In vitro and in vivo inhibition of LPS-induced tumor necrosis factor-α production by dimeric gallotannin analogues
Designed dimeric gallotannin analogues featuring two tetragalloylglucopyranose cores connected by various hydrocarbon linkers inhibit tumor necrosis factor-α secretion from lipopolysaccharide-stimulated human peripheral blood mononuclear cells by up to 53% (5-24 μM concentration range) compared to control. Comparable suppression of tumor necrosis factor-α levels (~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-β stimulating activity. Copyright
Feldman, Ken S,Wilson, Sarah L,Lawlor, Michael D,Lang, Charles H,Scheuchenzuber, William J
Gallotannins and ellagitannins as regulators of cytokine release
A means and method for increasing or inhibiting the secretion of cytokines using gallotannins and ellagitannins is described. The preferred cytokine release inhibiting compounds are dimeric gallotannins having a linker molecule that misaligns the carbohydrate cores of the compounds. The preferred cytokine release promoting gallotannins and ellagitannins include a diaryl ether linker unit. In comparison to the more structurally complex ellagitannins, the compounds of this invention are structurally simpler, easier to synthesize, and more potent.
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(2010/11/28)
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