Design and One-Pot and Microwave-Assisted Synthesis of 2-Amino/5-Aryl-1,3,4-oxadiazoles Bearing a Benzimidazole Moiety as Antioxidants
In this study, two new series of 2-amino-1,3,4-oxadiazoles and 5-aryl-1,3,4-oxadiazoles carrying a benzimidazole... more In this study, two new series of 2-amino-1,3,4-oxadiazoles and 5-aryl-1,3,4-oxadiazoles carrying a benzimidazole moiety were synthesized. The antioxidant properties of these compounds were investigated in vitro by the determination of the microsomal NADPH-dependent inhibition of lipid peroxidation levels (LP), the microsomal ethoxyresorufin O-deethylase activity (EROD), and DPPH radical scavenger effects. Among the tested compounds, 2-[(2-(4-chlorophenyl)-1H-benzo[d]imidazole-1-yl)methyl]-5-(4-fluorophenyl)-1,3,4-oxadiazole (9) was found to be the most active compound in all three in vitro systems.
Synthesis and Evaluation of Antioxidant Properties of Novel 2-[2-(4-chlorophenyl)benzimidazole-1-yl]-N-(2-aryl methylene amino) acetamides and 2-[2-(4-chlorophenyl)benzimidazole-1-yl]-N-(4-oxo- 2-aryl-thiazolidine-3-yl) acetamides-I
Our approach was to synthesize and examine the antioxidant properties of some new... more Our approach was to synthesize and examine the antioxidant properties of some new 2-[2-(4-chlorophenyl)benzimidazole-1-yl]-N-(2-arylmethyleneamino) acetamide (1-18) and 2-[2-(4-chlorophenyl)benzimidazole-1-yl]-N-(4-oxo-2-aryl-thiazolidine-3-yl)acetamide (1t-18t) derivatives. Their in vitro effects on rat liver microsomal NADPH-dependent lipid peroxidation levels (LP assay) and microsomal ethoxyresorufin O-deethylase activities (EROD assay) were determined. The free radical scavenging properties of the compounds were also examined in vitro determining the interaction of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical. The compounds showed significant effects in the above tests.
2012: Quantification of particle-induced inflammatory stress response: a novel approach for toxicity testing of earth materials
Andrea D Harrington, Stella E Tsirka and Martin A.A. Schoonen Geochemical Transactions 2012, 13:4 doi:10.1186/1467-4866-13-4
Background
Reactive oxygen species (ROS) are vital regulators of many cellular functions in the body. The... more
Background
Reactive oxygen species (ROS) are vital regulators of many cellular functions in the body. The intracellular ROS concentration is highly regulated by a balance between pro-oxidants and anti-oxidants. A chronic excess of pro-oxidants leads to elevated ROS concentrations and inflammation, possibly initiating or enhancing disease onset. Mineral-induced generation of ROS, the role of minerals in upregulating cellular ROS, and their role in the development of several occupational diseases are now widely recognized. However, there is no standard protocol to determine changes in ROS production in cells after exposure to mineral dust or earth materials in general. In this study, a new method for determining the degree of cellular toxicity (i.e., cytotoxicity) of particles is described that will help bridge the gap in knowledge.
Results
By measuring the production of ROS and the viability of cells, an inflammatory stress response (ISR) indicator is defined. This approach normalizes the ROS upregulation with respect to the number of viable cells at the time of measurement. We conducted experiments on a series of minerals and soils that represent materials that are inert (i.e., glass beads, anatase, and a soil with low trace element content), moderately reactive (i.e., soil with high trace element content), and highly reactive (i.e., pyrite). Inert materials generated the lowest ISR, averaging 350% compared to the control. Acid washed pyrite produced the highest ISR (1,100 fold higher than the control). The measurements conducted as a function of time showed a complex response. Most materials showed an increase in ISR with particle loading.
Conclusions
The amount of cellularly generated ROS and cell viability combined provide a better understanding of particle-induced oxidative stress. The results indicate that some earth materials may solicit an initial burst of ROS, followed by a second phase in which cell viability decreases and ROS production increases, leading to a high ISR value. Hence, measurements conducted over a range of particle loading combined with multiple data measurements up to 24 hours can provide new insights in the possible effect of exposure to earth materials on human health.
BLOOD GLUCOSE RESPONSE OF CLARIAS GARIEPINUSEXPOSED TO ACUTE CONCENTRATIONS OF GLYPHOSATE-ISOPROPYLAMMONIUM (SUNSATE®)
Co-authored by Ataguba G.A.. Published in Journal of Agriculture and Veterinary Sciences
Clarias gariepinus with mean weight 6.86g +0.34 obtained from a homogenous source
through induced breeding were... more
Clarias gariepinus with mean weight 6.86g +0.34 obtained from a homogenous source
through induced breeding were exposed to different concentrations of Sunsate® for 96hours
using static bioassays with continuous aeration under laboratory conditions to determine the
acute toxicity of glyphosate in Sunsate® on the fish. LC50 of the exposed fingerlings were
found to be 17.5 mg l-1. The fish showed toxicosis symptoms such as loss of balance,
respiratory distress, vertical and erratic movement, accumulation of mucus on the body
surface and death. Result on blood glucose response shows that as the concentration
increases so the blood glucose, therefor precautious use of Sunsate®in the control of aquatic
weed is advised.
