a Department of Radiation Medicine , Institute of Modern Physics, Chinese Academy of Sciences , Lanzhou , China.
b Key Laboratory of Heavy Ion Radiation Biology and Medicine, Institute of Modern Physics, Chinese Academy of Sciences , Lanzhou , China.
Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):1273-1280. doi: 10.1080/21691401.2019.1596922.
Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3b1 subunit of the spliceosome. There is considerable interest in the compound as a tool to study SF3b1 function in cancer. However, so far little information is available on the molecular mechanism of SF3b1 eliciting apoptosis in cancer cells. Here, we investigated the molecular mechanism of SF3b1 eliciting apoptosis in human cervical carcinoma cells. We demonstrated that inhibition of SF3b1 by pladienolide B inhibited proliferation of HeLa cells at low nanomolar concentrations in a dose- and time-dependent manner. It also induced G2/M phase arrest and significant rise of apoptotic cells. Moreover, it is indicated that inhibition of SF3b1 by pladienolide B induced Tap73/ΔNp73 expression and consequently down-regulated Bax/Bcl-2 ratio, cytochrome c release and caspase-3 expression. Thus, our results showed that SF3b1 plays a pivotal role in cycle arrest, apoptosis induction, and p73 splicing in human cervical carcinoma cells, suggesting that SF3b1 could be used as a potential candidate for cervical cancer therapy.
普拉地诺内酯 B 是一种强效的癌细胞生长抑制剂,其作用靶点是剪接体的 SF3b1 亚基。该化合物作为一种研究 SF3b1 在癌症中的功能的工具,引起了广泛的关注。然而,目前关于 SF3b1 如何在癌细胞中引发细胞凋亡的分子机制的信息还很少。在这里,我们研究了 SF3b1 在人宫颈癌细胞中引发细胞凋亡的分子机制。我们证明,普拉地诺内酯 B 抑制 SF3b1 的作用可在低纳摩尔浓度下以剂量和时间依赖性方式抑制 HeLa 细胞的增殖。它还诱导 G2/M 期阻滞和凋亡细胞的显著增加。此外,结果表明,普拉地诺内酯 B 抑制 SF3b1 诱导 Tap73/ΔNp73 的表达,进而下调 Bax/Bcl-2 比值、细胞色素 c 释放和 caspase-3 的表达。因此,我们的结果表明,SF3b1 在人宫颈癌细胞的周期阻滞、凋亡诱导和 p73 剪接中发挥关键作用,提示 SF3b1 可作为宫颈癌治疗的潜在候选药物。