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Open AccessArticle

In Vitro Human Metabolism and Inhibition Potency of Verbascoside for CYP Enzymes

Department of Plant and Soil Sciences, University of Pretoria, Pretoria 0002, South Africa
School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio FI-70210, Finland
LC-MS Metabolomics Center, Biocentre, Kuopio, Kuopio FI-70210, Finland
School of Natural Resources, University of Missouri, Columbia, MO 65211, USA
College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru 570015, India
Author to whom correspondence should be addressed.
Academic Editor: Isabel Ferreira
Molecules 2019, 24(11), 2191;
Received: 11 May 2019 / Revised: 30 May 2019 / Accepted: 6 June 2019 / Published: 11 June 2019
(This article belongs to the Collection Bioactive Compounds)
Verbascoside is found in many medicinal plant families such as Verbenaceae. Important biological activities have been ascribed to verbascoside. Investigated in this study is the potential of verbascoside as an adjuvant during tuberculosis treatment. The present study reports on the in vitro metabolism in human hepatic microsomes and cytosol incubations as well as the presence and quantity of verbascoside within Lippia scaberrima. Additionally, studied are the inhibitory properties on human hepatic CYP enzymes together with antioxidant and cytotoxic properties. The results yielded no metabolites in the hydrolysis or cytochrome P450 (CYP) oxidation incubations. However, five different methylated conjugates of verbascoside could be found in S-adenosylmethionine incubation, three different sulphate conjugates with 3′-phosphoadenosine 5′-phosphosulfate (PAPS) incubation with human liver samples, and very low levels of glucuronide metabolites after incubation with recombinant human uridine 5’-diphospho-glucuronosyltransferase (UGT) 1A7, UGT1A8, and UGT1A10. Additionally, verbascoside showed weak inhibitory potency against CYP1A2 and CYP1B1 with IC50 values of 83 µM and 86 µM, respectively. Potent antioxidant and low cytotoxic potential were observed. Based on these data, verbascoside does not possess any clinically relevant CYP-mediated interaction potential, but it has effective biological activity. Therefore, verbascoside could be considered as a lead compound for further drug development and as an adjuvant during tuberculosis treatment. View Full-Text
Keywords: cytochrome P450; verbascoside; metabolism; antioxidant; cytotoxicity; liver cytochrome P450; verbascoside; metabolism; antioxidant; cytotoxicity; liver
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MDPI and ACS Style

Reid, A.-M.; Juvonen, R.; Huuskonen, P.; Lehtonen, M.; Pasanen, M.; Lall, N. In Vitro Human Metabolism and Inhibition Potency of Verbascoside for CYP Enzymes. Molecules 2019, 24, 2191.

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