Zhang Liang, Cui Li
School of Pharmacy, Soochow University, Renai Road, Soochow, Jiangsu Province 215123, China.
Toxicol In Vitro. 2007 Sep;21(6):1095-103. doi: 10.1016/j.tiv.2007.04.008. Epub 2007 Apr 27.
ACTX-6 is a protein isolated from Agkistrodon acutus snake venom and demonstrated cytotoxic activity to various cancer cells in vitro. In this paper the exact mechanism in ACTX-6-induced cell death was investigated and it was found that ACTX-6 could induce cell apoptosis. The results of Western blot and RT-PCR showed that ACTX-6 could induce Fas and FasL protein expression. When Fas signaling pathway was blocked by neutralizing antibodies to Fas or FasL, ACTX-6-induced apoptosis was inhibited. DISC formation was also detected by immunoprecipitation. These results suggested that Fas pathway was involved in ACTX-6-induced apoptosis. The activities of caspase-3, 8 and 9 were assayed and the activation of caspase-9 demonstrated that mitochondrial pathway was also involved in ACTX-6-induced apoptosis. Bid cleavage and dissipation of mitochondrial membrane potential (delta psi(m)) verified the involvement of mitochondria. ACTX-6 is an L-amino acid oxidase and can oxidize L-amino acid to generate hydrogen peroxide. The production of ROS in ACTX-6-treated cells was detected and the ROS scavenger catalase could inhibit ACTX-6-induced apoptosis. Western blot analysis showed that JNK was phosphorylated in ACTX-6-treated cells and c-Jun was also activated. JNK inhibitor SP600125 could inhibit ACTX-6-induced apoptosis and catalase could inhibit JNK and c-Jun phosphorylation. It could be concluded that JNK pathway was necessary in ACTX-6-induced apoptosis and the oxidative stress generated by ACTX-6 was responsible for the activation of JNK.
尖吻蝮蛇毒素-6(ACTX-6)是一种从尖吻蝮蛇毒中分离出的蛋白质,在体外对多种癌细胞具有细胞毒性活性。本文研究了ACTX-6诱导细胞死亡的确切机制,发现ACTX-6可诱导细胞凋亡。蛋白质免疫印迹法(Western blot)和逆转录聚合酶链反应(RT-PCR)结果表明,ACTX-6可诱导Fas和FasL蛋白表达。当用抗Fas或FasL的中和抗体阻断Fas信号通路时,ACTX-6诱导的凋亡受到抑制。免疫沉淀法也检测到死亡诱导信号复合物(DISC)的形成。这些结果表明,Fas途径参与了ACTX-6诱导的凋亡。检测了半胱天冬酶-3、8和9的活性,半胱天冬酶-9的激活表明线粒体途径也参与了ACTX-6诱导的凋亡。Bid裂解和线粒体膜电位(Δψm)的消散证实了线粒体的参与。ACTX-6是一种L-氨基酸氧化酶,可氧化L-氨基酸生成过氧化氢。检测了ACTX-6处理细胞中活性氧(ROS)的产生,ROS清除剂过氧化氢酶可抑制ACTX-6诱导的凋亡。蛋白质免疫印迹分析表明,ACTX-6处理的细胞中JNK被磷酸化,c-Jun也被激活。JNK抑制剂SP600125可抑制ACTX-6诱导的凋亡,过氧化氢酶可抑制JNK和c-Jun的磷酸化。可以得出结论,JNK途径在ACTX-6诱导的凋亡中是必需的,ACTX-6产生的氧化应激负责JNK的激活。