Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives.

Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives. Research Abstract Details 

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Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives. Abstract Text:

Juri Takahashi,Takashi Sekine,Masayuki Nishishiro,Atsuhiro Arai,Hidetsugu Wakabayashi,Teruo Kurihara,Ken Hashimoto,Kazue Satoh,Noboru Motohashi,Hiroshi Sakagami,

The effect of 20 trihaloacetylazulene derivatives with one halogen atom, on nitric oxide (NO) production by mouse macrophage-like cells Raw 264.7 was investigated. 2-Methoxyazulenes and 2-ethoxyazulenes exhibited comparable cytotoxicity. Trichloroacetylazulenes generally exhibited higher cytotoxicity, as compared with the corresponding trifluoroacetylazulenes. Substitution of chloride, bromide or iodine at the C-3 position further enhanced their cytotoxicity. All of these compounds failed to stimulate the Raw 264.7 cells to produce detectable amounts of NO, but did inhibit NO production by LPS-activated Raw 264.7 cells to different extents. 1-Trichloroacetyl-2-methoxyazulene and 1-trichloroacetyl-2-ethoxyazulene, with less cytotoxic activity, inhibited NO production to the greatest extent, producing the highest selectivity index (SI) of >24.7 and >28.7, respectively. This was accompanied by the efficient inhibition of inducible NO synthase (iNOS) mRNA expression, but not by iNOS protein abundance. Electron spin resonance (ESR) spectroscopy showed that neither of these compounds produced radicals, nor scavenged NO, superoxide anion or diphenyl-2-picrylhydrazyl radicals. The present study suggests that the inhibitory effects of trifluoroacetylazulenes and trichloroacetylazulenes on NO production by activated macrophages might be derived from the perturbation of NO anabolism (inhibition of iNOS mRNA expression and possibly the inactivation of iNOS protein) rather than NO catabolism (NO scavenging).

Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives. Publishing Authors By Initials

J Takahashi,T Sekine,M Nishishiro,A Arai,H Wakabayashi,T Kurihara,K Hashimoto,K Satoh,N Motohashi,H Sakagami,

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Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Anticancer research

VOLUME: 28

Page Numbers: 171-8

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ISSN: 0250-7005

DAY: 3

MONTH: 04

YEAR: 2008

Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives. Information

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LANGUAGE: eng

NlmUniqueID: 8102988

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Grant and Affiliation Information for Inhibition of NO production in LPS-stimulated mouse macrophage-like cells by trihaloacetylazulene derivatives.

AFFILIATION: Faculty of Science, Josai University, Sakado, Saitama, Japan.

Country: Greece

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MEDLINETA: Anticancer Res

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