Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin
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. View Full-Text
- Supplementary File 1:
ZIP-Document (ZIP, 4294 KB)
Share & Cite This Article
Baskaran, P.; Covington, K.; Bennis, J.; Mohandass, A.; Lehmann, T.; Thyagarajan, B. Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin. Molecules 2018, 23, 3198.
Baskaran P, Covington K, Bennis J, Mohandass A, Lehmann T, Thyagarajan B. Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin. Molecules. 2018; 23(12):3198.Chicago/Turabian Style
Baskaran, Padmamalini; Covington, Kyle; Bennis, Jane; Mohandass, Adithya; Lehmann, Teresa; Thyagarajan, Baskaran. 2018. "Binding Efficacy and Thermogenic Efficiency of Pungent and Nonpungent Analogs of Capsaicin." Molecules 23, no. 12: 3198.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.