Rocaglamide (Roc-A), sourced from the Aglaia genus, is utilized for various ailments like coughs, injuries, asthma, and inflammatory skin disorders. It is a potent inhibitor of NF-κB activation in T-cells, a significant and selective suppressor of heat shock factor 1 (HSF1) activation with an IC50 value close to 50 nM, restricts the function of the translation initiation factor eIF4A, and exhibits anticancer effects, particularly against leukemia[1].[2].[3].
体内研究
In vivo studies show that tumor volumes in Rocaglamide-treated groups are reduced to 45±12% compared to the control group, indicating a significant suppression of tumor growth. Importantly, Rocaglamide treatment does not result in weight loss or display any signs of toxicity in mice, demonstrating its general tolerability[2].
体外研究
Rocaglamide effectively boosts TRAIL-induced apoptosis in resistant hepatocellular carcinoma (HCC) cells. Treatment with Rocaglamide alone induces apoptosis in 9% of HepG2 cells and 11% of Huh-7 cells, while TRAIL treatment leads to apoptosis in 16% of HepG2 and 17% of Huh-7 cells. Notably, the combined treatment with Rocaglamide and TRAIL induces apoptosis in 55% of HepG2 and 57% of Huh-7 cells, suggesting a synergistic effect. This enhanced apoptotic effect is also reflected in cell viability assessments via crystal violet staining. Thus, Rocaglamide has the potential to make highly chemoresistant HepG2 and Huh-7 cells more responsive to TRAIL-based treatments[2].
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