Original Articles

Effects on animal tumors and toxicity of lycobetaine acetate

Su-yin Zhang, Fei-li Lu, Jin-long Yang, Long-jiang Wang, Bin Xu


Lycobetaine, a derivative of lycorine, is a new type of antitumor drug. When lycobetaine acetate (AT-1840) was given ip to mice and rats inoculated with Ehrlich ascites carcinoma, ascites hepatoma, leukemia L-1210, leukemia P-388, Lewis lung cardinoma or Yoshida ascites sarcoma, the survival times of the tumor-bearing animals were prolonged significantly. Lycorine exhibited only negligible effect on the above-mentioned tumors.
The acute ip LD50 of AT-1840 in mice was 72 mg/kg. In dogs iv 3 or 9 mg/kg of AT-1840 once every other day for 7 times produced no apparent toxic action except mild leucopenia and thrombopenia in the group of large dosage.
It seems that the presence of phenolic betaine in the molecule of AT-1840 bears some relationship to its antitumor activity.
AT-1840 has been recommended for clinical trials.

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