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Cross-linked lipoic acid nanocapsules serve as H_(2)O_(2) amplifier to strengthen the H_(2)O_(2)-sensitive prodrug activation

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中国科学:化学英文版 2023年第9期66卷 2654-2663页

作者： Jiangbing Tan Pei Jing Xiao Xiao Yulong Liao Chunyan Liao Shiyong Zhang College of Biomedical Engineering and National Engineering Research Center for Biomaterials Sichuan UniversityChengdu 610064China Department of Pharmacy the Affiliated Hospital of Southwest Medical UniversityLuzhou 646000China

The H_(2)O_(2) -triggered prodrug activation represents a hot topic while the low H_(2)O_(2) level of cancer cells hindered the complete activation of parent drugs and resulted in the poor therapeutic effect. Here, we developed an H_(2)O_(2) amplifier fabricated by crosslinked lipoic acid nanocapsules(cLANCs), which would selectively elevate the intracellular H_(2)O_(2) level of cancer cells 3.4-fold higher than that of untreated cancer cells so as to speed up the activation of parent drug from the loaded prodrugs(Pro-5-FU). The cytotoxicity showed that the killing effect of Pro-5-FU loaded in cLANCs(Pro-5-FU@cLANCs) arrived up to 1.6-time higher than that of Pro-5-FU alone against A549 cells, and was even close to free 5-FU. The in vivo anticancer evaluation gave the tumor inhibition rate(TIR) and survival rate(SR) of Pro-5-FU@cLANCs against A549 tumor-bearing nude mice up to 73.1% and 80%,respectively, much higher than those of Pro-5-FU(TIR: 41.2%, SR: 20%) or free 5-FU(TIR: 50.6%, SR: 0%). This nanodrug constructed the first example that utilizes the drug carriers as H_(2)O_(2) amplifier to strengthen the prodrug activation.

关键词： cancer therapy prodrug activation H_(2)O_(2)amplifier drug carrier

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Nanozyme-activating prodrug therapies:A review

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Chinese Chemical Letters 2024年第2期35卷 138-150页

作者： Yudong Wu Wujun Chen Chao Wang Dongming Xing The Affiliated Hospital of Qingdao University Qingdao UniversityQingdao 266071China School of Life Sciences Tsinghua UniversityBeijing 100084China

Enzyme prodrug therapies(EPTs)have been intensively explored as attractive approaches to selective activation of systemically administered benign prodrugs by the exogenous enzymes or enzymes expressed at the desired target site,thus achieving localized,site-specific therapeutic effect.Many effective strategies(e.g.,antibody-,viral-,gene-,as well as polymer-directed EPT)have been developed for enzyme localization to locally activate systemically administered benign prodrugs.Nevertheless,intrinsic limitations(e.g.,complex intracellular environment and catalyst instability)make the practical application of EPT strategies a task that presents itself as highly challenging.As a promising alternative to natural enzyme,nanozyme has attracted substantial attention since its discovery in 2007,mainly due to the advantages of robust catalytic activity,high stability,low cost,and facile synthesis.Recently,nanozyme-activated prodrug strategies bring a new opportunity for targeted therapy,referred to as nanozyme-activating prodrug therapies.This review focuses on recently reported nanozyme-activated prodrug strategies,aiming to provide some new insights into the potential applications in site-specific drug synthesis.

关键词： Enzyme prodrug therapy Nanozyme prodrug activation Chemotherapy Drug synthesis

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Time-course monitoring of in vitro biotransformation reaction via solid-phase microextraction-ambient mass spectrometry approaches

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Journal of Pharmaceutical Analysis 2022年第1期12卷 186-191页

作者： Karol Jaroch Janusz Pawliszyn Department of Chemistry University of WaterlooWaterlooN2L 3G1Canada Department of Pharmacodynamics and Molecular Pharmacology Faculty of PharmacyCollegium Medicum in BydgoszczNicolaus Copernicus University in Toruń Poland85090BydgoszczPoland

The solid-phase microextraction technique quantifies analytes without considerably affecting the sample composition.Herein,a proof-of-concept study was conducted to demonstrate the use of coated probe electrospray ionization(coated-PESI)and coated blade spray(CBS)as ambient mass spectrometry approaches for monitoring drug biotransformation.The ability of these methods was investigated for monitoring the dephosphorylation of a prodrug,combretastatin A4 phosphate(CA4P),into its active form,combretastatin A4(CA4),in a cell culture medium supplemented with fetal bovine serum.The CBS spot analysis was modified to achieve the same extraction efficiency as protein precipitation and obtained results in 7 min.Because coated-PESI performs extraction without consuming any samples,it is the preferred technique in the case of a limited sample volume.Although coated-PESI only extracts small quantities of analytes,it uses the desorption solvent volume of 5-10 pL,resulting in high sensitivity,thus allowing the detection of compounds after only 1 min of extraction.The biotransformation of CA4P into CA4 via phosphatases occurs within the simple matrix,and the proposed sample preparation techniques are suitable for monitoring the biotransformation.

关键词： Solid-phase microextraction Coated probe electrospray ionization Coated blade spray Combretastatin Biotransformation prodrug activation

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