Phase 3 study: Tapentadol ER lowers incidence of gastrointestinal adverse events..

Tapentadol (see structure) is a new molecular entity that is structurally similar to tramadol (Ultram). It is a centrally-acting analgesic with a dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor. While its action reflects aspects of tramadol and morphine its ability to kill pain is more on the order of hydrocodone and oxycodone. Interestingly it  has opioid and nonopioid acitivity in a single compound.  Tapentadol is FDA approved for the treatment of moderate to severe acute pain. Due to the dual mechanism of action as an opioid agonist and norepinephrine reuptake inhibitor is potential for off use in chronic pain.

Tapentadol was developed by Grünenthal in conjunction with Johnson & Johnson Pharmaceutical Research and Development. It is being marketed as immediate release oral tablets of 50 mg, 75 mg, and 100 mg under the brabd name Nucynta.

A Phase 3 open-label study (by Johnson & Johnson Pharmaceutical Research & Development, L.L.C), recently published online by Pain Practice, has compared tapentadol extended release (ER) tablets, an investigational pain medication, to an existing prescription pain medication, oxycodone controlled release (CR) tablets.

The study found tapentadol ER was associated with a lower overall incidence of gastrointestinal adverse events than oxycodone CR (tapentadol ER, 52.0 percent; oxycodone CR, 64.1 percent) in patients with chronic knee or hip osteoarthritis pain or chronic low back pain, including: Constipation (tapentadol ER, 22.6 percent; oxycodone CR, 38.6 percent); Nausea (tapentadol ER, 18.1 percent; oxycodone CR, 33.2 percent); and Vomiting (tapentadol ER, 7.0 percent; oxycodone CR, 13.5 percent).

The median duration of treatment was substantially longer with tapentadol ER (268 days) than with oxycodone CR (59 days), and the incidence of overall gastrointestinal treatment-emergent adverse events (TEAEs) leading to study discontinuation was approximately 2.5 times greater in the oxycodone CR group than in the tapentadol ER group (oxycodone CR, 21.5 percent; tapentadol ER, 8.6 percent). In addition, the incidence of constipation leading to study discontinuation was 4.5 times greater in the oxycodone CR group than in the tapentadol ER group (oxycodone CR, 7.2 percent; tapentadol ER, 1.6 percent).

The study also found tapentadol ER provided sustainable relief of moderate to severe chronic knee or hip osteoarthritis pain or chronic low back pain for up to one year. At baseline, mean pain intensity scores in the tapentadol ER and oxycodone CR groups, respectively, were 7.6 and 7.6; at endpoint, they had decreased to 4.4 and 4.

"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).

Ref : http://www.jnjpharmarnd.com/jnjpharmarnd/news_release_02042010.html

Toward a new generation of superplastics

Toward a new generation of superplastics

No Firm Conclusions About HDL Cholesterol Can Be Drawn from JUPITER Sub-Analysis

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.....

Ref : http://www.thelancet.com/journals/lancet/article/PIIS0140-6736%2810%2960713-1/fulltext

Proteasome inhibitor bortezomib inhibits T cell-dependent inflammatory responses - a new hope for autoimmune and inflammatory diseases?

In continuation of my update on Bortezomib, I found this info interesting to share with..

Japanese scientists lead by Dr. Koichi Yanaba, of Department of Dermatology at Nagasaki University Graduate School of Biomedical Sciences used mice to show that bortezomib, currently used to treat cancers that affect white blood cells, induces cell death only in harmful (active and proliferating) T cells, leaving the rest unharmed. If the results prove true in humans, it offers hope that this drugs or others similar to it might be used to treat inflammatory diseases without the side effects of current drugs that affect all T cells equally.

