Riboflavin phosphate

Riboflavin phosphate sodium is a water-soluble phosphate of riboflavin, which retains the main structure and function of riboflavin. the pure Riboflavin phosphate sodium solution exhibits the maximum emission peak at 565nm^[1]. Riboflavin phosphate sodium is a well-known oral nutritional supplement, has been widely used to treat localized inflammatory diseases, such as angulus infectiosus, chilitis, glossitis and radiotherapy related esophagitis^[2][3].

In vitro, the macrophages were treated with various concentrations of Riboflavin phosphate sodium (6.25-200µg/ml) and were incubated for 24h at 37℃ in slide chambers. Phagocytic activity was then determined. Riboflavin phosphate sodium directly activated macrophages in vitro^[4].

In vivo, Riboflavin phosphate sodium (100mg/kg) was injected intraperitoneally or intravenously into ICR male mice at 1 day before the phagocytosis assay. The treated mice showed a significantly higher phagocytic index. Riboflavin phosphate sodium could enhance macrophage function in vivo^[4]. Riboflavin phosphate sodium can be applied as the treatment of sepsis and septic shock. Riboflavin phosphate sodium (10, 20, 40, 80mg/kg) was administered into ICR mice 6h after lipopolysaccharide injection or 1h after bacterial infection by 6h i.v. infusion. Riboflavin phosphate sodium significantly improved lipopolysaccharide-induced endotoxin shock and reduced the lethality of Escherichia coli and Staphylococcus aureus infection. The i.v. infusion of Riboflavin phosphate sodium reduced the elevations of proinflammatory cytokines and nitric oxide induced by lipopolysaccharide^[5].

References:
[1] Feng G Y, Zhang S T, Zhong S L, et al. Temperature and pH dual-responsive supramolecular hydrogels based on riboflavin sodium phosphate and 2,6-Diaminopurine with thixotropic and fluorescent properties. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2021 Dec. Volume 630, 127548
[2] Kodama K, Suzuki M, Toyosawa T, Araki S. Inhibitory mechanisms of highly purified vitamin B2 on the productions of proinflammatory cytokine and NO in endotoxin-induced shock in mice. Life Sci. 2005 Nov 26;78(2):134-9.
[3] Shen K, Huang X E. Clinical investigation in effect of riboflavin sodium phosphate on prevention and treatment for patients with radiotherapy related esophagitis. Asian Pac J Cancer Prev. 2015;16(4):1525-7.
[4] Kimura, M., Suzuki, M., Araki, S., et al. In vitro and in vivo effects of riboflavin sodium phosphate on the phagocytic activity of peritoneal macrophages in mice. Animal Science and Technology. 1996. 67, 368 – 373.
[5] Toyosawa T, Suzuki M, Kodama K, Araki S. Effects of intravenous infusion of highly purified vitamin B2 on lipopolysaccharide-induced shock and bacterial infection in mice. Eur J Pharmacol. 2004 May 25;492(2-3):273-80.

Riboflavin phosphate sodium是核黄素的水溶性磷酸盐衍生物，保留了核黄素的主要结构和功能。纯Riboflavin phosphate sodium溶液在565nm处出现最大发射峰^[1]。Riboflavin phosphate sodium是一种公认的口服营养补充剂，已被广泛用于治疗局部炎症性疾病，如感染性口角炎、唇炎、舌炎以及放疗相关食管炎^[2][3]。

体外实验中，将不同浓度的Riboflavin phosphate sodium（6.25-200µg/ml）加入巨噬细胞，在37℃的腔室载玻片中孵育24h后测定其吞噬活性。Riboflavin phosphate sodium可直接体外激活巨噬细胞^[4]。

体内实验中，Riboflavin phosphate sodium（100mg/kg）在吞噬实验前1天腹腔或静脉注射到ICR雄性小鼠体内。处理过的小鼠显示出显著更高的吞噬指数，Riboflavin phosphate sodium可以增强体内的巨噬细胞功能^[4]。Riboflavin phosphate sodium可用于脓毒症和感染性休克的治疗。在ICR小鼠中，于脂多糖注射后6h或细菌感染后1h，经静脉缓慢输注Riboflavin phosphate sodium（10、20、40、80mg/kg）6h。Riboflavin phosphate sodium显著改善脂多糖诱导的内毒素休克，并降低大肠杆菌和金黄色葡萄球菌感染的致死率。静脉输注Riboflavin phosphate sodium可抑制脂多糖诱导的促炎细胞因子和一氧化氮升高^[5]。