Cafestol, a Bioactive Substance in Coffee, Stimulates Insulin Secretion and Increases Glucose Uptake in Muscle Cells: Studies in Vitro

Abstract

Diet and exercise intervention can delay or prevent development of type-2-diabetes (T2D), and high habitual coffee consumption is associated with reduced risk of developing T2D. This study aimed to test whether selected bioactive substances in coffee acutely and/or chronically increase insulin secretion from β-cells and improve insulin sensitivity in skeletal muscle cells. Insulin secretion from INS-1E rat insulinoma cells was measured after acute (1-h) and long-term (72-h) incubation with bioactive substances from coffee. Additionally, we measured uptake of radioactive glucose in human skeletal muscle cells (SkMC) after incubation with cafestol. Cafestol at 10(-8) and 10(-6) M acutely increased insulin secretion by 12% (p < 0.05) and 16% (p < 0.001), respectively. Long-term exposure to 10(-10) and 10(-8) M cafestol increased insulin secretion by 34% (p < 0.001) and 68% (p < 0.001), respectively. Caffeic acid also increased insulin secretion acutely and chronically. Chlorogenic acid, trigonelline, oxokahweol, and secoisolariciresinol did not significantly alter insulin secretion acutely. Glucose uptake in SkMC was significantly enhanced by 8% (p < 0.001) in the presence of 10(-8) M cafestol. This newly demonstrated dual action of cafestol suggests that cafestol may contribute to the preventive effects on T2D in coffee drinkers and be of therapeutic interest.

Coffee, type 2 diabetes and pancreatic islet function – A mini-review

“…The beneficial, but moderate effect of caffeic acid on acute insulin secretion reported by (Mellbye et al, 2015) was consistent with the findings of Bhattachaya et al 2014, who also showed that chronic exposure to the phenolic acid further enhanced the secretory response from INS1E beta cells. This effect was maintained following chronic treatment with high glucose concentrations, suggesting a protective effect of the compound on beta cell survival when exposed to stressful conditions typical of type 2 diabetes.…”

“…More significant changes regarding glucose uptake were observed in a liver cell line (Huang, Shen, & Wu, 2009). In addition Mellbye et al reported of clear beneficial effects on glucose uptake in a muscle cells by another coffee component, cafestol (Mellbye, Jeppesen, Hermansen, & Gregersen, 2015).…”

“…In contrast, there are a limited number of studies directly investigating the role of noncaffeine coffee derivatives with regard to insulin secretion. Mellbye et al (Mellbye et al, 2015) performed an in vitro study with the rat insulinoma beta cell line INS1E, where they investigated acute insulin release in response to selected compounds representative of the main components in coffee, that is, cafestol, caffeic acid, chlorogenic acid, trigonelline, secoisolariciresinol and oxokahweol. Only cafestol and caffeic acid modestly, but significantly, stimulated glucose-induced insulin release and also improved release following prolonged exposure to the two coffee components at metabolically relevant concentrations (10 -10 -10 -8 mol/l).…”

Association between the Prevalence of Metabolic Syndrome and the Level of Coffee Consumption among Korean Women

“…Not only does cafestol stimulate the secretion of insulin, but it also improves insulin sensitivity, increasing the uptake of glucose in muscle cells. [33]…”

Chemical and Biological Aspects of Extracts from Medicinal Plants with Antidiabetic Effects

“…Cafestol, stevioside, and isosteviol are diterpenes that increase insulin sensitivity and secretion by modifying the expression of genes and transcriptional factors of insulin regulation, and increasing glucose uptake [75][76][77].…”