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• W2903422290 endingPage "3198" @default.
• W2903422290 startingPage "3198" @default.
• W2903422290 abstract "(1) Background: Capsaicin, a chief ingredient of natural chili peppers, enhances metabolism and energy expenditure and stimulates the browning of white adipose tissue (WAT) and brown fat activation to counter diet-induced obesity. Although capsaicin and its nonpungent analogs are shown to enhance energy expenditure, their efficiency to bind to and activate their receptor—transient receptor potential vanilloid subfamily 1 (TRPV1)—to mediate thermogenic effects remains unclear. (2) Methods: We analyzed the binding efficiency of capsaicin analogs by molecular docking. We fed wild type mice a normal chow or high fat diet (± 0.01% pungent or nonpungent capsaicin analog) and isolated inguinal WAT to analyze the expression of thermogenic genes and proteins. (3) Results: Capsaicin, but not its nonpungent analogs, efficiently binds to TRPV1, prevents high fat diet-induced weight gain, and upregulates thermogenic protein expression in WAT. Molecular docking studies indicate that capsaicin exhibits the highest binding efficacy to TRPV1 because it has a hydrogen bond that anchors it to TRPV1. Capsiate, which lacks the hydrogen bond, and therefore, does not anchor to TRPV1. (4) Conclusions: Long-term activation of TRPV1 is imminent for the anti-obesity effect of capsaicin. Efforts to decrease the pungency of capsaicin will help in advancing it to mitigate obesity and metabolic dysfunction in humans." @default.
• W2903422290 created "2018-12-11" @default.
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• W2903422290 date "2018-12-04" @default.
• W2903422290 modified "2023-10-03" @default.
• W2903422290 title "Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin" @default.
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• W2903422290 doi "https://doi.org/10.3390/molecules23123198" @default.
• W2903422290 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6321193" @default.
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