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2017 Volume 80 Issue 10
2017, 80(10): 891-899
Abstract:
Over the last decades, remarkable progress has been made in the field of drug delivery in tumor.But, tumor therapy is still a tough nut to crack.However, in spite of significant advances to tumor targeting, an effective treatment strategy for malignant tumors still remains elusive.The research focus gradually shifted from the aggregation of carriers in the tumor to precise targeting and deep tumor penetration.How to overcome all obstacles to achieve its uniform distribution in the entire tumor tissue, to achieve an effective anti-tumor drug concentration are payed particular attention.In this paper, the mechanism of tumor tissue penetration were introduced, the effects of particles size, Zeta potential, particles shape, structure and chemical composition on tumor tissue penetration were discussed, and methods for assessing tumor tissue permeability were presented.The future research direction of this field was also prospected.
Over the last decades, remarkable progress has been made in the field of drug delivery in tumor.But, tumor therapy is still a tough nut to crack.However, in spite of significant advances to tumor targeting, an effective treatment strategy for malignant tumors still remains elusive.The research focus gradually shifted from the aggregation of carriers in the tumor to precise targeting and deep tumor penetration.How to overcome all obstacles to achieve its uniform distribution in the entire tumor tissue, to achieve an effective anti-tumor drug concentration are payed particular attention.In this paper, the mechanism of tumor tissue penetration were introduced, the effects of particles size, Zeta potential, particles shape, structure and chemical composition on tumor tissue penetration were discussed, and methods for assessing tumor tissue permeability were presented.The future research direction of this field was also prospected.
2017, 80(10): 900-907
Abstract:
Human Hand, Foot and Mouth Disease (HFMD) has always outbroken frequently and extensively in Southeast Asia, especially in China.Coxasckie virus A16 and Enterovirus 71 are the major pathogens to cause HFMD.EV71 is the main pathogen which caused HFMD in our country currently, it could lead to mild to severe clinical symptoms, and even to death.Approved inactivated vaccine for prevention of EV71 has been available recently, however it could not prevent all HFMD, and there is also a certain degree of risk when the vaccine is used.Only some commonly used broad-spectrum antiviral drugs could be applied for the treatment of HFMD in clinical at present.This review focus on the progress in drug syntheses of small molecule inhibitors of HFMD caused by EV71, and provides the reference for the development of effective therapeutic drugs for HFMD.
Human Hand, Foot and Mouth Disease (HFMD) has always outbroken frequently and extensively in Southeast Asia, especially in China.Coxasckie virus A16 and Enterovirus 71 are the major pathogens to cause HFMD.EV71 is the main pathogen which caused HFMD in our country currently, it could lead to mild to severe clinical symptoms, and even to death.Approved inactivated vaccine for prevention of EV71 has been available recently, however it could not prevent all HFMD, and there is also a certain degree of risk when the vaccine is used.Only some commonly used broad-spectrum antiviral drugs could be applied for the treatment of HFMD in clinical at present.This review focus on the progress in drug syntheses of small molecule inhibitors of HFMD caused by EV71, and provides the reference for the development of effective therapeutic drugs for HFMD.
2017, 80(10): 908-917
Abstract:
The broad spectrum of biological activity of sulfone compounds endows a wide applications in chemistry, medicine, agrochemistry and material science.Being an strong electron-withdrawing group, elongation of carbon chain could easily achieved via reaction of aliphatic sulfones with various electrophiles under basic condition.As a result, novel synthetic methodologies have continuous been developed especially during the past decades.This paper aimed at summarizing the synthetic methods of the sulfone compounds appeared in recent years, emphasizing the oxidation of sulfides, sulfonylation with sulfonyl chlorides and coupling of sulfinic acid salts.
The broad spectrum of biological activity of sulfone compounds endows a wide applications in chemistry, medicine, agrochemistry and material science.Being an strong electron-withdrawing group, elongation of carbon chain could easily achieved via reaction of aliphatic sulfones with various electrophiles under basic condition.As a result, novel synthetic methodologies have continuous been developed especially during the past decades.This paper aimed at summarizing the synthetic methods of the sulfone compounds appeared in recent years, emphasizing the oxidation of sulfides, sulfonylation with sulfonyl chlorides and coupling of sulfinic acid salts.
