Study On The Synthesis And Bioactivity Screening Of Taurine-derivatives And Their Metal Complexes

Obeject:Considering the cardiovascular function of taurine and the biological activi-ty of some metals, we design and synthesize a serious of metal compounds containing the derivatives of taurine and some transition metals, and then try to find a new kind of cardiovascular drug or antitumor drug by animal studies.Methods:First, synthesize three derivatives of taurine (Taurine-Salicylic Schiff base sodium (TSSBNa), Reducing Taurine-Salicylic Schiff base (RTSSB), and Taurine-Sal icylic Schiff base magnesium (TSSBMg)) on the basis of studying about Taurine Magnesium Complex (TMC). Crystals of TSSBNa were obtained by recrystallization of crude solid in C2H5OH/H2O and an animal study about the TSSBNa was done for its potential cardiovascular function. Second, synthesize seven derivatives of taurine (Taurine-2-Pyridinecarboxaldehyde Schiff base (TPCSB),[Cu(TPCSB)(dca)]NO3, Taurine-3-Hydroxyl-p-anisaldehyde Schiff base(THA),N,N-(2-pyridyl)methyl](TBM),[Cu(TBM)Cl]-2H2O,[Co2(TBM)(THM)(AC)2], et al) in view of lots of reports about the antibacteria or antitumor effects of metal complexes with Schiff base or tripodal ligands. The interactions between DNA and complex [Cu(TBM)Cl]-2H2O has been studied. Antibacterial effect of several compounds were investigated by measuring the diameter antibacterial rings of Bacillus coli. During the experiment, infrared spectrum, nuclear magnetic resonance-1H, emission spectrum, and X-ray crystallogra-phy are used to determine the crystal structures.Result:1. The result indicated that TSSBNa protect heart from ventricular fibrillation induced by chloroform in mice. Compared with the physiological salt solution group, the death time in2mg/10g of TSSBNa group is remarkably lower (P<0.05).2. We succeeded in synthesizing seven new compounds and determining their crystal structures by X-ray crystallography. The results of the DNA experiment indicated that interaction between pBR322DNA and the complex [Cu(TBM)Cl]-2H2O is very weak. And the results of microbial inhibition experiment showed that the complexes of [Cu(TPCSB)(dca)]NO3,[Cu(TBM)Cl]·2H2O and [Co2(TBM)(THM)(AC)2] have some antibacterial activity. Of them, the compound with the strongest antibacterial activity is TBM, whose diameter of antibacterial rings is about14.5mm.Further experiment about the antitumor activity of complex [Cu(TBM)Cl]-2H2O, such as cytotoxicity test, is under way.Conclusion:Taurine is a weak-coordinated ligand and hard to chelate with magnesium, so we design and synthesis its Schiff-base derivations to enhance the coordination ability. As a prodrug, the cardiovascular function of Taurine-Salicylic Schiff base sodium (TSSBNa) was studied. The result indicated that TSSBNa protect heart from ventricular fibrillation induced by chloroform in mice. Compared with the physiological salt solution group, the death time in2mg/10g TSSBNa group is remarkably lower (P<0.05). Seven new compounds were synthesized and their crystal structures were determined by X-ray crystallography in view of their potential antitumor effects. According to the mechanism of cisplatin, many metal complexes can kill the tumour cell by DNA interaction, so we made a test to check the interaction between pBR322DNA and [Cu(TBM)Cl]-2H2O. However, the electro-phoretogram indicated that the DNA interaction with [Cu(TBM)Cl]-2H2O are irregular and weak. We also made a study about the antibacterial activity of all these compounds. And the results showed that the compounds of [Cu(TPCSB)(dca)]NO3,[Cu(TBM)Cl]·2H2O,[Co2(TBM)(THM)(AC)2] and TBM have some antibacterial activity. Of them, the compound of TBM has the strongest antibacterial activity. The cytotoxicity test of complex will be carried out to make clear wheather it can affect the tumour cells. The DNA interaction of other complexes was being studied.