Zirconia nanotube array films(ZNAF)prepared by anodic oxidation method were used as immobilization materials for acridine orange(AO),rhodamine B(RB)and AO-RB systems.A comparative study on their fluorescence emission ...Zirconia nanotube array films(ZNAF)prepared by anodic oxidation method were used as immobilization materials for acridine orange(AO),rhodamine B(RB)and AO-RB systems.A comparative study on their fluorescence emission intensity,fluorescence resonance energy transfer(FRET)and fluorescence detection of nitrite in aqueous solutions and on immobilization films with ZNAF as carriers was carried out.Results demonstrate that the solution pH values and immobilization on ZNAF have a great influence on the per-formance of these fluorescent molecules.Compared with aqueous solutions,the fluorescence emission in-tensity of AO and RB is considerably increased by immobilization,which is 8.0 and 4.2 times higher than the original,respectively.The energy transfer efficiency(E)of the AO-RB system increases from 40.9%to 84.8%by loading it on ZNAF.Moreover,after immobilization onto ZNAF,the fluorescence detection performance of nitrite is also significantly improved.The limit of detection decreases from 0.95 ng/mL to 0.22 ng/mL and the sensitivity increases from 939.18 to 15,031.68 mL/μg through loading AO onto ZNAF.展开更多
We have developed an on-line detection method using acridine orange as the fluorescence probe and applied this method to rapidly identify active compounds in herbal medicines. This on-line method was equipped with a h...We have developed an on-line detection method using acridine orange as the fluorescence probe and applied this method to rapidly identify active compounds in herbal medicines. This on-line method was equipped with a high-performance liquid chromatography tandem diode array detector, electrospray ionization-ion-trap time-of-flight mass spectrometry and DNA- acridine orange fluorescence detection （HPLC-DAD-MSn-DNA-AO-FLD）. A large amount of information could be simultaneously obtained during one run, which included HPLC fingerprint, ultraviolet spectra, total ion chromatograms, MSn data of high-resolution mass spectrometry and activity profile of each compound binding with DNA. The method also provided information on structureactivity relationships and mechanism of interaction. We used this on-line method to identify five DNA-binding activity components from Lithospermum erythrorhizon sample for the first time. The result showed that the parent nucleus of shikonin derivatives could bind with DNA. The structure-activity relationship showed that the parent nucleus of shikonin derivatives plays a major role in DNA binding, not the carboxyl group on the side chain. This simple, rapid, high precision and good stability on-line method should be useful for compound separation, structural identification and screening of DNA-binding compounds in herbal medicines.展开更多
Hydrogen has been deemed as one of the most efficient energy carriers for a broad variety of industrial applications[1,2].Large-scale,low-cost hydrogen production,safe storage and delivery represent a tremendous techn...Hydrogen has been deemed as one of the most efficient energy carriers for a broad variety of industrial applications[1,2].Large-scale,low-cost hydrogen production,safe storage and delivery represent a tremendous technological challenge and have become a subject of intense research and development activities in the past few decades[3–5].展开更多
Graphene/acridine （G-Acr） hybrid structures were synthesized through covalent functionalization of graphene oxide with 9-（4- aminophenyl）acridine （APA） and its derivatives. The G-Act hybrids were characterized b...Graphene/acridine （G-Acr） hybrid structures were synthesized through covalent functionalization of graphene oxide with 9-（4- aminophenyl）acridine （APA） and its derivatives. The G-Act hybrids were characterized by Fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometry, thermal gravimetric analysis and Raman spectroscopy. X-ray photoelectron spectroscopy confirms that the binding energies of APA and its derivatives shifted to higher values, revealing pronounced charge transfer at the interface of graphene and organic molecules.展开更多
Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of cancers.Discovery of new multi-target scaffolds are important for developing such agents. A series ...Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of cancers.Discovery of new multi-target scaffolds are important for developing such agents. A series of five novel acridine analogues,LXL 1-5,were synthesized and their antiproliferative activity against HepC-2 cell lines were evaluated,among which the 9-benzyloxyacridine analogue,LXL-5, showed inhibitory activity against tyrosine kinases,VEGFR-2 and Src.The results of UV-visible absorption spectra and fluorescence emission spectra,as well as DNA topoisomerase I inhibition assay, indicated topoisomerase I inhibitory activity.Our study suggested that acridine scaffold,previously shown to have no multi-target kinase and topoisomerase inhibitory activity,might be potentially developed as a multi-target inhibitor of tyrosine kinases and topoisomerase I.展开更多
Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and He...Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV-vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization.展开更多
1,4-Bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base were synthesized first.Using 1,4- bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base as the monomers,poly(aryl imino) ...1,4-Bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base were synthesized first.Using 1,4- bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base as the monomers,poly(aryl imino) containing acridine units(PAIA) was synthesized via palladium-catalyzed amination.The structure of PAIA was characterized by means of FTIR,~1H-NMR spectroscopy and elemental analysis,the results show an agreement with the proposed structure.The UV absorption and photoluminescence spectra were t...展开更多
The N-cyclopropyl-9-（3,4-dicholophenyl）- 1,2,3,4,5,6,7,8,9,10-decahydroacri- dine-1,8-dione was synthesized by the reaction of 1,3-cyclohexanedione, N-cyclopropylamine and 3,4-dicholoaldehyde in water and glycol und...The N-cyclopropyl-9-（3,4-dicholophenyl）- 1,2,3,4,5,6,7,8,9,10-decahydroacri- dine-1,8-dione was synthesized by the reaction of 1,3-cyclohexanedione, N-cyclopropylamine and 3,4-dicholoaldehyde in water and glycol under microwave irradiation. Its crystal structure was determined by single-crystal X-ray diffraction analysis. It possesses P212121 space group, with a = 9.9103（5）, b = 13.3597（8）, c = 14.5633（8）A, V= 1928.16（18）A3 ,Mr = 402.30, Z = 4, Dc= 1.386 g/cm^3, 2 = 0.7107A,μ（MoKα）=0.354mm^-1 and F （000） = 840. The structure was refined to R = 0.0280 and wR = 0.0757. In the structure, the pyridine ring adopts a boat conformation.展开更多
The emergence of multidrug-resistant bacteria creates an urgent need for alternative antibiotics with new mechanisms of action. In this study, we synthesized a novel type of antimicrobial agent, Ac r_3-NLS, by conjuga...The emergence of multidrug-resistant bacteria creates an urgent need for alternative antibiotics with new mechanisms of action. In this study, we synthesized a novel type of antimicrobial agent, Ac r_3-NLS, by conjugating hydrophobic acridines to the N-terminus of a nuclear localization sequence(NLS), a short cationic peptide. To further improve the antimicrobial activity of our agent, dimeric(Acr_3-NLS)_2 was simultaneously synthesized by joining two monomeric Acr_3-NLS together via a disulfide linker. Our results show that Acr_3-NLS and especially(Acr_3-NLS)_2 display signifi cant antimicrobial activity against gramnegative and gram-positive bacteria compared to that of the NLS. Subsequently, the results derived from the study on the mechanism of action demonstrate that Acr_3-NLS and(Acr_3-NLS)_2 can kill bacteria by membrane disruption and DNA binding. The double targets—cell membrane and intracellular DNA—will reduce the risk of bacteria developing resistance to Acr_3-NLS and(Acr_3-NLS)_2. Overall, this study provides a novel strategy to design highly eff ective antimicrobial agents with a dual mode of action for infection treatment.展开更多
The crystal structure N-methyl-9-(4-bromophenyl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10- decahydroacridine(C20H20BrNO2) was determined by single-crystal X-ray diffraction analysis. It belongs to P21/n space group, with a = ...The crystal structure N-methyl-9-(4-bromophenyl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10- decahydroacridine(C20H20BrNO2) was determined by single-crystal X-ray diffraction analysis. It belongs to P21/n space group, with a = 10.7999(18), b = 13.845(3), c = 11.4031(3) ?, β = 99.324(4)°, Dc = 1.525 g/cm3, Z = 4, λ = 0.71070 ?, μ(MoKα) = 2.455 mm-1, Mr = 386.28, V = 1682.5(5) ?3, F(000) = 792, the final R = 0.0463 and wR = 0.1053. In the crystal structure, the pyridine ring adopts a boat conformation, the two six-numbered rings fused with pyridine ring adopt twisting boat con- formation.展开更多
In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells p...In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells proliferation.In addition,all the compounds displayed Topo Ⅱ inhibition activity at 10 mol/L,and also possessed good PARP-1 inhibitory activities.Subsequent mechanistic studies showed that compound 9 a induced remarkable apoptosis and caused prominent S cell cycle arrest in HCT116 cells.Our study suggested that 9 a inhibiting Topo and PARP concurrently can be a potential lead compound for cancer therapy.展开更多
