Saturday, July 31, 2010
I have read about co-operative catalysis (heterogeneous catalysts), but this is something interesting to me..
"Cooperative catalysis by carbens and Lewis acids in a highly stereoselective route to γ-lactams."
Ref : http://www.nature.com/nchem/journal/vaop/ncurrent/full/nchem.727.html
Friday, July 30, 2010
UMass Medical School will be the coordinating site for a $2.1 million, three-year clinical trial funded by the Foundation Fighting Blindness/National Neurovision Research Institute quantifying the potential of valproic acid as a treatment for RP. The clinical trials will build upon Kaushal's work in the retrospective study in which patients were treated off-label with doses of valproic acid ranging from 500mg to 750mg per day over the course of two to six months. Treated at a time when patients normally experience rapid vision loss as a result of RP, five of the seven patients in the study experienced improvement in their field of vision.
"Inflammation and cell death are key components of RP," said Kaushal. "It appears the valproic acid protects photoreceptor cells from this. If our observations can be further substantiated by randomized clinical trials then low dose valproic acid could have tremendous potential to help the thousands of people suffering from RP."
Dr. Kaushal and colleagues, having previously demonstrated the use of the small molecule, retinoid, as a pharmacological agent capable of increasing the yield of properly folded RP rhodopsins, began screening other small molecules for similar attributes. Because of its already known qualities as a potent inhibitor of the inflammatory response pathway and cell death, valproic acid was believed to have a unique profile making it a potential candidate as a retinal disease treatment...
Thursday, July 29, 2010
Wednesday, July 28, 2010
Cytrx’s tamibarotene achieves molecular complete remission in advanced acute promyelocytic leukemia..
"This event represents a very significant milestone for CytRx and our drug candidate tamibarotene. Tamibarotene has saved a life and nothing can compare with that," said CytRx President and CEO Steven A. Kriegsman. "These important results indicate that tamibarotene warrants further evaluation as a third-line treatment and in combination as a first-line treatment for APL. We are also considering developing tamibarotene for other cancers as well.
Previously published reports indicate that tamibarotene is 10-times more potent and may be better tolerated than all trans retinoic acid (ATRA). Researchers believe that the combination of tamibarotene and arsenic trioxide (ATO) could produce a complete response rate similar to the ATRA and ATO combination with fewer toxicities such as APL differentiation syndrome. The company is currently conducting a dose escalation trial combining tamibarotene with ATO as an important step in their ultimate goal of evaluating tamibarotene as a first-line treatment for APL. The company claims that, In addition to maintaining a complete remission six months following the last dose, tamibarotene was also well tolerated. In the CytRx's STAR-1 registration trial, patient was treated with tamibarotene for 56 days at the Department of Biopathology at the University of Rome 'Tor Vergata'. A molecular complete remission in the bone marrow was documented at the end of the treatment period and again six months following the last treatment with tamibarotene...
Tuesday, July 27, 2010
"These changes provide valuable new molecular insights into the mechanism of the antiobesity effects of capsaicin the scientists say"...
Through secretion of adipokines into the blood, adipose tissue plays a central role in development of these syndromes. In particular, white adipose tissue (WAT) functions as an energy storage organ through formation of triacylglycerol and release of fatty acids into the bloodstream during a shortage of energy. In association with overnutrition, excess WAT play a major role in obesity and obesity-related disorders through dysregulation of adipokine secretion from WAT. Therefore, inhibition of excess WAT can be an efficient strategy for prevention of obesity and metabolic disorders.
Researchers concludes that, thermogenesis and lipid metabolism related proteins were markedly altered upon capsaicin treatment in WAT, suggesting that capsaicin may be a useful phytochemical for attenuation of obesity....
Monday, July 26, 2010
"We are encouraged by these study results as they illustrate the tolerability of tapentadol ER compared with oxycodone CR, a standard chronic pain treatment," said Dr. Bruce Moskovitz, Therapeutic Area Leader for Pain, Ortho-McNeil Janssen Scientific Affairs, LLC. "We are pleased about the possibility of bringing this important investigational compound forward to patients in the future."
This study of tapentadol ER examined its long-term safety and tolerability compared to oxycodone CR and the primary objective of this study was to evaluate the safety of twice-daily doses of tapentadol ER (100 to 250 mg) over one year. Patients were randomized in a 4:1 ratio to receive controlled, adjustable, oral, twice-daily doses of tapentadol ER (100-250 mg) or oxycodone HCl CR (20-50 mg) in open-label treatment for up to one year. There were 1,117 patients in the study that received at least one dose of study medication (tapentadol).
Sunday, July 25, 2010
Saturday, July 24, 2010
The European Society of Cardiology (ESC) is concerned that interpretations of a paper about cholesterol, published in the Lancet , could act to deter ongoing research efforts into developing new therapeutic strategies to increase high density lipoprotein (HDL) cholesterol. Caution, the ESC experts advise, should be displayed in the interpretation of the results.....
