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[多烯抗生素的失活机制。左菌素失活过程中功能成分的变化]

[Inactivation mechanism of polyene antibiotics. The change in the functional component of levorin during inactivation].

作者信息

Bronov L V, Kroshilova T M, Komarov E V, Krunchak V G

出版信息

Antibiotiki. 1980 Aug;25(8):566-71.

PMID:7406467
Abstract

The inactivation process of levorin, a polyenic antibiotic was studied in the presence of oxygen. It was found that the biological activity did not sufficiently correlate with the optical density of the antibiotic solution. This indicates that destruction of the double bonds was not the only process resulting in the biological activity loss. In this connection methods for qualitative determination of the levorin main functional groups, i.e. aromatic and aliphatic amines and carbonyl groups were developed. The methods were used for the control of the changes in these functional groups on levorin inactivation. It was found that the inactivation level was directly proportional to the amount of the oxygen absorbed, 1 molecule of oxygen being required for inactivation of 2 levorin molecules. The number of the carbonyl groups and aromatic amines did not change during the inactivation process. In the first stages of inactivation the biological activity was directly proportional to the level of amino sugars. If the heptaen chromophore is not absorbed, 3 double bonds remain in inactivated levorin.

摘要

在有氧条件下研究了多烯抗生素左菌素的失活过程。发现其生物活性与抗生素溶液的光密度没有充分的相关性。这表明双键的破坏并非导致生物活性丧失的唯一过程。就此而言,开发了定性测定左菌素主要官能团(即芳香胺、脂肪胺和羰基)的方法。这些方法用于控制左菌素失活过程中这些官能团的变化。发现失活水平与吸收的氧量成正比,2个左菌素分子失活需要1个氧分子。失活过程中羰基和芳香胺的数量没有变化。在失活的初始阶段,生物活性与氨基糖水平成正比。如果七烯发色团未被吸收,失活的左菌素中会保留3个双键。

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