Determination of α-glucosidase inhibitors from Scutellaria baicalensis using liquid chromatography with quadrupole time of flight tandem mass spectrometry coupled with centrifugal ultrafiltration / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 208-214, 2015.
Article
在 En
| WPRIM
| ID: wpr-812155
Responsible library:
WPRO
ABSTRACT
The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with quadrupole time of flight tandem mass spectrometry (LC-Q/TOF-MS/MS) determination to screen α-glucosidase inhibitors in complex Scutellaria baicalensis Georgi (SBG) extract. By adding a second filter to the screening process, the level of non-specific binding of Compounds 1, 3, 10 and 11 was significantly decreased, and the level of non-specific binding of Compounds 5 and 15 also was reduced. As a result, five flavonoids identified as baicalein, baicalein, wogonin, chrysin, and oroxylin A, were rapidly found to interact with α-glucosidase and possess potent anti-α-glucosidase activity in vitro. Specific binding of ligands to α-glucosidase was demonstrated though the proposed method and the ligands could be ranked in order of affinity for α-glucosidase, which were corresponded to the order of inhibitory activity in vitro. In conclusion, our results indicated that the developed method is a rapid and effective screening method for rat intestinal α-glucosidase inhibitors from complex herbal medicines such as SBG.
Key words
全文:
1
索引:
WPRIM
主要主题:
Flavonoids
/
Plant Extracts
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Ultrafiltration
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Chemistry
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Chromatography, Liquid
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Allergy and Immunology
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Tandem Mass Spectrometry
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Glycoside Hydrolase Inhibitors
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Hypoglycemic Agents
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Methods
限制:
Animals
语言:
En
期刊:
Chinese Journal of Natural Medicines (English Ed.)
年:
2015
类型:
Article