KINETIC-ANALYSIS OF MOLECULAR INTERCONVERSION OF IMMUNOSUPPRESSANT FK506 BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY

被引:26
作者
NISHIKAWA, T
HASUMI, H
SUZUKI, S
KUBO, H
OHTANI, H
机构
[1] DEPT BIOPHYS CHEM,SAGAMIHARA,KANAGAWA,JAPAN
[2] KITASATO UNIV,SCH PHARMACEUT SCI,DEPT PHARMACEUT ANAL,MINATO KU,TOKYO 108,JAPAN
关键词
FK506; CYCLOSPORINS; IMMUNOSUPPRESSANT; CONFORMATIONAL ISOMERIZATION; HPLC;
D O I
10.1023/A:1018938618032
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
High-performance liquid chromatography of FK506, a macrolide immunosuppressant, was performed on a reversed-phase column. The peak was broad with the column kept at room temperature, which was accounted for by slow interconversion between the two forms of FK506. With the use of a heated column, a sharp peak was observed because of the rapid interconversion at high temperature. When the column was cooled to 0-degrees-C, two sharp peaks were observed because essentially no interconversion occurred at 0-degrees-C during elution. Analysis of the chromatograms obtained at various eluant flow rates indicated that the conversion of the two forms follows first-order kinetics, and the apparent activation energies for the conversions were calculated. The interconvertibility between two molecular forms may be related to the immunosuppressive activity.
引用
收藏
页码:1785 / 1789
页数:5
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