Search

Cancer is the most severe health problem facing most people today. Photodynamic therapy (PDT) for tumors has attracted attention because of its non-invasive nature, negligible adverse reactions, and high spatiotemporal selectivity. Developing biocompatible photosensitizers that can target, guide, and efficiently kill cancer cells is desirable in PDT. Here, two amphiphilic organic compounds, PS-I and PSS-II, were synthesized based on the D-π-A structure with a positive charge. The two AIEgens exhibited near-infrared emission, large Stokes shift, high 1 O 2 and O 2 -∙ generation efficiency, good biocompatibility, and photostability. They were co-incubated with cancer cells and eventually accumulated to lysosomes by cell imaging experiments. In vitro and in vivo experiments demonstrated that PS-I and PSS-II could effectively kill cancer cells and sufficiently inhibit tumor growth under light irradiation. PS-I had a higher fluorescence quantum yield in the aggregated state, which made it better for bio-imaging in imaging-guided photodynamic therapy. In contrast, PSS-II with a longer conjugated structure had more ROS generation to kill tumor cells under illumination, and the tumor growth inhibition of mice reached 71.95% during the treatment. No observable injury or undesirable outcomes were detected in the vital organs of the mice within the treatment group, suggesting that PSS-II/PS-I had a promising future in efficient imaging-guided PDT for cancer., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Inc. All rights reserved.)

In most biophysiological processes, sulfur dioxide (SO 2 ) is an important intracellular signaling molecule that plays an important role. The change of SO 2 in cells are closely related to various diseases such as neurological disorders and lung cancer, so it is necessary to develop fluorescent probes with the ability to accurately detect SO 2 during physiological processes. In this work, we designed and synthesized a multifunctional fluorescent probe TIS. TIS has excellent properties such as near-infrared emission, large stokes shift, excellent SO 2 detection capabilities, low detection limit, high specificity and visualization of color change before and after reaction. Simultaneously, TIS has low cytotoxicity, good biocompatibility, clear cell imaging capability and mitochondrial targeting ability. In addition, the ability of TIS to be applied to different material surfaces for latent fingerprint fluorescence imaging was also explored. TIS provides an excellent method for the accurate detection of SO 2 derivatives and shows great potential applications in near-infrared cellular imaging and latent fingerprint fluorescence imaging., Competing Interests: Declaration of competing interest No conflict of interest exits in the submission of this manuscript, and manuscript is approved by all authors for publication. I would like to declare on behalf of my co-authors that the work described is original research that has not been published previously, and not under consideration for publication elsewhere, in whole or in part. All the authors listed have approved the manuscript that is enclosed. We declare that we have no financial and personal relationships with other people or organizations that can inappropriately influence our work. There is no professional or other personal interest of any nature or kind in any product, service and/or company that could be construed as influencing the position presented in, or the review of, the manuscript entitled., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Abnormally high levels of copper in tumors stimulate malignant proliferation and migration of cancer cells, which proposes a formidable challenge for the thorough therapy of malignant tumors. In this work, we developed a reliable, mitochondria-targeted near-infrared aggregation-induced emission fluorescent probe, TTQ-Th, whose thiourea moiety specifically could recognize mitochondria even both upon loss of mitochondrial membrane potential or in fixated cells, and can capture copper overexpressed by tumor cells, leading to severe copper deficiency. In parallel, TTQ-Th can generate sufficient reactive oxygen species (ROS) upon photoexcitation, while copper deficiency inhibits expression of related copper-based enzymes, resulting in a decline in ATP production. Such energy deficiency, combined with reduced MMP and elevated oxidative stress can lead to critical cell oncosis. Both in vitro and intracellular experiments can illustrate that the elevated ROS has remarkable damage to tumor cells and contributes to the elimination of the primary tumor, while copper deficiency further hinder tumor cell migration and induces G0/G1 cell cycle arrest in a dose-dependent manner, which is an efficacious strategy for the treatment of malignant tumors., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023. Published by Elsevier Inc.)

