Harnessing the modulation of redox homeostasis represents a promising anticancer strategy. Here, we design and evaluate Se-SN38, a prodrug of the camptothecin (CPT) derivative 7-ethyl-10-hydroxycamptothecin (SN38) with a cyclic five-membered diselenide moiety for redox-triggered activation. We demonstrate that Se-SN38 exhibits superior cytotoxicity in various cancer cell lines over the parent drug SN38 or the control prodrug S-SN38, a sulfur analogue of Se-SN38. This increased potency is attributed to the efficient release of SN38 and induction of oxidative stress, as demonstrated by a significant rise in reactive oxygen species production, along with a marked depletion of cellular total thiols and a decreased GSH/GSSG ratio. Furthermore, Se-SN38 treatment leads to inhibition of thioredoxin reductase activity, disruption of mitochondrial membrane potential, and induction of DNA damage, culminating in apoptosis. These findings suggest that Se-SN38 represents a promising strategy to enhance the therapeutic efficacy of CPT derivatives by exploiting the unique redox-active properties of cyclic five-membered diselenide to induce oxidative stress and apoptosis.

01 May 2025·International Journal of Biological Macromolecules

Graphene quantum dot-induced photo redox ATRP synthesis of lignin-based copolymers for the fabrication of silver-bearing and camptothecin-loaded micelles

Article

Author: Li, Zhihui ; Li, Hailiang ; Yang, Chufen ; Lin, Yibin ; Chen, Duoqu ; Li, Jiaxin ; Lin, Wenjing ; Liang, Xiaobing ; Xiao, Yonghui ; Yi, Guobin

Photo redox atom transfer radical polymerization (ATRP) represents an excellent technique for forming multifunctional polymers. However, there was little report on photo redox ATRP of graphene quantum dots (GQDs). Herein, we reported that introduced GQDs to ATRP in DMF solvent for the first time, significantly reducing the amount of copper catalyst (<500 ppm) required for the synthesis of alkali lignin-poly(N-isopropylacrylamide)-poly(N, N-dimethylaminoethyl methacrylate)-poly(poly(ethylene glycol) methyl ether methacrylate) (AL-(PNIPAM-PDMAEMA-PPEGMA)₂). The copolymer had molecular weight of 46,884 and polydispersity index (PDI) of 1.07. The micelles self-assembled from AL-(PNIPAM-PDMAEMA-PPEGMA)₂ in aqueous solution served as an excellent template for the simultaneous in situ preparation of silver nanoparticles (AgNPs) and the encapsulation of the hydrophobic anticancer drug camptothecin (CPT). By adjusting the mole ratio of [DMAEMA]:[AgNO₃], a series of AgNPs with controllable sizes (2.5-20.6 nm) could be obtained. AL-(PNIPAM-PDMAEMA-PPEGMA)₂@Ag@CPT exhibited temperature and pH-sensitive release properties, releasing 80 % of the drug in an acidic and 37 °C tumor environment within 120 h. Furthermore, 150 μg/mL AL-(PNIPAM-PDMAEMA-PPEGMA)₂@Ag@CPT effectively killed 75 % of cells within 48 h. 800 μg/mL AL-(PNIPAM-PDMAEMA-PPEGMA)₂@Ag@CPT demonstrated highly efficient antibacterial effects. All these results suggest its potential application value in synergistic antitumor and antibacterial treatment system.

01 May 2025·International Journal of Biological Macromolecules

Targeting matrix metalloproteinases activating and indoleamine 2,3-dioxygenase suppression for triple-negative breast cancer multimodal therapy

Article

Author: Dou, Qingqing ; Jiang, Peixiao ; Hu, Xiaoxiao ; Zhang, Mo ; Wang, Jing

The dense extracellular matrix (ECM) and immunosuppressive tumor microenvironment represent two major challenges in the treatment of triple-negative breast cancer (TNBC). To address these obstacles, this study has developed a polymer micelle (NTP) for ECM remodeling and mitigation the immune microenvironment, based on activating endogenous matrix metalloproteinases (MMP) and suppression indoleamine 2,3-dioxygenase (IDO). Through self-assembly technology, this micelle effectively incorporates chemotherapy drugs (camptothecin (CPT) and cinnamaldehyde (CA)), reactive oxygen species (ROS) stimulants, nitric oxide (NO) donor and IDO inhibitor (NLG919), where CPT and CA have been reported to help generating ROS mainly in the mitochondrion. The guanidine group of poly-L-arginine (PArg), as an NO donor, can react with ROS to generate NO. The micelles aim to achieve significant therapeutic outcomes through robust drug penetration and anti-tumor immunity in multimodal therapy. They exhibit remarkable tumor tissue penetration ability, facilitating precise targeting of mitochondria and ROS production stimulation. Building upon this therapeutic foundation, the micellar system achieves in situ NO release, which effectively degrades the ECM through the activation of MMPs, while simultaneously promoting tumor cells apoptosis. Furthermore, the encapsulated NLG919 can be released and effectively mitigating the immunosuppressive milieu and triggering anti-tumor immune responses. Experimental results demonstrate that the micelles exhibit significant anti-tumor effects both in vitro and in vivo, accompanied by favorable biocompatibility. This study provides new insights into the application of subcellular targeting drug delivery systems in TNBC treatment, potentially heralding a new breakthrough in TNBC therapy.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Preclinical	China	Shanghai Jiao Tong University	01 Sep 2024
Pain	Preclinical	China	Shanghai Jiao Tong University	01 Sep 2024

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