Pyridoxine HCl is the hydrochloride form of vitamin B6 that functions as an antioxidant[1]. Pyridoxine HCl can inhibit the α-glucosidase on the brush border of the small intestine, delaying the digestion of oligosaccharides and disaccharides into monosaccharides, thereby reducing the absorption rate of glucose[2]. Pyridoxine HCl acts as a co-factor to improve the conversion of glyoxylic acid into glycine in ethylene glycol poisoning[3]. Pyridoxine HCl can be used as a model compound to design new drugs and develop related derivatives[4].
In vitro, Pyridoxine HCl treatment for 24 hours significantly inhibited the cell viability of HepG2 cells, with an IC50 value of 6.32±0.98mM[5]. Treatment with 250μg/ml Pyridoxine HCl for 24 hours significantly altered the expression of cell surface markers in lipopolysaccharides (LPS)-stimulated U937 cells, and reduced the secretion of IL-1β, IL-6, IL-10 and TNF-α in the cells[6]. Treatment with 100mg/l Pyridoxine HCl for 24 hours can fully restore the migration ability and response to shear stress of human aortic endothelial cells cultured in 30.5mM glucose[7].
In vivo, Pyridoxine HCl treatment through intraperitoneal injection (350mg/kg; twice a day) for 2 weeks led to the increase in glial fibrillary acidic protein (GFAP)-positive cells in the subgranular zone of the dentate gyrus of C57BL/6 mice and promoted neuroblast differentiation[8]. A single intraperitoneal injection of 180mg/kg dose of Pyridoxine HCl for 30 minutes increased the GABA level in the mouse brain and reduced the levels of glutamate and nitrite, and decreased the anxiety-related behaviors of the mice[9].
References:
[1] Bilski P, Li M Y, Ehrenshaft M, et al. Vitamin B6 (pyridoxine) and its derivatives are efficient singlet oxygen quenchers and potential fungal antioxidants[J]. Photochemistry and photobiology, 2000, 71(2): 129-134.
[2] Kim H H, Kang Y R, Choi H Y, et al. Postprandial anti-hyperglycemic effect of vitamin B6 (pyridoxine) administration in healthy individuals[J]. Food science and biotechnology, 2019, 28(3): 907-911.
[3] Lheureux P, Penaloza A, Gris M. Pyridoxine in clinical toxicology: a review[J]. European Journal of Emergency Medicine, 2005, 12(2): 78-85.
[4] Shtyrlin Y G, Petukhov A S, Strelnik A D, et al. Chemistry of pyridoxine in drug design[J]. Russian Chemical Bulletin, 2019, 68(5): 911-945.
[5] Balakina A, Prikhodchenko T, Amozova V, et al. Preparation, antioxidant properties and ability to increase intracellular no of a new pyridoxine derivative B6NO[J]. Antioxidants, 2021, 10(9): 1451.
[6] Mikkelsen K, Dargahi N, Fraser S, et al. High-dose vitamin B6 (pyridoxine) displays strong anti-inflammatory properties in lipopolysaccharide-stimulated monocytes[J]. Biomedicines, 2023, 11(9): 2578.
[7] Kelso B G, Brower J B, Targovnik J H, et al. Pyridoxine restores endothelial cell function in high glucose[J]. Metabolic Syndrome and Related Disorders, 2011, 9(1): 63-68.
[8] Yoo D Y, Kim W, Kim D W, et al. Pyridoxine enhances cell proliferation and neuroblast differentiation by upregulating the GABAergic system in the mouse dentate gyrus[J]. Neurochemical research, 2011, 36(5): 713-721.
[9] Walia V, Garg C, Garg M. Anxiolytic-like effect of pyridoxine in mice by elevated plus maze and light and dark box: Evidence for the involvement of GABAergic and NO-sGC-cGMP pathway[J]. Pharmacology Biochemistry and Behavior, 2018, 173: 96-106.
Pyridoxine HCl是维生素B6的盐酸盐形式，具有抗氧化剂的作用[1]。Pyridoxine HCl通过抑制小肠刷状缘上的α-葡萄糖苷酶，延缓寡糖和二糖分解为单糖，从而降低葡萄糖的吸收速率[2]。在乙二醇中毒治疗中，Pyridoxine HCl可作为辅因子促进乙醛酸向甘氨酸的转化[3]。此外，Pyridoxine HCl还可作为模型化合物用于新药设计及相关衍生物开发[4]。
在体外，Pyridoxine HCl处理24小时能显著抑制HepG2细胞活力，IC50值为6.32±0.98 mM[5]。使用250μg/ml的Pyridoxine HCl处理脂多糖刺激的U937细胞24小时，可显著改变细胞表面标志物的表达，并降低细胞内IL-1β、IL-6、IL-10和TNF-α的分泌[6]。用100mg/l的Pyridoxine HCl处理24小时，能完全恢复高糖（30.5mM）条件下培养的人主动脉内皮细胞的迁移能力及对剪切力的响应[7]。
在体内，通过每日两次腹腔注射Pyridoxine HCl（350mg/kg），连续两周，可增加C57BL/6小鼠齿状回颗粒下区的胶质纤维酸性蛋白阳性细胞数量，并促进神经母细胞分化[8]。单次腹腔注射180mg/kg剂量的Pyridoxine HCl 30分钟后，能提高小鼠脑内GABA水平，降低谷氨酸和亚硝酸盐含量，并减少焦虑相关行为[9]。