Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:1.6.3.1 (NADPH oxidase)
 11,281 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We tested the relative efficacy of free dexamethasone, dexamethasone containing liposomes and free liposomes in preventing superoxide anion, O-2 generation by neutrophils. O-2 production by 5 x 10(5) neutrophils, whether primed or not with lipopolysaccharide, was stimulated by phorbol 12-myristate 13-acetate (PMA) to 13.4 +/- 1.3 nmoles after 15 minutes compared to 1.2 +/- 0.3 nmoles with nonstimulated cells. Free liposomes but not dexamethasone (dexa) decreased non-stimulated as well as PMA-induced O-2 generation. Dexa-containing phosphatidylcholine from egg yolk: phosphatidylserine from bovine brain (PC:PS 7:3) liposomes, unlike free dexa, diminished PMA-stimulated O-2 production in a dose-dependent manner with a maximal effect at 37.5 micrograms/ml phospholipid (6.6 +/- 1.6 nmoles). The kinetics of cytochrome-c reduction revealed that decreased O-2 production resulted from an extended lag-time of release to almost 8 minutes with PMA induction and consequently led to the conclusion that liposomes modified the activity of NADPH oxidase as well as that of protein kinase C. Liposomes prepared with PC and PS of natural origin had a greater inhibitory effect on O-2 generation by neutrophils than dipalmitoylphosphatidylcholine (DPPC) and phosphatidylethanolamine from egg yolk (PE):PC (3:1) liposomes. When 100 microM of Ca2+ was added to the medium, the inhibitory action of liposomes prepared with egg yolK PC and DPPC was increased by 30 and 60% respectively, while that of PS and PE:PC was prevented. We also verified that liposomes by themselves, even if phagocytized, did not induce O-2 generation or its concentration was too low to be detected by this technique. From the clinical point of view, some formulations delayed non-induced and PMA-induced O-2 generation, thus adding to the anti-inflammatory effect of the glucocorticoid they transported.
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PMID:Modulation of noninduced and phorbol ester-induced generation of superoxide anion by free liposomes and liposomes containing dexamethasone. 904 63

The antioxidant activity of molecules constitutes an important factor for the regulation of redox homeostasis and reduction of the oxidative stress. Cells affected by oxidative stress can undergo genetic alteration, causing structural changes and promoting the onset of chronic diseases, such as cancer. We have performed an in silico study to evaluate the antioxidant potential of two molecules of the zinc database: ZINC08706191 (Z91) and ZINC08992920 (Z20). Molecular docking, quantum chemical calculations (HF/6-31G**) and Pearson's correlation have been performed. Molecular docking results of Z91 and Z20 showed both the lower binding affinity (BA) and inhibition constant (Ki) values for the receptor-ligand interactions in the three tested enzymes (cytochrome P450-CP450, myeloperoxidase-MP and NADPH oxidase-NO) than the control molecules (5-fluorouracil-FLU, melatonin-MEL and dextromethorphan-DEX, for each receptor respectively). Molecular descriptors were correlated with Ki and strong correlations were observed for the CP450, MP and NO receptors. These and other results attest the significant antioxidant ability of Z91 and Z20, that may be indicated for further analyses in relation to the control of oxidative stress and as possible antioxidant agents to be used in the pharmaceutical industry.
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PMID:An In Silico Study of the Antioxidant Ability for Two Caffeine Analogs Using Molecular Docking and Quantum Chemical Methods. 3038 Jun