Center for Clinical Pharmacology, Washington University School of Medicine and St. Louis College of Pharmacy, St. Louis, MO, United States of America.
PLoS One. 2020 Oct 1;15(10):e0236000. doi: 10.1371/journal.pone.0236000. eCollection 2020.
Non-alcoholic fatty liver disease (NAFLD) affects a significant number of people worldwide and currently there are no pharmacological treatments. NAFLD often presents with obesity, insulin resistance, and in some cases cardiovascular diseases. There is a clear need for treatment options to alleviate this disease since it often progresses to much more the much more severe non-alcoholic steatohepatitis (NASH). The REV-ERB nuclear receptor is a transcriptional repressor that regulates physiological processes involved in the development of NAFLD including lipogenesis and inflammation. We hypothesized that pharmacologically activating REV-ERB would suppress the progression of fatty liver in a mouse model of NASH. Using REV-ERB agonist SR9009 in a mouse NASH model, we demonstrate the beneficial effects of REV-ERB activation that led to an overall improvement of hepatic health by suppressing hepatic fibrosis and inflammatory response.
非酒精性脂肪性肝病(NAFLD)影响着全球大量人群,目前尚无药物治疗方法。NAFLD 常伴有肥胖、胰岛素抵抗,在某些情况下还伴有心血管疾病。由于该病常进展为更严重的非酒精性脂肪性肝炎(NASH),因此非常需要治疗方法来缓解这种疾病。REV-ERB 核受体是一种转录抑制剂,可调节参与 NAFLD 发展的生理过程,包括脂肪生成和炎症。我们假设通过药物激活 REV-ERB 可抑制 NASH 小鼠模型中脂肪肝的进展。我们使用 REV-ERB 激动剂 SR9009 在 NASH 小鼠模型中证明了 REV-ERB 激活的有益效果,通过抑制肝纤维化和炎症反应,从而整体改善肝脏健康。