Immunopharmacology and immunotoxicology · 2026
The anti-inflammatory activity and toxicological safety of synthetic chalcone derivatives in preclinical trials.
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de Oliveira Paula G F, Lubschinski Tainá L, Fernandes Octavio L G, Tizziani Tiago, Buss Ziliani da S, Sandjo Louis P, Daltoé Felipe P, Dalmarco Eduardo M
Аннотация
BACKGROUND: Inflammation is an essential physiological defense mechanism that aims to maintain homeostasis. However, it can lead to chronic or autoimmune diseases. The chalcones structural flexibility represents a promising class for developing new drugs and exhibits diverse activities, including anti-inflammatory effects.
MATERIAL AND METHODS: To evaluate the cell viability and anti-inflammatory potential of 23 chalcone derivative compounds by measuring nitric oxide metabolites in a model of lipopolysaccharide-stimulated J774A.1 cells. After using the acute lung injury model in mice, the acute oral toxicity of compounds with favorable in vitro profiles was determined according to guideline 423 of the Organization for Economic Cooperation and Development.
RESULTS: Of the compounds tested in J774A.1 cells (n = 23) and seventeen showed acceptable results and were subjected to nitric oxide inhibition after lipopolysaccharide stimulation; two (RX10.2 and RX10.4) compounds showed significant inhibition under this inflammatory parameter. The compounds were then tested in vivo. RX10.4 failed to reproduce the in vitro anti-inflammatory effect. Nevertheless, RX10.2 demonstrated exciting performance, reducing the leukocyte migration on the bronchoalveolar lavage by limiting neutrophil influx and exudation levels. The compound also significantly reduced nitric oxide levels and myeloperoxidase activity. Lastly, RX10.2 did not show signs of acute oral toxicity.
CONCLUSIONS: RX10.2 showed important anti-inflammatory activity in vitro and in vivo without acute toxicity. This finding justifies further investigation, as it proved to be a promising prototype for developing new anti-inflammatory drugs.
MATERIAL AND METHODS: To evaluate the cell viability and anti-inflammatory potential of 23 chalcone derivative compounds by measuring nitric oxide metabolites in a model of lipopolysaccharide-stimulated J774A.1 cells. After using the acute lung injury model in mice, the acute oral toxicity of compounds with favorable in vitro profiles was determined according to guideline 423 of the Organization for Economic Cooperation and Development.
RESULTS: Of the compounds tested in J774A.1 cells (n = 23) and seventeen showed acceptable results and were subjected to nitric oxide inhibition after lipopolysaccharide stimulation; two (RX10.2 and RX10.4) compounds showed significant inhibition under this inflammatory parameter. The compounds were then tested in vivo. RX10.4 failed to reproduce the in vitro anti-inflammatory effect. Nevertheless, RX10.2 demonstrated exciting performance, reducing the leukocyte migration on the bronchoalveolar lavage by limiting neutrophil influx and exudation levels. The compound also significantly reduced nitric oxide levels and myeloperoxidase activity. Lastly, RX10.2 did not show signs of acute oral toxicity.
CONCLUSIONS: RX10.2 showed important anti-inflammatory activity in vitro and in vivo without acute toxicity. This finding justifies further investigation, as it proved to be a promising prototype for developing new anti-inflammatory drugs.