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三种新型环丙沙星衍生物的声动力学活性研究。

Investigation into the Sonodynamic Activity of Three Newly Synthesized Derivatives of Ciprofloxacin.

机构信息

Artemisinin Research Center, China Academy of Chinese Medical Sciences, Beijing 100700, China.

School of Pharmaceutical Sciences, Liaoning University, Shenyang 110036, China.

出版信息

Molecules. 2024 Aug 7;29(16):3735. doi: 10.3390/molecules29163735.

Abstract

Sonosensitizers play a crucial role in the efficacy of sonodynamic antitumor therapy (SDT) and sonodynamic antimicrobial chemotherapy (SACT), highlighting the necessity for the development of new compounds with good sonodynamic activity. In this study, three novel 3-substituted ciprofloxacin derivatives (CIPD1, CIPD2, and CIPD3) were designed and synthesized. Their sonodynamic activities were evaluated by assessing the damage to bovine serum albumin (BSA) and (). Furthermore, the potential mechanism underlying their sonodynamic damage activities was investigated by detecting reactive oxygen species (ROS) under ultrasound irradiation (US). The results demonstrated that all three derivatives exhibited enhanced sonodynamic damage to BSA and under US, with CIPD1 and CIPD2 showing superior effectiveness compared to CIP. Both the concentrations of derivatives and the duration of ultrasound irradiation were found to significantly impact their sonodynamic effects. All three CIP derivates could be activated to produce ROS following ultrasound irradiation, primarily consisting of O and ·OH. The levels of ROS production were positively correlated with their sonodynamic activities, potentially explaining the mechanism underlying their sonodynamic damage activities.

摘要

声敏剂在声动力抗肿瘤治疗(SDT)和声动力抗菌化疗(SACT)的疗效中起着至关重要的作用,这凸显了开发具有良好声动力学活性的新型化合物的必要性。在这项研究中,设计并合成了三种新型的 3-取代环丙沙星衍生物(CIPD1、CIPD2 和 CIPD3)。通过评估牛血清白蛋白(BSA)和()的损伤来评估它们的声动力学活性。此外,通过在超声辐射(US)下检测活性氧(ROS)来研究它们声动力学损伤活性的潜在机制。结果表明,所有三种衍生物在 US 下均增强了对 BSA 和 的声动力学损伤,CIPD1 和 CIPD2 的效果优于 CIP。衍生物的浓度和超声辐射的持续时间都对其声动力学效应有显著影响。所有三种 CIP 衍生物在超声辐射后都能被激活产生 ROS,主要包括 O 和·OH。ROS 的产生水平与它们的声动力学活性呈正相关,这可能解释了它们声动力学损伤活性的机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9c33/11357595/5b5e71c274ba/molecules-29-03735-g001.jpg

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