2017, 80(10): 918-924
Abstract:
Surfactin belongs to biosurfactant.It is a series of cyclic lipopeptides with similar basic structures produced by fermentation of Bacillus subtilis. Compared with synthetic surfactant, surfactin has following advantages:(1) It is a natural product produced by microbial fermentation technology using renewable energy such as hydrocarbon; (2) It has high surface activity, no pollution to the environment, easy to biodegrade, good antibacterial effect and other excellent features; (3) It is consistent with the modern concept of the development of green chemistry, and used in a wide range of applications.In this paper, the basic structure, main characteristics, production process, purification methods and application of surfactin were reviewed in detail, and the research prospect on surfactin is discussed, which could facilitate the further study of surfactin.
Surfactin belongs to biosurfactant.It is a series of cyclic lipopeptides with similar basic structures produced by fermentation of Bacillus subtilis. Compared with synthetic surfactant, surfactin has following advantages:(1) It is a natural product produced by microbial fermentation technology using renewable energy such as hydrocarbon; (2) It has high surface activity, no pollution to the environment, easy to biodegrade, good antibacterial effect and other excellent features; (3) It is consistent with the modern concept of the development of green chemistry, and used in a wide range of applications.In this paper, the basic structure, main characteristics, production process, purification methods and application of surfactin were reviewed in detail, and the research prospect on surfactin is discussed, which could facilitate the further study of surfactin.
2017, 80(10): 925-934
Abstract:
In recent years, the research of environmentally responsive block copolymers has attracted wide attention from researchers.The structures, physical and chemical properties of the copolymers responded to change, when they were stimulated by external environment.According to the different response mechanism and types of external stimuli, the stimulus-responsive block copolymers were classified into three categories:single stimulus response, dual stimulus response and triple stimulus response.As for each type of system, this review discussed the design, synthesis, self-assembly and application of stimuli-responsive polymers in aqueous solution.Meanwhile, the various ordered aggregates (such as micelles, vesicles, etc.) changed with stimulus response (pH, temperature, light, CO2, redox agent, etc.) were summarized in brief.Finally, the potential application value of intelligent block copolymers in drug controlled release, the synthesis of nano container, biological functional materials and the possible development direction in the future were prospected.
In recent years, the research of environmentally responsive block copolymers has attracted wide attention from researchers.The structures, physical and chemical properties of the copolymers responded to change, when they were stimulated by external environment.According to the different response mechanism and types of external stimuli, the stimulus-responsive block copolymers were classified into three categories:single stimulus response, dual stimulus response and triple stimulus response.As for each type of system, this review discussed the design, synthesis, self-assembly and application of stimuli-responsive polymers in aqueous solution.Meanwhile, the various ordered aggregates (such as micelles, vesicles, etc.) changed with stimulus response (pH, temperature, light, CO2, redox agent, etc.) were summarized in brief.Finally, the potential application value of intelligent block copolymers in drug controlled release, the synthesis of nano container, biological functional materials and the possible development direction in the future were prospected.
2017, 80(10): 935-941, 975
Abstract:
In this paper, using polystyrene (PS) spheres as the template, In2O3/ZrO2-TiO2 hollow spheres (In2O3/ZrO2-TiO2-H) with different proportions were prepared by one-step method combined with calcination treatment.The structures, compositions and morphologies of as-prepared composites were characterized by XRD, XPS, UV-Vis/DRS, SEM and N2 absorption-desorption measurements.The results showed that In2O3/ZrO2-TiO2 composites had a hollow spherical structure after being treated by PS template, and the spherical wall was formed by the nanoparticles.After compounding In2O3 with ZrO2-TiO2, its optical absorption had red-shifted slightly, moreover, the specific surface area of In2O3/ZrO2-TiO2-H (1:4) hollow sphere was larger (66.92 m2·g-1).In2O3/ZrO2-TiO2-H (1:4) showed higher photocatalytic activity in the degradation of methyl orange (MO) under multimodes photocatalysis, compared with P25, ZrO2, In2O3/ZrO2-TiO2, and other ratio In2O3/ZrO2-TiO2-H.