To make this discovery, scientists used two groups of mice the first treated with bortezomib and the second with saline. Researchers induced contact hypersensitivity reaction with oxazolone, a chemical allergen used for immunological experiments and found that bortezomib significantly inhibited the contact hypersensitivity responses. Results strongly suggest that bortezomib treatment enhanced T cell death by inhibiting NF-kappa B activation, which plays a key role in regulating the immune response to infection. This in turn led to the suppression of inflammatory responses in immune cells by reducing interferon-gamma production.

"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.

Ref :http://www.jleukbio.org/cgi/content/abstract/88/1/117

How honey kills bacteria..........

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.

http://www.fasebj.org/cgi/content/abstract/24/7/2576

Cholesterol's Other Way out ....

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...

Ref : http://www.cell.com/cell-metabolism/abstract/S1550-4131%2810%2900186-5

Anti-Cancer Effects of Broccoli Ingredient Explained......

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.

Ref :  http://www.molecular-cancer.com/content/pdf/1476-4598-9-189.pdf

Predator-released hydrocarbons repel oviposition by a mosquito - nature's insect repellents ?

                                                                   N-Heneicosane 

                                                                    N-Tricosane

Many animals use chemicals to communicate with each other. Pheromones (most of us are familiar with these class of semi-synthetic compounds-used mainly as insect repellents) which influence social and reproductive behaviors within a particular species, are probably the best known and studied. Kairomones are produced by an individual of one species and received by an individual of a different species, with the receiving species often benefiting at the expense of the donor.

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.

To reproduce conditions of temporary pools in the field, the researchers used aged tap water with fish food added as a source of nutrients. Individual backswimmers were then placed in vials containing samples of the temporary pools, and air samples were collected from the headspace within the vials. The researchers used gas chromatography-mass spectrometry to analyze the chemicals emitted by the backswimmers.

Cohen and his colleagues identified two chemicals, hydrocarbons called n-heneicosane and n-tricosane (see structures), which repelled egg-laying by mosquitoes at the concentrations of those compounds found in nature. Together, the two chemicals had an additive effect.

Since the mosquitoes can detect the backswimmer's kairomones from above the water's surface, predator-released kairomones can reduce the mosquito's immediate risk of predation, says Cohen. But they also increase the female mosquito's chance of dying from other causes before she finds a pool safe for her to lay her eggs in.

Researchers conclude that, these newly identified compounds, and others that remain to be discovered, might be effective in controlling populations of disease-carrying insects. It's far too soon to say, but there's the possibility of an advance in the battle against infectious disease.

http://www3.interscience.wiley.com/journal/123572945/abstract?CRETRY=1&SRETRY=0

Cashew Seed Extract an Effective Anti-Diabetic ?

Cashew seed extract (hydroethanolic extract) shows promise as an effective anti-diabetic, according to a new study from the University of Montreal (Canada) and the Université de Yaoundé (Cameroun). The investigation analyzed the reputed health benefits of cashew tree products on diabetes, notably whether cashew extracts could improve the body's response to its own insulin.

The researchers claims that hydroethanolic extract of cashew seed (CSE) and its active component, anacardic acid (see structure), stimulated glucose transport into C2C12 myotubes in a concentration-dependent manner. Extracts of other parts (leaves, bark and apple) of cashew plant were inactive. Significant synergistic effect on glucose uptake with insulin was noticed at 100 g/mL CSE. CSE and AA caused activation of adenosine monophosphate-activated protein kinase in C2C12 myotubes after 6 h of incubation. No significant effect was noticed on Akt and insulin receptor phosphorylation. Both CSE and AA exerted significant uncoupling of succinate-stimulated respiration in rat liver mitochondria.

"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.

Cashew tree products have long been reported to be effective anti-inflammatory agents, counter high blood sugar and prevent insulin resistance among diabetics. This study validates the traditional use of cashew tree products in diabetes and points to some of its natural components that can serve to create new oral therapies...

Ref  : http://www3.interscience.wiley.com/journal/123573729/abstract?CRETRY=1&SRETRY=0

Discovery of a Proneurogenic, Neuroprotective Chemical.....

