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. 2017:2017:4684962.
doi: 10.1155/2017/4684962. Epub 2017 Nov 13.

"VSports在线直播" Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat

Shunjun Xu  1 , Jiejing Yu  2 , Jingjing Zhan  2 , Liu Yang  1   2 , Longgang Guo  1 , Yijuan Xu  1
Affiliations

Pharmacokinetics, Tissue Distribution, and Metabolism Study of Icariin in Rat (VSports注册入口)

Shunjun Xu et al. Biomed Res Int. 2017.

Abstract

Icariin is one of the predominant flavonoids contained in Herba Epimedii (Yin-yang-huo in Chinese), a well-known Chinese medicine for the treatment of cancers and immune system diseases. Although Herba Epimedii has been widely used in China and there are so many and various research reports on the herbal drug and its main flavones, very limited data is available on the tissue distribution and biotransformation of icariin VSports手机版. In the present study, a liquid chromatographic method combined with electrospray ionization tandem mass spectrometry was developed to quantify the concentration of icariin in rat plasma and various tissues collected at different time points after oral administration of the total flavonoid extract of Herba Epimedii at a dose of 0. 69 g/kg (corresponding to 42 mg/g icariin). Biological samples were processed by simple protein precipitation. Genistein was chosen as internal standard. The method was successfully applied to plasma pharmacokinetic and tissue distribution studies of icariin in rat. As a result, it was worth noting that the tissue distribution characteristics of icariin exhibited a significant gender difference. Moreover, in vivo metabolism of icariin was also investigated. A total of 11 potential metabolites were found in rat feces collected in different time periods after oral and intramuscular administration of icariin. In vivo metabolic pathways were involved in hydrolysis, demethylation, oxidation, and conjugation. The preclinical data would be useful for fully understanding in vivo disposition of this compound and interpreting the mechanism of its biological response. .

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Figures

Figure 1
Figure 1
Chemical structure of icariin (a) and genistein (internal standard, b).
Figure 2
Figure 2
Full scan mass spectrum of icariin (a-1) and internal standard (genistein, b-1); product ion spectrum of icariin (a-2) and internal standard (genistein, b-2).
Figure 3
Figure 3
Representative MRM chromatograms of blank plasma (a-1), blank liver (a-2), blank plasma spiked with IS (b-1), blank liver spiked with IS (b-2), blank plasma spiked with icariin at LOQ (c-1), blank liver spiked with icariin at LOQ (d-1), rat plasma sample obtained at 0.5 h after administration (c-2), and rat liver sample obtained at 0.5 h after administration (d-2).
Figure 4
Figure 4
Plasma concentration versus time profile of icariin in rats (n = 6) following a single oral dose of Herba Epimedii extract (corresponding 42 mg/g icariin).
Figure 5
Figure 5
Tissue distribution of icariin in rats after a single oral dose of Herba Epimedii extract (corresponding 42 mg/g icariin, (a) male rat, (b) female rat).
Figure 6
Figure 6
Representative chromatograms of icariin metabolites in rat feces of 0–24 h: (a) blank feces sample; (b) feces sample after oral administration; and (c) feces sample after intramuscular administration.
Figure 7
Figure 7
Representative LC-MSn spectra of icariin and its metabolites M1–M11 in rat feces.
Figure 8
Figure 8
Proposed metabolic pathways for icariin in rat feces.
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References

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