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3',4',7-三-O-(β-羟乙基)芦丁糖苷和7-单-O-(β-羟乙基)芦丁糖苷在小鼠体内的处置与代谢

The disposition and metabolism of 3',4',7-tri-O-(beta-hydroxyethyl)rutoside and 7-mono-O-(beta-hydroxyethyl)rutoside in the mouse.

作者信息

Hackett A M, Griffiths L A

出版信息

Xenobiotica. 1977 Oct;7(10):641-51. doi: 10.3109/00498257709038686.

Abstract
  1. Following intravenous administration of 3',4',7-tri-O-(beta-hydroxy[14C2]ethyl)rutoside or 7-mono-O-(beta-hydroxy[14C2]ethyl)rutoside to male mice, 68% of the dose of each is excreted in faeces as the corresponding hydroxyethyl-quercetin within 72 h of dosage. Mean urinary excretions of mono- and tri-hydroxyethylrutosides in 72 h were 27 and 21% respectively. Unchanged rutosides and their glucuronides were detected in urine. 2. In biliary-cannulated animals, the mean biliary excretion of both tri- and mono-hydroxyethylrutosides was 71%, in 24 h of dosage. In both cases most 14C was excreted in 3 h, as unchanged rutosides and glucuronide conjugates. 3. Fall of blood 14C concn, was rapid for both compounds. Neither compound was detected in brain but there was short-term accumulation in liver and kidney, and 2--3 h after dosage, most 14C for both compounds was associated with the gastro-intestinal contents. 4. Animals killed 72 h after dosage of either compound contained less than 7% of dose, mostly in the colon and caecal contents. 5. Foetuses removed 3 h after dosage of either compound to the dams did not contain 14C; foetuses removed 5 min after dosage contained low levels of 14C, substantially below the maternal blood level and equiv. to less than 0-1% of dose in each case. No 14C was detected in amniotic fluid.
摘要
  1. 给雄性小鼠静脉注射3',4',7-三-O-(β-羟基[¹⁴C₂]乙基)芦丁或7-单-O-(β-羟基[¹⁴C₂]乙基)芦丁后,在给药后72小时内,每种药物剂量的68%以相应的羟乙基槲皮素形式经粪便排出。72小时内单-和三-羟乙基芦丁的平均尿排泄量分别为27%和21%。尿液中检测到未变化的芦丁及其葡萄糖醛酸苷。2. 在胆管插管动物中,给药24小时内三-和单-羟乙基芦丁的平均胆汁排泄量均为71%。在这两种情况下,大部分¹⁴C在3小时内以未变化的芦丁和葡萄糖醛酸苷结合物形式排出。3. 两种化合物的血液¹⁴C浓度下降都很快。在脑中均未检测到这两种化合物,但在肝脏和肾脏中有短期蓄积,给药后2 - 3小时,两种化合物的大部分¹⁴C与胃肠道内容物相关。4. 给予任一化合物后72小时处死的动物体内所含药物剂量不到7%,大部分在结肠和盲肠内容物中。5. 给母鼠给药后3小时取出的胎儿不含¹⁴C;给药后5分钟取出的胎儿含有低水平的¹⁴C,大大低于母血水平,每种情况下相当于剂量的不到0.1%。羊水内未检测到¹⁴C。

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