MADURAMICIN - RAT-METABOLISM OF A HIGHLY POTENT POLYETHER ANTICOCCIDIAL EXAMINED BY C-13 NMR

MADURAMICIN - RAT-METABOLISM OF A HIGHLY POTENT POLYETHER ANTICOCCIDIAL EXAMINED BY C-13 NMR
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DOI:
10.1021/jf00069a024
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发表时间:
1986-05-01
影响因子:
6.1
通讯作者:
RAJAN, S
RAJAN, S
中科院分区:
农林科学1区
文献类型:
--
作者:
BROWN, MA;RAJAN, S

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马杜霉素在农业上重要的聚醚离子载体抗生素中是独特的,因为它的结构含有糖部分。在饲料中以 5.2 ppm 的碳 14 标记的马杜霉素给药 1 周后,停药 0 天后,在大鼠肝组织中仅检测到母体化合物 (36%) 和单一代谢物 (64%)。 12 只大鼠单次口服 1 mg 剂量可提供 3 mg 纯代谢物。尽管这种物质与鸡肝中发现的主要代谢物(由不与糖部分相连的两个甲氧基进行O-去甲基化产生)不同,但质谱分析表明它是一种异构体。碳13核磁共振谱表明它是一种异构体。碳 13 NMR 光谱表明,它是主要鸡肉代谢物的异构体,其中糖部分选择性地发生 O-去甲基化。
Maduramicin is unique among the agriculturally important polyether ionophore antibiotics in that its structure contains a sugar moiety. Exclusively the parent compound (36%) and a single metabolite (64%) are detected in rat liver tissues at 0-day withdrawal after administering carbon-14-labeled maduramicin in feed at 5.2 ppm for 1 week. A single oral dose of 1 mg to 12 rats provided 3 mg of the metabolites in a pure form. Although this material was not the same as the major metabolite found in chicken liver (produced by the O-demethylation of one two methoxy groups not attached to the sugar moiety), mass spectroscopy shows that it is an isomer. Carbon-13 NMR spectroscopy shows that it is an isomer. Carbon-13 NMR spectroscopy shows that it is an isomer of the major chicken metabolite in which O-demethylation occurs selectively at the sugar moiety.