The crystal structure of the title compound (C26H33NO4 (C25.68H32.04N0.68O4.32, Mr = 419.35)) has been determined by single-crystal X-ray diffraction. The crystal is of triclinic, space P21/c with a = 7.519(2), b = ...The crystal structure of the title compound (C26H33NO4 (C25.68H32.04N0.68O4.32, Mr = 419.35)) has been determined by single-crystal X-ray diffraction. The crystal is of triclinic, space P21/c with a = 7.519(2), b = 28.933(5), c = 10.654(3) ?, β = 91.78(2)°, V = 2316.7(7) ?3, Z = 4, Dc = 1.202 g/cm3, μ = 0.081 mm-1, F(000) = 902, Mr = 423, the final R = 0.0424 and wR = 0.0911. In the structure, the pyridine ring adopts a boat conformation.展开更多
A novel fluorescent probe 9-（4-（1,2-diamine）benzene-N1-phenyl）acridine（DABPA） was synthesized for the detection of nitric oxide（NO） and characterized by IR, 1H-NMR and EI-MS spectroscopy. Based on a photoelect...A novel fluorescent probe 9-（4-（1,2-diamine）benzene-N1-phenyl）acridine（DABPA） was synthesized for the detection of nitric oxide（NO） and characterized by IR, 1H-NMR and EI-MS spectroscopy. Based on a photoelectron transfer mechanism, the fl uorescence intensities of DABPA were investigated with the different concentrations of NO. Under the optimal experimental conditions, the fl uorescence intensity of DABPA had a good linear relationship（R2=0.9977） with NO concentration in the range from 1×10-7 to 1.5×10-6 mol/L with a detection limit of 1×10-8 mol/L. The cytotoxicity induced by DABPA was evaluated by the MTT（3-（4,5-dimethylthiazol-2-yl）-2,5diphenyl tetrazolium bromide） assay for biological application. Furthermore, the probe DABPA had also been successfully applied to real-time image NO produced in PC12 cells in the presence of L-arginine.展开更多
In this work, noncovalent functionalization of multiwalled carbon nanotube （MWNT） with acridine orange （AO） by electropolymerization is studied. The obtained composite film is a viable alternate electrode material...In this work, noncovalent functionalization of multiwalled carbon nanotube （MWNT） with acridine orange （AO） by electropolymerization is studied. The obtained composite film is a viable alternate electrode material, non-toxic, chemical inert, not volatile, using to construct modified electrode. The new type modified electrode has both of unique properties of MWNT and poly acridine orange （POAO）, can provide good sensitivity, low limits of detection, good response precision, and superb response stability.展开更多
Flower shaped antimony oxide (Sb2O3) microstructures were synthesized in a large quantity via simple solution method using aqueous mixtures of antimony chloride and hexamethylene diamine (HMDA). The morphological char...Flower shaped antimony oxide (Sb2O3) microstructures were synthesized in a large quantity via simple solution method using aqueous mixtures of antimony chloride and hexamethylene diamine (HMDA). The morphological characterizations were done by field emission scanning electron microscopy (FESEM), which revealed that the synthesized products possess flower-shaped microstructures. The detailed structural characterizations performed by X-ray diffraction (XRD), Fourier transform infrared spectrophotometer (FT-IR) and Raman spectrophotometer confirmed that the synthesized microstructures are well-crystalline antimony oxide. The Energy dispersive spectroscopy (EDS) shows that the grown products are composed of Sb and O. Optical properties of the synthesized products were characterized by UV-Visible spectrophotometer which exhibits a well defined peak at ~ 291.0 nm. The photo-catalytic activity of the Sb2O3 microstructures was evaluated by degradation of acridine orange (AO), which mineralized almost 63.0% in 150 min. The chemical sensing properties of Sb2O3 microstructures was also studied by I-V technique using chloroform as a detecting solvent. The fabricated chloroform sensor demonstrates good sensitivity of 0.1154 μA cm–2 mM–1, lower-detection limit (~0.1 mM), large-linear dynamic range (LDR, 0.122 mM to 1.22 M) with linearity (R = 0.7898) in short response time (10.0 sec).展开更多
The surface enhanced fluorescence effect of acridine orange fluorophore in the proximity of Au nanoparticles has been investigated experimentally in the system of aqueous solution.Significant enhancement of the fluore...The surface enhanced fluorescence effect of acridine orange fluorophore in the proximity of Au nanoparticles has been investigated experimentally in the system of aqueous solution.Significant enhancement of the fluorescence intensity was observed when the system was excited with 532 nm or 442 nm CW lasers.The influence of the distances between neighboring Au particles as well as that between the fluorophore molecules and the Au surface were explored experimentally.The results demonstrated that a compact distribution of metallic particles was able to produce stronger fluorescence enhancement.Proper separation between the fluorophore molecules and the metal surface was favorable for a better enhancement.展开更多
