Structure Modification Of Caffeic Acid And Active Research

It is a long history for using Blumea riparia(Bl.)DC at clinic in Guangxi.It has been used to treat rheumatoid arthritis and gynecological diseases,such as erosion of vulva,menorrhagia,infertility,postpartum bleeding,puerperal edema etc.Blumea riparia(Bl.)DC as a specialized plant is the only raw material of Guangxi famous Traditional Chinese Medicine "FUXUE KANG".It plays an important role in gynecological diseases,its chemical composition has been researched and applied.Cafifeic acid is one of the main ingredient of Blumea riparia(Bl.)DC.Sulfonamide as organic antimicrobial agent refers to a class of drugs that have the sulfanilamide structure.It has been used to prevent and treat bacterial infectious disease.The chemical structure of the sulfonamide is similar to para amlnobenzoic acid,so it can prevent the formation of dihydrofolate,and ultimately affect the synthesis of bacterial nucleoprotein to inhibit the breeding of bacteria.Sulfonamide has many davantanges,but with the discovery and application of a variety of antibiotics and synthetic antibacterial drugs,the bacteria have produced a wide range of drug tolerance and sulfonamide has many side effects.According to the structure and property of the Blumea riparia(Bl.)DC and sulfonamide,23 kinds of caffeic acid derivatives have been synthetized.The sulfonamides include SN,SD,SM2,SMD,SMM,SPDZ,SPZ,SQ-Na,SDM,ST,SMZ.Therefore,the synthesized products theoretically can play to the advantages of these two types of compounds,and show significant bacteriostasis and hemostatic effect,reducing the side effects of the metabolic process.The route of synthesis ultimately was determined after long-term exploration.According to the significant differences of chemical and physical properties of product and raw materials,pure target products were obtained after extraction,separation and crystallization.Comprehensive utilization of the IR,MS,IH-NMR,13C-NMR,elemental analysis and single crystal diffraction,the structure of 23 kinds of the target products was identified to be 16 kinds of new compounds and 5 kinds of new crystals.Activity determination of the products has been studied.MIC was obtained by bacteriostatic activity.PT,TT,APTT and FIB were obtained by hemostatic activity.The uterine tension and frequency were obtained by experiment on the mice in vitro.Through interaction with BSA,the type,structure,environment and distribution of the fluorescent protein molecules were realized to provide theoretical foundation for the pharmacological research.