In this paper, L-valine and menthol was used as raw materials，then valine menthyl eater was synthesized with DCC / DMAP as catalyst, The structure of the compound was identified by MS, MR and IR.Then, bioactivity of anti-epilepsy and antitumor were carefully measured by the method of maximal electrical shock convulsion experiment（MES）and Inhibition of HeLa cell growth experiment respectively。it showed that:(1) In the maximal electrical shock convulsion experiment, mice were injected intraperitoneally, when valine melaminate was dosed at 100 mg / kg, compared with saline and carbamazepine groups, four experimental mice, The convulsions number of mice after 0.5, 1, 2, 3 and 4 h were 2, 2, 2, 1 and 0, respectively, which showing antiepileptic activity similar to the reference substance carboplatin ;(2) In the antitumor experiments, growth of HeLa cells were significantly inhibited,and the highest inhibition rate reached 52.5%.