Insights into the pharmacologic effect on cellular processes and the potential toxicological effects are vital to new drug development and evaluation,yet research on these subjects remains a great challenge due to the...Insights into the pharmacologic effect on cellular processes and the potential toxicological effects are vital to new drug development and evaluation,yet research on these subjects remains a great challenge due to the lack of information regarding the spatiotemporal distribution of drugs and metabolites within a single cell.Mass spectrometry imaging(MSI)has proven to be a label-free and high-throughput approach for visualizing drug distribution in spatial and temporal domains.However,single-cell drug imaging has been limited so far by detection sensitivity and microscale lateral resolution.Herein,we report near-field laser desorption/laser postionization mass spectrometry(NDPI-MS)for single-cell imaging of two structurally similar drugs,proflavine and ethacridine,and subcellular distributions of proflavine at different drug concentrations were investigated.The NDPI-MS imaging results indicate that proflavine was accumulated in lysosomes,which was verified by laser scanning confocal microscopy(LSCM).Additionally,a distinguished subcellular distribution pattern of ethacridine from proflavine could be visualized,highlighting the complexity of the interaction between the drugs and biological environment even though these two drugs possess similar structures.Taken together,the present results demonstrate the great potential of the integrated single-cell MSI platform for characterizing the drug distribution and its phenotype changes within individual cells,expediting the identification and evaluation of newly developed drugs.展开更多
A simple and sensitive method for detection of captopril was established based on its obstructive effect on nanomaterial sur- face energy transfer （NSET）. It was found that the acridine orange （AO） could be adsorb...A simple and sensitive method for detection of captopril was established based on its obstructive effect on nanomaterial sur- face energy transfer （NSET）. It was found that the acridine orange （AO） could be adsorbed onto the surface of citrated-gold nanoparticles （AuNPs） through electrostatic interaction. Incidentally, the fluorescence of AO was quenched owing to the dipole-dipole interaction of NSET between AO fluorophore and the AuNPs. However, captopril could obstruct the occurrence of NSET between AO and AuNPs effectively with the formation of Au-S covalent bonds between it and the AuNPs. Consequently, AO molecules were moved away from the surface of AuNPs leading to a decline of the energy transfer efficiency. Moreover, the fluorescence of AO could be gradually restored with the addition of captopril. Under the optimal conditions, the recovered fluorescence intensity correlated linearly with the concentration of captopril in the range of 400 nmol/L-2.0μmol/L with a detection limit of 71 μmol/L. Besides, the proposed method was successfully applied for the detection of captopril in troches with the recovery of 93%-102% and the RSD lower than 2.24%. The results were in good agreement with those obtained from the HPLC method,展开更多
A new photocatalyst, TiO_2 powder immobilized on polystyrene (PS) thin films,was prepared using a novel method and its photocatalytic activity on the photodegradation ofacridine dye in aqueous solution was tested. By ...A new photocatalyst, TiO_2 powder immobilized on polystyrene (PS) thin films,was prepared using a novel method and its photocatalytic activity on the photodegradation ofacridine dye in aqueous solution was tested. By this method, the crystal form and grain size of theimmobilized TiO_2 were well maintained. Compared with TiO_2 powder, the photocatalytic activity ofTiO_2/PS thin films was not significantly reduced. The catalyst is stable and can be reused severaltimes without the loss of activity, which makes wastewater treatment using this photocatalyticdegradation technique of this way possible in the practical application.展开更多
基金supported by the National Natural Science Foundation of China(No.51972095).
文摘Zirconia nanotube array films(ZNAF)prepared by anodic oxidation method were used as immobilization materials for acridine orange(AO),rhodamine B(RB)and AO-RB systems.A comparative study on their fluorescence emission intensity,fluorescence resonance energy transfer(FRET)and fluorescence detection of nitrite in aqueous solutions and on immobilization films with ZNAF as carriers was carried out.Results demonstrate that the solution pH values and immobilization on ZNAF have a great influence on the per-formance of these fluorescent molecules.Compared with aqueous solutions,the fluorescence emission in-tensity of AO and RB is considerably increased by immobilization,which is 8.0 and 4.2 times higher than the original,respectively.The energy transfer efficiency(E)of the AO-RB system increases from 40.9%to 84.8%by loading it on ZNAF.Moreover,after immobilization onto ZNAF,the fluorescence detection performance of nitrite is also significantly improved.The limit of detection decreases from 0.95 ng/mL to 0.22 ng/mL and the sensitivity increases from 939.18 to 15,031.68 mL/μg through loading AO onto ZNAF.
