Synthesis Of Disulfoethylaminogossypol And Its Anti-tumor Effects

Tumor is the leading disease that affects human health, it has important value to research and develop new anti-tumor drugs. This research prepares disulfoethylaminogossypol using gossypol as the starting material and investigates the anti-tumor effects.In this paper, disulfoethylaminogossypol was synthesized by the gossypol acetate and taurine. The yield and the purity were above 90% and 95% respectively. The research corroborated the chemical structure of disulfoethylaminogossypol which determined the element structure, the melting point, infrared spectrophotometry (IR), nuclear magnetic resonance spectroscopy (NMR), purity and content measurement was developed during the experiments.The research investigates the antitumor effect of the disulfoethylaminogossypol in vitro and in vivo. The disulfoethylaminogossypol shows wide and active anti-tumor effect and the inhibition rate of hepatocarcinoma and peneumon cancer are above 80% (P<0.001) an d 50% (P<0.01) respectively.The toxicity test and antitumor experiments of different administration route in vitro and vivo (oral intragastric administration and celiac injection) shows that disulfoethylaminogossypol is better than the gossypol acetate for the better pesticide effect, higher selectivity and lower toxicity. disulfoethylaminogossypol has a significant inhibitive effect on scrcoma S180, cervical carcinoma U14 and heps of the laboratory mouse, it can extend life span of leps laboratory mouse and has significant effect on the Lewis lung cancer and carcinoma of Liver.The study of the mechanism of the antitumor activity shows the disulfoethylaminogossypol can obviously restrain the growth and reproduction of the tumor cells from three respects. The first is to inhibit the energy metabolism of the tumor cells and divest the energy which supply the growth of tumor cells; the second is to strengthen the activity of the ribonuclease, superoxide dismutase (SOD) and the peroxidase which have the anti-tumor effect; the third is to combine the intranuclear basic protein in the tumor cells and inhibit the synthesis of DNA.The research provides the theoretical basis for searching new anti-tumor drugs, studying the metabolism of anti-tumor drugs and molecular rebuilding of anti-tumor drugs, and shows the broad perspective for the fully utilizing of gossypol.