Preparation And Bioactivity Of Three Medicinal And Food Functional Factors:The Tea Ketone,Biobiotin And Naringin Derivatives

Drug-food functional factors mainly exist in drug-food plants and have diversified functional activities.It is of great significance for the research and development of drugs,food preservatives and food antibacterial agents to carry out structural transformation of drug-food functional factors and carry out anti-tumor,anti-virus and bacteriostatic studies.Tea ketone is a natural product,which mainly exists in tea plants,and is an important intermediate for the synthesis of vitamin E,carotenoids and medicine.The study found that the active substances in tea have anti-new coronavirus activity,and indole oxide is an important antiviral and anti-tumor bioactive skeleton.The active skeleton oxido indole is spliced to the tea ketone skeleton in order to obtain the anti-new coronavirus function.Compounds;chickpea sprouts are mainly derived from beans and have pharmacological activities such as anti-inflammatory,antioxidant and anti-tumor,and the chromene skeleton has a wide range of biological activities.Good anti-tumor compound;naringenin is a flavonoid widely present in citrus fruits,and has medicinal activities such as anti-inflammatory,hypolipidemic and bacteriostatic,naringenin is prepared into naringenin derivatives,and bacteriostatic studies are carried out with a view to discovering compounds with better bacteriostatic activity.The main research contents of this paper are as follows:(1)Preparation and antiviral activity of tea ketone derivatives,a medicinal and food functional factorThe michael addition cyclization reaction between theophylone and indole oxide was performed,and 10 indole oxide compounds were obtained by theophylone splicing.In addition,molecular docking technology was used to screen the active components of indole oxidation compounds by means of chemical binding between specific targets and ligands.The results showed that novel coronavirus 3CL hydrolase and indole oxidation compounds 3e and 3h had better binding activity.In this part of the study,it was shown that theavanone derivatives 3e and 3h can be used as potential inhibitors of novel coronavirus 3CL hydrolase,providing theoretical basis for the development and application of anti-novel coronavirus drugs.(2)Preparation and antitumor activity of biochanin derivatives of medicinal and food functional factorsThe michael addition cyclization reaction between biochanin and malonitrile arolefin was performed,and nine biochanin chromoene splicing derivatives were obtained.MTT assay,AO/EB assay,Hoechst 33258 staining assay and colony formation analysis were used to study the anti-tumor activity of the congeners on A549 cells.The results showed that compound 6g could significantly inhibit the malignant proliferation of A549 cells.This part of the study showed that biobiotin had good anti-tumor activity,which provided compound sources and research ideas for the development of anti-tumor drugs from drug-food functional factors.(3)Preparation of naringenin derivatives of medicinal and food functional factors and their antibacterial activity,enzyme inhibitory activity and mechanism researchNaringenin and hydrated ninhydrin raw material column chromatography to obtain naringenin spliced hydrated ninhydrin derivative 9.The bacteriostatic effect was explored through the inhibition zone,MBC and MIC experiments.The results showed that naringenin derivative 9 had a good bacteriostatic and bactericidal effect on Staphylococcus aureus.Its inhibition zone size was 13.41 mm,its MIC value was0.3125 m M,and its MBC value was 1.25 m M.The results of combined antibacterial experiments: streptomycin and gentamicin showed additive effect on Staphylococcus aureus,and their FIC values were 0.625.Chloramphenicol also showed additive effect on Staphylococcus aureus,and their FIC values were 1.0.The rhodamine 123 experiment was used to explore the antibacterial mechanism: the addition of naringenin derivatives depolarized the cell membrane of Staphylococcus aureus,reducing the membrane potential,affecting the metabolic activity of the bacteria,thereby inhibiting its growth.The inhibitory activity of naringenin derivative 9 on tyrosinase,α-glucosidase and other enzymes was studied,and it was found that naringenin derivative 9 showed good enzyme inhibitory activity on tyrosinase andα-glucosidase.Its IC50 values were 0.312 μM and 0.2 m M,respectively.This part of the research has an important theoretical basis for the subsequent development of food preservatives,food bacteriostatic agents,and tyrosinase inhibitors.