Search results for "Lua"
showing 10 items of 3286 documents
Polyketides from the marine-derived fungus Aspergillus falconensis: In silico and in vitro cytotoxicity studies.
2020
Abstract Fermentation of the marine-derived fungus Aspergillus falconensis, isolated from sediment collected from the Red Sea, Egypt on solid rice medium containing 3.5% NaCl yielded a new dibenzoxepin derivative (1) and a new natural isocoumarin (2) along with six known compounds (3–8). Changes in the metabolic profile of the fungus were induced by replacing NaCl with 3.5% (NH4)2SO4 that resulted in the accumulation of three further known compounds (9–11), which were not detected when the fungus was cultivated in the presence of NaCl. The structures of the new compounds were elucidated by HRESIMS and 1D/2D NMR as well as by comparison with the literature. Molecular docking was conducted fo…
Computational Evaluation and In Vitro Validation of New Epidermal Growth Factor Receptor Inhibitors
2020
Background:The Epidermal Growth Factor Receptor (EGFR) is a transmembrane protein that acts as a receptor of extracellular protein ligands of the epidermal growth factor (EGF/ErbB) family. It has been shown that EGFR is overexpressed by many tumours and correlates with poor prognosis. Therefore, EGFR can be considered as a very interesting therapeutic target for the treatment of a large variety of cancers such as lung, ovarian, endometrial, gastric, bladder and breast cancers, cervical adenocarcinoma, malignant melanoma and glioblastoma.Methods:We have followed a structure-based virtual screening (SBVS) procedure with a library composed of several commercial collections of chemicals (615,46…
Present status of the application of cryopreserved hepatocytes in the evaluation of xenobiotics: consensus of an international expert panel.
1999
Successful cryopreservation of freshly isolated hepatocytes would significantly decrease the need for freshly-procured livers for the preparation of hepatocytes for experimentation. Hepatocytes can be prepared, cryopreserved, and used for experimentation as needed at different times after isolation. Cryopreservation is especially important for research with human hepatocytes because of the limited availability of fresh human livers. Based on the cumulative experience of this international expert panel, a consensus was reached on the various aspects of hepatocyte cryopreservation, including cryopreservation and thawingprocedures and applications of the cryopreserved hepatocytes. Key to succe…
Presenilin is the molecular target of acidic γ-secretase modulators in living cells.
2012
The intramembrane-cleaving protease γ-secretase catalyzes the last step in the generation of toxic amyloid-β (Aβ) peptides and is a principal therapeutic target in Alzheimer's disease. Both preclinical and clinical studies have demonstrated that inhibition of γ-secretase is associated with prohibitive side effects due to suppression of Notch processing and signaling. Potentially safer are γ-secretase modulators (GSMs), which are small molecules that selectively lower generation of the highly amyloidogenic Aβ42 peptides but spare Notch processing. GSMs with nanomolar potency and favorable pharmacological properties have been described, but the molecular mechanism of GSMs remains uncertain an…
Treatment of Dimpling from Cellulite.
2018
Background:. Cellulite can be seen on the skin in widespread alterations of the skin surface and dimpling. The purpose of this study was to assess the effectiveness and safety of the manual subcision technique to treat dimpling from cellulite, using a specific class IIA medical device (Celluerase). Methods:. The multi-center observational study assessed 200 women treated in a single session for different dimpling, using manual subcision administered by Celluerase. Aesthetic outcomes were evaluated by the authors, and the patients assessed satisfaction levels. Results:. Two hundred women between 20 and 55 years were treated. The medical evaluation of patients saw improvements with an average…
The isolated perfused rat brain as a model for studying drugs acting on the CNS
1974
An isolated perfused brain preparation is regarded as offering some important advantages over intact animals or tissue slices for studying drug effects on the CNS. The rat is by far the most suitable laboratory animal for this technique because of low cost, ease of preparation and extensive literature available for comparative purposes. In this paper various preparation techniques and perfusion systems for an isolated rat brain are reported. Investigations are presented proving the viability of the isolated perfused rat brain for more than seven hours and its suitability for studies on cerebral metabolism. Until now this preparation has been successfully used for pharmacological investigati…
Diffusion in slice preparations bathed in unstirred solutions
1987
A diffusion model is described here, which allows for the estimations of drug concentration changes in porous media, such as in slice tissues of the central nervous system (CNS) bathed in unstirred solutions following abrupt changes of drug concentration. This model may be used for the interpretation of data obtained in neuropharmacological studies if (i) the diffusion coefficient of the molecules under investigation is constant within the excised tissue, (ii) drug molecules are diffusing only in the extracellular space (ECS) and are not bound by the tissue, (iii) drug molecules diffuse mainly within one dimension, (iv) the drug concentration in the bath is changed within 5 s, and (v) the b…
Synthesis and inhibitory activity of dimethylamino-chalcone derivatives on the induction of nitric oxide synthase.
2002
A series of nine dimethylamino-chalcone derivatives (1,3-diaryl-propenones) was synthesized and screened as potential inhibitors of NO and PGE(2) production in the RAW 264.7 macrophage cell line. 4-Dimethylamino-2',5'-dimethoxychalcone (6) was found to be the most potent and dual inhibitor (IC(50s) in the submicromolar range) of NO and PGE(2) production. 2',6'-Dimethoxylation appeared to be an effective requirement for selective and potent inhibition of nitric oxide synthase induction as it was confirmed by Western blot analysis. Chalcone (6) at 25 mg kg(-1) by oral route, inhibited significantly the formation of oedema in the carrageenan-induced model of inflammation in mice.
Synthesis, biological evaluation, and: In silico studies of novel chalcone: In pyrazoline-based 1,3,5-triazines as potential anticancer agents
2020
A novel series of triazin-chalcones (7,8)a-g and triazin-N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were synthesized and evaluated for their anticancer activity against nine different cancer strains. Triazine ketones 5 and 6 were synthesized from the cyanuric chloride 1 by using stepwise nucleophilic substitution of the chlorine atom. These ketones were subsequently subjected to a Claisen-Schmidt condensation reaction with aromatic aldehydes affording chalcones (7,8)a-g. Then, N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were obtained by cyclocondensation reactions of the respective chalcones (7,8)a-g with 3,5-dichlorophenylhydrazine. Among all the evaluated compounds, chalcones 7d,g and 8g…
On the Performance of Channel Assembling and Fragmentation in Cognitive Radio Networks
2014
[EN] Flexible channel allocation may be applied to multi-channel cognitive radio networks (CRNs) through either channel assembling (CA) or channel fragmentation (CF). While CA allows one secondary user (SU) occupy multiple channels when primary users (PUs) are absent, CF provides finer granularity for channel occupancy by allocating a portion of one channel to an SU flow. In this paper, we investigate the impact of CF together with CA for SU flows by proposing a channel access strategy which activates both CF and CA and correspondingly evaluating its performance. In addition, we also consider a novel scenario where CA is enabled for PU flows. The performance evaluation is conducted based on…