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The Metabolism of Salidroside to Its Aglycone p-Tyrosol in Rats following the Administration of Salidroside

机译:红景天苷给药后大鼠中红景天苷的代谢及其苷元对酪氨醇。

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摘要

Salidroside is one of the major phenolic glycosides in Rhodiola, which has been reported to possess various biological activities. In the present study the in vivo deglycosylation metabolism of salidroside was investigated and its aglycone p-tyrosol but not the original salidroside was identified as the main form in rat tissues following the administration of salidroside. After the i.v. administration of salidroside at a dose of 50 mg/kg in rats, salidroside was quantified only in the liver, kidney and heart tissues. The highest level of p-tyrosol was detected in the heart, followed by the spleen, kidney, liver and lungs, in order. Salidroside was detected only in the liver, in contrast, p-tyrosol was detectable in most tissues except the brain, and the kidney tissues contained a significant amount of p-tyrosol compared to the other tissues after the i.g. administration of 100 mg/kg salidroside. The excretion behaviour revealed that the administrated salidroside mainly eliminated in the form of salidroside but not its aglycone metabolite p-tyrosol through urine. After i.v. and i.g. administration in rats, 64.00% and 23.80% of the total dose was excreted through urine in the form of salidroside, respectively. In addition, 0.19% and 2.25% of the dose was excreted in the form of p-tyrosol through urine after i.v. and i.g. administration, respectively. The faecal salidroside and p-tyrosol concentrations were 0.3% and 1.48% of the total dose after i.v. administration, respectively. After the i.g. administration of salidroside, trace salidroside and p-tyrosol were quantified in faeces within 72 h. In addition, the biliary excretion levels of salidroside after i.v. and i.g. administration were 2.86% and 0.02% of the dose, respectively. The obtained results show that salidroside was extensively metabolised to its aglycone p-tyrosol and distributed to various organs and the orginal salidroside was cleared rapidly through urine following the administration of salidroside.
机译:红景天苷是红景天中主要的酚类糖苷之一,据报道具有多种生物活性。在本研究中,对红景天苷的体内去糖基化代谢进行了研究,并且在施用红景天苷后,其糖苷配基对酪氨醇而不是原始的红景天苷被鉴定为大鼠组织中的主要形式。在i.v.之后在大鼠中以50 mg / kg的剂量给予红景天苷时,仅在肝脏,肾脏和心脏组织中对红景天苷进行了定量。在心脏中检测到最高水平的对-酪醇,依次是脾脏,肾脏,肝脏和肺脏。相比之下,仅在肝脏中检出了红景天苷,而在除脑外的大多数组织中均检出了对酪氨醇,与之相比,肾脏组织中与其他组织相比,肾脏组织中含有大量的对酪醇。给予100 mg / kg红景天苷。排泄行为表明,施用的红景天苷主要以红景天苷的形式消除,但不能通过尿液清除其糖苷代谢物对酪氨酸。在i.v.之后和例如在大鼠中,总剂量的64.00%和23.80%分别以红景天苷的形式通过尿液排泄。另外,静脉内注射后,0.19%和2.25%的剂量以对-酪醇的形式通过尿排泄。和例如行政管理。静脉注射后粪便中红景天苷和对-酪醇的浓度分别为总剂量的0.3%和1.48%。行政管理。在之后在72小时内对粪便中的红景天苷,微量红景天苷和对-酪醇进行定量。另外,静脉输注红景天苷的胆汁排泄水平。和例如分别为剂量的2.86%和0.02%。获得的结果表明,红景天苷在被红景天苷给药后被广泛地代谢成其糖苷配基对酪氨醇并分布到各个器官,并且通过尿液快速清除了原始的红景天苷。

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