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Study On The Structure And Pharmacological Action Of Ruthenic Acid Metal Complexes

Posted on:2015-05-03Degree:MasterType:Thesis
Country:ChinaCandidate:H XiangFull Text:PDF
GTID:2134330467471610Subject:Medicinal chemistry
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Object:Now,many reseach suggest that the traditional Chinese medicine chemical composition equals to the extract and separation product of the medicine,they less attention the metal complex of these product.Through the traditional Chinese medicine theory of coordination,the active ingredients of medicine may exist in the form of their comlexes,but they have been destroyed because of extraction and separation process.Many study report that after natural-product form metal complexes,their biological activity enhense.In this experiment,we use mental complexse as the reseach object,choose Rhein as the ligand,synthesis9Rhein metal complexes,then comfirm their structrue,in order to provide ideas of structure reseach to complex.By comparing with the ligand rhein,study the changes of antibacterial activity、antioxidant activity、antitumor activity,then screen out the optimal complex,hope to provide gist to further development and utilization.Method:This experiment chooses Rhein-anthraquinone in Rhubarb, as the ligand,choose9essential trace element of human as the central iron.Through the process inspection experiment,we choose the preferred plan to synthesis9rhein mental complexes.Using titration、infrared spectroscopy(IR)、ultraviolet spectroscopy(UV)、H NMR spectroscopy(NMR) to affirm the structure of the rhein mental complexes.According to the atlas and data of complexes,we analyze the structure of the complexes.In the part of pharmacological experiment,by the method of filter paper we test the inhibiting capacity to3bacteria(staphylococcus aureus、streptococcus pneumoniae、escherichia coli)of the metal complex,using double dilution method to test the MIC of the9complexes.Using the UV spectrum,study the clearance rate of Rhein and9Rhein metal complex to DPPH free redical、O2-·free redicals and·OH free redical,then caculate the half of the clearance.Using the MTT test to study the antitumor activity of rhein and complexes to HepG2(hepatoma cell of human) cell and then caculate the IC50.Through analysing the date of the above experiments,we sort these complexes by their pharmacological active strength,and screen out the optimal complex.Results:(1) Through the synthesis process, we can see the optimal process of Rhein complexes is:Choose the synthesis temperature as40℃,the synthesis time as4h,the synthesis pH as10.The synthetic products compared with the Rhein,we can see that the appearence and physical property of the Rhein metal complexes have changed a lot.(2)Use titration、infrared spectroscopy(IR)、ultraviolet spectroscopy(UV)、H NMR spectroscopy(NMR) to affirm the structure of the rhein mental complexes,the resault shows:The rhein forms complex throught the1-hydroxide radical and9-carbonyl,the complex contain2Rhein and1metal ion (Ca Complex contain1Rhein and1metal ion)(3)The experiment resault shows that:The pharmacological activity of most of the complex enhence compare with Rhein.In the antibacterial experiment,the strongest inhibition to streptococcus pneumoniae and escherichia coli is Rhein-Cr (Ⅲ),the strongest inhibition to staphylococcus aureus is Rhein-Fe(Ⅱ);In the antioxidation experiments,the scavenging action to DPPH redical of Rhein and complexes is weaker.The scavenging action to OH· and O2-· of Rhein-Fe(Ⅱ) are the strongest.In the antitumur experiments,the antitumor activity of Rhein-Fe (Ⅲ) is strongger than other complexesConclusion:Through structure characterization, we can see that the Rhein forms complex throught the1-hydroxide radical and9-carbonyl,the complex contain2Rhein and1metal ion.After Rhein form complex (Rhein-Ca contain1Rhein and1metal ion),the antioxidation,and the nntibacterial activity and antitumur activity of most of the complexes enhence a lot compare with the Rhein,this suggest that,Rhein and metal ion can produce synergistic effect.Among them,the pharmacological activity of Rhein-Cr (Ⅲ) and Rhein-Fe(Ⅱ) are the best.
Keywords/Search Tags:Rhein, Complex, Structure, Pharmacological activity
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