中国药科大学学报2024，Vol.55Issue(3)：375-380,6.DOI:10.11665/j.issn.1000-5048.2023060703
水溶性冰片磷酸酯前药的设计、合成及生物活性评价
Design,synthesis and biological activity evaluation of water-soluble borneol phosphate prodrug
摘要
Abstract
In this study,structural optimization of borneol was carried out to improve their solubility and promote their further application in stroke therapy.BP-3,a prodrug of borneol,was designed and synthesized based on the principle of phosphate modification.The solubility of BP-3 was determined by evaporative light scattering detector(ELSD),and the degree and speed of drug release were tested in mouse plasma,and the neuroprotective effect of BP-3 was evaluated in mouse model of transient middle cerebral artery occlusion(tMCAO).According to the results,BP-3 was completely soluble in saline at 20 mg/mL;in mouse plasma,approximately 40%of the borneol were released within 2 h;in the tMCAO mouse model,TTC staining showed that BP-3 was effective in reducing the infarct area;Nissl staining showed that BP-3 ameliorated the neuronal injury;the grip and grasping strength tests elucidated that BP-3 reduced the damage of sports ability caused by injury;and the rotating rod test proved that BP-3 could promote the recovery of motor ability in mice.BP-3 has good water solubility,suitable drug release rate and excellent neuroprotective effects,and has broad prospects for drug development.关键词
冰片/磷酸酯/缺血性脑卒中/水溶性改善Key words
borneol/phosphate/ischemic stroke/improved water solubility分类
医药卫生引用本文复制引用
张璐璐,孙美玲,秦亚娟,厉廷有..水溶性冰片磷酸酯前药的设计、合成及生物活性评价[J].中国药科大学学报,2024,55(3):375-380,6.基金项目
国家自然科学基金项目(No.81573280 （）
No.81803349) This study was supported by the National Natural Science Foundation of China(No.81573280 （）
No.81803349) （）
