JOURNAL OF MOLECULAR LIQUIDS
·
2016
·
IF 2.74
Muhammad Asim Akhtar,Sara Riaz,Akhtar Hayat,Muhammad Nasir,Nawshad Muhammad,Abdur Rahim,Mian Hasnain Nawaz
trans -Porphyrin containing phenyl group at both ends was synthesized via corresponding dipyrromethanes (DPM) in the presence of TFA and DDQ. The polyethyleneglycole (PEG) chains were attached at the trans positions of ABA type porphyrinic moiety. The prepared PEGylated porphyrin (with PEG arms at the periphery) P-(PEO) 2 was self-assembled into spheres of uniform diameter while their DMF solution was dialyzed into water. Furthermore, the addition of fullerene (C 60 ) to P-(PEO) 2 caused complexation between porphyrin and fullerene which lead to interesting and trenchant morphology having worm like lateral aggregates. The assembly process and the as-prepared edifices were characterized using UV–vis absorption spectroscopy and the morphology of these assemblies was investigated using transmission electron microscope (TEM). Furthermore, the DNA binding with porphyrin aggregates has been demonstrated via electrochemical (cyclic voltammetric) response of screen printed electrodes modified . The obvious increase in redox current disclosed the intermolecular interactions of the adducts with the DNA. These studies of unprecedented adducts can further be explored for potential applications in biosensors .
研究领域:
生物化学
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材料科学
·
分子生物学
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DOI
高影响因子
AUSTRALIAN JOURNAL OF CHEMISTRY
·
2019
·Vol. 72
·期 5
·400-406
·
IF 1.226
Xukui Liu,Xuanhao Zhao,Yumei Li,Kangdi Zheng,Qiong Wu,Wenjie Mei,Xukui Liu,Xuanhao Zhao,Yumei Li,Kangdi Zheng,Qiong Wu,Wenjie Mei
Three novel norfloxacin-based ruthenium(ii) complexes, [Ru(bpy)2(NFLX)]Cl·2H2O (1), [Ru(phen)2(NFLX)]Cl·2H2O (2), and [Ru(dmbpy)2(NFLX)]Cl·2H2O (3) (bpy = 2,2′-bipyridine, phen = 1,10-phenanthroline, dmbpy = 4,4′-dimethyl-2,2′-bipyridine, and NFLX = norfloxacin), were synthesised and characterised with electrospray ionisation mass spectrometry and 1H and 13C NMR spectroscopy. The antitumour properties were evaluated by MTT assay, and the data revealed that 2 can inhibit the growth of human lung adenocarcinoma A549 efficiently. Furthermore, the DNA-binding behaviours of these complexes were investigated by a multiple spectroscopy assay and viscosity study. The results indicated that these complexes interact with calf thymus DNA through electrostatic interactions with a strong binding affinity in the order 2 > 3 > 1. Therefore, these results suggested that 2 might be a suitable anticancer agent due to its excellent DNA-binding abilities.
研究领域:
生物化学
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药理学
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肿瘤学
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DOI
高影响因子
JOURNAL OF FLUORESCENCE
·
2013
·Vol. 24
·期 2
·533-539
·
IF 1.789
Liu Chengxuan,Liang Gaiting,Liu Zhen,Zu Lily
Time-resolved fluorescence anisotropy spectroscopy was applied to study the interaction between a peptide truncated from the binding site of tumor suppressor p53 protein and the DNAs covalently labeled with 6-carboxyfluorescein (FAM) dye. Fluorescence intensity quenching and changes of anisotropy decay lifetime were monitored when FAM labeled DNA formed complex with the peptide. The results demonstrated that the sequence of DNA could not define the binding specificity between the peptide and DNA. But the anisotropy decay of FAM can be used to examine the binding affinity of the peptide to DNA. The fluorescent dynamics of FAM can also be used to represent the rigidity of the complex formed between the peptide and DNA.