基金Peking University Comprehensive Platform for Innovative Drug Research and Development(Grant No.2009ZX--09301--010)
文摘We have developed an on-line detection method using acridine orange as the fluorescence probe and applied this method to rapidly identify active compounds in herbal medicines. This on-line method was equipped with a high-performance liquid chromatography tandem diode array detector, electrospray ionization-ion-trap time-of-flight mass spectrometry and DNA- acridine orange fluorescence detection （HPLC-DAD-MSn-DNA-AO-FLD）. A large amount of information could be simultaneously obtained during one run, which included HPLC fingerprint, ultraviolet spectra, total ion chromatograms, MSn data of high-resolution mass spectrometry and activity profile of each compound binding with DNA. The method also provided information on structureactivity relationships and mechanism of interaction. We used this on-line method to identify five DNA-binding activity components from Lithospermum erythrorhizon sample for the first time. The result showed that the parent nucleus of shikonin derivatives could bind with DNA. The structure-activity relationship showed that the parent nucleus of shikonin derivatives plays a major role in DNA binding, not the carboxyl group on the side chain. This simple, rapid, high precision and good stability on-line method should be useful for compound separation, structural identification and screening of DNA-binding compounds in herbal medicines.
基金the financial support from the National Natural Science Foundation of China(Nos.21473164,21603195 and 21875225)Major project of Technical Innovation of Hubei Province(No.2017AAA126)the Fundamental Research Funds for Central Universities,China University of Geosciences(Wuhan)(Nos.CUGL170405 and CUG180604)。
文摘Hydrogen has been deemed as one of the most efficient energy carriers for a broad variety of industrial applications[1,2].Large-scale,low-cost hydrogen production,safe storage and delivery represent a tremendous technological challenge and have become a subject of intense research and development activities in the past few decades[3–5].
基金the financial support from the National Natural Science Foundation of China(Nos.21072040,21071040, 21101051 and 21272050)the Program for New Century Excellent Talents in University of the Chinese Ministry of Education(No.NCET-11-0627)
文摘Graphene/acridine （G-Acr） hybrid structures were synthesized through covalent functionalization of graphene oxide with 9-（4- aminophenyl）acridine （APA） and its derivatives. The G-Act hybrids were characterized by Fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometry, thermal gravimetric analysis and Raman spectroscopy. X-ray photoelectron spectroscopy confirms that the binding energies of APA and its derivatives shifted to higher values, revealing pronounced charge transfer at the interface of graphene and organic molecules.
基金supports from the Ministry of Science and Technology of China(Nos. 2012ZX09506001-010,2012AA020305 and 2011DFA30620)the National Natural Science Foundation of China(Nos.21272134 and 20902053)Shenzhen Sci & Tech Bureau(No. JCYJ20120831165730905)
文摘Multi-target agents against tyrosine kinases and topoisomerases are potentially useful for the effective treatment of cancers.Discovery of new multi-target scaffolds are important for developing such agents. A series of five novel acridine analogues,LXL 1-5,were synthesized and their antiproliferative activity against HepC-2 cell lines were evaluated,among which the 9-benzyloxyacridine analogue,LXL-5, showed inhibitory activity against tyrosine kinases,VEGFR-2 and Src.The results of UV-visible absorption spectra and fluorescence emission spectra,as well as DNA topoisomerase I inhibition assay, indicated topoisomerase I inhibitory activity.Our study suggested that acridine scaffold,previously shown to have no multi-target kinase and topoisomerase inhibitory activity,might be potentially developed as a multi-target inhibitor of tyrosine kinases and topoisomerase I.
