Abstract: Heme oxygenase-1 (HO-1), an enzyme degrading heme to carbon monoxide, iron, and biliverdin, has been recognized as playing a crucial role in cellular defense against stressful conditions, not only related to heme release. In the present study, the effects of TNF-a on the expression of heme oxygenase-1 (HO-1) in human aortic endothelial cells (HAECs) as well as the related mechanisms were investigated. 10 ng/mL TNF-α treatment significantly increased HO-1 expression after 6h, then a further increase at 12h and declined at 24h. Treatment with 2 ng/mL of TNF-a after 12 h resulted in a significant increase in HO-1 expression, which peaked at 10 ng/mL, then declined at 20 ng/mL. TNF-α induced HO-1 expression and then HO-1 expression reduced vascular cell adhesion molecule-1 (VCAM-1) expression. Phosphorylation studies of ERK1/2, JNK, and p38, three subgroups of mitogen-activated protein kinases (MAPKs) demonstrated TNF-α-induced ERK1/2, JNK, and p38 phosphorylation. The increase in HO-1 expression in response to TNF-α treatment was affected by pretreatment with SP600125 (a JNK inhibitor) and SB203580 (a p38 inhibitor), not with PD98059 (an ERK1/2 inhibitor). The expression of HO-1 was stronger in aortas of TNF-α-treated apo-E deficient mice when compared with control mice. These results suggest that low dose of TNF-α treatment notably induced HO-1 expression was mediated through JNK/p38 phosphorylation and may have a protective potential in cardiovascular diseases and inflammatory response through the regulation of HO-1 expression.
Abstract: Currently, mathematical and computer modeling are widely used in different biological studies to predict or assess behavior of such a complex systems as a biological are. This study deals with mathematical and computer modeling of bi-substrate enzymatic reactions, which play an important role in different biochemical pathways. The main objective of this study is to represent the results from in silico investigation of bi-substrate enzymatic reactions in the presence of uncompetitive inhibitors, as well as to describe in details the inhibition effects. Four models of uncompetitive inhibition were designed using different software packages. Particularly, uncompetitive inhibitor to the first [ES1] and the second ([ES1S2]; [FS2]) enzyme-substrate complexes have been studied. The simulation, using the same kinetic parameters for all models allowed investigating the behavior of reactions as well as determined some interesting aspects concerning influence of different cases of uncompetitive inhibition. Besides, it has been shown that uncompetitive inhibitors exhibit specific selectivity depending on mechanism of bi-substrate enzymatic reaction.
Abstract: Microorganisms can be removed, inhibited or killed by physical agents, physical processes or chemical agents but they have their inherent disadvantages such as increased resistance against antibiotics etc. Since, plants have endless ability to synthesize aromatic substances which act as the master agents for plant defense mechanisms against microorganisms, insects and herbivores. Thus, secondary metabolites or phytochemicals obtained from plants can be used as agents of disease control nowadays. In the present study effect of different concentrations of acetone fraction of leaves and alcohol fraction of inflorescence of Euphorbia pulcherrima on various cytomorphological parameters i.e. cell number, mycelium width, conidial size, conidiophore size etc. of Aspergillus fumigatus has been studied. Change in mycelium/ hyphal cell width, conidium size, conidiophore size etc. was measured with the help of a previously calibrated oculometer. To study effect on morphology, fungal mycelium along with conidiophore and conidia were stained with cotton blue and mounted in lactophenol and observed microscopically. Inhibitory action of the acetone extract of Euphorbia pulcherrima leaf on growth of Aspergillus fumigatus was investigated. Control containing extract free medium supported profuse growth of the fungus. Although decrease in growth was observed even at 3.95μg/ml but significant inhibition of growth was started at7.81μg/ml concentration of the extract. Complete inhibition was observed at 15.62μg/ml and above. Microscopic examination revealed that at 3.95, 7.81 and 15.62μg/ml extract concentration hyphal cell width was found to be increased from 1.44μm in control to 3.86, 5.24 and 8.98 μm respectively giving a beaded appearance to the mycelium. Vesicle size was reduced from 24.78x20.08μm (control) to 11.34x10.06μm at 3.95μg/ml concentration. At 7.81 and 15.62μg/ml concentration no phialides and sterigmata were observed. Inhibitory action of the alcohol extract of inflorescence on the growth of Aspergillus fumigatus was also studied. Control containing extract free medium supported profuse growth of the fungus. Although decrease in growth was observed even at 3.95μg/ml but complete inhibition was observed at 62.5μg/ml and above. Microscopic examination revealed that hyphal cell width of Aspergillus fumigatus was found to be increased from 1.67μm in control to 5.84μm at MIC i.e. at 62.5μg/ml. Vesicle size was reduced from 44.76x 24.22μm (control) to 11.36x 6.80μm at 15.62μg/ml concentrations. At 31.25 μg/ml and 62.5μg/ml concentration no phialides and sterigmata was found. Spore germination was completely found to be inhibited at 3.95μg/ml concentration. Similarly 92.87% reduction in vesicle size was observed at 15.62μg/ml concentration. It is evident from the results that plant extracts inhibit fungal growth and this inhibition is concentration dependent.
