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Dual-action Platinum(II) Schiff Base Complexes: Photocytotoxicity and Cellular Imaging
摘要： Nine photo-stable Pt(II) Schiff base complexes [Pt(O^N^N^O)] (Pt1-Pt9) containing tetradentate salicylaldimine chelating ligands have been synthesized and characterized as potential photosensitisers for photodynamic therapy (PDT). The effects of electron-withdrawing versus electron-donating substituents on their electronic spectral properties are investigated. Pt1-Pt9 show broad absorption bands between 400-600 nm, which makes them useful for green-light photodynamic therapy. The complexes showed intense phosphorescence with emission maxima at ca. 625 nm. This emission was used to track their cellular localization in cancer cells. Confocal cellular imaging showed that the complexes localized mostly in the cytoplasm. In the dark, the complexes were non-toxic to A549 human lung cancer cells, but exhibited high photo-toxicity upon low-dose green light (520 nm, 7.02 J/cm2) irradiation via photo-induced singlet oxygen generation. Thus, these photoactive Pt(II) complexes have the potential to overcome the problem of drug resistance and side effects of current clinical Pt(II) drugs, and to act as both theranostic as well as therapeutic agents.
关键词： Schiff Base,Platinum(II),Photocytotoxicity,Cellular Imaging,Singlet oxygen
更新于2025-11-21 11:08:12
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Harnessing Natural Product Diversity for Fluorophore Discovery: Naturally Occurring Fluorescent Hydroxyanthraquinones from the Marine Crinoid <i>Pterometra venusta</i>
摘要： Fluorescent small molecules are important tools in many aspects of modern biology. A two-stage evaluation process involving fluorescence screening and live-cell imaging was developed to facilitate the identification of new fluorescent probes from extracts housed within the NCI Natural Products Repository. To this end, over 2000 extracts and prefractionated samples were examined, including an extract from the marine crinoid Pterometra venusta. An optically guided evaluation involving stepwise fluorescence screening and live-cell imaging was developed to enable the isolation of fluorescent natural products. These efforts resulted in the isolation of six hydroxyanthraquinone compounds, three of which are new natural products. These purified metabolites were examined for their potential as cellular imaging probes, and they demonstrate that natural product libraries can be a good source of new fluorescent agents.
关键词： natural products,fluorescent small molecules,Pterometra venusta,hydroxyanthraquinones,cellular imaging
更新于2025-09-23 15:21:01
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Chlorination <i>vs.</i> fluorination: a study of halogenated benzo[ <i>c</i> ][1,2,5]thiadiazole-based organic semiconducting dots for near-infrared cellular imaging
摘要： Red/near-infrared organic dyes are becoming increasingly widespread in biological applications. However, designing these dyes with long-wavelength emission, large Stokes shifts, and high fluorescence quantum efficiency is still a very challenging task. In this work, five donor-acceptor (D-A) red/near-infrared fluorophores based on different chlorinated/fluorinated benzo[c][1,2,5]thiadiazole units are designed and synthesized. The photophysical, theoretical calculations, and electrochemical properties explored in this study have proved that the introducing of chlorine atoms will lead to a lower HOMO level, stronger steric hindrance, and a relative lower quantum yield in solutions. When the organic dots are fabricated, the chlorinated dots demonstrate much higher fluorescence quantum yield, larger Stokes shift, and better photostability than that of the fluorinated dots. After labeling A549 cells, all the chlorinated/fluorinated dots exhibit high red emission intensities. All these results indicated that the subtle change in the halogen atom of the benzo[c][1,2,5]thiadiazole unit is a unique method to tune the photophysical properties of those materials, which also provides good guidelines to design highly efficient red/near-infrared molecules for cellular imaging applications.
