首页> 外文期刊>Life sciences >Orally administered rosmarinic acid is present as the conjugated and/or methylated forms in plasma, and is degraded and metabolized to conjugated forms of caffeic acid, ferulic acid and m-coumaric acid.
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Orally administered rosmarinic acid is present as the conjugated and/or methylated forms in plasma, and is degraded and metabolized to conjugated forms of caffeic acid, ferulic acid and m-coumaric acid.

机译:口服迷迭香酸在血浆中以结合和/或甲基化形式存在,并被降解并代谢为咖啡酸,阿魏酸和间香豆酸的结合形式。

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Rosmarinic acid (RA) is contained in various Lamiaceae herbs used commonly as culinary herbs. Although RA has various potent physiological actions, little is known on its bioavailability. We therefore investigated the absorption and metabolism of orally administered RA in rats. After being deprived of food for 12 h, RA (50 mg/kg body weight) or deionized water was administered orally to rats. Blood samples were collected from a cannula inserted in the femoral artery before and at designated time intervals after administration of RA. Urine excreted within 0 to 8 h and 8 to 18 h post-administration was also collected. RA and its related metabolites in plasma and urine were measured by LC-MS after treatment with sulfatase and/or beta-glucuronidase. RA, mono-methylated RA (methyl-RA) and m-coumaric acid (COA) were detected in plasma, with peak concentrations being reached at 0.5, 1 and 8 h after RA administration, respectively. RA, methyl-RA, caffeic acid (CAA), ferulic acid (FA) and COA were detected in urine after RA administration. These components in plasma and urine were present predominantly as conjugated forms such as glucuronide or sulfate. The percentage of the original oral dose of RA excreted in the urine within 18 h of administration as free and conjugated forms was 0.44 +/- 0.21% for RA, 1.60 +/- 0.74% for methyl-RA, 1.06 +/- 0.35% for CAA, 1.70 +/- 0.45% for FA and 0.67 +/- 0.29% for COA. Approximately 83% of the total amount of these metabolites was excreted in the period 8 to 18 h after RA administration. These results suggest that RA was absorbed and metabolized as conjugated and/or methylated forms, and that the majority of RA absorbed was degraded into conjugated and/or methylated forms of CAA, FA and COA before being excreted gradually in the urine.
机译:迷迭香科草药中含有迷迭香酸(RA),通常用作烹饪草药。尽管RA具有多种有效的生理作用,但对其生物利用度知之甚少。因此,我们研究了大鼠口服RA的吸收和代谢。禁食12小时后,对大鼠口服RA(50 mg / kg体重)或去离子水。在施用RA之前和之后,从插入股动脉的套管中收集血液样本。还收集在给药后0至8小时和8至18小时内排泄的尿液。用硫酸酯酶和/或β-葡糖醛酸糖苷酶处理后,通过LC-MS测定血浆和尿液中的RA及其相关代谢产物。在血浆中检测到RA,单甲基化RA(甲基-RA)和间香豆酸(COA),分别在施用RA后0.5、1和8 h达到峰值浓度。服用RA后尿液中检出了RA,甲基RA,咖啡酸(CAA),阿魏酸(FA)和COA。血浆和尿液中的这些成分主要以共轭形式存在,例如葡糖醛酸苷或硫酸盐。给药后18小时内以游离形式和结合形式从尿中排泄的RA最初口服剂量的百分数为:RA为0.44 +/- 0.21%,甲基-RA为1.60 +/- 0.74%,1.06 +/- 0.35%对于CAA,FA为1.70 +/- 0.45%,对于COA为0.67 +/- 0.29%。在RA给药后8到18小时内,这些代谢物总量的大约83%被排出了。这些结果表明,RA以结合和/或甲基化的形式被吸收和代谢,吸收的大部分RA被降解为CAA,FA和COA的结合和/或甲基化的形式,然后逐渐在尿中排泄。

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