Growth, development and incidence of deformities in amphibian larvae exposed as embryos to naphthenic acid concentrations detected in the Canadian oil sands region
Melvin SD and VL Trudeau. 2012. Environmental Pollution. 167:178-183.
Naphthenic acids (NAs) have been identified as harmful environmental contaminants that influence survival, growth and... more Naphthenic acids (NAs) have been identified as harmful environmental contaminants that influence survival, growth and development of wildlife. Amphibian larvae are particularly susceptible to waterborne contaminants, but little information exists regarding exposure of amphibian embryos or tadpoles to NAs. Our results demonstrate that embryos of Lithobates pipiens and Silurana tropicalis exposed to 2 - 4 mg/l of a commercial NA blend suffer significant reductions (32% and 25%, respectively) in growth and development upon hatching. Increased incidences of deformities were observed in exposed individuals of both species, but were only significant in L. pipiens. Embryos suffered 100% mortality following exposure to 6 mg/l NAs, and narcosis at lower concentrations. LC50 estimates were 4.10 mg/l for 72-hrs exposure in L. pipiens and 4.13, 3.51, and 2.95 mg/l for 24-, 48-, and 72-hrs exposure in S. tropicalis. These data suggest that exposure to NAs at environmentally realized concentrations may negatively affect tadpole populations.
A comparison of venlafaxine and SSRIs in deliberate self-poisoning
Chan, Agnes N., Naren Gunja, and Christopher J. Ryan. 2010. A comparison of venlafaxine and SSRIs in deliberate self-poisoning. Journal of Medical Toxicology 6: 116-121.
To compare the clinical features of deliberate self- poisoning with venlafaxine and selective serotonin reuptake... more To compare the clinical features of deliberate self- poisoning with venlafaxine and selective serotonin reuptake inhibitors (SSRIs) presenting to the emergency department of an Australian tertiary referral hospital. A retrospective cohort study comparing all 36 patients who presented with venlafaxine self-poisoning with 44 randomly selected patients with SSRI self-poisoning between 1997 and 2006. Patients who had overdosed on venlafaxine were older (mean age 37.4 versus 28.8 years (p ≤ 0.001) and generally exhibited a higher degree of suicidal intent (p≤0.017). Median venlafaxine dose taken was 35 defined daily doses (DDDs) compared with SSRIs 19.4 DDDs. Those who ingested venlafaxine were more likely to become confused (25% versus 0%; p = 0) and have mydriasis (19.4% versus 2%; p ≤ 0.02), than those who took SSRIs. One patient from the venlafaxine group died. Compared with SSRI self-poisoners, patients who deliberately ingested venlafaxine were more likely to exhibit serious suicide intent. They were also more likely to be older, take a higher DDD of the drug, and have confusion and mydriasis. This has implications for management of severely depressed and suicidal patients.
Modafinil-induced psychosis
Wu, P., S. G. Jones, C. J. Ryan, D. Michail, and T. Robinson. 2008. Modafinil-induced psychosis. Internal Medicine Journal 38 (8): 677-678.
Modafinil is a relatively new wakefulness-promoting agent used for the treatment of excessive sleepiness due to... more Modafinil is a relatively new wakefulness-promoting agent used for the treatment of excessive sleepiness due to narcolepsy and other sleep disorders. We report on a man who had an acute psychotic episode after ingesting too much modafinil.
Strychnine Poisoning [Letter]
Ryan, Christopher James, and Josephine Anderson. 2002. Strychnine Poisoning [Letter] New England Journal of Medicine 345: 1577.
In an otherwise excellent discussion of strychnine poisoning in Case 12-2001 (April 19 issue), a diagnosis is assigned... more
In an otherwise excellent discussion of strychnine poisoning in Case 12-2001 (April 19 issue), a diagnosis is assigned that is unsupported by the data provided. The case concerned a 16-year-old boy with confusion.
The boy, who was born in Cambodia, had been given an herbal preparation that contained strychnine. The presentation was entirely consistent with strychnine poisoning, which is recorded as one of the anatomical diagnoses. However, for unclear reasons, the patient was also given an anatomical diagnosis of bipolar disease. This diagnosis is almost certainly wrong.
