Transitional ecosystems,estuaries and the coastal seas,are distinctively affected by natural and anthropogenic factors.Organic matter(OM)originating from terrestrial sources is exported by rivers and forms a key compo...Transitional ecosystems,estuaries and the coastal seas,are distinctively affected by natural and anthropogenic factors.Organic matter(OM)originating from terrestrial sources is exported by rivers and forms a key component of the global biogeochemical cycles.Most previous studies focused on the bulk biochemical and anthropogenic aspects affecting these ecosystems.In the present study,we examined the sources and fate of OM entrained within suspended particulate matter(SPM)of the Zuari River and its estuary,west coast of India.Besides using amino acid(AA)enantiomers(L-and D-forms)as biomarkers,other bulk biochemical parameters viz.particulate organic carbon(POC),δ13C,particulate nitrogen(PN),δ15N and chlorophyll a were analyzed.Surprisingly no significant temporal variations were observed in the parameters analyzed;nonetheless,salinity,POC,δ13C,PN,δ15N,glutamic acid,serine,alanine,tyrosine,leucine and D-aspartic acid exhibited significant spatial variability suggesting source differentiation.The POC content displayed weak temporal variability with low values observed during the post-monsoon season attributed to inputs from mixed sources.Estuarine samples were less depleted than the riverine samples suggesting contributions from marine plankton in addition to contributions from river plankton and terrestrial C3 plants detritus.Labile OM was observed during the monsoon and post-monsoon seasons in the estuarine region.More degraded OM was noticed during the pre-monsoon season.Principal component analysis was used to ascertain the sources and factors influencing OM.Principally five factors were extracted explaining 84.52%of the total variance.The first component accounted for 27.10%of the variance suggesting the dominance of tidal influence whereas,the second component accounted for heterotrophic bacteria and their remnants associated with the particulate matter,contributing primarily to the AA pool.Based on this study we ascertained the role of the estuarine turbidity maximum(ETM)controlling the sources of POM and its implications to small tropical rivers.Thus,changes in temporal and regional settings are more likely to affect the natural biogeochemical cycles of small tropical rivers.展开更多
A novel UV-curable prepolymer neopentyl glycol diglycidyl ether diacrylate (NPGGEA) was synthesized by using neopentyl glycol diglycidyl ether (NPGGE) and acrylic acid (AA) as starting materials, N, N-dimethylbenzylam...A novel UV-curable prepolymer neopentyl glycol diglycidyl ether diacrylate (NPGGEA) was synthesized by using neopentyl glycol diglycidyl ether (NPGGE) and acrylic acid (AA) as starting materials, N, N-dimethylbenzylamine as catalyst and p-hydroxyanisole as inhibitor. The optimum synthetic conditions were taken as follows: The concentration of N,N-dimethylbenzylamine, 0.80% of reactants; the concentration of p-hydroxyanisole, 0.3% of reactants; the reaction temperature, 90-110 ; the molar ratio of NPGGE to AA, 1:2.2. Meanwhile, 1-hydroxycyclohexyl phenyl ketone of a UV-cured initiator was added to the synthesized NPGGEA to prepare a kind of UV-cured coating. Mechanical properties of the UV-cured films were determined, giving 28.75 MPa of tensile strength, 923.82 MPa of Young’s modulus and 5.51% of elongation at tear.展开更多
<strong>Background:</strong> <span><span style="font-family:Verdana;">Omega-3 polyunsaturated fatty acids (PUFAs) have some protective benefits for patients with coronary artery and c...<strong>Background:</strong> <span><span style="font-family:Verdana;">Omega-3 polyunsaturated fatty acids (PUFAs) have some protective benefits for patients with coronary artery and cerebrovascular diseases. Eicosapentaenoic acid (EPA) drugs are prescribed as branded (B: EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;">) or generic products but no data exist concerning the differences in treatment outcomes between these products. </span><b><span style="font-family:Verdana;">Methods and Results: </span></b><span style="font-family:Verdana;">We investigated the differences in the serum levels of EPA, docosahexaenoic acid (DHA) and arachidonic acid (AA), and the EPA/AA ratios