Abstract:

In this study,three cordyceps derivatives were synthesized with cordycepin as the raw material to study their anti-tumor activity in vitro and pharmacokinetics in rats.The human hepatoma cell HepG2 was used as the research object,and the inhibitory effects of the three cordycepin derivatives on HepG2 were determined by MTT assay.The plasma drug concentration of three cordycepin derivatives was observed by HPLC method.The pharmacokinetics of rat plasma was evaluated.The results showed that,the inhibition rate of cordycepin derivatives on HepG2 cells is increased.The IC₅₀ values of cordycepin and derivatives are 0.12,0.11,0.07,0.06 μM,respectively.The T_max  time of the cordycepin derivative is prolonged,and the time of the drug in the body is prolonged;when the C_max is increased,the concentration of the drug in the body is increased.

Key words: cordycepin, modification, activity, anti-tumor, pharmacokinetics