Pellitorine | TRPV1 blocker and anti-inflammatory agent

Pellitorine chemical structure

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Pellitorine (18836-52-7) is a weak TRPV1 blocker.1 Suppresses lipid accumulation in developing 3T3-L1 adipocytes.2 Inhibits LPS-induced production of TNFα and IL-6 and activation of NFκB in HUVECs at 10 µM.3 Inhibits free fatty acid uptake in Caco-2 cells.4 Inhibits LPS-induced nitric oxide production in RAW264.7 cells (IC50=14.5 µM) exhibiting anti-inflammatory activity by activation of the Nrf2/HO-1 pathway.5

References/CItations:

  1. Olah et al. (2017), Pellitorine, an extract of Tetradium daniellii, is an antagonist of the ion channel TRPV1; Phytomedicine, 34 44
  2. Lieder et al. (2017), The Alkamide trans-Pellitorine Targets PPARγ via TRPV1 and TRPA1 to Reduce Lipid Accumulation in Developing 3T3-L1 Adipocytes; Front. Pharmacol., 8 316
  3. Lee et al. (2014), Vascular barrier protective effects of pellitorine in LPS-induced inflammation in vitro and in vivo; Fitoterapia, 92 177
  4. Rohm et al. (2015), Capsaicin, nonivamide and trans-pellitorine decrease free fatty acid uptake without TRPV1 activation and increase acetyl-coenzyme A synthetase activity in Caco-2 cells; Food Function, 6 173
  5. Ngo et al. (2017), Alkaloids from Piper nigrum Exhibit Antiinflammatory Activity via Activating the Nrf2/HO-1 Pathway; Phytother. Res., 31 663
18836-52-7, pellitorine, Pellitorine supplier

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Pellitorine (18836-52-7) is a weak TRPV1 blocker.1 Suppresses lipid accumulation in developing 3T3-L1 adipocytes.2 Inhibits LPS-induced production of TNFα and IL-6 and activation of NFκB in HUVECs at 10 µM.3 Inhibits free fatty acid uptake in Caco-2 cells.4 Inhibits LPS-induced nitric oxide production in RAW264.7 cells (IC50=14.5 µM) exhibiting anti-inflammatory activity by activation of the Nrf2/HO-1 pathway.5

References/CItations:

  1. Olah et al. (2017), Pellitorine, an extract of Tetradium daniellii, is an antagonist of the ion channel TRPV1; Phytomedicine, 34 44
  2. Lieder et al. (2017), The Alkamide trans-Pellitorine Targets PPARγ via TRPV1 and TRPA1 to Reduce Lipid Accumulation in Developing 3T3-L1 Adipocytes; Front. Pharmacol., 8 316
  3. Lee et al. (2014), Vascular barrier protective effects of pellitorine in LPS-induced inflammation in vitro and in vivo; Fitoterapia, 92 177
  4. Rohm et al. (2015), Capsaicin, nonivamide and trans-pellitorine decrease free fatty acid uptake without TRPV1 activation and increase acetyl-coenzyme A synthetase activity in Caco-2 cells; Food Function, 6 173
  5. Ngo et al. (2017), Alkaloids from Piper nigrum Exhibit Antiinflammatory Activity via Activating the Nrf2/HO-1 Pathway; Phytother. Res., 31 663