Department of Pharmacy, School of Basic Medical Sciences, Henan University of Science and Technology, 263 Kaiyuan Avenue, Luoyang, 471023, China.
Mol Cell Biochem. 2021 Apr;476(4):1651-1661. doi: 10.1007/s11010-020-04032-x. Epub 2021 Jan 9.
JS-K as an exogenous NO donor could release NO after activation by glutathione S-transferases (GSTs). The present study explores the effects of JS-K on MAPK pathway in HepG2 and Bel-7402 cells. JS-K significantly prompted apoptosis and SB203580 (a p38 inhibitor) and SP600125 (a JNK inhibitor) prior to JS-K could partly reverse apoptosis and activation of cleaved-caspase-3 and cleaved PARP. However, U0126 (a MEK inhibitor) strengthened the cell apoptosis and the expressions of cleaved-caspase-3 and cleaved PARP. JS-K caused phosphorylation of p38 MAPK and JNK but attenuated phosphorylation of ERK, which were reversed by Carboxy-PTIO (a NO scavenger). Meanwhile, the phosphorylation of HSP27, c-JUN and ATF-2 were activated in JS-K-treated cells. SB203580 and SP600125 could attenuate phosphorylation of p38 MAPK and JNK, respectively. The phosphorylation in downstream substrates of p38 MAPK and JNK was also abolished by SB203580 and SP600125 in JS-K-treated cells. Additionally, JS-K decreased phosphorylation of c-Raf, which subsequently caused a decrease of MEK1/2 phosphorylation. Several downstream targets of ERK1/2 including p90RSK and transcription factors (e.g., Elk-1, c-Myc and c-Fos) were inhibited. U0126 potentiated JS-K-induced inhibitory effect of Raf/MEK/ERK pathway. The same results were also observed in the downstream substrates of ERK1/2 including p90RSK, Elk-1, c-Myc and c-Fos. Moreover, Carboxy-PTIO abolished the inhibitory effect of Raf/MEK/ERK pathway triggered by JS-K. Finally, JS-K significantly suppressed the growth of rat primary hepatic carcinoma via MAPK pathway in vivo. Taken together, JS-K can induce hepatocellular carcinoma cells apoptosis through its activation of JNK and p38 MAPK and inactivation of Raf/MEK/ERK signaling pathways.
JS-K 作为一种外源性的一氧化氮供体,在谷胱甘肽 S-转移酶(GSTs)的激活下可以释放一氧化氮。本研究探讨了 JS-K 对 HepG2 和 Bel-7402 细胞中 MAPK 通路的影响。JS-K 显著促进了细胞凋亡,而在 JS-K 之前使用 SB203580(一种 p38 抑制剂)和 SP600125(一种 JNK 抑制剂)可以部分逆转细胞凋亡以及 cleaved-caspase-3 和 cleaved PARP 的激活。然而,U0126(一种 MEK 抑制剂)增强了细胞凋亡以及 cleaved-caspase-3 和 cleaved PARP 的表达。JS-K 引起 p38 MAPK 和 JNK 的磷酸化,但减弱了 ERK 的磷酸化,而这些变化被羧基-PTIO(一种一氧化氮清除剂)所逆转。同时,在 JS-K 处理的细胞中,HSP27、c-JUN 和 ATF-2 的磷酸化被激活。SB203580 和 SP600125 分别减弱了 p38 MAPK 和 JNK 的磷酸化。在 JS-K 处理的细胞中,p38 MAPK 和 JNK 的下游底物的磷酸化也被 SB203580 和 SP600125 所消除。此外,JS-K 降低了 c-Raf 的磷酸化,进而导致 MEK1/2 磷酸化的减少。ERK1/2 的几个下游靶标,包括 p90RSK 和转录因子(如 Elk-1、c-Myc 和 c-Fos)被抑制。U0126 增强了 JS-K 诱导的 Raf/MEK/ERK 通路的抑制作用。在包括 p90RSK、Elk-1、c-Myc 和 c-Fos 在内的 ERK1/2 的下游底物中也观察到了相同的结果。此外,羧基-PTIO 消除了由 JS-K 触发的 Raf/MEK/ERK 通路的抑制作用。最后,JS-K 体内通过 MAPK 通路显著抑制大鼠原发性肝癌的生长。总之,JS-K 可以通过激活 JNK 和 p38 MAPK 以及失活 Raf/MEK/ERK 信号通路诱导肝癌细胞凋亡。