A dual donor-acceptor photosensitizer TCN-2 prepared based on single donor-acceptor could fulfil lipid droplets targeting to trigger apoptosis and tumor growth arrest. Meanwhile, all of experiments both in phosphate buffer solution and intracellular surroundings have demonstrated that TCN-2 catalyzed the production of type I as well as type II reactive oxygen species, forming a hybrid reactive oxygen species pattern, indicating that TCN-2 could be applied to initiate a series of biological responses triggered by oxidative stress within most high-viscosity solid tumors. In addition, TCN-2 also has the capability of fluorescence imaging, which could perfectly combine therapeutic imaging to achieve therapeutic effects while identifying cancerous lesions. Due to the structural design of double electron-absorbing groups, TCN-2 retained excellent lipophilicity while enhancing solubility in the biological environment. Terrific biocompatibility, minimal phototoxic damage to normal cells and tissues, and specific driving to prescriptive organelles to maximize therapeutic effects were used to enhance the therapeutic effect of photodynamic therapy to cease disease progression., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

High-fidelity imaging and long-term visualization of lysosomes are pivotal factors in the functional assessment of lysosomes, which perform an instrumental role in the physiological activity of cells. However, commercial probes have great limitations in lysosome exploration resulting from the aggregation-caused quenching effect as well as photobleaching instability and small Stokes shift. Therefore, we constructed a novel probe named TTAM with triphenylamine as the matrix and morpholine ring as the targeting group. In contrast with commonly accessible Lyso-tracker Red, TTAM has the merits of aggregation-induced emission effect, extremely high quantum yields (51.57 % solid-state) as well as fluorescence intensity, significant photostability, and high resolution. These properties make it ideal for imaging and activity monitoring lysosomes, which provides a powerful condition for bio-imaging., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

In this study, we identified HIF 1α as a potential target for reversing taxol resistance in lung cancer by combining bioinformatics analysis with pharmacological analysis. Furthermore, pomalidomide derivative LY103 was also be synthesized by introducing an isatin analogue into the amino terminal ofpomalidomide, and it has a broad antitumor spectrum and showed excellent activity against A549/Taxol cells (IC 50  = 6.33 ± 0.51 μM). The results of molecular docking showed that not only LY103 was inclined to bind to HIF 1α stably, it could also form multiple hydrogen bonds with VAL376, ASP256, ILE454, and GLU455 of HIF 1α even was reduced to LY103-NH 2 by nitroreductase, which was further stabilized the complex formed by them, thereby inhibiting the activity of HIF 1α. LY103 was able to significantly induce DNA damage and inhibit angiogenesis. Concurrently, LY103 activated the immune response, reduced the expression of cytokines TNF-α, IL-6, and IL-1β, thus might be inhibit the proliferation and metastasis of tumor cells. Pharmacological analysis proved that LY103 led to cell apoptosis through the mitochondrial pathway, and its combination with taxol significantly promoted this process. In general, the consumption of glutathione, the crosstalk of energy metabolism, and the improvement of the tumor microenvironment caused by LY103 eventually led to the decrease of ABCC1 protein expression and the drug resistance was reversed. The rational design of LY103 provided a basis for the application of nitro compounds in the treatment of hypoxic tumors and the reversal of taxol resistance., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Inc. All rights reserved.)

Organelle-targeted photodynamic therapy has been increasingly investigated in recent decades, but little attention has been paid to the damage caused to other non-primary target organelles during the course of action, even though these non-primary target organelles may play a substantial role in inhibiting the growth of cancer cells. In this contribution, we report an AIE-type strong endoplasmic reticulum-targeted luminogen (MTOQS) with a distorted structure, which is efficient in producing ROS both in cellular and non-cellular environment, causing an effective reduction of high levels of GSH and MDA in cancer cells through the efficient accumulation of intracellular ROS, and the levels of ATP, l-lactic acid, anti-apoptotic factor Bcl-2 and apoptotic protein caspase-3 were determined. Through the identification of these markers, it was evidenced that MTOQS-induced dual organelle oxidative stress could diminish the degree of oxidative phosphorylation and glycolysis in cancer cells and trigger an alteration in the culture environment of cancer cells, while causing damage to the endoplasmic reticulum and mitochondria through multiorganelle oxidative stress, turning on the pathway of apoptosis and consequently driving cancer cells to apoptosis., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Inc. All rights reserved.)

The complex environment of solid tumors and the migration of cancer cells are important obstacles to the cure of tumors through conventional therapy. Developing secure and efficient photosensitizers (PSs) is the crux to the application of photodynamic therapy (PDT) in the noninvasive clinical treatment of tumors. Herein, a series of PSs (DCTPys) with the same skeleton structure was designed and prepared. The unique molecular structure of DCTPys endows them with aggregation-induced emission (AIE) property and efficient reactive oxygen species (ROS) generation ability. Interestingly, due to their hydrophilic and lipophilic nature, DCTPys have fine staining and visual identification performance for the plasma membrane. In addition (e.g., MeDCTPy-OH), ROS is produced by MeDCTPy-OH under white light irradiation, which could destroy the completeness of cell membranes and cause cell necrosis. Importantly, morphology imaging of the cell membrane using MeDCTPy-OH enables real-time tracking of cancer cell ablation. This allowed cell necrosis and PDT effects to be observed under mild conditions. We conclude that DCTPys are potential cell membrane-selective PSs for PDT, and it is worth systematically exploring the phototherapeutic effect of these PSs on tumors in vivo., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022. Published by Elsevier B.V.)

