Thyagarajan Anita, Saylae Jeremiah, Sahu Ravi P
Department of Pharmacology and Toxicology, Boonshoft School of Medicine at Wright State University, Dayton, OH, USA.
Oncotarget. 2017 Jul 25;8(30):49959-49972. doi: 10.18632/oncotarget.18326.
Acquired resistance to standard therapies remains a serious challenge, requiring novel therapeutic approaches that incorporate potential factors involved in tumor resistance. As cancers including melanoma express inflammatory cyclooxygenases generating prostaglandins implicated in tumor growth, we investigated mechanism of anti-inflammatory drug, acetylsalicylic acid (ASA) which has been shown to inhibit various tumor types, however, its effects against highly aggressive melanoma model are unclear. Given our reports that an activation of platelet-activating factor-receptor (PAF-R) augments the growth and impede efficacies of therapeutic agents in experimental melanoma, we also sought to determine if PAF-R mediates anti-melanoma activity of ASA. The current studies using stably PAF-R-positive (B16-PAFR) and negative (B16-MSCV) murine melanoma cells and PAF-R-expressing and deficient mice, demonstrate that ASA inhibits the in-vitro and in-vivo growth of highly aggressive B16F10 melanoma via bypassing tumoral or stromal PAF-R signaling. Similar ASA-induced effects in-vitro were seen in human melanoma and nasopharyngeal carcinoma cells positive or negative in PAF-R. Mechanistically, the ASA-induced decrease in cell survival and increase in apoptosis were significantly blocked by prostaglandin F2 alpha (PGF2α) agonists. Importantly, PCR array and qRT-PCR analysis of B16-tumors revealed significant downregulation of sry-related high-mobility-box-2 (SOX2) oncogene by ASA treatment. Interestingly, modulation of SOX2 expression by PGF2α agonists and upregulation by fibroblast growth factor 1 (FGF-1) rescued melanoma cells from ASA-induced decreased survival and increased apoptosis. Moreover, PGF2α-receptor antagonist, AL8810 mimics ASA-induced decreased melanoma cells survival which was significantly blocked by PGF2α and FGF-1. These findings indicate that ASA inhibits the growth of aggressive melanoma via SOX2-dependent-PAF-R-indepedent pathway.
对标准疗法产生获得性耐药仍然是一个严峻挑战,这需要采用新的治疗方法,纳入与肿瘤耐药相关的潜在因素。由于包括黑色素瘤在内的癌症会表达炎性环氧化酶,生成与肿瘤生长有关的前列腺素,我们研究了抗炎药物乙酰水杨酸(ASA)的作用机制,该药物已被证明可抑制多种肿瘤类型,但其对高侵袭性黑色素瘤模型的作用尚不清楚。鉴于我们之前的报道显示,血小板活化因子受体(PAF-R)的激活会促进实验性黑色素瘤的生长并阻碍治疗药物的疗效,我们还试图确定PAF-R是否介导了ASA的抗黑色素瘤活性。目前使用稳定表达PAF-R阳性(B16-PAFR)和阴性(B16-MSCV)的小鼠黑色素瘤细胞以及表达和缺乏PAF-R的小鼠进行的研究表明,ASA通过绕过肿瘤或基质PAF-R信号传导来抑制高侵袭性B16F10黑色素瘤的体外和体内生长。在PAF-R呈阳性或阴性的人黑色素瘤和鼻咽癌细胞中也观察到了类似ASA诱导的体外效应。从机制上讲,前列腺素F2α(PGF2α)激动剂可显著阻断ASA诱导的细胞存活率下降和凋亡增加。重要 的是,对B16肿瘤进行的PCR阵列和qRT-PCR分析显示,ASA治疗可使sry相关的高迁移率族盒2(SOX2)癌基因显著下调。有趣的是,PGF2α激动剂对SOX2表达的调节以及成纤维细胞生长因子1(FGF-1)对SOX2表达的上调可使黑色素瘤细胞免受ASA诱导的存活率下降和凋亡增加的影响。此外,PGF2α受体拮抗剂AL8810模拟了ASA诱导的黑色素瘤细胞存活率下降,而PGF2α和FGF-1可显著阻断这种下降。这些发现表明,ASA通过SOX2依赖的PAF-R非依赖途径抑制侵袭性黑色素瘤的生长。