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Wyświetlanie 1-3 z 3
Tytuł:
Effect of carboxymethylated pyridoindoles on free radical-induced haemolysis of rat erythrocytes in vitro
Autorzy:
Juskova, Maria
Snirc, Vladimir
Krizanova, Ludmila
Stefek, Milan
Powiązania:
https://bibliotekanauki.pl/articles/1040396.pdf
Data publikacji:
2010
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
pyridoindoles
aldose reductase inhibitors
antioxidants
haemolysis
erythrocytes
oxidative stress
Opis:
Recently novel carboxymethylated pyridoindoles, analogues of the efficient chain-breaking antioxidant stobadine, have been designed, synthesised and characterised as bifunctional compounds with joint antioxidant/aldose reductase inhibitory activities with the potential of preventing diabetic complications. The critical property for the efficacy of the novel aldose reductase inhibitors in vivo is their ability to penetrate into target tissues. In this study, the issue was addressed by measuring the antioxidant activity of compounds 1 [(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid] and 2 [(±)-2-benzyl-(4a,9b)-cis-1,2,3,4,4a,9b-hexahydro-1H-pyrido[4,3-b] indole-8-yl acetic acid] in the cellular system of intact erythrocytes exposed to peroxyl radicals generated by thermal degradation of the azoinitiator 2,2'-azobis(2-amidinopropane) hydrochloride (AAPH) in vitro. Isolated washed rat erythrocytes were incubated in the presence of the azoinitiator AAPH and the compounds tested for increasing periods of time up to 4 h at 37 °C. The degree of haemolysis was determined by absorbance of the haemoglobin released. The onset of AAPH-induced haemolysis was found to be shifted from the starting zero point by the time interval assigned as a lag period. In the presence of the compounds studied the lag period was prolonged significantly. The free radical-initiated haemolysis was retarded by the compounds studied with decreasing efficiency: stobadine > compound 1 ~ Trolox > compound 2. The results have demonstrated an antioxidant activity of the novel carboxymethylated pyridoindoles developed as potential agents for multitarget pharmacology of diabetic complications.
Źródło:
Acta Biochimica Polonica; 2010, 57, 2; 153-156
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Effects of olive leaf polyphenols against H2O2 toxicity in insulin secreting β-cells
Autorzy:
Cumaoğlu, Ahmet
Rackova, Lucia
Stefek, Milan
Kartal, Murat
Maechler, Pierre
Karasu, Çimen
Powiązania:
https://bibliotekanauki.pl/articles/1039946.pdf
Data publikacji:
2011
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
olive
glucose
insulin
hydrogen peroxide
polyphenol
apoptosis
β-cells
oxidative stress
oleuropein
Opis:
In pancreatic β-cells, although H2O2 is a metabolic signal for glucose stimulated insulin secretion, it may induce injury in the presence of increased oxidative stress (OS) as in the case of diabetic chronic hyperglycemia. Olea europea L. (olive) leaves contain polyphenolic compounds that may protect insulin-secreting cells against OS. The major polyphenolic compound in ethanolic olive leaf extract (OLE) is oleuropein (about 20 %), thus we compared the effects of OLE with the effects of standard oleuropein on INS-1 cells. The cells were incubated with increasing concentrations of OLE or oleuropein for 24 h followed by exposure to H2O2 (0.035 mM) for 45 min. H2O2 alone resulted in a significantly decreased viability (MTT assay), depressed glucose-stimulated insulin secretion, increased apoptotic and necrotic cell death (AO/EB staining), inhibited glutathione peroxidase activity (GPx) and stimulated catalase activity that were associated with increased intracellular generation of reactive oxygen species (ROS) (fluorescence DCF). OLE and oleuropein partly improved the viability, attenuated necrotic and apoptotic death, inhibited the ROS generation and improved insulin secretion in H2O2-exposed cells. The effects of oleuropein on insulin secretion were more pronounced than those of OLE, while OLE exerted a stronger anti-cytotoxic effect than oleuropein. Unlike OLE, oleuropein had no significant preserving effect on GPx; however, both compounds stimulated the activity of catalase in H2O2-exposed cells. These findings indicate different modulatory roles of polyphenolic constituents of olive leaves on redox homeostasis that may have a role in the maintenance of β-cell physiology against OS.
Źródło:
Acta Biochimica Polonica; 2011, 58, 1; 45-50
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
[5-(Benzyloxy)-1H-indol-1-yl]acetic acid, an aldose reductase inhibitor and PPARγ ligand
Autorzy:
Soltesova Prnova, Marta
Majekova, Magdalena
Milackova, Ivana
Díez-Dacal, Beatriz
Pérez-Sala, Dolores
Ceyhan, Muserref
Banerjee, Sreeparna
Stefek, Milan
Powiązania:
https://bibliotekanauki.pl/articles/1038997.pdf
Data publikacji:
2015
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
aldose reductase inhibitor
PPARγ ligand
diabetes
indole
Opis:
Based on overlapping structural requirements for both efficient aldose reductase inhibitors and PPAR ligands, [5-(benzyloxy)-1H-indol-1-yl]acetic acid (compound 1) was assessed for inhibition of aldose reductase and ability to interfere with PPARγ. Aldose reductase inhibition by 1 was characterized by IC50 in submicromolar and low micromolar range, for rat and human enzyme, respectively. Selectivity in relation to the closely related rat kidney aldehyde reductase was characterized by approx. factor 50. At organ level in isolated rat lenses, compound 1 significantly inhibited accumulation of sorbitol in a concentration-dependent manner. To identify crucial interactions within the enzyme binding site, molecular docking simulations were performed. Based on luciferase reporter assays, compound 1 was found to act as a ligand for PPARγ, yet with rather low activity. On balance, compound 1 is suggested as a promising lead-like scaffold for agents with the potential to interfere with multiple targets in diabetes.
Źródło:
Acta Biochimica Polonica; 2015, 62, 3; 523-528
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-3 z 3

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