人参皂苷Rb2在大鼠体内的药代动力学行为及代谢产物研究

引用本文: 张喆, 滕亚然, 吕子燕, 吴巍, 刘淑莹. 人参皂苷Rb2在大鼠体内的药代动力学行为及代谢产物研究[J]. 分析化学, 2017, 45(2): 191-198. doi: 10.11895/j.issn.0253-3820.160684 shu

Citation: ZHANG Zhe, TENG Ya-Ran, LYU Zi-Yan, WU Wei, LIU Shu-Ying. Pharmacokinetic and Metabolic Studies of Ginsenoside Rb2 in Rats[J]. Chinese Journal of Analytical Chemistry, 2017, 45(2): 191-198. doi: 10.11895/j.issn.0253-3820.160684 shu

人参皂苷Rb2在大鼠体内的药代动力学行为及代谢产物研究

张喆 ^1, ,
滕亚然 ^1, ,
吕子燕 ^1, ,
吴巍 ^1, ,
刘淑莹 ^1,2,

1.
长春中医药大学, 吉林省人参科学研究院, 长春 130117;
2.
中国科学院长春应用化学研究所, 长春质谱中心, 长春 130022
基金项目:
本文系吉林省科技厅人参化学与药理重点实验室探索项目基金资助（No.20160101334JC）

摘要: 建立快速高分离度液相色谱-四极杆飞行时间质谱联用方法（RRLC-Q-TOF-MS），分析人参皂苷Rb2在大鼠体内的药代动力学行为，并探索人参皂苷Rb2在大鼠体内的代谢过程。采用Agilent SB-C₁₈色谱柱，流动相A为0.1%甲酸溶液，B为乙腈，流速为0.2 mL/min，进样量为5 μL，二元线性梯度洗脱分离，采用电喷雾负离子模式进行质谱检测。方法的检出限（S/N=3）和定量限（S/N=10）分别为0.08 μg/mL和0.1 μg/mL，线性范围为0.10~1.26 μg/mL。结果表明，人参皂苷Rb2静脉注射后的体内代谢过程符合二室模型特征，血药浓度半衰期的α相（t_1/2α）和β相（t_1/2β）分别为（23.58±1.10）和（1306.55±147.23）min。通过对静脉注射人参皂苷Rb2的大鼠尿液和口服后的粪便样本进行分析，发现Rb2的代谢产物为M6，M2（C-Y），F2，C-K。

关键词:

English

Pharmacokinetic and Metabolic Studies of Ginsenoside Rb2 in Rats

1.
Jilin Ginseng Academy, Changchun University of Chinese Medicine, Changchun 130117, China;
2.
Changchun Center of Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
Received Date: 12 September 2016
Revised Date: 14 November 2016

Abstract: A rapid resolution liquid chromatography coupled with quadrupole-time-of-flight mass spectrometric (RRLC-Q-TOF-MS) method was established and optimized for the analysis of pharmacokinetic behavior of ginsenoside Rb2 in rats by intravenous injection administration. The metabolism of ginsenosides Rb2 in vivo rat was also explored. In the experiment, Agilent SB C₁₈ column was selected for the sample separation with 0.1% aqueous formic acid solution as mobile phase (A) and acetonitrile as mobile phase (B) at a flow rate of 0.2 mL/min, and the injection volume was set to 5 μL. Q-TOF-MS was carried out in electron pray ionization (ESI) negative ion mode. The limit of quantification (LOQ, S/N=10) and limit of detection (LOD, S/N=3) were 0.10 and 0.08 μg/mL, respectively, and the linear range was 0.1-1.26 μg/mL. The experiment results showed that the concentration-time profile of ginsenoside Rb2 conformed to a two-compartment pharmacokinetic model after intravenous administration for rats. The mean plasma elimination half-lives were (23.58±1.10) min (t_1/2α), (1306.55±147.23) min (t_1/2β) for Rb2. By analyzing the urine of rats after intravenous administration and the fecal samples after oral administration of ginsenoside Rb2, it was found that the metabolites were M6, M2(CY), F2, and C-K.

