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1.
Chem Asian J ; 19(6): e202301081, 2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38377056

RESUMO

A series of novel styryl dye derivatives incorporating indolium and quinolinium core structures were successfully synthesized to explore their interacting and binding capabilities with tau aggregates in vitro and in cells. The synthesized dyes exhibited enhanced fluorescence emission in viscous environments due to the rotatable bond confinement in the core structure. Dye 4, containing a quinolinium moeity and featuring two cationic sites, demonstrated a 28-fold increase in fluorescence emission upon binding to tau aggregates. This dye could also stain tau aggregates in living cells, confirmed by cell imaging using confocal fluorescence microscopy. A molecular docking study was conducted to provide additional visualization and support for binding interactions. This work offers novel and non-cytotoxic fluorescent probes with desirable photophysical properties, which could potentially be used for studying tau aggregates in living cells, prompting further development of new fluorescent probes for early Alzheimer's disease detection.


Assuntos
Corantes Fluorescentes , Corantes Fluorescentes/química , Simulação de Acoplamento Molecular , Microscopia de Fluorescência
2.
Fitoterapia ; 173: 105781, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38128619

RESUMO

Six anthraquinones were isolated from Morinda scabrida Craib, an unexplored species of Morinda found in the tropical forest of Thailand. All six anthraquinones showed cytotoxicity against A549 lung cancer cells, with the most active compound, nordamnacanthal (MS01), exhibiting the IC50 value of 16.3 ± 2.5 µM. The cytotoxic effect was dose-dependent and led to cell morphological changes characteristic of apoptosis. In addition, flow cytometric analysis showed dose-dependent apoptosis induction and the G2/M phase cell cycle arrest, which was in agreement with the tubulin polymerization inhibitory activity of MS01. Molecular docking analysis illustrated the binding between MS01 and the α/ß-tubulin heterodimer at the colchicine binding site, and UV-visible absorption spectroscopy revealed the DNA binding capacity of MS01.


Assuntos
Neoplasias Pulmonares , Morinda , Humanos , Estrutura Molecular , Morinda/química , Proliferação de Células , Linhagem Celular Tumoral , Polimerização , Neoplasias Pulmonares/tratamento farmacológico , Simulação de Acoplamento Molecular , Tubulina (Proteína)/química , Tubulina (Proteína)/metabolismo , Antraquinonas/farmacologia , Moduladores de Tubulina/farmacologia , Moduladores de Tubulina/química , Moduladores de Tubulina/metabolismo
3.
Artigo em Inglês | MEDLINE | ID: mdl-24263127

RESUMO

A series of novel, highly selective azo dye-thiosemicarbazones based anion sensors (3e-f) have been synthesized from the condensation reaction between thiosemicarbazide and six different azo salicylaldehydes. The structure of the sensors was confirmed by spectroscopic methods. The selectivity and sensitivity in the recognition for acetate anion over other anions such as fluoride, chloride, iodide and dihydrogenphosphate anions were determined by naked-eyes and UV-vis spectra. The color of the solution containing sensor had an obvious change from light yellow to orange only after the addition of acetate anion in aqueous solution (water/dimethylsulfoxide, 7:3, v/v) while other anions did not cause obvious color change. The anion recognition property of the receptor via proton-transfer is monitored by UV-vis titration and (1)H NMR spectroscopy. Under condition in aqueous solution of sensor 3e (water/dimethylsulfoxide, 7:3, v/v), linearity range for the quantification of acetate anion was 1-22 µM and limit of detection (LOD) of acetate anion was 0.71 µM.


Assuntos
Ânions/análise , Compostos Azo/síntese química , Colorimetria/instrumentação , Colorimetria/métodos , Corantes/química , Tiossemicarbazonas/síntese química , Compostos Azo/química , Dimetil Sulfóxido/química , Espectroscopia de Ressonância Magnética , Espectrofotometria Ultravioleta , Tiossemicarbazonas/química , Água/química
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