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硒化壳聚糖对K 562和K 562/ADM作用的比较研究 总被引:1,自引:0,他引:1
应用MTT法和细胞集落形成率法观察了硒化壳聚糖对K562和K562/ADM肿瘤细胞株生长的影响,结果发现硒化壳聚糖可有效地抑制两种K562细胞生长,呈量效关系。同等剂量的硒化壳聚糖对K562细胞的作用强度高于对K562/ADM细胞。硒化壳聚糖对耐药的细胞株可产生抑制作用,若与化疗药合用则可减慢甚至部分逆转临床上K562细胞耐药性的发生。 相似文献
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Visualization and Quantification of Transmembrane Ion Transport into Giant Unilamellar Vesicles 下载免费PDF全文
Dr. Hennie Valkenier Néstor López Mora Dr. Alexander Kros Prof. Dr. Anthony P. Davis 《Angewandte Chemie (International ed. in English)》2015,54(7):2137-2141
Transmembrane ion transporters (ionophores) are widely investigated as supramolecular agents with potential for biological activity. Tests are usually performed in synthetic membranes that are assembled into large unilamellar vesicles (LUVs). However transport must be followed through bulk properties of the vesicle suspension, because LUVs are too small for individual study. An alternative approach is described whereby ion transport can be revealed and quantified through direct observation. The method employs giant unilamellar vesicles (GUVs), which are 20–60 μm in diameter and readily imaged by light microscopy. This allows characterization of individual GUVs containing transporter molecules, followed by studies of transport through fluorescence emission from encapsulated indicators. The method provides new levels of certainty and relevance, given that the GUVs are similar in size to living cells. It has been demonstrated using a highly active anion carrier, and should aid the development of compounds for treating channelopathies such as cystic fibrosis. 相似文献
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Hyo-Jin Kang Eun-Hee Kang Sang-Wook Park Jae-Wook Lee Jin- Kook Lee 《Macromolecular Symposia》2006,235(1):195-200
Summary: Polyethylene glycol substituted titanyl phthalocyanine was prepared in two steps starting from phthalonitrile and characterized by FT-IR, UV-vis spectrophotometry, and fluorescence spectrophotometry. The titanyl phthocyanine derivatives (TiOPcs) showed high solubility in common organic solvents, such as, CH3Cl and DMF. These compounds decreased in absorbance intensity with increase of molecular weight of polyethylene glycol at maxima wavelength of visible range. The fluorescence spectra showed a fluorescence emission near 690 nm with a quantum yield of 0.05–0.32 (λex = 625 nm). 相似文献
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合成得到3-(5-氨基-萘氧基)邻苯二甲腈(C18H11N3O)、4-(5-氨基-萘氧基)邻苯二甲腈(C18H11N3O)、3-联苯氧基邻苯二甲腈(C20H12N2O)及4-联苯氧基邻苯二甲腈(C20H12N2O)4种未见报导的取代邻苯二甲腈,以此为前躯体合成了四[α-(5-氨基-萘氧基)]酞菁锌(C72H44N12O4Zn)、四[β-(5-氨基-萘氧基)]酞菁锌(C72H44N12O4Zn)、四[α-(联苯氧基)]酞菁锌(C80H48N8O4Zn)和四[β-(联苯氧基)]酞菁锌(C80H48N8O4Zn)4种未见报导的芳氧基取代酞菁锌配合物。通过测定它们的紫外-可见吸收光谱、荧光发射光谱,获得其最大吸收波长及其摩尔消光系数、最大发射波长、荧光量子产率(ΦF)、单线态氧量子产率(ΦΔ)及光降解速率常数并与其类似物进行了比较,探讨了它们的光物理光化学性质的构效关系。研究结果表明四[α-(联苯氧基)]酞菁锌在红光区具有大的摩尔消光系数,且具有较高的ΦΔ,有望开发成为光动力治疗用光敏剂。 相似文献
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使用ESR波谱技术研究铝酞菁光化反应,以2,2,6.6-四甲基-4-羟基哌啶醇为探针,探测光化反应的中间产物及反应机制,结果表明,反应体系中氮氧自由基的生成依赖于氧的存在,D_2O的增进效应及β-胡萝卜素的抑制效应表明铝酞菁光化反应产生了单线态氧(~1O_2),SOD及细胞色素C的部分抑制效应表明光化反应中有少量超氧阴离子自由基(O_2)生成。 相似文献
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Jean-Pierre Daziano Steen Steenken Christian Chabannon Patrice Mannoni Michel Chanon Michel Julliard 《Photochemistry and photobiology》1996,64(4):712-719
Abstract— The photodynamic therapy (PDT) efficiency of five phthalocyanines, chloroaluminum phthalocyanine (AlPc), dichlorosilicon phthalocyanine (SiPc), bis (tri- n -hexylsi-loxy)silicon phthalocyanine (PcHEX), bis (triphenyl-siloxy)silicon phthalocyanine (PcPHE) and nickel phthalocyanine (NiPc), was assessed on two leukemic cell lines TF-1 and erythroieukemic and B lymphoblastic cell lines, Daudi, respectively. AlPc showed the best photocytotox-icity leading to 0.008 surviving fraction at 2 × 10−9 M for TF-1 and 4 × 10−9 M for Daudi. At 5 × 10−7 M , SiPc and PcHEX induced a significant photokilling, whereas NiPc and PcPHE were inactive. Laser flash photolysis and photoredox properties of the phthalocyanines were investigated to try to relate these parameters with the biological effects. AlPc showed the longest triplet lifetime: 484 fis in dimethyl sulfoxide/H2 O. This value was increased up to 820 u.s when AlPc was complexed with human serum albumin used as a membrane model. Such an enhancement was not observed with the silicon phthalocyanines. Upon irradiation, all the phthalocyanines generated singlet oxygen with 0.29–0.37 quantum yield values. The reduction potentials of the excited states obtained from measurement in the ground state and energy of the excited triplets show that AlPc is the best electron acceptor. The in vitro photocytotoxicity observed and the measured parameters are in agreement with a key role of electron transfer in PDT assays involving these phthalocyanines. 相似文献
