Litcius/Paper detail

Design of Sonosensitizers Integrated with Resveratrol Motif for Synergetic Sonodynamic Therapy and Nuclear Factor Kappa B Transcription Suppression of Breast Cancer

Yuanyuan Li, Ming Sun, Jie Yu, Wei Jiang, Wei Tian, Xin Chen, Silong Zhang, Huan He

2023Journal of Medicinal Chemistry15 citationsDOI

Abstract

Sonodynamic therapy (SDT) has been recognized as a spatial–temporal and noninvasive modality for the treatment of deep-seated tumors. However, current sonosensitizers suffer from low sonodynamic efficacy. Herein, we reported the design of nuclear factor kappa B (NF-κB) targeting sonosensitizers ( TR1, TR2, and TR3 ) by integrating a resveratrol motif into a conjugated electron donor–acceptor (triphenylamine benzothiazole) skeleton. Among these sonosensitizers, TR2 with two resveratrol units in one molecule was the most potent for inhibiting NF-κB signaling. Owing to the synergy of high sonodynamic efficacy and NF-κB activation inhibition, TR2 displayed a remarkable sonocytotoxicity to MCF-7 breast cancer cells. Xenograft mice studies demonstrated that TR2 had excellent anticancer potency and biosafety. This study thus opens up a new avenue for the development of efficient organic sonosensitizers for cancer ablation.

Topics & Concepts

ChemistryResveratrolSonodynamic therapyBreast cancerKappaTranscription factorCancer researchCancerPharmacologyInternal medicineBiochemistryApoptosisGeneMedicinePhilosophyLinguisticsUltrasound and Hyperthermia ApplicationsNanoplatforms for cancer theranosticsPhotoacoustic and Ultrasonic Imaging