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in vitro metabolism of daphnetin in rat liver S9 fractions
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Si-cheng LIANG1, 2, Guang-bo GE1, *, Yang-liu XIA1, Xiao-yi QI3, *, Ao-xue WANG3, Cai-xia TU3, Ling YANG1
Acta Pharmaceutica Sinica | 2017, 52(2) : 291 - 295
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Acta Pharmaceutica Sinica | 2017, 52(2): 291-295
• Pharmaceutical Analysis •
in vitro metabolism of daphnetin in rat liver S9 fractions
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Si-cheng LIANG1, 2, Guang-bo GE1, *, Yang-liu XIA1, Xiao-yi QI3, *, Ao-xue WANG3, Cai-xia TU3, Ling YANG1
Affiliations
  • 1. Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China
  • 2. Second Affiliated Hospital of Dalian Medical University, Dalian 116027, China
  • 3. University of Chinese Academy of Sciences, Beijing 100049, China
Published: 2017-02-12 doi: 10.16438/j.0513-4870.2016-0847
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Daphnetin is quickly eliminated in rats after dosing, but the mechanism remains unclear. This study was aimed to investigate the in vitro metabolism of daphnetin using rat liver S9 fractions (RLS9). The metabolites formed in RLS9 were identified and the kinetic parameters for different metabolic pathways were determined. HPLC-DAD-MS analysis showed that daphnetin was biotransformed to six metabolites, which were identified as 7 or 8 mono-glucuronide and mono-sulfate, 8-methylate, and 7-suflo-8-methylate. Methylation and glucuronidation of daphnetin exhibited the Michaelis-Menten kinetic characteristics, whereas the substrate inhibition kinetic and the two-site kinetic were observed for 8-sulfate and 7-sulfate formations. Of the 3 conjugation pathways, the intrinsic clearance rate for sulfation was highest, followed by methylation and glucuronidation. By in vitro-in vivo extrapolation of the kinetic data measured in RLS9, the hepatic clearance were estimated to be 54.9 mL·min-1·kg-1 which is comparable to the system clearance (58.5 mL·min-1·kg-1) observed in rats. In conclusions, the liver might be the main site for daphnetin metabolism in rats. Sulfation, methylation and glucuronidation are important pathways of the hepatic metabolism of daphnetin in rats.

daphnetin  /  phase II enzyme  /  enzyme kinetics  /  hepatic clearance
Si-cheng LIANG, Guang-bo GE, Yang-liu XIA, Xiao-yi QI, Ao-xue WANG, Cai-xia TU, Ling YANG. in vitro metabolism of daphnetin in rat liver S9 fractions[J]. Acta Pharmaceutica Sinica, 2017 , 52 (2) : 291 -295 . DOI: 10.16438/j.0513-4870.2016-0847
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Article Info
doi: 10.16438/j.0513-4870.2016-0847
  • Receive Date：2016-09-10
  • Online Date：2026-01-14
  • Published：2017-02-12
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History
  • Received：2016-09-10
  • Revised：2016-11-18
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Affiliations
    1. Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China
    2. Second Affiliated Hospital of Dalian Medical University, Dalian 116027, China
    3. University of Chinese Academy of Sciences, Beijing 100049, China
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表12种不同金属材料的力学参数
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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