Abstract

Pancreatic lipase, a key enzyme for lipid absorption, is one of the most important targets for the treatment of obesity, while natural compounds have recently attracted much interest as potential inhibitors of this enzyme. Here, in an attempt to find new effective agents, the methanolic extract from Moricandia arvensis (L.) DC. and its sub-extracts were investigated for their potential inhibitory activity. The ability to inhibit pancreatic lipase was verified through the in vitro evaluation of the prevention of p-nitrophenyl caprylate hydrolysis. The antioxidant activity was also verified by means of DPPH and β-carotene bleaching tests. Compositional profiling revealed that flavonoid glycosides were the main specialized metabolites present in the methanolic extract from the aerial parts of the plant with kaempferol and quercetin representing the two O-glycosylated aglycones. Kaempferol-3-O-β-(2″-O-glucosyl)-rutinoside and kaempferol-3-O-a-arabinosyl-7-O-rhamnoside were the most abundant flavonols. The crude methanolic extract and the dichloromethane and ethyl acetate sub-extracts showed a strong lipase inhibitory activity, with IC50 values of 2.06 ± 0.02, 1.52 ± 0.02 and 1.31 ± 0.02 mg/mL, respectively. The best capacity to scavenge DPPH radical was detected for the ethyl acetate sub-extract (IC50 = 171.9 ± 1.0 µg/mL), which was also effective in protecting linoleic acid from peroxidation (IC50 = 35.69 ± 2.30 µg/mL). Obtained results support the hypothesis that M. arvensis can be a source of bioactive phytochemicals for the pharmacological inhibition of dietary lipids absorption.

Highlights

  • The World Health Organization (WHO) defines the overweight and obesity as abnormal or excessive fat accumulation states representing a health risk

  • Aims of the present study were to characterize for the first time the phytochemical composition of the methanolic extractives of M. arvensis aerial parts collected wild in Calabria region, Italy, and determine for the first time their effect on lipid absorption trough inhibition of pancreatic lipase and antioxidant activity

  • Apolar constituents present in the n-Hex and DCM sub-extracts were identified by means of gas chromatography–mass spectrometry (GC–MS) analyses (Table 1)

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Summary

Introduction

The World Health Organization (WHO) defines the overweight and obesity as abnormal or excessive fat accumulation states representing a health risk. Orlistat is a clinically available anti-obesity drug that acts as inhibitor of gastric and pancreatic lipase and has been shown to block the absorption of dietary fats of about 30% at the therapeutic oral dosage of 120 mg per three times a day The use of this drug is being gradually decreased due to its side effects such as insomnia, constipation, vomiting, emesis, headache, and stomachache [1,2]. Aims of the present study were to characterize for the first time the phytochemical composition of the methanolic extractives of M. arvensis aerial parts collected wild in Calabria region, Italy, and determine for the first time their effect on lipid absorption trough inhibition of pancreatic lipase and antioxidant activity

Phytochemical Profile
Antioxidant Activity
Pancreatic Lipase Inhibition
Discussion
Collection of Plant Material and Preparation of the Extracts
GC–MS Analysis
Glucosinolates Extraction and Desulfation
Chemical Analysis and Quantitation of Glucosinolates
HPLC of Phenolics
HPLC-HRMS Analyses of Phenolics
4.11. In Vitro Pancreatic Lipase Assay
4.12. Statistical Analysis
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