Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecule...Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecules due to the restricted structural features to serve in the laser desorption/ionization mechanism with a problem of background signals appearing in the low mass region. This paper describes the application of Schiff base derivatives of acylhydrazide and isatin as alternate UV-LDI matrices for the analysis of peptides with significantly low background signals. Thirty one compounds have been successfully employed as matrices for the analysis of low molecular weight (LMW) peptides (α-Cyano-4-hydroxycinnamic acid (HCCA), a preferred choice for peptide analysis.展开更多
A type of unique azole-hybridized acylhydrazonyl aloe emodins(AAEs)were developed as new antibacterial agents for combating bacterial infections.Some target AAEs showed strong antibacterial activities,especially,tetra...A type of unique azole-hybridized acylhydrazonyl aloe emodins(AAEs)were developed as new antibacterial agents for combating bacterial infections.Some target AAEs showed strong antibacterial activities,especially,tetrazolylthioether AAE 27a exhibited broad antibacterial spectrum with 16-256 folds and 8-64 folds more active antibacterial efficacy than the reference drugs aloe emodin and norfloxacin,respectively.Tetrazolylthioether AAE 27a also gave low hemolysis and cytotoxicity,as well as favorable bioavailability.Preliminary mechanism explorations revealed that tetrazolylthioether AAE 27a could cause bacterial membrane depolarization and damage the cell membrane,resulting in nucleic acid leakage.Moreover,compound 27a could intercalate into DNA to impede its replication and form supramolecular 27a-DNA gyrase complex to disturb the function of DNA gyrase.These findings would provide valuable insights for the further exploration of azolyl acylhydrazonyl aloe emodins as new potential antibacterial candidates.展开更多
文摘Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecules due to the restricted structural features to serve in the laser desorption/ionization mechanism with a problem of background signals appearing in the low mass region. This paper describes the application of Schiff base derivatives of acylhydrazide and isatin as alternate UV-LDI matrices for the analysis of peptides with significantly low background signals. Thirty one compounds have been successfully employed as matrices for the analysis of low molecular weight (LMW) peptides (α-Cyano-4-hydroxycinnamic acid (HCCA), a preferred choice for peptide analysis.
基金supported by the National Natural Science Foundation of China(No.21971212)the Key Project of Innovation Research 2035 Pilot Plan of Southwest University(SWU-XDZD22007).
文摘A type of unique azole-hybridized acylhydrazonyl aloe emodins(AAEs)were developed as new antibacterial agents for combating bacterial infections.Some target AAEs showed strong antibacterial activities,especially,tetrazolylthioether AAE 27a exhibited broad antibacterial spectrum with 16-256 folds and 8-64 folds more active antibacterial efficacy than the reference drugs aloe emodin and norfloxacin,respectively.Tetrazolylthioether AAE 27a also gave low hemolysis and cytotoxicity,as well as favorable bioavailability.Preliminary mechanism explorations revealed that tetrazolylthioether AAE 27a could cause bacterial membrane depolarization and damage the cell membrane,resulting in nucleic acid leakage.Moreover,compound 27a could intercalate into DNA to impede its replication and form supramolecular 27a-DNA gyrase complex to disturb the function of DNA gyrase.These findings would provide valuable insights for the further exploration of azolyl acylhydrazonyl aloe emodins as new potential antibacterial candidates.
