- Anti-inflammatory effect of caffeic acid methyl ester and its mode of action through the inhibition of prostaglandin E2, nitric oxide and tumor necrosis factor-alpha production.
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The anti-inflammatory effects of caffeic acid (CA), caffeic acid methyl ester (CM) and di-O-acetylcaffeic acid (DAC) were investigated in rats using the carrageenin-induced edema model and the antinociceptive effects of these compounds were also assessed in mice by means of the acetic acid-induced abdominal constriction test and hot plate test. CM (10mg/kg, p.o.) showed the most potent anti-inflammatory and antinociceptive effects in these animal models. To investigate the mechanism of the anti-inflammatory action, we examined the effects of these compounds on the lipopolysaccharide (LPS)-induced NO and PGE2 responses in the murine macrophage cell line, RAW 264.7. Our data indicate that CM is the most potent inhibitor of NO and PGE2 production and it also significantly decreased tumor necrosis factor-alpha (TNF-alpha) release. Consistent with these observations, the protein and mRNA expression levels of iNOS and COX-2 were found to be inhibited by CM in a dose-dependent manner. Furthermore, CM inhibited the nuclear factor-kappaB (NF-kappaB) activation induced by LPS, which was associated with the prevention of the degradation of the inhibitor kappaB, and subsequently with decreased p65 protein levels in the nucleus. Taken together, our data indicate that the anti-inflammatory properties of CM might result from the inhibition of iNOS, COX-2 and TNF-alpha expression through the down-regulation of NF-kappaB binding activity.
- Richardson, Katherine A.,Vega, Tanya P.,Richardson, Frank C.,Moore, Chad L.,Rohloff, John C.,Tomkinson, Blake,Bendele, Raymond A.,Kuchta, Robert D.
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- Synthesis of 4'-thio-β-D-arabinofuranosylcytosine (4'-thio-ara-C) and comparison of its anticancer activity with that of ara-C
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4'-thio-β-D-arabinofuranosylcytosine was synthesized by a facile route in high yields. It was evaluated for antitumor activity against a panel of human tumors, both in vitro and in vivo.
- Tiwari, Kamal N.,Shortnacy-Fowler, Anita T.,Cappellacci, Loredana,Parker, William B.,Waud, William R.,Montgomery, John A.,Secrist III, John A.
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- Preparation of thioarabinofuranosyl compounds and use thereof
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Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells,
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