Scientists from University of Texas Southwestern Medical Center, Dallas, lead by Dr.Steven McKnight,  have discovered a compound (see structure)  that restores the capacity to form newmemories in aging rats, likely by improving the survival of newborn neurons in the brain's memory hub. The research has turned up clues to a neuroprotective mechanism that could lead to a treatment for Alzheimer's disease.

"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

In hopes of finding compounds that might protect such vulnerable neurons during this process, Pieper, McKnight and colleagues tested more than 1000 small molecules in living mice. One of the compounds, designated P7C3 (see structure), corrected deficits in the brains of adult mice engineered to lack a gene required for the survival of newborn neurons in the hippocampus. Giving P7C3 to the mice reduced programmed death of newborn cells,  normalizing stunted growth of branch-like neuronal extensions and thickening an abnormally thin layer of cells by 40 percent. Among clues to the mechanism by which P7C3 works, the researchers discovered that it protects the integrity of machinery for maintaining a cell's energy level.

To find out if P7C3 could similarly stem aging-associated neuronal death and cognitive decline, the researchers gave the compound to aged rats. Rodents treated with P7C3 for two months significantly outperformed their placebo-treated peers on a water maze task, a standard assay of hippocampus-dependent learning. This was traced to a three fold higher-than-normal level of newborn neurons in the dentate gyrus of the treated animals. Rats were used instead of mice for this phase of the study because the genetically engineered mice could not swim.

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.

The key to the treatment's success is the protection of newborn neurons, the researchers report. In fact, they explained, the normal process by which newborn neurons are incorporated into the brain as mature cells is a long and perilous one. Notably, they say that two other drugs (Dimebon and Serono compounds) -- both of which bear structural similarities to P7C3 -also encourage the growth of new neurons. It's tempting to think that all three compounds work in the same way the researchers pinpointed a derivative of P7C3, called A20, which is even more protective than the parent compound. They also produced evidence suggesting that two other neuroprotective compounds eyed as possible Alzheimer's cures may work through the same mechanism as P7C3. The A20 derivative proved 300 times more potent than one of these compounds currently in clinical trials for Alzheimer's disease. This suggested that even more potent neuroprotective agents could potentially be discovered using the same methods. Following up on these leads, the researchers are now searching for the molecular target of P7C3 -  key to discovering the underlying neuroprotective mechanism.

Ref : http://www.cell.com/retrieve/pii/S0092867410006720

Plant extract may be effective against inflammatory bowel disease

In continuation of my update on Broccoli and other Brassica family...
Plant extract may be effective against inflammatory bowel disease

How Dietary Supplement (Broccoli, Cabbage) May Block Cancer Cells....

In continuation of  how dietary supplement may block cancer cells... In my earlier blogs,  I have mentioned that, natural compound formed during the autolytic breakdown of glucobrassicin present in food plants of the Brassica genus, including broccoli, cabbage, Brussels sprouts, cauliflower and kale) are responsible for the anticancer activity associated with broccoli and other Brassica genus.

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.

Compelling evidence indicates that the substance, indole-3-carbinol [(above structure, I3C) : Glucobrassicin (right structure) is a type of glucosinolate that can be found in almost all cruciferous plants, such as cabbages  and broccoli, degradation by the enzyme myrosinase is expected to produce an isothiocyanate, indol-3-ylmethylisothiocyanate- which is unstable and hydrlyses to give, I3C, as most dominant degradation product], may have anticancer effects and other health benefits, the researchers say. These findings show how I3C affects cancer cells and normal 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.,

Antihypertensive Drugs May Protect Against Alzheimer's Disease....

Researchers at Mount Sinai School of Medicine have found that the drug carvedilol (see structure), currently prescribed for the treatment of hypertension, may lessen the degenerative impact of Alzheimer's Disease and promote healthy memory functions.  

"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....

