Pharmacy College, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; Department of Pharmacy, 302 Military Hospital of China, Beijing 100039, China.
Department of Respiration, 302 Military Hospital of China, Beijing 100039, China.
Biomed Pharmacother. 2017 May;89:696-704. doi: 10.1016/j.biopha.2017.02.084. Epub 2017 Mar 6.
Apoptosis induced by the bile acids in the liver is considered to play a pivotal role in the pathogenesis of cholestatic disease. Increasing evidence has demonstrated that Paeoniflorin (PF) exerts therapeutic effect on severe cholestatic liver diseases. However, whether PF could protect against alpha-naphthylisothiocyanate (ANIT)-induced cholestasis by inhibiting apoptosis remains unclear. In this study, we mainly investigated the effect and anti-apoptosis mechanism of PF on cholestasis. Experimental results indicated that PF pretreatment could attenuate liver damage and cholestasis by ANIT in rats, lift the biliary excretion in addition to decrease serum indices (ALT, AST, DBIL, TBIL, TBA, ALP and ϒ-GT) and conspicuous neutrophil infiltration and cell apoptosis in liver evidenced by TUNEL staining. Furthermore, the pro-apoptosis genes expression of Bax, Caspase-9 and Caspase-3 increased by ANIT were prominently reduced after PF treatment. The increase of anti-apoptosis gene and main regulator Bcl-2 in mitochondria by ANIT was largely reversed by PF pre-treatment. In summary, our study demonstrated that PF pre-treatment not only significantly attenuated ANIT-induced cholestasis and liver injury, but also largely reduced cell apoptosis in liver, thus may act as a potential therapeutic agent for cholestasis disease.
在肝脏中,胆汁酸诱导的细胞凋亡被认为在胆汁淤积性疾病的发病机制中起关键作用。越来越多的证据表明,芍药苷(PF)对严重胆汁淤积性肝病具有治疗作用。然而,PF 是否可以通过抑制细胞凋亡来防止α-萘基异硫氰酸酯(ANIT)诱导的胆汁淤积仍不清楚。在这项研究中,我们主要研究了 PF 对胆汁淤积的保护作用及其抗凋亡机制。实验结果表明,PF 预处理可减轻 ANIT 诱导的大鼠肝损伤和胆汁淤积,增加胆汁排泄,降低血清指标(ALT、AST、DBIL、TBIL、TBA、ALP 和 γ-GT),并减少肝内中性粒细胞浸润和细胞凋亡,这可通过 TUNEL 染色证实。此外,PF 处理后可明显降低 ANIT 诱导的促凋亡基因 Bax、Caspase-9 和 Caspase-3 的表达。PF 预处理还可明显逆转 ANIT 诱导的线粒体抗凋亡基因和主要调节因子 Bcl-2 的增加。综上所述,我们的研究表明,PF 预处理不仅可显著减轻 ANIT 诱导的胆汁淤积和肝损伤,还可明显减少肝内细胞凋亡,因此可能是胆汁淤积性疾病的一种潜在治疗药物。