关键词： 5]thiadiazole,organic semiconducting dots,chlorination,benzo[c][1,fluorination,near-infrared cellular imaging,2
更新于2025-09-23 15:19:57
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Cisplatin-Loaded Polymeric Micelles with Aggregation-Induced Emission Feature for Cellular Imaging and Chemotherapy
摘要： Imaging-guided disease theranostic nanoplatforms based on polymeric micelles have drawn a broad attention because of their clear visualization, reduced systemic toxicity, enhanced utilization of drugs, and suppressed chemoresistance of tumors, which makes them possess potential application for cancer therapy. Herein, we synthesized a polymeric nanoparticles (Poly (MAD-alt-OCE)-PTZ-PEG) with novel aggregation-induced emission (AIE) characteristic based on cheap commercial polymer by the simple and environmental method. These Poly(MAD-alt-OCE)-PTZ-PEG nanoparticles (NPs) show excellent biocompatibility and fluorescence property, which makes them huge application potential for cellular imaging. Furthermore, the antitumor drug cisplatin Pt(IV) can be loaded efficiently onto the surface of Poly(MAD-alt-OCE)-PTZ-PEG NPs due to the existence of abundant carboxyl groups on the NPs surface. The well-controlled Pt(IV)-loaded yield and great acid-responsive drug release of these polymeric micelles enhance cytotoxicity against cancer cells in vitro. Given the cheap raw materials, eco-friendly method, excellent AIE property, efficient antitumor drug delivery and pH-controlled drug release, these polymeric NPs would be a potential candidate for cancer diagnosis and therapy in the future.
关键词： Aggregation-induced emission,Drug delivery,Cellular imaging,Polymeric nanoparticles
更新于2025-09-23 15:19:57
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Pyrazole appended quinoline-BODIPY based arene ruthenium complexes: their anticancer activity and potential applications in cellular imaging
摘要： Synthesis of an entirely new series of arene ruthenium complexes [Ru(η6-C6H6)(L1)Cl]PF6, (1), [Ru(η6-C10H14)(L1)Cl]PF6 (2), [Ru(η6-C6H6)(L2)Cl]PF6 (3) and [Ru(η6-C10H14)(L2)Cl]PF6 (4) involving 5-[2-(1H-pyrazol-1-yl)quinoline]-BODIPY (L1) and 5-[6-methoxy-2-(1H-pyrazol-1-yl)quinoline]-BODIPY (L2) was described. The ligands and complexes were thoroughly characterized by various physicochemical techniques and the structures of L1, 1 and 4 were determined by X-ray single crystal analyses. Photo-/ and electrochemical property, DNA binding, cytotoxicity, cellular uptake and apoptotic studies on 1–4 were performed by various methods, while singlet oxygen-mediated cytotoxicity via photo-irradiation by visible light was supported by 1,3-diphenylisobenzofuran titration studies. Binding of the complexes in the minor groove of CT-DNA via van der Waals forces and electrostatic interactions was affirmed by molecular docking studies. In vitro antiproliferative activity and photocytotoxicity of 1–4 were examined against the human cervical cancer cell line (HeLa) which clearly showed that these are extremely photocytotoxic under visible light (400–700 nm, 10 J cm?2; IC50 49.15, 1; 25.18, 2; 15.85, 3; 12.87, 4), less toxic in the dark (IC50 > 100 μM) and preferentially accumulate in the lysosome of the HeLa cells. Further, these complexes behave as a potential theranostic agent and their ability to kill cancer cells under visible light lies in the order 4 > 3 > 2 > 1.
关键词： singlet oxygen,arene ruthenium complexes,DNA binding,cellular imaging,BODIPY,photodynamic therapy,anticancer activity
更新于2025-09-19 17:15:36
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Fluorogenic probes for super-resolution microscopy
摘要： Fluorogenic probes efficiently reduce non-specific background signals, which often results in highly improved signal-to-noise ratios. Although this implies improved resolution, fluorogenic probes in the context of super-resolution microscopy are somewhat overlooked. Several excellent reviews summarize recent developments in SRM techniques, labeling techniques or different aspects of small synthetic fluorophores, however there is no comprehensive review on fluorogenic probes suitable for super-resolution microscopy. Herein we wish to fill this gap by providing the readers with an up-to-date summary of fluorogenic probes applied to super-resolution imaging of cellular structures.
关键词： signal-to-noise ratio,background reduction,super-resolution microscopy,cellular imaging,fluorogenic probes
更新于2025-09-19 17:15:36
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N,S-self-doped carbon quantum dots from fungus fibers for sensing tetracyclines and for bioimaging cancer cells
摘要： In this work, nitrogen and sulfur dual-doped carbon quantum dots (N,S-CDs) from naturally renewable bio-material fungus fibers were prepared by a biosynthesis and hydrothermal method. The N,S-CDs displayed good water solubility, excellent stability, high quantum yield (QY = 28.11%) as well as remarkable features for fluorescence quenching-based detection and cellular imaging of cancer cells. It was worth mentioning that the heteroatoms doped carbon quantum dots made from the fungus fibers had a satisfactory QY and could be used as a selective, efficient, and sensitive fluorescent probe to determine tetracyclines by the synergistic effects of static quenching and internal filtration effect. The probe demonstrated a wide linear range and low detection limit. For tetracycline, the linear range was 0.5 μM to 47.6 μM, and the corresponding detection limit was 15.6 nM. Significantly, the test papers prepared by using N,S-CDs could detect tetracyclines in aquiculture wastewater rapidly. The produced N,S-CDs did not affect the cell viability and showed great promises for cellular imaging.
