Department of Immunology, Keimyung University, 1095 Dalgubeoldaero, Dalseo-Gu, Daegu 42601, Korea.
Department of Medical Biology, Jessenius Faculty of Medicine, Comenius University in Bratislava, 03601 Martin, Slovakia.
Biomolecules. 2019 Dec 6;9(12):838. doi: 10.3390/biom9120838.
Honokiol is a natural biphenolic compound extracted from traditional Chinese medicine species, which have been known to display various biological effects including anti-cancer, anti-proliferative, anti-angiogenic, and anti-metastatic activities in cancer cells. Here, we found that honokiol sensitizes cancer cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis through downregulation of anti-apoptotic proteins survivin and c-FLIP. Ectopic expression of survivin and c-FLIP markedly abolished honokiol and TRAIL-induced apoptosis. Mechanistically, honokiol induced protein degradation of c-FLIP and survivin through STAMBPL1, a deubiquitinase. STAMBPL1 interacted with survivin and c-FLIP, resulted in reduction of ubiquitination. Knockdown of STAMBPL1 reduced survivin and c-FLIP protein levels, while overexpression of STAMBPL1 inhibited honokinol-induced survivin and c-FLIP degradation. Our findings provided that honokiol could overcome TRAIL resistance through survivin and c-FLIP degradation induced by inhibition of STAMBPL1 expression.
和厚朴酚是一种从传统中药品种中提取的天然双酚类化合物,已被证明具有多种生物效应,包括在癌细胞中具有抗癌、抗增殖、抗血管生成和抗转移活性。在这里,我们发现和厚朴酚通过下调抗凋亡蛋白生存素和 c-FLIP 使癌细胞对肿瘤坏死因子相关凋亡诱导配体(TRAIL)诱导的凋亡敏感。生存素和 c-FLIP 的异位表达明显消除了和厚朴酚和 TRAIL 诱导的凋亡。在机制上,和厚朴酚通过去泛素化酶 STAMBPL1 诱导 c-FLIP 和生存素的蛋白降解。STAMBPL1 与生存素和 c-FLIP 相互作用,导致泛素化减少。STAMBPL1 的敲低降低了生存素和 c-FLIP 蛋白水平,而 STAMBPL1 的过表达抑制了和厚朴酚诱导的生存素和 c-FLIP 降解。我们的研究结果表明,和厚朴酚可以通过抑制 STAMBPL1 表达诱导的 survivin 和 c-FLIP 降解来克服 TRAIL 耐药性。