- DPPH radical scavenging activity of paracetamol analogues
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Biochemical studies suggest a direct relationship between the radical scavenging activity of paracetamol (I) and its antipyretic and analgesic action. To evaluate the effect of chemical modifications on the radical scavenging activity of compounds of type I, analogues 1-14 were prepared and submitted to a stable free radical (DPPH; 1,1-diphenyl-2-picryl-hydrazyl) assay. All paracetamol derivatives showed a significant higher efficiency than the parent compound. This study showed that radical scavenging activity can be increased by decreasing the phenolic ortho substituents steric hindrance or by introducing substituents on the acyl moiety like an indazole ring or the ionic N-methyl morpholinium group. A significant activating effect was also observed by replacing the 1,4-acylamidophenol with a 1,4-acylamidonaphthol system.
- Alisi, Maria Alessandra,Brufani, Mario,Cazzolla, Nicola,Ceccacci, Francesca,Dragone, Patrizia,Felici, Marco,Furlotti, Guido,Garofalo, Barbara,La Bella, Angela,Lanzalunga, Osvaldo,Leonelli, Francesca,Marini Bettolo, Rinaldo,Maugeri, Caterina,Migneco, Luisa Maria,Russo, Vincenzo
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p. 10180 - 10187
(2013/01/15)
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- Immunomodulating compositions for treatment of immune system disorders
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The present invention relates to a composition for use as an immunomodulator comprising small molecular weight components of less than 3000 daltons, and having the following properties: a) is extractable from bile of animals; b) is capable of stimulating monocytes and macrophages in vitro and in vivo; c) is capable of modulating tumor necrosis factor production; d) contains no measurable IL-1α, IL-1β, TNF, IL-6, IL-8, IL-4, GM-CSF or IFN-γ; e) has an anti-proliferative effect in a malignant mouse hybridoma cell line; f) shows no cytotoxicity to human peripheral blood mononuclear cells or lymphocytes; and g) is not an endotoxin. The invention also relates to a method of preparing the composition, its use as an immunomodulator, and its use in the treatment of diseases and conditions having an immunological component.
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