through blood sampling six months after daily administration of 1800 mg of EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;"> and a generic EPA drug was initiated for 96 patients with cardiovascular diseases. All patients received these PUFA treatments while continuing with baseline therapy. After 6 months of administration, EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;"> produced better results than the generic (G) product (EPA;baseline: 59.4 ± 25.5 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B: 215.5 ± 58.8 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, G: 199.7 ± 63.8 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B vs G, p < 0.0005;AA;baseline: 197.4 ± 44.6 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B: 158.3 ± 36.3 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, G: 163.6 ± 38.9 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B vs G, p < 0.02, as mean ± SD). </span><b><span style="font-family:Verdana;">Conclusions</span></b></span><b><span style="font-family:Verdana;">:</span></b><span style="font-family:Verdana;"> There were clear differences between EPA branded and the generic products. Further study is required to determine whether the benefits from the branded product justify the higher price compared to the generic drug cost.</span>展开更多
A novel spectrofluorimetric method for the determination of L ascorbic acid is proposed. It is based on the inhibition of L ascorbic acid on the formation of 2,3 diaminophenazine, which is an oxidation product of ...A novel spectrofluorimetric method for the determination of L ascorbic acid is proposed. It is based on the inhibition of L ascorbic acid on the formation of 2,3 diaminophenazine, which is an oxidation product of o phenylenediamine catalyzed by laccase .The fluorescence (at λ ex /λ em =464 nm /530 nnm) was enhanced strongly in the presence of organic media . The mechanism of o phenylenediamine oxidation reaction catalyzed by laccase in the presence of L ascorbic acid is discussed .L ascorbic acid is determined in the ethanol, 1,4 dioxane and acetone over the linear range of 4.0×10 -7 ~1.2×10 -4 mol/L, 4.0×10 -7 ~ 8.0×10 -5 mol/L and 4.0×10 -7 ~1.0×10 -4 mol/L with a detection limit of 1.20×10 -8 mol/L,1.19×10 -8 mol/L and 1.24×10 -8 mol/L, respectively. The method has been successfully applied to the simple and rapid determination of L ascorbic acid in pharmaceuticals and milk powder.展开更多
The kinetics of free-radical crosslinking co-polymerization(FRCCP)of acrylic acid(AA)with both methacrylic acid(MA)(PAMA hydrogel)and maleic acid(MAL)(PAMAL hydrogel)was investigated under the conditions of isothermal...The kinetics of free-radical crosslinking co-polymerization(FRCCP)of acrylic acid(AA)with both methacrylic acid(MA)(PAMA hydrogel)and maleic acid(MAL)(PAMAL hydrogel)was investigated under the conditions of isothermal conventional heating(CH)and under the conditions of microwave heating(MWH)with controlled cooling.The kinetics curves of FRCCP of PAMA and PAMAL hydrogels under the conditions of CH are described with the kinetics model of second order chemical reaction,whereas the kinetics curves under the conditions of CH are described with the kinetics model of Polany-Winger.It is proved that MWH leads to the changes in the rate of FRCCP and to the changes in the values of the kinetic parameters activation energy(Ea)and pre-exponential factor(lnA).It was found the existence of relationship between the values of the kinetic parameters calculated for MWH and CH for PAMA and PAMAL hydrogel synthesis process,which is well-known as compensation effect.The effect of MWH on the kinetics of FRCCP for PAMA and PAMAL hydrogel formation were explained by applying the model of activation by selective energy transfer(SET).The changes in kinetics model,rate of FRCCP and kinetics parameters,caused with the MWH can found wide application in designing novel technologies for obtaining polymers and for synthesis of polymers with novel physico-chemical properties.The suggested mechanism of activation for polymerisation under the conditions of MWH also enables development of novel reaction systems and technologies for polymers productions.展开更多
