Bristol Heart Institute, School of Clinical Sciences, University of Bristol, Bristol BS2 8HW, UK.
National Heart and Lung Institute, Imperial College London, London SW3 6LY, UK.
Int J Mol Sci. 2020 Mar 3;21(5):1733. doi: 10.3390/ijms21051733.
MicroRNAs (miRs) regulate complex processes, including angiogenesis, by targeting multiple mRNAs. miR-24-3p-3p directly represses eNOS, GATA2, and PAK4 in endothelial cells (ECs), thus inhibiting angiogenesis during development and in the infarcted heart. miR-24-3p is widely expressed in cardiovascular cells, suggesting that it could additionally regulate angiogenesis by acting on vascular mural cells. Here, we have investigated: 1) new miR-24-3p targets; 2) the expression and the function of miR-24-3p in human vascular ECs; 3) the impact of miR-24-3p inhibition in the angiogenesis reparative response to limb ischemia in mice. Using bioinformatics target prediction platforms and 3'-UTR luciferase assays, we newly identified Notch1 and its Delta-like ligand 1 (Dll1) to be directly targeted by miR-24-3p. miR-24-3p was expressed in human ECs and pericytes cultured under normal conditions. Exposure to hypoxia increased miR-24-3p in ECs but not in pericytes. Transfection with a miR-24-3p precursor (pre-miR-24-3p) increased miR-24-3p expression in ECs, reducing the cell survival, proliferation, and angiogenic capacity. Opposite effects were caused by miR-24-3p inhibition. The anti-angiogenic action of miR-24-3p overexpression could be prevented by simultaneous adenovirus (Ad)-mediated delivery of constitutively active Notch intracellular domain (NICD) into cultured ECs. We next demonstrated that reduced Notch signalling contributes to the anti-angiogenic effect of miR-24-3p in vitro. In a mouse unilateral limb ischemia model, local miR-24-3p inhibition (by adenovirus-mediated miR-24-3p decoy delivery) restored endothelial Notch signalling and increased capillary density. However, the new vessels appeared disorganised and twisted, worsening post-ischemic blood perfusion recovery. To better understand the underpinning mechanisms, we widened the search for miR-24-3p target genes, identifying several contributors to vascular morphogenesis, such as several members of the Wingless (Wnt) signalling pathway, β-catenin signalling components, and VE-cadherin, which synergise to regulate angiogenesis, pericytes recruitment to neoformed capillaries, maturation, and stabilization of newly formed vessels. Among those, we next focussed on β-catenin to demonstrate that miR-24-3p inhibition reduces β-catenin expression in hypoxic ECs, which is accompanied by reduced adhesion of pericytes to ECs. In summary, miR-24-3p differentially targets several angiogenesis modulators and contributes to autonomous and non-autonomous EC crosstalk. In ischemic limbs, miR-24-3p inhibition increases the production of dysfunctional microvessels, impairing perfusion. Caution should be observed in therapeutic targeting of miR-24-3p.
微小 RNA(miRs)通过靶向多个 mRNA 来调节包括血管生成在内的复杂过程。miR-24-3p-3p 可直接抑制内皮细胞(ECs)中的 eNOS、GATA2 和 PAK4,从而抑制发育过程中和梗死心脏中的血管生成。miR-24-3p 在心血管细胞中广泛表达,这表明它可以通过作用于血管壁细胞来额外调节血管生成。在这里,我们研究了:1)新的 miR-24-3p 靶标;2)miR-24-3p 在人血管 ECs 中的表达和功能;3)miR-24-3p 抑制在小鼠肢体缺血后血管生成修复反应中的作用。使用生物信息学靶标预测平台和 3'-UTR 荧光素酶测定法,我们新鉴定出 Notch1 和其 Delta 样配体 1(Dll1)是 miR-24-3p 的直接靶标。miR-24-3p 在正常条件下培养的人 ECs 和周细胞中表达。缺氧暴露增加了 EC 中的 miR-24-3p,但不增加周细胞中的 miR-24-3p。转染 miR-24-3p 前体(pre-miR-24-3p)增加了 EC 中的 miR-24-3p 表达,降低了细胞存活、增殖和血管生成能力。miR-24-3p 抑制产生相反的作用。同时用腺病毒(Ad)介导的组成型活性 Notch 细胞内结构域(NICD)转染培养的 ECs 可防止 miR-24-3p 过表达的抗血管生成作用。接下来,我们证明了 Notch 信号通路的减少有助于 miR-24-3p 在体外的抗血管生成作用。在小鼠单侧肢体缺血模型中,局部 miR-24-3p 抑制(通过腺病毒介导的 miR-24-3p 诱饵传递)恢复内皮 Notch 信号并增加毛细血管密度。然而,新血管看起来排列混乱和扭曲,使缺血后血液灌注恢复恶化。为了更好地理解潜在机制,我们扩大了对 miR-24-3p 靶基因的搜索,鉴定出几个参与血管形态发生的基因,如 Wingless(Wnt)信号通路的几个成员、β-catenin 信号成分和 VE-钙粘蛋白,它们协同调节血管生成、周细胞募集到新形成的毛细血管、成熟和新形成的血管的稳定。在这些基因中,我们接下来集中研究β-catenin,以证明 miR-24-3p 抑制降低了缺氧 EC 中的β-catenin 表达,同时减少了周细胞与 EC 的黏附。总之,miR-24-3p 差异靶向几个血管生成调节剂,并有助于自主和非自主 EC 间的相互作用。在缺血肢体中,miR-24-3p 抑制增加了功能失调的微血管的产生,损害了灌注。在治疗性靶向 miR-24-3p 时应谨慎。