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Further evidence on the intramolecular lactonization in rat liver microsomal metabolism of 12-O-Acetylated retronecine-Type pyrrolizidine alkaloids

机译:关于大鼠肝脏微粒体代谢12-O-乙酰化的反硝化型吡咯并立核生物碱分子内内酯化的进一步证据

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摘要

We have previously found evidence of intramolecular lactonization in rat liver microsomal metabolism of isoline, a 12-O-acetylated pyrrolizidine alkaloid. In this study, the metabolism of another 12-O-acetylated pyrrolizidine alkaloid, acetylduciformine, by the proposed transformation pathway was investigated under the same incubation conditions. Two deacetylated metabolites from acetylduciformine were isolated and purified by chromatographic methods, and further characterized based on their physical properties and spectral data. One metabolite (lankongensisine A) was the lactone of another one (duciformine). Both compounds were first obtained as hydrolyzed metabolites from acetylduciformine by rat liver microsomes. More importantly, the present study provided further evidence for the intramolecular lactonization in the microsomal metabolism of 12-O-acetylated retronecine-type PAs.
机译:我们以前已经发现在大鼠肝微粒体代谢的异族化合物(一种12-O-乙酰化吡咯烷核生物碱)中分子内内酯化的证据。在这项研究中,在相同的温育条件下,通过拟议的转化途径研究了另一种12-O-乙酰化的吡咯烷核生物碱乙酰基二甲双胍的代谢。通过色谱法分离和纯化了乙酰基二甲双胍中的两种脱乙酰基代谢物,并根据其物理性质和光谱数据对其进行了进一步表征。一种代谢物(lankongensisine A)是另一种代谢物(duciformine)的内酯。两种化合物都是由大鼠肝脏微粒体从乙酰基二甲双胍中水解得到的代谢产物。更重要的是,本研究为12-O-乙酰化逆转录酶型PA的微粒体代谢中的分子内内酯化提供了进一步的证据。

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