Design, synthesis and biological activity evaluation of water-soluble borneol phosphate prodrug / 中国药科大学学报
Journal of China Pharmaceutical University
; (6): 375-380, 2024.
Article
de Zh
| WPRIM
| ID: wpr-1045658
Bibliothèque responsable:
WPRO
ABSTRACT
@#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.
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Indice:
WPRIM
langue:
Zh
Texte intégral:
Journal of China Pharmaceutical University
Année:
2024
Type:
Article