RESUMO
The pore dimension and surface property directly dictate the transport of guests, endowing diverse gas selective adsorptions to porous materials. It is highly relevant to construct metal-organic frameworks (MOFs) with designable functional groups that can achieve feasible pore regulation to improve their separation performances. However, the role of functionalization in different positions or degrees within framework on the separation of light hydrocarbon has rarely been emphasized. In this context, four isoreticular MOFs (TKL-104-107) bearing dissimilar fluorination are rationally screened out and afforded intriguing differences in the adsorption behavior of C2 H6 and C2 H4 . Ortho-fluoridation of carboxyl allows TKL-105-107 to exhibit enhanced structural stabilities, impressive C2 H6 adsorption capacities (>125 cm3 g-1 ) and desirable inverse selectivities (C2 H6 over C2 H4 ). The more modified ortho-fluorine group and meta-fluorine group of carboxyl have improved the C2 H6 /C2 H4 selectivity and adsorption capacity, respectively, and the C2 H6 /C2 H4 separation potential can be well optimized via linker fine-fluorination. Meanwhile, dynamic breakthrough experiments proved that TKL-105-107 can be used as highly efficient C2 H6 -selective adsorbents for C2 H4 purification. This work highlights that the purposeful functionalization of pore surfaces facilitates the assembly of highly efficient MOF adsorbents for specific gas separation.
RESUMO
Highly adjustable photonic modules were constructed based on the heterostructures crystals of a new series of donor-acceptor metal-organic framework (D-A MOF) featuring highly tunable thermally activated delayed fluorescence (TADF). By introducing N-phenylcarbazole and derivatives as donor guests into the acceptor host NKU-111, highly tunable through-space charge transfer based TADF could be achieved through the engineering of heavy atom effect, which result in modulatable emission wavelength (540 to 600â nm) and enhanced quantum yield (up to 30.86 %). Furthermore, by rationally integrating the D-A MOFs with distinctive emissions, rod-like heterostructures crystals featuring excitation position dependent tip emissions in wide wavelength range (495 to 598â nm) could be fabricated, which could serve as highly potential photonic modules for photonic circuit applications.
RESUMO
In order to provide rationale for selection of good germplasm in Rubus chingii, main effective medicinal ingredients of green fruit such as gallic acid, ellagic acid, kaempferol-3-rutinoside, astragalin and tiliroside were measured using UPLC for the samples collected from Chun'an county of Zhejiang province, and such parameters as soluble solid contents of ripe fruit of some samples were also measured to study variation among individuals and correlation. It has been found that there were differences among individuals in the contents of gallic acid, ellagic acid, kaempferol-3-rutinoside, astragalin and tiliroside, which ranged from 0.010 2%-0.027 4%, 0.089 5%-0.291 1%, 0.010 5%-0.114 8%, 0.005 8%-0.041 2% and 0.010 9%-0.086 3%, respectively, with a CV of 18.60%, 27.02%, 44.23%, 44.17% and 47.29%, respectively. Gallic acid was positively correlated with ellagic acid, but negatively with kaempferol-3-rutinoside and astragalin significantly. Significantly positive correlation existed between kaempferol-3-rutinoside, astragalin and linden glycoside as well as between ellagic acid and fruit shape index of ripe fruit and between linden glycoside and the content of soluble solids. 51.35% of the individuals had a content of soluble solids more than 15%. Therefore, abundant variations have been found among individuals in effective medicinal ingredients in R. chingii, which shows great potential for selection, but only do 7.61% of the individuals meet the requirement of Chinese pharmacopoeia in terms of the contents of effective medicinal ingredients. Therefore, selection could be first performed in terms of fruit shape index of ripe red fruit, followed by the contents of ellagic acid and kaempferol-3-rutinoside measured. The individuals, in which the contents of effective medicinal ingredients don't meet the requirement of Chinese pharmacopoeia, could be considered for the selection in terms of edible fresh fruit.
