Effect of Korean Red Ginseng extracts on drug-drug interactions

Abstract

BackgroundGinseng has been the subject of many experimental and clinical studies to uncover the diverse biological activities of its constituent compounds. It is a traditional medicine that has been used for its immunostimulatory, antithrombotic, antioxidative, anti-inflammatory, and anticancer effects. Ginseng may interact with concomitant medications and alter metabolism and/or drug transport, which may alter the known efficacy and safety of a drug; thus, the role of ginseng may be controversial when taken with other medications.MethodsWe extensively assessed the effects of Korean Red Ginseng (KRG) in rats on the expression of enzymes responsible for drug metabolism [cytochrome p450 (CYP)] and transporters [multiple drug resistance (MDR) and organic anion transporter (OAT)] in vitro and on the pharmacokinetics of two probe drugs, midazolam and fexofenadine, after a 2-wk repeated administration of KRG at different doses.ResultsThe results showed that 30 mg/kg KRG significantly increased the expression level of CYP3A11 protein in the liver and 100 mg/kg KRG increased both the mRNA and protein expression of OAT1 in the kidney. Additionally, KRG significantly increased the mRNA and protein expression of OAT1, OAT3, and MDR1 in the liver. Although there were no significant changes in the metabolism of midazolam to its major metabolite, 1′-hydroxymidazolam, KRG significantly decreased the systemic exposure of fexofenadine in a dose-dependent manner.ConclusionBecause KRG is used as a health supplement, there is a risk of KRG overdose; thus, a clinical trial of high doses would be useful. The use of KRG in combination with P-glycoprotein substrate drugs should also be carefully monitored.

Pharmacological potential of ginseng and its major component ginsenosides

“…Ginsenosides Rg1, Re, and Rh1 and R1 saponins show better bioavailability than ginsenosides Ra3, Rb1, Rd, Rg3, and Rh2 saponins. In humans, the half-lives (T1/2) of saponins are usually less than 24 hours [ [24] , [25] , [26] ]. Possible drug interactions have been reported between P. ginseng and warfarin, phenelzine, and alcohol.…”

Antiepileptic and anti-neuroinflammatory effects of red ginseng in an intrahippocampal kainic acid model of temporal lobe epilepsy demonstrated by electroencephalography

“…Red ginseng (RG) (Panax ginseng; harvested after at least 6 years) has anti-inflammatory effects and fewer side effects than fresh or white ginseng [4]. Korean red ginseng (KRG) is an effective natural drug that possesses various biological activities, including boosting the immune system[1,5,6]. Ginsenosides are the main ingredients of KRG and their value in neurodegenerative disease has been studied extensively [7].…”

Protection by ginseng saponins against cyclophosphamide‐induced liver injuries in rats by induction of cytochrome P450 expression and mediation of the l‐arginine/nitric oxide pathway based on metabolomics

“…CAA has been found to induce hepatotoxicity, neurotoxicity and nephrotoxicity (McDonald et al, 2003;Rzeski et al, 2004). Some reports about the pharmacokinetic interactions between ginsenosides and cytochrome CYP enzymes revealed that different ginsenosides can affect CYP enzyme activities (Kawase et al, 2009;Kim et al, 2018;Liu et al, 2006). Changes in these activities might affect CP metabolism.…”