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A Near Infrared-Modulated Thermosensitive Hydrogel for Stabilization of Indocyanine Green and Combinatorial Anticancer Phototherapy
摘要： Indocyanine green (ICG), a multifunctional near-infrared (NIR) imaging agent approved by the FDA, has been extensively used in clinical cancer theranosis, but limited by its inherent instability, short plasma half-life and lack of targeting ability. Herein, an in situ formed photothermal network based thermosensitive hydrogel (PNT-gel) constructed by supramolecular cross-linking conjugated polymers was developed for stabilization of ICG and efficient combinatorial photothermal/photodynamic antitumor therapy. While the conjugated polymeric backbone in PNT-gel anchored the aromatic phototherapeutic agent ICG via π–π stacking interactions to avoid premature leakage, it also directly converted low-dose NIR light to induce localized hyperthermia to enhance the photothermal effect. The PNT-gel shows a reversible gel-to-sol upper critical solution temperature (UCST) that is slightly above the body temperature. Therefore, the controlled release of ICG was switched on or off by NIR via photothermal-induced gel-sol transition. In vitro and in vivo antitumor experiments demonstrated that ICG loaded PNT-gel not only efficiently induced the killing of 4T1 cancer cells, but also achieved almost complete eradication of 4T1 cells by one-dose in combinatorial photothermal/photodynamic therapy under irradiation of a low-dose 808 nm laser (0.14 W cm-2). Additionally, the combinational therapy proved to enhance the effectiveness of photodestruction without tumor recurrence compared with intratumoral injection photothermal therapy (PTT) or photodynamic therapy (PDT) treatment alone.
关键词： Near Infrared-Modulated Thermosensitive Hydrogel,Combinatorial Anticancer Phototherapy,Indocyanine Green,Photodynamic Therapy,Photothermal Therapy
更新于2025-11-21 11:08:12
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Effect of the Photodynamic Therapy Applications with Potent Microalgae Constituents on Several Types of Tumor
摘要： Background: In recent years, microalgae (MA) have attracted much interest considering their possible therapeutic application. They contain active natural compounds or derivatives (extracts, pure or chemically modified compounds) that have increasing applications in the pharmaceutical industry. Methods: The present study aims to examine microalgae for new photosensitizers, with a potential to be used in the light-associated treatment of tumors. Semi-purified extracts of several microalgae strains were evaluated as photosensitizers for photodynamic therapy (PDT) applications. Four tumor cell lines (A549, LNCap, MCF-7, and MDA-MB 435) were used to assess 34 samples extracted by three methods: cellulase enzyme, lysozyme enzyme and ultra-sonication. The fluorescence measurements and the recorded images alongside the spectral intensities between 650–800 nm wavelengths provided characteristic features to some of the contents of the examined extracts. Results: Several microalgae constituents activated by blue light (BL), red light (RL) or both (in sequence) exhibited significant effects on the viability of the tumor cell lines, decreasing it as much as 95% for certain MA constituents. Majority of the MA constituents showed a higher phototoxicity after exposure to both blue and red lights than the photo-induced toxicity when exposed to a single light source. The viability of the tumor cells exhibited the dose dependent response with the MA constituents. Conclusion: The results clearly showed that MA constituents are potential photosensitizers that have a significant photo-damage effects on the tested cancer cells.
关键词： Anticancer agent,Microalgae,Enzymatic extraction,Photodynamic therapy,Photosensitizers
更新于2025-09-23 15:23:52
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2D Ti2C (MXene) as a novel highly efficient and selective agent for photothermal therapy
摘要： Photothermal therapy (PTT) has shown significant potential for anti-cancer modality. In this report, according to our best knowledge, we explore for the first time Ti2C-based MXene as a novel, highly efficient and selective agent for photothermal therapy (PTT). Ti2C superficially modified with PEG was obtained from the layered, commercially available Ti2AlC MAX phase in the process of etching aluminum layers using concentrated HF, and characterized by scanning electron microscopy (SEM), high-resolution transmission electron microscopy (HREM) as well as X-Ray photoelectron spectroscopy for chemical analysis (ESCA-XPS). The PEG-coated Ti2C flakes showed a satisfactory photothermal conversion efficacy (PTCE) and good biocompatibility in wide range of the tested concentrations. Through in vitro studies, the PEG-modified Ti2C demonstrated notable NIR-induced ability to cancerous cells’ ablation with minimal impact on non-malignant cells up to the concentration of 37.5 μg ml-1. The applied doses of Ti2C_PEG in our work were even 24 times lower comparing other MXene-based photothermal agents. This work is expected to expand the utility of 2D MXenes to biomedical applications through the development of an entirely novel agents for photothermal therapy.
