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Pharmacokinetic interactions of herbs with cytochrome p450 and p-glycoprotein.

Cho HJ, Yoon IS - Evid Based Complement Alternat Med (2015)

Bottom Line: The concurrent use of drugs and herbal products is becoming increasingly prevalent over the last decade.Several herbal products have been known to modulate cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) which are recognized as representative drug metabolizing enzymes and drug transporter, respectively.The main focus is placed on previous works on the ability of herbal extracts and their phytochemicals to modulate the expression and function of CYP and P-gp in several in vitro and in vivo animal and human systems.

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy, Kangwon National University, Chuncheon 200-701, Republic of Korea.

ABSTRACT
The concurrent use of drugs and herbal products is becoming increasingly prevalent over the last decade. Several herbal products have been known to modulate cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) which are recognized as representative drug metabolizing enzymes and drug transporter, respectively. Thus, a summary of knowledge on the modulation of CYP and P-gp by commonly used herbs can provide robust fundamentals for optimizing CYP and/or P-gp substrate drug-based therapy. Herein, we review ten popular medicinal and/or dietary herbs as perpetrators of CYP- and P-gp-mediated pharmacokinetic herb-drug interactions. The main focus is placed on previous works on the ability of herbal extracts and their phytochemicals to modulate the expression and function of CYP and P-gp in several in vitro and in vivo animal and human systems.

No MeSH data available.


Related in: MedlinePlus

Chemical structures of glycyrrhizin (a) and glycyrrhetic acid (b).
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Related In: Results  -  Collection


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fig3: Chemical structures of glycyrrhizin (a) and glycyrrhetic acid (b).

Mentions: The root of Glycyrrhiza glabra (licorice) is used as a herbal medicine for the treatment of peptic ulcer and cough and as a food additive for sweetening candies, beverages, and chewing gums [6, 51]. The main phytochemicals of licorice include glycyrrhizin (Figure 3(a)), liquiritigenin, coumarins, stilbenoids, fatty acids, phenols, and sterols [52]. Glycyrrhizin is metabolized by intestinal flora into its pharmacologically active form, glycyrrhetinic acid (Figure 3(b)). Licorice is known to have antimalarial, ulcer-healing, immunosuppressive, antihepatotoxic, antianemic, and anti-inflammatory properties [6, 53]. In mice and rats, multiple oral doses of licorice extract during 4 or 10 days induced the mRNA and protein expression of CYP3A and activity of CYP1A2, 2B1, and 3A [54]. Concurrent administration of glycyrrhizin altered the oral pharmacokinetics of midazolam in healthy male subjects possibly by a modest induction of CYP3A4 [55]. Moreover, glycyrrhetinic acid inhibited P-gp-mediated efflux of daunorubicin in P-gp-overexpressing KB-C2 cells [56].


Pharmacokinetic interactions of herbs with cytochrome p450 and p-glycoprotein.

Cho HJ, Yoon IS - Evid Based Complement Alternat Med (2015)

Chemical structures of glycyrrhizin (a) and glycyrrhetic acid (b).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4302358&req=5

fig3: Chemical structures of glycyrrhizin (a) and glycyrrhetic acid (b).
Mentions: The root of Glycyrrhiza glabra (licorice) is used as a herbal medicine for the treatment of peptic ulcer and cough and as a food additive for sweetening candies, beverages, and chewing gums [6, 51]. The main phytochemicals of licorice include glycyrrhizin (Figure 3(a)), liquiritigenin, coumarins, stilbenoids, fatty acids, phenols, and sterols [52]. Glycyrrhizin is metabolized by intestinal flora into its pharmacologically active form, glycyrrhetinic acid (Figure 3(b)). Licorice is known to have antimalarial, ulcer-healing, immunosuppressive, antihepatotoxic, antianemic, and anti-inflammatory properties [6, 53]. In mice and rats, multiple oral doses of licorice extract during 4 or 10 days induced the mRNA and protein expression of CYP3A and activity of CYP1A2, 2B1, and 3A [54]. Concurrent administration of glycyrrhizin altered the oral pharmacokinetics of midazolam in healthy male subjects possibly by a modest induction of CYP3A4 [55]. Moreover, glycyrrhetinic acid inhibited P-gp-mediated efflux of daunorubicin in P-gp-overexpressing KB-C2 cells [56].

Bottom Line: The concurrent use of drugs and herbal products is becoming increasingly prevalent over the last decade.Several herbal products have been known to modulate cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) which are recognized as representative drug metabolizing enzymes and drug transporter, respectively.The main focus is placed on previous works on the ability of herbal extracts and their phytochemicals to modulate the expression and function of CYP and P-gp in several in vitro and in vivo animal and human systems.

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy, Kangwon National University, Chuncheon 200-701, Republic of Korea.

ABSTRACT
The concurrent use of drugs and herbal products is becoming increasingly prevalent over the last decade. Several herbal products have been known to modulate cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) which are recognized as representative drug metabolizing enzymes and drug transporter, respectively. Thus, a summary of knowledge on the modulation of CYP and P-gp by commonly used herbs can provide robust fundamentals for optimizing CYP and/or P-gp substrate drug-based therapy. Herein, we review ten popular medicinal and/or dietary herbs as perpetrators of CYP- and P-gp-mediated pharmacokinetic herb-drug interactions. The main focus is placed on previous works on the ability of herbal extracts and their phytochemicals to modulate the expression and function of CYP and P-gp in several in vitro and in vivo animal and human systems.

No MeSH data available.


Related in: MedlinePlus