<strong>Background:</strong> Oncolytic herpes simplex virus (oHSV) have been proved effective and safe to treat tumors. Glycoprotein D (gD) has been engineered for targeting cancer cells and de-targeting n...<strong>Background:</strong> Oncolytic herpes simplex virus (oHSV) have been proved effective and safe to treat tumors. Glycoprotein D (gD) has been engineered for targeting cancer cells and de-targeting normal cells successfully, however, the effectiveness and safety of oHSVs still need to be improved. <strong>Method:</strong> Here we sequenced the DNA encoding gD of our recently isolated new strain HSV-1-LXMW and compared the gD amino acid sequence with the gDs of other 7 HSV-1 and 3 HSV-2 strains. <strong>Results:</strong> Phylogenetic analysis revealed that HSV-1-LXMW is evolutionarily close to HSV-1-Patton and -KOS strains. The gD amino acid sequence alignment identified 19 conserved and 8 variable regions. We further predicted 10 new motifs in HSV gD for the first time and identified motif differences in HSV-1 and HSV-2. We summarized the gD-engineered oHSVs and found that some of the newly identified gD motifs are actually functional. <strong>Conclusion:</strong> Our results shed light on HSV gD biology and provided new directions for future gD functional studies and engineering in order to make better oHSVs.展开更多
Tea polyphenols have been shown to have anticancer activity in many studies.In the present study,we investigated effects of theaflavin-3-3'-digallate(TF3),one of the major theaflavin monomers in black tea,in combi...Tea polyphenols have been shown to have anticancer activity in many studies.In the present study,we investigated effects of theaflavin-3-3'-digallate(TF3),one of the major theaflavin monomers in black tea,in combination with ascorbic acid(AA),a reducing agent,and(-)-epigallocatechin-3-gallate(EGCG),the main polyphenol presented in green tea,in combination with AA on cellular viability and cell cycles of the human lung adenocarcinoma SPC-A-1 cells.The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide(MTT) assay showed that the 50% inhibition concentrations(IC50) of TF3,EGCG,and AA on SPC-A-1 cells were 4.78,4.90,and 30.62 μmol/L,respectively.The inhibitory rates of TF3 combined with AA(TF3+AA) and EGCG combined with AA(EGCG+AA) at a molar ratio of 1:6 on SPC-A-1 cells were 54.4% and 45.5%,respectively.Flow cytometry analysis showed that TF3+AA and EGCG+AA obviously increased the cell population in the G0/G1 phase of the SPC-A-1 cell cycle from 53.9% to 62.8% and 60.0%,respectively.TF3-treated cells exhibited 65.3% of the G0/G1 phase at the concentration of its IC50.Therefore,TF3+AA and EGCG+AA had synergistic inhibition effects on the proliferation of SPC-A-1 cells,and significantly held SPC-A-1 cells in G0/G1 phase.The results suggest that the combination of TF3 with AA or EGCG with AA enhances their anticancer activity.展开更多
A rapid and sensitive colorimetric detection of ascorbic acid(AA)through the morphology transformation of silver triangular nanoplates(Ag TNPs)is developed.By virtue of the redox reaction among silver nitrate and A A,...A rapid and sensitive colorimetric detection of ascorbic acid(AA)through the morphology transformation of silver triangular nanoplates(Ag TNPs)is developed.By virtue of the redox reaction among silver nitrate and A A,the newly formed Ag atoms deposited on the surfaces of Ag TNPs.Subsequently,the morphology of Ag TNPs transforms from triangle to circle,resulting in a more than 160 nm blue shift of localized surface plasmon resonance absorption peak.The corresponding color of the solution converting from blue to yellow with the concentration of AA can be observed by naked eyes within 15 min.A linear relationship between the blue shift of absorption peak and the concentration of A A ranging from 0.2 to 6μM is obtained with a limit of detection(LOD)of 100 nM(3σ).Some potential species(e.g.,glucose,urea and various amino acids)coexisting in the system showed little or no interference.The proposed assay is successfully employed to determine the amount of A A in pharmaceutical products with recoveries from 96.9 to 106.5%and offers a sensitive,low-cost,rapid and simple assay of visual analysis of ascorbic acid.展开更多