Abstract: Probiotic bacteria especially Lactobacillus spp. and Bifidobacterium exert suppressive effect on Helicobacter pylori. Cinnamon and licorice have been traditionally used for the treatment of gastric ulcer. The objectives of this study were to determine the effects of herbs on yogurt fermentation, the level of probiotic bacteria in yogurt during 28 days storage and the effect of herbal yogurt on the growth of H. pylori in vitro. Cinnamon or licorice was mixed with milk and the mixture was fermented with probiotic bacteria to form herbal-yogurt. Changes of pH and total titratable acids were monitored and the viability of probiotic bacteria was evaluated during and after refrigerated storage. The in vitro inhibition of H. pylori growth was determined using agar diffusion and minimum inhibitory concentration (MIC) method. The presence of herbs did not affect the probiotic population during storage. There were no significant differences in pH and TTA between herbal-yogurts and plain-yogurt during fermentation and storage. Water extract of cinnamon-yogurt showed the highest inhibition effect (13.5mm) on H. pylori growth in comparison with licorice-yogurt (11.2mm). The present findings indicate cinnamon and licorice has bioactive components to decrease the growth of H. pylori.
Abstract: Adenylate kinase (AK) catalyse the phosphotransferase
reaction plays an important role in cellular energy homeostasis. The
inhibitors of bacterial AK are useful in the treatment of several
bacterial infections. To the novel inhibitors of AK, docking studies
performed by using the 3D structure of Bacillus stearothermophilus
adenylate kinase from protein data bank (IZIP). 46 Quinoxaline
analogues were docked in 1ZIP and selected the highly interacting
compounds based on their binding energies, for further studies
Abstract: Verapamil has been shown to inhibit fentanyl uptake in vitro and is a potent P-glycoprotein inhibitor. Tissue partitioning of loperamide, a commercially available opioid, is closely controlled by the P-gp efflux transporter. The following studies were designed to evaluate the effect of opioids on verapamil partitioning in the lung and brain, in vivo. Opioid (fentanyl or loperamide) was administered by intravenous infusion to Sprague Dawley rats alone or in combination with verapamil and plasma, with lung and brain tissues were collected at 1, 5, 6, 8, 10 and 60 minutes. Drug dispositions were modeled by recirculatory pharmacokinetic models. Fentanyl slightly increased the verapamil lung (PL) partition coefficient yet decreased the brain (PB) partition coefficient. Furthermore, loperamide significantly increased PLand PB. Fentanyl reduced the verapamil volume of distribution (V1) and verapamil elimination clearance (ClE). Fentanyl decreased verapamil brain partitioning, yet increased verapamil lung partitioning. Also, loperamide increased lung and brain partitioning in vivo. These results suggest that verapamil and fentanyl may be substrates of an unidentified inward transporter in brain tissue and confirm that verapamil and loperamide are substrates of the efflux transporter P-gp.
Abstract: By using the method of coincidence degree and constructing suitable Lyapunov functional, some sufficient conditions are established for the existence and global exponential stability of antiperiodic solutions for a kind of impulsive Cohen-Grossberg shunting inhibitory cellular neural networks (CGSICNNs) on time scales. An example is given to illustrate our results.
