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拜氏小克银汉霉对普萘洛尔的代谢

Propranolol metabolism by Cunninghamella bainieri.

作者信息

Foster B C, Buttar H S, Qureshi S A, McGilveray I J

机构信息

Bureau of Drug Research, Sir Frederick Banting Research Centre, Ottawa, Ontario, Canada.

出版信息

Xenobiotica. 1989 May;19(5):539-46. doi: 10.3109/00498258909042293.

Abstract
  1. Incubations of racemic propranolol alone or in the presence of either quinidine or sparteine were performed with Cunninghamella bainieri. 2. Five mammalian metabolites of propranolol (4-hydroxypropranolol, desisopropyl-propranolol, 1-naphthoxylactic acid, propranolol glycol and 1-naphthoxyacetic acid) were present in unhydrolysed extracts of the incubation medium according to h.p.l.c. and g.l.c. analyses. The relative proportion of 4-hydroxypropranolol increased after enzymic treatment. 3. Propranolol not only had a fungistatic effect, but also caused morphological changes in the organism, which were accompanied by decomposition of 4-hydroxypropranolol and formation of a greenish-brown colour in the incubation medium. 4. Drug interaction experiments yielded results which paralleled those reported in mammals. 5. The findings indicate that C. bainieri may be a useful microbial model for drug disposition and interaction studies.
摘要
  1. 用拜氏小克银汉霉对消旋普萘洛尔单独孵育,或在奎尼丁或司巴丁存在的情况下进行孵育。2. 根据高效液相色谱法和气相色谱法分析,孵育培养基的未水解提取物中存在普萘洛尔的五种哺乳动物代谢产物(4-羟基普萘洛尔、去异丙基普萘洛尔、1-萘氧基乳酸、普萘洛尔二醇和1-萘氧基乙酸)。酶处理后,4-羟基普萘洛尔的相对比例增加。3. 普萘洛尔不仅具有抑菌作用,还会引起该生物体的形态变化,同时伴随着4-羟基普萘洛尔的分解以及孵育培养基中出现绿褐色。4. 药物相互作用实验的结果与在哺乳动物中报道的结果相似。5. 这些发现表明,拜氏小克银汉霉可能是药物处置和相互作用研究的有用微生物模型。

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