As a serine hydrolase,monoacylglycerol lipase(MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol(2-AG) in the central nervous system(CNS),leading to the formation of arachidonic acid(AA).Dys...As a serine hydrolase,monoacylglycerol lipase(MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol(2-AG) in the central nervous system(CNS),leading to the formation of arachidonic acid(AA).Dysfunction of MAGL has been associated with multiple CNS disorders and symptoms,including neuroinflammation,cognitive impairment,epileptogenesis,nociception and neurodegenerative diseases.Inhibition of MAGL provides a promising therapeutic direction for the treatment of these conditions,and a MAGL positron emission tomography(PET) probe would greatly facilitate preclinical and clinical development of MAGL inhibitors.Herein,we design and synthesize a small library of fluoropyridyl-containing MAGL inhibitor candidates.Pharmacological evaluation of these candidates by activity-based protein profiling identified 14 as a lead compound,which was then radiolabeled with fluorine-18 via a facile SNAr reaction to form 2-[^(18)F]fluoropyridine scaffold.Good blood-brain barrier permeability and high in vivo specific binding was demonstrated for radioligand [^(18)F]14(also named as [^(18)F]MAGL-1902).This work may serve as a roadmap for clinical translation and further design of potent 18F-labeled MAGL PET tracers.展开更多
基金The National Natural Science Foundation of China under contract No.41530960
文摘Transitional ecosystems,estuaries and the coastal seas,are distinctively affected by natural and anthropogenic factors.Organic matter(OM)originating from terrestrial sources is exported by rivers and forms a key component of the global biogeochemical cycles.Most previous studies focused on the bulk biochemical and anthropogenic aspects affecting these ecosystems.In the present study,we examined the sources and fate of OM entrained within suspended particulate matter(SPM)of the Zuari River and its estuary,west coast of India.Besides using amino acid(AA)enantiomers(L-and D-forms)as biomarkers,other bulk biochemical parameters viz.particulate organic carbon(POC),δ13C,particulate nitrogen(PN),δ15N and chlorophyll a were analyzed.Surprisingly no significant temporal variations were observed in the parameters analyzed;nonetheless,salinity,POC,δ13C,PN,δ15N,glutamic acid,serine,alanine,tyrosine,leucine and D-aspartic acid exhibited significant spatial variability suggesting source differentiation.The POC content displayed weak temporal variability with low values observed during the post-monsoon season attributed to inputs from mixed sources.Estuarine samples were less depleted than the riverine samples suggesting contributions from marine plankton in addition to contributions from river plankton and terrestrial C3 plants detritus.Labile OM was observed during the monsoon and post-monsoon seasons in the estuarine region.More degraded OM was noticed during the pre-monsoon season.Principal component analysis was used to ascertain the sources and factors influencing OM.Principally five factors were extracted explaining 84.52%of the total variance.The first component accounted for 27.10%of the variance suggesting the dominance of tidal influence whereas,the second component accounted for heterotrophic bacteria and their remnants associated with the particulate matter,contributing primarily to the AA pool.Based on this study we ascertained the role of the estuarine turbidity maximum(ETM)controlling the sources of POM and its implications to small tropical rivers.Thus,changes in temporal and regional settings are more likely to affect the natural biogeochemical cycles of small tropical rivers.
基金supported by the National High-Technology Research and Development Program of China (Grant No.2002AA6Z3083)
文摘A novel UV-curable prepolymer neopentyl glycol diglycidyl ether diacrylate (NPGGEA) was synthesized by using neopentyl glycol diglycidyl ether (NPGGE) and acrylic acid (AA) as starting materials, N, N-dimethylbenzylamine as catalyst and p-hydroxyanisole as inhibitor. The optimum synthetic conditions were taken as follows: The concentration of N,N-dimethylbenzylamine, 0.80% of reactants; the concentration of p-hydroxyanisole, 0.3% of reactants; the reaction temperature, 90-110 ; the molar ratio of NPGGE to AA, 1:2.2. Meanwhile, 1-hydroxycyclohexyl phenyl ketone of a UV-cured initiator was added to the synthesized NPGGEA to prepare a kind of UV-cured coating. Mechanical properties of the UV-cured films were determined, giving 28.75 MPa of tensile strength, 923.82 MPa of Young’s modulus and 5.51% of elongation at tear.
