Capsiate is a non-pungent analog of capsaicin that has been found in C. annuum and has diverse biological activities.1,2,3,4 It inhibits Src in, as well as VEGF-induced proliferation of and tube formation by, human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 25 µM.1 Capsiate activates transient receptor potential vanilloid 1 (TRPV1) in HEK293 cells expressing the human channel (EC50 = 290 nM) and induces licking and biting behaviors, markers of nociception, in mice.2 Topical application of capsiate reduces antigen-induced increases in ear thickness in a mouse model of passive cutaneous anaphylaxis and decreases epidermal thickness and eosinophil and mast cell infiltration in a mouse model of atopic dermatitis.3 Capsiate (10 mg/kg) decreases body weight gain and perirenal fat weight, as well as increases oxygen consumption, fat oxidation, and carbohydrate oxidation, in a mouse model of ad libitum feeding-induced weight gain.4
1.Pyun, B.-J., Choi, S., Lee, Y., et al.Capsiate, a nonpungent capsaicin-like compound, inhibits angiogenesis and vascular permeability via a direct inhibition of Src kinase activityCancer Res.68(1)227-235(2008) 2.Iida, Y., Kobata, T.M., Morita, A., et al.TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiateNeuropharmacology44(7)958-967(2003) 3.Lee, J.J., Lee, Y.S., Lee, E.-J., et al.Capsiate inhibits DNFB-induced atopic dermatitis in NC/Nga mice through mast cell and CD4+ T-cell inactivationJ. Invest. Dermatol.135(8)1977-1985(2015) 4.Haramizu, S., Kawabata, F., Ohnuki, K., et al.Capsiate, a non-pungent capsaicin analog, reduces body fat without weight rebound like swimming exercise in miceBiomed. Res.32(4)279-284(2011)