Differential systemic exposure to galangin after oral and intravenous administration to rats

Feng Chen, Yin Feng Tan, Hai Long Li, Zhen Miao Qin, Hong Die Cai, Wei Yong Lai, Xiao Po Zhang, Yong Hui Li, Wei Wei Guan, You Bin Li, Jun Qing Zhang

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Background: Galangin (3,5,7-trihydroxyflavone) is present in high concentrations in herbal medicine such as Alpinia officinarum Hance. Galangin shows multifaceted in vitro and in vivo biological activities. The number and position of hydroxyl groups in this molecule play an important role in these biological activities. However, these hydroxyl groups undergo glucuronidation and sulfation in in vitro assay system. However, the systemic exposure to galangin after dosing in animals and/or humans remains largely unknown. Thus it is not clear whether the galangin exists in the body at concentrations high enough for the biological effects. Furthermore, the metabolite identification and the corresponding plasma pharmacokinetics need to be characterized. Results: Two LC-MS/MS methods were developed and validated and successfully applied to analyze the parent drug molecules and aglycones liberated from plasma samples via β-glucuronidase hydrolysis. Our major findings were as follows: (1) The routes of administration showed significant influences on the systemic exposure of galangin and its metabolites. (2) Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication. (3) Kaempferol conjugates were detected demonstrating that oxidation reaction occurred; however, both glucuronidation and sulfation were more efficient. (4) Oral bioavailability of free parent galangin was very low. Conclusions: Systemic exposure to galangin and its metabolites was different in rat plasma between oral and intravenous administration. Further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.

Original languageEnglish (US)
Article number14
JournalChemistry Central Journal
Volume9
Issue number1
DOIs
StatePublished - Mar 31 2015

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Rats
Metabolites
Bioactivity
Plasmas
Hydroxyl Radical
galangin
Molecules
Pharmacokinetics
Glucuronidase
Hydrolysis
Assays
Animals
Oxidation
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Chemistry(all)

Cite this

Chen, F., Tan, Y. F., Li, H. L., Qin, Z. M., Cai, H. D., Lai, W. Y., ... Zhang, J. Q. (2015). Differential systemic exposure to galangin after oral and intravenous administration to rats. Chemistry Central Journal, 9(1), [14]. https://doi.org/10.1186/s13065-015-0092-5

Differential systemic exposure to galangin after oral and intravenous administration to rats. / Chen, Feng; Tan, Yin Feng; Li, Hai Long; Qin, Zhen Miao; Cai, Hong Die; Lai, Wei Yong; Zhang, Xiao Po; Li, Yong Hui; Guan, Wei Wei; Li, You Bin; Zhang, Jun Qing.

In: Chemistry Central Journal, Vol. 9, No. 1, 14, 31.03.2015.

Research output: Contribution to journalArticle

Chen, F, Tan, YF, Li, HL, Qin, ZM, Cai, HD, Lai, WY, Zhang, XP, Li, YH, Guan, WW, Li, YB & Zhang, JQ 2015, 'Differential systemic exposure to galangin after oral and intravenous administration to rats', Chemistry Central Journal, vol. 9, no. 1, 14. https://doi.org/10.1186/s13065-015-0092-5
Chen, Feng ; Tan, Yin Feng ; Li, Hai Long ; Qin, Zhen Miao ; Cai, Hong Die ; Lai, Wei Yong ; Zhang, Xiao Po ; Li, Yong Hui ; Guan, Wei Wei ; Li, You Bin ; Zhang, Jun Qing. / Differential systemic exposure to galangin after oral and intravenous administration to rats. In: Chemistry Central Journal. 2015 ; Vol. 9, No. 1.
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abstract = "Background: Galangin (3,5,7-trihydroxyflavone) is present in high concentrations in herbal medicine such as Alpinia officinarum Hance. Galangin shows multifaceted in vitro and in vivo biological activities. The number and position of hydroxyl groups in this molecule play an important role in these biological activities. However, these hydroxyl groups undergo glucuronidation and sulfation in in vitro assay system. However, the systemic exposure to galangin after dosing in animals and/or humans remains largely unknown. Thus it is not clear whether the galangin exists in the body at concentrations high enough for the biological effects. Furthermore, the metabolite identification and the corresponding plasma pharmacokinetics need to be characterized. Results: Two LC-MS/MS methods were developed and validated and successfully applied to analyze the parent drug molecules and aglycones liberated from plasma samples via β-glucuronidase hydrolysis. Our major findings were as follows: (1) The routes of administration showed significant influences on the systemic exposure of galangin and its metabolites. (2) Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication. (3) Kaempferol conjugates were detected demonstrating that oxidation reaction occurred; however, both glucuronidation and sulfation were more efficient. (4) Oral bioavailability of free parent galangin was very low. Conclusions: Systemic exposure to galangin and its metabolites was different in rat plasma between oral and intravenous administration. Further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.",
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AU - Zhang, Xiao Po

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AU - Guan, Wei Wei

AU - Li, You Bin

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AB - Background: Galangin (3,5,7-trihydroxyflavone) is present in high concentrations in herbal medicine such as Alpinia officinarum Hance. Galangin shows multifaceted in vitro and in vivo biological activities. The number and position of hydroxyl groups in this molecule play an important role in these biological activities. However, these hydroxyl groups undergo glucuronidation and sulfation in in vitro assay system. However, the systemic exposure to galangin after dosing in animals and/or humans remains largely unknown. Thus it is not clear whether the galangin exists in the body at concentrations high enough for the biological effects. Furthermore, the metabolite identification and the corresponding plasma pharmacokinetics need to be characterized. Results: Two LC-MS/MS methods were developed and validated and successfully applied to analyze the parent drug molecules and aglycones liberated from plasma samples via β-glucuronidase hydrolysis. Our major findings were as follows: (1) The routes of administration showed significant influences on the systemic exposure of galangin and its metabolites. (2) Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication. (3) Kaempferol conjugates were detected demonstrating that oxidation reaction occurred; however, both glucuronidation and sulfation were more efficient. (4) Oral bioavailability of free parent galangin was very low. Conclusions: Systemic exposure to galangin and its metabolites was different in rat plasma between oral and intravenous administration. Further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.

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