Analyzing polysorbate 20(PS20)composition and the impact of each component on stability and safety is crucial due to formulation variations and individual tolerance.The similar structures and polarities of PS20 compon...Analyzing polysorbate 20(PS20)composition and the impact of each component on stability and safety is crucial due to formulation variations and individual tolerance.The similar structures and polarities of PS20 components make accurate separation,identification,and quantification challenging.In this work,a high-resolution quantitative method was developed using single-dimensional high-performance liquid chromatography(HPLC)with charged aerosol detection(CAD)to separate 18 key components with multiple esters.The separated components were characterized by ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UHPLC-Q-TOF-MS)with an identical gradient as the HPLC-CAD analysis.The polysorbate compound database and library were expanded over 7-time compared to the commercial database.The method investigated differences in PS20 samples from various origins and grades for different dosage forms to evaluate the composition-process relationship.UHPLC-Q-TOF-MS identified 1329 to 1511 compounds in 4 batches of PS20 from different sources.The method observed the impact of 4 degradation conditions on peak components,identifying stable components and their tendencies to change.HPLC-CAD and UHPLC-Q-TOF-MS results provided insights into fingerprint differences,distinguishing quasi products.展开更多
Photocatalytic H2 production and CO2 reduction have attracted considerable attention for clean energy development.In this work,we designed an efficient photocatalyst by integrating lamellar oxygen-doped carbon nitride...Photocatalytic H2 production and CO2 reduction have attracted considerable attention for clean energy development.In this work,we designed an efficient photocatalyst by integrating lamellar oxygen-doped carbon nitride(CNO)nanosheets into ZnIn2S4(ZIS)microflowers by a one-step hydrothermal method.A well-fitted 2D hierarchical hybrid heterostructure was fabricated.Under visible light irradiation,the ZIS@CNO composite with 40 wt%CNO(ZC 40%)showed the highest hydrogen evolution rate from water(188.4μmol·h-1),which was approximately 2.1 times higher than those of CNO and ZIS(88.6 and 90.2μmol·h-1,respectively).Furthermore,the selective CO production rates of ZC 40%(12.69μmol·h-1)were 2.2 and 14.0 times higher than those of ZIS(5.85μmol·h-1)and CNO(0.91μmol·h-1),respectively,and the CH4 production rate of ZC 40%was 1.18μmol·h-1.This enhanced photocatalytic activity of CNO@ZIS is due mainly to the formation of a heterostructure that can promote the transfer of photoinduced electrons and holes between CNO and ZIS,thereby efficiently avoiding recombination of electron-hole pairs.展开更多
Photothermal material applied in environmental governance has attracted growing attention.By combining the Stober method and dopamine-triggered coating strategy,Co-Mn precursor was in situ incorporated into the poly d...Photothermal material applied in environmental governance has attracted growing attention.By combining the Stober method and dopamine-triggered coating strategy,Co-Mn precursor was in situ incorporated into the poly dopamine(PDA)layer over the surface of silica cores.Afterwards,a unique photothermal nanosphere with SiO_(2)core and thin carbon layer and dual Co-Mn oxides shell was allowed to form by sequential heat treatment in the inert atmosphere(SiO_(2)@CoMn/C).The bimetallic fraction of Co/Mn in the carbon layer and post-treatment calcination temperature was comprehensively tuned to optimize the peroxymonosulfate(PMS)activation performance of the catalyst.The state of bimetallic species was studied including their physical distribution,chemical valence,and interplay by various characterizations.Impressively,Co oxides appear as dominant monodispersed nanoparticles(~10 nm),while Mn with cluster-like morphology is observed to uniformly distribute over thin-layer carbon and adhered to the surface of SiO_(2)nanospheres(~250 nm).The calcined temperature could tune the oxidized state of Co species,leading to the optimization of the catalytic performance of introduced dual metal species.As a result,this obtained optimal catalyst integrated the advantages of exposed bimetallic CoMn species and N-doped thin carbon to deliver excellent catalytic PMS activation performance and photothermal synergetic catalytic mineralization ability for diversiform pollutants.Further reactions condition controls and anion interference studies were conducted to identify the adaptability of the optimal catalyst.Moreover,the application of solar-driven interfacial water evaporation using optimal SiO_(2)@Co_3Mn_1/C-600 catalyst was explored,showing a high water evaporation rate of 1.48 kg·m^(-2)·h^(-1)and an efficiency of 95.2%,further revealing a comprehensive governance functionality of obtained material in the complex pollution condition.展开更多