In this paper, using polystyrene (PS) spheres as the template, In2O3/ZrO2-TiO2 hollow spheres (In2O3/ZrO2-TiO2-H) with different proportions were prepared by one-step method combined with calcination treatment.The structures, compositions and morphologies of as-prepared composites were characterized by XRD, XPS, UV-Vis/DRS, SEM and N2 absorption-desorption measurements.The results showed that In2O3/ZrO2-TiO2 composites had a hollow spherical structure after being treated by PS template, and the spherical wall was formed by the nanoparticles.After compounding In2O3 with ZrO2-TiO2, its optical absorption had red-shifted slightly, moreover, the specific surface area of In2O3/ZrO2-TiO2-H (1:4) hollow sphere was larger (66.92 m2·g-1).In2O3/ZrO2-TiO2-H (1:4) showed higher photocatalytic activity in the degradation of methyl orange (MO) under multimodes photocatalysis, compared with P25, ZrO2, In2O3/ZrO2-TiO2, and other ratio In2O3/ZrO2-TiO2-H.
2017, 80(10): 942-947
Abstract:
Cu/AC hydrolysis catalysts were prepared by sol-gel method and impregnation method, and the influence of the preparation methods on their desulfurization activities were investigated.XRD, BET and SEM were used to characterize the support and the catalysts.The influence of surface pretreatment and preparation methods on their desulfurization activities and the mechanism of hydrolysis desulfurization were discussed.The results showed that the desulfurization activity of the catalyst prepared by impregnation method is better than that prepared by sol-gel method.By expanding the specific surface area and increasing the number of pores of activated carbon in the process of pretreatment, the catalyst which was prepared by impregnated method can be uniformly dispersed on the surface of carrier and also into its pores.On the contrast, the catalyst prepared by sol-gel method resulted in active component dispersing only on the surface of activated carbon, leading to low desulfurization efficiency.Under the temperature of 80℃, 1.33g/m3 of COS concentration, 1500h-1 of space velocity, 5% of mass fraction copper oxide, Cu/AC hydrolysis catalyst prepared by impregnation method exhibits the highest sulfur capacity of 29mgS/g.
Cu/AC hydrolysis catalysts were prepared by sol-gel method and impregnation method, and the influence of the preparation methods on their desulfurization activities were investigated.XRD, BET and SEM were used to characterize the support and the catalysts.The influence of surface pretreatment and preparation methods on their desulfurization activities and the mechanism of hydrolysis desulfurization were discussed.The results showed that the desulfurization activity of the catalyst prepared by impregnation method is better than that prepared by sol-gel method.By expanding the specific surface area and increasing the number of pores of activated carbon in the process of pretreatment, the catalyst which was prepared by impregnated method can be uniformly dispersed on the surface of carrier and also into its pores.On the contrast, the catalyst prepared by sol-gel method resulted in active component dispersing only on the surface of activated carbon, leading to low desulfurization efficiency.Under the temperature of 80℃, 1.33g/m3 of COS concentration, 1500h-1 of space velocity, 5% of mass fraction copper oxide, Cu/AC hydrolysis catalyst prepared by impregnation method exhibits the highest sulfur capacity of 29mgS/g.
2017, 80(10): 948-952
Abstract:
Three kinds of binder systems (PVDF, LA133, CMC+SBR with 1:1 mass ratio) were employed for constructing sulfur electrode of Li-S battery.The molecule structures, crystallization properties, thermodynamic properties, electrolyte absorption and binding strength of various materials were characterized.The effects of binder type on the electrochemical properties of Li-S battery were investigated.Low electrolyte uptake, weak peel strength and poor cycle capability appears in the sulfur cathode fabricated by CMC+SBR.Amorphous LA133 favors high binding strength and stable electrode structure.PVDF leads to poor adhesion quality due to its semi crystalline, and the constructed cathode produces high electrolyte absorption but low charge transfer resistance.In contrast, a reversible capacity of 722mAh·g-1 and capacity retention rate of 82.9% after 100 cycles at 0.2 C is exhibited in the PVDF-based cathode, which is the best performance level among mentioned three binder systems.
Three kinds of binder systems (PVDF, LA133, CMC+SBR with 1:1 mass ratio) were employed for constructing sulfur electrode of Li-S battery.The molecule structures, crystallization properties, thermodynamic properties, electrolyte absorption and binding strength of various materials were characterized.The effects of binder type on the electrochemical properties of Li-S battery were investigated.Low electrolyte uptake, weak peel strength and poor cycle capability appears in the sulfur cathode fabricated by CMC+SBR.Amorphous LA133 favors high binding strength and stable electrode structure.PVDF leads to poor adhesion quality due to its semi crystalline, and the constructed cathode produces high electrolyte absorption but low charge transfer resistance.In contrast, a reversible capacity of 722mAh·g-1 and capacity retention rate of 82.9% after 100 cycles at 0.2 C is exhibited in the PVDF-based cathode, which is the best performance level among mentioned three binder systems.
