Didesmethylrocaglamide

Didesmethylrocaglamide is a flavagline that has been found in A. perviridis and has NF-κB inhibitory and anticancer activities.^1,2,3 It inhibits NF-κB activation induced by TNF-α or phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in Jurkat T cells (IC₅₀s = 58.4 and 43.6 nM, respectively); however, it is not active in an ELISA NF-κB assay (EC₅₀ = >20 µM).^1,2 Didesmethylrocaglamide is selectively cytotoxic to HT-29 colon cancer cells over CCD-112CoN normal colon cells (IC₅₀s = 0.021 and >50 µM, respectively).¹ It decreases protein levels of mitogenic kinases and STAT3, which is consistent with protein translation inhibition, in MG-63 osteosarcoma cells but does not affect protein levels of eukaryotic translation initiation factor 4A1 (eIF4A1) or eIF4A2 in the same cells.³ Didesmethylrocaglamide reduces tumor volume and induces intratumoral apoptosis in a patient-derived xenograft (PDX) mouse model of canine osteosarcoma.

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1. Pan, L., Acuña, U.M., Li, J., et al. Bioactive flavaglines and other constituents isolated from Aglaia perviridis. J. Nat. Prod. 76(3), 394-404 (2013).

2. 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).

3. Oblinger, J.L., Wang, J., Wetherell, G.D., et al. Anti-tumor effects of the eIF4A inhibitor didesmethylrocaglamide and its derivatives in human and canine osteosarcomas. Sci. Rep. 14(1), 19349 (2024).