Department of Pharmacology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou, Guangdong 510080, PR China.
Biochimie. 2010 Oct;92(10):1354-61. doi: 10.1016/j.biochi.2010.06.018. Epub 2010 Jun 30.
Severe acute pancreatitis (SAP) remains a challenging disease to manage, with high mortality, limited understanding of pathogenesis and lack of specific therapy. Recombinant fibrinogenase II (rFII) from Agkistrodon acutus venom has been found to degrade tumor necrosis factor-alpha (TNF-α) which is vital in mortality of SAP. Here we investigate the in vivo effects of rFII in rat SAP and confirm the degradation effect of rFII for TNF-αin vitro. The SAP model was prepared by retrograde infusion of 5% sodium taurocholate into the biliopancreatic duct in male Sprague-Dawley rats. Treatment with 1 mg/kg rFII could significantly increase survival rate of SAP rats (P = 0.006) as well as 8 mg/kg Infliximab treatment did. The pancreatic and pulmonary injury and the peritoneal and systemic inflammatory response were also attenuated by rFII as well as Infliximab. Furthermore, rFII inhibited TNF-α secretion by rat peritoneal macrophages in a time- and concentration-dependent manner but didn't influence interleukin (IL) -1β secretion in vitro. The degradation potency of rFII for human TNF-α was greater than that for rat TNF-α. Our findings suggest that rFII could have protective effect on taurocholate-induced SAP in rats, mainly depending on direct degradation of TNF-α.
重症急性胰腺炎(SAP)仍然是一种难以治疗的疾病,死亡率高,对发病机制的了解有限,缺乏特异性治疗方法。从尖吻蝮蛇毒液中提取的重组纤维蛋白溶酶 II(rFII)已被发现可降解肿瘤坏死因子-α(TNF-α),这对于 SAP 的死亡率至关重要。在这里,我们研究了 rFII 在大鼠 SAP 中的体内作用,并证实了 rFII 在体外对 TNF-α的降解作用。通过逆行输注 5%牛磺胆酸钠到胆胰管制备 SAP 模型。用 1mg/kg rFII 治疗可显著提高 SAP 大鼠的存活率(P = 0.006),与 8mg/kg 英夫利昔单抗治疗的效果相当。rFII 以及英夫利昔单抗还减轻了胰腺和肺损伤以及腹膜和全身炎症反应。此外,rFII 以时间和浓度依赖的方式抑制大鼠腹腔巨噬细胞分泌 TNF-α,但体外不影响白细胞介素(IL)-1β的分泌。rFII 对人 TNF-α的降解能力大于对大鼠 TNF-α的降解能力。我们的研究结果表明,rFII 对牛磺胆酸钠诱导的 SAP 大鼠具有保护作用,主要取决于对 TNF-α的直接降解。