Abstract
Inflammatory bowel diseases (IBD) are at the top of the worldwide rankings for gastrointestinal diseases as regards occurrence, yet efficient and side-effect-free treatments are currently unavailable. In the current study, we proposed a new concept for anti-inflammatory treatment based on gold (III) complexes. A new gold (III) complex TGS 121 was designed and screened in the in vitro studies using a mouse macrophage cell line, RAW264.7, and in vivo, in the dextran sulphate sodium (DSS)-induced mouse model of colitis. Physicochemical studies showed that TGS 121 was highly water-soluble; it was stable in water, blood, and lymph, and impervious to sunlight. In lipopolysaccharide (LPS)-stimulated RAW264.7 cells, the complex showed a potent anti-inflammatory profile, as evidenced in neutral red uptake and Griess tests. In the DSS-induced mouse model of colitis, the complex administered in two doses (1.68 μg/kg, intragastrically, and 16.8 μg/kg, intragastrically, once daily) produced a significant (* p < 0.05) anti-inflammatory effect, as shown by macroscopic score. The mechanism of action of TGS 121 was related to the enzymatic and non-enzymatic antioxidant system; moreover, TGS 121 induced changes in the tight junction complexes expression in the intestinal wall. This is the first study proving that gold (III) complexes may have therapeutic potential in the treatment of IBD.
Highlights
The biomedical potential of gold has been discussed in numerous reports, concentrating both on its nanoparticle [1,2,3,4,5] and complex forms
Physicochemical studies showed that TGS 121 was highly water-soluble; it was stable in water, blood, and lymph, and impervious to sunlight
The in vitro studies consisted of a neutral red uptake (NRU) test to verify the cytotoxicity of the compound and a Griess test to assess the NO production
Summary
The biomedical potential of gold has been discussed in numerous reports, concentrating both on its nanoparticle [1,2,3,4,5] and complex forms. Marmol et al tested an alkynyl gold (I) complex on the colorectal adenocarcinoma Caco-2 cell line [12] This compound showed an anticancer activity, as it triggered necroptosis, which could provide a treatment option in cases of apoptosis resistance [12]. Gold (I)-coumarin-caffeine-based complexes were tested as potential anticancer and anti-inflammatory agents [13]. They showed antiproliferative properties on breast, prostate, and colon cancer cell lines. Auranofin, a gold(I)-containing compound registered as a drug against rheumatoid arthritis, has shown anticancer activity in animal models and is approved for clinical trials for lung and ovarian carcinoma [16]. We investigated the molecular mechanism of its action through modulation of antioxidant mechanisms and the influence on tight junction proteins
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