Department of Medicine, Division of Bioorganic Chemistry and Molecular Pharmacology, Washington University School of Medicine, St. Louis, MO 63110, USA.
J Biol Chem. 2012 Aug 24;287(35):29837-50. doi: 10.1074/jbc.M112.373654. Epub 2012 Jul 9.
Herein, we demonstrate that calcium-independent phospholipase A(2)γ (iPLA(2)γ) is a critical mechanistic participant in the calcium-induced opening of the mitochondrial permeability transition pore (mPTP). Liver mitochondria from iPLA(2)γ(-/-) mice were markedly resistant to calcium-induced swelling in the presence or absence of phosphate in comparison with wild-type littermates. Furthermore, the iPLA(2)γ enantioselective inhibitor (R)-(E)-6-(bromomethylene)-3-(1-naphthalenyl)-2H-tetrahydropyran-2-one ((R)-BEL) was markedly more potent than (S)-BEL in inhibiting mPTP opening in mitochondria from wild-type liver in comparison with hepatic mitochondria from iPLA(2)γ(-/-) mice. Intriguingly, low micromolar concentrations of long chain fatty acyl-CoAs and the non-hydrolyzable thioether analog of palmitoyl-CoA markedly accelerated Ca(2+)-induced mPTP opening in liver mitochondria from wild-type mice. The addition of l-carnitine enabled the metabolic channeling of acyl-CoA through carnitine palmitoyltransferases (CPT-1/2) and attenuated the palmitoyl-CoA-mediated amplification of calcium-induced mPTP opening. In contrast, mitochondria from iPLA(2)γ(-/-) mice were insensitive to fatty acyl-CoA-mediated augmentation of calcium-induced mPTP opening. Moreover, mitochondria from iPLA(2)γ(-/-) mouse liver were resistant to Ca(2+)/t-butyl hydroperoxide-induced mPTP opening in comparison with wild-type littermates. In support of these findings, cytochrome c release from iPLA(2)γ(-/-) mitochondria was dramatically decreased in response to calcium in the presence or absence of either t-butyl hydroperoxide or phenylarsine oxide in comparison with wild-type littermates. Collectively, these results identify iPLA(2)γ as an important mechanistic component of the mPTP, define its downstream products as potent regulators of mPTP opening, and demonstrate the integrated roles of mitochondrial bioenergetics and lipidomic flux in modulating mPTP opening promoting the activation of necrotic and necroapoptotic pathways of cell death.
在此,我们证明钙非依赖性磷脂酶 A2γ(iPLA2γ)是钙诱导的线粒体通透性转换孔(mPTP)开放的关键机制参与者。与野生型同窝仔相比,iPLA2γ(-/-)小鼠的肝线粒体在存在或不存在磷酸盐的情况下对钙诱导的肿胀具有明显的抗性。此外,iPLA2γ 对映体选择性抑制剂(R)-(E)-6-(溴亚甲基)-3-(1-萘基)-2H-四氢吡喃-2-酮((R)-BEL)在抑制野生型肝线粒体 mPTP 开放方面比(S)-BEL 更有效与 iPLA2γ(-/-)小鼠的肝线粒体相比。有趣的是,长链脂肪酸酰基辅酶 A 的低微摩尔浓度和棕榈酰基辅酶 A 的不可水解硫醚类似物明显加速了野生型小鼠肝线粒体中 Ca2+诱导的 mPTP 开放。添加左旋肉碱使酰基辅酶 A 通过肉碱棕榈酰转移酶(CPT-1/2)进行代谢通道化,并减弱了棕榈酰辅酶 A 介导的钙诱导的 mPTP 开放的放大作用。相比之下,iPLA2γ(-/-)小鼠的线粒体对脂肪酸酰基辅酶 A 介导的钙诱导的 mPTP 开放增强作用不敏感。此外,与野生型同窝仔相比,iPLA2γ(-/-)小鼠肝线粒体对 Ca2+/叔丁基过氧化物诱导的 mPTP 开放具有抗性。这些发现的支持证据是,与野生型同窝仔相比,钙存在或不存在叔丁基过氧化物或苯胂氧化物时,iPLA2γ(-/-)线粒体的细胞色素 c 释放明显减少。总之,这些结果将 iPLA2γ 确定为 mPTP 的重要机制成分,将其下游产物确定为 mPTP 开放的有效调节剂,并证明了线粒体生物能学和脂质组学通量在调节 mPTP 开放促进坏死和坏死凋亡细胞死亡途径的激活中的综合作用。