孙国玲;钱大玮;段金廒;李向明;万建义;郭建明;
SUN Guoling 1,QIAN Dawei2*,DUAN Jin'ao2,LI Xiangming 3,WAN Jianyi3,GUO Jianming2 (1.School of Pharmacological Science,Jiangsu University,Zhenjiang 212013,China;2.Nanjing University of Chinese Medicine,Nanjing 210046,China;3.Huazhou Green Life Co.,Ltd.,Guangzhou 510016,China)

• 1:江苏大学药学院
• 2:南京中医药大学
• 3:广东化州市绿色生命有限公司

摘要(Abstract)：

目的:分析大鼠灌胃毛橘红醇提物后血浆中柚皮苷、柚皮素及其代谢产物。方法:健康雄性SD大鼠按50 g.kg-1剂量经口给予毛橘红醇提物,1.0 h后采集眼眶静脉血液制备血浆,采用UPLC-Q-TOF的MSE功能与M etabolynxTM软件联合的方法分析。结果:在大鼠血浆中检测到柚皮苷(M1)、柚皮素(M2)、柚皮苷5-O-葡萄糖醛酸苷(M3)、柚皮苷4′-O-葡萄糖醛酸苷(M4)、柚皮素葡萄糖醛酸苷(M5)、柚皮苷4′-O-硫酸酯(M6)、羟基化柚皮素甲醚(M7)、柚皮素葡萄糖醛酸基和硫酸酯基共价结合物(M8)、羟基化柚皮素葡萄糖醛酸苷(M9)。其中M3,M4,M6为首次报道的柚皮苷代谢物,M7,M9为首次报道的柚皮素代谢物。结论:柚皮苷、柚皮素在大鼠体内以葡萄糖醛酸化、硫酸化的形式被代谢,柚皮素还以氧甲基化、羟化葡萄糖醛酸化的形式被代谢。
Objective: To analyze naringin,naringenin and its metabolites in rat plasma after intragastric administration of exocarpium Citri grandis alcohol extract.Method: Rat blood samples were collected 1.0 hour after oral administration of 50 g·kg-1 exocarpium Citri grandis alcohol extract and analyzed by UPLC-Q-TOF with MSE function.The post-acquisition data were processed using MetabolynxTM.Result: Naringin(M1),naringenin(M2),naringin-5-O-glucuronide(M3),naringin-4-O-glucuronide(M4),glucuronide conjugate of naringenin(M5),naringin-4-O-sulfate(M6),methylated conjugate of hydroxylated naringenin(M7),glucuronide and sulfate conjugate of naringenin(M8),glucuronide conjugate of hydroxylated naringenin(M9) in rat plasma were detected.M3,M4,M6 were first reported as the metabolites of naringin.M7,M9 were first reported as the metabolites of naringenin.Conclusion: The results indicated that naringin,naringenin can be metabolited as the forms of glucuronidation,sulfation and naringenin can also be metabolited as the forms of methylation with hydroxylation and glucuronidation with hydroxylation in vivo after administration.

关键词(KeyWords)： 毛橘红醇提物;柚皮苷;柚皮素;代谢产物;UPLC-Q-TOF-MS联用
Citri grandis;naringin;naringenin;metabolites;UPLC-Q-TOF-MS

Abstract:

Keywords:

基金项目(Foundation):

作者(Authors): 孙国玲;钱大玮;段金廒;李向明;万建义;郭建明;
SUN Guoling 1,QIAN Dawei2*,DUAN Jin'ao2,LI Xiangming 3,WAN Jianyi3,GUO Jianming2 (1.School of Pharmacological Science,Jiangsu University,Zhenjiang 212013,China;2.Nanjing University of Chinese Medicine,Nanjing 210046,China;3.Huazhou Green Life Co.,Ltd.,Guangzhou 510016,China)

参考文献(References)：

• [1]中国药典.一部[S].2005:51.
• [2]袁旭江,林励,陈志霞.化橘红中酚性成分的研究[J].中草药,2004,35(5):498.
• [3]杨宏亮,田珩,李沛波,等.柚皮苷及柚皮素的生物活性研究[J].中药材,2007,30(6):752.
• [4]Junmei Zhang,Jennifer S Brodbelt.Screening flavonoid metabo-lites of naringin and narirutin in urine after human consumption ofgrapefruit juice by LC-MS and LC-MS/MS[J].Analyst,2004,129:1227.
• [5]裴利宽,郭宝林.黄酮类化合物吸收和代谢研究进展[J].中国中药杂志,2006,31(8):568.
• [6]曾佑炜,赵金莲,彭永宏.黄酮的吸收和代谢研究进展[J].中草药,2008,39(3):460.
• [7]吕鹏,黄晓舞,吕秋军.黄酮类化合物吸收、分布和代谢的研究进展[J].中国中药杂志,2007,32(19):1961.
• [8]陈志霞,林励.化橘红药材中香豆素类成分的研究[J].中药材,2004,27(8):577.