Appraisal of the antichemotactic activity of flavonoids on polymorphonuclear neutrophils.
Flavonoids are polyphenols that are ubiquitous in plants and frequently consumed in the diet. They are suggested to have many beneficial actions on human health, including anti-inflammatory activity. Their properties have been studied in a number of cell types, but little is known about their effects on neutrophil biology. Consequently, we selected 25 flavonoids with different structural features to evaluate their in vitro inhibition of rat polymorphonuclear neutrophil (PMN) chemotaxis, employing a modified Boyden chamber. Migratory activity was measured towards a chemotactic stimulant, formyl-Met-Leu-Phe or lipopolysaccharide. Furthermore, the cytotoxic effect of flavonoids on PMNs was determined by the release of cytosolic lactate dehydrogenase (LDH). Ten flavonoids significantly retarded the migration of PMNs with at least one of the concentrations tested in a range between 0.625 and 100 µM; the best antichemotactic agents were flavone, flavonol, quercetin and rutin. None of the flavanones evaluated presented any significant inhibition of migration in this assay. Our findings indicated that non-hydroxylated flavones possess a better antichemotactic activity when compared to flavones with hydroxy groups. The presence of a sugar moiety in rutin did not produce any increase in this effect, when compared to the respective aglycone analogue. Finally, none of the flavonoids exhibited cell toxicity and for many of these flavonoids this is the first report of the inhibition of PMN chemotaxis.
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Edna Sayuri
ES
Suyenaga
Eduardo Luis
EL
Konrath
Roger Remy
RR
Dresch
Miriam Anders
MA
Apel
José Angelo
JA
Zuanazzi
Célia Gervásio
CG
Chaves
Amélia Teresinha
AT
Henriques
D036921:Achyrocline / Q000737:chemistry; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D002464:Cell Migration Inhibition / Q000187:drug effects; D002630:Chemotactic Factors / Q000037:antagonists & inhibitors / Q000494:pharmacology; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D003603:Cytotoxins / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects* / Q000276:immunology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D000893:Anti-Inflammatory Agents; D002630:Chemotactic Factors; D003603:Cytotoxins; D005419:Flavonoids; D008070:Lipopolysaccharides; D010936:Plant Extracts; D009240:N-Formylmethionine Leucyl-Phenylalanine