http://www.sciencedirect.com/science/article/B6T12-4V0MTG8-1/2/7b7f3913eea3a6f05047e8c1927696a9
Suppression of estrogen biosynthesis by aromatase inhibition is an effective approach for the treatment of hormone sensitive breast cancer. Third generation non-steroid aromatase inhibitors have shown important benefits in recent clinical trials with postmenopausal women. In this study we have developed a new ligand-based strategy combining important pharmacophoric and structural features according to the postu...
High levels of endogenous estrogens are associated with increased risks of breast cancer. Estrogen levels are mainly increased by the activity of the aromatase enzyme and reduced by oxidative/conjugative metabolic pathways. In this paper, we demonstrate for the first time that catechol estrogen metabolites are potent aromatase inhibitors, thus establishing a link between aromatase activity and the processes inv...
Oxidative modification of low-density lipoprotein (LDL) represents an important factor in atherogenesis. In the present study, we have investigated the antioxidant capability of diphenyl diselenide (PhSe)2, a simple organoseleno compound, against copper (Cu2+) and peroxyl radical-induced human LDL oxidation in vitro. In initial studies using human serum, (PhSe)2 caused a dose-dependent inhibition of Cu2+-induce...
Aromatase, an enzyme of the cytochrome P450 family, is a very important pharmacological target, particularly for the treatment of breast cancer. The anti-aromatase activity of a set of natural polyphenolic compounds was evaluated in vitro. Strong aromatase inhibitors including flavones, flavanones, resveratrol, and oleuropein, with activities comparable to that of the reference anti-aromatase drug aminoglutethi...
Atherosclerosis, the main cause of cardiovascular disease (CD), is a chronic inflammatory condition associated with an overproduction of oxidant species, namely peroxynitrite, which is a powerful oxidant that reacts directly with all biomolecules. Glutathione is an efficient scavenger of peroxynitrite, so, modulation of glutathione synthesis may provide a strategy to selectively protect cells from this oxidant....
It is now recognized that the antioxidant defences in the colonic mucosa from patients with inflammatory bowel disease (IBD) are particularly low. On account of this we studied the antioxidant capacity of 5-ASA, the first choice therapy in this pathological situation, in combination with the endogenous antioxidants vitamins C (ASC) and E ([alpha]-tocopherol ([alpha]-T)) against lipid peroxidation in phosphatidy...
Financiadores do RCAAP | |||||||
![]() |
![]() |
![]() |
![]() |
![]() |
![]() |