Assuntos
Rubus , Ácido Elágico , Frutas , Glicosídeos , Humanos , Extratos VegetaisRESUMO
Three new ruthenium(II) complexes-[Ru(bpy)2(adppz)](ClO4)2, [Ru(dmb)2(adppz)](ClO4)2, and [Ru(dmp)2(adppz)](ClO4)2 (bpy is 2,2'-bipyridine, adppz is 7-aminodipyrido[3,2-a:2',3'-c]phenazine, dmb is 4,4'-dimethyl-2,2'-bipyridine, and dmp is 2,9-dimethyl-1,10-phenanthroline)-were synthesized. [Ru(dmp)2(adppz)](ClO4)2 exhibits higher cytotoxicity than cisplatin toward A549, MG-63, and SKBR-3 cells. The apoptosis and cellular uptake were studied by fluorescence microscopy. [Ru(dmp)2(adppz)](ClO4)2 enhances the level of reactive oxygen species (ROS) and decreases the mitochondrial membrane potential. These complexes induce cell cycle arrest in S phase in BEL-7402 cells, and inhibit the antiproliferation of SKBR-3 cells at G0/G1 phase. Western blotting analysis shows that [Ru(dmp)2(adppz)](ClO4)2 induces apoptosis in BEL-7402 cells through activation of caspase 3, caspase 7, and procaspase 7 and ROS-mediated mitochondrial dysfunction pathways.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Rutênio/química , Rutênio/farmacologia , 2,2'-Dipiridil/química , 2,2'-Dipiridil/farmacologia , Apoptose/efeitos dos fármacos , Western Blotting , Linhagem Celular Tumoral , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Fenantrolinas/química , Fenantrolinas/farmacologia , Fenazinas/química , Fenazinas/farmacologia , Piridinas/química , Piridinas/farmacologia , Espécies Reativas de Oxigênio/metabolismoRESUMO
A new ligand DBHIP and its two ruthenium(II) complexes [Ru(dmb)(2)(DBHIP)](ClO(4))(2) (1) and [Ru(dmp)(2)(DBHIP)](ClO(4))(2) (2) have been synthesized and characterized. The cytotoxicity of DBHIP and complexes 1 and 2 has been assessed by MTT assay. The apoptosis studies were carried out with acridine orange/ethidium bromide (AO/EB) staining methods. The binding behaviors of these complexes to calf thymus DNA (CT-DNA) were studied by absorption titration, viscosity measurements, thermal denaturation and photoactivated cleavage. The DNA-binding constants of complexes 1 and 2 were determined to be 8.64 +/- 0.16 x 10(4) (s = 1.34) and 2.79 +/- 0.21 x 10(4) (s = 2.17) M(-1). The results suggest that these complexes interact with DNA through intercalative mode. The studies on the mechanism of photocleavage demonstrate that superoxide anion radical (O(2)(*-)) and singlet oxygen ((1)O(2)) may play an important role in the DNA cleavage. The experiments on antioxidant activity show that these compounds also exhibit good antioxidant activity against hydroxyl radical (OH*).
Assuntos
Antioxidantes , Apoptose/efeitos dos fármacos , DNA/efeitos dos fármacos , DNA/metabolismo , Fenantrolinas/química , Compostos de Rutênio , Animais , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Bovinos , Linhagem Celular , DNA/química , Clivagem do DNA/efeitos dos fármacos , Ligantes , Estrutura Molecular , Desnaturação de Ácido Nucleico , Compostos de Rutênio/síntese química , Compostos de Rutênio/química , Compostos de Rutênio/farmacologia , ViscosidadeRESUMO
Many ruthenium(II) complexes show high antitumor activities, and the in vitro antitumor activities are usually related to DNA binding. We designed and synthesized two Ru(II) polypyridyl complexes, [Ru(dmp)2(fpp)]2+ (dmp=2,9-dimethyl-1,10-phenanthroline; fpp=2-[3,4-(difluoromethylenedioxy)phenyl]imidazo[4,5-f] [1,10]phenanthroline and [Ru(phen)(2)(fpp)]2+ (phen=1,10-phenanthroline). The DNA-binding properties of these complexes have been investigated by spectroscopic titration, DNA melting experiments, viscosity measurements, and photoactivated cleavage. The mechanism studies of photocleavage revealed that singlet oxygen (1O2) and superoxide anion radical (O2(.-)) may play an important role in the photocleavage. The cytotoxicity of complexes 1 and 2 have been evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) method; complex 2 shows slightly higher anticancer potency than 1 does against all the cell lines screened.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , DNA/metabolismo , Neoplasias/tratamento farmacológico , Compostos de Rutênio/química , Compostos de Rutênio/farmacologia , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Modelos Moleculares , Estrutura Molecular , Desnaturação de Ácido Nucleico/efeitos dos fármacos , Fenantrolinas/síntese química , Fenantrolinas/química , Fenantrolinas/farmacologia , Processos Fotoquímicos/efeitos dos fármacos , Compostos de Rutênio/síntese química , Viscosidade/efeitos dos fármacosRESUMO