关键词： photothermal therapy,biological activity,light-to-heat conversion,2D Ti2C MXenes,anticancer therapy
更新于2025-09-23 15:23:52
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Novel π-conjugated systems based on pyrimidine N-Oxide
摘要： Pyrimidine N-oxide moiety for the first time was used as a heterocyclic core for the construction of π-conjugated molecules with fluorescent properties. For the synthesis of the title compounds a simple two-step protocol starting from readily available 4-fluoro-2-methylpyrimidine N-oxides was elaborated. A series of 17 novel pyrimidine N-oxide derivatives containing various functional substituents and π-conjugated systems of different length were obtained. The title compounds revealed fluorescent properties in visible region, possessing emission maximum up to 575 nm. Deoxygenation of the N-oxide group led to the loss of visible fluorescence. The chemosensor properties towards TFA and a number of metal cations were demonstrated for 3a, the first representative of the title series. Cytotoxic activity against breast adenocarcinoma cell line was found for three pyrimidine N-oxide derivatives 3b,i,n. Pyrimidine N-oxide 3a was shown to possess excellent biocompatibility and capability to enter cells, that makes it a promising structure for development of bioimaging fluorescent probes.
关键词： Anticancer activity,Pyrimidines,π-Conjugated systems,Fluorescence,Knoevenagel condensation,Metal cations
更新于2025-09-23 15:23:52
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Polypyrrole microcapsules loaded with gold nanoparticles: Perspectives for biomedical imaging
摘要： We report the facile preparation of polypyrrole microcapsules with a hydrophobic liquid core that is loaded with gold nanoparticles. Through the oxidative polymerization of pyrrole, the polymer is deposited onto the surface of the droplets, which results in the encapsulation of both the liquid phase and the metal nanoparticles. We demonstrate the preparation of the microcapsules loaded with organic solvents (toluene, hexane) or 2-oxoheptyl isothiocyanate (new promising anticancer agent) as the liquid cores and stable or radioactive gold nanoparticles (Au-197 or Au-198 isotopes). The resulting microcapsules have been demonstrated as promising agents for medical applications such as computed tomography or gamma imaging. Moreover, the capsules can be applied as drug carriers, which has been shown in vitro on cancer and normal cell cultures.
关键词： Targeted drug delivery,Gold nanoparticles doped with Au-198,Computed tomography,Anticancer agents,Polypyrrole microcapsules,Gamma imaging
更新于2025-09-23 15:22:29
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Histology and antitumor activity study of PTX-loaded micelle, a fluorescent drug delivery system prepared by PEG-TPP
摘要： We synthesized PEG-TPP as carrier to encapsulate paclitaxel (PTX) in the form of micelles to overcome its water-solubility problem. PTX-loaded micelles possess a-week stability and appropriate particle size (152.1±1.2 nm) which is beneficial for enhanced permeability and retention (EPR) effect. Strong pH dependence of PTX releasing from micelles is verified by in vitro release study. At cellular level, PTX-loaded micelles can target mitochondria effectively which may results a better cytotoxicity of micelles (especially IC50 = 0.123±0.035 μmol/L of micelles and 0.298±0.067 μmol/L of PTX alone on MCF-7 cells). The fluorescence distributions of both isolated and sliced organs show that the micelles can effectively target tumors. Moreover, we further prove the enhanced therapeutic effects of micelles in tumor-bearing mice comparing with PTX alone. The results show that the biodegradable drug delivery system prepared by PEG-TPP can overcome the poor solubility of paclitaxel and improve its tumor targeting and antitumor activity.
关键词： PEG-TPP,Mitochondria,Paclitaxel,EPR,Micelles,Anticancer
更新于2025-09-23 15:22:29
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A Ratiometric Fluorescence Probe for Cisplatin: Investigating Intracellular Reduction of Platinum(IV) Prodrug Complexes
摘要： Pt(IV) prodrug strategy has emerged as an excellent alternative to tackle the problems associated with conventional Pt(II) drug therapy. However, there is a lack of tools to study how this new class of Pt(IV) drugs are processed at the cellular level. Herein, we report the first ratiometric fluorescence probe designed for detecting cisplatin, applied to investigate Pt(IV) anticancer complexes in biological systems. The probe was able to distinguish between cisplatin and its Pt(IV) derivatives, allowing us to probe the intracellular reduction of Pt(IV) prodrug complexes. The correlation between the amount of active Pt(II) species available after intracellular reduction of Pt(IV) complexes to their cytotoxicity and the role glutathione plays in their reduction were investigated.
