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1.
ACS Omega ; 7(41): 36786-36794, 2022 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-36278105

RESUMO

To enhance the infrared radiation efficiency and the heat transfer performance simultaneously, graphene (Gr) was synthesized in situ on hexagonal boron nitride (h-BN) to prepare Gr/h-BN composites by a scalable combustion synthesis in CO2 atmosphere using Mg as sacrificial solder. The synthesized Gr/h-BN composites were added in polydimethylsiloxane polymer to prepare composite coatings, which show an infrared emissivity greater than 0.95 and a through-plane thermal conductivity up to 2.584 W·m-1·K-1. When functioning on an Al heatsink, such a composite coating can reduce the temperature by as much as 21.7 °C. Meanwhile, the composite coating exhibits superior adhesion on the Al substrate. Therefore, Gr/h-BN composite coatings with noteworthy infrared radiation and thermal conductivity are expected to be a promising candidate for heat dissipation applications.

2.
ChemMedChem ; 16(22): 3477-3483, 2021 11 19.
Artigo em Inglês | MEDLINE | ID: mdl-34313010

RESUMO

The peroxiredoxin 5 (PRDX5) is a member of peroxiredoxins with antitumor activity. However, as a recombinant protein, PRDX5 is restricted in clinic due to high cost and keeping high dose in medication. The alternative way is to explore the antitumor active fragments of PRDX5 for potential of peptide drugs. According to the sequence, crystal structure and enzyme function of PRDX5, seven peptides were designed and named as IMB-P1∼7. The peptide IMB-P1 (AFTPGCSKTHLPGFVEQAEAL) containing critical residue C47 exhibited antitumor activity similar to PRDX5 in vivo. Transcriptome analysis showed peptide IMB-P1 could make influence on expression of multiple genes involved in tumorigenesis and deterioration. Besides, an important discovery is the down-regulation of oxidation-related genes. In CT26 cells, IMB-P1 carried similar antitumor activity with increasing ROS level to intact PRDX5. The results demonstrated that peptide IMB-P1 with easier synthesis from PRDX5 may serve as a promising antitumor candidate.


Assuntos
Antineoplásicos/farmacologia , Peptídeos/farmacologia , Peroxirredoxinas/química , Sequência de Aminoácidos , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Peptídeos/síntese química , Peptídeos/química , Conformação Proteica , Alinhamento de Sequência
3.
J Nat Prod ; 81(1): 178-187, 2018 01 26.
Artigo em Inglês | MEDLINE | ID: mdl-29308897

RESUMO

Analysis of the whole genome sequence of Streptomyces sp. IMB7-145 revealed the presence of seven type I polyketide synthase biosynthetic gene clusters, one of which was highly homologous to the biosynthetic gene cluster of azalomycin F. Detailed bioinformatic analysis of the modular organization of the PKS gene suggested that this gene is responsible for niphimycin biosynthesis. Guided by genomic analysis, a large-scale cultivation ultimately led to the discovery and characterization of four new niphimycin congeners, namely, niphimycins C-E (1-3) and 17-O-methylniphimycin (4). The configurations of most stereocenters of niphimycins have not been determined to date. In the present study, the relative configurations were elucidated by spectroscopic analysis, including J-based analysis and the CNMR database method. Further, the full absolute configurations of niphimycins were completely proposed for the first time based on biosynthetic gene cluster analysis of the ketoreductase and enoylreductase domains for hydroxy- and methyl-bearing stereocenters. Compounds 1, 3, 4, and niphimycin Iα (5) showed antimicrobial activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci (MIC: 8-64 µg/mL), as well as cytotoxicity against the human HeLa cancer cell line (IC50: 3.0-9.0 µM). In addition, compounds 1 and 5 displayed significant activity against several Mycobacterium tuberculosis clinical isolates (MIC: 4-32 µg/mL).


Assuntos
Organismos Aquáticos/química , Streptomyces/química , Streptomyces/genética , Antibacterianos/química , Antibacterianos/farmacologia , Linhagem Celular Tumoral , Genômica/métodos , Guanidinas/química , Guanidinas/farmacologia , Células HeLa , Células Hep G2 , Humanos , Células K562 , Células MCF-7 , Macrolídeos/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Família Multigênica/genética , Policetídeo Sintases/genética
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