葡萄籽低聚原花青素作为新型眼用抑菌剂的可行性研究

Feasibility study on grape seed proanthocyanidins as a new ophthalmic antibacterial agent

目的考察葡萄籽低聚原花青素在滴眼剂型中的抑菌能力,为开发新型滴眼液用抑菌剂提供实验基础。方法参照《中华人民共和国药典》(2020年版)四部通则1121测定葡萄籽原花青素的抑菌效力,参照国家卫生和计划生育委员会颁布的《新药(西药)临床前研究指导原则汇编》评价其对健康家兔眼部刺激作用。采用MTT比色法,考察葡萄籽原花青素对人角膜上皮细胞(HCEC)的毒性和对甲型流感病毒H1N1的抑制作用。结果以葡萄籽低聚原花青素为抑菌剂,最低有效添加量为0.10 mg·mL^(-1),抑菌效力可达到A级。0.10 mg·mL^(-1)的葡萄籽低聚原花青素对兔眼无刺激、对HCEC抑制率较低、对甲型H1N1流感病毒有一定抑制作用。结论葡萄籽低聚原青花素可做为滴眼液抑菌剂选择之一。

Objective To investigate the bacteriostatic ability of grape seed proanthocyanidins in eye drops and provide experimental basis for the development of new antibacterial agents for eye drops.Methods The antibacterial ability and antibacterial efficacy of the original antibacterial agents and grape seed proanthocyanidins in eye drops were determined with reference to the general rule 1121 of theⅣvolume of the Chinese Pharmacopoeia,2020 edition,and the ocular irritation of healthy rabbits was evaluated with reference to the compilation of guiding principles for preclinical research of new drugs(western medicines)issued by the national health and Family Planning Commission.In addition,in order to study the advantages of grape seed oligoprocyanidins as bacteriostatic agents,the cytotoxicity of grape seed procyanidins on HCEC cells and the inhibition of influenza A virus H1N1 were investigated by MTT colorimetry.Results With grape seed oligomeric proanthocyanidins as antibacterial agent,the reasonable addition was 0.10 mg·mL^(-1),and the antibacterial ability could reach grade 0.10 mg·mL^(-1)grape seed procyanidins aqueous solution had no irritation to rabbit eyes and had a certain inhibitory effect on influenza A(H1N1)virus.Conclusion Grape seed proanthocyanidin can be used as one of the antibacterial agents in eye drops.