Simultaneous determination of intestinal permeability and potential drug interactions of complex mixtures using Caco-2 cells and high-resolution mass spectrometry: Studies with Rauwolfia serpentina extract

Chemico-biological Interactions
Thomas J Flynn, Sanah N Vohra

Abstract

Caco-2 cells are a commonly used model for estimating the intestinal bioavailability of single chemical entity pharmaceuticals. Caco-2 cells, when induced with calcitriol, also express other biological functions such as phase I (CYP) and phase II (glucuronosyltransferases) drug metabolizing enzymes which are relevant to drug-supplement interactions. Intestinal bioavailability is an important factor in the overall safety assessment of products consumed orally. Foods, including herbal dietary supplements, are complex substances with multiple chemical components. Because of potential interactions between components of complex mixtures, more reliable safety assessments can be obtained by studying the commercial products "as consumed" rather than by testing individual chemical components one at a time. The present study evaluated the apparent intestinal permeability (Papp) of a model herbal extract, Rauwolfia serpentina, using both whole plant extracts and the individual purified Rauwolfia alkaloids. All test compounds, endpoint substrates, and their metabolites were quantified using liquid chromatography and high-resolution mass spectrometry. The Papp values for individual Rauwolfia alkaloids were comparable whether measured indivi...Continue Reading

Citations

Jan 31, 2020·Frontiers in Pharmacology·Sílvia M IllamolaElena Y Enioutina
May 19, 2020·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Magali AraujoRobert L Sprando
May 18, 2021·Evidence-based Complementary and Alternative Medicine : ECAM·Tong LinLisheng Peng

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