OBJECTIVE: To investigate the mechanisms that coagulation factor VIIa promotes proliferation and migration of a colon cancer cell line (SW620 cells) in vitro. METHODS: The expression of interleukin 8 (IL-8), tissue factor (TF), caspase-7 and p-p38 MAPK in SW620 cells treated with factor VIIa or protease activated receptor 2 agonist (PAR2-AP) was measured by ELISA, Western-blotting and QT-PCR. RESULTS: Factor VIIa and PAR2-AP induced IL-8 expression at both mRNA and protein levels, upregulated TF mRNA expression and TF activity, but down-regulated caspase-7 mRNA and p-p38 MAPK levels in SW620 cells. The effects of factor VIIa were not only blocked by anti-TF but also by anti-PAR2 antibodies. CONCLUSION: Factor VIIa binds to TF on cell surface, forming a complex which activates PAR2, then provoking IL-8 and TF expression, and suppresses caspase-7 expression, thus promotes the tumor cell proliferation and migration. p38 MAPK may negatively regulate this process.
Assuntos
Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Neoplasias do Colo/patologia , Fator VIIa/farmacologia , Caspase 7/biossíntese , Caspase 7/genética , Linhagem Celular Tumoral , Neoplasias do Colo/metabolismo , Humanos , Interleucina-8/biossíntese , Interleucina-8/genética , Oligopeptídeos/farmacologia , RNA Mensageiro/metabolismo , Receptor PAR-2/agonistas , Tromboplastina/biossíntese , Tromboplastina/genética , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismoRESUMO
Three new iridium (III) complexes [Ir (ppy)2 (ipbc)](PF6) (1), [Ir (bzq)2 (ipbc)](PF6) (2) and [Ir (piq)2 (ipbc)](PF6) (3) were designed and synthesized. All the complexes were tested for anticancer activity using 3-(4,5-dimethylthiazole)-2,5-diphenyltetraazolium bromide (MTT) method. The complexes show no cytotoxic activity toward cancer BEL-7402, SGC-7901, Eca-109, A549, HeLa and HepG2 cells. However, upon irradiation with white light, the complexes display high cytotoxicity against BEL-7402â¯cells with an IC50 value of 5.5⯱â¯0.8, 7.3⯱â¯1.3 and 11.5⯱â¯1.6⯵M for 1, 2 and 3, respectively. AO/EB staining and comet assay show that the complexes can induce apoptosis in BEL-7402â¯cells. The complexes can increase intracellular ROS and Ca2+ levels and cause a decrease in the mitochondrial membrane potential. Autophagic assays exhibit that the complexes can induce autophagy and regulate the expression of Beclin-1 and LC3 proteins. The cell cycle distribution in BEL-7402â¯cells was carried out by flow cytometry. The expression of Bcl-2 family proteins was studied by western blot. Additionally, the complexes can release cytochrome c and inhibit the polymerization of α-tubulin. Our study reveals that the complexes inhibit the cell growth in BEL-7402â¯cells through an ROS-mediated mitochondria dysfunction and targeting tubules pathways. These complexes are a promising new entity for the development of multi-target anticancer drugs.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Irídio/química , Irídio/farmacologia , Microtúbulos/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Microtúbulos/metabolismo , Microtúbulos/patologia , Mitocôndrias/metabolismo , Mitocôndrias/patologia , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Neoplasias/patologia , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/farmacologia , Espécies Reativas de Oxigênio/metabolismoRESUMO
OBJECTIVE: To construct a novel kind of nonviral gene delivery vector based on polyethylenimine (PEI) conjugated with polypeptides derived from ligand FGF with high transfection efficiency and according to tumor targeting ability. METHODS: The synthetic polypeptides CR16 for binding FGF receptors was conjugated to PEI and the characters of the polypeptides including DNA condensing and particle size were determined. Enhanced efficiency and the targeting specificity of the synthesized vector were investigated in vitro and in vivo. RESULTS: The polypeptides were successfully coupled to PEI. The new vectors PEI-CR16 could efficiently condense pDNA into particles with around 200 nm diameter. The PEI-CR16/pDNA polyplexes showed significantly greater transgene activity than PEI/pDNA in FGF receptors positive tumor cells in vitro and in vivo gene transfer, while no difference was observed in FGF receptors negative tumor cells. The enhanced transfection efficiency of PEI-CR16 could be blocked by excess free polypeptides. CONCLUSION: The synthesized vector could improve the efficiency of gene transfer and targeting specificity in FGF receptors positive cells. The vector had good prospect for use in cancer gene therapy.