关键词： Biosynthesis,Cellular imaging,Tetracyclines,Fungus fibers,N,S-self-doped carbon dots
更新于2025-09-19 17:13:59
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Rapid synthesis of B-N co-doped yellow emissive carbon quantum dots for cellular imaging
摘要： In order to avoid the interference of autofluorescence and improve tissue penetration capability of carbon quantum dots (CQDs) in biological imaging, the synthesis of long-wavelength emission CQDs was achieved in this work. Boron and nitrogen co-doped CQDs (BN-CQDs) were synthesized by one-step microwave assisted hydrothermal method with o-phenylenediamine as carbon and nitrogen source, boric acid as boron source. The BN-CQDs (QY ? 13.79%) synthesized under the optimal conditions exhibit excitation independence, a large Stoke shift, satisfactory fluorescent stability, good biocompatibility and low toxicity, which can meet the basic requirements as cell imaging agent. Cell imaging measurements prove their increased intracellular accumulation with the extension of incubation time with HeLa cells, and clearly observable BN-CQDs imaging for cell morphology. Hence BN-CQDs can be used as a good cell imaging agent.
关键词： Rapidity,Cellular imaging,Yellow emission,B-N co-doped carbon quantum dots
更新于2025-09-16 10:30:52
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Fabrication and characterization of novel cRGD modified graphene quantum dots for chemo-photothermal combination therapy
摘要： In this work, an innovative drug delivery system based on cyclic RGD-modified (as the targeting agent) and doxorubicin-loaded graphene quantum dots (R–GQDs@DOX) was fabricated for chemo-photothermal combination therapy. These tasks include drug loading capacity, photothermal efficiency, cellular uptake and combination therapeutic effect of R–GQDs@DOX. The structure of R–GQDs@DOX was characterized by FT-IR spectrum, UV–vis spectrum and AFM. The results indicated that the doxorubicin (DOX) could be loaded onto graphene quantum dots (GQDs) via van der Waals interaction (π–π stacking) and the drug loading capacity was 96.6 % (wt). The R–GQDs@DOX not only showed obvious pH-responsive release of DOX, but also exhibited great photothermal efficacy for cancer cells. The fluorescence intensity indicated that R–GQDs@DOX was effectively taken up by SK–mel–5 and H460 cells. The combination of chemotherapy and photothermal therapy could more effectively inhibit growth of tumor cells, compared to photothermal therapy or chemotherapy alone.
关键词： Cellular imaging,Graphene quantum dots,Synergetic therapy,Composite drug-loaded carrier,Drug delivery
更新于2025-09-16 10:30:52
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pH-Controlled fluorescence switching in water-dispersed polymer brushes grafted to modified boron nitride nanotubes for cellular imaging
摘要： pH-Switchable, fluorescent, hybrid, water-dispersible nanomaterials based on boron nitride nanotubes (BNNTs) and grafted copolymer brushes (poly(acrylic acid-co-fluorescein acrylate) – P(AA-co-FA)) were successfully fabricated in a two-step process. The functionalization of BNNTs was confirmed by spectroscopic, gravimetric and imaging techniques. In contrast to “pure” BNNTs, P(AA-co-FA)-functionalized BNNTs demonstrate intense green fluorescence emission at 520 nm. Under neutral or alkaline pH values, P(AA-co-FA)-functionalized BNNTs are highly emissive in contrast to acidic pH conditions where the fluorescent intensity is absent or low. No increase in the absorption was observed when the suspension pH was increased from 7 to 10. The functionalized BNNTs are easily taken up by human normal prostate epithelium (PNT1A) and human prostate cancer cell lines (DU145) and are suitable for further evaluation in cellular imaging applications.
关键词： pH switching,surface modification,cellular imaging,fluorescence,boron nitride nanotubes,polymer brushes
更新于2025-09-12 10:27:22