Purpose: To investigate the effect
of Betong watercress and phenethyl isothiocyanate (PEITC)
on the N-demethylation of caffeine (CF) in rats
Methods: Male Wistar rats were
subjected to 2 phases of experiment. Phase I, they
received a single oral dose of CF (10 mg/kg), while in
phase II, they were pretreated with the following
regimens: 10 mg/kg fluvoxamine, i.p.; a single oral dose
of 2, 10, and 20 mg/kg PEITC; 2, 10, and 20 mg/kg PEITC,
once daily for five days; single oral dose of 800 mg/kg
Betong watercress; 800 mg/kg Betong watercress once
daily for five days, before receiving the same dose of
CF as in phase I. Serum concentrations of CF and its
metabolites after 3 h of CF administration were
measured. Caffeine metabolic ratios (CMRs) and ratio of
serum concentration of metabolites to that of CF were
calculated and compared.
Results: CMRs were decreased by a
single pretreatment \with fluvoxamine (30 – 40%), PEITC
(2 - 20 mg/kg) (40 – 55%), and Betong watercress (9 –
22%). The decreases caused by 10 and 20 mg/kg PEITC
were significantly greater than those by fluvoxamine.
CMRs were also decreased after five days of pretreatment
with all doses of PEITC (43 – 69%) and Betong watercress
(28 – 44%). The reduction in metabolic ratio after
single- and multiple PEITC pretreatments was dose- and
time-independent.
Conclusion: Betong watercress and PEITC
inhibit N-demethylation of CF in rats. Such an effect
indicates that they have inhibitory activity on CYP1A2
and CYP2C.
Keywords: Watercress, Phenethyl
isothiocyanate, Caffeine, N-demethylation, Fluvoxamine,
Cytochrome