Abstract: In the Fe-3%Si sheets, grade Hi-B, with AlN and MnS
as inhibitors, the Goss grains which abnormally grow do not have a
size greater than the average size of the primary matrix. In this
heterogeneous microstructure, the size factor is not a required
condition for the secondary recrystallization. The onset of the small
Goss grain abnormal growth appears to be related to a particular
behavior of their grain boundaries, to the local texture and to the
distribution of the inhibitors. The presence and the evolution of
oriented clusters ensure to the small Goss grains a favorable
neighborhood to grow. The modified Monte-Carlo approach, which
is applied, considers the local environment of each grain. The grain
growth is dependent of its real spatial position; the matrix
heterogeneity is then taken into account. The grain growth conditions
are considered in the global matrix and in different matrixes
corresponding to A component clusters. The grain growth behaviour
is considered with introduction of energy only, energy and mobility,
energy and mobility and precipitates.
Abstract: Alcohol and water extracts of Cymbopogon citratus
was investigated for anti-bacterial properties and phytochemical
constituents. The extract was screened against four gram-negative
bacteria Escherichia coli, Klebsiella pneumoniae, Pseudomonas
aeruginosa, Proteus vulgaris) and two grampositive bacteria Bacillus
subtilis and Staphylococcus aureus at four different concentrations
(1:1, 1:5, 1:10 and 1:20) using disc diffusion method. The antibacterial
examination was by disc diffusion techniques, while the
photochemical constituents were investigated using standard
chemical methods. Results showed that the extracts inhibited the
growth of standard and local strains of the organisms used. The
treatments were significantly different (P = 0.05). The minimum
inhibitory concentration of the extracts against the tested
microorganisms ranged between 150mg/ml and 50mg/ml. The
alcohol extracts were found to be generally more effective than the
water extract. The photochemical analysis revealed the presence of
alkaloids and phenol but absence of cardiac and cyanogenic
glycosides. The presence of alkaloid and phenols were inferred as
being responsible for the anti-bacterial properties of the extracts.
Abstract: An experiment was conducted under controlled
conditions to study the effect of water extract of leaves, shoots and
roots of either Sisymbrium irio L. =SISIR and or Descurainia
sophia (L.) Schur =DESSO on the germination and primary growth
of barley. A split-split plot experiment in CRD with three
replications was used. The main plots were the type of weed: i.e.
SISIR and DESSO and the sub-plots were type of organ: i.e. leaf,
stem and root and, the sub-sub plots were concentration of the
water extract of each organ of the weeds: i.e. 0, 2, 4 and 8 % w/v.
The results showed that the SISIR water extracts had a greater
inhibitory effects on the germination and primary growth of barley
than those of DESSO water extracts. The water extracts of the
leaves of both weeds had the greatest inhibitory effects on the
germination and primary growth of barley, compared to those of
stems and roots. Increasing the concentration of water extracts of
leaves, stems and roots of both weeds up to 8 % caused the greatest
inhibitory effects to barley and reduced the germination rate and
primary growth of it linearly.
Abstract: Platinum oxide nanoparticles were prepared by a
simple hydrothermal route and chemical reduction using
carbohydrates (Fructose and sucrose) as the reducing and
stabilizing agents. The crystallite size of these nanoparticles was
evaluated from X-ray diffraction (XRD), atomic force microscopy
(AFM) and transmission electron microscopy (TEM) and was
found to be 10 nm as shown in figure 1, which is the
demonstration of EM bright field and transmission electron
microscopy. The effect of carbohydrates on the morphology of the
nanoparticles was studied using TEM (Figure 1). The
nanoparticles (100 μg/ml) were administered to the Pseudomonas
Stutzeri and Lactobacillus cultures and the incubation was done at
35 oC for 24 hours. The nanocomposites exhibited interesting
inhibitory as well as bactericidal activity against P. Stutzeri and
and Lactobacillus species. Incorporation of nanoparticles also
increased the thermal stability of the carbohydrates.