The development of effective and sustainable solutions for pleiotropic water purification becomes urgent and attractive.Heterogeneous Fenton-like catalysts for activation of peroxymonosulfate(PMS)to purify organic was...The development of effective and sustainable solutions for pleiotropic water purification becomes urgent and attractive.Heterogeneous Fenton-like catalysts for activation of peroxymonosulfate(PMS)to purify organic wastewater show great promise.In this work,by tuning metal loading with an in-situ polydopamine coating strategy,oxygen vacancy-enriched Co_(3)O_(4) loading on N-doped carbon nanotubes(CNTs)were constructed to enhance PMS activation efficiency for pollutants degradation.Impressively,the obtained modified CNTs afford a well-developed N-containing network structure,which is further endowed with abundant Co(Ⅱ)/Co(Ⅲ)redox cycles and significant metal-carbon interactions.In particular,the surface N doping in CNTs might induce the oriented enrichment of pollutants around the catalyst,which reduces the migration distance and correspondingly improves the utilization of reactive oxidative species.The electron transfer efficiency of the catalyst can be further improved by incorporating oxygen vacancy-enriched Co_(3)O_(4).The performance results show that the optimal NC/Co-1 could mineralize 20×10^(-6)of bisphenol A(BPA)by almost 98%in 8 min.A low reaction activation energy(26.05 kJ·mol^(-1))in BPA degradation was demonstrated by the NC/Co-1.More importantly,NC/Co-1 can inherit excellent degradation performance towards oxytetracycline,2,4-dichlorophenol,and tetracycline,showing wide practical flexibility.In addition,by virtue of the photothermal conversion property,NC/Co-1 achieves an additive function for interfacial solar water evaporation(1.84 kg·m^(-2)·h^(-1),112.51%),showing impressive potential for clean water recovery under complicated environmental pollution conditions.展开更多
In recent years,the application of smartphone in various fields has received great attention,and it has become a promising tool in virus detection,data processing and data exchange.During the rapid spread of COVID-19 ...In recent years,the application of smartphone in various fields has received great attention,and it has become a promising tool in virus detection,data processing and data exchange.During the rapid spread of COVID-19 around the world,many traditional detection methods have been combined with smartphone to assist in the analysis and detection of the novel coronavirus(SARS-CoV-2),including electrochemistry,fluorescence and colorimetry.With the gradual development of artificial intelligence(AI),the combination of AI and smartphone to analyze SARS-CoV-2 was also the focus of research.Based on the summary of the traditional methods combined with smartphone to detect SARS-CoV-2 virus,in addition to AI-based data processing,AI algorithms are also employed for SARS-CoV-2 detection itself.This review discussed both strategies and focused on the application of the former.The combination of AI algorithm and smartphone to detect SARS-CoV-2 has high accuracy,which is more conducive to meeting the needs of portable detection.In addition,the classification of SARS-CoV-2 virus samples in biological fluids such as blood and saliva was also discussed.Finally,this paper briefly discussed the limitations of using smartphone analysis to detect SARS-CoV-2,as well as the prospect and future development of virus detection.In conclusion,the detection methods based on smartphone and AI algorithms show great potential in the detection of SARS-CoV-2 and can be a valuable complement to traditional analysis methods.展开更多
Owing to the serious potential side-effects on the environment and human health,the rapid detection and removal of antibiotics have become an important research focus.In this work,four zinc-based metal-organic framewo...Owing to the serious potential side-effects on the environment and human health,the rapid detection and removal of antibiotics have become an important research focus.In this work,four zinc-based metal-organic frameworks(MOFs)with different functional groups,i.e.,Zn-MOF,Zn-MOF-CH_(3),Zn-MOF-NO_(2),Zn-MOF-COOH,were utilized for the construction of LDO/MOF composite materials with a nickel-iron-cobalt-based layered double oxide,NiFeCo-LDO.The results showed that the LDO/MOF composites not only had high sensitivity in detecting sulfonamide and quinolone antibiotics,but also had an appreciable ability to adsorb them from wastewater.The maximum adsorption capacities of all the four types of LDO@Zn-MOFs to all antibiotics can at least reach 150 mg/g,and the limits of detection in relation to all four antibiotics were at least as low as 100μg/L.Our work suggested the dual-function extraction performance can be attributed to the synergistic effects between the LDO and the MOFs.Moreover,the strong ferromagnetism derived from the LDO provided great convenience for the separation and regeneration of the LDO/MOF composites.展开更多
