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| Spiro-indolinone |
From the result of p53-MDM2 complex crystal structure, tryptophan
residues on the indole ring of p53 is the most critical binding element for p53
binding MDM2 protein, which was buried in the hydrophobic pocket, and indole on
the NH and MDM2 formed a hydrogen bond. Wang and his team members used
computer-assisted drug screening to find compounds that mimic the indole ring
and found that the structural properties of 2-indolinone were most consistent
with that of indole. 6-chloro-2-indolinone was identified as a predominant
fragment on the basis of previous work on peptide compounds and Nutlin (Trp
pocket with key chlorine atoms capable of occupying MDM2 protein). The Spiro
cyclic backbone provides the necessary platform for introducing side chains so
that the hydrophobic side chains can be inserted into Leu and Phe pockets. The
crystal structures of the resulting compounds MI-63 and MDM2 were recently
reported by Popowicz et al. Read more>>>>>>>>>
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| Micro/Nano Plastics |
Given that plastic polymers are highly resistant to degradation, the
influx of these persistent, complex materials is a risk to human and
environmental health. Microplastics is described as a truly heterogeneous
mixture of particles ranging in size form a few microns to several millimeters
in diameter; including particles of various shapes from completely spherical to
elongated fibers. Microplastic pollution has been reported on a global scale
from the poles to the equator. The main route of concern is currently as a
consequence of ingestion, which could lead to physical and toxicological
effects on aquatic organisms. To this end, in order to minimize the negative
impacts posed by plastic pollution (microplastics), a plethora of strategies
have been developed at various levels to reduce and manage the plastic wastes.
The main objective of this paper is to review some of the published literatures
on management measures of plastic wastes. Read more>>>>>>>
About defence
system of vertebrate, the complexed problems of developing our dual system, the
innate and inductive do not seem to guard or even protect the maturation of one
internal threat to survival. Also, all the individual suffers from the risk of immunodeficiencyin daily activities with both internal and/or externals events, such personalhabitat of individual, such in lifestyle related disease. Recently,
complementary, and alternative medicines (CAM) have interested more and more
attractive since they are able to treat many life-style related diseases, such
as Diabetes mellitus, fatigue syndrome that spurred in the industrialized
world. The present report had showed that typical styles of CAM, preparing
special molecule for both digestive and easy to augmented human complement
component that regulated the functions of leukocytes in human immune defence
system.
We had been published and proposed that the health promoting supplement
could work after depredated the polysaccharide to appropriate fragment they
possible to activate complement component. This was especially being part of
alternative complement pathway. Dietary Supplements and fermented derivatives
suggested as potent agent food supplement for regulating an acquired immunity
through alternative complement pathway. These processes were close
concollection of the complement activating process different from invasion of
infectious agent where the immune complex and/or toxic polysaccharide such as
LPS worked as pathway of complement.(Read More)
The advent of
targeted therapies, i.e., small molecules or antibodies that interfere with
signaling proteins involved in the etiology of cancer, revolutionized thetreatment of tumors with an addiction to specific oncogenes (e.g., ALK in lung
cancer, Bcr-Abl in chronic myeloid leukemia, KIT in GIST, EGFR in lung cancer,
HER2 in breast cancer or MET in liver tumors). However, for many cancers, the
progressionfree survival of patients treated with targeted therapy is less than
one year, which justify for a regain of interest in cytotoxic agents including
metallodrugs.
Indeed, the prevalent success of cisplatin in the treatment of
various types of cancers has placed organometallic compounds on the forefront
in the development of anticancer drugs. In this quest, copper derivatives hold
promising opportunities due to opportunities provided by the hypoxic
environment that is a hallmark of cancer cells coupled with the ability of
copper complexes to catalyze the formation of Reactive Oxygen and Nitrogen
species (ROS and RNS).(Read More)
Such known
programs as Lukas Program, ThermoCalc, ChemSage, FACTSage, MTDATA, PanEngine,
PANDAT are created for the calculations of phase equilibria. Thanks to them itbecame possible the use of more realistic models of the thermodynamicproperties of phases, the calculation of phase diagrams in the complex
two-component systems and the systems with the large number of components. The
CALPHAD-method, which makes possible to generalize and to refine within the
framework information about the phase equilibria and the thermodynamics of
phases for one model, is most claimed today. It is effective means for
decreasing the volumes of the experiments, necessary for understanding of phase
transformations in the alloys and the ceramics. The CALPHAD ideology became the
powerful means of theoretical studies and obtaining of adequate information
about the phase equilibria.