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A new synthesized benzene nitrogen mustard was converted into glycosyl donor-trichloroacetimidate that was glycosylated with p-nitrophenol(glycosyl donors) to form β-lactosyl p-nitrobenzene under the protection of acetyl in a stereoselective manner, was prepared and evaluated for its cytotoxicity towards cultured K562 cell line. Methylthiazoy tetrazolium(MTT) assay, transmission electron microscopy(TEM), flow cytometry(FCM) and immunohistochemistry were utilized to explore the mechanisms of how the compound arrests the growth of HCT-T cells. This new synthesed benzene nitrogen mustard glucoside derivate(BNMGD) presented a lower toxicity to normal cells, but is significantly more toxic to K562 cells compared with nitrogen mustard, meanwhile it can induce the apoptosis of K562 cells. These results indicate that the new synthesized BNMGD can inhibit the growth of K562 cells and induce the apoptosis, and its cytotoxicity towards cultured K562 cell line is much more effective than that of nitrogen mustard. 相似文献
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Observation and Photophysical Characterization of Silicon Phthalocyanine J‐Aggregate Dimers in Aqueous Solutions 下载免费PDF全文
Dr. Tennyson Doane Andrew Chomas Shriya Srinivasan Prof. Clemens Burda 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(26):8030-8039
The use of macrocyclic molecules for both imaging and photodynamic therapy (PDT) has proven to be a powerful method for assessing and treating diseases, respectively. However, many potential candidates for these applications rely on rigid organic structures which are hydrophobic and thus lead to possible aggregation in aqueous solutions such as blood. Here, we describe the discovery of noncovalent J‐aggregate dimers of the asymmetrically, axially modified silicon phthalocyanine 4 (Pc 4) in aqueous solutions through steady‐state and time‐resolved spectroscopy. Remarkably, the monomer–dimer equilibrium is dictated by water content and pH, with free monomers resulting in favorable solvation conditions even after formation of the dimer complex. This work sheds light on previous observations of Pc 4 behavior in cells during PDT, and can further elucidate the structure–activity relationship of these important molecules. 相似文献
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Monique H. Rasch Karmi Tijssen John VanSteveninck Tom M. A. R. Dubbelman 《Photochemistry and photobiology》1996,64(3):586-593
Abstract— When CHO cells were exposed to hyperthermia and subsequently to photodynamic treatment, the combined effects were additive but in the reverse sequence the interaction was synergistic. The synergistic interaction comprised two quite different components: (1) photodynam-ically induced sensitization of cellular proteins and/or supramolecular structures for thermal inactivation and (2) a photodynamically induced inhibition of the cellular repair system for sublethal thermal damage. The first component of the synergistic interaction was reflected by a change of the Arrhenius parameters of thermal cell killing. A lowering of the activation energy of this process was responsible for the synergistic interactions, whereas a concomitant decrease of the frequency factor, opposing this effect, actually caused a much lower degree of synergism at higher temperatures. This component of the synergistic interaction did not respond to the insertion of an intermediate incubation period between the two treatments. The second component of the synergistic interaction, viz. the interference with the ability of cells to survive sublethal thermal damage, was