Dr. Pasinetti’s team found for the first time that carvedilol, a blood pressure lowering agent, is capable of exerting activities that significantly reduce Alzheimer’s disease-type brain and memory degeneration. This benefit was achieved without blood pressure lowering activity in mice genetically modified to develop Alzheimer’s disease brain degeneration and memory impairment.

They also found that carvedilol treatment was capable of promoting memory function, based on assessments of learning new tasks and information and recall of past information, which is already chemically stored in the brain. In the study, one group of mice received carvedilol treatment and the other group did not. The scientists conducted behavioral and learning tests with each group of mice, and determined that it took the mice in the carvedilol significantly less time to remember tasks than the other group.

Ongoing clinical research is in progress to test the benefits of carvedilol, which may prove to be an effective agent in the treatment of symptoms of Alzheimer’s disease,   hope they will come out with positive results...

Ref : http://www.j-alz.com/issues/21/vol21-2.html

Ingredient in red wine may prevent some blinding diseases

In continuation of my update on Resveratrol.......
Ingredient in red wine may prevent some blinding diseases

Palladium-Catalyzed Trifluoromethylation of Aryl Chlorides..

When I  was working with one of the leading agrochemicals company, I was using 4-chlorobenzotriflouride as starting material for my two projects (trifluralin and a pyrazole derivative with diflouromethyl substituted phnyl).  I know how difficult is to introduce the triflouromethyl group (use of anhydrous HF to convert CCl3 to CF3) and that is why we got the starting material imported. 

Now, MIT chemists have designed a new way to attach a trifluoromethyl group to certain compounds, which they believe could allow pharmaceutical companies to create and test new drugs much faster and potentially reduce the cost of drug discovery. 

MIT Chemistry Professor Stephen Buchwald, who led the research team, says achieving the synthesis has been a long-standing challenge for chemists. "Some people said it couldn't be done, so that's a good reason to try," says Buchwald, the Camille Dreyfus Professor of Chemistry at MIT.

With the new reaction, the CF₃ group can be added at a much later stage of the overall drug synthesis. The reaction can also be used with a broad range of starting materials, giving drug developers much more flexibility in designing new compounds.  Though many groups are trying, the major challenge has been finding a suitable catalyst  to transfer the CF₃ entity from another source to the carbon ring. 

CF₃^- (trifluoromethyl negative ion) tends to be unstable when detached from other molecules, so the catalyst must act quickly to transfer the CF₃ group before it decomposes. The MIT team chose to use a catalyst built from palladium i.e., BrettPhos (see structure). MIT team is not the first to try palladium catalysis for this reaction, but the key to their success was the use of a ligand (a molecule that binds to the metal to stabilize it and hasten the reaction) called BrettPhos 2-(Dicyclohexylphosphino)-3,6-dimethoxy-2'-4'-6'-tri-i-propyl-1,1'-biphenyl,  which they had previously developed for other purposes. 

During the reaction, a CF₃ group is transferred from a silicon carrier to the palladium, displacing a chlorine atom. Subsequently, the aryl-CF₃ unit is released and the catalytic cycle begins anew. The researchers tried the synthesis with a variety of aryl compounds and achieved yields ranging from 70 to 94 percent of the trifluoromethylated products. 

Researchers conclude that, in its current state the process is too expensive for manufacturing use. For drug discovery, however, it may lower overall costs because it streamlines the entire synthesis process.

"For discovery chemistry, the price of the metal is much less important," says Kinzel....

Ref :  http://www.sciencemag.org/cgi/content/abstract/328/5986/1679

Blueberry consumption is beneficial for hepatic diseases....

We know that blueberry has many chemicals such as anthocyanins, proanthocyanidins, resveratrol, flavonols and tannins and how blueberry inhibit mechanisms of cancer cell development and inflammation in vitro. Similar to red grape, some blueberry species contain in their skins significant levels of resveratrol a phytochemical. 

