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Part Used : ราก

Activity : CYP1A2 INHIBITION

Solvent/Active Compound : cudratricusxanthone A (CTXA)

Type of experiment : in vitro

Type of animal : -

Type of study : -

N(Total) : -

N(Treatment) : -

Sex : -

Age : -

Route : -

Dose/Conc.(herb) : -

Duration : -

Type of interaction : Pharmacokinetics

Interaction with drug : -

Dose/Conc.(drug) : -

Result : Positive

Remark : CTXA reversibly inhibited the CYP1A2-catalyzed phenacetin O-deethylation, CYP2C8-catalyzed paclitqxel 6-hydroxylation, and CYP2C9-catalyzed diclofenac 4'-hydroxylation with half-maximal inhibitory concentration (IC50) values of 3.9, 4.7, and 2.9 micromolar, respectively. The IC50 values did not change under different preincubation conditions. CTXA showed marked dose dependent, but not time-dependent, inhibition of CYP1A2 and 2C9 activities in HLMs. Further, CTXA inhibited CYP2C8 in a non-competitive manner with a Ki value of 2.2 micromolar. Our results showed that CTXA reversibly inhibits CYP1A2, 2C8, and 2C9.

Note : Type of experiment : in pooled human liver microsomes

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