The site-selective C-H fluorination of heteroarenes is a straightforward approach to accessing valuable heteroaryl fluorides but remains a formidable challenge.Herein,we report a general strategy for visible-light-ind...The site-selective C-H fluorination of heteroarenes is a straightforward approach to accessing valuable heteroaryl fluorides but remains a formidable challenge.Herein,we report a general strategy for visible-light-induced C-H fluorination of heteroarenes via the merger of N-F fluorinating reagents and silane.Electron paramagnetic resonance experiments provide evidence for the homolytic cleavage of the N-F bond under blue light-emitting diode irradiation,which is the key step in the process.This transformation is metal-free,photocatalysts-free,and site-selective under mild reaction conditions(ambient temperature,visible-light irradiation,tolerant to H2O).The robustness of this protocol has also been highlighted by late-stage modification of complex and medicinally relevant molecules.展开更多
In recent years,Fe_(3)O_(4)nanomaterials have received much attention in analytical chemistry due to their excellent magnetic and peroxidase-like activity.As the catalytic characteristics of Fe_(3)O_(4)nanomaterials i...In recent years,Fe_(3)O_(4)nanomaterials have received much attention in analytical chemistry due to their excellent magnetic and peroxidase-like activity.As the catalytic characteristics of Fe_(3)O_(4)nanomaterials is similar to those of horseradish peroxidase(HRP),Fe_(3)O_(4)nanomaterials are also used as peroxidase mimics and have achieved a certain development in many fields based on latest research results.To improve the stability and catalytic ability of simple Fe_(3)O_(4)nanomaterials,various modification strategies of Fe_(3)O_(4)nanomaterials have been developed.The recent advances of these strategies have been presented and discussed.In addition,this paper introduces the application of Fe_(3)O_(4)nanozymes in the detection of food and industrial pollutants,as well as in the field of biosafety.展开更多
A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against c...A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant(MDR)Gram-negative strains,with a highly druglike nature.The checkerboard assay reveals its significant synergistic effect withβ-lactamase inhibitor avibactam,and the MIC values against MDR enterobacteria were reduced up to 4—512folds.X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and Cβ-lactamases.Accordingly,preclinical studies of 33a alone and 33a-avibactam combination as potential innovative candidates are actively going on,in the treatment ofβ-lactamase-producing MDR Gram-negative bacterial infections.展开更多
We found compound 12N-p-trifluoromethylbenzenesulfonyl matrinane(1)was a potent anti-diabetic agent.Thirty-five tricyclic matrinic derivatives were synthesized and determined for their stimulatory effects on glucose c...We found compound 12N-p-trifluoromethylbenzenesulfonyl matrinane(1)was a potent anti-diabetic agent.Thirty-five tricyclic matrinic derivatives were synthesized and determined for their stimulatory effects on glucose consumption in L6 myotubes,taking 1 as the lead.In high-fat diet(HFD)and STZ induced diabetic mice,9a significantly lowers blood glucose,improves glucose tolerance,and especially alleviates diabetic nephropathy and islet damage.Mechanism study indicates that 9a simultaneously targets mitochondrial complex I to increase AMP/ATP ratio,as well as liver kinase B1(LKB1)and calcium/calmodulindependent protein kinase(Ca MKK),which synergistically activates AMPKαand then stimulates glucose transporter 4(GLUT4)membrane translocation and 2-deoxyglucose(2-DG)uptake to exert anti-diabetic efficacy.Therefore,compound 9a with a novel structure is a promising anti-diabetic candidate with the advantage of multiple-target mechanism,worthy of further investigation.展开更多
Tuberculosis is a serious threat to public health throughout the world.A series of new l3-n-nonylprotoberberine derivatives was designed,synthesized and evaluated for anti-mycobacterial activity against Mycobacterium ...Tuberculosis is a serious threat to public health throughout the world.A series of new l3-n-nonylprotoberberine derivatives was designed,synthesized and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis strain H_(37)Rv.Several compounds(2,11a-c,11g,13d,15c)exhibited excellent anti-tubercular activity with an MIC below 1.0μg/mL.Notably,compound 13d showed potential antibacterial effect against both drug-susceptible and multidrug-resistant(MDR)M.tuberculosis with MIC ranges of 0.0625-1.0μg/mL.These results suggest a mode of action different from that of the current anti-mycobacterial drugs rifampicin and isoniazid.Hence,compound 13d is an attractive lead compound for the development of new antitubercular agents.展开更多