Lamoure J. How Do You Treat Internet Addiction. Cdn J of CME 2012; 24(3): 14
Lamoure J. How Do You Treat Internet Addiction. Cdn J of CME 2012; 24(3): 14
There are not many formats or forums at this point that address Internet addiction, and there is even some debate over... more
There are not many formats or forums at this point that address Internet addiction, and there is even some debate over whether internet addiction is a true addiction. In my clinical experience and given definitions of addiction, "I would place internet as
being a very highly addictive medium."........
...... It provides a strong “hook” to those who are looking for a form of escapism. That being said, it is legal, cost effective, accessible, and provides instant gratification. It can, however, have a deleterious impact on the patient’s quality and quantity of life, with psychosocial retardation, financial challenges, and relationship challenges.
Much like patients with food or shopping addictions, there is the challenge that it cannot be easily extricated from daily life, especially in western and first/second world countries. Standard strategies that include removal of the offending agent will not work with internet addictions as there is exposure in insidious ways.......
From "Lamoure J. How Do You Treat Internet Addiction. Cdn J of CME 2012; 24(3): 14" (In press)
Dr. Joel W. Lamoure RPh., DD., FASCP
http://www.joelwlamoure.com/id6.html
Concentration-Dependent, Size-Independent Toxicity of Citrate Capped AuNPs in Drosophila melanogaster
Giuseppe Vecchio*, Antonio Galeone, Virgilio Brunetti, Gabriele Maiorano, Stefania Sabella, Roberto Cingolani, Pier Paolo Pompa*
PLoS ONE 7(1): e29980. doi:10.1371/journal.pone.0029980
The expected potential benefits promised by nanotechnology in various fields have led to a rapid increase of the... more The expected potential benefits promised by nanotechnology in various fields have led to a rapid increase of the presence of engineered nanomaterials in a high number of commercial goods. This is generating increasing questions about possible risks for human health and environment, due to the lack of an in-depth assessment of the physical/chemical factors responsible for their toxic effects. In this work, we evaluated the toxicity of monodisperse citrate-capped gold nanoparticles (AuNPs) of different sizes (5, 15, 40, and 80 nm) in the model organism Drosophila melanogaster, upon ingestion. To properly evaluate and distinguish the possible dose- and/or size-dependent toxicity of the AuNPs, we performed a thorough assessment of their biological effects, using two different dose-metrics. In the first approach, we kept constant the total surface area of the differently sized AuNPs (Total Exposed Surface area approach, TES), while, in the second approach, we used the same number concentration of the four different sizes of AuNPs (Total Number of Nanoparticles approach, TNN). We observed a significant AuNPs-induced toxicity in vivo, namely a strong reduction of Drosophila lifespan and fertility performance, presence of DNA fragmentation, as well as a significant modification in the expression levels of genes involved in stress responses, DNA damage recognition and apoptosis pathway. Interestingly, we found that, within the investigated experimental conditions, the toxic effects in the exposed organisms were directly related to the concentration of the AuNPs administered, irrespective of their size.
APPLICATION OF THE “TRIANGULAR ECO-KINEMATICS THEORY” (TEKT) (PART I) - THE PARADIGM OF ECOLOGY, PUBLIC HEALTH AND ECONOMY AS A SYNERGISTIC EFFECT UPON HUMAN RIGHTS
Presented at the International Conference "Human Ecology: Health, Culture and Quality of Life, Oct. 26-27, 2011, Moscow, Russian Federation and Published in the "Herald of the International Academy of Science, Russian Section", 2011, Vol 1, ISSN 2221-7479 Full article [22 pages] in English with a Russian abstract and English abstract. Free download at http://www.heraldrsias.org/online/2011/1/203/
Upcoming updates on TEKT are on the way. Introductory presentation made during conference excerpts at http://youtu.be/kZkGKkbnGKE Comments and collaboration proposals are welcome. Thank you!
The laws governing natural economic flow are recommended to be used as model for a sustainable anthropogenic economy.... more
The laws governing natural economic flow are recommended to be used as model for a sustainable anthropogenic economy. Life can't be monopolized. Biodiversity has a paramount importance to sustainable development. This article is intended to be the first in a series of applicative works based on the Triangular Eco-Kinematics Theory «TEKT» proposed here as foundation for global cooperation mechanisms. It is an urgent call for global anthropogenic economic reforms. Planet Earth can sustain a maximum population load if it's properly managed. The Universal Declaration of Human Rights needs to be revised. A Life Equivalent Etalon [LEE] as currency reference is proposed. Key words: natural rights, Life Equivalent Etalon, LEE, gold, energy, protein, organization equilibrium theory, monetary system, entropy, antientropy, negentropy, syntropy, UNESCO, intangible commodities, economics, religion, protein, amino acids, seed germination, carbon dioxide, oxigen, dinitrogen, nitrogen, air, global warming, occupy wall street, occupy movement, evolution, macroeconomics.
Introduction.
