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Pharmacokinetic studies on Schisandrae Fructus lignans and the affecting factors on pharmacokinetic actions of the lignans

Jianxiu Zhai, Zhihui Liu, Na Han, Jun Yin*   

  1. School of Traditional Chinese Materia, Shenyang Pharmaceutical University; Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110016, China
  • 收稿日期:2014-04-20 修回日期:2015-10-31 出版日期:2016-02-20 发布日期:2015-10-31

Pharmacokinetic studies on Schisandrae Fructus lignans and the affecting factors on pharmacokinetic actions of the lignans

Jianxiu Zhai, Zhihui Liu, Na Han, Jun Yin*   

  1. School of Traditional Chinese Materia, Shenyang Pharmaceutical University; Liaoning Key Laboratory of Northeast Genuine Medicinal Materials Resource, Shenyang 110016, China
  • Received:2014-04-20 Revised:2015-10-31 Online:2016-02-20 Published:2015-10-31
  • Contact: Jun Yin*, School of Traditional Chinese Materia Medica 48#, Shenyang Pha rma c eut i c a l Unive r s i ty, 103 Wenhua Road, Shenhe District, Shenyang 110016, China; Tel./fax: +86-24-23986491; E-mail: yinjun2002@yahoo.com

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摘要： The main lignans of Schisandra chinensis are known as the therapeutic components. The absorption, distribution, metabolites, and metabolic pathways of them were concluded in this paper. Potential effects on experiment results of different subjects were also discussed. Results: 1. Deoxyschisandrin (DS), schisandrin (SCH) and schisandrin B (SCH B/γ-SCH) can be regarded as the main therapeutic components absorbed into blood. 2. All the lignans showed the same distribution trend: highest concentration in liver and lungs, then in kidney and heart, least in spleen and intestines. DS and SCH can cross the blood-brain barrier (BBB). 3. CYP3A4 is the only subtype that catalysis metabolic pathway of DS and SCH. The metabolic order of DS and SCH differed in in vivo and in vitro environment. 4. After oral administration, the Tmax of DS was about 4~5 h, the Tmax of SCH distributed from 0.33 to 0.7 h. The secondary absorption of γ-SCH had been observed. 5. Gender difference is found in the metabolism of SCH and γ-SCH in vitro using the liver microsomes of male and female rats. The blood pretreatment methods had also been compared and using plasma turned to be a better choice than using serum for Schisandrae lignan analyzation.

关键词: Schisandrae Fructus, lignan, pharmacokinetic study, gender difference

Abstract: The main lignans of Schisandra chinensis are known as the therapeutic components. The absorption, distribution, metabolites, and metabolic pathways of them were concluded in this paper. Potential effects on experiment results of different subjects were also discussed. Results: 1. Deoxyschisandrin (DS), schisandrin (SCH) and schisandrin B (SCH B/γ-SCH) can be regarded as the main therapeutic components absorbed into blood. 2. All the lignans showed the same distribution trend: highest concentration in liver and lungs, then in kidney and heart, least in spleen and intestines. DS and SCH can cross the blood-brain barrier (BBB). 3. CYP3A4 is the only subtype that catalysis metabolic pathway of DS and SCH. The metabolic order of DS and SCH differed in in vivo and in vitro environment. 4. After oral administration, the Tmax of DS was about 4~5 h, the Tmax of SCH distributed from 0.33 to 0.7 h. The secondary absorption of γ-SCH had been observed. 5. Gender difference is found in the metabolism of SCH and γ-SCH in vitro using the liver microsomes of male and female rats. The blood pretreatment methods had also been compared and using plasma turned to be a better choice than using serum for Schisandrae lignan analyzation.

Key words: Schisandrae Fructus, lignan, pharmacokinetic study, gender difference

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