Now research team led by Ming-Liang Cheng, MD, from Department of Infectious Diseases, Guiyang Medical College, Guiyang,  have found that blueberries could reduce liver indices, serum levels of hyaluronic acid and alanine aminotransferase, and increase levels of superoxide dismutase and decrease levels of malondialdehyde in liver homogenates compared with the model group.  Meanwhile, the stage of hepatic fibrosis was significantly weakened. Blueberries increased the activity of glutathione-S-transferase in liver homogenates and the expression of Nrf2 and Nqo1 compared with the normal group, but there was no significant difference compared with the model group. 

The authors suggest that blueberry consumption is beneficial for hepatic diseases (including fibrosis)....

I read an article in the same lines, where in the  researchers from Miyazaki prefecture of southern Japan and University of Miyazaki, screened nearly 300 different agricultural products for potential compounds that suppress HCV replication and uncovered a strong candidate in the leaves of rabbit-eye blueberry (native to the southeastern US). They purified the compound and identified it as proanthocyandin (a polyphenol similar to the beneficial chemicals found in grapes and wine). While proanthocyandin can be harmful, Kataoka and colleagues noted its effective concentration against HCV was 100 times less than the toxic threshold. The researchers are  hoping to explore the detailed mechanisms of how this chemical stops HCV replication....

Ref :  http://www.biologynews.net/archives/2009/08/07/the_hepatitis_healing_power_of_blueberry_leaves.html

Liquid Crystals - A New Way to Better Data Storage ?

In continuation of my update on liquid crystals (after a long gap)....

As cell phones and computers continue to shrink, many companies are seeking better ways to store hundreds of gigabytes of data in small, low-power devices. A special type of liquid crystal (similar to those used in computer displays and televisions) offers a solution  and lasers can encode data throughout a liquid crystal known as holographic storage, the technique makes it possible to pack much more information in a tiny space.   

But attempts to use liquid crystals for data storage have had limited success. In order to reliably record and rewrite data, researchers must figure out a way to uniformly control the orientation of liquid crystal molecules as the most liquid crystal technologies currently rely on physical or chemical manipulation, such as rubbing in one direction, to align molecules in a preferred direction. 

In an important advance, scientists at the Tokyo Institute of Technology have created a stable, rewritable memory device that exploits a liquid crystal property called the "anchoring transition". Researchers  demonstrated memory and rewritable bistable devices based on an anchoring transition of a nematic liquid crystal on a perfluoropolymer surface. Spontaneous orientation changes between planar and homeotropic occur on cooling and heating with a large temperature hysteresis. Orientation switching also occurs by applying an electric field with a response time of several milliseconds depending on the field strength claims the researchers.

Using either a laser beam or an electric field, the researchers can align rod-like liquid crystal molecules in a polymer. Their tests show that the liquid crystal created by the team can store data, be erased and used again...

"This is the first rewritable memory device utilizing anchoring transition," said Hideo Takezoe, who led the research. And because the device is bi-stable -- the liquid crystals retain their orientation in one of two directions -- it needs no power to keep images, adds Takezoe.

 Ref : http://jap.aip.org/japiau/v107/i12/p123108_s1?isAuthorized=no

Resveratrol in Red Wine Neutralizes Toxicity of Proteins Related to Alzheimer's

We know that, Resveratrol (found in the skin of red grapes and is a constituent of red wine, see structure)  (trans-resveratrol) is a phytoalexin produced naturally by several plants when under attack by pathogens such as bacteria or fungi.  And also it has been reported to possess diverse activities such as, anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects in mouse and rat models of testings. In the only positive human trial, extremely high doses (3–5 g) of resveratrol in a proprietary formulation have been necessary to significantly lower blood sugar.Claims of anti-aging effects of the same compounds is to be still established.

Now researchers led by Rensselaer Professor Peter M. Tessier, have come up with an interesting finding i.e., resveratrol - has the ability to neutralize the toxic effects of proteins linked to Alzheimer's disease. 