Thermodynamic properties and phase diagrams for the
technologically important multi-component materials can be predicted with its
use. The reliable thermodynamic descriptions of two-component systems are the
basis of the data bases with such characteristics. However, the CALPHAD
application is limited by a deficiency in reliable thermodynamic data and the
weak possibilities of the visualization of three-dimensional objects. In
addition to this, using of thermodynamic methods of the states diagram
calculating is hindered by the need of evaluating the thermodynamic properties
of phases (in the absence of experimental data) and the agreement of
experimental data of phase equilibria with the thermodynamic models. The
innovation technology of assembling the space models of multidimensional phase
diagrams from the entire totality of the geometric images corresponding to them
is proposed: “To decode the diagrams topology the schemes of uni- and invariant
states had been elaborated. This sort of schemes with phase’s routes
designations makes possible to calculate the number of phase regions, surfaces
and to know a type of every surface (plane, ruled or unruled surface). Detailed
analysis of T-x-y diagrams geometrical constructions had been carried out with
their aid, and their computer models had been designed” .(Read more)
In
the last decades, the use of agrochemicals has been a common practice in
intense agriculture, which has considerably increased pollution problems of
surface and ground water. Oxyfluorfen
[2-chloro-1-(3-ethoxy-4-nitrophenoxy)-4-(trifluromethyl)-benzene], a member of
the herbicide class nitrodiphenyl ether, has a high degree of weed control and
great versatility of application. Oxyfluorfen is considered to be highly resistant
to degradation in water. And has Potential adverse effects on the ecosystemeven if present at very low concentration levels, where the half-life of
oxyfluorfen ranged from 72 to 160 days for water. Many conventional methods
have been successfully applied for the efficient removal of oxyfluorfen from water
sources such as adsorption, advanced oxidation, photo Fenton, UV/H2O2
, and biological treatment.
In recent years novel methods for water
purification have been developed including chemical, electrochemical and
photochemical processes. In this scenario, the electrocoagulation (EC) is an
electrochemical has attracted increasing interest as a promising powerful
method for efficiently removing pesticides from water such as Malathion, methyl
parathion, atrazine and triazophos, imidacloprid and chlorpyrifos, and 2,4-
dichlorophenoxyacetic Acid (2,4-D).The
aim of this study is to conduct an experimental investigation on the removal of
a oxyfluorfen and COD from the aqueous solution using the electrocoagulation
method. and to investigate the kinetic and adsorption isotherm studies on the
removal efficiency.(Read more)
The
toxicity of free heme has been documented in several disease types. For
example, in hemolytic anemias such as sickle cell disease and thalassemia, release of heme from hemoglobin followinglysis of red blood cells is known to cause cell death. In a critical care
situation such as hemorrhagic injury, neuronal cell death is caused by the
lysis of red blood cells, which release hemoglobin and its breakdown product
hemin. Physiological levels of free heme in the blood are maintained at low
levels (0.1 -1 μM) by the high binding affinity of proteins such as serum albumin,
hemopexin and haptoglobin. When internalized, free heme is catabolized by heme
oxygenases (HO1 and HO2 isoforms) and therefore the amount of cellular damage
free heme produces is limited by the stress-responsive HO1 isoform.
In addition
to HO1 and HO2 isoform regulated cellular damage, the oxidative state of iron
(from Fe2+ to Fe3+ via the Fenton reaction) within heme
can produce harmful superoxide free radicals in the brain that can lead to
oxidative stress, initiation of lipid peroxidation and neuronal death.Pathological
conditions can increase the level of heme and iron. For example in acute
conditions such as severe hemolytic crisis in sickle cell disease,
heme levels can increase up to 20 μM or to greater than 200 μM (supraphysiological
levels) in thalassemia. Therefore, further studies on the cross talk between
neuroinflammatory mediators and iron-containing hemoproteins such as hemin are
warranted.(Read more)
