AUTHOR=Chang Yaqing , Zhang Dan , Yang Guiya , Zheng Yuguang , Guo Long TITLE=Screening of Anti-Lipase Components of Artemisia argyi Leaves Based on Spectrum-Effect Relationships and HPLC-MS/MS JOURNAL=Frontiers in Pharmacology VOLUME=12 YEAR=2021 URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.675396 DOI=10.3389/fphar.2021.675396 ISSN=1663-9812 ABSTRACT=

Pancreatic lipase is a key lipase for triacylglyceride digestion and absorption, which is recognized as a promising target for treatment of metabolic disorders. Natural phytochemicals are hopeful sources for pancreatic lipase inhibitors. The leaves of Artemisia argyi H.Lév. and Vaniot (AL) is commonly used as herbal medicine or food supplement in China and other Asian countries for hundreds of years. AL mainly contains essential oils, phenolic acids, flavonoids and terpenoids, which exhibit many pharmacological activities such as antioxidant, anti-inflammatory, antimicrobial, analgetic, anti-cancer, anti-diabetes and immunomodulatory effects. However, the anti-lipase activity of AL was lack of study and the investigation of anti-lipase ingredients from AL was also insufficient. In the present study, the anti-lipase activity of AL was evaluated in vitro and the potentially pancreatic lipase inhibitors of AL were investigated. High performance liquid chromatography was used to establish fingerprints of AL samples, and fifteen peaks were selected. The anti-lipase activities of AL samples were evaluated by a pancreatic lipase inhibition assay. Then, the spectrum-effect relationships between fingerprints and pancreatic lipase inhibitory activities were investigated to identify the anti-lipase constitutes in AL. As the results, four caffeoylquinic acids, which were identified as neochlorogenic acid, chlorogenic acid, isochlorogenic acid B, and isochlorogenic acid A by high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry, were selected as potential pancreatic lipase inhibitors in AL. Moreover, anti-lipase activity assessment and molecular docking study of the four compounds were performed to validate the potential lipase inhibitors in AL. The results revealed that the four caffeoylquinic acids in AL as bioactive compounds displayed with anti-lipase activity. The present research provided evidences for the anti-lipase activity of AL, and suggested that some bioactive compounds in AL could be used as lead compounds for discovering of new pancreatic lipase inhibitors.