Assuntos
Técnicas de Transferência de Genes , Neoplasias Hepáticas/terapia , Peptídeos/farmacologia , Polietilenoimina/farmacologia , Neoplasias da Próstata/terapia , Receptores de Fatores de Crescimento de Fibroblastos/metabolismo , Animais , Sítios de Ligação , Carcinoma/terapia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Feminino , Fatores de Crescimento de Fibroblastos/metabolismo , Vetores Genéticos/síntese química , Vetores Genéticos/química , Vetores Genéticos/farmacologia , Humanos , Técnicas In Vitro , Ligantes , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Tamanho da Partícula , Peptídeos/química , Peptídeos/metabolismo , Polietilenoimina/química , Polietilenoimina/metabolismo , Receptores de Fatores de Crescimento de Fibroblastos/efeitos dos fármacos , Receptores de Fatores de Crescimento de Fibroblastos/genética , Relação Estrutura-Atividade , Propriedades de Superfície , Transfecção , Transplante Heterólogo , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
A Ru(II) polypyridyl complex [Ru(bpy)2(HMSPIP)](ClO4)2 (1) (bpy=2,2'-bipyridine, HMSPIP=2-(4-methylsulfonyl)phenyl-1H-imidazo[4,5-f][1,10] phenanthroline) was synthesized. The IC50 value of the complex against human hepatocellular cell BEL-7402 is 21.6±2.7 µM. The complex shows no cytotoxic activity toward human lung adenocarcinoma cell A549, human osteosarcoma cell MG-63 and human breast cancer cell SK-BR-3 cells. It is easily for complex 1 to be taken up by BEL-7402 cells. The complex can enhance the reactive oxygen species (ROS) levels and induce the decrease in the mitochondrial membrane potential. The complex inhibits the cell growth in BEL-7402 cells at G2/M phase. Complex 1 can regulate the expression of Bcl-2 family proteins. The results show that the complex induces apoptosis of BEL-7402 cells through a ROS-mediated mitochondrial dysfunction pathway.
Assuntos
2,2'-Dipiridil/análogos & derivados , Antineoplásicos/química , Antineoplásicos/farmacologia , Neoplasias Hepáticas/tratamento farmacológico , Compostos Organometálicos/química , Compostos Organometálicos/farmacologia , 2,2'-Dipiridil/química , 2,2'-Dipiridil/farmacologia , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismoRESUMO
Two new ruthenium(II) polypyridyl complexes [Ru(dmb)2(dcdppz)](ClO4)2 (1) and [Ru(bpy)2(dcdppz)](ClO4)2 (2) were prepared and characterized. The crystal structure of the complex 2 was solved by single crystal X-ray diffraction. The complex crystallizes in the monoclinic system, space group P21/n with a=12.9622(14)Å, b=17.1619(19)Å, c=22.7210(3)Å, ß=100.930(2)(°), R=0.0536, Rω=0.1111. The DNA-binding constants for complexes 1 and 2 were determined to be 1.92×10(5) (s=1.72) and 2.24×10(5) (s=1.86)M(-1), respectively. The DNA-binding behaviors showed that complexes 1 and 2 interact with DNA by intercalative mode. The antioxidant activities of the ligand and the complexes were performed. Ligand, dcdppz, has no cytotoxicity against the selected cell lines. Complex 1 shows higher cytotoxicity than complex 2, but lower than cisplatin toward selected cell lines. The apoptosis and cell cycle arrest were investigated, and the apoptotic mechanism of BEL-7402 cells was studied by reactive oxygen species (ROS), mitochondrial membrane potential and western blot analysis. Complex 1 induces apoptosis in BEL-7402 cells through ROS-mediated mitochondrial dysfunction pathway and by regulating the expression of Bcl-2 family proteins.
