Química medicinal

Hsp70 Induction and Anticancer Activity of U-133, the Acetylated Trisglucosydic Derivative of Echinochrome

Abstract

Ekaterina A Yurchenko, Ekaterina S Menchinskaya, Sergei G Polonik, Irina G Agafonova, Irina V Guzhova, Boris A Margulis and Dmitry L Aminin

Acetylated trisglucosydic derivative of 2,3,5,6,8-pentahydroxy-7-ethyl-1,4-naphthoqinone (natural sea urchin pigment echinochrome), compound U-133, was synthesized. The effect of U-133 upon mouse Ehrlich ascitic carcinoma(EAC) cells in vitro and its antitumor activity in vivo was investigated. The synthesized U-133 did not display the pronounced cytotoxicity against EAC cells in the concentrations up to 80 μM. In non-cytotoxic concentration of 5 μM U-133 significantly induced Hsp70 expression in cancer cells and enhanced cell-mediated cytotoxicity of mouse splenocytes against EAC cells. The administration of U-133 in dosage of 100 mg/kg in carcinoma bearing mice resulted in significant inhibition of tumor growth and increase in mouse lifespan.