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1.
Braz J Biol ; 83: e268859, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37132741

RESUMO

The use of medicinal plants as raw material for extracts production and pure substances isolation and subsequence development of new drugs represents a constantly growing area. However, some stages are indispensable before pharmacologically evaluating natural products such as medicines. Toxicity tests in mammalian cells are essential to initiate new drugs development or verify the substance's biocompatibility. Thus, we verified the toxicity of crude extracts and fractions with different polarities obtained from the leaves and stems of eight plant species. The toxic effect was evaluated on macrophages obtained from the bone marrow and peritoneal cavity of a Swiss webster mouse and J774 macrophages. G8 cell lineage. These macrophages were cultured in a 96-well plate, and the compounds were added at a concentration of 100 µg/mL for 24 hours. After this time, the supernatant was removed. The toxicity was evaluated for lactate dehydrogenase (LDH) release assay and the resazurin assay, which uses an indicator dye to measure oxidation-reduction reactions. The results showed a difference in the percentage of toxicity when comparing the same extract in different types of macrophages. This outcome indicates that these cells from different origins may exhibit different responses when exposed to the same natural compounds.


Assuntos
Extratos Vegetais , Plantas Medicinais , Camundongos , Animais , Extratos Vegetais/toxicidade , Macrófagos , Folhas de Planta , Mamíferos
2.
Bioorg Med Chem ; 27(8): 1449-1455, 2019 04 15.
Artigo em Inglês | MEDLINE | ID: mdl-30528164

RESUMO

Extracellular adenosine 5'-triphosphate (ATP) triggers the P2X7 receptor (P2X7R) ionic channel to stimulate the release of the interleukin-IL-1ß cytokine into macrophages. The current study explored the reaction of six structurally diverse triazole derivatives on P2X7-mediated dye uptake into murine peritoneal macrophages. P2X7R activity determined by ATP-evoked fluorescent dye uptake. Triazole derivatives toxicity measured using dextran rhodamine exclusion based colorimetric assay. A740004 and BBG, both P2X7R antagonist, inhibited ATP-induced dye uptake. In contrast, the derivatives 5a, 5b, 5e, and 5f did not diminish P2X7R activity in concentrations until 100 µM. 5c and 5d analogs caused a potent inhibitory activity on P2X7-induced dye uptake. Dextran Rhodamine exclusion measurements after 24 h of continuous treatment with triazole derivatives indicated a moderated toxicity for all molecules. In conclusion, this study showed that a series of new hybrid 1,2,3-triazolic naphthoquinones reduces P2X7R-induced dye uptake into murine macrophages. In silico analysis indicates a good pharmacokinetic profile and molecular docking results of these analogs indicate the potential to bind into an allosteric site located into the P2X7R pore and juxtaposed with the ATP binding pocket. In this manner, the compounds 5c and 5d may be used as a scaffold for new P2X7R inhibitors with reduced toxicity, and good anti-inflammatory activity.


Assuntos
Naftoquinonas/química , Antagonistas do Receptor Purinérgico P2X/química , Receptores Purinérgicos P2X7/metabolismo , Triazóis/química , Sítio Alostérico , Animais , Sítios de Ligação , Células CACO-2 , Linhagem Celular , Corantes/metabolismo , Humanos , Macrófagos/citologia , Macrófagos/metabolismo , Camundongos , Microssomos Hepáticos/metabolismo , Simulação de Acoplamento Molecular , Permeabilidade/efeitos dos fármacos , Estrutura Terciária de Proteína , Antagonistas do Receptor Purinérgico P2X/metabolismo , Antagonistas do Receptor Purinérgico P2X/farmacologia , Receptores Purinérgicos P2X7/química , Triazóis/metabolismo , Triazóis/farmacologia
3.
Artigo em Inglês | MEDLINE | ID: mdl-23848794

RESUMO

We study the absorption of an intense electromagnetic wave in a plasma by inverse bremsstrahlung, in the relativistic quantum regime, by using the Klein-Gordon (KG) equation. We examine the following points: (1) the solutions of the KG equation in the absence of collisions; (2) the transition probabilities between electron momentum states, and (3) the effective collision frequency in the weak and strong field limits.

