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1.
ACS Appl Bio Mater ; 6(11): 4814-4827, 2023 11 20.
Artigo em Inglês | MEDLINE | ID: mdl-37886889

RESUMO

Bacterial infections and persistent inflammation can impede the intrinsic healing process of wounds. To combat this issue, researchers have delved into the potential use of carbon dots (CDs) in the regulation of inflammation and counteract infections. These CDs were synthesized using a microwave-assisted hydrothermal process and have demonstrated outstanding antibacterial and antibiofilm properties against Gram-positive and Gram-negative bacteria. Additionally, CDs displayed biocompatibility at therapeutic concentrations and the ability to specifically target mitochondria. CD treatment effectively nullified lipopolysaccharide-triggered reactive oxygen species production by macrophages, while simultaneously promoting macrophage polarization toward an anti-inflammatory phenotype (M2), leading to a reduction in inflammation and an acceleration in wound healing. In vitro scratch assays also revealed that CDs facilitated the tissue-repairing process by stimulating epithelial cell migration during reepithelialization. In vivo studies using CDs topically applied to lipopolysaccharide (LPS)-stimulated wounds in C57/BL6 mice demonstrated significant improvements in wound healing due to enhanced fibroblast proliferation, angiogenesis, and collagen deposition. Crucially, histological investigations showed no indications of systemic toxicity in vital organs. Collectively, the application of CDs has shown immense potential in speeding up the wound-healing process by regulating inflammation, preventing bacterial infections, and promoting tissue repair. These results suggest that further clinical translation of CDs should be considered.


Assuntos
Antibacterianos , Infecções Bacterianas , Camundongos , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Lipopolissacarídeos/farmacologia , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Cicatrização , Macrófagos , Inflamação
2.
Nat Prod Res ; 37(15): 2568-2574, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35343322

RESUMO

Piscidinol A (1), a major compound isolated from Aphanamixis polystachya, showed modest anticancer activity against cancer cell lines. Subsequently, a series of analogues were synthesised by modification of the key structural functionalities of this high yield natural product and assessed for their anticancer potential against various cancer cell lines. Among the tested derivatives, the compounds 6e and 6i are significantly reduced the cell viability at 5.38 and 5.02 µM against DU145 prostate cancer cells, respectively. Additionally, both the compounds arrested the cell cycle at S phase and induced the late apoptosis in DU145 cells. Together, the results demonstrated that the compounds 6e and 6i could be a promising lead for the development of anticancer agents against DU145 and well worth further investigation aiming to generate potential anticancer agents.


Assuntos
Antineoplásicos , Masculino , Humanos , Relação Estrutura-Atividade , Linhagem Celular Tumoral , Proliferação de Células , Antineoplásicos/farmacologia , Antineoplásicos/química , Apoptose , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular
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