Ecological issues should not be separated from economic issues or from public health concerns as they correlate. The global crises have their beginnings back in the history of mankind. Lately they are acutely identified and discussed as our natural resources are depleting visibly. Furthermore, the strong polarization of wealth, abusive exploitation of natural resources and excessive material accumulation do not just hinder the free economic flow, but are also unethical. It conducts to social segregation and conflicts; the expanding “occupy movement” is just one of the latest examples. With this paper, I am also calling for an urgent and closer look at Human Rights principles. Human Rights need to be a section of a future Universal Declaration of Natural Rights.
This paper (as part 1) is an attempt to address several interconnected issues in a fashion such as an overture to an upcoming series of work (work is in progress) with the belief that readers have a fairly strong natural inducement to co-operate [20] with the author in order to build and consolidate the proposed model, the presently included applications and the upcoming ones as well.
Fighting Nature is a historical human endeavor for which we just recently started to see the beginning of its outcome. Public health, ecological systems and global economics, being intimately interconnected, undergo a cycle of crises that I take the freedom to call “The Bermuda Triangle of Human Endeavors”. Planet Earth offers us as Humanity the means to support our very material existence. Health and ecology together are the primary life supporting elements that form the structures of a sustainable social and economic development.
Deprivation of proper living conditions represents an acute denial of Human Rights. No one has the right to deprive others from the inherited Natural Rights, the rights to exist. The economic principles need to be brought up to date and restructured such as to observe the non-monetary values going beyond Human Rights. For the economic system to be sustainable it needs to use a currency that has a sustainable etalon as reference. Life Equivalent Etalons (LEE) can assure economic and international stability as they are fixed and indispensable.
Each one of us is responsible for the global economy as it is an expression of human endeavor and its dynamics, more so in the context of globalization. I’ll tailor my work in a way to make it accessible to most people. It does not matter how good are whatever ideas one may have if they are not well understood by the intended audience, in this particular case, Humanity at large.The M.A.Sholokhov Moscow State University of Humanities is a great place to present this paper addressing ecological issues; such subjects are only about Humanity and concerns Humanity at large. What can be more human than human activity and its overall outcome?
Primary conclusions – Life’s properties and limitations
1) Acute and severely disastrous possible outcomes are due, a total collapse of the system is expected if one living entity is lowering its entropy (increasing anti-entropy) and comes too close to exhausting its own life support, regardless of the energy that may be available. Outgrowing life’s support capacity induces the destruction of the entire system, its entire collapse to decay possibly into lifeless while keeping the energy tightly locked into a stinky slime form of existence.
2) If our planet was to be populated only by forests and plants, cyanobacteria and green algae, Earth could have exhausted its life support and its destiny would have been limited to a continuous energy and structural accumulation up to the point when a total decay would have follow, perhaps a slimy world. Strange as it may appear my statement, we’ve seen in the above experimental example that as long as there are living entities consuming oxygen, ready synthesized sugars and proteins, having CO2 as waste on which the plants can feed on, the cycle of life can continue as long as the relative organizational equilibrium is being kept to a sustainable level or why not a sustainable rapport as represented by TEKT.
3) Based on the above, the biological classifications are forming two major groups:
a) The self-sustaining, food independent living entities (i.e. cyanobacteria, plantae),
b) The by-sustaining, food dependent living entities (i.e. animalia, etc.)
4) Thermodynamically, utilization of energy is not a mere “emerging property” of life, it is Life itself. Utilization of energy by living forms of existence is a self organizing and a conducting mechanism that “knows” to use energy efficiently. It knows when and how to accumulate the dissipated free energy, to “pump it” in the re-assembled structures. It concentrates energy reserves; it creates protective resistant ergonomic structures. The Life forms of material existence have as main property (as opposed to emerging property) the thermo-dynamical ability to act as heat energy pumps; Life forms of material existence are structures of concentrated energy ready to be used. A small seed has the ability to act as a heat energy pump concentrating dissipated free energy into a chemical structure with energy ready to use (i.e. burning wood producing heat).
5) The minerals and vitamins play a key roll in the kinematics of the Life phenomena, the energy, the dynamics of it, but the mother of all dynamics is the mystery of Life, the low entropy or high anti-entropy of information encoded in the DNA folds confers the ability to use and further concentrate more energy into a structural body, into the high anti-entropy of the newly grown living entity, the plants, the trees with their fruits and byproducts holding enormous incorporated energy as well. The high anti-entropy of information has the ability to concentrate low negentropy (high entropy) into high anti-entropy, ready to use concentrated forms of energy, a real gift of Life.
The ability to self-acquiring, holding, using and transmitting information we can also identify it as being a main property of Life.
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See the full article [ free PDF DOWNLOAD ] from
http://www.heraldrsias.org/online/2011/1/203/
Comments and contributions are welcome.

