In vitro and in vivo inhibition of LPS-induced tumor necrosis factor-alpha production by dimeric gallotannin analogues.
Designed dimeric gallotannin analogues featuring two tetragalloylglucopyranose cores connected by various hydrocarbon linkers inhibit tumor necrosis factor-alpha secretion from lipopolysaccharide-stimulated human peripheral blood mononuclear cells by up to 53% (5-24 microM concentration range) compared to control. Comparable suppression of tumor necrosis factor-alpha levels (approximately 50% vs control) was observed in the plasma of rats co-treated with lipopolysaccharide and specific tannin analogues selected for their lack of interleukin 1-beta stimulating activity.
Feldman
Ken S
KS
Department of Chemistry, The Pennsylvania State University, University Park, PA 16802, USA. kfs@chem.psu.edu
Wilson
Sarah L
SL
Lawlor
Michael D
MD
Lang
Charles H
CH
Scheuchenzuber
William J
WJ
D000818:Animals; D019281:Dimerization; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D047348:Hydrolyzable Tannins / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D008070:Lipopolysaccharides / Q000494:pharmacology*; D051381:Rats; D013057:Spectrum Analysis; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis*
D047348:Hydrolyzable Tannins; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha