Stem Cell and Tissue Engineering Lab, Beijing Institute of Transfusion Medicine, Beijing, China.
Capital Medical University Youan hospital, Beijing, China.
J Cell Mol Med. 2017 Dec;21(12):3214-3223. doi: 10.1111/jcmm.13225. Epub 2017 May 30.
Both primary hepatocytes and stem cells-derived hepatocyte-like cells (HLCs) are major sources for bioartificial liver (BAL). Maintenance of hepatocellular functions and induction of functional maturity of HLCs are critical for BAL's support effect. It remains difficult to assess and improve detoxification functions inherent to hepatocytes, including ammonia clearance. Here, we aim to assess ammonia metabolism and identify ammonia detoxification enhancer by developing an imaging strategy. In hepatoma cell line HepG2, and immortalized hepatic cell line LO2, carbamoyl phosphate synthetase 1 (CPS1) gene, the first enzyme of ammonia-eliminating urea cycle, was labelled with fluorescence protein via CRISPR/Cas9 system. With the reporter-based screening approach, cellular detoxification enhancers were selected among a collection of 182 small molecules. In both CPS1 reporter cell lines, the fluorescence intensity is positively correlated with cellular CPS1 mRNA expression, ammonia elimination and secreted urea, and reflected ammonia detoxification in a dose-dependent manner. Surprisingly, high-level CPS1 reporter clones also reserved many other critical hepatocellular functions, for example albumin secretion and cytochrome 450 metabolic functions. Sodium phenylbutyrate and resveratrol were identified to enhance metabolism-related gene expression and liver-enriched transcription factors C/EBPα, HNF4α. In conclusion, the CPS1-reporter system provides an economic and effective platform for assessment of cellular metabolic function and high-throughput identification of chemical compounds that improve detoxification activities in hepatic lineage cells.
原代肝细胞和干细胞来源的肝细胞样细胞(HLC)是生物人工肝(BAL)的主要来源。维持肝细胞功能和诱导 HLC 的功能成熟对于 BAL 的支持作用至关重要。评估和改善固有肝细胞的解毒功能,包括氨清除,仍然具有挑战性。在这里,我们旨在通过开发一种成像策略来评估氨代谢并确定氨解毒增强剂。在肝癌细胞系 HepG2 和永生化肝细胞系 LO2 中,通过 CRISPR/Cas9 系统将氨消除尿素循环的第一酶氨甲酰磷酸合成酶 1(CPS1)基因标记为荧光蛋白。通过基于报告基因的筛选方法,从 182 种小分子化合物中选择细胞解毒增强剂。在 CPS1 报告细胞系中,荧光强度与细胞 CPS1 mRNA 表达、氨消除和分泌的尿素呈正相关,并以剂量依赖的方式反映氨解毒作用。令人惊讶的是,高水平的 CPS1 报告基因克隆还保留了许多其他关键的肝细胞功能,例如白蛋白分泌和细胞色素 450 代谢功能。苯丁酸钠和白藜芦醇被鉴定为增强与代谢相关的基因表达和肝富集转录因子 C/EBPα、HNF4α。总之,CPS1 报告基因系统为评估细胞代谢功能和高通量鉴定改善肝系细胞解毒活性的化学化合物提供了一种经济有效的平台。