Quercetin-Loaded Microcapsules Ameliorate Experimental Colitis in Mice by Anti-inflammatory and Antioxidant Mechanisms

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• 作者：Carla F. S. Guazelli ; Victor Fattori ; Barbara B. Colombo ; Sandra R. Georgetti ; Fabiana T. M. C. Vicentini ; Rubia Casagrande ; Marcela M. Baracat ; Waldiceu A. Verri ; Jr.
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：February 22, 2013
• 年：2013
• 卷：76
• 期：2
• 页码：200-208
• 全文大小：488K
• 年卷期：v.76,no.2(February 22, 2013)
• ISSN：1520-6025

文摘

Quercetin (1) is an anti-inflammatory and antioxidant flavonoid. However, the oral administration of 1 did not lead to beneficial effects in experimental animal colitis models, which involve cytokines and oxidative stress. A possible explanation is that the absorption profile of 1 prevents its activity. Therefore, it was reasoned that the controlled release of 1 would improve its therapeutic effect. Thus, the therapeutic effect and mechanisms of 1-loaded microcapsules in acetic acid-induced colitis in mice were evaluated. Microcapsules were prepared using pectin/casein polymer and 1. The oral administration of 1-loaded microcapsules decreased neutrophil recruitment, attenuated histological alterations, and reduced macroscopical damage, edema, and IL-1尾 and IL-33 production in the colon samples. Microcapsules loaded with 1 also prevented the reduction of anti-inflammatory cytokine IL-10 and the antioxidant capacity of the colon. These preclinical data indicate that pectin/casein polymer microcapsules loaded with 1 improved the anti-inflammatory and antioxidant effects of 1 compared to the nonencapsulated drug. Therefore, quercetin seems to be a promising active molecule in inflammatory bowel disease if provided with adequate controlled release.