reversible, as an intermediate incubation between photodynamic treatment and hyperthermia resulted in its repair. The photodynamically induced inhibition of the ability of cells to survive sublethal thermal damage was not related to ATP or glutathione depletion, inhibition of de novo protein synthesis or impairment of degradation of damaged protein molecules. Restoration of the repair system for sublethal damage depended on a metabolic process and required free intracellular Ca2+, suggesting that a cell signaling pathway may be involved. Thus, in a practical sense the magnitude of the synergistic interaction between photodynamic treatment and hyperthermia depends on the length of the interval between the two treatments and on the temperature and duration of the subsequent thermal treatment. This may have significant consequences for the development of clinical protocols. 相似文献
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Andressa Oliveira Stefany Moura Luiz Pimentel Joo Neto Rafael Dantas Floriano Silva-Jr Monica Bastos Nubia Boechat 《Molecules (Basel, Switzerland)》2022,27(3)
Tyrosine kinase enzymes are among the primary molecular targets for the treatment of some human neoplasms, such as those in lung cancer and chronic myeloid leukemia. Mutations in the enzyme domain can cause resistance and new inhibitors capable of circumventing these mutations are highly desired. The objective of this work was to synthesize and evaluate the antiproliferative ability of ten new analogs that contain isatins and the phenylamino-pyrimidine pyridine (PAPP) skeleton, the main pharmacophore group of imatinib. The 1,2,3-triazole core was used as a spacer in the derivatives through a click chemistry reaction and gave good yields. All the analogs were tested against A549 and K562 cells, lung cancer and chronic myeloid leukemia (CML) cell lines, respectively. In A549 cells, the 3,3-difluorinated compound (3a), the 5-chloro-3,3-difluorinated compound (3c) and the 5-bromo-3,3-difluorinated compound (3d) showed IC50 values of 7.2, 6.4, and 7.3 μM, respectively, and were all more potent than imatinib (IC50 of 65.4 μM). In K562 cells, the 3,3-difluoro-5-methylated compound (3b) decreased cell viability to 57.5% and, at 10 µM, showed an IC50 value of 35.8 μM (imatinib, IC50 = 0.08 μM). The results suggest that 3a, 3c, and 3d can be used as prototypes for the development of more potent and selective derivatives against lung cancer. 相似文献
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Fernando Moyano Dr. Patricia G. Molina Dr. Juana J. Silber Prof. Leonides Sereno Prof. N. Mariano Correa Prof. 《Chemphyschem》2010,11(1):236-244
Herein, we investigate the behavior of the electroactive molecular probe 6‐propionyl‐2‐dimethyl amino naphthalene (PRODAN) in large unilamellar vesicles (LUV) formed with the phospholipid 1,2‐di‐oleoyl‐sn‐glycero‐3‐phosphatidylcholine (DOPC) by using cyclic voltammetry (CV). The CV studies in pure water confirm our previous spectroscopic results that PRODAN self‐aggregates due to its low water solubility. Moreover, the electrochemical results also reveal that the PRODAN aggregated species are non‐electroactive within the studied electrochemical potential region. In DOPC LUV media, the redox behavior of PRODAN shows how the LUV bilayer interacts with PRODAN aggregated species to form PRODAN monomer species. Moreover, the electrochemical response of PRODAN allows us to propose a model for explaining the electrochemical experimental results and—in conjunction with our measurements—for calculating the value of the partition constant (Kp) of PRODAN between the water and LUV bilayer pseudophases. This value coincides with that obtained through an independent technique. Moreover, our electrochemical model allows us to calculate the diffusion coefficient (D) for the DOPC LUV, which coincides with the D value obtained through dynamic light scattering (DLS). Thus, our data clearly show that electrochemical measurements could be a powerful alternative approach to investigate the behavior of nonionic electroactive molecules embed in a confined environment such as the LUV bilayer. Moreover, we believe that this approach can be used to investigate the behavior of non‐optical molecular drugs embedded in bilayer media. 相似文献
