Circadian time-dependent effects of experimental colitis on theophylline
disposition and toxicity
Abstract
Background and purpose: The impact of inflammatory bowel disease (IBD)
on drug disposition is a critical concern, yet whether this impact is
circadian time-dependent remains unexplored. We aim to discern the
temporal effects of colitis on drug disposition and toxicity.
Experimental Approach: The RNA-sequencing was used to screen
colitis-affecting genes. The liver microsomal incubation and the
pharmacokinetic study were used to analyze the enzymatic activity of key
enzymes. Dual luciferase assays and chromatin immunoprecipitation (ChIP)
were employed to elucidate regulatory relationships among molecules. Key
Results: CYP1A2 and CYP2E1, pivotal in theophylline metabolism, exhibit
reduced hepatic expression at Zeitgeber time (ZT)8 in colitis mice, a
difference diminishing by ZT20. Moreover, theophylline metabolism is
suppressed, and hepato-cardiac toxicities are markedly elevated in
colitis mice at ZT8, while remaining unchanged at ZT20. The circadian
clock component BMAL1 positively regulates CYP1A2 and CYP2E1 in the
liver of colitis mice. A combination of assays, integrating
liver-specific Bmal1 knockout mice and targeted activation of BMAL1 have
unveiled that the dysregulation observed in Cyp1a2 and Cyp2e1 during
colitis can be attributed to the perturbation in BMAL1 functionality in
the liver. Luciferase reporter and ChIP assays collectively substantiate
the role of BMAL1 in the modulation of Cyp1a2 and Cyp2e1 transcription
through its binding affinity to E-box-like sites. Conclusion and
implication: Our findings establish a strong link between IBD and
chronopharmacology, shedding light on how IBD affects drug disposition
and toxicity over time. Our research establishes a theoretical
foundation for chronopharmacological approaches In the treatment of IBD.