Le Goffic F, Sicsic S, Vincent C
Biochimie. 1977;59(11-12):927-32.
In order to produce specifically N-monoalkylated derivatives of aminoglycoside antibiotics of potential therapeutic values, we have developed an enzymatic reactor. This system uses the aminoglycoside acetyltransferase as catalyst and acetylcoenzyme A as acetyl donor. The immobilization of one aminoglycoside acetyltransferase on different resins has been studied. The coreticulation of this enzyme on DEAE cellulose in the presence of glutaraldehyde gives rise to an enzymatic resin of high efficiency. On the other hand, we have also studied the acetylation of coenzyme A in a simple manner. Acetylation occurs in a quantitative yield when the reaction is performed in the presence of polyvinyl-4 pyridine/divinylbenzene 2 per cent. These conclusions enabled to develop two types of acetylating reactors which give rise without purification to 3-acetyl gentamicin.
为了制备具有潜在治疗价值的氨基糖苷类抗生素的特定N-单烷基化衍生物，我们开发了一种酶反应器。该系统使用氨基糖苷乙酰转移酶作为催化剂，乙酰辅酶A作为乙酰供体。研究了一种氨基糖苷乙酰转移酶在不同树脂上的固定化。在戊二醛存在下，该酶在DEAE纤维素上的交联产生了一种高效的酶树脂。另一方面，我们也以简单的方式研究了辅酶A的乙酰化。当反应在2%的聚乙烯基-4-吡啶/二乙烯基苯存在下进行时，乙酰化以定量产率发生。这些结论使得能够开发出两种类型的乙酰化反应器，它们无需纯化即可产生3-乙酰庆大霉素。