Assuntos
Antioxidantes/farmacologia , Complexos de Coordenação/farmacologia , DNA/metabolismo , Rutênio/farmacologia , Animais , Apoptose/efeitos dos fármacos , Caspases/metabolismo , Bovinos , Ciclo Celular/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Cristalografia por Raios X , Elétrons , Endocitose/efeitos dos fármacos , Citometria de Fluxo , Sequestradores de Radicais Livres/farmacologia , Humanos , Radical Hidroxila/química , Concentração Inibidora 50 , Ligantes , Luminescência , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Conformação Molecular , Proteínas de Neoplasias/metabolismo , Espectrometria de Fluorescência , ViscosidadeRESUMO
A new ligand dmdppz and its four ruthenium(II) polypyridyl complexes [Ru(dmb)2(dmdppz)](ClO4)2 (1), [Ru(bpy)2(dmdppz)](ClO4)2 (2), [Ru(phen)2(dmdppz)](ClO4)2 (3) and [Ru(dmp)2(dmdppz)](ClO4)2 (4) (where dmb, bpy, phen, dmp and dmdppz stand for 4,4'-dimethyl-2,2'-bipyridine, 2,2'-bipyridine, 1,10-phenanthroline, 2,9-dimethyl-1,10-phenanthroline and 5,8-dimethoxylpyrido[3,2-a:2',3'-c]phenazine, respectively) have been synthesized and characterized. Their DNA binding behaviors show that the complexes bind to calf thymus DNA by intercalation. The complexes exhibit efficient photocleavage of pBR322 DNA on irradiation. The cytotoxicity of the ligand and the complexes toward HepG-2, HeLa, MG-63, A549 and BEL-7402 were assayed by MTT ((3-(4,5-dimethylthiazo-2-yl)-2,5-diphenyltetrazolium bromide)) method. The IC50 values of the complexes 1, 2, 3 and 4 toward BEL-7402 cells are 14.6, 16.8, 18.0 and 16.7 µM, respectively. Dmdppz shows no cytotoxic activity against selected cell lines. The cellular uptake, apoptosis, comet assay, reactive oxygen species (ROS), mitochondrial membrane potential and western blot analysis were investigated. These results indicate that complexes 1-4 exert their toxicity through the intrinsic ROS-mediated mitochondrial pathway, which is accompanied by the regulation of Bcl-2 family proteins.
Assuntos
Antineoplásicos/síntese química , Complexos de Coordenação/síntese química , Citotoxinas/síntese química , Substâncias Intercalantes/síntese química , Mitocôndrias/efeitos dos fármacos , Espécies Reativas de Oxigênio/agonistas , Rutênio/química , Antineoplásicos/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cisplatino/farmacologia , Complexos de Coordenação/farmacologia , Citotoxinas/farmacologia , DNA/química , Regulação Neoplásica da Expressão Gênica , Células HeLa , Células Hep G2 , Humanos , Substâncias Intercalantes/farmacologia , Mitocôndrias/metabolismo , Plasmídeos/química , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Piridinas/química , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-AtividadeRESUMO
Three novel aryloxazole compounds 1-3 were synthesized and characterized. The crystal structures of compounds 2 and 3 show that N atom locates at ß-position and O atom at α-position in naphthalene cycle. The DNA binding constants for compounds 1-3 are 4.44 × 10(3), 5.31 × 10(3) and 2.64 × 10(3) M(-1), respectively. The viscosity measurements indicate that these compounds intercalate between the DNA base pairs. Upon irradiation, compounds 1-3 can effectively cleave pBR322 DNA. The cytotoxicity of the compounds against BEL-7402, A549, MG-63 and SKBR-3 were assayed by MTT method. The apoptosis and cell cycle arrest were investigated towards A549 cells. The antioxidant activities of the compounds against hydroxyl radicals were also explored.
