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白杨素在模式生物斑马鱼中的代谢研究
  • ISSN号:1001-2494
  • 期刊名称:《中国药学杂志》
  • 时间:0
  • 分类:R969.1[医药卫生—药理学;医药卫生—药学]
  • 作者机构:[1]江苏省中医药研究院,国家中医药管理局中药口服释药系统重点研究室,南京210028
  • 相关基金:国家自然科学基金资助项目(30973978);江苏省中医药领军人才专项资助项目
中文摘要:

目的采用模式生物斑马鱼研究白杨素的代谢,探索斑马鱼用于研究药物Ⅱ相代谢的可行性及合理性。方法将斑马鱼暴露于白杨素溶液中,定时取鱼体及药液,采用高效液相色谱一电喷雾质谱联用检测,根据正、负离子模式准分子离子峰获得化合物相对分子质量信息,通过与文献数据或对照品对照,推测代谢产物。结果在斑马鱼体内或体外药液检测到白杨素原形及其2个单羟基葡萄糖醛酸结合物和1个单羟基硫酸结合物。结论斑马鱼对白杨素的代谢与白杨素已有体内、体外的Ⅱ相代谢机制高度一致,提示斑马鱼用于药物Ⅱ相代谢具合理性,更具有化合物用量少、成本低、方法简单、高效的优势,为建立一种模式的、生物的在体药物代谢新模型提供重要参考价值。

英文摘要:

OBJECTIVE To study the metabolism of chrysin by model organism zebrafish for the first time, thus to investigate the reasonability of applying zebrafish in drug phase Ⅱ metabolism. METHODS Zebrafish was exposed to chrysin solution for 24 h, and the samples of solution and zebrafish body were analyzed by high performance liquid chromatography-electrospray mass spectrometry (HPLC-ESI-MS) method. The quasi-molecular ions of compounds in both negative and positive mode were observed for molecule mass information, and the potential structures of the compounds were identified by studying on the mass spectra and comparing with reference data or standards. RESULTS In addition to the parent compound, three phase Ⅱ metabolites were identified,including two glucuroni- dation products and one sulfation product. CONCLUSION The metabolism of chrysin in zebrafish is highly consistent with that iden- tified by current in vivo and in vitro methods, which indicates that it is reasonable using zebrafish to sutdy phase Ⅱ metabolism. Ze- brafish model has the advantages of using far less amount of compound, lower cost, higher efficiency and simple procedure, which may become a novel organism model for quick predication of metabolism of compounds and enrich the available models greatly.

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期刊信息
  • 《中国药学杂志》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:中国药学会
  • 主编:桑国卫
  • 地址:北京市朝阳区建外大街四号建外SOHO九号楼18层
  • 邮编:100022
  • 邮箱:zgyxzz@cpa.org.cn
  • 电话:010-58698009
  • 国际标准刊号:ISSN:1001-2494
  • 国内统一刊号:ISSN:11-2162/R
  • 邮发代号:2-232
  • 获奖情况:
  • 首届国家期刊奖,第一、二届全国优秀科技期刊一等奖,中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),荷兰文摘与引文数据库,荷兰医学文摘,日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘,中国北大核心期刊(2000版)
  • 被引量:54982