The Synthesis And Anti-Inflammation Activities Of The Derivatives Of Luteolin

Luteolin, 3', 4', 5, 7-tetrahydroxyflavone, a representative natural flavone, had anti-inflammation, anti-virus, anti-atherosclerosis and so on. To enhance the pharmaceutical activities, two series derivatives of luteolin, series I metallic complexes and series II 3', 4', 7-trichloro-5-hydroxyflavone and its Schiff bases, were designed and synthesized on the basis of the review of the pharmaceutical activities of flavonoids and luteolin.According to the concordance effect, which the biological activity of metallic complex was obviously stronger than the single component; sixteen series I compounds were synthesized by luteolin with metal ions. The characterization of the complexes by element analysis, FTIR and DSC analysis indicated their components and connection ways.Due to the strong and broad spectrum anti-bacterium and the solution acidity closing to physiological pH value, it was a luciferous perspective for Schiff bases as a medicine for anti-inflammation and anti-bacterium. Thus, six series II compounds of luteolin were synthesized and characterized by ~1H-NMR, FTIR and MS.The experiments of anti-inflammation activities in models of acute inflammation indicated that the series I derivatives of luteolin had obvious inhibition to xylene-induced ear edema in mice, in which BHQ-1, BHQ-2, BHQ-4, BHQ-5, BHQ-11, BHQ-14, BHQ-15 and BHQ-16 took on equivalently to dexamethasone(DXM) and carrageenin-induced paw edema in mice, in which BHQ-3 was equivalent to luteolin and DXM.