4.
Rev Sci Instrum ; 82(2): 023504, 2011 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-21361592

RESUMO

A frequency scanning O-mode reflectometer was used for studies of plasma density oscillations during local Alfvén wave (LAW) excitation in the Tokamak Chauffage Alfvén Brésilien (TCABR) at the frequency f(A) = 5 MHz. It was found that the spectrum of the reflectometer output signal, which consists mainly of the "beat" frequency f(B), is modified by the LAW excitation, and two additional frequency peaks appear, which are symmetrical in relation to the LAW excitation frequency f = f(A) ± f(B). This result opens the possibility to improve the efficiency of studying the LAW induced density oscillations. The symmetry of these frequency peaks yields the possibility of finding the microwave frequency at which the reflectometer cutoff layer coincides with radial position of the LAW resonance zone in the TCABR tokamak.

5.
Rev Sci Instrum ; 81(10): 10D529, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21033884

RESUMO

We present the first simultaneous measurements of the Thomson scattering and electron cyclotron emission radiometer diagnostics performed at TCABR tokamak with Alfvén wave heating. The Thomson scattering diagnostic is an upgraded version of the one previously installed at the ISTTOK tokamak, while the electron cyclotron emission radiometer employs a heterodyne sweeping radiometer. For purely Ohmic discharges, the electron temperature measurements from both diagnostics are in good agreement. Additional Alfvén wave heating does not affect the capability of the Thomson scattering diagnostic to measure the instantaneous electron temperature, whereas measurements from the electron cyclotron emission radiometer become underestimates of the actual temperature values.

6.
Rev Sci Instrum ; 78(4): 043509, 2007 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-17477662

RESUMO

The method for plasma rotation measurement in the tokamak TCABR is reported in this article. During a discharge, an optical spectrometer is used to scan sequentially spectral lines of plasma impurities and spectral lines of a calibration lamp. Knowing the scanning velocity of the diffraction grating of the spectrometer with adequate precision, the Doppler shifts of impurity lines are determined. The photomultiplier output voltage signals are recorded with adequate sampling rate. With this method the residual poloidal and toroidal plasma rotation velocities were determined, assuming that they are the same as those of the impurity ions. The results show reasonable agreement with the neoclassical theory and with results from similar tokamaks.

7.
Artigo em Inglês | MEDLINE | ID: mdl-11970341

RESUMO

Hydrodynamic equations to describe relativistic and ultrarelativistic plasma dynamics were obtained by Dzhavakhishvili and Tsintsadze [Sov. Phys. JETP 37, 666 (1973)] using the Chapman and Enskog scheme to solve the relativistic kinetic equations for the different plasma species. This approach leads to a representation of the particle viscosities in the Navier-Stokes form and, therefore, some relevant physical processes, such as the Burnett type of particle viscosity, cannot be properly dealt with in this scheme. In this paper we employ the extended Grad method to derive hydrodynamic equations which include ultrarelativistic viscosities of the Burnett type, i.e., viscosities that depend not only on derivatives of the particle macroscopic velocities but also on derivatives of particle heat fluxes.

8.
Artigo em Inglês | MEDLINE | ID: mdl-11970692

RESUMO

The laser-assisted stopping power of a fully ionized plasma for the system of two correlated test charges is investigated. The general expressions for the stopping power are applied to a low-density and a low-temperature plasma in a low-energy beam-plasma experiment [J. Jacoby et al., Phys. Rev. Lett. 74, 1550 (1995)]. The effect of the interaction between the beam test charges, described by a correlation term, is to increase the stopping power of the laser-assisted plasma compared to the case where the charges are infinitely separated. However, the laser field affects the correlation between the test charges and contributes to decrease the plasma stopping power, as compared to the laser-free dicluster case.

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