Qi Jia, Yang Ping, Yi Bing, Huo Yan, Chen Ming, Zhang Jian, Sun Jianxin
Department of Pharmacy, Xinhua Hospital, Shanghai Jiaotong University, Shanghai, China; and Center for Translational Medicine, Thomas Jefferson University, Philadelphia, Pennsylvania.
Department of Pharmacy, Xinhua Hospital, Shanghai Jiaotong University, Shanghai, China; and.
Am J Physiol Heart Circ Physiol. 2015 Apr 15;308(8):H841-52. doi: 10.1152/ajpheart.00470.2014. Epub 2015 Jan 30.
Abdominal aortic aneurysm (AAA) is a common degenerative vascular disease whose pathogenesis is associated with activation of multiple signaling pathways including Jun NH2-terminal kinases (JNK) and NF-κB. It is now well recognized that these pathways are chaperoned by the heat shock protein 90 (Hsp90), suggesting that inhibition of Hsp90 may be a novel strategy for inhibiting AAAs. The aim of this study is to investigate whether inhibition of Hsp90 by 17-DMAG (17-dimethyl-aminothylamino-17-demethoxy-geldanamycin) attenuates ANG II-induced AAA formation in mice, and, if so, to elucidate the mechanisms involved. Apolipoprotein E-null mice were infused with ANG II to induce AAA formation and simultaneously treated by intraperitoneal injection with either vehicle or 17-DMAG for 4 wk. ANG II infusion induced AAA formation in 80% of mice, which was accompanied by increased matrix metalloproteinase (MMP) activity, enhanced tissue inflammation, oxidative stress, and neovascularization. Importantly, these effects were inhibited by 17-DMAG treatment. Mechanistically, we showed that 17-DMAG prevented the formation and progression of AAA through its inhibitory effects on diverse biological pathways including 1) by blocking ANG II-induced phosphorylation of ERK1/2 and JNK that are critically involved in the regulation of MMPs in vascular smooth muscle cells, 2) by inhibiting IκB kinase expression and expression of MCP-1, and 3) by attenuating ANG II-stimulated angiogenic processes critical to AAA formation. Our results demonstrate that inhibition of Hsp90 by 17-DMAG effectively attenuates ANG II-induced AAA formation by simultaneously inhibiting vascular inflammation, extracellular matrix degradation, and angiogenesis, which are critical in the formation and progression of AAAs.
腹主动脉瘤(AAA)是一种常见的退行性血管疾病,其发病机制与包括Jun氨基末端激酶(JNK)和核因子κB(NF-κB)在内的多种信号通路激活有关。现在人们已经充分认识到,这些信号通路由热休克蛋白90(Hsp90)陪伴,这表明抑制Hsp90可能是抑制腹主动脉瘤的一种新策略。本研究的目的是探讨17-二甲基氨基乙基氨基-17-去甲氧基格尔德霉素(17-DMAG)抑制Hsp90是否能减轻血管紧张素II(ANG II)诱导的小鼠腹主动脉瘤形成,如果可以,则阐明其中涉及的机制。给载脂蛋白E基因敲除小鼠输注ANG II以诱导腹主动脉瘤形成,并同时通过腹腔注射溶剂或17-DMAG进行4周治疗。输注ANG II可在80%的小鼠中诱导腹主动脉瘤形成,同时伴有基质金属蛋白酶(MMP)活性增加、组织炎症增强、氧化应激和新生血管形成。重要的是,17-DMAG治疗可抑制这些作用。从机制上讲,我们发现17-DMAG通过对多种生物学途径的抑制作用来预防腹主动脉瘤的形成和进展,包括:1)通过阻断ANG II诱导的细胞外信号调节激酶1/2(ERK1/2)和JNK磷酸化,而ERK1/2和JNK磷酸化在血管平滑肌细胞中对MMP的调节至关重要;2)通过抑制IκB激酶表达和单核细胞趋化蛋白-1(MCP-1)的表达;3)通过减弱ANG II刺激的对腹主动脉瘤形成至关重要的血管生成过程。我们的结果表明,17-DMAG抑制Hsp90可通过同时抑制血管炎症、细胞外基质降解和血管生成,有效减轻ANG II诱导的腹主动脉瘤形成,而这些过程在腹主动脉瘤的形成和进展中至关重要。