As per the claims by the researchers, resveratrol picks out the clumps of peptides that are bad and leaves alone the ones that are benign, it helps us to think about the structural differences between the peptide isoforms (different packing arrangements of a particular peptide) Deformations of a particular peptide  the Aβ1-42 peptide,   have been linked to Alzheimer's disease. 

Improperly folded peptides have been shown to collect in accumulations called "plaques (often found near areas of cell death in diseased brain)" within the brain.

Researchers conclude that, though it is not clear that resveratrol is able to cross the blood-brain barrier. However, the molecule has garnered interest in recent years for its potential impact on cancer and aging...

Ref : http://www.jbc.org/content/early/2010/05/28/jbc.M110.133108....

New use of old drugs (Metformin & AICAR ) in treating hepatitis C...

In continuation of my update on Metformin...

Researchers from  University of Leeds have found drugs such as antidiabetic  drug  Metformin  (right  structure)  and                AICAR, (5-Amino-4-imidazole carboxamide ribonucleotide) below right structure) used to combat obesity, can prevent the hepatitis C virus from replicating in the body.

Drugs such as Metformin and AICAR work by stimulating an enzyme called AMP kinase (AMPK) which regulates energy within our cells,  the very enzyme that hepatitis C virus represses to enable it to replicate. As per the claim by the researchers, the hepatitis C virus switches off AMPK so that the cell continues production of lipids and membranes, both of which are vital to its survival. 

AMPK's usual function is to conserve the energy balance in cells (it does by temporarily shutting down the production of lipids (fats) and membranes) when it senses an increase in energy requirements. Researchers  claim that, when a cell becomes infected by a virus,  AMPK gets activated and  shuts down certain functions of the cell temporarily until the cell's energy is rebalanced. 

Building on this finding, the research team were able to examine how cells would react when treated with common drugs that stimulate AMPK. They found that in infected cells, the drugs were able to halt virus replication, enabling cells to clear the infection...

"We're very excited about these findings," says Professor Mark Harris from the University's Faculty of Biological Sciences. "These drugs are already on the market, and whilst substantial clinical trials still need to take place before they can be used to treat hepatitis C infection, we think it could be an enormous step forward in the battle against the virus."  ....

Ref : http://www.leeds.ac.uk/news/article/825/new_use_for_old_drugs_in_treating_hepatitis_c?research

Crizotinib Shows Dramatic Results for Shrinking Tumors (lung cancer)....

Patients with a specific kind of lung cancer may benefit from a Phase III clinical trial offered by the Moores UCSD Cancer Center. The new drug, crizotinib (structure), under development by Pfizer, showed dramatic results in reducing lung cancer tumors in some patients during Phase I and II clinical trials.

"The results of the first two trials have been very encouraging," said Lyudmila Bazhenova, MD, assistant clinical professor at UC San Diego School of Medicine and a member of the Moores UCSD Cancer Center...

According to a preliminary study,  57% of patients had their tumors reduced and at eight weeks of the treatment, 87% showed disease stabilization.

The Phase III clinical trial will compare crizotinib with standard-of-care chemotherapy in the treatment of ALK-positive recurrent NSCLC. Through a randomized selection process, patients will either be treated with chemotherapy or crizotinib. If the patients who are given the chemotherapy do not respond to treatment, they will be given crizotinib at the end of the trial....

Ref : http://ucsdnews.ucsd.edu/newsrel/health/06-22ShrinkingTumors.asp

FDA approves Jevtana to treat men with prostate cancer

In continuation of my update on Cabazitaxel......

FDA approves Jevtana to treat men with prostate cancer

Synergistic activity of Sorafenib and Sulforaphane abolishes pancreatic cancer...

In continuation of my update on "Sorafenib", I find this info interesting to share with...

A team led by Professor Dr. Ingrid Herr, Head of the Department of Molecular Oncosurgery, a group of the Department of Surgery at Heidelberg University Hospital, have come up with an interesting finding, i.e.,  Sorafenib  (used for advanced liver and kidney cancer) also appears to be effective against cancer stem cells in pancreatic cancer. It inhibits resistant tumor stem cells and is also especially effective in combination with sulforaphane, an organic compound found in broccoli. 

