Abstract:
:Rift Valley fever virus (RVFV) is a mosquito-borne hemorrhagic fever virus affecting both humans and animals with severe morbidity and mortality and is classified as a potential bioterror agent due to the possible aerosol transmission. At present there is no human vaccine or antiviral therapy available. Thus, there is a great need to develop new antivirals for treatment of RVFV infections. Benzavir-2 was previously identified as potent inhibitor of human adenovirus, herpes simplex virus type 1, and type 2. Here we assess the anti-RVFV activity of benzavir-2 together with four structural analogs and determine pre-clinical pharmacokinetic parameters of benzavir-2. In vitro, benzavir-2 efficiently inhibited RVFV infection, viral RNA production and production of progeny viruses. In vitro, benzavir-2 displayed satisfactory solubility, good permeability and metabolic stability. In mice, benzavir-2 displayed oral bioavailability with adequate maximum serum concentration. Oral administration of benzavir-2 formulated in peanut butter pellets gave high systemic exposure without any observed toxicity in mice. To summarize, our data demonstrated potent anti-RVFV activity of benzavir-2 in vitro together with a promising pre-clinical pharmacokinetic profile. This data support further exploration of the antiviral activity of benzavir-2 in in vivo efficacy models that may lead to further drug development for human use.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Islam MK,Strand M,Saleeb M,Svensson R,Baranczewski P,Artursson P,Wadell G,Ahlm C,Elofsson M,Evander Mdoi
10.1038/s41598-018-20362-9subject
Has Abstractpub_date
2018-01-31 00:00:00pages
1925issue
1issn
2045-2322pii
10.1038/s41598-018-20362-9journal_volume
8pub_type
杂志文章abstract::Knowing the distribution of marine animals is central to understanding climatic and other environmental influences on population ecology. This information has proven difficult to gain through capture-based methods biased by capture location. Here we show that marine location can be inferred from animal tissues. As the...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep00021
更新日期:2011-01-01 00:00:00
abstract::We discuss a scheme to retrieve transient conformational molecular structure information using photoelectron angular distributions (PADs) that have averaged over partial alignments of isolated molecules. The photoelectron is pulled out from a localized inner-shell molecular orbital by an X-ray photon. We show that a t...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep23655
更新日期:2016-03-30 00:00:00
abstract::As the magnetic storage density increases in commercial products, e.g. the hard disc drives, a full understanding of dynamic magnetism in nanometer resolution underpins the development of next-generation products. Magnetic force microscopy (MFM) is well suited to exploring ferromagnetic domain structures. However, ato...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep05594
更新日期:2014-07-11 00:00:00
abstract::The extent to which the details of past experiences are retained or forgotten remains controversial. Some studies suggest massive storage while others describe memories as fallible summary recreations of original events. The discrepancy can be ascribed to the content of memories and how memories are evaluated. Many st...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-33792-2
更新日期:2018-11-12 00:00:00
abstract::Studies of tumor models using syngeneic transplantation have advanced our understanding of tumor immunity, including both immune surveillance and evasion. Murine mammary carcinoma 4T1 cells secrete immunosuppressive soluble factors as demonstrated in splenocyte culture. Cultured primary splenocytes secrete IFN-γ, whic...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep08913
更新日期:2015-03-09 00:00:00
abstract::Run-and-tumble motility is widely used by swimming microorganisms including numerous prokaryotic and eukaryotic organisms. Here, we experimentally investigate the run-and-tumble dynamics of the bacterium E. coli in polymeric solutions. We find that even small amounts of polymer in solution can drastically change E. co...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep15761
更新日期:2015-10-28 00:00:00
abstract::We have systematically investigated the influence of oxygen vacancy defects on the structural, electronic and magnetic properties of La(1-x)Sr(x)MnO3 (x = 1/3) film by means of ab initio calculations using bare GGA as well as GGA+U formalism, in the latter of which, the on-site Coulombic repulsion parameter U for Mn 3...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep22422
更新日期:2016-03-01 00:00:00