文摘<strong>Background:</strong> <span><span style="font-family:Verdana;">Omega-3 polyunsaturated fatty acids (PUFAs) have some protective benefits for patients with coronary artery and cerebrovascular diseases. Eicosapentaenoic acid (EPA) drugs are prescribed as branded (B: EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;">) or generic products but no data exist concerning the differences in treatment outcomes between these products. </span><b><span style="font-family:Verdana;">Methods and Results: </span></b><span style="font-family:Verdana;">We investigated the differences in the serum levels of EPA, docosahexaenoic acid (DHA) and arachidonic acid (AA), and the EPA/AA ratios through blood sampling six months after daily administration of 1800 mg of EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;"> and a generic EPA drug was initiated for 96 patients with cardiovascular diseases. All patients received these PUFA treatments while continuing with baseline therapy. After 6 months of administration, EPADEL</span><sup><span style="font-family:Verdana;"><span style="color:#4F4F4F;font-family:-apple-system, " font-size:14px;white-space:normal;background-color:#ffffff;"="">?</span></span></sup><span style="font-family:Verdana;"> produced better results than the generic (G) product (EPA;baseline: 59.4 ± 25.5 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B: 215.5 ± 58.8 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, G: 199.7 ± 63.8 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B vs G, p < 0.0005;AA;baseline: 197.4 ± 44.6 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B: 158.3 ± 36.3 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, G: 163.6 ± 38.9 </span><span style="font-family:Verdana;">μ</span><span style="font-family:Verdana;">g, B vs G, p < 0.02, as mean ± SD). </span><b><span style="font-family:Verdana;">Conclusions</span></b></span><b><span style="font-family:Verdana;">:</span></b><span style="font-family:Verdana;"> There were clear differences between EPA branded and the generic products. Further study is required to determine whether the benefits from the branded product justify the higher price compared to the generic drug cost.</span>
文摘A novel spectrofluorimetric method for the determination of L ascorbic acid is proposed. It is based on the inhibition of L ascorbic acid on the formation of 2,3 diaminophenazine, which is an oxidation product of o phenylenediamine catalyzed by laccase .The fluorescence (at λ ex /λ em =464 nm /530 nnm) was enhanced strongly in the presence of organic media . The mechanism of o phenylenediamine oxidation reaction catalyzed by laccase in the presence of L ascorbic acid is discussed .L ascorbic acid is determined in the ethanol, 1,4 dioxane and acetone over the linear range of 4.0×10 -7 ~1.2×10 -4 mol/L, 4.0×10 -7 ~ 8.0×10 -5 mol/L and 4.0×10 -7 ~1.0×10 -4 mol/L with a detection limit of 1.20×10 -8 mol/L,1.19×10 -8 mol/L and 1.24×10 -8 mol/L, respectively. The method has been successfully applied to the simple and rapid determination of L ascorbic acid in pharmaceuticals and milk powder.
基金the Ministry of Science and Technical Development of the Republic of Serbia,through Project No.172015 OI.
文摘The kinetics of free-radical crosslinking co-polymerization(FRCCP)of acrylic acid(AA)with both methacrylic acid(MA)(PAMA hydrogel)and maleic acid(MAL)(PAMAL hydrogel)was investigated under the conditions of isothermal conventional heating(CH)and under the conditions of microwave heating(MWH)with controlled cooling.The kinetics curves of FRCCP of PAMA and PAMAL hydrogels under the conditions of CH are described with the kinetics model of second order chemical reaction,whereas the kinetics curves under the conditions of CH are described with the kinetics model of Polany-Winger.It is proved that MWH leads to the changes in the rate of FRCCP and to the changes in the values of the kinetic parameters activation energy(Ea)and pre-exponential factor(lnA).It was found the existence of relationship between the values of the kinetic parameters calculated for MWH and CH for PAMA and PAMAL hydrogel synthesis process,which is well-known as compensation effect.The effect of MWH on the kinetics of FRCCP for PAMA and PAMAL hydrogel formation were explained by applying the model of activation by selective energy transfer(SET).The changes in kinetics model,rate of FRCCP and kinetics parameters,caused with the MWH can found wide application in designing novel technologies for obtaining polymers and for synthesis of polymers with novel physico-chemical properties.The suggested mechanism of activation for polymerisation under the conditions of MWH also enables development of novel reaction systems and technologies for polymers productions.
文摘<strong>Background:</strong> Oncolytic herpes simplex virus (oHSV) have been proved effective and safe to treat tumors. Glycoprotein D (gD) has been engineered for targeting cancer cells and de-targeting normal cells successfully, however, the effectiveness and safety of oHSVs still need to be improved. <strong>Method:</strong> Here we sequenced the DNA encoding gD of our recently isolated new strain HSV-1-LXMW and compared the gD amino acid sequence with the gDs of other 7 HSV-1 and 3 HSV-2 strains. <strong>Results:</strong> Phylogenetic analysis revealed that HSV-1-LXMW is evolutionarily close to HSV-1-Patton and -KOS strains. The gD amino acid sequence alignment identified 19 conserved and 8 variable regions. We further predicted 10 new motifs in HSV gD for the first time and identified motif differences in HSV-1 and HSV-2. We summarized the gD-engineered oHSVs and found that some of the newly identified gD motifs are actually functional. <strong>Conclusion:</strong> Our results shed light on HSV gD biology and provided new directions for future gD functional studies and engineering in order to make better oHSVs.
