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替考拉宁,源自游动放线菌新种(Actinoplanes teichomyceticus nov. sp. VI)的抗生素。VI. 化学降解:酸水解产物的物理化学和生物学特性

Teicoplanin, antibiotics from Actinoplanes teichomyceticus nov. sp. VI. Chemical degradation: physico-chemical and biological properties of acid hydrolysis products.

作者信息

Malabarba A, Strazzolini P, Depaoli A, Landi M, Berti M, Cavalleri B

出版信息

J Antibiot (Tokyo). 1984 Sep;37(9):988-99. doi: 10.7164/antibiotics.37.988.

Abstract

Teicoplanin is an antibiotic complex consisting of five closely related factors, T-A2-1, 2, 3, 4 and 5 and a more polar factor, T-A3-1. By controlled acid hydrolysis the complex is transformed into pseudoaglycones and finally into a single aglycone with consecutive removal of three sugar units. Quantitative determination of sugars obtained by degradative reactions and NMR/LC-MS studies on suitable derivatives confirmed that all the components carry one N-acyl-D-glucosamine and that at least two of them are characterized by N-decanoyl and N-undecanoyl chains on the D-glucosamine unit. The hydrolysis products still possess in vitro and in vivo activity.

摘要

替考拉宁是一种由五个密切相关的因子(T-A2-1、2、3、4和5)以及一个极性更强的因子(T-A3-1)组成的抗生素复合物。通过控制酸水解,该复合物转化为假苷元,最终转化为单个苷元,同时连续去除三个糖单元。对降解反应得到的糖进行定量测定,并对合适的衍生物进行核磁共振/液相色谱-质谱研究,证实所有组分都带有一个N-酰基-D-葡萄糖胺,并且其中至少两个组分的特征是在D-葡萄糖胺单元上带有N-癸酰基和N-十一酰基链。水解产物仍具有体外和体内活性。

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