Abstract

Coumarin (1,2-benzopyrone) is a natural compound whose metabolism in humans was established in the 1970s. However, a new metabolite was recently identified in human plasma, indicating that the metabolism of coumarin has not been completely elucidated. To complement the knowledge of its metabolism, a rapid and sensitive method using UPLC-QTOF-MS was developed. A total of 12 metabolites was identified using MetaboLynxTM software, including eight metabolites not previously reported in human urine. The identified biotransformation included hydroxylation, glucuronidation, sulfation, methylation, and conjugation with N-acetylcysteine. The present work demonstrates that the metabolism study of coumarin was incomplete, possibly due to limitations of old techniques. The identification of eight inedited metabolites of such a simple molecule suggests that the information regarding the metabolism of other drugs may also be incomplete, and therefore, new investigations are necessary.

Highlights

  • IntroductionCoumarin (Figure 1), known as 1,2-benzopyrone, is present in a variety of plants [1,2,3]

  • Coumarin (Figure 1), known as 1,2-benzopyrone, is present in a variety of plants [1,2,3].It is found in large quantities in some essential oils, mainly in cinnamon bark oil, cassia leaf oil, and lavender oil

  • Humans are exposed to coumarin on a daily basis [5,6]

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Summary

Introduction

Coumarin (Figure 1), known as 1,2-benzopyrone, is present in a variety of plants [1,2,3]. It is found in large quantities in some essential oils, mainly in cinnamon bark oil, cassia leaf oil, and lavender oil. Coumarin is a white crystalline solid with a monoisotopic mass of 146.0368 Da. Its taste is bitter and aromatic, and its odour is similar to vanilla [4]. Its taste is bitter and aromatic, and its odour is similar to vanilla [4] Due to this last characteristic, it is added to cosmetics, hygienic products, and beverages as a flavouring. Humans are exposed to coumarin on a daily basis [5,6]

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