基金supported by the Key Program of Science and Technology of Zhejiang Province(No.2007C12068)of Chinathe National Natural Science Foundation of China(No.30901002)
文摘Tea polyphenols have been shown to have anticancer activity in many studies.In the present study,we investigated effects of theaflavin-3-3'-digallate(TF3),one of the major theaflavin monomers in black tea,in combination with ascorbic acid(AA),a reducing agent,and(-)-epigallocatechin-3-gallate(EGCG),the main polyphenol presented in green tea,in combination with AA on cellular viability and cell cycles of the human lung adenocarcinoma SPC-A-1 cells.The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide(MTT) assay showed that the 50% inhibition concentrations(IC50) of TF3,EGCG,and AA on SPC-A-1 cells were 4.78,4.90,and 30.62 μmol/L,respectively.The inhibitory rates of TF3 combined with AA(TF3+AA) and EGCG combined with AA(EGCG+AA) at a molar ratio of 1:6 on SPC-A-1 cells were 54.4% and 45.5%,respectively.Flow cytometry analysis showed that TF3+AA and EGCG+AA obviously increased the cell population in the G0/G1 phase of the SPC-A-1 cell cycle from 53.9% to 62.8% and 60.0%,respectively.TF3-treated cells exhibited 65.3% of the G0/G1 phase at the concentration of its IC50.Therefore,TF3+AA and EGCG+AA had synergistic inhibition effects on the proliferation of SPC-A-1 cells,and significantly held SPC-A-1 cells in G0/G1 phase.The results suggest that the combination of TF3 with AA or EGCG with AA enhances their anticancer activity.
基金Key Lab of Process Analysis and Control of Sichuan Universities(No.2019003)provided support for this projectsponsored by the Chongqing Talent Program(Leading Talent)
文摘A rapid and sensitive colorimetric detection of ascorbic acid(AA)through the morphology transformation of silver triangular nanoplates(Ag TNPs)is developed.By virtue of the redox reaction among silver nitrate and A A,the newly formed Ag atoms deposited on the surfaces of Ag TNPs.Subsequently,the morphology of Ag TNPs transforms from triangle to circle,resulting in a more than 160 nm blue shift of localized surface plasmon resonance absorption peak.The corresponding color of the solution converting from blue to yellow with the concentration of AA can be observed by naked eyes within 15 min.A linear relationship between the blue shift of absorption peak and the concentration of A A ranging from 0.2 to 6μM is obtained with a limit of detection(LOD)of 100 nM(3σ).Some potential species(e.g.,glucose,urea and various amino acids)coexisting in the system showed little or no interference.The proposed assay is successfully employed to determine the amount of A A in pharmaceutical products with recoveries from 96.9 to 106.5%and offers a sensitive,low-cost,rapid and simple assay of visual analysis of ascorbic acid.
基金the financial support from the NIH grants (DA038000 and DA043507 to S. H. L. and DA033760 to B. F. C.)the Swiss National Science Foundation for a postdoctoral fellowship to Michael A. Schafroth (Grant No. P2EZP3_175137, Switzerland)。
文摘As a serine hydrolase,monoacylglycerol lipase(MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol(2-AG) in the central nervous system(CNS),leading to the formation of arachidonic acid(AA).Dysfunction of MAGL has been associated with multiple CNS disorders and symptoms,including neuroinflammation,cognitive impairment,epileptogenesis,nociception and neurodegenerative diseases.Inhibition of MAGL provides a promising therapeutic direction for the treatment of these conditions,and a MAGL positron emission tomography(PET) probe would greatly facilitate preclinical and clinical development of MAGL inhibitors.Herein,we design and synthesize a small library of fluoropyridyl-containing MAGL inhibitor candidates.Pharmacological evaluation of these candidates by activity-based protein profiling identified 14 as a lead compound,which was then radiolabeled with fluorine-18 via a facile SNAr reaction to form 2-[^(18)F]fluoropyridine scaffold.Good blood-brain barrier permeability and high in vivo specific binding was demonstrated for radioligand [^(18)F]14(also named as [^(18)F]MAGL-1902).This work may serve as a roadmap for clinical translation and further design of potent 18F-labeled MAGL PET tracers.