A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine（1）and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suita...A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine（1）and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suitable substituent at the N’-end of matrinic amide might greatly enhance the potency.Among them,matrinic acid 17 and N’-substituted matrinic amides 18a-d exhibited promising potency with low micromolar EC50 values ranging from 1.03μmol/L to 7.54 μmol/L,and better therapeutic window with SI from 66 to 132.Moreover,compound 17 displayed an excellent PK and safety profile in vivo,demonstrating good drug-like characteristics.Thus,it has been selected for further investigation,with an advantage of decreased chances of inducing drug-resistance mutations.展开更多
Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus(EBOV)activities. Structure–activity...Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus(EBOV)activities. Structure–activity relationship analysis indicated:(i) 12 N-dichlorobenzyl motif was beneficial for the activity;(ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound 7d exhibited the most potent potency against EBOV with an IC_(50) value of 5.29 μmol/L and an SI value of over 37.8. Further in vivo anti-EBOV assay of 7d identified its high effectiveness, and in vivo anti-MARV assay of 7d suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses.展开更多
Seven photoaffinity-based and sixteen biotin-based berberine(BBR)probes were constructed and screened for their effects on c-Jun N-terminal protein kinases(JNK)phosphorylation(p-JNK)suppression at the cellular level.T...Seven photoaffinity-based and sixteen biotin-based berberine(BBR)probes were constructed and screened for their effects on c-Jun N-terminal protein kinases(JNK)phosphorylation(p-JNK)suppression at the cellular level.Taking active-photoaffinity probe 7c as a chemical tool,we first identified mitogen-activated protein kinase 7(MAP2K7),an upstream protein on the JNK/stress activated protein kinase(SAPK)pathway,as a direct proteomic target of BBR using activity-based protein profiling(ABPP)and other chemical proteomic techniques.Furthermore,BBR’s inhibitory effect on p-JNK was significantly attenuated in both the MAP2K7-knockdown and models,indicating a MAP2K7-dependent inhibition on the JNK signaling pathway.For the first time,we demonstrate the unique mechanism of BBR that directly targets MAP2K7 to inhibit p-JNK rather than JNK activity with the advantages of multiple activities and a good safety profile.展开更多
Severe sex ratio imbalance at birth is now becoming an important issue in several Asian countries. Its leading immediate cause is prenatal sex-selective abortion following illegal sex identification by ultrasound scan...Severe sex ratio imbalance at birth is now becoming an important issue in several Asian countries. Its leading immediate cause is prenatal sex-selective abortion following illegal sex identification by ultrasound scanning. In this paper, a fast automatic recognition and location algorithm for fetal genital organs is proposed as an effective method to help prevent ultrasound technicians from unethically and illegally identifying the sex of the fetus. This automatic recognition algorithm can be divided into two stages. In the 'rough' stage, a few pixels in the image, which are likely to represent the genital organs, are automatically chosen as points of interest (POIs) according to certain salient characteristics of fetal genital organs. In the 'fine' stage, a specifically supervised learning framework, which fuses an effective feature data preprocessing mechanism into the multiple classifier architecture, is applied to every POI. The basic classifiers in the framework are selected from three widely used classifiers: radial basis function network, backpropagation network, and support vector machine. The classification results of all the POIs are then synthesized to determine whether the fetal genital organ is present in the image, and to locate the genital organ within the positive image. Experiments were designed and carried out based on an image dataset comprising 658 positive images (images with fetal genital organs) and 500 negative images (images without fetal genital organs). The experimental results showed true positive (TP) and true negative (TN) results from 80.5% (265 from 329) and 83.0% (415 from 500) of samples, respectively. The average computation time was 453 ms per image.展开更多
基金financial support from the Science Research Program Project for Drug Regulation,Jiangsu Drug Administration,China(Grant No.:202207)the National Drug Standards Revision Project,China(Grant No.:2023Y41)+1 种基金the National Natural Science Foundation of China(Grant No.:22276080)the Foreign Expert Project,China(Grant No.:G2022014096L).
文摘Analyzing polysorbate 20(PS20)composition and the impact of each component on stability and safety is crucial due to formulation variations and individual tolerance.The similar structures and polarities of PS20 components make accurate separation,identification,and quantification challenging.In this work,a high-resolution quantitative method was developed using single-dimensional high-performance liquid chromatography(HPLC)with charged aerosol detection(CAD)to separate 18 key components with multiple esters.The separated components were characterized by ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UHPLC-Q-TOF-MS)with an identical gradient as the HPLC-CAD analysis.The polysorbate compound database and library were expanded over 7-time compared to the commercial database.The method investigated differences in PS20 samples from various origins and grades for different dosage forms to evaluate the composition-process relationship.UHPLC-Q-TOF-MS identified 1329 to 1511 compounds in 4 batches of PS20 from different sources.The method observed the impact of 4 degradation conditions on peak components,identifying stable components and their tendencies to change.HPLC-CAD and UHPLC-Q-TOF-MS results provided insights into fingerprint differences,distinguishing quasi products.
基金supported by the National Natural Science Foundation of China(21503096,21407067)the Natural Science Foundation of Educational Committee of Anhui Province(KJ2018A0387),ChinaProject of Anhui Province for Excellent Young Talents in Universities(gxyq2019029),China
文摘Photocatalytic H2 production and CO2 reduction have attracted considerable attention for clean energy development.In this work,we designed an efficient photocatalyst by integrating lamellar oxygen-doped carbon nitride(CNO)nanosheets into ZnIn2S4(ZIS)microflowers by a one-step hydrothermal method.A well-fitted 2D hierarchical hybrid heterostructure was fabricated.Under visible light irradiation,the ZIS@CNO composite with 40 wt%CNO(ZC 40%)showed the highest hydrogen evolution rate from water(188.4μmol·h-1),which was approximately 2.1 times higher than those of CNO and ZIS(88.6 and 90.2μmol·h-1,respectively).Furthermore,the selective CO production rates of ZC 40%(12.69μmol·h-1)were 2.2 and 14.0 times higher than those of ZIS(5.85μmol·h-1)and CNO(0.91μmol·h-1),respectively,and the CH4 production rate of ZC 40%was 1.18μmol·h-1.This enhanced photocatalytic activity of CNO@ZIS is due mainly to the formation of a heterostructure that can promote the transfer of photoinduced electrons and holes between CNO and ZIS,thereby efficiently avoiding recombination of electron-hole pairs.
基金financially supported by the China National Natural Science Foundation(No.21908085)China Postdoctoral Science Foundation(No.2022M711686)Jiangsu Provincial Founds for the Young Scholars(No.BK20190961)。
文摘Photothermal material applied in environmental governance has attracted growing attention.By combining the Stober method and dopamine-triggered coating strategy,Co-Mn precursor was in situ incorporated into the poly dopamine(PDA)layer over the surface of silica cores.Afterwards,a unique photothermal nanosphere with SiO_(2)core and thin carbon layer and dual Co-Mn oxides shell was allowed to form by sequential heat treatment in the inert atmosphere(SiO_(2)@CoMn/C).The bimetallic fraction of Co/Mn in the carbon layer and post-treatment calcination temperature was comprehensively tuned to optimize the peroxymonosulfate(PMS)activation performance of the catalyst.The state of bimetallic species was studied including their physical distribution,chemical valence,and interplay by various characterizations.Impressively,Co oxides appear as dominant monodispersed nanoparticles(~10 nm),while Mn with cluster-like morphology is observed to uniformly distribute over thin-layer carbon and adhered to the surface of SiO_(2)nanospheres(~250 nm).The calcined temperature could tune the oxidized state of Co species,leading to the optimization of the catalytic performance of introduced dual metal species.As a result,this obtained optimal catalyst integrated the advantages of exposed bimetallic CoMn species and N-doped thin carbon to deliver excellent catalytic PMS activation performance and photothermal synergetic catalytic mineralization ability for diversiform pollutants.Further reactions condition controls and anion interference studies were conducted to identify the adaptability of the optimal catalyst.Moreover,the application of solar-driven interfacial water evaporation using optimal SiO_(2)@Co_3Mn_1/C-600 catalyst was explored,showing a high water evaporation rate of 1.48 kg·m^(-2)·h^(-1)and an efficiency of 95.2%,further revealing a comprehensive governance functionality of obtained material in the complex pollution condition.
