Inhibitory interactions of Aspalathus linearis (Rooibos) extracts and compounds, aspalathin and Z-2-(β-D-glucopyranosyloxy)-3-phenylpropenoic acid, on cytochromes metabolizing hypoglycemic and hypolipidemic drugs

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dc.contributor.authorPatel, Oelfahen_ZA
dc.contributor.authorMuller, Christoen_ZA
dc.contributor.authorJoubert, Elizabethen_ZA
dc.contributor.authorLouw, Johanen_ZA
dc.contributor.authorRosenkranz, Bernden_ZA
dc.contributor.authorAwortwe, Charlesen_ZA
dc.date.accessioned2017-07-19T08:41:59Z
dc.date.available2017-07-19T08:41:59Z
dc.date.issued2016-11-12
dc.descriptionCITATION: Patel, O. et al. 2016. Inhibitory interactions of Aspalathus linearis (Rooibos) extracts and compounds, aspalathin and Z-2-(β-D-glucopyranosyloxy)-3-phenylpropenoic acid, on cytochromes metabolizing hypoglycemic and hypolipidemic drugs. Molecules, 21(11):1515, doi:10.3390/molecules21111515.
dc.descriptionThe original publication is available at http://www.mdpi.com/journal/molecules
dc.description.abstractRooibos extract, due to its glucose and lipid lowering effects, has potential as a nutraceutical for improvement of metabolic dysfunction. Potential herb-drug interactions as a result of the use of natural products are of increasing concern. Cytochrome P450 enzymes, CYP2C8, CYP2C9, and CYP3A4, are important in the metabolism of hypoglycemic drugs, such as thiazolidinediones (TZDs) and sulfonylureas, and hypocholesterolemic drugs, such as atorvastatin. This study investigated the effects of rooibos extracts, prepared from “unfermented” and “fermented” rooibos plant material and two of the major bioactive compounds, Z-2-(β-d-glucopyranosyloxy)-3-phenylpropenoic acid (PPAG) and aspalathin (ASP), on Vivid® recombinant CYP450 enzymes. Unfermented (GRT) and fermented (FRE) rooibos extracts inhibited the activity of CYP2C8 (7.69 ± 8.85 µg/mL and 8.93 ± 8.88 µg/mL, respectively) and CYP3A4 (31.33 ± 4.69 µg/mL and 51.44 ± 4.31 µg/mL, respectively) based on their respective IC50 concentrations. Both extracts dose- and time-dependently inhibited CYP2C8 activity, but only time-dependently inhibited CYP2C9. CYP3A4 showed concentration-dependent inhibition by ASP, GRT, and FRE at 25, 50, and 100 µg/mL concentrations. ASP, GRT, and FRE time-dependently inhibited CYP3A4 activity with GRT and FRE showing a more potent time-dependent inhibition, comparable to erythromycin. These findings suggest that herb-drug interactions may occur when nutraceuticals containing rooibos extracts are co-administered with hypoglycemic drugs such as TZDs, sulfonylureas, and dyslipidemic drug, atorvastatin.en_ZA
dc.description.urihttp://www.mdpi.com/1420-3049/21/11/1515
dc.description.versionPublisher's version
dc.format.extent13 pages
dc.identifier.citationPatel, O. et al. 2016. Inhibitory interactions of Aspalathus linearis (Rooibos) extracts and compounds, aspalathin and Z-2-(β-D-glucopyranosyloxy)-3-phenylpropenoic acid, on cytochromes metabolizing hypoglycemic and hypolipidemic drugs. Molecules, 21(11):1515, doi:10.3390/molecules21111515.
dc.identifier.issn1420-3049 (online)
dc.identifier.otherdoi:10.3390/molecules21111515
dc.identifier.urihttp://hdl.handle.net/10019.1/101993
dc.language.isoen_ZAen_ZA
dc.publisherMDPI
dc.rights.holderAuthors retain copyright
dc.subjectAspalathus linearisen_ZA
dc.subjectRooibos teaen_ZA
dc.subjectMedicinal plantsen_ZA
dc.subjectCytochrome P-450en_ZA
dc.subjectAspalathinen_ZA
dc.titleInhibitory interactions of Aspalathus linearis (Rooibos) extracts and compounds, aspalathin and Z-2-(β-D-glucopyranosyloxy)-3-phenylpropenoic acid, on cytochromes metabolizing hypoglycemic and hypolipidemic drugsen_ZA
dc.typeArticleen_ZA
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