Abstract

This study aims to evaluate the bioactive components, in vitro bioactivities, and in vivo hypoglycemic effect of P. frutescens leaf, which is a traditional medicine-food homology plant. P. frutescens methanol crude extract and its fractions (petroleum ether, chloroform, ethyl acetate, n-butanol fractions, and aqueous phase residue) were prepared by ultrasound-enzyme assisted extraction and liquid–liquid extraction. Among the samples, the ethyl acetate fraction possessed the high total phenolic (440.48 μg GAE/mg DE) and flavonoid content (455.22 μg RE/mg DE), the best antioxidant activity (the DPPH radical, ABTS radical, and superoxide anion scavenging activity, and ferric reducing antioxidant power were 1.71, 1.14, 2.40, 1.29, and 2.4 times higher than that of control Vc, respectively), the most powerful α-glucosidase inhibitory ability with the IC50 value of 190.03 μg/mL which was 2.2-folds higher than control acarbose, the strongest proliferative inhibitory ability against MCF-7 and HepG2 cell with the IC50 values of 37.92 and 13.43 μg/mL, which were considerable with control cisplatin, as well as certain inhibition abilities on acetylcholinesterase and tyrosinase. HPLC analysis showed that the luteolin, rosmarinic acid, rutin, and catechin were the dominant components of the ethyl acetate fraction. Animal experiments further demonstrated that the ethyl acetate fraction could significantly decrease the serum glucose level, food, and water intake of streptozotocin-induced diabetic SD rats, increase the body weight, modulate their serum levels of TC, TG, HDL-C, and LDL-C, improve the histopathology and glycogen accumulation in liver and intestinal tissue. Taken together, P. frutescens leaf exhibits excellent hypoglycemic activity in vitro and in vivo, and could be exploited as a source of natural antidiabetic agent.

Highlights

  • Type 2 diabetes mellitus (T2DM), which is characterized by postprandial hyperglycemia and chronic hyperglycemia, is one of the most serious metabolic diseases worldwide and its pathogenesis is associated with oxidative stress [1]

  • Oxidative stress is an imbalance between reactive oxygen species (ROS) and cellular antioxidative systems; excessive ROS accumulation induces oxidative stress, leading to cell damage, which in turn is involved in diabetes and various complications [2]

  • The results showed that total phenolic content (TPC) was highest in the crude extract (CE), followed by the ethyl acetate fraction (EtOAc), n-butanol fraction (n-BuOH), chloroform fraction (CF), petroleum ether fraction (PE), and the aqueous phase residue (AQ)

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Summary

Introduction

Oxidative stress is an imbalance between reactive oxygen species (ROS) and cellular antioxidative systems; excessive ROS accumulation induces oxidative stress, leading to cell damage, which in turn is involved in diabetes and various complications [2]. Many other metabolic diseases are associated with oxidative stress, including obesity, cancer, neurodegenerative disorders, and cardiovascular complications [3]. These diseases influence each other through the metabolic abnormalities associated with oxidative stress, for example, there is a close and direct link between diabetes and Alzheimer’s disease (AD) [4]. Consumption of antioxidant-rich foods has been considered to have the ability to potentially modulate oxidative stress, which in turn, has beneficial impacts on oxidative stress-related diseases [6]. Ever-growing consumer demand for healthy, combined with a preference for natural ingredients, has led to very big growth in plant-based extracts functional foods and dietary supplements markets in recent years, especially during coronavirus disease 2019

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