研究领域:
生物化学
·
分子生物学
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DOI
PubMed
高影响因子
IMMUNITY
·
2023
·
IF 32.4
Lina Wang,Siru Li,Kai Wang,Na Wang,Qiaoling Liu,Zhen Sun,Li Wang,Lulu Wang,Quentin Liu,Chengli Song,Qingkai Yang
Self-nonself discrimination is vital for the immune system to mount responses against pathogens while maintaining tolerance toward the host and innocuous commensals during homeostasis. Here, we investigated how indiscriminate DNA sensors, such as cyclic GMP-AMP synthase (cGAS), make this self-nonself distinction. Screening of a small-molecule library revealed that spermine, a well-known DNA condenser associated with viral DNA, markedly elevates cGAS activation. Mechanistically, spermine condenses DNA to enhance and stabilize cGAS-DNA binding, optimizing cGAS and downstream antiviral signaling. Spermine promotes condensation of viral, but not host nucleosome, DNA. Deletion of viral DNA-associated spermine, by propagating virus in spermine-deficient cells, reduced cGAS activation. Spermine depletion subsequently attenuated cGAS-mediated antiviral and anticancer immunity. Collectively, our results reveal a pathogenic DNA-associated molecular pattern that facilitates nonself recognition, linking metabolism and pathogen recognition.
研究领域:
免疫学
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分子生物学
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病毒学
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癌症研究
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DOI
PubMed
高影响因子
ENVIRONMENT INTERNATIONAL
·
2022
·
IF 13.352
Hao Cheng,Chao Qin,Bing Yang,Xiaojie Hu,Michael Gatheru Waigi,Galina K. Vasilyeva,Yanzheng Gao
The interaction of phthalic acid esters (PAEs) with DNA is known to be responsible for the disruption of endocrine functions and the teratogenic and carcinogenic effects. However, the binding strength and mechanism of this important process has often been neglected. Here, we confirmed the binding interaction between PAEs and DNA via fluorescence titration quenching experiment. The linear fitting curve proved that PAEs could bind to DNA, and the binding constants ( K A ) were 4.11 × 10 5 , 1.04 × 10 5 , 7.60 × 10 4 , 1.99 × 10 4 , and 1.42 × 10 3 L/mol for diethyl phthalate (DEP), bis(2-ethylhexyl) phthalate (DEHP), dibutyl phthalate (DBP), dimethyl phthalate (DMP), and benzyl butyl phthalate (BBP), respectively. DNA melting point, UV–vis spectra and Fourier transform infrared spectroscopy (FTIR) analyses revealed that PAEs interact predominantly with thymines in the DNA minor groove. Quantum chemical calculations showed that hydrogen bonding and van der Waals force formation between PAEs and DNA bases dominated the binding interaction. However, PAEs-DNA binding did not induce any DNA conformation change since the circular dichroism and FTIR spectra of B-DNA were not change. The electrostatic surface potential (ESP) might act an important role in PAEs-DNA binding interaction. This work will broaden our understanding of the interaction between PAEs and genetic materials.
研究领域:
分子生物学
·
毒理学
·
环境科学
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DOI
PubMed
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2019
·Vol. 34
·期 1
·e5264
·
IF 3.259
Ruixue Wu,Caifeng Bi,Xia Zhang,Ziao Zong,Chuanbin Fan,Xiaoyin Zhang,Nana Li,Yuhua Fan
Three novel Cu (II) coordination complexes, formulated as [Cu 3 (C 14 H 8 NO 3 F) 2 (CH 3 COO) 2 ] n ( 1 ), [Cu 2 (C 14 H 9 NO 3 F) 2 (CH 3 COO)Cl] ( 2 ) and [Cu(C 14 H 8 NO 3 F)(CH 3 OH) 2 ] ( 3 ), have been synthesized by 3-Fluoroanthranilic acid, Salicylaldehyde and Cu (II) salt as sources in different reaction conditions and characterized by single crystal X-ray diffraction, X-ray powder diffraction, IR spectroscopy and elemental analysis. Single-crystal diffraction analysis revealed that the complexes exhibited different coordination modes and conformations which were linked into multidimensional networks through some weak interactions. The biological activities vary greatly on account of the different Cu (II) numbers among the three complexes. In order to discuss the bioactivities, the complexes have been screened for antimicrobial activities against E. coli and S. aureus , antitumor activities against A549 (human lung cancer cells), Hela (human cervical cancer cells) and HepG-2(human liver hepatocellular carcinoma cells). Their interactions with calf thymus DNA were investigated by UV–visible and fluorescence spectrometry, as well as viscosity measurements. Interestingly, 1 (the rare 3-core Cu (II) coordination polymer) shows great antibacterial activities and highest DNA binding affinities. Antitumor studies revealed that complex 1 also exhibited highest activity.
