Liguzinediol在不同种属肝微粒体中代谢产物的比较研究

戴贞丽; 文红梅; 单晨啸; 尤晓亲; 董棒; 孙学; 李伟

Liguzinediol在不同种属肝微粒体中代谢产物的比较研究

南京中医药大学药学院，江苏南京 210023

计量
- 文章访问数: 782
- HTML全文浏览量: 15
- PDF下载量: 625
- 被引次数: 0
出版历程
- 刊出日期: 2016-01-10

Comparing Metabolites of Liguzinediol in Liver Microsomes among Different Species

摘要

摘要: 目的比较研究不同种属间liguzinediol的体外代谢产物。方法建立liguzinediol及其体外代谢产物的LC-MS/MS检测方法，采用肝微粒体温孵法研究liguzinediol在大鼠、犬、猴、人等多种属肝微粒体中的代谢产物。结果 liguzinediol在肝脏可发生Ⅰ相和Ⅱ相代谢，并且在大鼠、犬、猴、人肝微粒体温孵体系中均孵育有氧化产物和葡萄糖醛酸结合产物。结论 liguzinediol在大鼠、犬和猴等动物的肝微粒体中的Ⅰ相和Ⅱ相代谢产物与人肝微粒体基本一致，该研究结果可为liguzinediol临床前安全性评价的实验动物选择提供依据。
- 代谢产物 /
- liguzinediol /
- 肝微粒体温孵 /
- 不同种属
Abstract: OBJECTIVE To compare metabolites of liguzinediol in liver microsomes among different species， such as rats， dogs， monkeys and human. METHODS LC-MS/MS method was established to determine liguzinediol and its metabolites. The liver microsome incubation systems among different species were built to research the metabolites of liguzinediol. RESULTS Phase Ⅰ and phase Ⅱ metabolism of liguzinediol can be occurred in liver. The oxidation and glucuronidase acid binding products were all found in four kinds of liver microsomes. CONCLUSION The metabolites of liguzinediol in liver microsome from rats， dogs and monkeys were consistent with that from human. The results can be used to select laboratory animal for safety evaluation of liguzinediol in preclinical study.
- metabolites /
- liguzinediol /
- liver microsome incubation /
- different species

HTML全文

参考文献(11)

[1]	刘峥，周淑媛，李伟，等．liguzinediol对正常大鼠离体心脏的正性肌力作用[J]．中国新药与临床杂志，2009， 28（4）：293-296．
[2]	Liu Z， Zhou SY， Li W， et al. Liguzinediol induced positive inotropic effect in normal isolated rat hearts[J]. Chin J New Drug Clin Remed， 2009， 28(4): 293-296.
[3]	郭瑶，周静，卞慧敏，等．川芎嗪衍生物liguzinediol对戊巴比妥钠致急性心力衰竭大鼠血流动力学的影响[J]．中国实验方剂学杂志，2012， 18（6）：170-174．
[4]	Guo Y， Zhou J， Bian HM， et al. The effect of liguzinediol on hemodynamics in rats with acute heart failure induced by pentobarbital[J]. Chin J Exper Tradit Med Form， 2012， 18(6): 170-174.
[5]	Chen L， Xu Y， Li W， et al. The novel compound liguzinediol exerts positive inotropic effects in isolated rat heart via sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism[J]. Life Sci， 2012， 91(11/12): 402-408.
[6]	张路，李伟，文红梅，等．LC-MS/MS测定大鼠血浆中liguzinediol浓度及药动学[J]．中国新药杂志，2013， 22（9）：1024-1028， 1046．
[7]	Zhang L， Li W， Wen HM， et al. An LC-MS/MS method for determining liguzinediol in rat plasma and studying its pharmacokinetics[J]. Chin J New Drug， 2013， 22(9): 1024-1028， 1046.
[8]	朱晓雯，李伟，文红梅，等．LC-MS/MS法定量研究比格犬注射liguzinediol的血浆药代动力学[J]．中国药理学通报，2014， 30（3）：443-444．
[9]	Zhu XW， Li W， Wen HM， et al. Pharmacokinetic study of liguzinediol in beagle dogs using LC-MS/MS method[J]. Chin Pharm Bull， 2014， 30(3): 443-444.
[10]	Shan CX， Li W， Wen HM， et al. Identification of liguzinediol metabolites in rats by ultra performance liquid chromatography/quadrupole-time-of-flight mass spectrometry[J]. J Pharm Biomed Anal， 2012， 62(3): 187-190.
[11]	Shan CX， Li W， Wen HM， et al. Metabolite identification of liguzinediol in dogs by ultra-flow liquid chromatography/tandem mass spectrometry[J]. J Chromatogr B， 2014， 967: 63-68.