2017, 80(10): 958-962
Abstract:
In this paper, two mononuclear coordination complexes Zn (L1)(Phen)2·CH3OH·2H2O (3) and Cd (L1)(Phen)2·2CH3OH·H2O (4), (L1=PropylTTF2-; Phen=1, 10-phenanthroline) derived from a water-soluble TTF-dicarboxylate salt PropylTTFK2(1)(PropylTTFK2=Propylenedithio-4', 5'-tetrathiafulavalene-4, 5-dicarboxylate dipotassium salt) were prepared.Their structures were characterized by elemental analysis.And the crystal structures of the complex 3 and 4 were analyzed by X-ray single crystal diffraction.Noticeable inter molecular S…S or/and H-bonding interactions have been found in 3 and 4, resulting in the formation of 1D chain.All of them have been characterized by UV-Vis, fluorescence and electrochemistry.The titration of TCNQ shows these complexes can form classical electron-acceptor salt with TCNQ.
In this paper, two mononuclear coordination complexes Zn (L1)(Phen)2·CH3OH·2H2O (3) and Cd (L1)(Phen)2·2CH3OH·H2O (4), (L1=PropylTTF2-; Phen=1, 10-phenanthroline) derived from a water-soluble TTF-dicarboxylate salt PropylTTFK2(1)(PropylTTFK2=Propylenedithio-4', 5'-tetrathiafulavalene-4, 5-dicarboxylate dipotassium salt) were prepared.Their structures were characterized by elemental analysis.And the crystal structures of the complex 3 and 4 were analyzed by X-ray single crystal diffraction.Noticeable inter molecular S…S or/and H-bonding interactions have been found in 3 and 4, resulting in the formation of 1D chain.All of them have been characterized by UV-Vis, fluorescence and electrochemistry.The titration of TCNQ shows these complexes can form classical electron-acceptor salt with TCNQ.
2017, 80(10): 963-970
Abstract:
In this article, the mechanism and rate constant for the reaction of HCl+NO3 without and with a water molecule were studied at the CCSD (T)/aug-cc-pVTZ//UB3LYP/6-311+G (2d, p) level of theory.The results show that there is only one channel for the NO3+HCl reaction, labeled as HNO3+Cl formation channel.When one water molecule is added, the product of the reaction does not change, but the potential energy surface of the reaction becomes quite complex, yielding three different channels of NO3…H2O+HCl, H2O…HCl+NO3 and HCl…H2O+NO3.Channel HCl…H2O+NO3 is the dominant channel for water molecules to participate in the reaction.Besides, the rate constant of HCl…H2O+NO3 channel is predicted to be faster by 0.33×104~1.07×107 times than that of the NO3+HCl naked reaction.Its effective rate constant k'RW3/k'total is up to 95.9% at 298 K, that is, the single water molecule has a obvious influence on the atmospheric reaction of NO3+HCl.
In this article, the mechanism and rate constant for the reaction of HCl+NO3 without and with a water molecule were studied at the CCSD (T)/aug-cc-pVTZ//UB3LYP/6-311+G (2d, p) level of theory.The results show that there is only one channel for the NO3+HCl reaction, labeled as HNO3+Cl formation channel.When one water molecule is added, the product of the reaction does not change, but the potential energy surface of the reaction becomes quite complex, yielding three different channels of NO3…H2O+HCl, H2O…HCl+NO3 and HCl…H2O+NO3.Channel HCl…H2O+NO3 is the dominant channel for water molecules to participate in the reaction.Besides, the rate constant of HCl…H2O+NO3 channel is predicted to be faster by 0.33×104~1.07×107 times than that of the NO3+HCl naked reaction.Its effective rate constant k'RW3/k'total is up to 95.9% at 298 K, that is, the single water molecule has a obvious influence on the atmospheric reaction of NO3+HCl.
