Screening of flavor compounds using <i>Ucp1</i>-luciferase reporter beige adipocytes identified 5-methylquinoxaline as a novel UCP1-inducing compound
Screening of flavor compounds using <i>Ucp1</i>-luciferase reporter beige adipocytes identified 5-methylquinoxaline as a novel UCP1-inducing compound
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使用<i>Ucp1</i>-荧光素酶报告基因米色脂肪细胞筛选风味化合物，鉴定出 5-甲基喹喔啉是一种新型 UCP1 诱导化合物
DOI：
10.1093/bbb/zbab216
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发表时间：
2021
期刊：
影响因子：
--
通讯作者：
Goto Tsuyoshi
中科院分区：
文献类型：
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作者：
Kawarasaki Satoko;Matsuo Kazuki;Kuwata Hidetoshi;Zhou Lanxi;Kwon Jungin;Ni Zheng;Takahashi Haruya;Nomura Wataru;Kenmotsu Hisanori;Inoue Kazuo;Kawada Teruo;Goto Tsuyoshi
棕色或米色脂肪细胞中的解偶联蛋白1（UCP 1）是一种线粒体蛋白，预计可增强全身能量消耗。为了高通量筛选UCP 1转录活性调节因子，我们建立了小鼠腹股沟白色脂肪组织来源的UCP 1-luciferase报告基因前体脂肪细胞系。使用该报告基因前脂肪细胞系，筛选了654种风味化合物，并鉴定了一种新的Ucp 1表达诱导化合物5-甲基喹喔啉。用5-甲基喹喔啉处理的脂肪细胞显示Ucp 1 mRNA表达水平增加，耗氧量增加。5-甲基喹喔啉通过过氧化物酶体增殖物激活受体γ共激活因子1α（PGC 1 α）诱导Ucp 1的表达，而5-甲基喹喔啉诱导的PGC 1 α激活似乎部分受其磷酸化或去乙酰化的调节。因此，我们的Ucp 1-荧光素酶报告基因前脂肪细胞系是筛选Ucp 1诱导化合物的有用工具。
Uncoupling protein 1 (UCP1) in brown or beige adipocytes is a mitochondrial protein that is expected to enhance whole-body energy expenditure. For the high-throughput screening of UCP1 transcriptional activity regulator, we established a murine inguinal white adipose tissue-derivedUcp1-luciferase reporter preadipocyte line. Using this reporter preadipocyte line, 654 flavor compounds were screened, and a novelUcp1expression-inducing compound, 5-methylquinoxaline, was identified. Adipocytes treated with 5-methylquinoxaline showed increasedUcp1mRNA expression levels and enhanced oxygen consumption. 5-Methylquinoxaline inducedUcp1expression through peroxisome proliferator-activated receptor γ coactivator 1α (PGC1α), and 5-methylquinoxaline-induced PGC1α activation seemed to be partially regulated by its phosphorylation or deacetylation. Thus, ourUcp1-luciferase reporter preadipocyte line is a useful tool for screening ofUcp1inductive compounds.