Rocaglaol

Description

Rocaglaol is a cytotoxic cyclopenta[b]benzofuran, shows in vitro cytotoxic activity against Lu1, LNCaP and MCF-7 cells with ED50 values of 13.8, 23.0 and 9.2 nM, respectively. Rocaglaol is a potent anticancer drug that induces apoptosis of LNCaP cells through the mitochondrial pathway and its G2/M-phase cell cycle arrest is associated with the down-regulation of Cdc25C and the dephosphorylation of Cdc 3. Rocaglaol can reduce tissue inflammation and neuronal cell death by inhibiting NF-kappa B and AP-1 signaling, resulting in significant neuroprotection in animal models of neurodegeneration. 4. Rocaglaol derivatives can prevent or to limit the cardiotoxicity of an antineoplastic agent, in particular to prevent or to limit the apoptosis of cardiomyocytes induced by such agent. 5. Rocaglaol, pyrimidinone and aglaiastatin are potent inhibitors of the growth of K--cells, with IC50 values of 1-10 ng/mL, and induce normal morphology in K--cells at 10-30 ng/mL, they also specifically inhibit protein synthesis.

Uses

Rocaglaol is an active derivative of rocaglamide with antifungal and apoptotic activity.

target

Bcl-2/Bax | TNF-α | AP-1 | NF-kB