Synthesis The Gossypol Derivatives And Study On The Biological Activity

The problem about the process of extracting gossypol from the cotton seed was studied in this paper, the gossypol derivatives (their structure were studied by FT-IR, ¹H NMR as well as MS methods) were synthesized , and then the biological activity such as the cell inhibition , the interaction with the ct-DNA and hydrolysis of the plasmid DNA by metal complexes with the gossypol derivative II were discussed . The experiment results were following:(1) Study on the production of gossypol from cotton seedThe technology of the aniline-acetone was choosed in this paper, this is to say, the free gossypol was extracted from the cotton seed with organic reagent, next reacted with the aniline, then was converted to the acetic acid gossypol by the sulphuric acid . During the gossypol recrystalled to the pure , we used the aether and acetone intersection and anti- oxidation treatment. All these methods succeed to settling the problem that gossypol is oxidized easily .The purity of the acetic acid gossypol reached to the expectant require.(2) Study on the cells inhibition of the gossypol acetic acid and its derivatives Gossypol acetic acid and its derivatives were found to be able to inhibit the survival of the K562 cell by MTT assay, the inhibition rate of which are greater than the cis-Platinum( II )-Diammine Dichloride. The IC₅₀ of the gossypol derivative II is 5 times of gossypol acetic acid, 12 times of gossypol derivative I, 6 times of gossypol III and IV.(3) Study on the interaction of gossypol derivatives with ct-DNAThe interaction between derivatives of gossypol and ct-DNA were studied by UV-Vis spectroscopy. The result showed that the compounds were bound to ct-DNA by intercalation and formed the 1:1 complexes. The order of the interaction is: gossypol II>gossypol I>gossypol acetic acid ?gossypol III,IV.(4) Study on the hydrolysis of the plasmid DNA by metal complexes with the gossypol derivative IIThe experiment of the agarose electrophoretic gels showed that the gossypol derivative II can be used as pUC19 DNA cleavage agent in the presence of Cu²⁺,Zn²⁺, while they had no cleavage activity respectively.