There is currently no approved antiviral therapy for treatment of Marburg virus disease (MVD). Although filovirus infection outbreaks are quite rare, the high mortality rates in such outbreaks make ...the development of anti-filoviral drugs an important goal of medical chemistry and virology. Here, we performed screening of a large library of natural derivatives for their virus entry inhibition activity using pseudotype systems. The bornyl ester derivatives containing saturated N-heterocycles exhibited the highest antiviral activity. It is supposed that compounds with specific inhibitory activity toward MarV-GP-dependent virus entry will inhibit the rVSIV-ΔG-MarV-GP pseudotype much more efficiently than the control rVSIV-ΔG-G pseudotype. At the same time, the compounds similarly inhibiting both pseudotypes will likely affect rVSIV capsid replication or the cellular mechanisms common to the entry of both viruses. Borneol itself is not active against both pseudotypes and is nontoxic, whereas its derivatives have varying toxicity and antiviral activity. Among low-toxic borneol derivatives, six compounds turned out to be relatively specific inhibitors of MarV-GP-mediated infection (SC > 10). Of them, compound
6
containing a methylpiperidine moiety exhibited the highest virus-specific activity. Notably, the virus-specific activity of this compound is twice as high as that of the reference.
Screening of a library of natural derivatives for their virus entry inhibition activity using pseudotype systems shows bornyl ester derivatives containing saturated N-heterocycles exhibiting the highest antiviral activity.
Screening of a library of natural derivatives for their virus entry inhibition activity using pseudotype systems shows bornyl ester derivatives containing saturated N-heterocycles exhibiting the ...highest antiviral activity.
There is currently no approved antiviral therapy for treatment of Marburg virus disease (MVD). Although filovirus infection outbreaks are quite rare, the high mortality rates in such outbreaks make the development of anti-filoviral drugs an important goal of medical chemistry and virology. Here, we performed screening of a large library of natural derivatives for their virus entry inhibition activity using pseudotype systems. The bornyl ester derivatives containing saturated N-heterocycles exhibited the highest antiviral activity. It is supposed that compounds with specific inhibitory activity toward MarV-GP-dependent virus entry will inhibit the rVSIV-ΔG-MarV-GP pseudotype much more efficiently than the control rVSIV-ΔG-G pseudotype. At the same time, the compounds similarly inhibiting both pseudotypes will likely affect rVSIV capsid replication or the cellular mechanisms common to the entry of both viruses. Borneol itself is not active against both pseudotypes and is nontoxic, whereas its derivatives have varying toxicity and antiviral activity. Among low-toxic borneol derivatives, six compounds turned out to be relatively specific inhibitors of MarV-GP-mediated infection (SC > 10). Of them, compound
6
containing a methylpiperidine moiety exhibited the highest virus-specific activity. Notably, the virus-specific activity of this compound is twice as high as that of the reference.
Reactor antineutrino detector iDREAM Gromov, M. B.; Lukyanchenko, G. A.; Novikova, G. J. ...
Physics of particles and nuclei,
11/2017, Letnik:
48, Številka:
6
Journal Article
Recenzirano
The prototype of an industrial reactor antineutrino detector iDREAM is constructed to demonstrate the capability of real-time remote monitoring of PWR operation by the neutrino method.
A two-phase emission detector containing 5 kg of liquid Xe is installed at the horizontal experimental channel of the research nuclear reactor IRT MEPhI to measure the liquid Xe response to nuclei ...recoils with kinetic energies below 1 keV. Preliminary tests have demonstrated that ≥ 15 μs electron lifetime in liquid Xe and ~ 10 photoelectrons single ionization electron signal are achieved. These parameters are sufficient to detect and identify events at the single electron level.
Spontaneously occurring spike-wave discharges (SWDs) and serum concentrations of ovarian steroid hormones were investigated before, during and after pregnancy in WAG/Rij rats, a rat strain with ...genetically determined absence seizures. Eight groups of rats were included in the assays of progesterone and estradiol: rats at diestrus, at various days of pregnancy and at lactating days. The number of SWDs in cortical EEG of WAG/Rij rats was decreased from the 3rd up to the 18th day of pregnancy and subsequently increased to control level. Thereafter, a new decrease was found 2–3 days after parturition. Serum concentration of progesterone was threefold increased at the 3rd day of pregnancy, remained elevated until the 18th day of pregnancy and returned to control values before delivery. Over measured days, estradiol was significantly elevated only at the 18th day of pregnancy.
Results demonstrate that physiological conditions induced by the state of pregnancy lead to suppression of occurrence of SWDs. Changes in plasma progesterone concentration correspond to the changes in number of SWDs: an increased level of progesterone during pregnancy is accompanied by a decreased number of SWDs, while a decrease in circulating progesterone before parturition is paralleled by an increase of SWDs. Of interest, the relationship between SWDs and concentration of progesterone found during pregnancy is diametrically opposite to results obtained in acute administration studies of progesterone in nonpregnant animals.
The neutrino method for monitoring the operating modes of nuclear reactors was proposed and tested in the 1980s–1990s at the Kurchatov Institute. Recent progress in the experimental techniques for ...antineutrino detection has enabled the development of projects that are focused on the introduction of techniques that are used in fundamental research in the nuclear-power industry. We report on the current status of the development of a test prototype of the iDREAM (industrial Detector for REactor Antineutrino Monitoring) detector. The detector is a scintillation spectrometer that is based on a liquid organic scintillator with a sensitive volume of 1 m
3
and is constructed with due regard for the current experience in the design of the most extensively studied detectors of reactor antineutrinos of this type.
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