Hydrogen sulfide and cysteine are momentous endogenous regulators of many physiological processes and maintain a dynamic balance of redox in living organisms. To investigate the inter-relationship of them in vivo, there is a pressing need to develop analytical molecular tools to identify related biomolecules. We construct a mitochondria-targeted single fluorescence probe (Mit-CM) for separately and continuously visualizing H 2 S, Cys and H 2 S/Cys with multi-response fluorescence signals. Mit-CM has the following advantages: (Ⅰ) colorimetric and ratiometric: two well-separated emission bands can ensure accurate detection of the analyte and significant color changes contribute to rapid identification of the analyte by the naked eye; (Ⅱ) mitochondrial localization: study the physiological functions of H 2 S and Cys in mitochondria; (Ⅲ) separate and continuous detection of H 2 S and Cys: reveal the inter-relationship and interconversion of them in biological system. Moreover, the desirable attributes of low cytotoxicity, better biocompatibility and excellent mitochondria enrichment ability indicate that Mit-CM can be employed to achieve detection and observe distribution of H 2 S, Cys and H 2 S/Cys in living organism., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Cysteine (Cys), an important organic small molecule containing sulfhydryl groups, plays paramount functions in human pathologies and physiologies. The detection of Cys in living vivo is essential for studying its roles. Here, we designed and synthesized a novel red-emission fluorescent probe AXPI-Cys with highly sensitivity (LOD = 48.9 ± 0.23 nM), rapidly response (<7 min) and colorimetric for detection cysteine. More importantly, the AXPI-Cys was determined Cys in real cystinuria urine samples for the first time with the satisfactory results (92%-99.96%) and employed for specifically location of endogenous/exogenous Cys in living cancer/normal cells and almost non-toxic, that is very valuable for diagnosis of cystinuria and observation of the distribution of Cys in normal cells. Notably, the AXPI-Cys was applied to imaging Cys in BALB/c nude mice with good biocompatibility and desirable tissue-penetration depth. Owing to the superior capability of AXPI-Cys, it provided a desired method to detect Cys in urine samples and cells, and exhibited munificent potential usage in biosystems and imaging studies in vivo., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Cysteine(Cys) is tightly related to physiological and pathological of human, and the imbalance of concentration of cysteine in the intracellular are associated with many diseases. Here, a novel NIR fluorescent probe TCF-Cys was designed and synthesized, and both the optimal excitation and emission wavelength of them were between 650 and 900 nm, that within the "optical window" of biological tissues. In aqueous solution, TCF-Cys, which with an acrylate extremity as a recognizing unit, exhibited excellent "turn-on" fluorescence response for Cys superior to other amino acids and thiols with a limit of detection of 0.1323 μM. Moreover, as an excellent naked-eye colorimetric indicator, TCF-Cys could effectively distinguishing the Cys, Hcy and GSH in aqueous solution through color change. Then, the response mechanism of TCF-Cys for Cys was revealed by TLC, 1 H NMR, HPLC, HRMS and DFT calculation. Finally, TCF-Cys was successfully employed to fluorescence specifically map of exogenous and endogenous Cys in living cells and zebrafish with low toxicity., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Fast, highly selective and sensitive thiophenol probes are highly desirable in the field of bioimaging and environmental monitoring. For that, based on the mechanism that thiophenol can effectively cleave the sulfonamide bond selectively, we herein report a dicyanoisophorone-based Red-emitting/NIR probe for thiophenol detection. This probe had some desirable properties such as rapid response, high selectivity and sensitivity, remarkable large Stokes shift (181 nm), Red-emitting/NIR fluorescence region and low LOD value (80 nM, according to 3σ/s). Moreover, this novel Red-emitting/NIR probe can potentially be applied to the detection of thiophenols in real water samples quantitatively and fluorescent imaging in living cells and zebrafishes., (Copyright © 2018 Elsevier B.V. All rights reserved.)

