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Evaluation of plasma stability and pharmacokinetics of parthenolide in rats with LC-MS/MS analysis
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Xuan QIN, Ang CHEN, Jian LU, Yuan-jin ZHANG, Ming-yao LIU, Xin WANG*
Acta Pharmaceutica Sinica | 2017, 52(4) : 609 - 614
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Acta Pharmaceutica Sinica | 2017, 52(4): 609-614
Evaluation of plasma stability and pharmacokinetics of parthenolide in rats with LC-MS/MS analysis
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Xuan QIN, Ang CHEN, Jian LU, Yuan-jin ZHANG, Ming-yao LIU, Xin WANG*
Affiliations
  • Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences, East China Normal University, Shanghai 200241, China
Published: 2017-04-12 doi: 10.16438/j.0513-4870.2016-1006
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Parthenolide is a sesquiterpene lactone derived from the plant feverfew (Tanacetum parthenium) that possesses multiple anti-inflammatory and anti-cancer properties. A specific, sensitive, accurate and precise LC-MS/MS method was developed and validated in the quantitative analysis of parthenolide in rat plasma. A liquid-liquid extraction method was used to separate the analyte and the internal standard (IS, costunolide) from plasma. A water-methanol mobile phase system was utilized in the gradient chromatographic separation. The calibration curve with good linearity (r2 > 0.99) was established between 2 and 128 ng·mL-1 with accuracy and precision within acceptable limits at different QC levels. High extraction recovery was achieved for both parthenolide (89.55%-95.79%) and IS (96.87%). Based on this LC-MS/MS method, the plasma stability and pharmacokinetics of parthenolide were assessed in rats. Parthenolide was proved to be very unstable in rat plasma, and was distributed and eliminated quickly in vivo, with a half-life less than 90 min. A high dose of parthenolide (80 mg·kg-1) resulted in a very low initial concentration (138.86±21.07 ng·mL-1). The systemic exposure of parthenolide (area under the curve) increased disproportionally from 40 mg·kg-1 dose group to 80 mg·kg-1 dose group. The present study may provide helpful information for the development of parthenolide as a drug candidate.

parthenolide  /  costunolide  /  LC-MS/MS  /  plasma stability  /  pharmacokinetics
Xuan QIN, Ang CHEN, Jian LU, Yuan-jin ZHANG, Ming-yao LIU, Xin WANG. Evaluation of plasma stability and pharmacokinetics of parthenolide in rats with LC-MS/MS analysis[J]. Acta Pharmaceutica Sinica, 2017 , 52 (4) : 609 -614 . DOI: 10.16438/j.0513-4870.2016-1006
Year 2017 volume 52 Issue 4
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doi: 10.16438/j.0513-4870.2016-1006
  • Receive Date:2016-10-30
  • Online Date:2026-01-14
  • Published:2017-04-12
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  • Received:2016-10-30
  • Revised:2016-12-30
Affiliations
    Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences, East China Normal University, Shanghai 200241, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
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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