A curcumin-based HDACs inhibitor for targeted sonodynamic therapy of breast cancer
Xing Lu1, Ziwei Wang2, Yu Zhang1
1Key laboratory of Plant Resource Conservation and Germplasm Innovation in Mountainous Region (Ministry of Education), Guizhou Engineering Laboratory for Synthetic Drugs, School of Pharmaceutical Sciences, Guizhou University, Guiyang 550025, PR China.
Abstract:
Histone Deacetylases (HDACs) have emerged as key therapeutic targets in cancer treatment. In this study, we designed CURSAHA, a multifunctional anticancer agent, through the pharmacophore fusion of Vorinostat and curcumin. CURSAHA demonstrates broad-spectrum inhibitory activity against HDACs, effectively suppressing tumor cells with overexpressed HDACs. Notably, CURSAHA generates reactive oxygen species (ROS) under ultrasonic conditions, exhibiting sonodynamic therapeutic activity. Additionally, CURSAHA downregulates HDACs through redox reactions involving ROS. These properties enable CURSAHA to exhibit robust antitumor activity in both in vitro and in vivo models, highlighting its potential as a promising candidate for further development in cancer therapy.
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