研究领域:
配位化学
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生物无机化学
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药物化学
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DOI
高影响因子
CHINESE JOURNAL OF CHEMISTRY
·
2015
·Vol. 33
·期 9
·1084-1088
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IF 1.578
Yafang Tan,Xiaohui Sun,Fuyue Dong,Haiyan Tian,Renwang Jiang
To enhance the structural diversity of tanshinones and provide more derivatives for the biological studies, a one-pot combinatorial modification strategy was performed on total tanshinones. Six new quinoxlinetanshinones 1 – 6 were subsequently isolated from the combinatorial modified semi-synthetic mixture. The structures were elucidated by spectroscopic analysis in combination with single-crystal X-ray diffraction. These quinoxlinetanshinones demonstrated strong DNA binding properties. Rapid synthesis of new quinoxlinetanshinones with significant biological activity highlights the great potential of one-pot combinatorial modification for the diversification of natural products.
研究领域:
药理学
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有机化学
·
天然产物研究
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DOI
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2022
·Vol. 36
·期 7
·e6759
·
IF 4.072
Lihua Chen,Pan Zhao,Jing Yang,Xiali Liao,Bo Yang,Chuanzhu Gao
A series of antitumor platinum (IV) complexes based on ammonia and fluoropyridine carrier groups with biotin and chloride ions as axial groups have been designed and synthesized in this paper. The structures of platinum (IV) complexes were fully characterized by 1 H NMR, ESI-MS, and IR. Such Pt (IV) complexes have certain tumor targeting properties, and the Pt (II) complexes released in the reducing microenvironment could combine with DNA. Compared with cisplatin, complexes S3 and S4 exhibited similar cytotoxicity against SW480, HCT116, and HepG2 cancer cell lines according to in vitro antitumor activity evaluation. Particularly, Complex S2 showed 1.5–3.0 times higher cytotoxicity than cisplatin and picoplatin against selected cell lines. According to the structure–activity relationship, the introduction of fluorine atoms and axial chloride has an important influence on the strong cytotoxic activity of Pt (IV) complex. In addition, the axial biotin molecule increased the targeting of the complex to tumor cells. Overall, the novel fluorine-containing Pt (IV) complex S2 is an attractive antitumor lead compound with further research value.
研究领域:
药物化学
·
肿瘤学
·
生物无机化学
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DOI
高影响因子
JOURNAL OF FLUORESCENCE
·
2016
·Vol. 27
·期 2
·701-714
·
IF 1.601
Gan Qian,Qi Yongyu,Xiong Yahong,Fu Yinlian,Le Xueyi
Two new mononuclear mixed ligand copper(II) complexes [Cu(PBO)(Gly-gly)(H 2 O)]·ClO 4 ·1.5H 2 O ( 1 ) and [Cu(PBO)(Gly- L -leu)(H 2 O)]·ClO 4 ( 2 ) (PBO is 2-(2′-pyridyl)benzoxazole, Gly-gly and Gly- L -leu are Glycyl-glycine anion and Glycyl- L -leucine anion, respectively), have been prepared and characterized by various analytical and spectral techniques. The interactions of the complexes with DNA were investigated using multi-spectroscopic methods (absorption, emission, circular dichroism), viscometry and electrochemical titration as well as molecular docking technique. The results indicated that 1 and 2 are bound to calf thymus DNA (CT-DNA) through an intercalative mode. The thermodynamic analyses revealed that the reactions between the Cu(II) complexes with DNA are spontaneous with negative Gibbs free energy (Δ G ). The positive changes of enthalpy (Δ H ) and entropy (Δ S ) suggested that the binding processes are dominated by hydrophobic interaction accompanying with endothermic. Also, the complexes exhibited efficient oxidative cleavage of pBR322 plasmid DNA in the presence of ascorbic acid, probably induced by •OH as reactive oxygen species. In addition, 1 and 2 displayed excellent antioxidant activities with the IC 50 values of 0.112 and 0.191 μM, respectively, using the mean of nitroblue tetrazolium (NBT) photochemical reduction under a nonenzymatic condition. Moreover, the complexes were screened for their in vitro cytotoxicity against three human carcinoma cell lines (HeLa, PC-3 and A549), in which 2 owns higher cytotoxicity, which was consistent with DNA binding and cleavage ability order of the complexes. This results showed the in vitro biochemical potentials of the Cu(II)-dipeptide complexes with aromatic heterocyclic, viz. effective metallopeptide-nucleases, SOD mimics and non-platinum chemotherapeutic metallopharmaceuticals and their structure-activity relationship, which may contribute to the rational molecular design of new metallopeptide based chemotherapeutic agents.
