Search results for "IPA"
showing 10 items of 5795 documents
Synthesis of Thymoquinone–Artemisinin Hybrids: New Potent Antileukemia, Antiviral, and Antimalarial Agents
2017
[Image: see text] A series of hybrid compounds based on the natural products artemisinin and thymoquinone was synthesized and investigated for their biological activity against the malaria parasite Plasmodium falciparum 3D7 strain, human cytomegalovirus (HCMV), and two leukemia cell lines (drug-sensitive CCRF-CEM and multidrug-resistant subline CEM/ADR5000). An unprecedented one-pot method of selective formation of C-10α-acetate 14 starting from a 1:1 mixture of C-10α- to C-10β-dihydroartemisinin was developed. The key step of this facile method is a mild decarboxylative activation of malonic acid mediated by DCC/DMAP. Ether-linked thymoquinone–artemisinin hybrids 6a/b stood out as the most…
Intramolecular structural parameters are key modulators of the gel-liquid transition in coarse grained simulations of DPPC and DOPC lipid bilayers
2018
The capability of coarse-grained models based on the MARTINI mapping to reproduce the gel-liquid phase transition in saturated and unsaturated model lipids was investigated. We found that the model is able to reproduce a lower critical temperature for 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) with respect to 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC). Nonetheless, the appearance of a gel phase for DOPC is strictly dependent on the intramolecular parameters chosen to model its molecular structure. In particular, we show that the bending angle at the coarse-grained bead corresponding to the unsaturated carbon-carbon bond acts as an order parameter determining the temperature of …
Dissipation in suspension system augmented by piezoelectric stack: port-Hamiltonian approach
2020
Analysis of damping in semi-active and active suspension systems is prerequisite for an advanced control and, eventually, energy harvesting functions. This paper addresses the damping in suspension system augmented by the piezoelectric (PE) stack. The Hamiltonian system approach with port-power modeling of single subsystems is used for describing and studying the dissipative properties of piezoelectric stack element, integrated in series with a standard quarter-car suspension. The slightly improved, compared to the underlying passive suspension system, frequency response of the sprung mass acceleration is demonstrated. Moreover, the overall power flow in the system, caused by the disturbing…
MicroRNA as crucial regulators of gene expression in estradiol-treated human endothelial cells.
2018
Background/Aims: Estrogen signalling plays an important role in vascular biology as it modulates vasoactive and metabolic pathways in endothelial cells. Growing evidence has also established microRNA (miRNA) as key regulators of endothelial function. Nonetheless, the role of estrogen regulation on miRNA profile in endothelial cells is poorly understood. In this study, we aimed to determine how estrogen modulates miRNA profile in human endothelial cells and to explore the role of the different estrogen receptors (ERα, ERβ and GPER) in the regulation of miRNA expression by estrogen. Methods: We used miRNA microarrays to determine global miRNA expression in human umbilical vein endothelial cel…
Understanding illnesses through a film festival: an observational study
2019
Abstract Audio-visual materials play a fundamental role in the context of education, care and clinical treatment, as they seem to have a high impact on public awareness. This study aims to describe what messages are perceived by the society at an International Festival of Short Films and Art on Diseases that may help to understand difficult topics, such as illness, dying and suffering. Through an observational, descriptive, cross-sectional study, using full participant observation and an open, self-administered questionnaire, 32 short films were analysed during a healthcare art festival. Categories were developed using inductive content analysis. The message perceived by the participants, a…
Evidence that the endometrial microbiota has an effect on implantation success or failure
2016
Background Bacterial cells in the human body account for 1–3% of total body weight and are at least equal in number to human cells. Recent research has focused on understanding how the different bacterial communities in the body (eg, gut, respiratory, skin, and vaginal microbiomes) predispose to health and disease. The microbiota of the reproductive tract has been inferred from the vaginal bacterial communities, and the uterus has been classically considered a sterile cavity. However, while the vaginal microbiota has been investigated in depth, there is a paucity of consistent data regarding the existence of an endometrial microbiota and its possible impact in reproductive function. Objecti…
New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8
2018
Abstract In the present work a series of aziridine-2,3-dicarboxylate inhibitors of papain-like cysteine proteases was designed, synthesized and tested. The compounds displayed selectivity for the parasitic protozoon Leishmania mexicana cathepsin L-like cysteine protease LmCPB2.8. The computational methods of homology modelling and molecular docking predicted some significant differences in the S2 pocket of LmCPB2.8 and cruzain, a related enzyme from Trypanosoma cruzi. Due to the presence of Tyr209 in LmCPB2.8 rather than Glu208 in cruzain sterically demanding, lipophilic ester groups (inhibitor 7d, 9d, 12d and 14d) are predicted to occupy the S2 pocket of the Leishmania protease, but do not…
Mandarin essential oils inhibit quorum sensing and virulence factors of Pseudomonas aeruginosa
2016
Pseudomonas aeruginosa produces biofilm and several virulence factors coordinated by quorum sensing (QS) in food. The interruption of QS is a target to control the bacterial virulence. Chemical preservatives used to control biofilm give rise to several food safety problems. For this reason, essential oils (EOs), generally recognized as safe products, are a hopeful alternative. The aim of this work was to determine the chemical composition of mandarin EOs obtained by cold-pressing (EOP) and cold-pressing followed by steam distillation (EOPD) and their antipathogenic properties against P. aeruginosa. Both EOs contained the highest quantities of monoterpene hydrocarbons, mainly limonene, follo…
The IASLC Lung Cancer Staging Project: Proposals for Revision of the TNM Stage Groupings in the Forthcoming (Eighth) Edition of the TNM Classificatio…
2016
AbstractThe IASLC Staging and Prognostic Factors Committee has collected a new database of 94,708 cases donated from 35 sources in 16 countries around the globe. This has now been analysed by our statistical partners at Cancer Research And Biostatistics and, in close collaboration with the members of the committee proposals have been developed for the T, N, and M categories of the 8th edition of the TNM Classification for lung cancer due to be published late 2016. In this publication we describe the methods used to evaluate the resultant Stage groupings and the proposals put forward for the 8th edition.
Generation of three human iPSC lines from PLAN (PLA2G6-associated neurodegeneration) patients
2021
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