Abstract
Pancreatic lipase (PL) is an enzyme that plays an essential role in the digestion of dietary lipids and is a suitable target for an anti-obesity dietary supplement. The objective of this study was to find a novel source of PL inhibitors from Korean medicinal plants and investigate the PL-inhibitory properties of the active constituents. From among 34 kinds of methanolic crude extracts, Polygonum aviculare L. showed the highest PL-inhibitory activity (63.97 ± 0.05% of inhibition). Solvent fractionation and liquid chromatography/mass spectrometry (LC/MS) analysis identified flavonol-3-O-glycosides, flavonol-3-O-(2″-galloyl)-glycosides, and flavonol aglycones as active constituents. Furthermore, the inhibitory characteristics of the major compounds were investigated in terms of enzyme kinetics and fluorescence quenching. The results suggested that the inhibitory activity of the major compounds is closely related to the tertiary structural change in PL, and that differences in inhibitory activity occurred due to slight discrepancies in their chemical structure.
Highlights
Obesity, considered an ongoing public health issue in the 21st century, is defined as excessive fat accumulation and superfluous body weight for height[1]
Pancreatic lipase (PL; EC 3.1.1.3), which plays an essential role in the digestion of dietary lipids[9], is a primary modulator of lipid metabolism and can be the most suitable target for the anti-obesity agent
We successfully identified the pancreatic lipase (PL)-inhibitory constituents in the solvent fractions of P. aviculare by liquid chromatography/mass spectrometry (LC/MS) analysis and evaluated the inhibitory characteristics of its major compounds by enzyme kinetics and fluorescence analysis
Summary
Obesity, considered an ongoing public health issue in the 21st century, is defined as excessive fat accumulation and superfluous body weight for height[1]. Excessive intake of lipids and carbohydrates beyond the energy needs of the individual can disrupt lipid metabolism and homeostasis, leading to increased fat deposition and blood lipid concentrations (e.g., triglyceride and low-density lipoprotein)[1,7,8]. In this context, the development of strategies to control lipid intake has been a major target in medical and dietary supplement research. We hypothesized that Korean medicinal plants could serve as novel sources of PL inhibitors for use in anti-obesity agents. We successfully identified the PL-inhibitory constituents in the solvent fractions of P. aviculare by liquid chromatography/mass spectrometry (LC/MS) analysis and evaluated the inhibitory characteristics of its major compounds by enzyme kinetics and fluorescence analysis
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