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首页> 外文期刊>Xenobiotica: the fate of foreign compounds in biological systems >In vivo and in vitro pharmacokinetics and metabolism studies of 26,26,26,27,27,27-F6-1,25(OH)2 vitamin D3 (Falecalcitriol) in rat: induction of vitamin D3-24-hydroxylase (CYP24) responsible for 23S-hydroxylation in target tissues and the drop in seru
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In vivo and in vitro pharmacokinetics and metabolism studies of 26,26,26,27,27,27-F6-1,25(OH)2 vitamin D3 (Falecalcitriol) in rat: induction of vitamin D3-24-hydroxylase (CYP24) responsible for 23S-hydroxylation in target tissues and the drop in seru

机译：大鼠体内26,26,26,27,27,27-F6-1,25（OH）2维生素D3（Falecalcitriol）的体内和体外药代动力学和代谢研究：维生素D3-24-羟化酶（CYP24）的诱导负责靶组织中的23S-羟基化和血清的下降

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1. 26,26,26,27,27,27-F6,-1,25(OH)2 vitamin D3, Falecalcitriol, the hexafluorinated analogue of 1,25(OH)2 vitamin D3, has been reported to be several times more potent than the parent compound regarding some vitamin D actions. The reason for enhanced biological activity appears related to F6-1,25(OH)2 vitamin D3 metabolism to F6-1,23S,25(OH)3 vitamin D3, a bioactive 23S-hydroxylated form which is resistant to further metabolism. 2. In the present in vivo studies, the repeated oral administration of [3H]F6-1,25(OH)2 vitamin D3 to rat resulted in a significant reduction of the radioactivity and the F6-1,25(OH)2 vitamin D3 concentrations in serum, especially at the 2 h maximum point after each dosing. Additionally, F6-1,23S,25(OH)3 vitamin D3 in the serum and small intestine was increased by the prior administration of F6-1,25(OH)2 vitamin D3. 3. Further in vitro investigation showed [3H]F6-1,25(OH)2 vitamin D3 to be metabolized to F6-1,23S,25(OH)3 vitamin D3 by kidney and small intestine homogenates of rat, the reaction being increased by the prior administration of F6-1,25(OH)2 vitamin D3. Moreover, this latter treatment was associated with a marked increase of CYP24 mRNA in the small intestine within 4 h after dosing. 4. The results indicate that in vivo metabolism of F6-1,25(OH)2 vitamin D3 to F6-1,23S,25(OH)3 vitamin D3 is catalysed by CYP24, the enzyme being induced by prior substrate exposure.
机译：1. 26,26,26,27,27,27-F6，-1,25（OH）2维生素D3，Falecalcitriol，1,25（OH）2维生素D3的六氟类似物，据报道有好几次在某些维生素D的作用方面比母体化合物更有效。生物学活性增强的原因似乎与F6-1,25（OH）2维生素D3代谢与F6-1,23S，25（OH）3维生素D3代谢有关，F6-1,23S，25（OH）3维生素D3是一种具有生物活性的23S-羟基化形式，可抵抗进一步的代谢。 2.在目前的体内研究中，向大鼠反复口服[3H] F6-1,25（OH）2维生素D3导致放射性和F6-1,25（OH）2维生素显着降低血清中的D3浓度，尤其是每次给药后2小时的最高点。另外，通过预先施用F6-1,25（OH）2维生素D3可增加血清和小肠中的F6-1,23S，25（OH）3维生素D3。 3.进一步的体外研究表明，[3H] F6-1,25（OH）2维生素D3被肾脏和大鼠小肠匀浆代谢为F6-1,23S，25（OH）3维生素D3。事先服用F6-1,25（OH）2维生素D3可增加此外，后一种治疗与给药后4小时内小肠中CYP24 mRNA的显着增加有关。 4.结果表明，CYP24催化F6-1,25（OH）2维生素D3体内代谢为F6-1,23S，25（OH）3维生素D3，该酶由先前的底物暴露诱导。

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