Preparation And Antitumor Activity Test Of Genistein Metal Chelates

Genistein(5-dihydroxy-3-（4-hydroxyphenyl）-4H-1-benzopyran-4-one;In recent years,genistein has become the focus of biological,chemical and medical research.The analytical methods and pharmacological effects of genistein and its derivatives have been studied by domestic and foreign scholars.The preparation process was studied.By consulting the literature,we know that genistein has good activity and efficacy in the prevention of breast cancer,prostate cancer,cardiovascular diseases and menopausal syndrome in women,as well as in the prevention of other cancers.Vision and potential.However,because of the lipophilicity of genistein,the hydrophilicity of genistein is relatively low,and there is a strong first-pass effect,which results in its actual drug effect is not so strong,the bioavailability is not high,and the utilization value is relatively low.This also limits the clinical application of genistein to a great extent.In this paper,genistein was used as the lead compound to chelate with the selected metal ions such as manganese,nickel,platinum,tin,titanium,ruthenium,palladium,gallium and so on,in order to find a better solubility of the metal ions,such as manganese,nickel,platinum,tin,titanium,ruthenium,palladium,gallium and so on.More active genistein chelates in order to be better placed Use genistein for the benefit of mankind.In the chelation experiment between genistein and metal ions,11 metal ions,such as manganese,nickel,platinum,tin,titanium,ruthenium,palladium and gallium,were chelated with genistein by controlling the reaction conditions such as pH,temperature and reagent ratio.Results the chelates of genistein manganese,genistein samarium,genistein palladium and genistein titanium chelate were successfully prepared.Then,using MTT reduction method and cisplatin as positive control,the successfully synthesized genistein metal samarium,palladium,manganese,titanium chelates and ligands were tested with lung cancer cell line K549 and cervical cancer HELA cell line.The results showed that genistein palladium chelate was used.The activity of genistein samarium chelate is much higher than that of genistein,but the activity is not as good as cisplatin.Then the synthesis process of the chelate of genistein palladium and genistein samarium was studied by orthogonal experiment and the optimum preparation technology was obtained.The optimum reaction conditions for the chelating experiment of genistein and palladium were as follows:reaction time was 10 h,reaction temperature was 55℃,reaction pH was 8.5,and the material ratio was 1:1;The optimum preparation parameters of the chelate of genistein and manganese are as follows:reaction time is 8 h,reaction temperature is 60℃,reaction pH is 8,material ratio is 2:1;The optimum technological parameters are reaction time of 8 h,reaction temperature of 50℃,reaction pH of 7.5 and material ratio of 1:1.The chelates of genistein palladium and genistein samarium chelate were characterized by HPLC,NMR,XRD,IR,UV spectra and elemental analysis.The most probable molecular formula of the two chelates is C₃₀H₂₀O₁₂Cl₂-Sm、C₃₀H₂₀O₁₂-Pd.However,the solubility experiment of genistein palladium chelate showed that the solubility of the chelate was not obtained by the samarium chelate of lignin.To fundamental improvement.In this paper,the reaction of genistein with betaine,L-carnitine and other organic alkaloids was also studied.The results showed that genistein betaine salts were successfully prepared.The anticancer activity and solubility of the salt were preliminarily discussed.The results showed that the salt had good water solubility and stronger anticancer activity than genistein itself.It will lay a foundation for further research and development of a new anti-tumor drug in the future.