Department of Biosciences, Biotechnology, and Biopharmaceutics, University of Bari, Bari, Italy.
Faculty of Medicine, Pharmacology and Experimental Therapeutics Unit, Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, Israel.
IUBMB Life. 2022 Jul;74(7):672-683. doi: 10.1002/iub.2553. Epub 2021 Sep 24.
Riboflavin (Rf), or vitamin B2, is the precursor of FMN and FAD, redox cofactors of several dehydrogenases involved in energy metabolism, redox balance and other cell regulatory processes. FAD synthase, coded by FLAD1 gene in humans, is the last enzyme in the pathway converting Rf into FAD. Mutations in FLAD1 gene are responsible for neuromuscular disorders, in some cases treatable with Rf. In order to mimic these disorders, the Caenorhabditis elegans (C. elegans) gene orthologue of FLAD1 (flad-1) was silenced in a model strain hypersensitive to RNA interference in nervous system. Silencing flad-1 resulted in a significant decrease in total flavin content, paralleled by a decrease in the level of the FAD-dependent ETFDH protein and by a secondary transcriptional down-regulation of the Rf transporter 1 (rft-1) possibly responsible for the total flavin content decrease. Conversely an increased ETFDH mRNA content was found. These biochemical changes were accompanied by significant phenotypical changes, including impairments of fertility and locomotion due to altered cholinergic transmission, as indicated by the increased sensitivity to aldicarb. A proposal is made that neuronal acetylcholine production/release is affected by alteration of Rf homeostasis. Rf supplementation restored flavin content, increased rft-1 transcript levels and eliminated locomotion defects. In this aspect, C. elegans could provide a low-cost animal model to elucidate the molecular rationale for Rf therapy in human Rf responsive neuromuscular disorders and to screen other molecules with therapeutic potential.
核黄素(Rf),又称维生素 B2,是 FMN 和 FAD 的前体,后者是几种参与能量代谢、氧化还原平衡和其他细胞调节过程的脱氢酶的氧化还原辅酶。黄素腺嘌呤二核苷酸合酶(FAD synthase),由人类 FLAD1 基因编码,是将 Rf 转化为 FAD 的途径中的最后一种酶。FLAD1 基因突变可导致神经肌肉疾病,在某些情况下可通过 Rf 治疗。为了模拟这些疾病,Caenorhabditis elegans(秀丽隐杆线虫)FLAD1(flad-1)的基因同源物在神经系统中对 RNA 干扰高度敏感的模型菌株中被沉默。flad-1 的沉默导致总黄素含量显著减少,同时依赖 FAD 的 ETFDH 蛋白水平降低,并可能导致总黄素含量降低的 Rf 转运蛋白 1(rft-1)的转录水平二次下调。相反,发现 ETFDH mRNA 含量增加。这些生化变化伴随着明显的表型变化,包括由于胆碱能传递改变导致的生育力和运动能力受损,这表明对 aldicarb 的敏感性增加。提出了神经元乙酰胆碱的产生/释放可能受到 Rf 动态平衡改变的影响。Rf 补充恢复了黄素含量,增加了 rft-1 转录水平,并消除了运动缺陷。在这方面,秀丽隐杆线虫可以提供一种低成本的动物模型,以阐明人类对 Rf 反应性神经肌肉疾病中 Rf 治疗的分子基础,并筛选具有治疗潜力的其他分子。