Department of Pharmacology, Kitasato University School of Medicine, Kanagawa, Japan.
Biomed Pharmacother. 2010 Feb;64(2):101-6. doi: 10.1016/j.biopha.2009.04.039. Epub 2009 Oct 20.
Prostaglandin E(2) (PGE(2)) and prostaglandin E (EP) receptor signaling pathways have been implicated in the promotion of tumor growth and angiogenesis. However, little is known about their roles in lymphangiogenesis during tumor development. The present study evaluates whether endogenous PGE(2) exhibits a critical role in tumor-associated lymphangiogenesis. Treatment of male C57BL/6 mice with a cyclooxygenase-2 inhibitor, celecoxib, for seven days resulted in a 52.4% reduction in tumor size induced by subcutaneous injection of murine Lewis lung cells. Celecoxib treatment down-regulated the expression of vascular endothelial growth factor receptor (VEGFR)-3 in stromal tissues by 73.9%, and attenuated expression of podoplanin, a marker for lymphatic endothelial cells. To examine the role of host PGE receptor signaling, we tested four kinds of EP receptor knockout mice. At Day 7 after tumor cell implantation, EP3 receptor knockout mice, but not EP receptor knockout mice lacking EP1, EP2, or EP4, exhibited a 53.3% reduction in tumor weight, which was associated with a 74.5% reduction in VEGFR-3 mRNA expression in tumor stromal tissues. At Day 14, VEGFR-3 expression in EP3-/- mice remained significantly lower than that of their wild-type (WT) counterparts. The expression of VEGF-C in the tumor stromal tissues in EP3-/- mice were also reduced by 22.1% (Day 7) and 44.1% (Day 14), respectively. In addition, the level of immunoreactive podoplanin in the tumor tissues from EP3-/- mice was less than that of WT. These results suggest that host EP3 receptor signaling regulates tumor-associated lymphangiogenesis by up-regulating expression of VEGF-C and its receptor, VEGFR-3, in tumor stromal tissues. Host EP3 blockade together with COX-2 inhibition may be a novel therapeutic strategy to suppress tumor-associated lymphangiogenesis.
前列腺素 E(2)(PGE(2))和前列腺素 E (EP)受体信号通路已被认为在促进肿瘤生长和血管生成中发挥作用。然而,关于它们在肿瘤发展过程中淋巴管生成中的作用知之甚少。本研究评估了内源性 PGE(2)是否在肿瘤相关淋巴管生成中发挥关键作用。用环氧化酶-2 抑制剂塞来昔布治疗雄性 C57BL/6 小鼠 7 天,可使皮下注射小鼠 Lewis 肺癌细胞诱导的肿瘤大小减少 52.4%。塞来昔布治疗使基质组织中血管内皮生长因子受体(VEGFR)-3 的表达下调 73.9%,并减弱了淋巴管内皮细胞标志物 podoplanin 的表达。为了研究宿主 PGE 受体信号的作用,我们测试了四种 EP 受体敲除小鼠。在肿瘤细胞植入后第 7 天,EP3 受体敲除小鼠,但不是缺乏 EP1、EP2 或 EP4 的 EP 受体敲除小鼠,肿瘤重量减少了 53.3%,肿瘤基质组织中 VEGFR-3 mRNA 表达减少了 74.5%。第 14 天,EP3-/-小鼠的 VEGFR-3 表达仍然明显低于其野生型(WT)对照。在 EP3-/-小鼠的肿瘤基质组织中,VEGF-C 的表达也分别减少了 22.1%(第 7 天)和 44.1%(第 14 天)。此外,EP3-/-小鼠肿瘤组织中免疫反应性 podoplanin 的水平也低于 WT。这些结果表明,宿主 EP3 受体信号通过上调肿瘤基质组织中 VEGF-C 及其受体 VEGFR-3 的表达来调节肿瘤相关淋巴管生成。宿主 EP3 阻断与 COX-2 抑制的联合可能是抑制肿瘤相关淋巴管生成的一种新的治疗策略。