基金financially supported by the China National Natural Science Foundation(No.201808085)the National Key Research and Development Program of China(No.2022YFB3504100)+2 种基金Jiangsu Provincial Founds for Young Scholars(No.BK20190961)the Natural Science Foundation of Jiangsu Higher Education Institutions of China(No.22KJB610012)the International Cooperation Foundation for the Chunhui Plan Program of Ministry of Education of China(No.HZKY20220136)。
文摘The development of effective and sustainable solutions for pleiotropic water purification becomes urgent and attractive.Heterogeneous Fenton-like catalysts for activation of peroxymonosulfate(PMS)to purify organic wastewater show great promise.In this work,by tuning metal loading with an in-situ polydopamine coating strategy,oxygen vacancy-enriched Co_(3)O_(4) loading on N-doped carbon nanotubes(CNTs)were constructed to enhance PMS activation efficiency for pollutants degradation.Impressively,the obtained modified CNTs afford a well-developed N-containing network structure,which is further endowed with abundant Co(Ⅱ)/Co(Ⅲ)redox cycles and significant metal-carbon interactions.In particular,the surface N doping in CNTs might induce the oriented enrichment of pollutants around the catalyst,which reduces the migration distance and correspondingly improves the utilization of reactive oxidative species.The electron transfer efficiency of the catalyst can be further improved by incorporating oxygen vacancy-enriched Co_(3)O_(4).The performance results show that the optimal NC/Co-1 could mineralize 20×10^(-6)of bisphenol A(BPA)by almost 98%in 8 min.A low reaction activation energy(26.05 kJ·mol^(-1))in BPA degradation was demonstrated by the NC/Co-1.More importantly,NC/Co-1 can inherit excellent degradation performance towards oxytetracycline,2,4-dichlorophenol,and tetracycline,showing wide practical flexibility.In addition,by virtue of the photothermal conversion property,NC/Co-1 achieves an additive function for interfacial solar water evaporation(1.84 kg·m^(-2)·h^(-1),112.51%),showing impressive potential for clean water recovery under complicated environmental pollution conditions.
基金the financial support from the National Natural Science Foundation of China(Nos.21605105,22204064 and 22276080)the Natural Science Foundation of Jiangsu Province,China(Nos.BK20211340 and BK20220645)。
文摘In recent years,the application of smartphone in various fields has received great attention,and it has become a promising tool in virus detection,data processing and data exchange.During the rapid spread of COVID-19 around the world,many traditional detection methods have been combined with smartphone to assist in the analysis and detection of the novel coronavirus(SARS-CoV-2),including electrochemistry,fluorescence and colorimetry.With the gradual development of artificial intelligence(AI),the combination of AI and smartphone to analyze SARS-CoV-2 was also the focus of research.Based on the summary of the traditional methods combined with smartphone to detect SARS-CoV-2 virus,in addition to AI-based data processing,AI algorithms are also employed for SARS-CoV-2 detection itself.This review discussed both strategies and focused on the application of the former.The combination of AI algorithm and smartphone to detect SARS-CoV-2 has high accuracy,which is more conducive to meeting the needs of portable detection.In addition,the classification of SARS-CoV-2 virus samples in biological fluids such as blood and saliva was also discussed.Finally,this paper briefly discussed the limitations of using smartphone analysis to detect SARS-CoV-2,as well as the prospect and future development of virus detection.In conclusion,the detection methods based on smartphone and AI algorithms show great potential in the detection of SARS-CoV-2 and can be a valuable complement to traditional analysis methods.
基金support from the National Natural Science Foundation of China(Nos.22276080,21605105)the Foreign Expert Project,China(No.G2022014096L)+1 种基金the Natural Science Foundation of Jiangsu Province,China(No.BK20211340)Graduate Research and Practice Innovation Program of Jiangsu Province,China(No.KYCX22_3835).
文摘Owing to the serious potential side-effects on the environment and human health,the rapid detection and removal of antibiotics have become an important research focus.In this work,four zinc-based metal-organic frameworks(MOFs)with different functional groups,i.e.,Zn-MOF,Zn-MOF-CH_(3),Zn-MOF-NO_(2),Zn-MOF-COOH,were utilized for the construction of LDO/MOF composite materials with a nickel-iron-cobalt-based layered double oxide,NiFeCo-LDO.The results showed that the LDO/MOF composites not only had high sensitivity in detecting sulfonamide and quinolone antibiotics,but also had an appreciable ability to adsorb them from wastewater.The maximum adsorption capacities of all the four types of LDO@Zn-MOFs to all antibiotics can at least reach 150 mg/g,and the limits of detection in relation to all four antibiotics were at least as low as 100μg/L.Our work suggested the dual-function extraction performance can be attributed to the synergistic effects between the LDO and the MOFs.Moreover,the strong ferromagnetism derived from the LDO provided great convenience for the separation and regeneration of the LDO/MOF composites.
