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The inhibition of carboxylesterases by praeruptorin C, D and E
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Zuo DU, Da-wei CHEN, Zhi-wei FU, Zhong-ze FANG*, Kun YANG*
Acta Pharmaceutica Sinica | 2017, 52(1) : 66 - 70
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Acta Pharmaceutica Sinica | 2017, 52(1): 66-70
• SPECIAL REPORTS •
The inhibition of carboxylesterases by praeruptorin C, D and E
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Zuo DU, Da-wei CHEN, Zhi-wei FU, Zhong-ze FANG*, Kun YANG*
Affiliations
  • School of Public Health, Tianjin Medical University, Tianjin 300070, China
Published: 2017-01-12 doi: 10.16438/j.0513-4870.2016-1024
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Praeruptorin C (PC), D (PD) and E (PE) are important compounds extracted from Peucedanum praeruptorum DUNN and have been reported to exert multiple pharmacological activities. The present study is purposed to determine the inhibition of PC, PD and PE on the activity of important phase I metabolic enzymes-carboxylesterases (CES). In vitro human liver microsomes (HLM) incubation system was used to determine the inhibition potential of PC, PD and PE on the activity of CES1 and CES2. Inhibition behaviour was determined, and in vitro-in vivo extrapolation was performed by using the combination of in vitro inhibition kinetic parameter (Ki) and in vivo exposure level of PD. PD exhibited the strongest inhibition on the activity of CES1, with 81.7% activity inhibited by 100 μmol·L-1 of PD. PD noncompetitively inhibited the activity of CES1 with the Ki to be 122.2 μmol·L-1, indicating inhibition potential of PD towards CES1 in vivo. Therefore, closely monitoring the endogenous metabolic disorders caused by PD and interaction between PD and drugs mainly undergoing CES1-catalyzed metabolism is very necessary.

praeruptorin C  /  praeruptorin D  /  praeruptorin E  /  carboxylesterase 1  /  carboxylesterase 2  /  herbdrug interaction
Zuo DU, Da-wei CHEN, Zhi-wei FU, Zhong-ze FANG, Kun YANG. The inhibition of carboxylesterases by praeruptorin C, D and E[J]. Acta Pharmaceutica Sinica, 2017 , 52 (1) : 66 -70 . DOI: 10.16438/j.0513-4870.2016-1024
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doi: 10.16438/j.0513-4870.2016-1024
  • Receive Date：2016-10-17
  • Online Date：2026-01-14
  • Published：2017-01-12
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  • Received：2016-10-17
  • Revised：2016-12-12
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    School of Public Health, Tianjin Medical University, Tianjin 300070, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
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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