Abstract

Antrodia cinnamomea (AC), an edible Taiwanese mushroom, has been recognized as a valuable natural resource with vast biological and medicinal benefits. Recently, the hypoglycemic and anti-diabetic effects of AC were mentioned in several studies. However, no studies have investigated α-glucosidase inhibitors from AC fruiting bodies (ACFB) as they relate to type 2 diabetes (T2D) treatment. The purpose of this study was to gain evidence of potent α-glucosidase inhibitory effects, as well as isolate, identify and characterize the active compounds of ACFB. The MeOH extract of ACFB demonstrated potent α-glucosidase inhibitory activity, and possessed high pH stability (pH 2–11) and thermostable properties at 40–50 °C. Further purification led to the isolation of eight constituents from ACFB, identified as: 25S-antcin K (1), 25R-antcin K (2), dehydrosulphurenic acid (3), 25S-antcin I (4), 25S-antcin B (5), 25R-antcin B (6), dehydroeburicoic acid (7) and eburicoic acid (8). Notably, the ACFB extract and its identified compounds, except 1, 4, and 6 demonstrated a greater effect (EC50 = 0.025–0.21 mg/mL) than acarbose (EC50 = 0.278 mg/mL). As such, these active compounds were determined to be new potent mushroom α-glucosidase inhibitors. These active compounds were also identified on the HPLC fingerprints of ACFB.

Highlights

  • The incidence of diabetes mellitus (DM), a chronic metabolic disorder, has been dramatically increasing and reducing people’s quality of life worldwide [1]

  • The results of this study contributed to the catalogue of novel biological activities of Antrodia cinnamomea (AC), as well as its constituents

  • AC fruiting bodies (ACFB) were extracted by methanol and used for bioassay

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Summary

Introduction

The incidence of diabetes mellitus (DM), a chronic metabolic disorder, has been dramatically increasing and reducing people’s quality of life worldwide [1]. People with DM are at high risk for many other complications, including kidney failure, depression, cardiovascular disease, frailty, cognitive decline or premature death [2]. The number of diabetics was reported to be 382 million. 90% of cases in 2013 were type 2 diabetes (T2D), and the number of total DM cases is estimated to increase to 592 million by 2035 [3]. Molecules 2018, 23, 2864 the use of α-glucosidase inhibitors (aGIs) [4]. Several commercial aGIs, such as acarbose, voglibose and miglitol, are available some side effects have been reported, including diarrhea, flatulence and abdominal discomfort [5]. The search for safe and natural sources of active aGIs, along with their isolation and identification, is a high priority

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