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Research ArticleSpecial Section on Drug Metabolism and the Microbiome

Intestinal Absorption and Metabolism of Epimedium Flavonoids in Osteoporosis Rats

Jing Zhou, Yi Hua Ma, Zhong Zhou, Yan Chen, Ying Wang and Xia Gao
Drug Metabolism and Disposition October 2015, 43 (10) 1590-1600; DOI: https://doi.org/10.1124/dmd.115.064386
Jing Zhou
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Yi Hua Ma
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Zhong Zhou
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Yan Chen
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Ying Wang
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Xia Gao
Multicomponent of Traditional Chinese Medicine and Microecology Research Center (J.Z., Y.H.M., Y.C., Y.W., X.G.) and Department of Orthopaedics (Z.Z.), Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People’s Republic of China
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Abstract

Herba Epimdii is a traditional Chinese medicine used to treat osteoporosis. Its main pharmacological ingredients are flavonoids. In previous studies conducted in healthy animals, we showed that epimedium flavonoids could be hydrolyzed into secondary glycosides or aglycon by intestinal flora or enzymes, thereby enhancing their absorption and antiosteoporosis activity. To study the medicine in the pathologic state, epimedium flavonoids were incubated with intestinal mucosa and feces in vitro and intestinal perfusion in situ to explore the differences in absorption and metabolism between sham and osteoporosis rats. For osteoporosis rats, the hydrolysis rates of icariin, epimedin A, epimedin B, and epimedin C incubated with intestinal flora for 1 hour were reduced by 0.19, 0.26, 0.19, and 0.14, respectively, compared with that in sham rats. Hydrolysis rates were reduced by 0.21, 0.24, 0.08, and 0.31 for icariin, epimedin A, epimedin B, and epimedin C incubated with duodenal enzymes for 1 hour and by 0.13, 0.09, 0.07, and 0.47 for icariin, epimedin A, epimedin B, and epimedin C incubated with jejunum enzymes, respectively, compared with the sham group. In addition, the apparent permeability coefficient and elimination percentage of the four epimedium flavonoids in the duodenum, jejunum, ileum, and colon decreased by 29%–44%, 32%–50%, 40%–56%, and 27%–53% compared with that in sham rats, respectively. The main metabolites of the four epimedium flavonoids were the same for the two groups after intestinal perfusion, or flora and enzyme incubation. In conclusion, the amount and activity of intestinal flora and enzymes changed in ovariectomized rats, which affected the intestinal absorption and hydrolysis of epimedium flavonoids whose structures contain 7-glucose.

Footnotes

    • Received March 19, 2015.
    • Accepted July 1, 2015.
  • J.Z. and Y.H.M contributed equally to this work.

  • This research was supported by the National Natural Science Foundation of China, funded by the Chinese government [Grant 81173557].

  • dx.doi.org/10.1124/dmd.115.064386.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 43 (10)
Drug Metabolism and Disposition
Vol. 43, Issue 10
1 Oct 2015
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Research ArticleSpecial Section on Drug Metabolism and the Microbiome

Absorption and Metabolism of Epimedium Flavonoids

Jing Zhou, Yi Hua Ma, Zhong Zhou, Yan Chen, Ying Wang and Xia Gao
Drug Metabolism and Disposition October 1, 2015, 43 (10) 1590-1600; DOI: https://doi.org/10.1124/dmd.115.064386

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Research ArticleSpecial Section on Drug Metabolism and the Microbiome

Absorption and Metabolism of Epimedium Flavonoids

Jing Zhou, Yi Hua Ma, Zhong Zhou, Yan Chen, Ying Wang and Xia Gao
Drug Metabolism and Disposition October 1, 2015, 43 (10) 1590-1600; DOI: https://doi.org/10.1124/dmd.115.064386
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