20 documents found, page 1 of 2
Effect of Diosgenin in Suppressing Viability and Promoting Apoptosis of Human P...
Figueira, Marília I; Marques, Ricardo; Cardoso, Henrique J.; Fonseca, Lara R. S.; Duarte, Ana Paula; Silvestre, Samuel; Socorro, SílviaDiosgenin is a phytosteroid sapogenin with reported antitumoral activity. Despite the evidence indicating a lower incidence of prostate cancer (PCa) associated with a higher consumption of phytosteroids and the beneficial role of these compounds, only a few studies have investigated the effects of diosgenin in PCa, and its mechanisms of action remain to be disclosed. The present study investigated the effect of...
Synthesis, In Vitro Biological Evaluation of Antiproliferative and Neuroprotect...
Brito, Vanessa; Marques, Mariana; Esteves, Marta; Serra-Almeida, Catarina; Alves, Gilberto; Almeida, Paulo; Bernardino, Liliana; Silvestre, SamuelSteroids constitute an important class of pharmacologically active molecules, playing key roles in human physiology. Within this group, 16E-arylideneandrostane derivatives have been reported as potent anti-cancer agents for the treatment of leukemia, breast and prostate cancers, and brain tumors. Additionally, 5α,6α-epoxycholesterol is an oxysterol with several biological activities, including regulation of cel...
Fighting Epilepsy with Nanomedicines-Is This the Right Weapon?
Matias, Mariana; Santos, Adriana O.; Silvestre, Samuel; Alves, GilbertoEpilepsy is a chronic and complex condition and is one of the most common neurological diseases, affecting about 50 million people worldwide. Pharmacological therapy has been, and is likely to remain, the main treatment approach for this disease. Although a large number of new antiseizure drugs (ASDs) has been introduced into the market in the last few years, many patients suffer from uncontrolled seizures, dem...
New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploi...
Guedes, Romina A.; Grilo, Jorge H.; Carvalho, Andreia N.; Fernandes, Pedro M. P.; Ressurreição, Ana S.; Brito, Vanessa; Santos, Adriana O.Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin-proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance to existing therapies and the occurrence of severe adverse effects is still a concern. The purpose of this study was the discovery of novel scaffolds of protea...
Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with...
Pires, Patrícia C.; Fernandes, Mariana; Nina, Francisca; Gama, Francisco; Gomes, Maria F; Rodrigues, Lina E; Meirinho, Sara; Silvestre, SamuelFormulating low-solubility or low-permeability drugs is a challenge, particularly with the low administration volumes required in intranasal drug delivery. Nanoemulsions (NE) can solve both issues, but their production and physical stability can be challenging, particularly when a high proportion of lipids is necessary. Hence, the aim of the present work was to develop a NE with good solubilization capacity for...
C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Ac...
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Pires, Patrícia; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoC-Ring oxidized estrone acetate derivatives as antiproliferative agents were prepared and tested against five cancer cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Flow cytometry assays to evaluate cell viability and modifications in cell cycle phases and molecular docking research against estrogen receptor α, steroid sulfatase, and 17β-hydroxysteroid dehydrogenase type 1 ...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Gomes, Filipa Ramilo; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L.; Pavan, Fernando R.; Gomes, Clara S.B.; Brito, VanessaSchiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn2(...
Discovery of Small Molecules as Membrane-Bound Catechol-O-methyltransferase Inh...
Cruz-Vicente, Pedro; Gonçalves, Ana M.; Ferreira, Octávio; Queiroz, João A.; Silvestre, Samuel; Passarinha, Luís A.; Gallardo, EugeniaA pharmacophore-based virtual screening methodology was used to discover new catecholO-methyltransferase (COMT) inhibitors with interest in Parkinson’s disease therapy. To do so, pharmacophore models were constructed using the structure of known inhibitors and then they were used in a screening in the ZINCPharmer database to discover hit molecules with the desired structural moieties and drug-likeness propertie...
New Estrone Oxime Derivatives: Synthesis, Cytotoxic Evaluation and Docking Studies
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoThe interest in the introduction of the oxime group in molecules aiming to improve their biological effects is increasing. This work aimed to develop new steroidal oximes of the estrane series with potential antitumor interest. For this, several oximes were synthesized by reaction of hydroxylamine with the 17-ketone of estrone derivatives. Then, their cytotoxicity was evaluated in six cell lines. An estrogenici...
Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically ...
Brito, Vanessa; Alves, Gilberto; Almeida, Paulo; Silvestre, SamuelSteroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Additionally, steroids have been associated with a relatively low toxicity and high bioavailability. Nowadays, multiple steroidal derivatives are clinically available for the treatment of numerous diseases. Moreover, different structural modifications on th...