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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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Development of <i>Lactobacillus kimchicus</i> DCY51 <sup>T</sup> -mediated gold nanoparticles for delivery of ginsenoside compound K: <i>in vitro</i> photothermal effects and apoptosis detection in cancer cells
摘要： We report a non-covalent loading of ginsenoside compound K (CK) onto our previously reported gold nanoparticles (DCY51T-AuCKNps) through one-pot biosynthesis using a probiotic Lactobacillus kimchicus DCY51T isolated from Korean kimchi. The ginsenoside-loaded gold nanoparticles were characterized by various analytical and spectroscopic techniques such as field emission transmission electron microscopy (FE-TEM), energy-dispersive X-ray (EDX) spectroscopy, elemental mapping, X-ray powder diffraction (XRD), selected area electron diffraction (SAED), Fourier-transform infrared (FTIR) spectroscopy and dynamic light scattering (DLS). Furthermore, drug loading was also determined by liquid chromatography–mass spectrometry (LC–MS). In addition, DCY51T-AuNps and DCY51T-AuCKNps were resistant to aggregation caused by pH variation or a high ionic strength environment. Cell-based study confirmed that DCY51T-AuCKNps exhibited slightly higher cytotoxicity compared to ginsenoside CK treatment in A549 cells (human lung adenocarcinoma cell line) and HT29 (human colorectal adenocarcinoma cell line). Upon laser treatment, DCY51T-AuCKNps showed enhanced cell apoptosis in A549, HT29 and AGS cells (human stomach gastric adenocarcinoma cell line) compared with only DCY51T-AuCKNps treated cells. In conclusion, this preliminary study identified that DCY51T-AuCKNps act as a potent photothermal therapy agents with synergistic chemotherapeutic effects for the treatment of cancer.
关键词： green synthesis,gold nanoparticles,Ginsenoside CK,photoluminescence,photothermal therapy,anticancer activity,drug delivery
更新于2025-09-19 17:15:36
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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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<p>Photoluminescent And Self-Assembled Hyaluronic Acid-Zinc Oxide-Ginsenoside Rh2 Nanoparticles And Their Potential Caspase-9 Apoptotic Mechanism Towards Cancer Cell Lines</p>
摘要： Background: Zinc oxide nanoparticles (ZnO NPs) are used in modern cancer therapy based on their specific target, efficacy, low toxicity and biocompatibility. The photocatalytic performance of Zinc oxide (ZnO) nanocomposites with hyaluronic acid (HA) was used to study anticancer properties against various human cancer cell lines. Methods: Zinc oxide (ZnO) nanocomposites functionalized by hyaluronic acid (HA) were prepared by a co-precipitation method (HA-ZnONcs). The submicron-flower-shaped nanocomposites were further functionalized with ginsenoside Rh2 by a cleavable ester bond via carbodiimide chemistry to form Rh2HAZnO. The physicochemical behaviors of the synthesized ZnO nanocomposites were characterized by various analytical and spectroscopic techniques. We carried out 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay to evaluate the toxicity of Rh2HAZnO in various human cancer cells (A549, MCF-7, and HT29). Furthermore, to confirm the apoptotic effects of Rh2HAZnO and to determine the role of the Caspase-9/p38 MAPK pathways by various molecular techniques such as RT-PCR and Western blotting. Furthermore, Rh2HAZnO induced morphological changes of these cell lines, mainly intracellular reactive oxygen species (ROS) were observed by ROS staining and nucleus by Hoechst staining. Results: We confirmed that Rh2HAZnO exhibits the anti-cancer effects on A549 lung cancer, HT29 colon cancer, and MCF7 breast cancer cells. Moreover, intracellular reactive oxygen species (ROS) were observed in three cancer cell lines. Rh2HAZnO induced apoptotic process through p53-mediated pathway by upregulating p53 and BAX and downregulating BCL2. Specifically, Rh2HAZnO induced activation of cleaved PARP (Asp214) in A549 lung cancer cells and upregulated Caspase-9/phosphorylation of p38 MAPK in other cell lines (HT29 and MCF-7). Furthermore, Rh2HAZnO induced morphological changes in the nucleus of these cell lines. Conclusion: These results suggest that the potential anticancer activity of novel Rh2HAZnO nanoparticles might be linked to induction of apoptosis through the generation of ROS by activation of the Caspase-9/p38 MAPK pathway.
关键词： anticancer activity,ginsenoside Rh2,zinc oxide nanocomposites,drug delivery,cytotoxicity,Dendropanax morbifera Léveille
更新于2025-09-11 14:15:04
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Supermagnetic Fe <sub/>3</sub> O <sub/>4</sub> -PEG nanoparticles combined with NIR laser and alternating magnetic field as potent anti-cancer agent against human ovarian cancer cells
摘要： In the present study the magnetite nanoparticles Fe3O4 capped with polyethylene glycol PEG were prepared by hydrothermal method. Syntheses bare Fe3O4, and Fe3O4-PEG were confirmed by various techniques including X-ray powder diffraction (XRD), Transmission electron microscope (TEM), Dynamic light scattering (DLS), Scanning electron microscope (SEM), and Vibrating sample magnetometer (VSM) techniques were used to examine the magnetic properties of the Fe3O4 MNPs. The bare Fe3O4 had an average size that ranged between 12-31nm while Fe3O4- PEG had a size range of 5-15 nm. The effect of bare Fe3O4 and Fe3O4-PEG on SKOV-3 cell proliferation was measured by MTT assay. The ability of bare Fe3O4 and Fe3O4-PEG in induction of apoptosis was tested using Acridine orange/ Ethedium bromide stain. Cytotoxicity effects of bare Fe3O4 and Fe3O4-PEG against SKOV-3 cells in the presence and absence of laser photo-thermal therapy and alternating magnetic field (AMF) was also assessed. The results showed that both bare Fe3O4 and Fe3O4-PEG caused inhibition of SKOV-3 cell proliferation, resulting in their programmed death. Cytotoxic activity against SKOV-3 cells increased with NIR laser irradiation, while highly increased cytotoxic activities were observed after exposure to induction heating with AMF. In addition, the toxicity of investigated nanoparticles in liver function enzymes and histological alterations for spleen, and the lungs were addressed. The findings indicated that these nanoparticles were biocompatible with liver function enzymes and no significant alterations were recorded in the spleen, and the lungs. Taken together the present data suggest that bare Fe3O4 and Fe3O4-PEG with NIR laser and AMF could be promising for photothermal therapy protocol for cancer cells.
关键词： NIR laser,Hydrothermal synthesis,SKOV-3 cells,anticancer activity,Fe3O4-PEG,AMF
更新于2025-09-11 14:15:04