3604-79-3Relevant articles and documents
Interference of the polyphenol epicatechin with the biological chemistry of nitric oxide- and peroxynitrite-mediated reactions
Wippel, Ruediger,Rehn, Margit,Gorren, Antonius C.F.,Schmidt, Kurt,Mayer, Bernd
, p. 1285 - 1295 (2004)
The formation of reactive nitrogen species in mammalians has both beneficial and undesirable effects. Nitric oxide (NO) production in endothelial cells leads to vascular smooth muscle relaxation, but if reactive nitrogen species are generated in high amounts by cells under inflammatory conditions they are toxic. Flavonoids like (-)-epicatechin show an inverse association of their intake with diseases thought to be associated with overproduction of reactive nitrogen species. We found that the formation of cyclic GMP in cultured porcine aortic endothelial cells was not affected by up to 1mM (-)-epicatechin. Half maximal inhibition of interferon-γ/ lipopolysaccharide induced nitrite accumulation in murine macrophages required about 0.5mM of the flavonoid. In contrast, nitration of free tyrosine triggered by 0.1 and 1mM authentic peroxynitrite was inhibited by (-)-epicatechin with IC50 values of 6.6 and 28.0μM, respectively. The presence of 15mM sodium bicarbonate had no significant effect. Nitration of protein-bound tyrosine in phorbol 12-myristate 13-acetate treated HL-60 cells in the presence of nitrite was inhibited by (-)-epicatechin at a similar concentration range (IC50=10-100μM). Myeloperoxidase activity of phorbol 12-myristate 13-acetate stimulated HL-60 cells was inhibited by (-)-epicatechin with an IC50 value of 77.4μM. Epicatechin inhibited dihydrorhodamine oxidation by 50μM authentic peroxynitrite and 1mM 3-morpholino-sydnonimine with IC50 values of 11.8 and 0.63μM, respectively. Our data suggest that at up to 0.1mM (-)-epicatechin preferentially inhibits NO-related nitration and oxidation reactions without affecting NO synthesis and cyclic GMP signaling.
NOVEL MULTIMERIC CD40 LIGANDS, METHOD FOR PREPARING SAME AND USE THEREOF FOR PREPARING DRUGS
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, (2010/08/07)
The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H—Xa—Xb—Xc—Xd—Xe—(Xf)i—, wherein i represents 0 or 1, Xn is in particular selected among lysine, arginine, ornithine residues, Xb is in particular selected among glycine, asparagine, L-proline or D-proline residues, Xc et Xd are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe et Xf are in particular selected among the following amino acid residues: NH2—(CH2)n—COOH, n ranging from 1 to 10 or NH2—(CH2—CH2—O)m—CH2CH2COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr-Tyr146 fragment
Metalloporphyrin treatment of neurologic disease
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, (2008/06/13)
The present invention provides a method of treating amyotrophic lateral sclerosis and other neurologic diseases by administering a compound of the formula where R is selected from the group consisting of (C6H4)CO2H, (Csub
