Preparation And Anticancer Evaluation Of Radix Aconiti Kusnezoffii Polysaccharide Metal Complexes;Synthesis And Biological Evaluation Of 1,2,4-triazole Triazene Derivatives

Radix aconiti kusnezoffii is the dried roots of Aconitum kusnezoffii Reichb.,containing a variety of biological active substances.Radix aconiti kusnezoffii has been used in Chinese herbal medicine to treat mang diseases,such as rheumatism and arthritis.So we decide to study on the extraction technology of the polysaccharides from Radix aconiti kusnezoffii,expecting to improve the development and utilization on this plant.At the same time,we study on the preparation and anticancer evaluation of Radix aconiti kusnezoffii polysaccharide metal complexes.The corresponding work is: 1.By using water as extraction reagent,the polysaccharides in Radix aconiti kusnezoffii were extracted.The results showed that optimum extraction condition was extraction temperature 90?,extraction time 4 h,liquid to material ratio 1:50.2.Four polysaccharide metal complexes were prepared by using four metal ions(Ca²⁺,Zn²⁺,Cu²⁺,Fe³⁺)and polysaccharides from Radix aconiti kusnezoffii,respectively.All complexes were evaluated for biological activity against three human cancer cell lines?HepG2,MCF-7 and HT-29?by the standard MTT method and the results showed that PRS-Cu possessed higher growth inhibitory effects.The complex was characterized by infrared spectrum?IR?,ultraviolet spectrum?UV?,circular dichroism?CD?,scanning electron microscopy?SEM?and thermogravimetric analysis?TGA?.Triazenes are a very useful and diverse class of compounds.They have been studied as chromogenic reagent for determination concentrations of metal ions,used to generate other functional groups,and used to synthesize heterocycle.With the development of researching,people found some triazenes compounds show anticancer activity,so scientists study out some triazenes drugs,such as dacarbazine?DTIC?and temozolomide?TMZ?,but these drugs have some shortcomings,such as poor absorption,great toxicity and so on.Aiming at theses side effects,we use 1,2,4-triazole as a lead compound,triazenes as substituent group,30 substituted 1,2,4-triazole triazene derivatives were synthesized by using combination principle.Hope these new compounds may improve the antitumor activity and less side effects.The corresponding work is: 1.Using 4-aminobenzoic acid as starting material,it through esterification reaction,diazotization reaction,coupling with dimethylamine?or Nmethylbenzylamine?,hydrazinolysis reaction,cyclization and nucleophilic substitution reaction with benzyl chloride to obtain a series of 1,2,4-triazole triazene derivatives.2.Mercaptan and thiourea as starting material react with 3-?4-?triaz-1-enyl?-phenyl?-4-?amino?-5-thiol-1,2,4-triazole to obtain a series of 3-?4-?triaz-1-en-yl?-phenyl?-4-?amino?-5-disulfide-1,2,4-triazole derivatives.The anticancer activity of all compounds were screened by using MTT assay in vitro.The results of cell experiments showed that some compoundes exhibit antitumor activity.