Screening of Anti-Lipase Components of Artemisia argyi Leaves Based on Spectrum-Effect Relationships and HPLC-MS/MS

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.

Caffeic Acid, an Allelochemical in Artemisia argyi, Inhibits Weed Growth via Suppression of Mitogen-Activated Protein Kinase Signaling Pathway and the Biosynthesis of Gibberellin and Phytoalexin

“…Interestingly, their allelopathic effects on weeds seemed to be identical to their content, exhibiting the following order: CA>4−CQA>5−CQA>3-CQA ( Figure 3 ). Notably, 5-CQA, 3-CQA, and 4-CQA are all condensed by CA and quinic acid at different binding sites and produced by plants through the shikimic acid pathway during aerobic respiration ( Chang et al, 2021 ). The differences in biological activity of these isomeric compounds could be caused by the presence of different binding sites.…”

A Review on Rhubarb-Derived Substances as Modulators of Cardiovascular Risk Factors—A Special Emphasis on Anti-Obesity Action

“…For that reason, the search for new and more effective inhibitors (including natural compounds) of this hydrolytic enzyme has gained increasing attention [ 63 ]. Moreover, numerous reports demonstrated the ability of phytochemicals belonging to various classes to inhibit PL activity [ 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 ]. Most of the examined plant-derived substances were weaker inhibitors of the pancreatic lipase than the reference drug, but some of them, i.e., ferulic acid and kaempferol-3- O -rutinoside, displayed comparable PL-inhibitory efficiency.…”

Rapid Screening of Lipase Inhibitors from Ophiopogonis Radix Using High-Performance Thin Layer Chromatography by Two Step Gradient Elution Combined with Bioautographic Method

“…Several techniques have been described for the screening of lipase inhibitors, such as fluorescence assay [13], liquid chromatography-mass spectrometry [14], capillary electrophoresis [15], and lipase immobilization [16]. However, they may suffer from falsepositive results, expensive instruments and/or sophisticated procedures.…”