CYP3A参与双吡酰胺单- n -脱烷基化的立体选择性的物种差异。
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张玲，Fitzloff JF, Engel LC, Cook CS
CYP3A参与双吡酰胺单- n -脱烷基化的立体选择性的物种差异。
Xenobiotica. 2001 Feb;31(2):73-83。
- PubMed ID
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11407536 (PubMed视图］
- 摘要
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1.为了确定哪种CYP同工酶参与了人和犬双吡酰胺(DP)代谢的n -脱烷基化，并确定DP代谢与人CYP和犬CYP同工酶的立体选择性，进行了DP体外代谢研究:人CYP同工酶活性与DP代谢与人肝颗粒体的相关性;CYP同工酶化学抑制剂对人和狗肝脏微粒体DP代谢的抑制作用人CYP抗体对人微粒体DP代谢的抑制作用人、犬CYP抗体对犬肝微粒体DP代谢的抑制作用DP与人(CYP3A4)和狗(CYP3A12) cdna表达同工酶的代谢;用cdna表达的CYP3A4和CYP3A12测定DP对映体的Km和Vmax。2.在人肝微粒体中，单- n -脱烷基化二吡酰胺(MNDP)代谢物的形成与CYP3A4活性最相关。酮康唑、曲兰霉素(TA)和人CYP3A4抗体可显著抑制DP代谢。 DP was metabolized by cDNA-expressed CYP3A isoenzymes. In dog liver microsomes, DP metabolism was inhibited by ketoconazole, TA and dog anti-CYP3A12. DP was also metabolized by cDNA-expressed CYP3A12. 3. CYP3A4 and CYP3A12 are the principal isoenzymes involved in DP metabolism in human and dog respectively. There was no stereoselectivity in N-dealkylation of DP by human CYP3A4. However, there was notable stereoselectivity in the N-dealkylation by dog CYP3A12.
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