Skip to main content
Elsevier - PMC COVID-19 Collection logoLink to Elsevier - PMC COVID-19 Collection
. 2011 Dec 25;9(6):461–465. doi: 10.3724/SP.J.1009.2011.00461

Metabolism of Epimedium-derived Flavonoid Glycosides in Intestinal Flora of Rabbits and Its Inhibition by Gluconolactone

Zhi-Hong YAO a,b,**, Ming-Yan LIU a,*, Yi DAI a,b, Yi ZHANG a, Zi-Fei QIN a, Feng-Juan TU c, Xin-Sheng YAO a,b,c
PMCID: PMC7128601

Abstract

Aim

The metabolism of Epimedium-derived flavonoid glycosides (EF, with icariin as the main component) in rabbit intestinal flora and its inhibition by gluconolactone were investigated in this paper to help reveal the metabolic pathway of EF in rabbits and to identify the in vivo bioactive components of EF in the prevention of steroid-associated osteonecrosis.

Methods

EF were incubated at 37 °C anaerobically with rabbit intestinal flora, and then water-saturated ethyl acetate was used for sample extraction at different time points. Furthermore, gluconolactone was added at different concentrations (8, 12 and 16 mg·mL−1) to study its inhibition of the metabolism of EF in rabbit intestinal flora. The separation was performed on a ODS column by gradient elution with acetonitrile-water (including 0.1% formic acid respectively) as mobile phase at detection wavelength of 335 nm.

Results

EF were metabolized to icariside II in 2 h, and then to icaritin when incubated for 8 h; gluconolactone showed the inhibition of EF metabolism in rabbit intestinal flora in a concentration-dependent manner.

Conclusion

EF were found to be metabolized rapidly by hydrolysis of rabbit intestinal flora to produce icariside II and icaritin; and the total inhibition was achieved by gluconolactone at a concentration of 16 mg·mL−1.

Key Words: Epimedium-derived flavonoid glycosides, Prevention of steroid-associated osteonecrosis, Metabolism in rabbit intestinal flora, Gluconolactone, Inhibition

Footnotes

Available online 20 Nov. 2011

Research funding The project was supported by the National Natural Science Foundation of China-Research Grant Council of Hong Kong(No. 30831160510).

These authors have no any conflict of interest to declare.

Contributor Information

Zhi-Hong YAO, Email: yaozhihong5198@163.com.

Ming-Yan LIU, Email: tyaozh@jnu.edu.cn.

References

  • 1.Zhonghuayaohai [M] Harbin Publishing Company; 1998. pp. 1714–1718. [Google Scholar]
  • 2.Wang M, Liu CM, Zhang JF. Effects of Epimedium icariine on rabbit and dog cerebral blood flow [J] J Shenyang Coll Pharm. 1991;8(4):272–276. [Google Scholar]
  • 3.He W, Sun H, Yang B. Immunoregulatory effects of the Herba Epimediia glycoside icariin [J] Arzneimittel-Forsch. 1995;45(8):910–913. [PubMed] [Google Scholar]
  • 4.Zhai YK, Li ZF, Cheng GZ. Current status of the anti-osteoporosis mechanism of icariin [J] Chin J Osteoporosis. 2009;15(7):543–545. 531. [Google Scholar]
  • 5.Zhang G, Qin L, Sheng H. Epimedium-derived phytoestrogen exert beneficial effect on preventing steroid-associated osteonecrosis in rabbits with inhibition of both thrombosis and lipid-deposition [J] Bone. 2007;40:685–692. doi: 10.1016/j.bone.2006.10.026. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 6.Zhang G, Wang XL, Sheng H. Constitutional flavonoids derived from epimedium dose-dependently reduce incidence of steroid-associated osteonecrosis not via direct action by themselves on potential cellular targets [J] PloS ONE. 2009:4. doi: 10.1371/journal.pone.0006419. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 7.Kang B. Microecology [M] Dalian Publishing Company; 1988. p. 95. [Google Scholar]
  • 8.Kobashi K. Metabolism of drug by intestinal bacteria [J] Bifidobacteria Microflora. 1992;11:23. [Google Scholar]
  • 9.Xu W, Zhang YP, Zhang WD. Metabolism of icariin and icariside ii by rat intestinal bacteria in vitro [J] World Sci Technol Mod Tradit Chin Med. 2006;8(6):98–100. 106. [Google Scholar]
  • 10.Liu TH, Wang Y, Wang BX. Metabolism of icariin by intestinal bacteria. Part. I. the transformation of icariin by intestinal flora [J] Chin Tradit Herb Drugs. 2000;31(11):834–836. [Google Scholar]
  • 11.Liu Y, Hu M. Absorption and metabolism of flavonoids in the CACO-2 cell culture model and a perused rat intestinal model [J] Drug Metab Dispos. 2002;30(4):370–377. doi: 10.1124/dmd.30.4.370. [DOI] [PubMed] [Google Scholar]
  • 12.Chen HX, Huang JL, Li J. Characterization of metabolites of worenine in rat biological samples using liquid chromatography-tandem mass spectrometry [J] J Pharm Biomed Anal. 2010;51(1):236–243. doi: 10.1016/j.jpba.2009.08.026. [DOI] [PubMed] [Google Scholar]
  • 13.Akao T, Che QM, Kyoichi K. A purgative action of barbaloin is induced by Eubacterium sp. strain BAR, a human intestinal anaerobe, capable of transforming barbaloin to aloeemodin anthrone [J] Biol Pharm Bull. 1996;19(1):136–138. doi: 10.1248/bpb.19.136. [DOI] [PubMed] [Google Scholar]
  • 14.Shen P, Wong SP, Yong EL. Sensitive and rapid method to quantify icaritin and desmethylicaritin in human serum using gas chromatography–mass spectrometry [J] J Chromatogr B. 2007;857(1):47–52. doi: 10.1016/j.jchromb.2007.06.026. [DOI] [PubMed] [Google Scholar]
  • 15.Shen P, Shih SP, Li L. Simple and sensitive liquid chromatography–tandem mass spectrometry assay for simultaneous measurement of five Epimedium prenylflavonoids in rat sera [J] J Chromatogr B. 2009;877(1–2):71–78. doi: 10.1016/j.jchromb.2008.11.030. [DOI] [PubMed] [Google Scholar]
  • 16.Shen J, Liang BL, Zeng QS. Report on the investigation of lower extremity osteonecrosis with magnetic resonance imaging in recovered severe acute respiratory syndrome in Guangzhou [J] Natl Med J China. 2004;84(21):1814–1817. [PubMed] [Google Scholar]
  • 17.Griffith JF, Antonio GE, Kumta SM. Osteonecrosis of hip and knee in patients with severe acute respiratory syndrome treated with steroids [J] Radiology. 2009;235(1):168–175. doi: 10.1148/radiol.2351040100. [DOI] [PubMed] [Google Scholar]

Articles from Chinese Journal of Natural Medicines are provided here courtesy of Elsevier

RESOURCES