Punta Active Ingredient Structural Modification Of A Year

Erigeron annuus is whole plant with roots of Erigeron annuus(L).Pers of genus Erigeron, whole plant can be used as medicine, which has the effect of treatment of malaria, it is the main treatment of dyspepsia, enteritis, infectious hepatitis, lymphadenitis, hematuria and so on. Pyromeconic acid and erigeroside belong to the pyrone compounds, widely exist in the Erigeron plant, and have a significant increase in cerebral blood flow, improve blood circulation and reduce cerebral vascular resistance, increase blood-brain barrier permeability, increase nutrient return of myocardial function, also have to improve the body immune function of macrophages and a strong role in the inhibition of coagulation.The present research has conducted the research to the preparation method of pyromeconic acid, ultimately determine the amount of 5 times of 95% ethanol reflux and extract herbs three times, carry on the silica gel column separation to ethyl acetate extract and n-butanol extract as the best preparation, get pyromeconic acid accounted for 0.5% of the dry weight of herbs. The preparation method of pyromeconic acid with high yield, simple operation, low solvent consumption, saving time and so on.In this research, pyromeconic acid as the starting material, the 3,4,5 - trimethoxy cinnamic acid, ferulic acid, nicotinic acid and aspirin were prepared as acyl chloride respectively and carries on the esterification with pyromeconic acid, get four compounds, by ultraviolet spectrum(UV),mass spectrum (ESI-MS and ESI-TOF-MS) and nuclear magnetic resonance spectrum (1H-NMR, 13C-NMR, HMQC, HMBC) spectrum and other modern methods and techniques, identification of their structures, determine that they are the target compounds, after SCIFINDER inquiry, they are the new compounds.In this research, applied OSIRIS Property Explorer system to measure and calculate pyromeconic acid and four kinds of acid, and the active simulation of the four new compounds were measured and calculated. Assessment tips: four new compounds hopefully become the therapeutic drug. This study provides the basis for further pharmacology research, provides the guideline for further design the preparation of pyromeconic acid derivatives.