About: A dual function of the furanocoumarin chalepensin in inhibiting Cyp2a and inducing Cyp2b in mice: the protein stabilization and receptor-mediated activation     Goto   Sponge   NotDistinct   Permalink

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  • Chalepensin, a furanocoumarin, is present in several medicinal Rutaceae plants and causes a mechanism-based inhibition of human and mouse cytochrome P450 (P450, CYP) 2A in vitro. To address the in vivo effect, we investigated the effects of chalepensin on multiple hepatic P450 enzymes in C57BL/6JNarl mice. Using cell-based reporter systems, chalepensin at a concentration near unbound plasma concentration activated mouse constitutive androstane receptor (CAR), in agreement with the observed induction of Cyp2b. These findings revealed that suicidal inhibition of Cyp2a5 and the CAR-mediated Cyp2b9/10 induction concurrently occurred in chalepensin-treated mice.
  • Chalepensin, a furanocoumarin, is present in several medicinal Rutaceae plants and causes a mechanism-based inhibition of human and mouse cytochrome P450 (P450, CYP) 2A in vitro. To address the in vivo effect, we investigated the effects of chalepensin on multiple hepatic P450 enzymes in C57BL/6JNarl mice. Using cell-based reporter systems, chalepensin at a concentration near unbound plasma concentration activated mouse constitutive androstane receptor (CAR), in agreement with the observed induction of Cyp2b. These findings revealed that suicidal inhibition of Cyp2a5 and the CAR-mediated Cyp2b9/10 induction concurrently occurred in chalepensin-treated mice. (en)
Title
  • A dual function of the furanocoumarin chalepensin in inhibiting Cyp2a and inducing Cyp2b in mice: the protein stabilization and receptor-mediated activation
  • A dual function of the furanocoumarin chalepensin in inhibiting Cyp2a and inducing Cyp2b in mice: the protein stabilization and receptor-mediated activation (en)
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  • A dual function of the furanocoumarin chalepensin in inhibiting Cyp2a and inducing Cyp2b in mice: the protein stabilization and receptor-mediated activation
  • A dual function of the furanocoumarin chalepensin in inhibiting Cyp2a and inducing Cyp2b in mice: the protein stabilization and receptor-mediated activation (en)
skos:notation
  • RIV/75010330:_____/12:00009839!RIV13-MZ0-75010330
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  • V
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  • 12
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  • 120179
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  • RIV/75010330:_____/12:00009839
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  • chalepensin; CYP2A; CYP2B; protein stability; mice (en)
http://linked.open.../riv/klicoveSlovo
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  • DE - Spolková republika Německo
http://linked.open...ontrolniKodProRIV
  • [BD60E8675779]
http://linked.open...i/riv/nazevZdroje
  • Archives of toxicology
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  • 86
http://linked.open...iv/tvurceVysledku
  • Souček, Pavel
  • Chen, C. C.
  • Ueng, Y.F.
  • Hsu, C. C.
  • Lim, Y. P.
  • Lo, W. S.
  • Xie, W.
  • Yun, C. H.
http://linked.open...ain/vavai/riv/wos
  • 000310990200013
issn
  • 0340-5761
number of pages
http://bibframe.org/vocab/doi
  • 10.1007/s00204-012-0902-7
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