In their tests on cancer cells and mice, the researchers showed that sorafenib inhibited typical properties of cancer stem cells from pancreas tumors and greatly reduced tumor growth. However, this effect lasted only for a short time and after four weeks, new colonies of cancer stem cells formed that no longer reacted to further treatment with sorafenib. The resistance is probably related to a certain metabolic pathway, the NF-kB pathway, that is activated by sorafenib, claims the researchers. 

Naturally occurring substance(s) e.g., sulforaphane (vegetables from the cruciferous family such as broccoli and cauliflower possess a high content of sulforaphane, an anti-cancer compound)  that block precisely this undesired NF-KB pathway and thus make the dangerous cells vulnerable.  The experiments show that sulforaphane prevents the activation of the NF-kB pathway by sorafenib and hence the combination treatment reinforces the effect of sorafenib without causing additional side effects. Researchers conclude that the invasive potential of cancer cells was prevented  and  metastasis was completely blocked in cell culture experiments. 

"We assume that nutrition may be a suited approach to break therapy resistance of cancer stem cells and thus make tumor treatment more effective," Professor Herr suggested....

Ref : http://cancerres.aacrjournals.org/content/70/12/5004

New evidence that chili pepper ingredient fights fat

In continuation of effect of chilli pepper on obesity.......

New evidence that chili pepper ingredient fights fat

New world Helicobacter pylori genome sequenced, dynamics of inflammation-related genes revealed

In continuation of my update on Helicobacter pylori.......
New world Helicobacter pylori genome sequenced, dynamics of inflammation-related genes revealed

Sulindac inhibits tumor growth !...

We know that, Sulindac(structure), is useful in the treatment of acute or  chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in the body to the active NSAID. More specifically, the agent is converted by liver enzymes to a sulfide that is excreted in the bile and then reabsorbed from the intestine. This is thought to help maintain constant blood levels with reduced gastrointestinal side effects. Some studies have shown sulindac to be relatively less irritating to the stomach than other NSAID's except for drugs of the COX-2 inhibitor class. The exact mechanism of its NSAID properties is unknown, but it is thought to act on enzymes COX-1 and COX-2, inhibiting prostaglandin synthesis.

Now researchers from Sanford-Burnham Medical Research Institute (Sanford-Burnham) and their colleagues have figured out how  Sulindac, inhibits tumor growth. The study reveals that Sulindac shuts down cancer cell growth and initiates cell death by binding to nuclear receptor RXRα, a protein that receives a signal and carries it into the nucleus to turn genes on or off. 

As per the claim by the researchers, RXRα normally suppresses tumors, but many types of cancer cells produce a truncated form of this nuclear receptor that does just the opposite. This study showed that shortened RXRα enhances tumor growth by stimulating other proteins that help cancer cells survive. Luckily, the researchers also found that Sulindac can be used to combat this deviant RXRα by switching off its pro-survival function and turning on apoptosis, a process that tells cells to self-destruct.  The interesting part of their research lies in the fact that, they were able to overcome the limitation (cardiovascular side effects associated with Sulindac and other NSAIDs), the researchers tweaked Sulindac, creating a new version of the drug now called K-80003 that both decreases negative consequences and increases binding to truncated RXRα..

"Depending on the conditions, the same protein, such as RXRα, can either kill cancer cells or promote their growth," Dr. Zhang said. "The addition of K-80003 shifts that balance by blocking survival pathways and sensitizing cancer cells to triggers of apoptosis."

Ref :  http://www.cell.com/cancer-cell/retrieve/pii/S1535610810001595

The Revolutionary alkaline diet

I am really happy to share an interesting and important article on Alkaline Diet, by Emma Deangela, who has written exclusively for the readers/followers of my blog. I thank Emma for this info, on behalf of  all my blog readers. Its good to see many  authors /writers coming forward to share the knowledge through the social media like facebook/blog/twitter and hope this awareness will help those needy people....