In the Lancet study, Paul Ridker and colleagues, from Brigham and Women's Hospital (Boston, MA, USA), undertook a retrospective post-hoc analysis of the JUPITER trial. The results show that if a normal, healthy individual has level of low density lipoprotein (LDL), known as "bad cholesterol", substantially lowered with a potent statin, then the level of HDL "good cholesterol" in that person no longer bears any relation to the remaining cardiovascular risk. More.....
Thursday, July 22, 2010
Proteasome inhibitor bortezomib inhibits T cell-dependent inflammatory responses - a new hope for autoimmune and inflammatory diseases?
"We believe that this new-type remedy for autoimmune and inflammatory disease could successfully treat them in the near future", claims Dr. Koichi Yanaba...
As per the claim by the researchers, bortezomib potently inhibited CHS responses. The attenuation of CHS responses was associated with decreased inflammatory cell infiltration in the challenged skin. Specifically, bortezomib-treated mice showed significantly decreased numbers of CD4+ and CD8+ T cells in the challenged skin and draining lymph nodes. Cytoplasmic IFN- production by CD4+ and CD8+ T cells in the draining lymph nodes was decreased substantially by bortezomib treatment. Notably, bortezomib enhanced T cell apoptosis by inhibiting NF-B activation during CHS responses. Thus, bortezomib treatment is likely to induce T cell death, thereby suppressing CHS responses by reducing IFN- production. These findings suggest that bortezomib treatment could be a promising strategy for treating autoimmune and inflammatory disease.
Wednesday, July 21, 2010
We know that, honey has antibiotic activity and has been used specially in burn injuries. Now researchers lead by Dr.Sebastian A.J. Zaat, of Department of Medical Microbiology at the Academic Medical Center in Amsterdam, have come up with an explanation for this antibiotic activity of honey. This first explanation to explain how honey kills bacteria. Specifically, the research shows that bees make a protein that they add to the honey, called defensin-1, which could one day be used to treat burns and skin infections and to develop new drugs that could combat antibiotic-resistant infections.
"We have completely elucidated the molecular basis of the antibacterial activity of a single medical-grade honey, which contributes to the applicability of honey in medicine," said Dr. Sebastian A.J. Zaat...
To make the discovery, Dr. Zaat and colleagues investigated the antibacterial activity of medical-grade honey in test tubes against a panel of antibiotic-resistant, disease-causing bacteria. They developed a method to selectively neutralize the known antibacterial factors in honey and determine their individual antibacterial contributions. Ultimately, researchers isolated the defensin-1 protein, which is part of the honey bee immune system and is added by bees to honey. All bacteria tested, including Bacillus subtilis, methicillin-resistant Staphylococcus aureus, extended-spectrum β-lactamase producing Escherichia coli, ciprofloxacin-resistant Pseudomonas aeruginosa, and vancomycin-resistant Enterococcus faecium, were killed by 10–20% (v/v) honey, whereas 40% (v/v) of a honey-equivalent sugar solution was required for similar activity.
After analysis, the scientists concluded that the vast majority of honey's antibacterial properties come from that protein. This information also sheds light on the inner workings of honey bee immune systems, which may one day help breeders create healthier and heartier honey bees.
Monday, July 19, 2010
Researchers lead by Mark Brown of Wake Forest University School of Medicine, have come up with an interesting finding that is "there is more than one way to get rid of that cholesterol, which can otherwise lead to atherosclerosis and heart disease".
A model of cholesterol loss first proposed way back in the 1920s suggested the existence of a route that didn't rely on bile. And indeed, studies in dogs unable to get cholesterol into bile showed that the animals actually experienced an increase in cholesterol loss. More recent studies in mice showed a similar thing. Even so, the researchers said that an alternative pathway has largely been ignored. As a result, scientists have made very little progress in defining the molecular pathways and players involved.
Now, Brown and his colleagues offer new evidence that helps support and clarify this alternate path for cholesterol. Researchers report that mice made unable to secrete cholesterol into bile through genetic manipulation or surgery still lose cholesterol through the feces at a normal rate. Macrophages in those animals also continued to take up cholesterol from blood vessels. The researchers believe that alternate path delivers cholesterol from the liver to the intestine directly through the bloodstream.
"The classic view of reverse cholesterol transport involved the delivery of peripheral cholesterol via HDL to the liver for secretion into bile," the researchers wrote. "In parallel, we believe that the liver also plays a gatekeeper role for nonbiliary fecal sterol loss by repackaging peripheral cholesterol into nascent plasma lipoproteins that are destined for subsequent intestinal delivery."
For the purposes of cholesterol-lowering drug discovery, it may prove fruitful to consider those two pathways as "separate and compel", claims the lead researcher.
Researchers claims that the drugs aimed to increase cholesterol loss without relying on bile will have fewer side effects (an excess of cholesterol in bile can lead to gallstones). Let us be optimistic and hope for the best, in the near future...
