Abstract

Gaultheria pumila (Ericaceae) (known as Chaura or Mutilla) is a Chilean native small shrub that produces berry fruits consumed by local Mapuche people. In this study, the chemical fingerprinting and antioxidant, enzyme inhibition, and antiproliferative activities of the berries were investigated for the first time. Thirty-six metabolites were identified in the fruits by ultra-high performance liquid chromatography-photodiode array detection, hyphenated with Orbitrap mass spectrometry analysis (UHPLC-DAD-Orbitrap-MS). Metabolites, included anthocyanins, phenolic acids, flavonoids, iridoids, diterpenes, and fatty acids. Moderate inhibitory activities against acetylcholinesterase (7.7 ± 0.3 µg/mL), butyrylcholinesterase (34.5 ± 0.5 µg/mL), and tyrosinase (3.3 ± 0.2 µg/mL) enzymes were found. Moreover, selected major compounds were subjected to docking assays in light of their experimental inhibition. Results indicated that hydrogen bonding, π–π interaction, and a salt bridge interaction contributed significantly. Gaultheria pumila berries showed a total phenolic content of 189.2 ± 0.2 mg of gallic acid equivalents/g, total flavonoid content of 51.8 ± 0.1 mg quercetin equivalents/g, and total anthocyanin content of 47.3 ± 0.2 mg of cianydin-3-glucoside equivalents/g. Antioxidant activity was assessed using DPPH (92.8 ± 0.1 µg/mL), FRAP (134.1 ± 0.1 μmol Trolox equivalents/g), and ORAC (4251.6 ± 16.9 μmol Trolox equivalents/g) assays. Conversely, Gaultheria pumila showed a scarce antiproliferative potential against several solid human cancer cells. Our findings suggest that Gaultheria pumila berries have several bioactive metabolites with inhibitory effects against acetylcholinesterase, butyrylcholinesterase, and tyrosinase, and have the potential for use in food supplements.

Highlights

  • This article is an open access articleThe human consumption of native berries has been increasing worldwide in part due to their potential impact on health promotion and disease prevention

  • The negative mode was used for the identification of phenolic compounds, while the positive mode was used for anthocyanins

  • Inhibition assays of Gaultheria pumila berries extract over tyrosinase turned out to be more potent than the known inhibitor kojic acid by three-folds

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Summary

Introduction

This article is an open access article. The human consumption of native berries has been increasing worldwide in part due to their potential impact on health promotion and disease prevention. Fruit berries from a variety of species have been associated with a reduction in the risk of cardiovascular, neurodegenerative, and inflammatory diseases, as well as potential benefits against some forms of cancer [1]. The effects against reactive oxygen species (ROS) have been described distributed under the terms and conditions of the Creative Commons. Metabolites 2021, 11, 523 forms of cancer [1]. The effects against reactive oxygen species (ROS) have been described as asthe themain mainantioxidant antioxidantprotective protectivemechanism mechanism[2].

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