Non-pungent capsaicin analogs (capsinoids) increase metabolic rate and enhance thermogenesis via gastrointestinal TRPV1 in mice

Biosci Biotechnol Biochem. 2009 Dec;73(12):2690-7. doi: 10.1271/bbb.90555. Epub 2009 Dec 7.


Capsinoids are non-pungent capsaicin analogs which increase energy expenditure like capsaicin. However, the mechanisms underlying the enhancement of their energy expenditure despite their non-pungency are poorly understood. We suggest here that capsinoids increase energy expenditure in wild-type mice, but not in transient receptor potential vanilloid 1 (TRPV1) knockout mice, implying that capsinoids increase energy expenditure via TRPV1. The jejunal administration of capsinoids to anesthetized mice raised the temperature of the colon and intrascapular brown adipose tissue. Denervation of the extrinsic nerves connected to the jejunum inhibited this temperature elevation. These findings suggest that capsinoids increase energy expenditure by activating the intestinal extrinsic nerves. Although the jejunal administration of capsinoids did not raise the tail skin temperature, an intravenous injection of capsinoids did, indicating that capsinoids could barely pass through the intestinal wall into the blood. Taken together, gastrointestinal TRPV1 may be a critical target for capsinoids to enhance energy expenditure.

MeSH terms

  • Adipose Tissue / drug effects
  • Adipose Tissue / metabolism
  • Animals
  • Capsaicin / administration & dosage
  • Capsaicin / analogs & derivatives*
  • Capsaicin / pharmacology*
  • Denervation
  • Energy Metabolism / drug effects
  • Gases / metabolism
  • Gastrointestinal Tract / drug effects*
  • Gastrointestinal Tract / innervation
  • Gastrointestinal Tract / metabolism*
  • Gastrointestinal Tract / physiology
  • Gene Knockout Techniques
  • Injections, Intravenous
  • Jejunum / drug effects
  • Jejunum / innervation
  • Jejunum / metabolism
  • Jejunum / physiology
  • Kinetics
  • Male
  • Mice
  • Oxidation-Reduction
  • Respiration / drug effects
  • Skin / drug effects
  • TRPV Cation Channels / deficiency
  • TRPV Cation Channels / genetics
  • TRPV Cation Channels / metabolism*
  • Thermogenesis / drug effects*


  • Gases
  • TRPV Cation Channels
  • TRPV1 protein, mouse
  • Capsaicin