Sunday, July 18, 2010
In continuation of my update on the dietary benefits of broccoli and how it helps to reduce the cancer risk....
Researchers writing in BioMed Central's open access journal Molecular Cancer have found that sulforaphane, a chemical found in broccoli, interacts with cells lacking a gene called PTEN to reduce the chances of prostate cancer developing.
Richard Mithen, from the Institute of Food Research, an institute of BBSRC, worked with a team of researchers on Norwich Research Park, UK, to carry out a series of experiments in human prostate tissue and mouse models of prostate cancer to investigate the interactions between expression of the PTEN gene and the anti cancer activity of sulforaphane.
"PTEN is a tumour suppressor gene, the deletion or inactivation of which can initiate prostate carcinogenesis, and enhance the probability of cancer progression. We've shown here that sulforaphane has different effects depending on whether the PTEN gene is present."
The research team found that in cells which express PTEN, dietary intervention with SF has no effect on the development of cancer. In cells that don't express the gene, however, sulforaphane causes them to become less competitive, providing an explanation of how consuming broccoli can reduce the risk of prostate cancer incidence and progression.
Saturday, July 17, 2010
Cohen and his Israeli colleagues focused on the interaction between two insect species found in temporary pools of the Mediterranean and the Middle East: larvae of the mosquito C. longiareolata and its predator, the backswimmer N. maculata. When the arriving female mosquitoes detect a chemical emitted by the backswimmer, they are less likely to lay eggs in that pool.
Thursday, July 15, 2010
"Of all the extracts tested (out of leaves, bark, seeds and apples), only cashew seed extract significantly stimulated blood sugar absorption by muscle cells," says senior author Pierre S. Haddad, a pharmacology professor at the University of Montreal's Faculty of Medicine. "Extracts of other plant parts had no such effect, indicating that cashew seed extract likely contains active compounds, which can have potential anti-diabetic properties."
Researchers conclude that, activation of adenosine monophosphate-activated protein kinase by CSE and AA likely increases plasma membrane glucose transporters, resulting in elevated glucose uptake. In addition, the dysfunction of mitochondrial oxidative phosphorylation may enhance glycolysis and contribute to increased glucose uptake. These results collectively suggest that CSE may be a potential anti-diabetic nutraceutical.
Tuesday, July 13, 2010
"This neuroprotective compound, called P7C3, holds special promise because of its medication-friendly properties. It can be taken orally, crosses the blood-brain barrier with long-lasting effects, and is safely tolerated by mice during many stages of development." claims Dr.Steven McKnight
Prolonged treatment of aged rats with P7C3 also enhanced the birth of new neurons. "Aged rats normally show a decline in neurogenesis associated with an inability to form new memories and learn tasks," Pieper explained..
In their study, rats treated with P7C3 each day showed evidence of an increase in the formation of newborn neurons and significant improvements in their ability to swim to the location of a missing platform, s standardized test of larning and memory in rats.
Monday, July 12, 2010
Plant extract may be effective against inflammatory bowel disease
Saturday, July 3, 2010
Now researchers at the Ohio State University Comprehensive Cancer Center-Arthur G. James Cancer Hospital and Richard J. Solove Research Institute (OSUCCC-James) have discovered how a substance (see below structure) that is produced when eating broccoli and Brussels sprouts can block the proliferation of cancer cells.
The laboratory and animal study discovered a connection between I3C and a molecule called Cdc25A, which is essential for cell division and proliferation. The research showed that I3C causes the destruction of that molecule and thereby blocks the growth of breast cancer cells.
"Cdc25A is present at abnormally high levels in about half of breast cancer cases, and it is associated with a poor prognosis," says study leader Xianghong Zou, assistant professor of pathology at the Ohio State University Medical Center.For this study, Zou and his colleagues exposed three breast cancer cell lines to I3C. These experiments revealed that the substance caused the destruction of Cdc25A. They also pinpointed a specific location on that molecule that made it susceptible to I3C, showing that if that location is altered (because of a gene mutation), I3C no longer causes the molecule's destruction.
Last, the investigators tested the effectiveness of I3C in breast tumors in a mouse model. When the substance was given orally to the mice, it reduced tumor size by up to 65 percent. They also showed that I3C had no affect on breast-cell tumors in which the Cdc25A molecule had a mutation in that key location.
Ref : American Association for Cancer Research : Cancer Prevention Research, Xianghong Zou et al.,
Friday, July 2, 2010
"These studies are certainly very exciting, and suggest for the first time that certain antihypertensive drugs already available to the public may independently influence memory functions while reducing degenerative pathological features of the Alzheimer’s disease brain," said study author Giulio Maria Pasinetti, MD, PhD, Saunders Family Professor of Neurology and Director of the Center of Excellence for Novel Approaches to Neurotherapeutics at Mount Sinai School of Medicine....
Thursday, July 1, 2010
Ingredient in red wine may prevent some blinding diseases