title: An activity-integrated strategy involving ultra-high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry and fraction collector for rapid screening and characterization of the α-glucosidase inhibitors in Coptis chinensis Franch. (Huanglian).
abstract: An activity integrated strategy was established and validated to screen α-glucosidase inhibitors by ultra-high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). UHPLC was used to separate the components in Coptis chinensis Franch. (Huanglian in Chinese) extract, which was identified by UHPLC-Q-TOF-MS to acquire structural information and collected by the fraction collector. Finally, the collected fractions were tested for inhibitory activity of α-glucosidase. The results showed that Huanglian extract had the α-glucosidase inhibitory activity with the IC50 value at 3.528mg mL(-1), which could be used for the treatment of diabetes. Alkaloids were the main components that had inhibitory activity of α-glucosidase in Huanglian extract, while the inhibitory activity of phenolic acids against α-glucosidase was relatively weaker. Coptisine, epiberberine, jatrorrhizin and berberine were screened and identified as α-glucosidase inhibitors from Huanglian extract in vitro. Compared with conventional methods, the integrated UHPLC/Q-TOF-MS-FC method could quantitatively analyze α-glucosidase inhibitory activity of individual constituent and provide the total α-glucosidase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying active ingredients from Traditional Chinese medicines.
authors.affiliation: Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Ai-Hua
authors.initials: AH
authors.lastname: Ge
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Bai
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Li
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Jiao
authors.initials: J
authors.lastname: Liu
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Jun
authors.initials: J
authors.lastname: He
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Er-Wei
authors.initials: EW
authors.lastname: Liu
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhang
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
authors.forename: Bo-Li
authors.initials: BL
authors.lastname: Zhang
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China. Electronic address: gaoxiumei@tjutcm.edu.cn.
authors.forename: Xiu-Mei
authors.initials: XM
authors.lastname: Gao
authors.affiliation: Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China. Electronic address: tcmcyx@126.com.
authors.forename: Yan-Xu
authors.initials: YX
authors.lastname: Chang
mesh_terms: D005591:Chemical Fractionation / Q000379:methods*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D039323:Coptis / Q000737:chemistry*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005240:Feasibility Studies; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D057166:High-Throughput Screening Assays / Q000379:methods*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*
chemical_list: D004365:Drugs, Chinese Herbal; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D010936:Plant Extracts
keywords: Alkaloids; Coptis chinensis Franch. (Huanglian); Diabetes; Phenolic acids; UHPLC/Q-TOF-MS-FC; α-Glucosidase inhibitors