Synthesis And Biological Interact With Bovine Serum Albumin Of 1,8-naphthalimide-Polyamine Conjugates

Objective:By mearns of changing the subsitutent groups at the 3-position of naphthalimide ring or changing the type of polyamine and composing alkyl group at the terminal of the polyamine.Except that synthesized a series of new naphthalene imides derivatives with high effect and low toxicity,selectivity and antitumor activity.Additionally,Exploring the interactions between MINS and bovine serum albumin.Methodes:Using the classical gabriel synthesis method get the polyamine side chains.Useing the mearns of spectroscopy and chromatography to study the relation of BSA and MINS Results:(1)A11 the compounds'have never been unreported and the structures of these compounds were confirmed by 1H NMR and ESI-MS.(2)We also analyzed the interaction with the bovine serum albumin based on the MINSas the representative drug.The binding of naphthalimide-polyamine conjugate to BSA resulted in a series of changes in the spectra characteristics.After binding to BSA,the absorption spectra of MINS showed a hyperchromic effect and the fluorescence emission of MINS and BSA was efficiently quenched.From these experimental results,it could be affirmed that MINS could effectively combine to BSA and that the quenching mechanism was overall static.Furthermore,the fluorescence quenching data measured at different temperatures(298,303 and 310K)suggested that the type of-BSA interaction was mainly hydrophobic interaction.However,synchronous and three-dimensional fluorescence spectral data didn't provide further evidence to the presence of the hydrophobic interactions between MINS and BSA.Moreover,MINS had weak influence on the conformational changes in BSA.Conclusion:(1)All the target compounds have never been reported and the structures of these compounds were confirmed;(2)Naphthalimide polyamine conjugate bound to BSA and caused a little BSA structural changes.