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)

• Published in: Journal of pharmaceutical and biomedical analysis 2014-11, Vol.100, p.79-87
• Main Authors: Ge, Ai-hua, Bai, Yang, Li, Jin, Liu, Jiao, He, Jun, Liu, Er-wei, Zhang, Peng, Zhang, Bo-li, Gao, Xiu-mei, Chang, Yan-xu
• Format: Article
• Language: English
• Subjects: Alkaloids; Chemical Fractionation - methods; Chromatography, High Pressure Liquid - methods; Coptis - chemistry; Coptis chinensis Franch. (Huanglian); Diabetes; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - isolation & purification; Drugs, Chinese Herbal - pharmacology; Feasibility Studies; Glycoside Hydrolase Inhibitors - chemistry; Glycoside Hydrolase Inhibitors - isolation & purification; Glycoside Hydrolase Inhibitors - pharmacology; High-Throughput Screening Assays - methods; Hypoglycemic Agents - chemistry; Hypoglycemic Agents - isolation & purification; Hypoglycemic Agents - pharmacology; Molecular Structure; Phenolic acids; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization - methods; UHPLC/Q-TOF-MS-FC; α-Glucosidase inhibitors
• ISSN: 0731-7085; 1873-264X
• DOI: 10.1016/j.jpba.2014.07.025

•An activity integrated strategy was developed to screen inhibitors of α-glucosidase.•Alkaloids were the main inhibitors of α-glucosidase in huanglian extract.•Coptisine, epiberberine, jatrorrhizin and berberine were α-glucosidase inhibitors.•A powerful tool for screening and identifying active ingredients from TCMs. 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 3.528mgmL−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.