abstract::Thermal management and simulation are becoming increasingly important in many areas of engineering applications. There are three cooling routes for thermal management, namely thermal conduction, thermal convection and thermal radiation, among which the first two approaches have been widely studied and applied, while t...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-21020-w
更新日期:2018-02-08 00:00:00
abstract::The known angiotensin II (AngII) physiological effect of aldosterone synthesis and secretion is mediated by either Gq/11 proteins or βarrestin1 (βarr1), both of which can couple to its type 1 receptors (AT₁Rs), present in adrenocortical zona glomerulosa (AZG) cell membranes. In the present study, we examined the relat...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep08116
更新日期:2015-01-29 00:00:00
abstract::Boron carbide (B4C) coating on diamond particle is synthesized by heating diamond particles in a powder mix of H3BO3 and B in Ar atmosphere. The composition, bond state and coverage fraction of boron carbide coating on diamond particles are investigated. The boron carbide coating favors to grow on diamond (100) surfac...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-017-11142-y
更新日期:2017-09-06 00:00:00
abstract::Soft tissue prostheses such as artificial ear, eye and nose are widely used in the maxillofacial rehabilitation. In this report we demonstrate how to fabricate soft prostheses mold with a low cost desktop 3D printer. The fabrication method used is referred to as Scanning Printing Polishing Casting (SPPC). Firstly the ...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep06973
更新日期:2014-11-27 00:00:00
abstract::Orbital angular momentum (OAM) multiplexing technique has recently emerged and generated widespread interests since the OAM was discovered as a property of electromagnetic wave and acoustic wave. It was widely acknowledged that OAM multiplexing can achieve very high effective degrees of freedom (EDOF) and improve the ...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-020-61329-z
更新日期:2020-03-23 00:00:00
abstract::GPS-derived Total Electron Content (TEC) is an integrated quantity; hence it is difficult to relate the detection of ionospheric perturbations in TEC to a precise altitude. As TEC is weighted by the maximum ionospheric density, the corresponding altitude (hmF2) is, generally, assumed as the perturbation detection alti...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-30476-9
更新日期:2018-08-14 00:00:00
abstract::Bilirubin neurotoxicity has been studied for decades and has been shown to affect various mechanisms via significant modulation of gene expression. This suggests that vital regulatory mechanisms of gene expression, such as epigenetic mechanisms, could play a role in bilirubin neurotoxicity. Histone acetylation has rec...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-32106-w
更新日期:2018-09-12 00:00:00
abstract::Mortality of glioblastoma multiforme (GBM) has not improved over the last two decades despite medical breakthroughs in the treatment of other types of cancers. Nanoparticles hold tremendous promise to overcome the pharmacokinetic challenges and off-target adverse effects. However, an inhibitory effect of nanoparticles...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-020-59146-5
更新日期:2020-02-11 00:00:00
abstract::Priming improves an organism's performance upon a future stress. To test whether cold priming supports protection in spring and how it is affected by cold acclimation, we compared seven Arabidopsis accessions with different cold acclimation potentials in the field and in the greenhouse for growth, photosynthetic perfo...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep44055
更新日期:2017-03-09 00:00:00
abstract::Tom40 is an integral protein of the mitochondrial outer membrane, which as the central component of the Translocase of the Outer Membrane (TOM) complex forms a channel for protein import. We characterize the diffusion properties of individual Tom40 molecules fused to the photoconvertable fluorescent protein Dendra2 wi...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep00195
更新日期:2011-01-01 00:00:00
abstract::Neuroinflammation in utero may result in life-long neurological disabilities. Microglia play a pivotal role, but the mechanisms are poorly understood. No early postnatal treatment strategies exist to enhance neuroprotective potential of microglia. We hypothesized that agonism on α7 nicotinic acetylcholine receptor (α7...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-017-09439-z
更新日期:2017-09-06 00:00:00
abstract::This study aims to determine the prevalence of health personnel with normal weight central obesity and to investigate whether this group had higher cardiovascular disease (CVD) risk factors than those of the people with normal weight and without central obesity. A waist-to-height ratio was calculated as waist circumfe...
