title: Differential systemic exposure to galangin after oral and intravenous administration to rats.
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. Graphical abstractGalangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication.
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Feng
authors: F
authors: Chen
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Yin-Feng
authors: YF
authors: Tan
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Hai-Long
authors: HL
authors: Li
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Zhen-Miao
authors: ZM
authors: Qin
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.|Nanjing University of Chinese Medicine, Nanjing, 210046 China.
authors: Hong-Die
authors: HD
authors: Cai
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Wei-Yong
authors: WY
authors: Lai
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Xiao-Po
authors: XP
authors: Zhang
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Yong-Hui
authors: YH
authors: Li
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Wei-Wei
authors: WW
authors: Guan
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: You-Bin
authors: YB
authors: Li
authors: Hainan Provincial Key Laboratory of R&D of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, 571199 China.
authors: Jun-Qing
authors: JQ
authors: Zhang
keywords: Administration routes; Galangin; Glucuronidation; LC-MS/MS; Sulfation