基金financial support from the National Natural Science Foundation of China (grant no.22201121)Jiangxi Provincial Natural Science Foundation (grant nos.20224BAB213006 and 20232BAB203002).
文摘The site-selective C-H fluorination of heteroarenes is a straightforward approach to accessing valuable heteroaryl fluorides but remains a formidable challenge.Herein,we report a general strategy for visible-light-induced C-H fluorination of heteroarenes via the merger of N-F fluorinating reagents and silane.Electron paramagnetic resonance experiments provide evidence for the homolytic cleavage of the N-F bond under blue light-emitting diode irradiation,which is the key step in the process.This transformation is metal-free,photocatalysts-free,and site-selective under mild reaction conditions(ambient temperature,visible-light irradiation,tolerant to H2O).The robustness of this protocol has also been highlighted by late-stage modification of complex and medicinally relevant molecules.
基金the financial support from the National Natural Science Foundation of China(Nos.31901799,21705060,21605105 and 32001804)the Natural Science Foundation of Jiangsu Province,China(Nos.BK20211340 and BK20180979)+1 种基金Opening Project of Key Laboratory of Impurity Spectrum of Chemical Drug,China(No.NMPA-KLIPCD-2020-09)the Emerging science and technology innovation team funding of JUST(No.1182921902)。
文摘In recent years,Fe_(3)O_(4)nanomaterials have received much attention in analytical chemistry due to their excellent magnetic and peroxidase-like activity.As the catalytic characteristics of Fe_(3)O_(4)nanomaterials is similar to those of horseradish peroxidase(HRP),Fe_(3)O_(4)nanomaterials are also used as peroxidase mimics and have achieved a certain development in many fields based on latest research results.To improve the stability and catalytic ability of simple Fe_(3)O_(4)nanomaterials,various modification strategies of Fe_(3)O_(4)nanomaterials have been developed.The recent advances of these strategies have been presented and discussed.In addition,this paper introduces the application of Fe_(3)O_(4)nanozymes in the detection of food and industrial pollutants,as well as in the field of biosafety.
基金supported by CAMS Innovation Fund for Medical Sciences(2021-12M-1-070)National Natural Science Foundation of China(32141003)。
文摘A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant(MDR)Gram-negative strains,with a highly druglike nature.The checkerboard assay reveals its significant synergistic effect withβ-lactamase inhibitor avibactam,and the MIC values against MDR enterobacteria were reduced up to 4—512folds.X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and Cβ-lactamases.Accordingly,preclinical studies of 33a alone and 33a-avibactam combination as potential innovative candidates are actively going on,in the treatment ofβ-lactamase-producing MDR Gram-negative bacterial infections.
基金supported by CAMS Innovation Fund for Medical Sciences(No.2021-12M-1-030)the Natural Science Foundation of Beijing Municipality(No.7202131)Chinese Pharmaceutical Association-Yiling Pharmaceutical Innovation Fund for Biomedicine(No.GL-1-B04-20190397)。
文摘We found compound 12N-p-trifluoromethylbenzenesulfonyl matrinane(1)was a potent anti-diabetic agent.Thirty-five tricyclic matrinic derivatives were synthesized and determined for their stimulatory effects on glucose consumption in L6 myotubes,taking 1 as the lead.In high-fat diet(HFD)and STZ induced diabetic mice,9a significantly lowers blood glucose,improves glucose tolerance,and especially alleviates diabetic nephropathy and islet damage.Mechanism study indicates that 9a simultaneously targets mitochondrial complex I to increase AMP/ATP ratio,as well as liver kinase B1(LKB1)and calcium/calmodulindependent protein kinase(Ca MKK),which synergistically activates AMPKαand then stimulates glucose transporter 4(GLUT4)membrane translocation and 2-deoxyglucose(2-DG)uptake to exert anti-diabetic efficacy.Therefore,compound 9a with a novel structure is a promising anti-diabetic candidate with the advantage of multiple-target mechanism,worthy of further investigation.
基金This work was supported by the National Natural Science Fund for Young Scientists(81102312)the National S&T Major Special Projecton Major New Drug Innovation(2012ZX09301002-001).
