Department of Pharmacology & Toxicology and Brown Cancer Center, University of Louisville School of Medicine, Louisville, Kentucky 40202, USA.
Toxicol Sci. 2022 Nov 23;190(2):158-172. doi: 10.1093/toxsci/kfac103.
Arylamine N-acetyltransferase 2 (NAT2) is well-known for its role in phase II metabolism of xenobiotics and drugs. More recently, genome wide association studies and murine models implicated NAT2 in regulation of insulin sensitivity and plasma lipid levels. However, the mechanism remains unknown. Transcript levels of human NAT2 varied dynamically in HepG2 (hepatocellular) cells, depending on the nutrient status of the culture media. Culturing the cells in the presence of glucose induced NAT2 mRNA expression as well as its N-acetyltransferase activity significantly. In addition, insulin or acetate treatment also significantly induced NAT2 mRNA. We examined and compared the glucose- and acetate-dependent changes in NAT2 expression to those of genes involved in glucose and lipid metabolism, including FABP1, CPT1A, ACACA, SCD, CD36, FASN, ACLY, G6PC, and PCK1. Genes that are involved in fatty acid transport and lipogenesis, such as FABP1 and CD36, shared a similar pattern of expression with NAT2. In silico analysis of genes co-expressed with NAT2 revealed an enrichment of biological processes involved in lipid and cholesterol biosynthesis and transport. Among these, A1CF (APOBEC1 complementation factor) showed the highest correlation with NAT2 in terms of its expression in normal human tissues. The current study shows, for the first time, that human NAT2 is transcriptionally regulated by glucose and insulin in liver cancer cell lines and that the gene expression pattern of NAT2 is similar to that of genes involved in lipid metabolism and transport.
芳香族胺 N-乙酰基转移酶 2(NAT2)因其在异生物质和药物的 II 期代谢中的作用而广为人知。最近,全基因组关联研究和小鼠模型表明 NAT2 参与了胰岛素敏感性和血浆脂质水平的调节。然而,其机制尚不清楚。人 NAT2 的转录水平在 HepG2(肝细胞)细胞中根据培养物中营养物质的状态动态变化。在存在葡萄糖的情况下培养细胞会显著诱导 NAT2 mRNA 表达及其 N-乙酰基转移酶活性。此外,胰岛素或乙酸盐处理也显著诱导了 NAT2 mRNA。我们检查并比较了 NAT2 表达的葡萄糖和乙酸盐依赖性变化与涉及葡萄糖和脂质代谢的基因的变化,包括 FABP1、CPT1A、ACACA、SCD、CD36、FASN、ACLY、G6PC 和 PCK1。参与脂肪酸转运和脂肪生成的基因,如 FABP1 和 CD36,与 NAT2 的表达模式相似。与 NAT2 共表达基因的计算机分析显示,与脂质和胆固醇生物合成和转运相关的生物学过程富集。在这些基因中,A1CF(APOBEC1 补体因子)在正常人类组织中与 NAT2 的表达相关性最高。本研究首次表明,人 NAT2 在肝癌细胞系中受葡萄糖和胰岛素的转录调控,并且 NAT2 的基因表达模式与参与脂质代谢和转运的基因相似。