Key words:

Ginsenoside Rb2
/ Pharmacokinetics
/ Metabolite
/ Rapid resolution liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry

1. [1]
  Shi W, Wang Y, Li J, Zhang H, Ding L. Food Chem.,2007,102(12):664-668
2. [2]
  Gao B, Huang Q, Jie Q, Zhang H Y, Wang L, Guo Y S, Sun Z, Wei B Y, Han Y H, Liu J, Yang L, Luo Z J. Stem. Cells and Development,2015,24(6):781-790
3. [3]
  Zhang Q K, Yang B X, Zhai X G, Zhao K L, Wu Z J, Zhu Q W, Zhang J L, Wei X F, Zhao Y L, Cai J, Zhu Z L. Int. J. Pharmacol.,2014,10(8):524-527
4. [4]
  Kim E J, Lee H I, Chung K J, Noh Y H, Ro Y, Koo J H. BMB Reports,2008:194-199
5. [5]
  Lee K, Jung T W, Lee H, Kim S, Shin Y, Whang W.Arch. Pharm. Res.,2011,34:1201-1208
6. [6]
  Kim Y C, Kim S R, Markelonis G J, Oh T H. J. Neurosci. Res.,1998,53(4):426-432
7. [7]
  DAI Yu-Lin, YUE Hao, SUN Chang-Jiang, GUO Yun-Long, ZHENG Fei, LI Jing, LIU Shu-Ying. Chinese J. Anal. Chem.,2015,43(8):1181-1186 戴雨霖, 越皓, 孙长江,郭云龙, 郑飞, 李晶, 刘淑莹.分析化学,2015,43(8):1181-1186
8. [8]
  Lee K, Jung T W, Lee H, Kim S, Shin Y, Whang W. Arch. Pharm. Res.,2011,34(7):1201-1208
9. [9]
  Fujimoto J, Sakaguchi H, Aoki I, Toyoki H, Khatun S, Tamaya T. Eur. J. Gynaecol. Oncol.,2001,22(5):339-415
10. [10]
  Yi J, Liu W, Chen S, Backman V, Sheibani N, Sorenson CM, Fawzi A A, Linsenmeier R A, Zhang H F. Light Sci. Appl.,2015,4(9):e334
11. [11]
  Wu W, Qin Q, Guo Y Y, Sun J H, Liu S Y. J. Agric. Food Chem.,2012,60(40):10007-10014
12. [12]
  Qian T, Cai Z, Wong R N S, Mark N K, Jiang Z H. J. Chromatogr. B,2005,816(1):223-232
13. [13]
  Karikura M, Miyase T, Tanizawa H, Takino Y, Taniyama T, Hayashi T. Chem. Pharm. Bull.,1990,38(10):2859-2861
14. [14]
  Karikura M, Miyase T, Tanizawa H, Taniyama T, Takino Y. Chem. Pharm. Bull.,1991,39(2):400-404
15. [15]
  Karikura M, Miyase T, Tanizawa H, Taniyama T, Takino Y. Chem. Pharm. Bull.,1991,39(9):2357-2361
16. [16]
  Jin Y R, Tian T T, Ma Y H, Xu H J, Du Y F. J. Chromatogr. B,2015,1000:112-119
17. [17]
  Liu S, Cui M, Liu Z, Song F. Am J. Soc. Mass Spectrom.,2004,15(2):133-141
18. [18]
  Sun J H, Wu W, Guo Y Y, Qin Q J, Liu S Y. J. Pharm. Biomed. Anal.,2013,88(25):16-21

扫一扫看文章

计量

PDF下载量: 3
文章访问数: 824
HTML全文浏览量: 109

通讯作者: 陈斌, bchen63@163.com

1.
沈阳化工大学材料科学与工程学院沈阳 110142

人参皂苷Rb2在大鼠体内的药代动力学行为及代谢产物研究

English

Pharmacokinetic and Metabolic Studies of Ginsenoside Rb2 in Rats

CCS Chemistry：嵌段共聚物自组装成 “三明治”二维有机材料，实现纳米级压力传感功能

CCS Chemistry：颜徐州、鲍哲南：你的皮肤可能是一片SPMs

CCS Chemistry：工作高效不疲劳，只须让催化剂动起来

CCS Chemistry：静电组装导向聚合- 聚电解质纳米凝胶量化制备新策略

CCS Chemistry：金黄色葡萄球菌醛基脱氢酶是如何识别特异性底物的？

计量

通讯作者: 陈斌, bchen63@163.com

中国化学会秘书处

人参皂苷Rb2在大鼠体内的药代动力学行为及代谢产物研究

English

Pharmacokinetic and Metabolic Studies of Ginsenoside Rb2 in Rats

CCS Chemistry：嵌段共聚物自组装成 “三明治”二维有机材料，实现纳米级压力传感功能

CCS Chemistry：颜徐州、鲍哲南： 你的皮肤可能是一片SPMs

CCS Chemistry：工作高效不疲劳，只须让催化剂动起来

CCS Chemistry：静电组装导向聚合- 聚电解质纳米凝胶量化制备新策略

CCS Chemistry：金黄色葡萄球菌醛基脱氢酶是如何识别特异性底物的？

计量

文章相关

通讯作者: 陈斌, bchen63@163.com

中国化学会秘书处

CCS Chemistry：颜徐州、鲍哲南：你的皮肤可能是一片SPMs