Antitumor Effect of Alkannin Derivative,SYUNZ-4

OBJECTIVE To explore in vitro cytotoxicity and in vivo antitumor effect of semi-dynthesized alkannin derivatives of[3,11-bis(2-hydroxyethanesulfonyl)-6-isohexenylnaph-thazarin,SYUNZ-4].METHODS The cytotoxicity of SYUNZ-4 was assayed using MTT method.Efficiency was evaluated using IC50.In vivo antitumor effect was tested by models of transplanted tumor in mice and nude mice.RESULTS SYUNZ-4 presented strong cytotoxicities on 7 kinds of human cancer cell lines.The IC50 were 0.30~7.75 mg·L-1.The IC50 of SYUNZ-4 to 2 kinds of MDR cells (MCF-7/ADR and KBV200) were 1.96 and 7.78 mg·L-1.Under the doses of 2.0, 6.0 and 10.0 mg·kg-1, ip, q2d×10 d, the tumor inhibitory rates of SYUNZ-4 to against sarcoma S-180 and HepS in mice, were 31.5%~69.7% and 45.9%~67.5%,respectively (P0.01~0.001).Under the doses of 2.0, 6.0, 10.0 and 14.0 mg·kg-1, the tumor inhibitory rates on tumor ESC in mice were 30.2%~58.1% (P0.05~0.01).Under the doses of 6.0 and 10.0 mg·kg-1, ip, q3d×18 d, the tumor inhibitory rates of SYUNZ-4 to human lung adenocarcinoma cell (GLC-82) xenografts in nude mice were 48.4% and 61.7% (P0.01~0.001).Under the doses of 2.0, 6.0 and 10.0 mg·kg-1, the tumor inhibitory rates of SYUNZ-4 on human nasopharyngeal carcinoma (CNE2) xenografts in nude mice were 35.5%, 41.9% and 48.3%, respectively (P0.01~0.001).CONCLUSION SYUNZ-4 has strong cytotoxity and antitumor activity.