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白藜芦醇口服给药对脂多糖诱导的全身炎症反应无效。

Lack of effect of oral administration of resveratrol in LPS-induced systemic inflammation.

机构信息

Department of Food Science and Technology, Research Group on Quality, Safety and Bioactivity of Plant Foods, CEBAS-CSIC, Campus de Espinardo, 30100, Murcia, Spain.

出版信息

Eur J Nutr. 2011 Dec;50(8):673-80. doi: 10.1007/s00394-011-0178-3. Epub 2011 Mar 4.

Abstract

PURPOSE

The high mortality index due to sepsis and the lack of an effective treatment requires the search for new compounds that can serve as therapy for this disease. Resveratrol, a well-known anti-inflammatory natural compound, might be a good candidate for the treatment of sepsis. The aim of this work was to study the effects of oral administration of resveratrol, before and after sepsis initiation, on inflammation markers in a murine model of endotoxin-induced sepsis.

METHODS

Sprague-Dawley male rats were treated with resveratrol the 3 days prior to LPS administration and 45 min later. Hematological parameters, TNF-α, IL-1β and CINC-1, FRAP and TBARS levels were determined. Resveratrol and resveratrol-derived metabolites profile in plasma was compared after oral and intraperitoneal administration.

RESULTS

Oral treatment with resveratrol had no apparent systemic protective effects. However, resveratrol reduced the levels of lipid peroxidation in the small intestine and colon. Importantly, the administration of LPS caused a decrease in resveratrol absorption. When resveratrol bioavailability after i.p. administration was compared to that observed after oral administration, a different profile of resveratrol metabolites was found in plasma.

CONCLUSION

These results highlight the importance of studying the bioavailability of the assayed compounds in the experimental models used to be able to choose the best route of administration depending on the target organ and to determine which compounds or derived metabolites are effective treating the studied disease.

摘要

目的

由于败血症的高死亡率和缺乏有效治疗方法,需要寻找新的化合物作为这种疾病的治疗方法。白藜芦醇是一种众所周知的抗炎天然化合物,可能是治疗败血症的一个很好的候选药物。本工作的目的是研究在脂多糖诱导的败血症的小鼠模型中,在败血症开始前和开始后口服白藜芦醇对炎症标志物的影响。

方法

雄性 Sprague-Dawley 大鼠在给予 LPS 前 3 天和给予 LPS 后 45 分钟给予白藜芦醇治疗。测定血液学参数、TNF-α、IL-1β和 CINC-1、FRAP 和 TBARS 水平。比较口服和腹腔内给予后血浆中白藜芦醇和白藜芦醇衍生代谢物的谱。

结果

口服白藜芦醇治疗没有明显的全身保护作用。然而,白藜芦醇降低了小肠和结肠的脂质过氧化水平。重要的是,LPS 的给予导致白藜芦醇的吸收减少。当比较 i.p. 给予后白藜芦醇的生物利用度与口服后观察到的生物利用度时,在血浆中发现了不同的白藜芦醇代谢物谱。

结论

这些结果强调了在用于选择最佳给药途径的实验模型中研究所测定化合物的生物利用度的重要性,这取决于靶器官,并确定哪些化合物或衍生代谢物对所研究的疾病有效。

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