The nuclear receptor, REV-ERBα, has a key role in circadian rhythms and requires heme as its ligand. The present study determined whether the heme precursor, 5-aminolevulinic acid (ALA), affects REV-ERBα and its target genes. When exposed to ALA, the human lung diploid cell line, WI-38, exhibited activation of REV-ERBα and repression of the transcription of REV-ERBα target genes, including BMAL1, an essential component of the circadian oscillator. Moreover, co-incubation of sodium ferrous citrate (SFC) and ALA also activated REV-ERBα and repressed the transcription of REV-ERBα target genes. These results indicate that ALA regulates human circadian rhythms via REV-ERBα.
Keywords: 5-Aminolevulinic acid; ALA, 5-aminolevulinic acid; Circadian rhythms; Ct, cycle threshold; DMEM, Dulbecco’s modified Eagle’s Medium; HPLC, high-performance liquid chromatography; Porphyrin metabolism; PpIX, protoporphyrin IX; REV-ERBα; SFC, sodium ferrous citrate.