Rocaglamide

Rocaglamide is an anti-inflammatory, insecticidal, and anticancer tetrahydrobenzofuran isolated from Aglaia species. It has been shown to inhibit both TNF-α and the activation of NF-κB in Jurkat T cells with IC₅₀ values in the nanomolar range.¹ At 25 nM, rocaglamide induces apoptosis in various human leukemia cell lines, activating p38 MAPK/JNK and suppressing ERK.² Rocaglamide also reduces IFN-γ, TNF-α, IL-2, and IL-4 production in peripheral blood T cells at a concentration of 50 nM.³ Furthermore, rocaglamide can inhibit the T cell expression of the immune response transcription factor, nuclear factor of activated T cells.³

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1. Baumann, B., Bohnenstengel, F., Siegmund, D., et al. Rocaglamide derivatives are potent inhibitors of NF-κB activation in T-cells. The Journal of Biological Chemisty 277(47), 44791-44800 (2002).

2. Zhu, J.Y., Lavrik, I.N., Mahlknecht, U., et al. The traditional Chinese herbal compound rocaglamide preferentially induces apoptosis in leukemia cells by modulation of mitogen-activated protein kinase activities. Int. J. Cancer 121(8), 1839-1846 (2007).

3. Proksch, P., Giaisi, M., Treiber, M.K., et al. Rocaglamide derivatives are immunosuppressive phytochemicals that target NF-AT activity in T cells. J. Immunol. 174(11), 7075-7084 (2005).