Datelliptium (chloride)

Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities. In Vitro: Datelliptium (100 μM) shows significantly cytotoxic effects after 2 hr of treatment in suspension and primary cultures of rat hepatocytes. Datelliptium mobilizes glycogen in both rat systems in vitro concentration dependently. The half-maximal effect is 14.3 μM in isolated hepatocytes, whereas in cultured rat hepatocytes it is 5.9 μM. Datelliptium also leads to a concentration-dependent decrease in gluconeogenesis from lactate in cells^[1]. Datelliptium acetate is selectively cytotoxic for solid tumors over leukemia L1210. Human tumors H-125 and HCT-116 demonstrates less sensitivity to datelliptium acetate^[2]. In Vivo: Upon intravenous administration, datelliptium acetate shows potent inhibitory activities in vivo against a variety of murine solid tumors. Datelliptium acetate is highly active against early-stage colon #38 with highest non-toxic dose (HNTD) of 170 mg/kg TD, and weight loss of 10%, T/C of 0%^[2].