The potential application of a designed self-assembly peptide CH3CO-Pro-Thr-Phe-CysPhe-Lys-Phe-Glu-Pro-NH2(named as P1) as a carrier of 5-Fluorouracil(5-Fu) for controlled release in vitro was studied. 5-Fluoroura...The potential application of a designed self-assembly peptide CH3CO-Pro-Thr-Phe-CysPhe-Lys-Phe-Glu-Pro-NH2(named as P1) as a carrier of 5-Fluorouracil(5-Fu) for controlled release in vitro was studied. 5-Fluorouracil(5-Fu) was selected as a representative anticancer drug due to its extensive use in treating digestive system cancer and breast cancer. The interaction between P1 and 5-Fu was detected by fluorescent quenching experiments and atomic force microscopy(AFM). The quenching mechanism of 5-Fu and P1 system was dynamic by performing fluorescent quenching experiments at different temperatures. The thermodynamic analysis demonstrated that the interaction between 5-Fu and P1 was hydrophobic interaction. The complexes prepared by the interaction between peptide and 5-Fu appeared as large granular particles of about 20 nm in height under AFM(denoted as5-Fu-P1), 24 times larger than the original 5-Fu particles. According to the results, an interaction model was proposed. Furthermore, 5-Fu-P1 complexes exhibited an efficient controlled release of 5-Fu in vitro. The research suggested that P1 might be a candidate carrier for drug delivery, providing a substitution agent for 5-Fu.展开更多
The interactions between the new organometallic complexes, ferrocenesubstituted dithioocarborane conjugates (denoted as FcSB1, FcSB2 and FcSBCO) and hemoglobin (Hb) are investigated by electrochemistry, fluorescen...The interactions between the new organometallic complexes, ferrocenesubstituted dithioocarborane conjugates (denoted as FcSB1, FcSB2 and FcSBCO) and hemoglobin (Hb) are investigated by electrochemistry, fluorescence and UVvis absorption spectroscopy. The results demonstrate that FcSB1, FcSB2 and FcSBCO can bind to the heme iron center through the replacement of the weakly bound H20/02 in the distal heme pocket of Hb by their sulfur donor atoms, inducing the allosteric change from the R state (oxygenated conformation, relax) to T state (deoxygenated conformation, tense). The binding affinity is in the order of FcSBCO〉FeSB2〉FeSB1. Moreover, the fluorescence study illustrates that the three ferrocenecarborane conjugates differently affect the quarterly and tertiary structures as well as the polarity in the surrounding of the Trp and Tyr residues in Hb. Typically, FcSB2 mainly induces alterations of the microenvironment around the 1337Trp residue which is located on the cql32 interface of Hb. Such distinct influences are attributed to the structural features of FcSB1, FcSB2 and FcSBCO containing hydrophobic ferrocenyl and carboranyl units as well as C=O group. Screening the proteinbinding behavior can signify the potential bioactivity of such molecules and may be helpful in the future development of promising multifunctional metallodrugs.展开更多
Critical algal blooms in great lakes increase the level of algal organic matters(AOMs),significantly altering the composition of natural organic matters(NOMs) in freshwater of lake.This study examined the AOM's c...Critical algal blooms in great lakes increase the level of algal organic matters(AOMs),significantly altering the composition of natural organic matters(NOMs) in freshwater of lake.This study examined the AOM's characteristics of Nitzschia palea(N.palea),one kind of the predominant diatom and an important biomarker of water quality in the great lakes of China,to investigate the effect of AOMs on the variation of NOMs in lakes and the process of algal energy.Excitation–emission matrix fluorescence(EEM) spectroscopy,synchronous fluorescence(SF) spectroscopy and deconvolution UV–vis(D-UV) spectroscopy were utilized to characterize AOMs to study the effects of nutrient loading on the composition change of AOMs.From results,it was revealed that the phosphorus is the limiting factor for N.palea's growth and the generation of both total organic carbon and amino acids but the nitrogen is more important for the generation of carbohydrates and proteins.EEM spectra revealed differences in the composition of extracellular organic matter and intracellular organic matter.Regardless of the nitrogen and phosphorus concentrations,aromatic proteins and soluble microbial products were the main components,but the nitrogen concentration had a significant impact on their composition.The SF spectra were used to study the AOMs for the first time and identified that the protein-like substances were the major component of AOMs,creating as a result of aromatic group condensation.The D-UV spectra showed carboxylic acid and esters were the main functional groups in the EOMs,with –OCH_3,–SO_2NH_2,–CN,–NH_2,–O– and –COCH_3functional groups substituting into benzene rings.展开更多
基金Supported by the National Natural Science Foundation of China(Nos.51003065 and 81000658)New Teachers’Fund for Doctor Stations,and Ministry of Education(No.20100181120077)
文摘The potential application of a designed self-assembly peptide CH3CO-Pro-Thr-Phe-CysPhe-Lys-Phe-Glu-Pro-NH2(named as P1) as a carrier of 5-Fluorouracil(5-Fu) for controlled release in vitro was studied. 5-Fluorouracil(5-Fu) was selected as a representative anticancer drug due to its extensive use in treating digestive system cancer and breast cancer. The interaction between P1 and 5-Fu was detected by fluorescent quenching experiments and atomic force microscopy(AFM). The quenching mechanism of 5-Fu and P1 system was dynamic by performing fluorescent quenching experiments at different temperatures. The thermodynamic analysis demonstrated that the interaction between 5-Fu and P1 was hydrophobic interaction. The complexes prepared by the interaction between peptide and 5-Fu appeared as large granular particles of about 20 nm in height under AFM(denoted as5-Fu-P1), 24 times larger than the original 5-Fu particles. According to the results, an interaction model was proposed. Furthermore, 5-Fu-P1 complexes exhibited an efficient controlled release of 5-Fu in vitro. The research suggested that P1 might be a candidate carrier for drug delivery, providing a substitution agent for 5-Fu.
