School of Pharmacy, Sungkyunkwan University, Suwon 16419, Korea.
College of Korean Medicine, Gachon University, Seongnam 13120, Korea.
Biomolecules. 2019 Aug 2;9(8):335. doi: 10.3390/biom9080335.
Insulin plays a key role in glucose homeostasis and is hence used to treat hyperglycemia, the main characteristic of diabetes mellitus. is an inedible ball-shaped wood-rotting fungus, and hypoxylon F is one of the major compounds of . The aim of this study is to evaluate the effects of hypoxylonol F isolated from on insulin secretion in INS-1 pancreatic β-cells and demonstrate the molecular mechanisms involved. Glucose-stimulated insulin secretion (GSIS) values were evaluated using a rat insulin ELISA kit. Moreover, the expression of proteins related to pancreatic β-cell metabolism and insulin secretion was evaluated using Western blotting. Hypoxylonol F isolated from was found to significantly enhance glucose-stimulated insulin secretion without inducing cytotoxicity. Additionally, hypoxylonol F enhanced insulin receptor substrate-2 (IRS-2) levels and activated the phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) pathway. Interestingly, it also modulated the expression of peroxisome proliferator-activated receptor γ (PPARγ) and pancreatic and duodenal homeobox 1 (PDX-1). Our findings showed that and its bioactive compounds are capable of improving insulin secretion by pancreatic β-cells. This suggests that can be used as a therapeutic agent to treat diabetes.
胰岛素在葡萄糖稳态中发挥着关键作用，因此被用于治疗高血糖，这是糖尿病的主要特征。 是一种不可食用的球状木质腐朽真菌，而 Hypoxylon F 是 的主要化合物之一。本研究旨在评估从 中分离出的 Hypoxylonol F 对 INS-1 胰腺 β 细胞胰岛素分泌的影响，并阐明其涉及的分子机制。使用大鼠胰岛素 ELISA 试剂盒评估葡萄糖刺激的胰岛素分泌 (GSIS) 值。此外，还使用 Western blot 评估与胰腺 β 细胞代谢和胰岛素分泌相关的蛋白质表达。从 中分离出的 Hypoxylonol F 被发现可显著增强葡萄糖刺激的胰岛素分泌，而不会诱导细胞毒性。此外，Hypoxylonol F 还可增强胰岛素受体底物-2 (IRS-2) 水平并激活磷脂酰肌醇 3-激酶/蛋白激酶 B (PI3K/Akt) 途径。有趣的是，它还调节过氧化物酶体增殖物激活受体 γ (PPARγ) 和胰腺十二指肠同源盒 1 (PDX-1) 的表达。我们的研究结果表明， 和其生物活性化合物能够改善胰腺 β 细胞的胰岛素分泌。这表明 可以用作治疗糖尿病的药物。
