Cytochrome P450 inhibitory potential of Triphala—A Rasayana from Ayurveda

• Published in: Journal of ethnopharmacology Vol. 133; no. 1; pp. 120 - 125
• Main Authors: Ponnusankar, S., Pandit, Subrata, Babu, Ramesh, Bandyopadhyay, Arun, Mukherjee, Pulok K.
• Format: Journal Article
• Language: English
• Published: Shannon Elsevier Ireland Ltd 07-01-2011; Amsterdam; New York: Elsevier; Elsevier
• Subjects: animal models; Animals; Antioxidants - pharmacology; Ayurveda; Ayurvedic medicine; Biological and medical sciences; chemical concentration; Cytochrome; cytochrome P-450; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P450; drug formulations; drug interactions; drug-modulating enzymes; Drugs; enzyme inhibition; enzyme inhibitors; Enzymes; Ethanol; Fluorescence; Fruit; gallic acid; General pharmacology; Herb-Drug Interactions; Herbal formulation; herbal medicines; Herb–drug interaction; Inhibition; inhibitory concentration 50; isozymes; Liver; Male; Medical sciences; medicinal plants; Medicine, Ayurvedic; metabolism; microsomes; Microsomes, Liver - drug effects; Microsomes, Liver - enzymology; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Phytotherapy; Plant Extracts - chemistry; Plant Extracts - pharmacology; Rasayana; Rats; Rats, Wistar; reversed-phase high performance liquid chromatography; Safety; synergism; Triphala; Asia; India; Ayurveda; Triphala; Cytochrome P450; EO; TB; Herb–drug interaction; TC; Rasayana; Herbal formulation; CYP450; TL; Inhibition; Safety; Herb-drug interaction; Enzyme; Pharmacognosy; Toxicity; Medicinal plant; Folk medicine; Formulation; Ayurvedic medicine; Plant origin; Drug interaction
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2010.09.022

‘
Triphala’ is one of the age-old, most commonly used polyherbal preparation from Ayurveda as Rasayana drug.
This study was aimed at evaluating the effect of ‘
Triphala’ on drug modulating enzymes to assess its safety through its potential to interact with co-administered drugs.
The cytochrome P450 inhibitory effect of ‘
triphala’ formulation was investigated on rat liver microsomes using CYP450–CO complex assay and on individual isoform such as CYP3A4 and 2D6 using fluorescence screening. RP-HPLC method was developed to standardize ‘
triphala’ and its individual components using gallic acid as analytical marker compound.
RP-HPLC analysis demonstrated the presence of gallic acid (4.30
±
2.09
mg/g) in the formulation. The formulation showed 23% inhibition of the rat liver microsomes through CYP450–CO complex assay which is comparatively less when compared with the individual components. Further, the effect of standardized formulation dissolved in ethanol showed CYP3A4 and CYP2D6 inhibitory activity at the IC
50 values of 119.65
±
1.91
μg/ml and 105.03
±
0.98
μg/ml respectively. Gallic acid was also found to inhibit both the isoforms at the IC
50 values of 87.24
±
1.11
μg/ml and 92.03
±
0.38
μg/ml respectively.
Various concentrations of the formulation and its individual components showed significantly less inhibitory activity (
p
<
0.001) on individual isoforms when compared with the positive control. Assessment on the
in vitro effect of ‘
triphala’ on drug modulating enzymes has important implications for predicting the likelihood of herb–drug interactions if these are administered concomitantly.