Search results for " 50"
showing 10 items of 2715 documents
In silico and in vitro prediction of the toxicological effects of individual and combined mycotoxins.
2018
3-Acetyldeoxynivalenol (3-AcDON) and 15-acetyldeoxynivalenol (15-AcDON) are converted to deoxynivalenol (DON) in vivo and their simultaneous presence may increase DON intake. Mixtures of DON and its derivatives are a public health concern. In this study DON, 3-AcDON and 15-AcDON were evaluated in vitro and in silico. The in vitro cytotoxicity of DON and its derivatives individually and combined was determined by the Neutral Red (NR) assay in human hepatocarcinoma (HepG2) cells. The concentrations tested were from 1.25 to 15 μM (DON) and from 0.937 to 7.5 μM (DON derivatives). The IC50 values were from >15 to 2.55 μM (DON), from 1.77 to 1.02 μM (3-AcDON), and from 4.05 to 1.68 μM (15-AcDON).…
Cytotoxic activity of medicinal plants of the Kakamega County (Kenya) against drug-sensitive and multidrug-resistant cancer cells
2018
Abstract Ethnopharmacological relevance The geographical location of Kakamega County proximal to the Kakamega Rain Forest in Kenya and its rich flora represents an interesting resource of traditional medicinal plants. The medicinal plants in the present study are traditionally used to treat cancer in Kakamega County as recorded in published literature. Aim of the study Due to multidrug resistance (MDR) and severe side effects of currently used drugs in clinical oncology, new candidate compounds are urgently required to improve treatment outcome. The present study explored the in vitro cytotoxic potential of 34 organic and 19 aqueous extracts of Kakamega medicinal plants towards sensitive an…
Bistacrine derivatives as new potent antimalarials
2016
Linking two tacrine molecules results in a tremendous increase of activity against Plasmodia in comparison to the monomer. This finding prompted the synthesis of a library of monomeric and dimeric tacrine derivatives in order to derive structure-activity relationships. The most active compounds towards chloroquine sensitive Plasmodium strain 3D7 and chloroquine resistant strain Dd2 show IC50 values in the nanomolar range of concentration, low cytotoxicity and target the cysteine protease falcipain-2, which is essential for parasite growth.
Effects of trans-stilbene and terphenyl compounds on different strains of Leishmania and on cytokines production from infected macrophages.
2017
Most of the antileishmanial modern therapies are not satisfactory due to high toxicity or emergence of resistance and high cost of treatment. Previously, we observed that two compounds of a small library of trans-stilbene and terphenyl derivatives, ST18 and TR4, presented the best activity and safety profiles against Leishmania infantum promastigotes and amastigotes. In the present study we evaluated the effects of ST18 and the TR4 in 6 different species of Leishmania and the modifications induced by these two compounds in the production of 8 different cytokines from infected macrophages. We observed that TR4 was potently active in all Leishmania species tested in the study showing a leishm…
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
2018
A family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also been tested against human cathepsins B and L1 for selectivity. Dipeptidyl enoates resulted to be irreversible inhibitors of these enzymes. Some of the members of the family are very potent inhibitors of parasitic cysteine proteases displaying k2nd (M−1s−1) values of seven orders of magnitude. In vivo antiprotozoal testing was also performed. Inhibitors exhibited IC50 values in the micromolar range against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi and ev…
New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.
2018
New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40&ndash
Statistical Explorations and Univariate Timeseries Analysis on COVID-19 Datasets to Understand the Trend of Disease Spreading and Death
2020
&ldquo
Numerical Study on the Heading Misalignment and Current Velocity Reduction of a Vessel-Shaped Offshore Fish Farm
2019
Recently, the concept of a vessel-shaped fish farm was proposed for open sea applications. The fish farm comprises a vessel-shaped floater, five fish cages, and a single-point mooring system. Such a system weathervanes, and this feature increases the spread area of fish waste. Still, the downstream cages may experience decreased exchange of water flow when the vessel heading is aligned with the current direction, and fish welfare may be jeopardized. To ameliorate the flow conditions, a dynamic positioning (DP) system may be required, and its power consumption should relate to the heading misalignment. This paper proposes an integrated method for predicting the heading misalignment between t…
A systematic review of immersive virtual reality applications for higher education: Design elements, lessons learned, and research agenda
2019
Abstract Researchers have explored the benefits and applications of virtual reality (VR) in different scenarios. VR possesses much potential and its application in education has seen much research interest lately. However, little systematic work currently exists on how researchers have applied immersive VR for higher education purposes that considers the usage of both high-end and budget head-mounted displays (HMDs). Hence, we propose using systematic mapping to identify design elements of existing research dedicated to the application of VR in higher education. The reviewed articles were acquired by extracting key information from documents indexed in four scientific digital libraries, whi…
Generating Executable Code from High-Level Social or Socio-Ecological Model Descriptions
2019
Agent-Based Modelling has been used for social simulation because of the several benefits it entails. Social models are often constructed by inter-disciplinary teams that include subject-matter experts with no programming skills. These experts are typically involved in the creation of the conceptual model, but not the verification or validation of the simulation model. The Overview, Design concepts, and Details (ODD) protocol has emerged as a way of presenting a model at a high level of abstraction and as an effort towards improving the reproducibility of Agent-Based Models (ABMs) but it is typically written after a model has been completed. This paper reverses the process and provides non-…