Font Size: a A A

Synthesis, Structure And Antitumor Activity Study Of Some Kinds Of Transition Metal-HTDA Complexes

Posted on:2015-05-22Degree:MasterType:Thesis
Country:ChinaCandidate:J J LiFull Text:PDF
GTID:2284330431479077Subject:Pharmacy
Abstract/Summary:PDF Full Text Request
Malignant tumors, is one of the most serious threat to human health, at present we use chemotherapeutic drug in treating. Cisplatin is one of the most effective anticancer drugs in the treatment of a variety of human tumors, and its extensive usage as an antitumor drug has initiated investigations in the medicinal bioinorganic research field toward numerous platinum complexes. Unfortunately, its clinical usefulness has frequently been limited by several negative side effects (nephrotoxicity, neurotoxicity, nausea, etc.) and the emergence of cancer cells resistant to cisplatin, so it has also stimulated and generated new areas of research, which mainly focused on the search for new metal-based complexes with lower toxicity and more improved therapeutic properties.As transition metal, Co, Ni and Zn is the first choice of central ions, because of their multiple Ligand forms.So the significances of study on metal complexes and their interaction with DNA are as follows:exploring thestructure probe that can specifically recognize the DNA target; revealing the structure and properties of DNA andthe mystery of life. research on the mechanisms of anti-cancer drugs at molecular level; develop novel drugs with less toxicity and higher activity.In this paper,1H-1,2,3-triazole-4,5-dicarboxylic acid(Htda) was taken as ligand to obtain Co single crystals and Ni, Zn complexes, which charter have been studied; the primary interaction mechanism of the complexes with DNA was studied by means off luorescence spectrum, Agarose gel electrophoresis experiment and the antitumour activity of them has been also tested. The main research in this paper includes four sections as follows:(I) Co single crystal and Ni, Zn complexes have been obtained at room temperature, molecular formula are as follows:[Co2(Htda)2(H20)6-5H20](complex1).[Ni2(Htda)2(H20)6-5H20](complex2)、[Zn2(Htda)2(H20)6-5H20](complex3),(Htda=1H-1,2,3-triazole-4,5-dicarboxylic acid).(Ⅱ) Co single crystalwas characterized and verified by IR, elemental analysis and single-crystal X-ray crystallography. The twocomplexes were characterized and verified by IR, elemental analysis. Compare the testing resultsof the twocomplexes with the testing result of the Co single crystal, we can get the possible structural forms of the twocomplexes.(III) The binding behavior to DNA were studied by means of fluorescencespectrum and Agarose gel electrophoresis experiment. The results show that there was strong interaction between complexes and DNA.(IV) The inhibition ability of the three complexes on Helaand KB cell lines were tested by MTT method and compared with the clinical drug cisplatin. The IC50value was calculated using the mathematical statistics, The results reveal that the complexes have inhibition ability to cancer cells. Complex1shows the most activity to cancer cells. This paper’s research is a good reference for studying on transition metal complexes. Complexes were studied in the method of cell apoptosis in tumor cells in vitro inhibitory activity.
Keywords/Search Tags:transition metal complex, structural characterization, fluorescencespectrum, Agarose gel electrophoresis, inhibition ability, Anticancer activity
PDF Full Text Request
Related items