META060 protects against diet-induced obesity and insulin resistance in a high-fat–diet fed mouse

“…Extracts of the hops plant ( Humulus lupulus L. ) used as flavoring agents in beer production have been shown to reduce weight and improve glucose homeostasis in rodents [1] , [2] , [3] , [4] , [5] , [6] , [7] , [8] and humans [1] , [9] , [10] . Thus, it is of considerable interest to identify the molecular mechanisms that mediate the benefits of bioactive ingredients of hops in metabolic disease.…”

Section: Introductionmentioning

confidence: 99%

“…Interestingly, this study also included a small double-blind, placebo-controlled trial in people with diabetes that showed that treatment for 8 weeks with isohumulones significantly reduced blood glucose and hemoglobin A1c levels. Subsequent studies [2] , [3] , [4] , [5] , [8] have reported positive effects of isohumulones in reducing weight gain and fat mass, improving glucose homeostasis and insulin sensitivity, decreasing liver lipid accumulation, and reducing plasma triglycerides in multiple rodent models (e.g., DIO, KK- A y , db/db mice, Wistar rats). Notably, a larger clinical trial in Japanese subjects with prediabetes showed that 12-week treatment with isohumulones significantly reduced body weight, body mass index, fat mass, fasting blood glucose, and hemoglobin A1c levels [9] .…”

Section: Introductionmentioning

confidence: 99%

Intestinal bitter taste receptor activation alters hormone secretion and imparts metabolic benefits

Kok

Galmozzi

Littlejohn

et al. 2018

Molecular Metabolism

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ObjectivesExtracts of the hops plant have been shown to reduce weight and insulin resistance in rodents and humans, but elucidation of the mechanisms responsible for these benefits has been hindered by the use of heterogeneous hops-derived mixtures. Because hop extracts are used as flavoring agents for their bitter properties, we hypothesized that bitter taste receptors (Tas2rs) could be mediating their beneficial effects in metabolic disease. Studies have shown that exposure of cultured enteroendocrine cells to bitter tastants can stimulate release of hormones, including glucagon-like peptide 1 (GLP-1). These findings have led to the suggestion that activation of Tas2rs may be of benefit in diabetes, but this tenet has not been tested. Here, we have assessed the ability of a pure derivative of a hops isohumulone with anti-diabetic properties, KDT501, to signal through Tas2rs. We have further used this compound as a tool to systematically assess the impact of bitter taste receptor activation in obesity-diabetes.MethodsKDT501 was tested in a panel of bitter taste receptor signaling assays. Diet-induced obese mice (DIO) were dosed orally with KDT501 and acute effects on glucose homeostasis determined. A wide range of metabolic parameters were evaluated in DIO mice chronically treated with KDT501 to establish the full impact of activating gut bitter taste signaling.ResultsWe show that KDT501 signals through Tas2r108, one of 35 mouse Tas2rs. In DIO mice, acute treatment stimulated GLP-1 secretion and enhanced glucose tolerance. Chronic treatment caused weight and fat mass loss, increased energy expenditure, enhanced glucose tolerance and insulin sensitivity, normalized plasma lipids, and induced broad suppression of inflammatory markers. Chronic KDT501 treatment altered enteroendocrine hormone levels and bile acid homeostasis and stimulated sustained GLP-1 release. Combined treatment with a dipeptidyl peptidase IV inhibitor amplified the incretin-based benefits of this pure isohumulone.ConclusionsActivation of Tas2r108 in the gut results in a remodeling of enteroendocrine hormone release and bile acid metabolism that ameliorates multiple features of metabolic syndrome. Targeting extraoral bitter taste receptors may be useful in metabolic disease.

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“…Studies in animal models of type 2 diabetes show that rosiglitazone improves glycaemic control by enhancing insulin‐stimulated whole‐body glucose uptake (Zheng, Shao, Wu, Shen, & Lin, ). It has been reported that rosiglitazone has an ability of enhancing metabolic flexibility of various tissues, including muscle, liver, adipose and bone tissue (Stage et al, ; Vroegrijk et al, ). Much evidence exists to suggest that rosiglitazone could influence male germinal cells (Rabbani, Devi, & Khanam, ).…”

Section: Introductionmentioning

confidence: 99%

Protective influence of rosiglitazone against time‐dependent deterioration of boar spermatozoa preserved at 17°C

Wang

Yang

Guo

et al. 2019

Reprod Domestic Animals

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Spermatozoa are highly specialized cells, and energy metabolism plays an important role in modulating sperm viability and function. Rosiglitazone is an antidiabetic drug in the thiazolidinedione class that regulates metabolic flexibility and glucose uptake in various cell types, but its effects on boar sperm metabolism are unknown. In this study, we investigated the potential effect of rosiglitazone against time‐dependent deterioration of boar spermatozoa during liquid preservation at 17°C. Freshly ejaculated semen was diluted with Beltsville Thawing Solution (BTS) containing different concentrations of rosiglitazone, and the motility, membrane and acrosome integrity of sperm were detected. Besides, we measured glucose uptake capacity, l‐lactate production level, mitochondrial membrane potential, adenosine triphosphate (ATP) content and mitochondrial reactive oxygen species (mROS) production of sperm after boar semen had been incubated with or without rosiglitazone, iodoacetate (glycolysis inhibitor) and rotenone (electron transport chain inhibitor) for 5 days. The addition of rosiglitazone significantly enhanced sperm quality and had a strong protective effect on the sperm membrane and acrosome integrity during storage. BTS containing 50 μM rosiglitazone maintained the total motility of liquid‐preserved sperm above 60% for 7 days. Rosiglitazone improved sperm quality by regulating energy metabolism manner of preserved sperm, protected the sperm mitochondrial membrane potential, enhanced sperm ATP production and in the meanwhile reduced mROS through enhancing glycolysis but not oxidative phosphorylation. The data suggested the practical feasibility of using rosiglitazone for improving boar spermatozoa quality during semen preservation.

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META060 protects against diet-induced obesity and insulin resistance in a high-fat–diet fed mouse

Abstract: META060 has potential therapeutic value for managing obesity and insulin resistance, and further research into the mechanism of action is warranted.

Cited by 18 publications

References 18 publications

Isohumulones from hops (Humulus lupulus) and their potential role in medical nutrition therapy

Isohumulones from hops (Humulus lupulus) and their potential role in medical nutrition therapy

Intestinal bitter taste receptor activation alters hormone secretion and imparts metabolic benefits

Protective influence of rosiglitazone against time‐dependent deterioration of boar spermatozoa preserved at 17°C

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