2017, 80(10): 971-975
Abstract:
In recent years, dense haze and fog occurs with increasing frequency in the world.There are a lot of researches on the composition, formation, enhancement and evolution of haze and fog with emphasis on weather conditions and human activities, but with little concerns on analysis of haze and fog based on the principles of physical chemistry.As the most common aerosol, the occurrence and evolution of haze and fog are closely related to many physiochemical phenomena such as precipitation, precipitation equilibrium, surface adsorption of water vapor and diffusion.In this work, the height-distribution, the difference between dry/humid haze, and the effectiveness of wet-cleaning of haze are discussed based on a simplified model using some physical chemistry principles.Some important conclusions meaningful for people to have a correct understanding of haze and fog are reached.
In recent years, dense haze and fog occurs with increasing frequency in the world.There are a lot of researches on the composition, formation, enhancement and evolution of haze and fog with emphasis on weather conditions and human activities, but with little concerns on analysis of haze and fog based on the principles of physical chemistry.As the most common aerosol, the occurrence and evolution of haze and fog are closely related to many physiochemical phenomena such as precipitation, precipitation equilibrium, surface adsorption of water vapor and diffusion.In this work, the height-distribution, the difference between dry/humid haze, and the effectiveness of wet-cleaning of haze are discussed based on a simplified model using some physical chemistry principles.Some important conclusions meaningful for people to have a correct understanding of haze and fog are reached.
2017, 80(10): 953-957
Abstract:
Here a novel cyanoacrylic ester, (E)-2-cyano-3-[4-(2, 4-difluorophenoxy) benzylamino]-3-methoxyacrylic acid 2-ethoxyethyl ester (MAE), which is capable of site-specific cleavage of supercoiled pUC19 DNA, was introduced.The cleavage specificity was investigated through UV absorption, fluorescence, agarose gel electrophoresis, and DNA sequencing techniques.Red shift and hypochromism in the absorption spectra and static fluorescence quenching suggested that a typical intercalation occurred between DNA and MAE.In addition, detectable varieties in the gel electrophoresis and DNA sequencing indicated that the cleavage was site-specific, and double strands of DNA were hydrolyzed step by step.
Here a novel cyanoacrylic ester, (E)-2-cyano-3-[4-(2, 4-difluorophenoxy) benzylamino]-3-methoxyacrylic acid 2-ethoxyethyl ester (MAE), which is capable of site-specific cleavage of supercoiled pUC19 DNA, was introduced.The cleavage specificity was investigated through UV absorption, fluorescence, agarose gel electrophoresis, and DNA sequencing techniques.Red shift and hypochromism in the absorption spectra and static fluorescence quenching suggested that a typical intercalation occurred between DNA and MAE.In addition, detectable varieties in the gel electrophoresis and DNA sequencing indicated that the cleavage was site-specific, and double strands of DNA were hydrolyzed step by step.
2017, 80(10): 976-979
Abstract:
A series of new 4'-(N-substitued-1-piperazinyl) furanyl chalcone derivatives have been synthesized, and their structures were characterized by 1H NMR and 13C NMR.The in vitro anti-inflammatory activities of synthesized compounds were evaluated in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages.The results demonstrated that sulfamide compounds showed higher anti-inflammatory activity than their amide analogs.In particular, compound 4d was found to be the most potent anti-inflammatory compound (IC50=3.88μmol/L), which has a comparable activity to the positive control drug dexamethasone.
A series of new 4'-(N-substitued-1-piperazinyl) furanyl chalcone derivatives have been synthesized, and their structures were characterized by 1H NMR and 13C NMR.The in vitro anti-inflammatory activities of synthesized compounds were evaluated in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages.The results demonstrated that sulfamide compounds showed higher anti-inflammatory activity than their amide analogs.In particular, compound 4d was found to be the most potent anti-inflammatory compound (IC50=3.88μmol/L), which has a comparable activity to the positive control drug dexamethasone.
2017, 80(10): 980-983, 952
Abstract:
Various 5-substitued 2-oxazolidinones were obtained by a ZnBr2 catalyzed cyclization of N-Boc alkynylamines in toluene with DMAP as a base.The effects of catalyst type, alkali and temperature on the reaction were investigated.A series of target products were obtained with good yield under the optimized conditions.
Various 5-substitued 2-oxazolidinones were obtained by a ZnBr2 catalyzed cyclization of N-Boc alkynylamines in toluene with DMAP as a base.The effects of catalyst type, alkali and temperature on the reaction were investigated.A series of target products were obtained with good yield under the optimized conditions.
