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Part Used : รากActivity : P-GLYCOPROTEIN INHIBITIONSolvent/Active Compound : 18beta-glycyrrhetic acid (18beta-GA), 18alpha-glycyrrhetic acid (18alpha-GA)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 50 micromolarsDuration : -Type of interaction : PharmacokineticsInteraction with drug : DigoxinDose/Conc.(drug) : -Result : PositiveRemark : Result: The inhibitory effects on P-gp mediated digoxin transport were investigated in MDR1-MDCKII cells. Emodin, 18 beta-GA, DAG, and 20 (S)-GF1 exhibited significant inhibition (> 50%) on P-gp. However, the isomers or analogs of the 4 herbal constituents (chrysophanol, 18alpha-GA, AG, and Rh1) and the remaining tested compounds relatively weak inhibition on digoxin transport in this cell model. The concentraion-dependent inhibition on P-gp-mediated digoxin transport was further investigated for emodin, 18beta-GA, DAG, and 20(S)-GF1. Emodin was the strongest herbal inhibitor of P-gp, followed by 18beta-GA, 20(S)-GF1 and DAG. Consistent with the data obtained from MDR1-MDCKII cells, emodin, 18 beta-GA, DAG, and 20(S)-GF1 significantly inhibited digoxin transport (>50%), while chrysophanol, 18alpha-GA, AG, and Rh1 showed no effects or relatively weak inhibition on P-gp.
Part Used : รากActivity : P-GLYCOPROTEIN INHIBITIONSolvent/Active Compound : 18 beta-glycyrrhetic acid (18beta-GA)Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 5-100 micromolarsDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: 18 beta-GA and 20(S)-GF1 did not show any stimulation at low concentraions, but exhibited an inhibition at 100 micromolars. The effects of 18beta-GA and 20(S)-GF1 on verapamil-stimulated P-gp ATPase activity were also investigated. The results showed that both herbal inhibitors exhibited concentration-dependent inhibition on verapamil-stimulated P-gp ATPase activity. Furthermore, 18beta-GA at 100 micromolars reduced the P-gp ATPase activity close to basal level.
Part Used : รากActivity : P-GLYCOPROTEIN INHIBITIONSolvent/Active Compound : 18beta-glycyrrhetic acid (18beta-GA), 18alpha-glycyrrhetic acid (18alpha-GA)Type of experiment : in silicoType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Although the 18-hydrogen atom of GA did not interact with any amino acid residues of P-gp, different binding conformations were observed for 18beta-GA and 18alpha-GA. Furthermore, 18beta-GA interacted with Gln191 via two strong hydrogen bonds, while there was no potential interaction except Van der Waals between 18alpha-GA and P-gp.