journal_title:Scientific reports
pub_type: 临床试验,杂志文章
doi:10.1038/srep37100
更新日期:2016-11-16 00:00:00
abstract::A nanotechnology-based approach for the inhibition of breast cancer cell proliferation is proposed. The innovative solution consists in a platform based on biocompatible piezoelectric nanoparticles able to target and remotely stimulate HER2-positive breast cancer cells. The anti-proliferative effects of the ultrasound...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-24697-1
更新日期:2018-04-19 00:00:00
abstract::Enterovirus A71 (EV-A71) is an emerging pathogen in the Enterovirus A species group. EV-A71 causes hand, foot and mouth disease (HFMD), with virulent variants exhibiting polio-like acute flaccid paralysis and other central nervous system manifestations. We analysed all enterovirus A71 complete genomes with collection ...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-019-41662-8
更新日期:2019-04-01 00:00:00
abstract::Germanium is an outstanding anode material in terms of electrochemical performance, especially rate capability, but its developments are hindered by its high price because it is rare in the crust of earth, and its huge volume variation during the lithium insertion and extraction. Introducing other cheaper elements int...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep11326
更新日期:2015-06-10 00:00:00
abstract::What is it like to be invisible? This question has long fascinated man and has been the central theme of many classic literary works. Recent advances in materials science suggest that invisibility cloaking of the human body may be possible in the not-so-distant future. However, it remains unknown how invisibility affe...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep09831
更新日期:2015-04-23 00:00:00
abstract::Obesity causes low-grade inflammation that is involved in male infertility. Interleukin 1 beta (IL1β) plays an important role in this process. A high-fat diet (HFD) is the most common cause of obesity. However, the effect of a HFD on IL1β and its consequence in reproduction remain unclear. We established a HFD model i...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-017-00505-0
更新日期:2017-04-03 00:00:00
abstract::Living organisms employ various mechanisms to escape harm. At the cellular level, mobile cells employ movement to avoid harmful chemicals or repellents. The present study is the first to report that cells move away from the site of injury in response to local wounding. When a migrating Dictyostelium cell was locally w...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-019-39678-1
更新日期:2019-03-12 00:00:00
abstract::Cardiovascular diseases are directly linked to smoking habits, which has both physiological and anatomical effects on the systemic and retinal circulations, and these changes can be detected with fundus photographs. Here, we aimed to 1- design a Convolutional Neural Network (CNN), using retinal photographs, to differe...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-019-43670-0
更新日期:2019-05-09 00:00:00
abstract::An empirical approach was taken to screen a novel synthetic compound library designed to be active against Gram-positive bacteria. We obtained five compounds that were active against spores from the model organism Bacillus subtilis and the food-borne pathogen Bacillus cereus during our population based experiments. Us...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-018-27529-4
更新日期:2018-06-14 00:00:00
abstract::Through a geomorphological study relying on statistically assessed classes of hilltop elevations, we reconstruct a suite of paleo-surfaces along the Tiber River Valley north of Rome that we identify as fluvial terraces formed by interplay between global sea-level fluctuations and regional upift. Using biostratigraphic...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-017-02437-1
更新日期:2017-05-31 00:00:00
abstract::The PRL phosphatases are oncogenic when overexpressed but their in vivo biological function is less well understood. Previous gene deletion study revealed a role for PRL2 in spermatogenesis. We report here the first knockout mice lacking PRL1, the most related homolog of PRL2. We found that loss of PRL1 does not affec...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/srep34211
更新日期:2016-09-26 00:00:00
abstract::A mathematical model has been developed to examine the magneto hydrodynamic micropolar nanofluid flow with buoyancy effects. Flow analysis is carried out in the presence of nonlinear thermal radiation and dual stratification. The impact of binary chemical reaction with Arrhenius activation energy is also considered. A...
journal_title:Scientific reports
pub_type: 杂志文章
doi:10.1038/s41598-017-13140-6
更新日期:2017-10-10 00:00:00