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
Objective To observe the ability of triple helix-forming oligonucleotides (TFOs) modified with manganese porphyrin to combine with and cleave HBV DNA fractions. Methods TFO were modified with manganese porphyrin and...Objective To observe the ability of triple helix-forming oligonucleotides (TFOs) modified with manganese porphyrin to combine with and cleave HBV DNA fractions. Methods TFO were modified with manganese porphyrin and acridines,and then reacted with the 32 P labeled HBV DNA fragments at 37℃ in vitro (pH 7.4). Electrophoretic mobility shift assays and DNase Ⅰ footprinting tests were used to show the affinity and specificity of TFO to bind to target sequences. The ability of TFO to cleave HBV DNA fragments was tested by cleavage experiments. Results TFO modified with manganese porphyrin and acridine could bind to the target sequence in a sequence-dependent manner,with a Kd value of 3.5×10 -7 mol/L and a relative affinity of 0.008. In the presence of potassium monopersulfate (KHSO 5),TFO modified with manganese porphyrin and acridine could cleave the target sequence where the triplex DNA was formed. Conclusion In the presence of KHSO 5,TFO modified with manganese porphyrin and acridine could bind and cleave the target HBV-DNA in a sequence-dependent manner.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
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
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
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
Objective To estimate the predictive value of double fluorescence [acridine orange （AO）/propidium iodide （PI）] staining results for fertilization rate and clinical outcomes and analyze the correlation between th...Objective To estimate the predictive value of double fluorescence [acridine orange （AO）/propidium iodide （PI）] staining results for fertilization rate and clinical outcomes and analyze the correlation between the results of AO/P1 staining and sperm apoptosis. Methods A prospective study was carried out, 235 infertile couples remedied using traditional in vitro fertilization （IVF） were included. Semen collected from 235 patients were stained by fluorescence dye, AO and PL at the same time the spermatozoa apoptosis rate was calculated by using flow cytometry to detect the rate of Annexin V＋/ PI- . The result of fluorescence was divided into 3 groups as green （G）, yellow （Y） and red （R） according to the color of fluorescence. The correlation between the percent of the 3 colors and clinical outcomes and spermatozoa apoptosis rate was evaluated. Results Significant negative correlation was observed between the percentage of Y and fertilization rate （r= -0.42, P=0.04）, no significant correlation was observed between the percentage of G, R and fertilization rate. The percentage of G, Y, R was not significantly different between pregnant patients and non-pregnant patients, respectiw,ly, while the percentage of Y was significant different between miscarriage patients and liveborn patients （r=0.6L P=0.01） and no significant difference exist in the percentage of G and R between liveborn patients and miscarriage patients. There was a significant positive correlation between the percentage of Y and the rate of Annexin V＋/ PI （r=0.53, P=0.04）, and no significant correlation was shown between the percentage of G, R and the rate of Annexin V＋/ PI-.Conclusion The percentage of yellow group of double fluorescence （AO/PI） staining will affect the fertilization rate and the miscarriage rate, and this group of spermatozoa may be connected with the spermatozoa apoptosis.展开更多
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ThisstudywassupportedbyagrantfromtheNationalNaturalScienceFoundationofChina (No 3 980 0 12 8)
文摘Objective To observe the ability of triple helix-forming oligonucleotides (TFOs) modified with manganese porphyrin to combine with and cleave HBV DNA fractions. Methods TFO were modified with manganese porphyrin and acridines,and then reacted with the 32 P labeled HBV DNA fragments at 37℃ in vitro (pH 7.4). Electrophoretic mobility shift assays and DNase Ⅰ footprinting tests were used to show the affinity and specificity of TFO to bind to target sequences. The ability of TFO to cleave HBV DNA fragments was tested by cleavage experiments. Results TFO modified with manganese porphyrin and acridine could bind to the target sequence in a sequence-dependent manner,with a Kd value of 3.5×10 -7 mol/L and a relative affinity of 0.008. In the presence of potassium monopersulfate (KHSO 5),TFO modified with manganese porphyrin and acridine could cleave the target sequence where the triplex DNA was formed. Conclusion In the presence of KHSO 5,TFO modified with manganese porphyrin and acridine could bind and cleave the target HBV-DNA in a sequence-dependent manner.
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.
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 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 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supported by a grant from STCSM (Subject No.:074207002)
文摘Objective To estimate the predictive value of double fluorescence [acridine orange （AO）/propidium iodide （PI）] staining results for fertilization rate and clinical outcomes and analyze the correlation between the results of AO/P1 staining and sperm apoptosis. Methods A prospective study was carried out, 235 infertile couples remedied using traditional in vitro fertilization （IVF） were included. Semen collected from 235 patients were stained by fluorescence dye, AO and PL at the same time the spermatozoa apoptosis rate was calculated by using flow cytometry to detect the rate of Annexin V＋/ PI- . The result of fluorescence was divided into 3 groups as green （G）, yellow （Y） and red （R） according to the color of fluorescence. The correlation between the percent of the 3 colors and clinical outcomes and spermatozoa apoptosis rate was evaluated. Results Significant negative correlation was observed between the percentage of Y and fertilization rate （r= -0.42, P=0.04）, no significant correlation was observed between the percentage of G, R and fertilization rate. The percentage of G, Y, R was not significantly different between pregnant patients and non-pregnant patients, respectiw,ly, while the percentage of Y was significant different between miscarriage patients and liveborn patients （r=0.6L P=0.01） and no significant difference exist in the percentage of G and R between liveborn patients and miscarriage patients. There was a significant positive correlation between the percentage of Y and the rate of Annexin V＋/ PI （r=0.53, P=0.04）, and no significant correlation was shown between the percentage of G, R and the rate of Annexin V＋/ PI-.Conclusion The percentage of yellow group of double fluorescence （AO/PI） staining will affect the fertilization rate and the miscarriage rate, and this group of spermatozoa may be connected with the spermatozoa apoptosis.
