COMPOSITAE (ASTERACEAE) Carthamus tinctorius  L.

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[1] EFFECTS OF HYDROXYSAFFLOR YELLOW A ON THE ACTIVITY AND MRNA EXPRESSION OF FOUR CYP ISOZYMES IN RATS.
REN-AI XU,ZHI-SHENG XU , REN-SHAN GE
J ETHNOPHARMACOL 2014 Vol.151(),1141-46  $50677 [Full]

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Tolbutamide
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; The pharmacokinetic parameters of tolbutamide in rats showed no significant difference among LSG, LLG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Tolbutamide
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; After pretreatment with HSYA, the t1/2 and Tmax of tolbutamide in HSG were increased significantly by 43.5% and 34.0% (P<0.05) compared to those of BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Tolbutamide
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; The pharmacokinetic parameters of tolbutamide in rats showed no significant difference among LSG, LLG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Tolbutamide
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; The t1/2, Tmax, Cmax and MRT (0-infinity) of tolbutamide in HLG were increased significantly by 74.0%, 53.3%, 45.2%, and 45.9% (P<0.05) compared to those of BCG, CL of tolbutamide in HLG was decreased significantly by 31.2% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg/day
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg/day
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg/day
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Positive
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP2C11 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg/day
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : -
Dose/Conc.(drug) : -
Result : Positive
Remark : Results; compared with BCG, the mRNA expression level of CYP1A2 in LLG and HLG was significantly decreased to 0.68 and 0.46 times, respectively. Meanwhile, the mRNA expression level of CYP2C11 in HLG was significantly decreased to 0.45 times. These results indicated that CYP1A2 and CYP2C11 enzyme activities were inhibited.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.


 หน้า  1