Richardson Terrilyn A, Sherman Melanie, Kalman Daniel, Morgan Edward T
Department of Pharmacology, Emory University School of Medicine, 5119 Rollins Research Center, 1510 Clifton Road, Atlanta, GA 30322, USA.
Drug Metab Dispos. 2006 Mar;34(3):351-3. doi: 10.1124/dmd.105.007435. Epub 2005 Dec 8.
Inflammation or infection down-regulates the activity and expression of cytochrome P450 (P450) enzymes involved in hepatic drug clearance, possibly altering drug effectiveness and leading to toxicity. The regulation of UDP-glucuronosyltransferases (UGTs) in inflammation and infection is less well characterized. To determine the response of hepatic and renal UGTs during inflammation and infection, mice were administered either saline or 1 mg/kg lipopolysaccharide (LPS) (16 h), or Citrobacter rodentium by oral gavage (6 days). Hepatic mRNA expression of UGT1A1, 1A9, and 2B5 was similarly down-regulated after LPS exposure and C. rodentium infection, whereas UGT1A2 and 1A6 mRNAs were unchanged. Effects of C. rodentium infection did not require a functional Toll-like receptor 4. Conversely, renal UGT isoforms were relatively unaffected, except for UGT2B5 induction after LPS treatment. Regulation of UGTs during the inflammatory response exhibits similarities to and differences from regulation of P450s, and may be cytokine-mediated.
炎症或感染会下调参与肝脏药物清除的细胞色素P450(P450)酶的活性和表达,这可能会改变药物疗效并导致毒性。炎症和感染中尿苷二磷酸葡萄糖醛酸转移酶(UGTs)的调节情况了解较少。为了确定炎症和感染期间肝脏和肾脏UGTs的反应,给小鼠注射生理盐水或1mg/kg脂多糖(LPS)(16小时),或通过灌胃给予鼠柠檬酸杆菌(6天)。LPS暴露和鼠柠檬酸杆菌感染后,UGT1A1、1A9和2B5的肝脏mRNA表达同样下调,而UGT1A2和1A6的mRNA表达未改变。鼠柠檬酸杆菌感染的影响不需要功能性Toll样受体4。相反,除了LPS处理后UGT2B5诱导外,肾脏UGT同工型相对未受影响。炎症反应期间UGTs的调节与P450s的调节既有相似之处也有不同之处,可能是由细胞因子介导的。