Return to search

Anti-inflammatory activity of electron-deficient organometallics

Yes / We report an evaluation of the cytotoxicity of a series of
electron-deficient (16-electron) half-sandwich precious metal
complexes of ruthenium, osmium and iridium ([Os/Ru(η6-pcymene)(
1,2-dicarba-closo-dodecarborane-1,2-dithiolato)] (1/2),
[Ir(η5-pentamethylcyclopentadiene)(1,2-dicarba-closo-dodecarborane-
1,2-dithiolato)] (3), [Os/Ru(η6-p-cymene)(benzene-1,
2-dithiolato)] (4/5) and [Ir(η5-pentamethylcyclopentadiene)
(benzene-1,2-dithiolato)] (6)) towards RAW 264.7 murine
macrophages and MRC-5 fibroblast cells. Complexes 3 and
6 were found to be non-cytotoxic. The anti-inflammatory
activity of 1–6 was evaluated in both cell lines after nitric
oxide (NO) production and inflammation response induced by
bacterial endotoxin lipopolysaccharide (LPS) as the stimulus.
All metal complexes were shown to exhibit dose-dependent
inhibitory effects on LPS-induced NO production on both cell
lines. Remarkably, the two iridium complexes 3 and 6 trigger
a full anti-inflammatory response against LPS-induced NO
production, which opens up new avenues for the development
of non-cytotoxic anti-inflammatory drug candidates with
distinct structures and solution chemistry from that of organic
drugs, and as such with potential novel mechanisms of action. / We thank the Royal Society (University Research Fellowship No. UF150295 to NPEB), and the University of Bradford for financial support.

Identiferoai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/13760
Date29 November 2017
CreatorsZhang, Jingwen, Pitto-Barry, Anaïs, Shang, Lijun, Barry, Nicolas P.E.
Source SetsBradford Scholars
LanguageEnglish
Detected LanguageEnglish
TypeArticle, Published version
Rights©2017 The Authors. Published by the Royal Society under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/, which permits unrestricted use, provided the original author and source are credited., ©2017 The Authors. Published by the Royal Society under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/, which permits unrestricted use, provided the original author and source are credited.

Page generated in 0.0017 seconds