Saquinavir-NO Inhibits IL-6 Production in Macrophages
2014
Аутори:
Momčilović, MiljanaMangano, Katia
Jevtić, Bojan
Mammana, Santa
Stošić-Grujičić, Stanislava
Nicoletti, Ferdinando
Miljković, Đorđe
Тип документа:
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт:
Covalent attachment of the nitric oxide (NO) moiety to the HIV protease
inhibitor Saquinavir (Saq) produced a new chemical entity, named
Saquinavir-NO, (Saq-NO) with reduced toxicity and potent
immunoregulatory influence on T lymphocytes. In this study, we have
compared head-to-head the effects of Saq-NO and Saq on mouse and rat
peritoneal macrophage cytokine secretion and NO production upon in
vitro, ex vivo and in vivo conditions. The results demonstrate that
Saq-NO, but not Saq, potently decreased interleukin (IL)-10, IL-6 and
nitrite accumulation and increased the levels of IL-1 and tumour
necrosis factor (TNF) in supernatants of mouse and rat macrophage
cultures in vitro. Treatment of mice with Saq-NO, but not Saq, inhibited
ex vivo secretion of IL-6 from macrophages. Consistent with these
findings, Saq-NO also reduced blood levels of IL-6 in
lipopolysaccharide-treated mice. The observed inhibitory influence of
Saq-NO on IL-6 generation in macrophages may be involved in the observed
antitumour and immunomodulatory effects of the drug.
Извор:
Basic & Clinical Pharmacology & Toxicology, 2014, 115, 6, 499-506
DOI: 10.1111/bcpt.12268
ISSN: 1742-7843