Helenalin

Helenalin is a sesquiterpene lactone first isolated from various species of Arnica. It has anti-inflammatory effects, most notably by inhibiting gene expression mediated by NF-κB at doses from 1 to 20 µM.^1,2 Like other sesquiterpene lactones, helenalin can modify sulfhydryl groups of cysteine residues and it alkylates these groups on the p65 subunit of NF-κB.¹ It also suppresses the proliferation of cancer cells through multiple mechanisms, including the prevention of signaling through NF-κB.^3,4,5 Helenalin has antibacterial and anti-protozoal activities.^6,7

WARNING This product is not for human or veterinary use.

1. Lyss, G., Knorre, A., Schmidt, T.J., et al. The anti-inflammatory sesquiterpene lactone helenalin inhibits the transcription factor NF-κB by directly targeting p65. The Journal of Biological Chemisty 273(50), 33508-33516 (1998).

2. Jin, F., Liu, X., Zhou, Z., et al. Activation of nuclear factor-κB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res. 65(14), 6354-6363 (2005).

3. Fernandes, K.M., Auld, C.A., Hopkins, R.G., et al. Helenalin-mediated post-transcriptional regulation of p21(Cip1) inhibits 3T3-L1 preadipocyte proliferation. J. Cell. Biochem. 105(3), 913-921 (2008).

4. Zhao, L., Lee, J.Y., and Hwang, D.H. Inhibition of pattern recognition receptor-mediated inflammation by bioactive phytochemicals. Nutr. Rev. 69(6), 310-320 (2011).

5. Lim, C.B., Fu, P.Y., Zhu, H.S., et al. NF-κB p65 repression by the sesquiterpene lactone, Helenalin, contributes to the induction of autophagy cell death. BMC Complement. Altern. Med. 12, 1-12 (2012).

6. Schmidt, T.J., Nour, A.M.M., Khalid, S.A., et al. Quantitative structure-antiprotozoal activity relationships of sesquiterpene lactones. Molecules 14(6), 2062-2076 (2009).

7. Boulanger, D., Brouillette, E., Jaspar, F., et al. Helenalin reduces Staphylococcus aureus infection in vitro and in vivo. Vet. Microbiol. 119, 330-338 (2007).