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首页> 外文期刊>Natural product communications >Possible Role of Fat Tissue in the Pharmacokinetics of Dodeca-2E,-4E,8Z,10E/Z,10E/Z-tetraenoic Acid Isobutylamides after Oral Administration of Echinacea angustifolia Extract in Rats
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Possible Role of Fat Tissue in the Pharmacokinetics of Dodeca-2E,-4E,8Z,10E/Z,10E/Z-tetraenoic Acid Isobutylamides after Oral Administration of Echinacea angustifolia Extract in Rats

机译:口服紫锥菊提取物在大鼠中Dodeca-2E,-4E,8Z,10E / Z,10E / Z-丁烯酸异丁酰胺的药代动力学中脂肪组织的可能作用

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摘要

Alkamides are one of the most important constituents of lipophilic extracts of Echinacea angustifolia roots. These compounds play an important role in the versatile pharmacological actions of this plant. The present study aimed to compare the concentrations of isomeric dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides (DTAI) in brain and periepididymal fat tissues and blood plasma of rats. Thirty, 60, 240 and 720 min after the oral administration of E. angustifolia root extract, tissue and plasma concentrations were determined by reversed-phase HPLC with ESI-MS/MS detection. The calculated terminal t_(1/2) of the mixture of DTAI was 8.28 h, which indicates a relatively slow elimination. In the 0.5-4 h period the brain/plasma and fat/plasma concentration ratios were continuously above 3 and 18, respectively, followed by equilibrium at 12 h. Our results indicate substantial accumulation of alkamides in lipid-rich tissues, which presumably contributes to a maintained pharmacological action.
机译:链烷酰胺是松果紫锥菊根的亲脂性提取物中最重要的成分之一。这些化合物在该植物的多种药理作用中起重要作用。本研究旨在比较大鼠脑和上皮周围脂肪组织和血浆中同分异构体dodeca-2E,4E,8Z,10E / Z-丁烯酸异丁酰胺(DTAI)的浓度。口服给予马尾草根提取物后第30、60、240和720分钟,采用ESI-MS / MS检测的反相HPLC测定组织和血浆浓度。 DTAI混合物的最终末端t_(1/2)为8.28 h,表明清除速度相对较慢。在0.5-4小时内,脑/血浆和脂肪/血浆的浓度比分别连续高于3和18,然后在12小时达到平衡。我们的结果表明,在富含脂质的组织中大量积累了酰胺,这可能有助于维持药理作用。

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