基金supported by the National Basic Research Program of China (2010CB732404, 2010CB923303)the National Natural Science Foundation of China (21175020, 90713023, 20925104)+4 种基金the Project of High Technology Research and Development Program of China (2007AA022007)Gongdong Province (2011B090400357)the Natural Science Foundation of Jiangsu Province (BK2008149, BK2010052)C. W. acknowledges the Fundamental Research Funds for the Central Universities (ZYGX2011J099)the support by the Open Research Fund of State Key Laboratory of Bioelectronics, Southeast University (2011E09)
文摘The interactions between the new organometallic complexes, ferrocenesubstituted dithioocarborane conjugates (denoted as FcSB1, FcSB2 and FcSBCO) and hemoglobin (Hb) are investigated by electrochemistry, fluorescence and UVvis absorption spectroscopy. The results demonstrate that FcSB1, FcSB2 and FcSBCO can bind to the heme iron center through the replacement of the weakly bound H20/02 in the distal heme pocket of Hb by their sulfur donor atoms, inducing the allosteric change from the R state (oxygenated conformation, relax) to T state (deoxygenated conformation, tense). The binding affinity is in the order of FcSBCO〉FeSB2〉FeSB1. Moreover, the fluorescence study illustrates that the three ferrocenecarborane conjugates differently affect the quarterly and tertiary structures as well as the polarity in the surrounding of the Trp and Tyr residues in Hb. Typically, FcSB2 mainly induces alterations of the microenvironment around the 1337Trp residue which is located on the cql32 interface of Hb. Such distinct influences are attributed to the structural features of FcSB1, FcSB2 and FcSBCO containing hydrophobic ferrocenyl and carboranyl units as well as C=O group. Screening the proteinbinding behavior can signify the potential bioactivity of such molecules and may be helpful in the future development of promising multifunctional metallodrugs.
基金the support of Fundamental Research Funds for the Central Universities (No.2015ZCQ-HJ-02)the National Natural Science Foundation of China (Nos.51578520,51378063,41273137 and 51108030)+1 种基金the Beijing Natural Science Foundation (No.8132033)Open Project of State Key Laboratory of Urban Water Resource and Environment,Harbin Institute of Technology (No.QAK201306)
文摘Critical algal blooms in great lakes increase the level of algal organic matters(AOMs),significantly altering the composition of natural organic matters(NOMs) in freshwater of lake.This study examined the AOM's characteristics of Nitzschia palea(N.palea),one kind of the predominant diatom and an important biomarker of water quality in the great lakes of China,to investigate the effect of AOMs on the variation of NOMs in lakes and the process of algal energy.Excitation–emission matrix fluorescence(EEM) spectroscopy,synchronous fluorescence(SF) spectroscopy and deconvolution UV–vis(D-UV) spectroscopy were utilized to characterize AOMs to study the effects of nutrient loading on the composition change of AOMs.From results,it was revealed that the phosphorus is the limiting factor for N.palea's growth and the generation of both total organic carbon and amino acids but the nitrogen is more important for the generation of carbohydrates and proteins.EEM spectra revealed differences in the composition of extracellular organic matter and intracellular organic matter.Regardless of the nitrogen and phosphorus concentrations,aromatic proteins and soluble microbial products were the main components,but the nitrogen concentration had a significant impact on their composition.The SF spectra were used to study the AOMs for the first time and identified that the protein-like substances were the major component of AOMs,creating as a result of aromatic group condensation.The D-UV spectra showed carboxylic acid and esters were the main functional groups in the EOMs,with –OCH_3,–SO_2NH_2,–CN,–NH_2,–O– and –COCH_3functional groups substituting into benzene rings.