ฐานข้อมูลอันตรกิริยาระหว่างสมุนไพรกับยาแผนปัจจุบัน

Part Used : ไม่ระบุ

Activity : UDP-GLUCURONYL TRANSFERASE INHIBITION

Solvent/Active Compound : Spray-dried 50% methanolic powder of Orthosiphon stamineus (sinensitin, eupatorin and 3'-hydroxy-5,6,7,4'-tetramethoxyflavone and rosmarinic acid)

Type of experiment : in vitro

Type of animal : -

Type of study : -

N(Total) : -

N(Treatment) : -

Sex : -

Age : -

Route : -

Dose/Conc.(herb) : Final concentrations of Orthosiphon stamineus extracts used were 0.01, 0.10, 1.0, 10 and 50 micrograms/mL

Duration : -

Type of interaction : Pharmacokinetics

Interaction with drug : -

Dose/Conc.(drug) : -

Result : Positive

Remark : Result: For Orthosiphon stamineus extract, the inhibitory potential was in the order: UGT1A7 > UGT1A1 > UGT1A6 > UGT1A8. The IC50 values for UGT1A3, UGT1A10, UGT2B7 and UGT2B15 were however higher than 50 micrograms/mL. This isolform most sensitive to the inhibitory effect of Orthosiphon stamineus extract was UGT1A7. Orthosiphon stamineus at 10 micrograms/mL reduced the activity of UGT1A7 by 60%. UGT1A7 is a non-hepatic glucuronosyltransferase which is responsible for the glucuronidation of mycophenolic acid, a standard immunosuppressive drug. Orthosiphon stamineus extract showed less than 70% inhibition of UGT2B15, so the IC50 values were >50 micrograms/mL.

Note : The potential inhibitory effects of the extracts on the activity of each of the UGT isoforms (recombinant human UGTs, UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A10, UGT2B7 and UGT2B15) were investigated using glucuronidation of 4-methylumbelliferone (4MU) as the substrate.

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