Abstract: The inhibition effect of brazilin to human bladder
tumor cell line T24 in vitro and in vivo was studied. The results of the
in vitro experiments showed that brazilin has strong inhibition activity
on the target cells. The inhibition ratio of 100 μg/mL brazilin and 100
μg/mL mitomycin to the target cells was 90.90 % and 63.24 %
respectively, which showed that brazilin has higher inhibition activity
than mitomycin under the same concentration. Brazilin could induce
cell apoptosis in T24 cells. Significant antitumor activity of brazilin
was also showed in the animals experiments. The life extention rate of
200 mg/mL, 300 mg/kg, and 400 mg/kg brazilin intraperitoneally
injected into Balb/c-nu-nu nude mice that with human bladder cancer
were 51.50 %, 56.90 %, and 58.42 %（P
Abstract: Glutathione S-transferase was purified from human
erythrocytes and effects of some polyphenols were investigated on
the enzyme activity. The purification procedure was performed on
Glutathione-Agarose affinity chromatography after preparation of
erythrocytes hemolysate with a yield of 81%. The purified enzyme
showed a single band on the SDS-PAGE. The effects of some
poliphenolic compounds such as catechin, dopa, dopamine, progallol
and catechol were examined on the in vitro GST activity. Catechin
was determined to be inhibitor for the enzyme, but others were not
effective on the enzyme as inhibitors or activators. IC50 value -the
concentration of inhibitor which reduces enzyme activity by 50%-
was estimated to be 10 mM. Ki constants were also calculated as 6.38
± 0,70 mM with GSH substrate, and 3.86 ± 0,78 mM with CDNB
substrate using the equations of graphs for the inhibitor, and its
inhibition type was determined as non-competitive.
Abstract: Saffron (Crocus sativus) is cultivated as spices,
medicinal and aromatic plant species. At autumn season, heavy
rainfall can cause flooding stress and inhibits growth of saffron. Thus
this research was conducted to study the effect of silver ion (as an
ethylene inhibitor) on growth of saffron under flooding conditions.
The corms of saffron were soaked with one concentration of nano
silver (0, 40, 80 or 120 ppm) and then planting under flooding stress
or non flooding stress conditions. Results showed that number of
roots, root length, root fresh and dry weight, leaves fresh and dry
weight were reduced by 10 day flooding stress. Soaking saffron
corms with 40 or 80 ppm concentration of nano silver rewarded the
effect of flooding stress on the root number, by increasing it.
Furthermore, 40 ppm of nano silver increased root length in stress.
Nano silver 80 ppm in flooding stress, increased leaves dry weight.
Abstract: The aim of this paper is to compare the effectiveness and electrochemical behavior of typical oilfield corrosion inhibitors with previous oilfield corrosion inhibitors under the same electrochemical techniques to control preferential weld corrosion of X65 pipeline steel in artificial seawater saturated with carbon dioxide at a pressure of one bar. A secondary aim is to investigate the conditions under which current reversal takes place. A flow channel apparatus was used in the laboratory to simulate the actual condition that occurs in marine pipelines. Different samples from the parent metal, the weld metal and the heat affected zone in the pipeline steel were galvanically coupled. The galvanic currents flowing between the weld regions were recorded using zero-resistance ammeters and tested under static and flowing conditions in both inhibited and uninhibited media. The results show that a current reversal took place when 30ppm of both green oilfield inhibitors were present, resulting in accelerated weld corrosion.
Abstract: A local wastewater treatment plant (WWTP)
experiencing poor nitrification tracked down high level of
surfactants in the plant-s influent and effluent. The aims of this project were to assess the potential inhibitory effect of surfactants on activated sludge processes. The effect of the
presence of TergitolNP-9, TrigetolNP-7, Trigetol15-S-9,
dodecylbenzene sulphonate (SDBS) and sodium dodecyl
sulfate (SDS) on activated sludge oxygen uptake rate (OUR) and nitrification were assessed. The average concentration of non-ionic and anionic
surfactants in the influent to the local WWTP were 7 and 8.7 mg/L, respectively. Removal of 67% to 90% of the non-ionic and 93-99% of the anionic surfactants tested were measured. All surfactants tested showed inhibitory effects both on OUR
and nitrification. SDS incurred the lowest inhibition whereas
SDBS and NP-9 caused severe inhibition to OUR and
Nitrification. Activated sludge flocs sizes slightly decreased
after 3 hours contact with the surfactant present in the test.
