Synthesis Of ?3',?8-apigenin Biflavone And Inhibitory Activity Evaluation As ?-glucosid As Einhibitors

Flavonoid,bearing a 2-phenyl substituted chromone scaffold,is widely existed in plant.Biflavonoid is a kind of flavonoids,which is made up of 2 flavone molecules or their derivatives.Biflavonoid has extensive pharmacological activities such as antitumor,anti-inflammatory,antibacterial,antiviral and hypoglycemic activities.At present,natural flavonoids are mainly extracted from plants.However,the abundance of some flavonoids in plants is low which limited its further application as medicine or health care products.In this thesis,we designed a simple and efficient synthetic route to prepare a series of natural 13',118-biapigenin type flavonoids and their derivatives.We synthesized Amentoflavone,Podocarpusflavone A,Ginkgetin,Sotetsuflavone,Putraflavone B,Isoginkgotin,Bilobetin,Sciadopitysin and the protection of methyl amentoflavone from 2,4,6-trihydroxyacetophenone by regio-selective iodiniation,aldol condensation,oxidative cyclization,Suzuki coupling and selective deprotection reaction.It is worthy to mention that,Podocarpusflavone A,Sotetsuflavone,Putraflavone B and Sciadopitysin have been synthesized for the first time.Then a-glucosidase inhibition activity of Apigenin,Amentoflavone,Podocarpusflavone A,Ginkgetin,Sotetsuflavone,Putraflavone B,Bilobetin and the protection of methyl amentoflavone was tested.The result showed that,their inhibitory rate was 18.7±7.8,94.6±2.14,82.7±5.0,104.0±6.7,72.3±5.1,84.1±2.2,14.9±6.3,83.9±0.3 under 10?mol respectively.Further test showed that the inhibitory rate of Amentoflavone,Podocarpusflavone A and Ginkgetin was 3.8±5.4,33.1 ±4.0,25.7±4.7,26.6±0.7,12.1 ± 1.2,21.9±1.7,20.7±2.8,43.1±9.4 under 1?mol.Hence,all of these biflavonoids showed good a-glucosidase inhibition activity and Podocarpusflavone A showed the best inhibition activity among them.