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Saccharolactone: The History, the Myth, and the Practice

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Background: Over the past two decades, saccharolactone has been routinely used in in vitro microsomal incubations, and sometimes in incubations with recombinant Uridine diphosphoglucuronosyl transferases (UGT) while investigating glucuronidation reactions. The addition of saccharolactone is aimed at completely inhibiting β- glucuronidases that may be present in the microsomes, in the anticipation of accurate identification and quantification of the formed glucuronide metabolites. Recent research has demonstrated that saccharolatone may not serve the intended objective, and may even lead to inhibition of certain UGTs.

Objective: This report investigates the historic evidence in the practice of saccharolactone addition in relation to - glucuronidases and UGTs. The chemical nature and inhibition potency of saccharolactone are explored in an attempt to unravel the myth in its application. Finally, the collective evidence is discussed in an effort to provide guidance to drug metabolism scientists on the utilization of saccharolactone.

Conclusion: In-depth evaluation of the experimental evidence in the literature points toward a weak rationale for general in vitro application of saccharolactone. Furthermore, inhibition of recombinant or microsomal UGTs by saccharolactone may be model dependent. Overall, the integrated data suggests that saccharolactone should not be utilized in in vitro microsomal incubations with the objective of inhibiting β-glucuronidases.
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Keywords: Saccharolactone; Uridine-diphosphoglucuronosyl transferases; glucuronidation; glucuronides; saccharic acid; β-glucuronidases

Document Type: Review Article

Publication date: April 1, 2018

This article was made available online on January 11, 2018 as a Fast Track article with title: "Saccharolactone: The History, the Myth, and the Practice".

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  • Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:

    In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.
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