Argikar, Upendra (2018) Saccharolactone: the history, the myth, and the practice. Current drug metabolism, 19. pp. 304-309. ISSN 1875-5453

Abstract

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. This report investigates the historic evidence in the practice of saccharolactone addition in relation to β-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.

Item Type:	Article
Date Deposited:	03 Jul 2018 00:45
Last Modified:	03 Jul 2018 00:45
URI:	https://oak.novartis.com/id/eprint/33915