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1.
J Biol Inorg Chem ; 29(2): 251-264, 2024 03.
Artículo en Inglés | MEDLINE | ID: mdl-38494554

RESUMEN

Organometallic η6-arene ruthenium(II) complexes with 3-chloro-6-(1H-pyrazol-1-yl)pyridazine (Ru1, Ru2, and Ru5) and 3-chloro-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine (Ru3-4) N,N' heterocyclic and η6-arene (cymene (Ru1-4) or toluene (Ru 5)) have been synthesized. The ruthenium(II) complexes have common "three-legged piano-stool" pseudo-octahedral structures known for half-sandwich complexes. Evolution of their UV-Visible absorption spectra in PBS buffer or DMSO over 24 h confirmed their good solvolysis stability. Titrations of the complexes with the calf thymus DNA (CT-DNA) were monitored using UV-Visible absorption and fluorescence spectroscopies. The complexes interact moderately with CT-DNA and their binding constants are in the order of 104 M-1. Competitive binding of the complexes to a DNA-Hoechst 33,258 depicted competitive displacement of Hoechst from DNA's minor grooves. These complexes bind to glutathione forming GSH-adducts through S coordination by replacement of a halide, with the iodo-analogues having higher binding constants than the chloro-complexes. Cyclic voltammograms of the complexes exhibited one electron-transfer quasi-reversible process. Trends in the molecular docking data of Ru1-5/DNA were similar to those for DNA binding constants. Of the five, only Ru1, Ru3 and Ru5 showed some activity (moderate) against the MCF-7 breast cancer cells with IC50 values in the range of 59.2-39.9 for which Ru5 was the most active. However, the more difficult-to-treat cell line, MDA-MB 231 cell was recalcitrant to the treatment by these complexes.


Asunto(s)
Antineoplásicos , Complejos de Coordinación , ADN , Glutatión , Rutenio , ADN/química , ADN/metabolismo , Humanos , Rutenio/química , Ligandos , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Complejos de Coordinación/síntesis química , Antineoplásicos/farmacología , Antineoplásicos/química , Antineoplásicos/síntesis química , Glutatión/química , Glutatión/metabolismo , Bovinos , Pirazoles/química , Pirazoles/farmacología , Pirazoles/síntesis química , Animales , Estructura Molecular , Ensayos de Selección de Medicamentos Antitumorales , Proliferación Celular/efectos de los fármacos , Células MCF-7 , Línea Celular Tumoral
2.
Planta Med ; 78(4): 383-6, 2012 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-22234410

RESUMEN

The ripe berries of Harrisonia abyssinica yielded two new prenylated acetophenones, namely 5-(ethan-1'''-one)-4,6-dihydroxy-7-(3'',3''-dimethylallyl)-2 S-(1' S-hydroxy-1',5'-dimethylhex-4'-enyl)-2,3-dihydrobenzofuran (1) and 5-(2'''-hydroxyethan-1'''-one)-4,6-dihydroxy-7-(3'',3''-dimethylallyl)-2 S-(1' S-hydroxy-1',5'-dimethylhex-4'-enyl)-2,3-dihydrobenzofuran (2), herein named harronin I and harronin II, respectively. The compounds were isolated following activity guided fractionation and the structures were determined using 1D, 2D NMR spectroscopic, CD and MS spectrometric techniques. The methanol-dichloromethane mixture (1 : 1 v/v) crude extract exhibited strong antimicrobial activity against Candida albicans, Bacillus cereus, Escherichia coli, Salmonella typhimurium, Staphylococcus aureus, and Lactobacillus casei. Harronin I (1) showed a MIC of 5 µg/mL against C. albicans, 6 µg/mL against B. cereus, and more than 20 µg/mL against other tested microorganisms. Harronin II (2) showed much weaker MIC values (> 100 µg/mL) against all the tested microorganisms.


Asunto(s)
Acetofenonas/farmacología , Antibacterianos/farmacología , Antifúngicos/farmacología , Simaroubaceae/química , Acetofenonas/química , Antibacterianos/química , Antifúngicos/química , Candida albicans/efectos de los fármacos , Frutas/química , Kenia , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Resonancia Magnética Nuclear Biomolecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Prenilación , Staphylococcus aureus/efectos de los fármacos
3.
J Biophys ; 2014: 687028, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25580117

RESUMEN

This study investigated the effects of ultraviolet-A (UV-A) and ultraviolet-C (UV-C) light on the mechanical properties in oyster mushrooms during the growth. Experiments were carried out with irradiation of the mushrooms with UV-A (365 nm) and UV-C (254 nm) light during growth. The exposure time ranged from 10 minutes to 60 minutes at intervals of 10 minutes and irradiation was done for three days. The samples for experimental studies were cut into cylindrical shapes of diameter 12.50 mm and thickness 3.00 mm. The storage modulus, loss modulus, and loss factor of the irradiated samples and control samples were determined for both UV bands and there was a significant difference between the storage modulus, loss modulus, and loss factor of the irradiated samples by both UV bands with reference to the control sample, P < 0.05. UV-C light irradiated samples had higher loss modulus and loss factor but low storage modulus as temperature increased from 35 to 100°C with respect to the control sample while UV-A light irradiated samples had lower loss modulus, low loss factor, and higher storage modulus than UV-C irradiated samples.

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