| Chrysin, 5, 7-dihydroxyflavone, which is widely distributed in plants has been known to have many biological activities including antioxidant, antibacterial, anticancery,anti-inflammatory, antiallergic, antiesrtogenic, and anxiolytic antivities. The recent studies on pharmacological action, extraction and isolation, pharmaceutical and structural modifications of chrysin were reviewed in Chapter one..Though chrysin, a flavone, has extensively pharmic values in clinic, there are still some flaws to confine its pharmic effects to some extent, including low dissolvability and imbibition. Efforts to improve the biological activity of chrysin have led to the development of its derivatives by appropriate modification of chrysin as mentioned in some published papers. The studies on phosphorous modification of chrysin and non-covalent interaction with protein were shown in dissertation. The relating works included:1. The recent studies on pharmacological action, extraction and isolation, pharmaceutics and structural modifications of chrysin were reviewed.2. Chrysin is firstly phosphorylated via dialkyl phosphite by Atherton-Todd reaction. Secondly, the N-phosphated amino acids are coupled with to form phosphoryl amino acids chrysin esters. Finally eleven chrysin derivatives were synthesized, including nine novel compounds. The structures of all the newly synthesized chrysin derivatives were elucidated by ESI-MS, NMR and IR3. The non-covalent interactions are studied between lysozyme and different phosphorous derivatives of chrysin by means of ESI-MS. The results indicate that the phosphorous derivatives of chrysin possess relatively stronger affinities and form non-covalent complexes with the lysozyme more easily than the unphosphorylated compounds. However, the non-covalent interactions between lysozyme and chrysin modified phosphoryl amino acids are more stronger than the non-covalent interactions between lysozyme and phosphoryl chrysin.
|
PDF Full Text Request