A near-infrared (NIR) and colorimetric fluorescent probe system was developed for Carbon Monoxide (CO) via a Pd 0 -mediated Tsuji-Trost reaction. In this probe, phenoxide anion formation (DPCO - ) was acted as the signal unit and an allyl carbonate group was used as the recognition unit. This non-fluorescent probe molecule can release the relevant fluorophore after conversion of Pd 2+ to Pd 0 by CO. The probe system including probe 1 and Pd 2+ can be used for "naked-eye" detection of CO, and exhibited high selectivity to CO over various other sensing objects. More importantly, the probe system has great potential for fluorescence imaging of intracellular CO in living cells., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Cytochrome P450s have brought considerable attention to researchers for their significant correlations with metabolic behaviors of procarcinogenic chemicals. To better understand the roles of CYP1A in biological and physiological systems, we developed a novel ratiometric fluorescence probe N-((2-hydroxyl ethoxy) ethyl)- 4-methoxy-1, 8-naphthalimide (NEMN) allowing for selectively and sensitively monitoring the target enzymes under physiological conditions and living cells. The probe was designed based on substrate predilection of CYP1A and its outstanding O-dealkylation capacity, and 1, 8-naphthalimide was chosen as fluorophore on account of its desirable photophysical properties. Absorption and emission spectra of the probe solution and reacted metabolism showed obvious red-shift with remarkable colour changes, which indicated that NEMN could be a promising ratiometric detector of CYP1A. Additionally, the selectivity assays displayed that NEMN only sensitive to CYP1A1 and CYP1A2 enzymes with scarce interference of other CYPs. Furthermore, the excellent linear relationships between the ratio of fluorescent intensities and incubation time and enzymes concentration signified time- and concentration- dependence of the probe, which were of desire benefit to quantify and monitor the CYP1A-involved biological behaviors in physiological conditions. The assay in real living samples (Human liver microsomes) further proved the analytical utility of the probe. Finally, the cytotoxicity assay and confocal fluorescence imaging demonstrated that this probe was of great promise for detecting the activity of endogenous CYP1A in human living cells., (Copyright © 2018 Elsevier B.V. All rights reserved.)

A novel label-free fluorescent chemodosimeter (C1) was synthesized, based on coumarin and N-(4-aminobenzoyl)-β-alanine, for the selective detection of cysteine (Cys) over glutathione (GSH), which involved a click reaction of Cys to CN of a Schiff base. The probe C1 featured a fast response (about 3 min), emission in the visible region, and high selectivity. Addition of Cys in HEPES-NaOH solution (pH 7.4) to C1 in water resulted in the appearance of a new emission peak at 445 nm, in company with remarkable enhancement of fluorescence intensity, while other amino acids did not induce any significant fluorescence change. Meanwhile, the addition reaction of Cys to C1 elicited 90.8-fold fluorescence intensity enhancement, which resulted in a change of emission color from orange to blue., (Copyright © 2016 Elsevier Inc. All rights reserved.)

The probe CT was synthesized and investigated as a novel label-free chemosensor for Ga(3+) detection in water. Probe CT showed remarkable selectivity and sensitivity for Ga(3+) in Tris-HCl aqueous buffer solution (pH7.0). The chemosensor responded rapidly to Ga(3+) with a 1:1 stoichiometry. Meanwhile, the unapparent changes of fluorescence lifetime decays suggest the turn-on process of probe CT by Ga(3+) which appears to be a static mechanism., (Copyright © 2015 Elsevier B.V. All rights reserved.)

Background: The detection of Epstein-Barr virus-derived latent membrane protein 1 (LMP-1) is essential for understanding its contribution to the development of malignancy in epithelial cells and the early screening of nasopharyngeal carcinoma tumors. It is important to explore novel means for enhancing detection sensitivity of LMP-1., Methods: The current strategy for enhancing sensitivity is based on signal amplification of LMP-1/cadmium telluride (CdTe) quantum dots (QDs) functionalized silica nanosphere labels (Si/QD/Ab2). Si/QD/Ab2 was fabricated by covalently binding LMP-1 antibody (denoted Ab2) to CdTe QDs, which have been previously coated onto the surface of silica nanoparticles with EDC Chemistry. The as-prepared Si/QD/Ab2 label can be brought to a modified gold slice by a "sandwiched" immunoreaction, which was confirmed by SEM images and detected by square wave voltammetry (SWV)., Results: The amount of captured Si/QD/Ab2 by sandwiched immunoreaction was related to the concentration of LMP-1 in the incubation solution. The calibration range for LMP-1 detection was found to be 0.001 to 10 ng/ml with a correlation coefficient of 0.9897 and the lowest detectable concentration of 0.001 ng/ml. Compared with traditional sandwich immunoassay, the detection sensitivity of presented approach was enhanced largely due to the large surface area of silica nanoparticle carriers, which increased in CdTe QDs loading per sandwiched immunoreaction., Conclusion: The ease of functionalization, good monodispersed sizes and uniformity of the silica nanoparticles allows the QDs coated silica nanospheres to be highly suited for immunological labeling of trace protein analysis. The proposed method is simple, selective, reproducible, and can be extended to study protein-protein, peptide-protein, and DNA-protein interaction., (Copyright © 2010 Elsevier B.V. All rights reserved.)