基金the Ministry of Science and Technology of the People’s Republic of China(Nos.2012AA020305and 2011DFA30620)the National Natural Science Foundation of China(Nos.21272134 and 21372141)Shenzhen Sci.&Tech.Bureau(No.JCYJ20120831165730905)for the financial supports
文摘Novel DNA binding agents against topoisomerases are needed for effective treatment of cancers. A series of new acridine-based derivatives 7a-7d were synthesized and their antiproliferative activity against K562 and HepG-2 cell lines were evaluated. Compound 7c with pyridin-2-yl-methanamino group substituted at the C9 position of acridine showed good antitumor activity against both cell lines. The DNA-binding affinity of compound 7c was evaluated by UV-vis absorption spectra and fluorescence emission spectra. DNA topoisomerase I mediated relaxation of plasmid pBR322 DNA was also tested. Our results suggested that compound 7c with good antitumor activity and topoisomerase I inhibition activity can be developed as a prime candidate for further chemical optimization.
基金supported by the Foundation of National Key Laboratory of High Temperature and Density Plasma Physics(No.9140C6806030807)the Science and Technology Development Foundation of China Academy of Physics Engineering(No.200708006)
文摘1,4-Bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base were synthesized first.Using 1,4- bis-(4-bromobenzoyl)benzene and proflavine,3,6-diaminoacridine free base as the monomers,poly(aryl imino) containing acridine units(PAIA) was synthesized via palladium-catalyzed amination.The structure of PAIA was characterized by means of FTIR,~1H-NMR spectroscopy and elemental analysis,the results show an agreement with the proposed structure.The UV absorption and photoluminescence spectra were t...
基金This work was supported by the National Natural Science Foundation of China (No. 20372057), the Natural Science Foundation of the Jiangsu Province (No. BK2001142), the Suzhou University Organic Syntheses Open Laboratory of Jiangsu Province (No. S8109111) and the Key Lab of Biotechnology for Medicinal Plants of Jiangsu Province (No. 01AXL 14)
文摘The N-cyclopropyl-9-（3,4-dicholophenyl）- 1,2,3,4,5,6,7,8,9,10-decahydroacri- dine-1,8-dione was synthesized by the reaction of 1,3-cyclohexanedione, N-cyclopropylamine and 3,4-dicholoaldehyde in water and glycol under microwave irradiation. Its crystal structure was determined by single-crystal X-ray diffraction analysis. It possesses P212121 space group, with a = 9.9103（5）, b = 13.3597（8）, c = 14.5633（8）A, V= 1928.16（18）A3 ,Mr = 402.30, Z = 4, Dc= 1.386 g/cm^3, 2 = 0.7107A,μ（MoKα）=0.354mm^-1 and F （000） = 840. The structure was refined to R = 0.0280 and wR = 0.0757. In the structure, the pyridine ring adopts a boat conformation.
基金the grants from the National Natural Science Foundation of China (81402776 and 81202400)the Key National S&T Progra m "Major New Drug Development" of the Ministry of Science and Technology of China (2012ZX09504001-003)+2 种基金the Fundamental Research Funds for the Central Universities (lzujbky-2014-142 and lzujbky-2015-169)the Specialized Research Fund for the Doctoral Program of Higher Education of China (20130211130005)China Postdoctoral Science Foundation (2013T60896)
文摘The emergence of multidrug-resistant bacteria creates an urgent need for alternative antibiotics with new mechanisms of action. In this study, we synthesized a novel type of antimicrobial agent, Ac r_3-NLS, by conjugating hydrophobic acridines to the N-terminus of a nuclear localization sequence(NLS), a short cationic peptide. To further improve the antimicrobial activity of our agent, dimeric(Acr_3-NLS)_2 was simultaneously synthesized by joining two monomeric Acr_3-NLS together via a disulfide linker. Our results show that Acr_3-NLS and especially(Acr_3-NLS)_2 display signifi cant antimicrobial activity against gramnegative and gram-positive bacteria compared to that of the NLS. Subsequently, the results derived from the study on the mechanism of action demonstrate that Acr_3-NLS and(Acr_3-NLS)_2 can kill bacteria by membrane disruption and DNA binding. The double targets—cell membrane and intracellular DNA—will reduce the risk of bacteria developing resistance to Acr_3-NLS and(Acr_3-NLS)_2. Overall, this study provides a novel strategy to design highly eff ective antimicrobial agents with a dual mode of action for infection treatment.
