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黄芩根重复给药后黄酮类药代动力学和组织分布。

Flavonoid pharmacokinetics and tissue distribution after repeated dosing of the roots of Scutellaria baicalensis in rats.

机构信息

School of Pharmacy, College of Pharmacy, China Medical University, Taichung, Taiwan.

出版信息

Planta Med. 2011 Mar;77(5):455-60. doi: 10.1055/s-0030-1250433. Epub 2010 Oct 18.


DOI:10.1055/s-0030-1250433
PMID:20957598
Abstract

Scutellariae Radix (root of Scutellaria baicalensis, SR) contains numerous flavonoids such as baicalin, baicalein, and wogonin. This study investigated the pharmacokinetics and tissue distribution of flavonoids and their metabolites in rats after repeated dosing of a SR decoction. Sprague-Dawley rats were orally administered SR at 2 g/kg for seven doses. After the 7th dose, blood samples were withdrawn at specific times and organs, including the liver, kidney, lung, and brain, and collected. The concentrations of baicalein and wogonin in the serum and various tissues were assayed by HPLC before and after hydrolysis with glucuronidase and sulfatase. Baicalein and wogonin were not detected in the serum, and the molecules found were their glucuronides/sulfates. In tissues, the free forms of baicalein and wogonin appeared in the liver, kidney, and lung in addition to their glucuronides/sulfates. Baicalein was the major form in the lung, whereas baicalein glucuronides/sulfates were the major forms in the liver and kidney. Wogonin was the major form in the liver, kidney, lung, and traces of wogonin glucuronides/sulfates were detected in the kidney and liver. Neither baicalein and wogonin nor their glucuronides/sulfates were detected in the brain. In conclusion, the glucuronides/sulfates of baicalein and wogonin were exclusively present in the circulation, whereas their free forms appeared in the lung, liver, and kidney.

摘要

黄芩根(黄芩,SR)含有多种黄酮类化合物,如黄芩苷、黄芩素和汉黄芩素。本研究考察了重复给予 SR 煎剂后黄酮类化合物及其代谢物在大鼠体内的药代动力学和组织分布。SD 大鼠经口给予 SR 2 g/kg,共 7 剂。第 7 次给药后,在特定时间点采集血样,并采集肝、肾、肺和脑等器官。采用 HPLC 法测定水解前后血清和各组织中黄芩素和汉黄芩素的浓度,用葡萄糖醛酸酶和硫酸酯酶。血清中未检测到黄芩素和汉黄芩素,发现的分子是它们的葡萄糖醛酸苷/硫酸酯。在组织中,除了葡萄糖醛酸苷/硫酸酯外,黄芩素和汉黄芩素的游离形式还出现在肝、肾和肺中。黄芩素在肺中主要以游离形式存在,而黄芩素葡萄糖醛酸苷/硫酸酯在肝和肾中主要以游离形式存在。汉黄芩素在肝、肾、肺中主要以游离形式存在,在肾和肝中检测到微量的汉黄芩素葡萄糖醛酸苷/硫酸酯。脑内未检测到黄芩素、汉黄芩素及其葡萄糖醛酸苷/硫酸酯。综上所述,黄芩素和汉黄芩素的葡萄糖醛酸苷/硫酸酯仅存在于循环中,而其游离形式则出现在肺、肝和肾中。

相似文献

[1]
Flavonoid pharmacokinetics and tissue distribution after repeated dosing of the roots of Scutellaria baicalensis in rats.

Planta Med. 2010-10-18

[2]
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[3]
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[4]
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[6]
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[7]
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[8]
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[10]
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[3]
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[4]
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[6]
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[7]
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[8]
An overview and comparison of a recombinant antigen-binding fragment and an antigen-binding fragment from a monoclonal antibody against wogonin glucuronide.

J Nat Med. 2017-10

[9]
Comparative research on stability of baicalin and baicalein administrated in monomer and total flavonoid fraction form of Radix scutellariae in biological fluids in vitro.

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[10]
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