深圳大学学报（理工版）2024，Vol.41Issue(4)：463-470,8.DOI:10.3724/SP.J.1249.2024.04463
比卡鲁胺配位铂的合成及抗肿瘤活性
Synthesis and antitumor activity of bicalutamide-platinum complex
摘要
Abstract
Platinum-based compounds are important anticancer drugs owing to their widespread clinical use and remarkable therapeutic efficacy.However,their side effects and drug resistance remain pressing clinical challenges.In order to improve drug efficacy and overcome drug resistance,we successfully prepared a novel platinum complex(platinum-bicalutamide,Pt-BIC)for photodynamic therapy of tumors by coupling platinum with clinical anti-tumor drug bicalutamide.The target complex was characterized by nuclear magnetic resonance and mass spectrometry.Using the 9,10-anthracenediyl-bis(methylene)dimalonic acid(ABDA)singlet oxygen probe,we detected that Pt-BIC was found to generate singlet oxygen(1O2)under 550 nm light irradiation,which subsequently oxidizes the intracellular reduced coenzyme I(NADH),disrupting the NADH-nicotinamide adenine dinucleotide(NAD+)banlance.Additionally,the phototoxicity of Pt-BIC on tumor cells was measured using 3-(4,5)-dimethylthiahiazo(-z-y1)-3,5-di-phenytetrazoliumromide(MTT)method,and the results showed that the anti-tumor activity of Pt-BIC was superior to that of cisplatin and bicalutamide.Pt-BIC can promote the production of intracellular reactive oxygen species using 2′,7′-dichlorofluorescin diacetate(DCFH-DA)probe under 550 nm light irradiation.This study not only provides a new strategy for the design and development of novel platinum-based drugs,but also holds promise for advancing cancer therapy.关键词
生物化学/光动力治疗/抗肿瘤药物/铂配合物/比卡鲁胺/还原型辅酶IKey words
biochemistry/photodynamic therapy/antitumor drugs/platinum complex/bicalutamide/nicotinamide adenine dinucleotide reduced coenzyme I(NADH)分类
生物科学引用本文复制引用
陈育婷,王浩冰,张平玉..比卡鲁胺配位铂的合成及抗肿瘤活性[J].深圳大学学报（理工版）,2024,41(4):463-470,8.基金项目
National Natural Science Foundation of China(22077085) （22077085）
Natural Science Foundation of Guangdong Province(2023B151502006) 国家自然科学基金资助项目(22077085) （2023B151502006）
广东省自然科学基金资助项目(2023B1515020060) （2023B1515020060）