文摘Tuberculosis is a serious threat to public health throughout the world.A series of new l3-n-nonylprotoberberine derivatives was designed,synthesized and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis strain H_(37)Rv.Several compounds(2,11a-c,11g,13d,15c)exhibited excellent anti-tubercular activity with an MIC below 1.0μg/mL.Notably,compound 13d showed potential antibacterial effect against both drug-susceptible and multidrug-resistant(MDR)M.tuberculosis with MIC ranges of 0.0625-1.0μg/mL.These results suggest a mode of action different from that of the current anti-mycobacterial drugs rifampicin and isoniazid.Hence,compound 13d is an attractive lead compound for the development of new antitubercular agents.
基金supported by the National Natural Science Foundation of China (Nos. 21472246 and 81321004)the Beijing Natural Science Foundation (No. 7152097)National Mega-Project for Innovation Drugs (No. 2012ZX09103101-037)
文摘A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine（1）and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suitable substituent at the N’-end of matrinic amide might greatly enhance the potency.Among them,matrinic acid 17 and N’-substituted matrinic amides 18a-d exhibited promising potency with low micromolar EC50 values ranging from 1.03μmol/L to 7.54 μmol/L,and better therapeutic window with SI from 66 to 132.Moreover,compound 17 displayed an excellent PK and safety profile in vivo,demonstrating good drug-like characteristics.Thus,it has been selected for further investigation,with an advantage of decreased chances of inducing drug-resistance mutations.
基金supported by the National Natural Science Foundation of China (Nos. 81673307 and 81321004)CAMS Innovation Fund for Medical Sciences (2016–I2M–3–009)
文摘Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus(EBOV)activities. Structure–activity relationship analysis indicated:(i) 12 N-dichlorobenzyl motif was beneficial for the activity;(ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound 7d exhibited the most potent potency against EBOV with an IC_(50) value of 5.29 μmol/L and an SI value of over 37.8. Further in vivo anti-EBOV assay of 7d identified its high effectiveness, and in vivo anti-MARV assay of 7d suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses.
基金supported by the CAMS Innovation Fund for Medical Sciences(nos.2020-I2M-2-010 and 2016-I2M-1-011)the Drug Innovation Major Project(no.2018ZX09711-001)the National Natural Science Foundation of China(no.81974494).
文摘Seven photoaffinity-based and sixteen biotin-based berberine(BBR)probes were constructed and screened for their effects on c-Jun N-terminal protein kinases(JNK)phosphorylation(p-JNK)suppression at the cellular level.Taking active-photoaffinity probe 7c as a chemical tool,we first identified mitogen-activated protein kinase 7(MAP2K7),an upstream protein on the JNK/stress activated protein kinase(SAPK)pathway,as a direct proteomic target of BBR using activity-based protein profiling(ABPP)and other chemical proteomic techniques.Furthermore,BBR’s inhibitory effect on p-JNK was significantly attenuated in both the MAP2K7-knockdown and models,indicating a MAP2K7-dependent inhibition on the JNK signaling pathway.For the first time,we demonstrate the unique mechanism of BBR that directly targets MAP2K7 to inhibit p-JNK rather than JNK activity with the advantages of multiple activities and a good safety profile.
文摘Severe sex ratio imbalance at birth is now becoming an important issue in several Asian countries. Its leading immediate cause is prenatal sex-selective abortion following illegal sex identification by ultrasound scanning. In this paper, a fast automatic recognition and location algorithm for fetal genital organs is proposed as an effective method to help prevent ultrasound technicians from unethically and illegally identifying the sex of the fetus. This automatic recognition algorithm can be divided into two stages. In the 'rough' stage, a few pixels in the image, which are likely to represent the genital organs, are automatically chosen as points of interest (POIs) according to certain salient characteristics of fetal genital organs. In the 'fine' stage, a specifically supervised learning framework, which fuses an effective feature data preprocessing mechanism into the multiple classifier architecture, is applied to every POI. The basic classifiers in the framework are selected from three widely used classifiers: radial basis function network, backpropagation network, and support vector machine. The classification results of all the POIs are then synthesized to determine whether the fetal genital organ is present in the image, and to locate the genital organ within the positive image. Experiments were designed and carried out based on an image dataset comprising 658 positive images (images with fetal genital organs) and 500 negative images (images without fetal genital organs). The experimental results showed true positive (TP) and true negative (TN) results from 80.5% (265 from 329) and 83.0% (415 from 500) of samples, respectively. The average computation time was 453 ms per image.
