA:

Acetic acid

FA:

Formic acid

PMG:

Physcion-8-O-β-d-monoglucoside

SPR:

Surface plasmon resonance

TFA:

Trifluoro acid

TNF:

Tumor necrosis factor

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Acknowledgments

This work was supported by the National Natural Science Foundation of China (Nos. 81202496 and 81273472) and grants from the Second Military Medical University (No. 2011QN04).

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Correspondence to Yi-feng Chai or Jun-** Zhang.

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The authors declare that they have no conflict of interest.

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Yan Cao, Ying-hua Li and Di-ya Lv contributed equally to this work.

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Cao, Y., Li, Yh., Lv, Dy. et al. Identification of a ligand for tumor necrosis factor receptor from Chinese herbs by combination of surface plasmon resonance biosensor and UPLC-MS. Anal Bioanal Chem 408, 5359–5367 (2016). https://doi.org/10.1007/s00216-016-9633-6

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