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Jeremias Sibold Katharina Kettelhoit Loan Vuong Fangyuan Liu Daniel B. Werz Claudia Steinem 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(49):17969-17977
The receptor lipid Gb3 is responsible for the specific internalization of Shiga toxin (STx) into cells. The head group of Gb3 defines the specificity of STx binding, and the backbone with different fatty acids is expected to influence its localization within membranes impacting membrane organization and protein internalization. To investigate this influence, a set of Gb3 glycosphingolipids labeled with a BODIPY fluorophore attached to the head group was synthesized. C24 fatty acids, saturated, unsaturated, α‐hydroxylated derivatives, and a combination thereof, were attached to the sphingosine backbone. The synthetic Gb3 glycosphingolipids were reconstituted into coexisting liquid‐ordered (lo)/liquid‐disordered (ld) giant unilamellar vesicles (GUVs), and STx binding was verified by fluorescence microscopy. Gb3 with the C24:0 fatty acid partitioned mostly in the lo phase, while the unsaturated C24:1 fatty acid distributes more into the ld phase. The α‐hydroxylation does not influence its partitioning. 相似文献
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《Electroanalysis》2017,29(3):828-834
A simple and rapid electrochemical aptamer cytosensor has been developed for direct detection of chronic myelogenous leukemia (CML) K562 cells based on a specific aptamer and a biotin conjugated concanavalin A (bio‐ConA) detection probe. The K562 cell could be specifically recognized by T2‐KK1B10 capture aptamer pre‐immobilized on gold modified electrode surface. Then, bio‐ConA was added in the reaction to identify K562 cell surface mannose, resulting in an aptamer‐K562 cell‐bio‐ConA sandwich complex. Finally, streptavidin conjugated alkaline phosphatase (ST‐ALP) combined with the bio‐ConA to catalyze α‐naphthyl (α‐NP) phosphate to form α‐naphthol which is highly electroactive at an operating voltage of 180 mV (vs. Ag/AgCl). Under optimum conditions, the DPV signals were proportional to the logarithm of K562 cell from 1×102 to 1×107 cells mL−1 with a detection limit of 79 cells mL−1. The cytosensor also exhibited high selectivity, stability and reproducibility. When applied to detect K562 cells in human blood samples, recoveries between 79.6 %–93.3 % were obtained, indicating the developed biosensor would be a potential alternative tool for CML K562 cell detection in real biological samples. 相似文献
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Formulation of Aluminum Chloride Phthalocyanine in Pluronic™ P‐123 and F‐127 Block Copolymer Micelles: Photophysical properties and Photodynamic Inactivation of Microorganisms 下载免费PDF全文
Bruno Henrique Vilsinski Adriana Passarella Gerola Junior Adalberto Enumo Katieli da Silva Souza Campanholi Paulo Cesar de Souza Pereira Gustavo Braga Noboru Hioka Elza Kimura André Luiz Tessaro Wilker Caetano 《Photochemistry and photobiology》2015,91(3):518-525
Aluminum Chloride Phthalocyanine (AlPcCl) can be used as a photosensitizer (PS) for Photodynamic Inactivation of Microorganisms (PDI). The AlPcCl showed favorable characteristics for PDI due to high quantum yield of singlet oxygen (ΦΔ) and photostability. Physicochemical properties and photodynamic inactivation of AlPcCl incorporated in polymeric micelles of tri‐block copolymer (P‐123 and F‐127) against microorganisms Staphylococcus aureus, Escherichia coli and Candida albicans were investigated in this work. Previously, it was observed that the AlPcCl undergoes self‐aggregation in F‐127, while in P‐123 the PS is in a monomeric form suitable for PDI. Due to the self‐aggregation of AlPcCl in F‐127, this formulation did not show any effect on these microorganisms. On the other hand, AlPcCl formulated in P‐123 was effective against S. aureus and C. albicans and the death of microorganisms was dependent on the PS concentration and illumination time. Additionally, it was found that the values of PS concentration and illumination time to eradicate 90% of the initial population of microorganisms (IC90 and D90, respectively) were small for the AlPcCl in P‐123, showing the effectiveness of this formulation for PDI. 相似文献