Fujita K, Nozaki Y, Wada K, Yoneda M, Endo H, Takahashi H, Iwasaki T, Inamori M, Abe Y, Kobayashi N, Kirikoshi H, Kubota K, Saito S, Nagashima Y, Nakajima A
Division of Gastroenterology, Yokohama City University Graduate School of Medicine, 3-9 Fuku-ura, Kanazawa-ku, Yokohama 236-0004, Japan.
Gut. 2008 Nov;57(11):1583-91. doi: 10.1136/gut.2007.144550. Epub 2008 Jul 2.
No effective drugs have been developed to date to prevent or treat non-alcoholic fatty liver disease (NAFLD), although diet modification and exercise to improve obesity have been attempted. Therefore, development of a novel drug/strategy to treat NAFLD is urgently needed. In the present study, a novel concept is proposed for the treatment of NAFLD.
Fisher 344 male rats were given a choline-deficient, l-amino acid-defined (CDAA) diet or a high-fat high-calorie (HF/HC) diet with or without the antiplatelet agents, aspirin, ticlopidine or cilostazol for 16 weeks. Liver steatosis, inflammation and fibrosis, and the possible mechanisms involved were investigated.
All three antiplatelet drugs, namely aspirin, ticlopidine and cilostazol, significantly attenuated liver steatosis, inflammation and fibrosis in the CDAA diet group. Of the three agents, cilostazol was the most effective, and the drug also suppressed HF/HC diet-induced liver steatosis. Cilostazol appeared to exert its beneficial effect against NAFLD by suppressing mitogen-activated protein kinase activation induced by oxidative stress and platelet-derived growth factor via intercepting signal transduction from Akt to c-Raf.
Antiplatelet agents, especially cilostazol, offer the promise of becoming key agents for the treatment of NAFLD.
尽管已经尝试通过饮食调整和运动来改善肥胖问题,但迄今为止尚未开发出有效的药物来预防或治疗非酒精性脂肪性肝病(NAFLD)。因此,迫切需要开发一种治疗NAFLD的新型药物/策略。在本研究中,提出了一种治疗NAFLD的新概念。
将Fisher 344雄性大鼠给予胆碱缺乏、l-氨基酸限定(CDAA)饮食或高脂高热量(HF/HC)饮食,并给予或不给予抗血小板药物阿司匹林、噻氯匹定或西洛他唑,持续16周。研究肝脏脂肪变性、炎症和纤维化以及可能涉及的机制。
三种抗血小板药物,即阿司匹林、噻氯匹定和西洛他唑,均显著减轻了CDAA饮食组的肝脏脂肪变性、炎症和纤维化。在这三种药物中,西洛他唑最为有效,该药物还抑制了HF/HC饮食诱导的肝脏脂肪变性。西洛他唑似乎通过拦截从Akt到c-Raf的信号转导,抑制氧化应激和血小板衍生生长因子诱导的丝裂原活化蛋白激酶激活,从而对NAFLD发挥有益作用。
抗血小板药物,尤其是西洛他唑,有望成为治疗NAFLD的关键药物。