基金This work was supported by the National Natural Science Foundation of China (No. 20372057) Natural Science Foundation of Jiangsu Province (No. BK2001142) the Suzhou University Organic Synthesis Open Laboratory of Jiangsu Province (No. S81091 11) and the Key Lab of Biotechnology for Medicinal Plants of Jiangsu Province (No. 01AXL 14)
文摘The crystal structure N-methyl-9-(4-bromophenyl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10- decahydroacridine(C20H20BrNO2) was determined by single-crystal X-ray diffraction analysis. It belongs to P21/n space group, with a = 10.7999(18), b = 13.845(3), c = 11.4031(3) ?, β = 99.324(4)°, Dc = 1.525 g/cm3, Z = 4, λ = 0.71070 ?, μ(MoKα) = 2.455 mm-1, Mr = 386.28, V = 1682.5(5) ?3, F(000) = 792, the final R = 0.0463 and wR = 0.1053. In the crystal structure, the pyridine ring adopts a boat conformation, the two six-numbered rings fused with pyridine ring adopt twisting boat con- formation.
基金financial supports from the Shenzhen Development and Reform Committee(Nos.20151961 and 2019156)Department of Science and Technology of Guangdong Province(No.2017B030314083)。
文摘In this study,we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors.MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells proliferation.In addition,all the compounds displayed Topo Ⅱ inhibition activity at 10 mol/L,and also possessed good PARP-1 inhibitory activities.Subsequent mechanistic studies showed that compound 9 a induced remarkable apoptosis and caused prominent S cell cycle arrest in HCT116 cells.Our study suggested that 9 a inhibiting Topo and PARP concurrently can be a potential lead compound for cancer therapy.
基金The project was supported by the National Natural Science Foundation of China (No. 20372057) Natural Science Foundation+4 种基金 of Jiangsu Province (No. BK.2001142) the Open-end Fund of the Key Experiments of Organic Synthesis Jiangsu Province (S8109111) the Fund of Jiangsu Provincial Key Lab of Biotechnology for Medicinal Plants (01AXL 14)
文摘The crystal structure of the title compound (C26H33NO4 (C25.68H32.04N0.68O4.32, Mr = 419.35)) has been determined by single-crystal X-ray diffraction. The crystal is of triclinic, space P21/c with a = 7.519(2), b = 28.933(5), c = 10.654(3) ?, β = 91.78(2)°, V = 2316.7(7) ?3, Z = 4, Dc = 1.202 g/cm3, μ = 0.081 mm-1, F(000) = 902, Mr = 423, the final R = 0.0424 and wR = 0.0911. In the structure, the pyridine ring adopts a boat conformation.
基金Funded by the National Natural Science Foundation of China(Nos.50802069,81100890,51272191)the Fundamental Research Funds for the Central Unversities(WUT:2013-IV-010)the Students Innovation and Entrepreneurship Training Program of WHUT(20141049701012)
文摘A novel fluorescent probe 9-（4-（1,2-diamine）benzene-N1-phenyl）acridine（DABPA） was synthesized for the detection of nitric oxide（NO） and characterized by IR, 1H-NMR and EI-MS spectroscopy. Based on a photoelectron transfer mechanism, the fl uorescence intensities of DABPA were investigated with the different concentrations of NO. Under the optimal experimental conditions, the fl uorescence intensity of DABPA had a good linear relationship（R2=0.9977） with NO concentration in the range from 1×10-7 to 1.5×10-6 mol/L with a detection limit of 1×10-8 mol/L. The cytotoxicity induced by DABPA was evaluated by the MTT（3-（4,5-dimethylthiazol-2-yl）-2,5diphenyl tetrazolium bromide） assay for biological application. Furthermore, the probe DABPA had also been successfully applied to real-time image NO produced in PC12 cells in the presence of L-arginine.
文摘In this work, noncovalent functionalization of multiwalled carbon nanotube （MWNT） with acridine orange （AO） by electropolymerization is studied. The obtained composite film is a viable alternate electrode material, non-toxic, chemical inert, not volatile, using to construct modified electrode. The new type modified electrode has both of unique properties of MWNT and poly acridine orange （POAO）, can provide good sensitivity, low limits of detection, good response precision, and superb response stability.
文摘Flower shaped antimony oxide (Sb2O3) microstructures were synthesized in a large quantity via simple solution method using aqueous mixtures of antimony chloride and hexamethylene diamine (HMDA). The morphological characterizations were done by field emission scanning electron microscopy (FESEM), which revealed that the synthesized products possess flower-shaped microstructures. The detailed structural characterizations performed by X-ray diffraction (XRD), Fourier transform infrared spectrophotometer (FT-IR) and Raman spectrophotometer confirmed that the synthesized microstructures are well-crystalline antimony oxide. The Energy dispersive spectroscopy (EDS) shows that the grown products are composed of Sb and O. Optical properties of the synthesized products were characterized by UV-Visible spectrophotometer which exhibits a well defined peak at ~ 291.0 nm. The photo-catalytic activity of the Sb2O3 microstructures was evaluated by degradation of acridine orange (AO), which mineralized almost 63.0% in 150 min. The chemical sensing properties of Sb2O3 microstructures was also studied by I-V technique using chloroform as a detecting solvent. The fabricated chloroform sensor demonstrates good sensitivity of 0.1154 μA cm–2 mM–1, lower-detection limit (~0.1 mM), large-linear dynamic range (LDR, 0.122 mM to 1.22 M) with linearity (R = 0.7898) in short response time (10.0 sec).
