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厚朴酚及其代谢产物在大鼠体内的药代动力学和组织分布

The Pharmacokinetics and Tissue Distribution of Honokiol and its Metabolites in Rats.

作者信息

Jun-Jun Wang, Xiao-Lei Miao, Jing-Ya Chen, Yong Chen

机构信息

Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan, 430062, China.

出版信息

Eur J Drug Metab Pharmacokinet. 2016 Oct;41(5):587-94. doi: 10.1007/s13318-015-0281-6.

DOI:10.1007/s13318-015-0281-6
PMID:25956504
Abstract

Honokiol (HK) is the main bioactive compound isolated from the bark of Magnolia officinalis. The present work is the first to report the pharmacokinetics and distribution of HK and its two metabolites of hydroxylated HK conjugated with glucuronic and sulfuric acid (M1) and HK monoglucuronide (M2) in plasma, liver, kidney and brain following oral administration of HK (40 mg/kg) to healthy Wistar rats. The results showed that only HK but not M1 or M2 was found in brain. Additionally, our work indicated that M2 not HK was the major compound in liver and plasma. The elimination of HK in liver, kidney and brain, and M2 in liver and kidney was more rapid than in plasma. The finding suggested that some of the pharmacological activity of HK might be generated by M2 but not HK.

摘要

厚朴酚(HK)是从厚朴树皮中分离出的主要生物活性化合物。本研究首次报道了在健康Wistar大鼠口服给予HK(40mg/kg)后,HK及其与葡萄糖醛酸和硫酸结合的两种羟基化HK代谢物(M1)和HK单葡萄糖醛酸苷(M2)在血浆、肝脏、肾脏和大脑中的药代动力学及分布情况。结果显示,在大脑中仅发现了HK,而未发现M1或M2。此外,我们的研究表明,肝脏和血浆中的主要化合物是M2而非HK。HK在肝脏、肾脏和大脑中的消除,以及M2在肝脏和肾脏中的消除比在血浆中更快。这一发现表明,HK的某些药理活性可能是由M2而非HK产生的。

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本文引用的文献

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Intravenous administration of Honokiol provides neuroprotection and improves functional recovery after traumatic brain injury through cell cycle inhibition.厚朴酚静脉给药通过抑制细胞周期提供神经保护并改善创伤性脑损伤后的功能恢复。
Neuropharmacology. 2014 Nov;86:9-21. doi: 10.1016/j.neuropharm.2014.06.018. Epub 2014 Jun 25.
2
Pharmacokinetics of honokiol after intravenous guttae in beagle dogs assessed using ultra-performance liquid chromatography-tandem mass spectrometry.采用超高效液相色谱-串联质谱法评估比格犬静脉滴注厚朴酚后的药代动力学。
Biomed Chromatogr. 2014 Oct;28(10):1378-83. doi: 10.1002/bmc.3179. Epub 2014 Mar 21.
3
厚朴酚及其从木兰属植物中提取的衍生物的神经药理学潜力:从治疗角度的理解
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Honokiol Inhibits SARS-CoV-2 Replication in Cell Culture at a Post-Entry Step.和厚朴酚在细胞培养中通过进入后步骤抑制 SARS-CoV-2 复制。
Microbiol Spectr. 2023 Jun 15;11(3):e0327322. doi: 10.1128/spectrum.03273-22. Epub 2023 May 4.
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Effectiveness in the Block by Honokiol, a Dimerized Allylphenol from , of Hyperpolarization-Activated Cation Current and Delayed-Rectifier K Current.厚朴酚,一种来自厚朴的二聚烯丙基酚,对超极化激活阳离子电流和延迟整流钾电流的阻断作用。
Int J Mol Sci. 2020 Jun 15;21(12):4260. doi: 10.3390/ijms21124260.
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Honokiol inhibits carotid artery atherosclerotic plaque formation by suppressing inflammation and oxidative stress.和厚朴酚通过抑制炎症和氧化应激抑制颈动脉粥样硬化斑块形成。
Aging (Albany NY). 2020 May 4;12(9):8016-8028. doi: 10.18632/aging.103120.
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Honokiol: A Review of Its Anticancer Potential and Mechanisms.厚朴酚:抗癌潜力及作用机制综述
Cancers (Basel). 2019 Dec 22;12(1):48. doi: 10.3390/cancers12010048.
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Inhibition of Rat CYP1A2 and CYP2C11 by Honokiol, a Component of Traditional Chinese Medicine.厚朴酚(一种中药成分)对大鼠CYP1A2和CYP2C11的抑制作用
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Biochem Pharmacol. 2008 Sep 1;76(5):589-96. doi: 10.1016/j.bcp.2008.06.012. Epub 2008 Jul 2.