葛根芩连汤中14种功效成分在大鼠体内的组织分布

刘昌顺; 晋臻; 陈飞龙; 谭晓梅

doi:10.13422/j.cnki.syfjx.20190549

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葛根芩连汤中14种功效成分在大鼠体内的组织分布

药物代谢 | 更新时间：2021-02-09

- 葛根芩连汤中14种功效成分在大鼠体内的组织分布
- Tissue Distribution of 14 Bioactive Components After Oral Administration of Gegen Qinlian Tang in Rats
- 中国实验方剂学杂志 2019年25卷第10期页码：93-101
- 作者机构：
  
  南方医科大学　中医药学院，广东省中药制剂重点实验室，广东省中药制剂技术工程实验室，广州　 510515
- 作者简介：
  
  刘昌顺，在读博士，从事中药体内过程研究，E-mail：lcshun1225@163.com
  *谭晓梅，博士，研究员，从事中药新制剂及中药复方配伍规律研究，Tel：020-61648265，E-mail：txm@fimmu.com
- 基金信息：
  
  国家自然科学基金项目(81374049)
- DOI：10.13422/j.cnki.syfjx.20190549
  中图分类号： R22; R24; R28; C37; R969.1
- 收稿日期：2018-10-03，
  
  网络出版日期：2018-11-21，
  
  纸质出版日期：2019-05-20
- 稿件说明：
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刘昌顺, 晋臻, 陈飞龙, 等. 葛根芩连汤中14种功效成分在大鼠体内的组织分布[J]. 中国实验方剂学杂志, 2019,25(10):93-101.

Chang-shun LIU, Zhen JIN, Fei-long CHEN, et al. Tissue Distribution of 14 Bioactive Components After Oral Administration of Gegen Qinlian Tang in Rats[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(10): 93-101.
刘昌顺, 晋臻, 陈飞龙, 等. 葛根芩连汤中14种功效成分在大鼠体内的组织分布[J]. 中国实验方剂学杂志, 2019,25(10):93-101. DOI： 10.13422/j.cnki.syfjx.20190549.

Chang-shun LIU, Zhen JIN, Fei-long CHEN, et al. Tissue Distribution of 14 Bioactive Components After Oral Administration of Gegen Qinlian Tang in Rats[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(10): 93-101. DOI： 10.13422/j.cnki.syfjx.20190549.

摘要

目的：

研究葛根芩连汤(GQT)功效成分在大鼠体内的组织分布特征，通过方药功效成分在体内各组织中的靶向性揭示其作用机制。

方法：

大鼠给予GQT后不同时间点取组织(小肠、大肠、肝、心、脾、肺、肾)，样品处理后采用HPLC-MS/MS分析14种功效成分在各组织匀浆液中的含量，Agilent ZORBAX SB-C

色谱柱(2.1 mm×100 mm，3.5 μm)，流动相0.1%甲酸水溶液-乙腈梯度洗脱，流速0.4 mL·min

－1

，电喷雾离子源，正离子模式检测，选择柚皮苷作为内标物。

结果：

建立了同时测定组织匀浆液中14种GQT主要功效成分的HPLC-MS/MS分析方法，该方法的专属性、标准曲线、回收率、基质效应、精密度、准确度和稳定性良好。在小肠组织中，异黄酮类主要成分葛根素、大豆苷元和3′-羟基葛根素的药时曲线下面积(AUC

0-10 h

)分别为22 174.9，3 882.5，15 893.1 h·mg·L

－1

，黄酮类主要成分黄芩素、汉黄芩素、汉黄芩苷和黄芩苷的AUC

0-10 h

分别为15 423.6，15 408.4，7 017.3，3 697.7 h·mg·L

－1

，生物碱类主要成分小檗碱的AUC

0-10 h

＝2 544.0 h·mg·L

－1

，这些成分在小肠组织的分布水平显著高于其他组织。

结论：

GQT的功效成分群主要分布于肠道组织，推测其抗炎、止泻的药理作用可能与其成分在肠道组织的作用趋向相关。

Abstract

Objective:

To investigate the tissue distribution of major bioactive components from Gegen qinlian Tang(GQT) in rats

and to reveal the mechanism for the efficacy of GQT by the tissue targeting of its bioactive ingredients

in vivo

Method:

After oral administration of GQT in rats

tissues were collected at different time points

including small and large intestine

liver

heart

spleen

lung

and kidney.Samples were prepared for determination of 14 bioactive components of GQT in tissue homogenate by HPLC-MS/MS.The chromatography separation was performed on an Agilent ZORBAX SB-C

column(2.1 mm×100 mm

3.5 μm) with acetonitrile-0.1% formic acid in water for gradient elution.Electrospray ionization(ESI) was applied and operated in the positive ion mode.Meanwhile

naringin was used as the internal standard for determining.

Result:

HPLC-MS/MS for simultaneous determination of 14 components from GQT in tissue homogenate was developed and validated by specificity

calibration curves

recovery test

matrix effect

precision

accuracy

and stability.In the small intestine

the the area under the curve(AUC

0-10 h

) of major isoflavonoids(puerarin

3′-hydroxypuerarin

and daidzein) were 22 174.9

15 893.1

3 882.5 h·mg·L

-1

major flavonoids(baicalein

wogonin

wogonoside

and baicalin) were 15 423.6

15 408.4

7 017.3

3 697.7 h·mg·L

-1

and major alkaloid(berberine) was 2 544.0 h·mg·L

-1

respectively.The distribution of these ingredients in the small intestine was significantly higher than that in other tissues.

Conclusion:

The effective ingredients of GQT are mainly distributed in the intestinal tissues

which speculates that the anti-inflammatory and antidiarrheal activities of GQT may be related to its targeting in the intestine.

关键词

Keywords

references

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