Inhibition of hepatic tumor cell proliferation in vitro and tumor growth in vivo by taltobulin,a synthetic analogue of the tripeptide hemiasterlin

AIM： To investigate the inhibitory effects of taltobulin （HTI-286）, a synthetic analogue of natural hemiasterlin derived from marine sponges, on hepatic tumor growth in vitro and in vivo. METHODS： The potential anti-proliferative effects of HTI-286 on different hepatic tumor cell lines in vitro and in vivo were examined. RESULTS： HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines （mean IC50 = 2 nmol/L ±1 nmol/L） in vitro. Interestingly, no decrease in viable primary human hepatocytes （PHH） was detected under HTI-286 exposure. Moreover, intravenous administration of HTI-286 significantly inhibited tumor growth in vivo （rat allograft model）. CONCLUSION： HFI-286 might be considered a potent promising drug in treatment of liver malignancies. HTI-286 is currently undergoing clinical evaluation in cancer patients.