兔肝酶高效生产环孢菌素代谢物AM1。

Efficient production of the cyclosporin metabolite AM1 by rabbit hepatic enzymes.

作者信息

Paroni R, Fermo I, Iavarone L, Del Puppo M, De Angelis L, Galli Kienle M

机构信息

Scientific Institute H. San Raffaele, Milan, Italy.

出版信息

Pharmacol Res. 1993 Jul-Aug;28(1):73-84. doi: 10.1006/phrs.1993.1111.

DOI:10.1006/phrs.1993.1111

PMID:8234147

Abstract

We describe here conditions for the in vitro preparation of the main metabolite of cyclosporin A, namely AM1, with rabbit liver enzymes. The compound was purified and was identified by comparison with the metabolite isolated from urine of rats treated with [3H]CsA and by its Mass-Spectrometry Fast Ion Bombardment (MS-FIB) and 1HNMR spectra. The procedure is simple and with the enzyme fraction derived from one rabbit liver 3-4 mg of the pure metabolite can be obtained.

摘要

我们在此描述了用兔肝酶体外制备环孢菌素A主要代谢物即AM1的条件。该化合物经纯化，并通过与从用[³H]环孢菌素A处理的大鼠尿液中分离出的代谢物进行比较以及通过其快速离子轰击质谱（MS-FIB）和¹H NMR光谱进行鉴定。该方法简单，从一只兔肝得到的酶组分可获得3 - 4毫克纯代谢物。