The results obtained indicated that high concentrations of
surfactants are likely to have an adverse effect on the
performance of WWTPs utilizing activated sludge processes.
Abstract: Hypertension is characterized with stress on the heart and blood vessels thus increasing the risk of heart attack and renal diseases. The Renin angiotensin system (RAS) plays a major role in blood pressure control. Renin is the enzyme that controls the RAS at the rate-limiting step. Our aim is to develop new drug-like leads which can inhibit renin and thereby emerge as therapeutics for hypertension. To achieve this, molecular dynamics (MD) simulation and receptor-based pharmacophore modeling were implemented, and three rennin-inhibitor complex structures were selected based on IC50 value and scaffolds of inhibitors. Three pharmacophore models were generated considering conformations induced by inhibitor. The compounds mapped to these models were selected and subjected to drug-like screening. The identified hits were docked into the active site of renin. Finally, hit1 satisfying the binding mode and interaction energy was selected as possible lead candidate to be used in novel renin inhibitors.
Abstract: Matrix metalloproteinases (MMP) are a class of
structural and functional related enzymes involved in altering the
natural elements of the extracellular matrix. Most of the MMP
structures are cristalographycally determined and published in
WorldWide ProteinDataBank, isolated, in full structure or bound to
natural or synthetic inhibitors. This study proposes an algorithm to
replace missing crystallographic structures in PDB database. We
have compared the results of a chosen docking algorithm with a
known crystallographic structure in order to validate enzyme sites
reconstruction there where crystallographic data are missing.
Abstract: Climate change and environmental pressures are
major international issues nowadays. It is time when governments,
businesses and consumers have to respond through more
environmentally friendly and aware practices, products and policies.
This is the prime time to develop alternative sustainable construction
materials, reduce greenhouse gas emissions, save energy, look to
renewable energy sources and recycled materials, and reduce waste.
The utilization of waste materials (slag, fly ash, glass beads, plastic
and so on) in concrete manufacturing is significant due to its
engineering, financial, environmental and ecological benefits. Thus,
utilization of waste materials in concrete production is very much
helpful to reach the goal of the sustainable construction. Therefore,
this study intends to use glass beads in concrete production.
The paper reports on the performance of 9 different concrete
mixes containing different ratios of glass crushed to 5 mm - 20 mm
maximum size and glass marble of 20 mm size as coarse aggregate.
Ordinary Portland cement type 1 and fine sand less than 0.5 mm were
used to produce standard concrete cylinders. Compressive strength
tests were carried out on concrete specimens at various ages. Test
results indicated that the mix having the balanced ratio of glass beads
and round marbles possess maximum compressive strength which is
3889 psi, as glass beads perform better in bond formation but have
lower strength, on the other hand marbles are strong in themselves
but not good in bonding. These mixes were prepared following a
specific W/C and aggregate ratio; more strength can be expected to
achieve from different W/C, aggregate ratios, adding admixtures like
strength increasing agents, ASR inhibitor agents etc.
Abstract: In this study, the effect of L-arginine was examined at the neuromuscular junction of the chick biventer cervicis muscle. LArginine at 500 μg/ ml, decreased twitch response to electerical stimulation, and produced rightward shift of the dose- response curve for acetylcholine or carbachol. L-Arginine at 1000μg/ ml produced a strong shift to the right of the dose – response curve for acetylcholine or carbachol with a reduction in the efficacy. The inhibitory effect of L-arginine on the twitch response was blocked by caffeine (200μg/ ml). NO levels were also measured in the chick biventer cervicis muscle homogenates, using spectrophotometric method for the direct detection of NO, nitrite and nitrate. Total nitrite (nitrite + nitrate) was measured by a spectrophotometer at 540 nm after the conversion of nitrate to nitrite by copperized cadmium granules. NO levels were found to be significantly increased in concentrations 500 and 1000μg/ ml of L-arginine in comparison with the control group (p