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Research ArticleArticle

ABSORPTION AND METABOLISM OF ASTRAGALI RADIX DECOCTION: IN SILICO, IN VITRO, AND A CASE STUDY IN VIVO

Feng Xu, Yue Zhang, Shengyuan Xiao, Xiaowei Lu, Donghui Yang, Xiaoda Yang, Changling Li, Mingying Shang, Pengfei Tu and Shaoqing Cai
Drug Metabolism and Disposition June 2006, 34 (6) 913-924; DOI: https://doi.org/10.1124/dmd.105.008300
Feng Xu
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Yue Zhang
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Shengyuan Xiao
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Xiaowei Lu
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Donghui Yang
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Xiaoda Yang
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Changling Li
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Mingying Shang
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Pengfei Tu
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Shaoqing Cai
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Abstract

To profile absorption of Astragali Radix decoction and identify its orally absorbable constituents and their metabolites, four complementary in silico, in vitro, and in vivo methods, i.e., a computational chemistry prediction method, a Caco-2 cell monolayer model experiment, an improved rat everted gut sac experiment, and a healthy human volunteer experiment, were used. According to the in silico computation result, 26 compounds of Astragali Radix could be regarded as orally available compounds, including 12 flavonoids. In the in vitro and in vivo experiments, 21 compounds were tentatively identified by high-performance liquid chromatography-diode array detection-electrospray ion trap tandem mass spectrometry data, which involved calycosin, formononetin, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan, calycosin-7-O-β-d-glucoside, formononetin-7-O-β-d-glucoside, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-7-O-β-d-glucoside-6″-O-malonate, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucoside, and phase II metabolites calycosin-7-O-β-d-glucuronide, formononetin-7-O-β-d-glucuronide, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucuronide, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-7-O-β-d-glucuronide, and calycosin sulfate. Calycosin and formononetin were proved absorbable by four methods; (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan and 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan were proved absorbable by three methods; formononetin-7-O-β-d-glucoside and (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucoside were proved absorbable by two methods. The existence of calycosin-7-O-β-d-glucuronide, formononetin-7-O-β-d-glucuronide, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucuronide, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-7-O-β-d-glucuronide, and calycosin sulfate was proved by two or three methods. We found that besides isoflavones, pterocarpans and isoflavans also could be metabolized by the intestine during absorption, and the major metabolites were glucuronides. In conclusion, the present study demonstrated that the flavonoids in Astragali Radix decoction, including isoflavones, pterocarpans, and isoflavans, could be absorbed and metabolized by the intestine. These absorbable compounds, which were reported to have various bioactivities related to the curative effects of Astragali Radix decoction, could be regarded as an important component of the effective constituents of Astragali Radix decoction.

Footnotes

  • This work was supported by National Natural Science Foundation of China (No. 30371721) and 985 Project of Peking University.

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

  • doi:10.1124/dmd.105.008300.

  • ABBREVIATIONS: HPLC-DAD-ESI-MSn, high-performance liquid chromatography-diode array detection-electrospray ion trap tandem mass spectrometry; ClogP, the log P value calculated by the ClogP 4.0 program (P is partition coefficient of the molecule); C1, calycosin-7-O-β-d-glucuronide; C2, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucuronide; C3, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-2′-O-β-d-glucuronide; C4, 7,2′-dihydroxy-3′,4′,5′-trimethoxyisoflavan-7-O-β-d-glucuronide; C5, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-7-O-β-d-glucuronide; C6, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-glucoside-6″-O-malonate; C7, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan-7-O-β-d-glucoside-6″-O-malonate; C8, calycosin-7-O-β-d-glucoside; C9, formononetin-7-O-β-d-glucoside; C10, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan-3-O-β-d-sambubioside; C11, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpane-3-O-β-d-glucoside; C12, 7,3′-dihydroxy-2′,4′-dimethoxyisoflavan-7-O-β-d-glucoside; C13, calycosin; C14, formononetin; C15, (6aR,11aR)-3-hydroxy-9,10-dimethoxypterocarpan; C16, 7,2′-dihydroxy-3′,4′-dimethoxyisoflavan; C17, formononetin-7-O-β-d-glucuronide; C18, calycosin sulfate; C19, 7,2′-dihydroxy-3′,4′,6′-trimethoxyisoflavan; C20, daidzein-7-O-β-d-glucuronide; C21, 7,3′-dihydroxy-2′,4′-dimethoxyisoflavan-7-O-β-d-glucosyl-3′-O-β-d-glucuronide.

  • ↵ Embedded Image The online version of this article (available at http://dmd.aspetjournals.org) contains supplemental material.

    • Received November 11, 2005.
    • Accepted February 22, 2006.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 34 (6)
Drug Metabolism and Disposition
Vol. 34, Issue 6
1 Jun 2006
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Research ArticleArticle

ABSORPTION AND METABOLISM OF ASTRAGALI RADIX DECOCTION: IN SILICO, IN VITRO, AND A CASE STUDY IN VIVO

Feng Xu, Yue Zhang, Shengyuan Xiao, Xiaowei Lu, Donghui Yang, Xiaoda Yang, Changling Li, Mingying Shang, Pengfei Tu and Shaoqing Cai
Drug Metabolism and Disposition June 1, 2006, 34 (6) 913-924; DOI: https://doi.org/10.1124/dmd.105.008300

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Research ArticleArticle

ABSORPTION AND METABOLISM OF ASTRAGALI RADIX DECOCTION: IN SILICO, IN VITRO, AND A CASE STUDY IN VIVO

Feng Xu, Yue Zhang, Shengyuan Xiao, Xiaowei Lu, Donghui Yang, Xiaoda Yang, Changling Li, Mingying Shang, Pengfei Tu and Shaoqing Cai
Drug Metabolism and Disposition June 1, 2006, 34 (6) 913-924; DOI: https://doi.org/10.1124/dmd.105.008300
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