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. 2016 Jul 13;66(1):59–69. doi: 10.1136/gutjnl-2015-310874

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This is an Open Access article distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0/

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Daily intrarectal thioguanine (TG), but not mercaptopurine (MP) at 1 mg/kg, effected a rapid local improvement in spontaneous colitis. (A) Combined diarrhoea score; (B) colon weight/length ratio and (C) histological scoring of colitis in distal colon (DC), mid-colon (MC) and proximal colon (PC) segments in the Winnie mice. Gut representative bacteria converted TG (and less so MP) to thioguanine nucleotides (TGN). In vitro: (D) mean (SEM) TGN in Escherichia coli (Gram negative), Enterococcus faecalis (Gram positive), Bacteroides thetaiotaomicron (Gram-negative anaerobe) cultures incubated with 1 mM TG or MP for up to 120 min, N=3–4, *versus T0, ^#versus T30 and ^&versus T60; (E) scatter plots, mean TGN at 6 hours in hypoxanthine (guanine) phosphoribosyltransferase (Hprt)^−/− mouse faeces incubated with 0, 5 or 10 µM TG. In vivo: (F) wild-type (WT) and Hprt^−/− mice gavaged 5 mg/kg TG: scatter plots, mean TGN in liver and faeces. Statistical analysis: Mann-Whitney non-parametric test. Symbols:*versus WT mice.