基金supported by the Foundation for the Key Project of the Chinese Ministry of Education (Grant No. 108118)the Fundamental Research Funds for the Central Universities (Grant No. GK200901022)
文摘The surface enhanced fluorescence effect of acridine orange fluorophore in the proximity of Au nanoparticles has been investigated experimentally in the system of aqueous solution.Significant enhancement of the fluorescence intensity was observed when the system was excited with 532 nm or 442 nm CW lasers.The influence of the distances between neighboring Au particles as well as that between the fluorophore molecules and the Au surface were explored experimentally.The results demonstrated that a compact distribution of metallic particles was able to produce stronger fluorescence enhancement.Proper separation between the fluorophore molecules and the metal surface was favorable for a better enhancement.
基金The authors are grateful for the national support received from the National Natural Science Foundation of China(Nos.21974116 and 21427813).
文摘Insights into the pharmacologic effect on cellular processes and the potential toxicological effects are vital to new drug development and evaluation,yet research on these subjects remains a great challenge due to the lack of information regarding the spatiotemporal distribution of drugs and metabolites within a single cell.Mass spectrometry imaging(MSI)has proven to be a label-free and high-throughput approach for visualizing drug distribution in spatial and temporal domains.However,single-cell drug imaging has been limited so far by detection sensitivity and microscale lateral resolution.Herein,we report near-field laser desorption/laser postionization mass spectrometry(NDPI-MS)for single-cell imaging of two structurally similar drugs,proflavine and ethacridine,and subcellular distributions of proflavine at different drug concentrations were investigated.The NDPI-MS imaging results indicate that proflavine was accumulated in lysosomes,which was verified by laser scanning confocal microscopy(LSCM).Additionally,a distinguished subcellular distribution pattern of ethacridine from proflavine could be visualized,highlighting the complexity of the interaction between the drugs and biological environment even though these two drugs possess similar structures.Taken together,the present results demonstrate the great potential of the integrated single-cell MSI platform for characterizing the drug distribution and its phenotype changes within individual cells,expediting the identification and evaluation of newly developed drugs.
基金the National Natural Science Foundation of China(21175109)the special fund of Chongqing key laboratory(CSTC)for financial assistance
文摘A simple and sensitive method for detection of captopril was established based on its obstructive effect on nanomaterial sur- face energy transfer （NSET）. It was found that the acridine orange （AO） could be adsorbed onto the surface of citrated-gold nanoparticles （AuNPs） through electrostatic interaction. Incidentally, the fluorescence of AO was quenched owing to the dipole-dipole interaction of NSET between AO fluorophore and the AuNPs. However, captopril could obstruct the occurrence of NSET between AO and AuNPs effectively with the formation of Au-S covalent bonds between it and the AuNPs. Consequently, AO molecules were moved away from the surface of AuNPs leading to a decline of the energy transfer efficiency. Moreover, the fluorescence of AO could be gradually restored with the addition of captopril. Under the optimal conditions, the recovered fluorescence intensity correlated linearly with the concentration of captopril in the range of 400 nmol/L-2.0μmol/L with a detection limit of 71 μmol/L. Besides, the proposed method was successfully applied for the detection of captopril in troches with the recovery of 93%-102% and the RSD lower than 2.24%. The results were in good agreement with those obtained from the HPLC method,
基金This project is financially supported by the Natural Science Foundation of China (QT program)
文摘A new photocatalyst, TiO_2 powder immobilized on polystyrene (PS) thin films,was prepared using a novel method and its photocatalytic activity on the photodegradation ofacridine dye in aqueous solution was tested. By this method, the crystal form and grain size of theimmobilized TiO_2 were well maintained. Compared with TiO_2 powder, the photocatalytic activity ofTiO_2/PS thin films was not significantly reduced. The catalyst is stable and can be reused severaltimes without the loss of activity, which makes wastewater treatment using this photocatalyticdegradation technique of this way possible in the practical application.
