Department of Medicine, Division of Endocrinology, David Geffen School of Medicine at UCLA, 650 Charles E. Young Dr., Los Angeles, CA 90095, USA.
Department of Molecular and Medical Pharmacology, David Geffen School of Medicine at UCLA, 650 Charles E. Young Dr., Los Angeles, CA 90095, USA.
Sci Transl Med. 2021 May 19;13(594). doi: 10.1126/scitranslmed.abd1869.
Although the role of hydrophilic antioxidants in the development of hepatic insulin resistance and nonalcoholic fatty liver disease has been well studied, the role of lipophilic antioxidants remains poorly characterized. A known lipophilic hydrogen peroxide scavenger is bilirubin, which can be oxidized to biliverdin and then reduced back to bilirubin by cytosolic biliverdin reductase. Oxidation of bilirubin to biliverdin inside mitochondria must be followed by the export of biliverdin to the cytosol, where biliverdin is reduced back to bilirubin. Thus, the putative mitochondrial exporter of biliverdin is expected to be a major determinant of bilirubin regeneration and intracellular hydrogen peroxide scavenging. Here, we identified ABCB10 as a mitochondrial biliverdin exporter. ABCB10 reconstituted into liposomes transported biliverdin, and ABCB10 deletion caused accumulation of biliverdin inside mitochondria. Obesity with insulin resistance up-regulated hepatic ABCB10 expression in mice and elevated cytosolic and mitochondrial bilirubin content in an ABCB10-dependent manner. Revealing a maladaptive role of ABCB10-driven bilirubin synthesis, hepatic ABCB10 deletion protected diet-induced obese mice from steatosis and hyperglycemia, improving insulin-mediated suppression of glucose production and decreasing lipogenic SREBP-1c expression. Protection was concurrent with enhanced mitochondrial function and increased inactivation of PTP1B, a phosphatase disrupting insulin signaling and elevating SREBP-1c expression. Restoration of cellular bilirubin content in ABCB10 KO hepatocytes reversed the improvements in mitochondrial function and PTP1B inactivation, demonstrating that bilirubin was the maladaptive effector linked to ABCB10 function. Thus, we identified a fundamental transport process that amplifies intracellular bilirubin redox actions, which can exacerbate insulin resistance and steatosis in obesity.
尽管亲水性抗氧化剂在肝胰岛素抵抗和非酒精性脂肪性肝病的发展中的作用已得到充分研究,但疏水性抗氧化剂的作用仍知之甚少。已知的疏水性过氧化氢清除剂是胆红素,它可以被氧化为胆绿素,然后被细胞质胆绿素还原酶还原回胆红素。胆红素在线粒体内部氧化为胆绿素后,必须将胆绿素输出到细胞质,在细胞质中胆绿素被还原回胆红素。因此,胆绿素的推定线粒体输出器预计是胆红素再生和细胞内过氧化氢清除的主要决定因素。在这里,我们鉴定出 ABCB10 是一种线粒体胆绿素输出器。ABC B10 重组到脂质体中可转运胆绿素,而 ABCB10 的缺失导致胆绿素在线粒体内部积累。肥胖伴胰岛素抵抗会导致小鼠肝脏 ABCB10 表达上调,并以 ABCB10 依赖性方式升高细胞溶质和线粒体胆红素含量。揭示了 ABCB10 驱动的胆红素合成的适应性不良作用,肝 ABCB10 缺失可防止饮食诱导的肥胖小鼠发生脂肪变性和高血糖,改善胰岛素介导的葡萄糖生成抑制作用,并降低脂肪生成 SREBP-1c 的表达。保护作用与增强的线粒体功能和 PTP1B 的失活同时发生,PTP1B 是一种破坏胰岛素信号并升高 SREBP-1c 表达的磷酸酶。在 ABCB10 KO 肝细胞中恢复细胞内胆红素含量可逆转线粒体功能和 PTP1B 失活的改善,表明胆红素是与 ABCB10 功能相关的适应性不良效应物。因此,我们确定了一种基本的转运过程,该过程放大了细胞内胆红素氧化还原作用,从而加剧了肥胖中的胰岛素抵抗和脂肪变性。