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A novel sample preparation and on-line HPLC-DAD-MS/MS-BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: case study of α-glucosidase.
J Pharm Biomed Anal. 2014 Jan; 88:130-5.JP

Abstract

Drug discovery from complex mixture like Chinese herbs is a challenge and extensive false positives make the obtainment of specific bioactive compounds difficult. In the present study, a novel sample preparation method was proposed to rapidly reveal the specific bioactive compounds from complex mixtures using α-glucosidase as a case. Firstly, aqueous and methanol extracts of 500 traditional Chinese medicines were carried out with the aim of finding new sources of α-glucosidase inhibitors. As a result, the extracts of fruit of Terminalia chebula (FTC), flowers of Rosa rugosa (FRR) and Eugenia caryophyllata (FEC) as well as husk of Punica granatum (HPG) showed high inhibition on α-glucosidase. On-line liquid chromatography-diode array detection-tandem mass spectrometry and biochemical detection (HPLC-DAD-MS/MS-BCD) was performed to rapidly screen and characterize α-glucosidase inhibitors in these four extracts. After tentative identification, most of compounds with inhibitory activity in the investigated crude extracts were found to be tannins commonly recognized as non-specific enzyme inhibitors in vitro. Subsequently, the four extracts were treated with gelatin to improve specificity of the on-line system. Finally, two compounds with specific α-glucosidase inhibition were identified as corilagin and ellagic acid. The developed method could discover specific α-glucosidase inhibitors in complex mixtures such as plant extracts, which could also be used for discovery of specific inhibitors of other enzymes.

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Authors+Show Affiliations

Li DQ
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Zhao J
No affiliation info available
Xie J
No affiliation info available
Li SP
No affiliation info available

MeSH

Chromatography, High Pressure LiquidDrug DiscoveryEllagic AcidEnzyme InhibitorsFlowersGelatinGlucosidesHydrolyzable TanninsKineticsLythraceaeMedicine, Chinese TraditionalPlant ExtractsPlant LeavesPlant PreparationsReproducibility of ResultsRosaSyzygiumTandem Mass SpectrometryTanninsTerminaliaalpha-Glucosidases

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24055848

Citation

Li, D Q., et al. "A Novel Sample Preparation and On-line HPLC-DAD-MS/MS-BCD Analysis for Rapid Screening and Characterization of Specific Enzyme Inhibitors in Herbal Extracts: Case Study of Α-glucosidase." Journal of Pharmaceutical and Biomedical Analysis, vol. 88, 2014, pp. 130-5.
Li DQ, Zhao J, Xie J, et al. A novel sample preparation and on-line HPLC-DAD-MS/MS-BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: case study of α-glucosidase. J Pharm Biomed Anal. 2014;88:130-5.
Li, D. Q., Zhao, J., Xie, J., & Li, S. P. (2014). A novel sample preparation and on-line HPLC-DAD-MS/MS-BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: case study of α-glucosidase. Journal of Pharmaceutical and Biomedical Analysis, 88, 130-5. https://doi.org/10.1016/j.jpba.2013.08.029
Li DQ, et al. A Novel Sample Preparation and On-line HPLC-DAD-MS/MS-BCD Analysis for Rapid Screening and Characterization of Specific Enzyme Inhibitors in Herbal Extracts: Case Study of Α-glucosidase. J Pharm Biomed Anal. 2014;88:130-5. PubMed PMID: 24055848.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A novel sample preparation and on-line HPLC-DAD-MS/MS-BCD analysis for rapid screening and characterization of specific enzyme inhibitors in herbal extracts: case study of α-glucosidase. AU - Li,D Q, AU - Zhao,J, AU - Xie,J, AU - Li,S P, Y1 - 2013/08/31/ PY - 2013/06/13/received PY - 2013/08/20/revised PY - 2013/08/21/accepted PY - 2013/9/24/entrez PY - 2013/9/24/pubmed PY - 2014/7/30/medline KW - Corilagin KW - Ellagic acid KW - LC–DAD–MS/MS–BCD KW - α-Glucosidase inhibitors SP - 130 EP - 5 JF - Journal of pharmaceutical and biomedical analysis JO - J Pharm Biomed Anal VL - 88 N2 - Drug discovery from complex mixture like Chinese herbs is a challenge and extensive false positives make the obtainment of specific bioactive compounds difficult. In the present study, a novel sample preparation method was proposed to rapidly reveal the specific bioactive compounds from complex mixtures using α-glucosidase as a case. Firstly, aqueous and methanol extracts of 500 traditional Chinese medicines were carried out with the aim of finding new sources of α-glucosidase inhibitors. As a result, the extracts of fruit of Terminalia chebula (FTC), flowers of Rosa rugosa (FRR) and Eugenia caryophyllata (FEC) as well as husk of Punica granatum (HPG) showed high inhibition on α-glucosidase. On-line liquid chromatography-diode array detection-tandem mass spectrometry and biochemical detection (HPLC-DAD-MS/MS-BCD) was performed to rapidly screen and characterize α-glucosidase inhibitors in these four extracts. After tentative identification, most of compounds with inhibitory activity in the investigated crude extracts were found to be tannins commonly recognized as non-specific enzyme inhibitors in vitro. Subsequently, the four extracts were treated with gelatin to improve specificity of the on-line system. Finally, two compounds with specific α-glucosidase inhibition were identified as corilagin and ellagic acid. The developed method could discover specific α-glucosidase inhibitors in complex mixtures such as plant extracts, which could also be used for discovery of specific inhibitors of other enzymes. SN - 1873-264X UR - https://www.unboundmedicine.com/medline/citation/24055848/A_novel_sample_preparation_and_on_line_HPLC_DAD_MS/MS_BCD_analysis_for_rapid_screening_and_characterization_of_specific_enzyme_inhibitors_in_herbal_extracts:_case_study_of_α_glucosidase_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0731-7085(13)00384-1 DB - PRIME DP - Unbound Medicine ER -