研究领域:
生物化学
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药理学
·
分子生物学
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DOI
高影响因子
TRANSITION METAL CHEMISTRY
·
2018
·Vol. 43
·期 3
·259-271
·
IF 1.261
Liu Ya-Xian,Mo Hui-Wen,Lv Zhen-Yu,Shen Fang,Zhang Chun-Lian,Qi Yong-Yu,Mao Zong-Wan,Le Xue-Yi
A copper complex [Cu(HPBM)( l -Phe)(H 2 O)]·ClO 4 (1) (HPBM = 5-methyl-2-(2′-pyridyl)benzimidazole, l -Phe = l -phenylalanine anion) was synthesized and characterized by elemental analysis, IR, ESI–MS, HR–ESI–MS, ESR spectroscopy, and by X-ray single-crystal analysis. The binding constant of the complex with calf thymus DNA (CT-DNA) was determined as 7.38 (± 0.57) × 10 4 M −1 . Further studies indicated that the complex interacts with CT-DNA through minor groove binding. The in vitro cytotoxic activities of both the free proligand and the complex against Eca-109, HeLa and A549 cancer cells and normal LO2 cells were evaluated by the MTT method. The IC 50 values range from 5.7 ± 0.1 to 8.3 ± 0.6 µM. Free HPBM displays no cytotoxic activity against the selected cancer cells, with IC 50 values more than 100 µM. Double staining analysis showed that the complex can induce apoptosis in Eca-109 cells. Comet assays demonstrated that the complex can damage DNA and cause apoptosis. The complex also induces an increase in intracellular reactive oxygen species and a reduction in mitochondrial membrane potential. The complex can also increase the intracellular Ca 2+ level and induce release of cytochrome c . The cell cycle arrest was investigated by flow cytometry. The results demonstrate that the complex induces apoptosis in Eca-109 cells through DNA-binding and ROS-mediated mitochondrial dysfunctional pathways.
研究领域:
生物化学
·
药理学
·
肿瘤学
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产品关联
DOI
高影响因子
MACROMOLECULAR CHEMISTRY AND PHYSICS
·
2013
·Vol. 214
·期 20
·2266-2275
·
IF 2.386
Jixian Liu,Zhen Liu,Xiong Luo,Xidan Zong,Jingquan Liu
The preparation of biodegradable and positively charged graphene–polymer nanocomposite for DNA uptake and release is presented. A pyrene-terminated poly(2-(dimethylamino) ethyl acrylate) is firstly synthesized via reversible addition–fragmentation chain transfer (RAFT) polymerization, followed by the attachment onto the graphene surface via the π–π stacking interaction. The positively charged polymer brushes benefit the uptake of the negatively charged DNA fragment via static interaction and the built-in disulfide linkage between the polymer chain and graphene surface allows the biodegradable release of DNA in the presence of reducing agents. X-ray photoelectron spectroscopy manifests the binding of DNA molecules to the polymer chains and agarose gel electrophoresis confirms the release of DNA.
研究领域:
材料科学
·
生物医学工程
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Qizhi Zhang,Wenmei Yu,Zhenhua Liu,Hui Li,Yihui Liu,Xin Liu,Zhaoshun Han,Jun He,Yaofu Zeng,Yu Guo,Yunmei Liu
Photodynamic therapy is a promising novel tumor treatment method. In this study, novel porphyrin-chrysin photosensitizer derivatives were synthesized. Most of the compounds showed antitumor activity against human cervical cancer HeLa cells and human lung cancer A549 cells, among which compound 4c had the best photodynamic therapy effect on HeLa cells and A549 cells, with IC 50 values of 6.26 μM and 23.37 μM, respectively. Free-base porphyrin-chrysin derivatives bind to DNA through surface self-stacking, and zinc metalloporphyrin-chrysin derivatives bind to ct-DNA through intercalation. Notably, the tightness of compound binding to ct-DNA was positively correlated with its antitumor activity. What's more, three-dimensional quantitative conformation studies have shown that increasing the positive charge of the porphyrin ring and introducing a strong electron-withdrawing group at the meso position of the porphyrin ring at the para-position of the benzene ring or reducing the space volume of the compound can enhance the antitumor activity.
研究领域:
药理学
·
肿瘤学
·
生物化学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）