Synthesis, Characterization, Antioxidant Activity And Hepatoprotective Of Silybin Lactosified Derivatives

Silybum marianum (L.) Gaertn. has been used for more than2000years to treat liver and gallbladder disorders. Silymarin is a mixture of several flavonolignans isolated from fruits and/or seeds of Silybum marianum. Silybin, as the main bioactive constituents in silymarin, is used for the prophylaxis and treatment of liver damage caused by metabolite toxins, e.g. alcohol, tissue poison, in liver dysfunction and after hepatitis (post-hepatic syndrome), and in chronic degenerative liver conditions. Recently, silybin received new attention due to its potential mostly anticancer, chemopreventive activity and resistance of diabetes. However, the bioavailability and therapeutic efficiency and clinical medication of silybin is rather limited by its very low solubility. At present the main drug clinical with amine salt or capsule form Silybin to improve the solubility and bioavailability. Given that the relationship between its functions and structures, silybin was modified via chemical methods in order to improve the solubility and the biological activity in this paper. To investigate silybin whether has bad effect on acute alcohol-induced hepatotoxicity to the glycosidlation of silybin. For the use of silybin in clinical medication provides a new solution.Chapter1The biological activity and the glycosidlation method of silybin and its andpharmacology pharmacodynamic research progress, clarify the direction and significance of this research, the researching aims, meanings and content.Chapter2The experiment was designed to synthesis the lactosified derivat ives from silybin and lactos which has best solution and well characteristics of the directional with the liver parenchyma cells and tumor cell to improve the solubility, bioavailability and the hepatic target. The structural of the target co-mpound was characterized by IR, ESI-MS,1HNMR and13CNMR methods.Chapter3The solubility of the silybin and its lactosified derivatives was researched by dynamic method in this section. The synthetic products were found to possess good antioxidant activity compared with the parent compound, as determined using DPPH radical scavenging, reducing power, osphomolybdenum method and determination of lipid peroxidation. Results show that the modified can effectively improve the lactose to water-soluble, guests of milk thistle antioxidant activity has been improved greatly.Chapter4Established acute alcohol-induced liver injury model, Evaluation of the effect of Silybin-23-O-lactoside(Sil-Lac.), acetylated lactoside(Sil-LacAc O8)by measuring the liver damage of various biochemical indicators, a-nd histo pathological change,its possible mechanism, The results show that:The lactosid lation of silybin improve its solubility, has no bad effect on acute alcohol-indu ced hepatotoxicity. and it was better than Silybin.