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人肝微粒体中15-去甲基FK-506和15,31-去甲基FK-506：分离、鉴定（通过快原子轰击质谱法和核磁共振）以及体外免疫抑制活性评估。

15-Desmethyl FK-506 and 15,31-desmethyl FK-506 from human liver microsomes: isolation, identification (by fast atom bombardment mass spectrometry and NMR), and evaluation of in vitro immunosuppressive activity.

作者信息

Lhöest G J, Maton N, Latinne D, Laurent A, Verbeeck R K

机构信息

Department of Pharmaceutical Sciences, UCL, FATC, Brussels, Belgium.

出版信息

Clin Chem. 1994 May;40(5):740-4.

PMID:7513627
Abstract

15-Desmethyl FK-506 and 15,31-desmethyl FK-506 metabolites extracted from incubated human liver microsomes were separated by normal and reversed-phase HPLC. The metabolites were identified by fast atom bombardment/mass spectrometry and nuclear magnetic resonance spectroscopy. The in vitro 50% inhibitory concentration, tested against bidirectional mixed lymphocyte reactions, was 325 mg/L for 15,31-desmethyl FK-506 and 4 mg/L for 15-desmethyl FK-506, indicating that these products of FK-506 demethylation retain in vitro immunosuppressive activity.

摘要

从人肝微粒体孵育物中提取的15-去甲基FK-506和15,31-去甲基FK-506代谢产物通过正相和反相高效液相色谱法进行分离。这些代谢产物通过快原子轰击/质谱法和核磁共振光谱法进行鉴定。针对双向混合淋巴细胞反应进行测试，15,31-去甲基FK-506的体外50%抑制浓度为325mg/L，15-去甲基FK-506为4mg/L，表明FK-506去甲基化的这些产物保留了体外免疫抑制活性。

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