Study On Alkaloid Composition Of Ripples Litsea Glutinosa And Its Regulation Of Glucose Metabolism Activity

Objective:The purpose of this paper is to obtain the main active components of Litsea glutinosa as aporphine alkaloids in the early stage,to deeply isolate such alkaloids in the effective site,and to evaluate their hypoglycemic effect,and to elucidate the composition and structure-activity relationship of Litsea glutinosa aporphine alkaloid anti-diabetic active ingredient.By evaluating the effects of laurolitsine on the overall epigenetic,blood glucose,insulin tolerance,glucose tolerance of ob/ob diabetic mice,the anti-diabetic effects of the main active ingredient,laurolitsine,were investigated.Methods:1.Using 95% ethanol to extract Litsea glutinosa roots under reflux,then the extract was dissolved with acid water.Chloroform extraction was used to remove the fat-soluble components,and the total alkaloids were further extracted by ethyl acetate in alkali water and later.The separation methods of alkaloids were systematically separated by silica gel column chromatography,gel column chromatography and preparation of high performance liquid chromatography(HPLC).The structure of the compounds was identified according to their physicochemical properties and spectral data,including NMR spectroscopy(NMR),mass spectrometry(MS)and ultraviolet spectroscopy(UV).2.In vitro(HepG2)cell grape consumption model was used to evaluate the hypoglycemic activity of the alkaloids and to analyze the relationship between structure and activity.3.Ob / ob mice were orally administered with laurolitsine(50100 and 200 mg / kg)for 4 weeks.Measure its blood sugar,blood lipid and other biochemical indicators,evaluate its anti-diabetic efficacy.Results:1.17 alkaloids were identified from the root skin of Litsea glutinosa: Litsine A(1),Litsine B(2),Litsine C(3),Glutinosine A(4),Litsine D(5),N-methylcoclaurine N-oxide(6),(E)-N-Formyllaurolitsine(7),(Z)-N-Formyllaurolitsine(8),Thalifoline(9),pharmaceutical alkali(10),Maculosidine(11),evolitrine(12),Pteleine(13),Bohr alkali(14),laurolitsine(15),N-trans-ferulic casein(16),N-trans-mustard amide(17).These include 10 aporphine alkaloids,compounds 1-4 are new compounds,and compounds 5-9,11,12,13 are isolated from the Litsea glutinosa for the first time.2.In vitro(HepG-2)cell grape consumption model was used to evaluate the hypoglycemic activity of the alkaloids.It was found that compounds 1,3,14,15 had a significant effect on glucose consumption.3.Laurolitsine can reduce body weight and fat weight without reducing the average food intake;laurolitsine can significantly reduce the serum levels of fasting blood glucose,glycosylated hemoglobin(HbAlc)and glycosylated serum protein(GSP),and the laurolitsine can also reduce dyslipidemia,improve liver fat degeneration,Increase the activity of serum lipase and relieve inflammation.Conclusions:1.A total of 17 alkaloids were found,including 4 new compounds,and 8 compounds were first isolated from the root bark of Litsea glutinosa,which enriched the chemical composition of the Litsea glutinosa.2.Using the cell model in vitro,it was found that alkaloids showed hypoglycemic effects.3.Laurolitsine has anti-diabetic effect.