Assuntos
Apoptose/efeitos dos fármacos , DNA/metabolismo , Oxazóis/síntese química , Oxazóis/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Técnicas de Química Sintética , Humanos , Radical Hidroxila/química , Substâncias Intercalantes/síntese química , Substâncias Intercalantes/química , Substâncias Intercalantes/metabolismo , Substâncias Intercalantes/farmacologia , Oxazóis/química , Oxazóis/metabolismoRESUMO
Two new Ru(II) complexes, [Ru(bpy)2(FAMP)](ClO4)2 1 and 2, are synthesized and characterized by elemental analysis, electrospray mass spectrometry, and 1H nuclear magnetic resonance. The in vitro cytotoxicities and apoptosis-inducing properties of these complexes are extensively studied. Complexes 1 and 2 exhibit potent antiproliferative activities against a panel of human cancer cell lines. The cell cycle analysis shows that complexes 1 and 2 exhibit effective cell growth inhibition by triggering G0/G1 phase arrest and inducing apoptosis by mitochondrial dysfunction. The in vitro DNA binding properties of the two complexes are investigated by different spectrophotometric methods and viscosity measurements.
Assuntos
Compostos Organometálicos/síntese química , Compostos Organometálicos/farmacologia , Rutênio/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Compostos Organometálicos/química , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
The waters around the South Georgia Island is one of the main fishing ground of Antarctic krill fishery and many predators such as sea seal and whale inhabited this island target Antarctic krill as a food source. So it is very important for further understanding Antarctic ecosystem to conduct the research on abundance fluctuation of Antarctic krill resource around this island. Consequently, based on the fine scale fishery data collected in the winter 2013, using the generalized additive model (GAM), the present study analyzed the relationship between environmental factors and the catch rate of Antarctic krill. The results showed the model could explain 32.0% of the accumulation of deviance of the catch rate. The variable that provided the maximum contribution was ten-day with a contribution rate of 21.4% and followed by the latitude (4.4%). Generally, the catch rate decreased from the first 10 days of July to September. Higher catch rates occurred in the eastern fishing ground, particularly the central-eastern part of survey area, and lower catch rates presented in the northern part. The mean catch rate deceased with the increasing change rate of bathymetry. The oceanographic condition with wind scale below 4 was suitable for fishing operation and associated with the higher catch rate, but the wind direction did not significantly affect the catch rate. The mean catch rate increased with the increasing sea surface temperature within 0.5 to 2.0 degrees C.
Assuntos
Euphausiacea , Pesqueiros , Estações do Ano , Animais , Regiões Antárticas , Ecossistema , Peixes , Ilhas , Análise Espaço-Temporal , TemperaturaRESUMO
Two new dibenzoxanthenes compounds 1 and 2 have been synthesized and characterized by analytical and spectral methods. The crystal structure of compound 2 informs that the five rings of compound are almost planar. The DNA binding properties of two compounds were studied by absorption titration, viscosity measurement and luminescence. These results indicate that two compounds interact with calf thymus DNA through intercalative mode. Agarose gel electrophoresis experiment shows that PBR 322 DNA can be induced to cleave by two compounds under photoactivated condition. Compound 1 exhibits higher cytotoxicity than compound 2 toward MG-63, BEL-7402 and A549 cells. The apoptosis and cellular uptake of MG-63 cells were studied by fluorescence microscopy. Two compounds can also enhance the level of reactive oxygen species (ROS) and decrease the mitochondrial membrane potential. Compound 1 induces cell cycle arrest in G2/M phase and compound 2 induces cell cycle arrest in G0/G1 phase in MG-63.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Xantenos/química , Xantenos/farmacologia , Animais , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Bovinos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , DNA/metabolismo , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Xantenos/síntese químicaRESUMO
The aim of our study was to investigate DNA-binding and cytotoxic activity of the four new Ru(II) polypyridyl complexes [Ru(dmb)2(HMHPIP)](ClO4)2 (1), [Ru(bpy)2(HMHPIP)](ClO4)2 (2), [Ru(phen)2(HMHPIP)](ClO4)2 (3) and [Ru(dmp)2(HMHPIP)](ClO4)2 (4). The complexes interact with DNA through intercalative mode and show relatively high cytotoxic activity against A549 cells, no cytotoxicity toward MG-63 cells. Complexes 1-4 can enhance the levels of ROS in A549 cells and induce the decrease of the mitochondrial membrane potential. These complexes inhibit the cell growth in A549 cells at G0/G1 or S phase. Complex 3 activated caspase 7, and down-regulated the expression of the anti-apoptotic protein Bcl-2. Complexes 1-4 induce apoptosis in A549 cells through ROS-mediated mitochondrial dysfunction pathway.
