ARALIACEAE Panax ginseng  C.A. Mey.

 Synonym

    none ...
 Thai / English name

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[1] MOLECULAR MECHANISMS GOVERNING DIFFERENT PHARMACOKINETICS OF GINSENOSIDES AND POTENTIAL FOR GINSENOSIDE-PERPETRATED HERB-DRUG INTERACTIONS ON OATP1B3.
JIANG,RONGRONG;DONG,JIAJIA;LI,XIUXUE;ET AL.
BR J PHARMACOL TOXICOL 2015 Vol.172(4),1059-73  $58311 [Full]

Part Used : ราก
Activity : DRUG INTERACTION
Solvent/Active Compound : ginsenoside Rg1, ginsenoside Re, notoginsenoside R1, ginsenosides Rb1, Rc, Rd
Type of experiment : in vitro
Type of animal : -
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : -
Dose/Conc.(herb) : 50 micromolar
Duration : The incubation time was set at 5 min
Type of interaction : Pharmacokinetics
Interaction with drug : Rifampicin*/Rifampin
Dose/Conc.(drug) : 10 micromolar
Result : Positive
Remark : Result: The ppt-type ginsenoside Rg1, ginsenoside Re and notoginsenoside R1 were found to be substrates of human OATP1B3, rather than those of human OATP1B1. Ginsenosides Rb1, Rc and Rd were not transported by OATP1B3 and OATP1B1. The ppt-type ginsenoside Rg1, ginsenoside Re and notoginsenoside R1 exhibited weak inhibitory properties towards the OATP1B transporters (IC50 values > 39 micromolar).

Part Used : ราก
Activity : DRUG INTERACTION
Solvent/Active Compound : ginsenoside Rg1, ginsenoside Re, notoginsenoside R1, ginsenosides Rb1, Rc, Rd
Type of experiment : in vitro
Type of animal : -
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : -
Dose/Conc.(herb) : 50 micromolar
Duration : The incubation time was set at 5 min
Type of interaction : Pharmacokinetics
Interaction with drug : Rifampicin*/Rifampin
Dose/Conc.(drug) : 10 micromolar
Result : Positive
Remark : Result: The Km values of the ppt-type ginsenosides for rat Oatp 1b2 were slightly greater than those for human OATP1B3. The Oatp 1b2-mediated uptake of the ppt-type ginsenosides was also inhibited competitively be rifampin. These ABC transporters did not exhibit any significant activity towards the transports of the ppd-type ginsenosides Rb1, Rc and Rd.

Part Used : ราก
Activity : DRUG INTERACTION
Solvent/Active Compound : ginsenoside Rg1, ginsenoside Re, notoginsenoside R1, ginsenosides Rb1, Rc, Rd
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : The individual compounds at 2.5 micromol/kg
Duration : In the first rat study, serial blood samples (60 microlitre; 0, 5, 15, 30 min, 1, 2, 4, 6, 8, 10 and 24 h) were collected after dosing and heparinized.
Type of interaction : Pharmacokinetics
Interaction with drug : Rifampicin*/Rifampin
Dose/Conc.(drug) : 20 mg/kg i.v.
Result : Positive
Remark : Result: Rifampin is an OATP/Oatp inhibitor and substrate. There were significant differences between the ppt-type ginsenosides (ginsenoside Rg1, ginsenoside Re and notoginsenoside R1) and the ppd-type ginsenosides (ginsenosides Rb1, Rc and Rd) in the systemic exposure and elimination kinetics after i.v. dosing with the individual compounds at 2.5 micromol/kg. This was shown by the plasma AUC0-inf and t1/2 values of the latter, which were 105-368 times and 26-88 times, respectively, greater than those of the former. To determine the role of the rapid hepatobiliary excretion of the ppt-type ginsenosides in the preceding differences relative to their ppd-type counterparts, rats were treated with rifampin. The treatment led to slowed biliary excretion of the ppt-type ginsenosides.

Part Used : ราก
Activity : DRUG INTERACTION
Solvent/Active Compound : ginsenoside Rg1, ginsenoside Re, notoginsenoside R1, ginsenosides Rb1, Rc, Rd
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : The individual compounds at 2.5 micromolar/kg
Duration : In the second rat study, bile samples were collected from rats between 0-2, 2-6, 6-12 and 12-24 h after dosing and were weighed.
Type of interaction : Pharmacokinetics
Interaction with drug : Rifampicin*/Rifampin
Dose/Conc.(drug) : 20 mg/kg i.v.
Result : Positive
Remark : Result: Rifampin is an OATP/Oatp inhibitor and substrate. There were significant differences between the ppt-type ginsenosides (ginsenoside Rg1, ginsenoside Re and notoginsenoside R1) and the ppd-type ginsenosides (ginsenosides Rb1, Rc and Rd) in the systemic exposure and elimination kinetics after i.v. dosing with the individual compounds at 2.5 micromol/kg. This was shown by the plasma AUC0-inf and t1/2 values of the latter, which were 105-368 times and 26-88 times, respectively, greater than those of the former. To determine the role of the rapid hepatobiliary excretion of the ppt-type ginsenosides in the preceding differences relative to their ppd-type counterparts, rats were treated with rifampin. The treatment led to slowed biliary excretion of the ppt-type ginsenosides. This was indicated by the CLB values of the ppt-type ginsenosides in the rifampin-treated rats, which were only 3.1-10.6% of those in the control rats.

Part Used : ราก
Activity : DRUG INTERACTION
Solvent/Active Compound : ginsenoside Rg1, ginsenoside Re, notoginsenoside R1, ginsenosides Rb1, Rc, Rd
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : The individual compounds at 2.5 micromolar/kg
Duration : In the third rat study, urine samples were collected at 0-8 and 8-24 h after dosing and were weighed.
Type of interaction : Pharmacokinetics
Interaction with drug : Rifampicin*/Rifampin
Dose/Conc.(drug) : 20 mg/kg i.v.
Result : Positive
Remark : Result: Rifampin is an OATP/Oatp inhibitor and substrate. There were significant differences between the ppt-type ginsenosides (ginsenoside Rg1, ginsenoside Re and notoginsenoside R1) and the ppd-type ginsenosides (ginsenosides Rb1, Rc and Rd) in the systemic exposure and elimination kinetics after i.v. dosing with the individual compounds at 2.5 micromol/kg. This was shown by the plasma AUC0-inf and t1/2 values of the latter, which were 105-368 times and 26-88 times, respectively, greater than those of the former. To determine the role of the rapid hepatobiliary excretion of the ppt-type ginsenosides in the preceding differences relative to their ppd-type counterparts, rats were treated with rifampin. The treatment led to slowed biliary excretion of the ppt-type ginsenosides. This was indicated by the CLB values of the ppt-type ginsenosides in the rifampin-treated rats, which were only 3.1-10.6% of those in the control rats.


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