关键词： Fluorescence probes,Ratiometric,Glutathione,Platinum prodrugs,Anticancer
更新于2025-09-23 15:21:21
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Fluorescent half-sandwich phosphine-sulfonate iridium(III) and ruthenium(II) complexes as potential lysosome-targeted anticancer agents
摘要： The synthesis, characterization and biological activity of neutral fluorescent Ir(III) and Ru(II) half-sandwich organometallic complexes containing phosphine-sulfonate ligands are reported. X-ray crystal structure of complexes 1-3, 10 and 11 exhibits the expected half-sandwich “three-legged piano-stool” pseudo-octahedral geometry. Spectroscopic properties study displays that these complexes show rich fluorescence properties. With the exception of 9, 10 and 11 toward A549 human lung cancer cells and 10 towards HeLa human cervical cancer cells, each complex shows promising cytotoxicity toward HeLa and A549 cells line with IC50 values in the range of 3.6-53.1 μM, and 6.5-34.5 μM, respectively. Hydrolysis, DNA cleavage and depolarization of the mitochondrial membrane potential (MMP) appear not to be the main mechanism of action. However, these complexes are able to covert NADH to NAD+ via the transfer hydrogenation. Mechanism studies by flow cytometry display that the complexes exert their anticancer efficacy by inducing apoptosis, perturbing the cell cycle and increasing the intracellular ROS level. Furthermore, fluorescence property of these complexes provides a tool to investigate the microscopic mechanism by confocal microscopy. Notably, the typical Ir(III) complex 3 can specially localize to lysosome and damage it. In addition, complex 3 enters into HeLa cells mainly through energy-dependent pathway.
关键词： phosphine-sulfonate,half-sandwich,fluorescent,anticancer complexes,lysosome-targeted
更新于2025-09-23 15:21:21
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The Strong Inhibitory Effect of Combining Anti-Cancer Drugs AT406 and Rocaglamide with Blue LED Irradiation on Colorectal Cancer Cells
摘要： There is still no satisfying method to treat colorectal cancer (CRC) currently. Inspired by cocktail therapy, the combination of 465 nm blue LED irradiation and two multi-target anticancer agents AT406 and Rocaglamide has been investigated for a revolutionary way to treat colorectal cancer cells in vitro. It showed a strong inhibitory effect on colorectal cancer cells, and its side effects on human normal cells are negligible. When applied to HCT116 cells, it can achieve an apoptotic rate up to 95%. It is also seen to significantly inhibit proliferation of HT29 cells. Furthermore, little to no cell inhibition or damage of normal MRC-5 cells were seen after treatment. The combination of blue LED irradiation and two anti-cancer drugs causes apoptosis of colorectal cancer cells by activating the apoptotic pathway, inhibiting autophagy and proliferation pathways as well as the production of reactive oxygen species (ROS).
关键词： Multi-targeted anticancer drugs,Colorectal cancer,Inhibitory effect,Blue LED irradiation
更新于2025-09-23 15:21:01
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Quantum dots encapsulated with curcumin inhibit the growth of colon cancer, breast cancer and bacterial cells
摘要： Aim: To synthesize and examine the impact of free Eudragit R(cid:2) RS 100 nanoparticles (LN01), Quantum dots curcumin-loaded Eudragit RS 100 nanoparticles (LN04), and un-encapsulated curcumin nanoparticles (LN06) on cancerous and bacterial cells. Materials & methods: The LN01, LN04, LN06 were synthesized and characterized by Fourier transform infrared, ζ potential, UV–Vis spectroscopy, transmission electron microscopy and scanning electron microscopy and their biological activities were evaluated. Results: LN04 profoundly inhibited the growth of colon (HCT-116) cancerous cells (10.64% cell viability) and breast cancer (MCF-7) cells (10.32% cell viability) with compared to LN01 and LN06. Normal cells (HEK-293) did not show any inhibition after treatments. In addition, LN04 show better inhibitory action on bacterial growth compared with LN01 and LN06. Conclusion: We suggest that LN04 selectively target cancerous and bacterial cells and therefore possess potential anticancer and antibacterial capabilities.
关键词： quantum dots,curcumin,antibacterial agent,drug delivery,anticancer agent
更新于2025-09-23 15:21:01