Assuntos
Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Complexos de Coordenação/toxicidade , DNA/metabolismo , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Rutênio/química , Western Blotting , Caspase 3/metabolismo , Caspase 7/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , DNA/química , Clivagem do DNA/efeitos dos fármacos , Clivagem do DNA/efeitos da radiação , Humanos , Substâncias Intercalantes/síntese química , Substâncias Intercalantes/química , Substâncias Intercalantes/toxicidade , Plasmídeos/química , Plasmídeos/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Raios UltravioletaRESUMO
Two novel ruthenium(II) complexes [Ru(dmb)2(addppn)](ClO4)2 (1) and [Ru(bpy)2(addppn)](ClO4)2 (2) were synthesized. The DNA-binding constants of complexes 1 and 2 were determined to be 4.78 (±0.49) × 10(5) and 7.42 (±0.53) × 10(5) M(-1). The results indicate that complexes 1 and 2 interact with CT DNA through intercalative mode. The cytotoxicity in vitro of the complexes toward BEL-7402, HeLa, MG-63 and SKBR-3 cells was assessed by MTT assay. The apoptosis was carried out with Hoechst 33258 staining method and flow cytometry. The cellular uptake was observed under fluorescence microscope. The cell cycle arrest shows that the antiproliferative mechanism induced by complexes 1 and 2 on BEL-7402 cells is G0/G1 phase arrest.
Assuntos
Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Compostos Organometálicos/farmacologia , Rutênio/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , DNA/química , DNA/metabolismo , Clivagem do DNA/efeitos dos fármacos , Clivagem do DNA/efeitos da radiação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Citometria de Fluxo , Células HeLa , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Compostos Organometálicos/química , Compostos Organometálicos/metabolismo , Fotoquímica , EspectrofotometriaRESUMO
Two new Ru(II) polypyridyl complexes [Ru(phen)2(adppz)](ClO4)2 (1) and [Ru(dip)2(adppz)](ClO4)2 (2) have been synthesized and characterized. The DNA-binding constants were determined to be 6.54 ± 0.42 × 10(5) and 7.65 ± 0.20 × 10(5)M(-1) for complexes 1 and 2. DNA binding experiments indicated that complexes 1 and 2 interact with DNA through intercalative mode. Antioxidant activity shows that the complexes have significant hydroxyl radical scavenging activity. Cytotoxic activities suggest that the complex 2 exhibits higher cytotoxic activity against BEL-7402, MG-63 and SKBR-3 cells than complex 1 under identical conditions. Complexes 1 and 2 can induce apoptosis of BEl-7402 cells. We have identified several cellular mechanisms induced by 1 and 2 in BEL-7402 cells, including the level detection of ROS, activation of procaspase 3, caspase 7, the expression of antiapoptotic proteins Bcl-x, Bcl-2, proapoptotic proteins Bad, Bax, Bid and cell cycle arrest. Thus, complexes 1 and 2 inhibit growth of BEL-7402 cells through induction of apoptotic cell death, enhancement of ROS levels and S-phase and G0/G1 cell cycle arrest. Further investigations have shown that complex 2 induces apoptosis by regulating the expression of Bcl-2 family proteins.
Assuntos
Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , DNA/metabolismo , Rutênio/química , Antineoplásicos/síntese química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 7/metabolismo , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/metabolismo , DNA/química , Humanos , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismoRESUMO
Two new ruthenium(II) polypyridyl complexes [Ru(dmb)(2)(HECIP)](ClO(4))(2) (1) (HECIP = N-ethyl-4-[(1,10)-phenanthroline(5,6-f)imidazol-2-yl]carbazole, dmb = 4,4'-dimethyl-2,2'-bipyridine) and [Ru(dmp)(2)(HECIP)](ClO(4))(2) (2) (dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and characterized. The DNA-binding behaviors of the two complexes were investigated by absorption spectra, viscosity measurements, and photoactivated cleavage. The DNA-binding constants for complexes 1 and 2 were determined to be 8.03 (± 0.12) × 10(4) M(-1) (s = 1.62) and 2.97 (± 0.15) × 10(4) M(-1) (s = 1.82), respectively. The results suggest that these complexes interact with DNA through intercalative mode. The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 has been evaluated by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide)] method. Complex 1 shows higher anticancer potency than 2 against the four tumor cell lines. Apoptosis and cellular uptake were investigated. The antioxidant activities of the ligand and these complexes were also performed.