Boost Your Healthy Simply by Alkalizing your Diet!

You've probably heard of alkalizing your body by now and how it will boost your health. But in order to fully appreciate how an alkaline body helps in our daily living, it is imperative to know the components of an alkaline diet and the importance of maintaining the pH of our body.

pH refers to the measure of acidity or basicity of a solution. More accurately, it pertains to the extent of dissociation of hydrogen ions of our body. If we consume the right types and amounts of nutrients and minerals conducive to our body's development, our body is able to maintain the right pH balance. But you may wonder for a moment what exactly are the 'right' nutrients and minerals? This is where alkaline diet comes into the picture.

The concept of alkaline diet is ultimately about foods that leaves an alkaline residue in our body after digestion. Our body's pH balance fluctuates with each intake of food, and in order to maintain it at the optimum pH, our body must have enough alkaline reserves which can only be obtained if we include at the minimum 80% of alkaline foods in our diet.

How do we classify foods into acidic or alkaline foods?

Chlorine, phosphorus and sulfur in food will probably give acidic residue after the food has been digested. Conversely, minerals such as calcium, sodium, magnesium and potassium found in food will leave an alkaline residue.

We should always bear in mind that all foods leave residue in our body after digestion. If you recall the food pyramid taught in Health education classes, meat and seafood, dairy products, alcoholic drinks, chemical sweeteners, sweets and chocolates, and even grains forms acidic residue! However, green leafy vegetables and fruits low in sugar contain organic aids and are full of alkaline goodness after digestion. So do remember to include a larger proportion of greens and fruits in your diet to maintain an alkaline pH in your body.

Why is it Important to Alkalize the Body?

People living in the modern society are plagued with many diseases and the growing number of sufferers far outstripped our ancestors? Why is such a scenario happening? It can be attributed to our diet which is heavily acidic. Foods that leaves a high content of acidic residues revolves in our circulatory system and are not rid of by our kidneys, lungs and bowels.

According to Dr Theodore Baroody, author of the critically acclaimed book "Alkalize or Diet", the reason for these diseases was due to excessive acidic residue in our body. Acidic mediums are conducive for the breeding of diet-related diseases, which will lead to death. When our body is deprived of the essential alkaline reserves, nutrients and minerals, excessive acids in our bloodstream may lead to slow poisoning of our body due to our diet which comprises of a high percentage of acidic foods. Excess acids will also weaken and in severe cases, damage our bodily functions and cellular actives such as respiration, digestion, hormone production and blood circulation.

Start with an Alkaline Diet Today!

If you are guilty of consuming acid-rich food, fret not. You can definitely reverse the situation through alkalizing your body today. We will be able to enjoy a new lease of energy if we maintain the pH balance in our body. On top of that, another benefit of the alkaline diet is to remove the acidic environment that serves as the breeding ground of acidic toxins which will over time result in an onslaught of diseases. Nutritionists and medical doctors recommends a daily consumption of at least five servings of vegetables and green foods which are highly alkaline.

Affluence and technology have resulted in an epidemic of diet-related diseases. However, there is no need to remain pessimistic. Instead of blindness pursuit of wealth and fame, which will come to naught without good health, why not change your health for the better starting today? We should all grab this opportunity and start incorporating the alkaline diet into our everyday life. It may be difficult to give up your favorite acidic foods at the start, but be assured that your efforts will pay off when you see your overall health being restored. Instead of consuming supplements and medicine, start with the root of the problem - diet. And the solution is to begin alkalizing your body by providing an alkaline environment for every cells and bodily functions in your body to thrive.

About the Author –Emma Deangela is one of the key authors for Alkaline Diet.  She loves to share her experience with her readers on tips to stay healthy, disease free, and how to lose weight the alkaline way. Her alkaline diet newsletter is available at Alkaline Diet, so if you would like to find out more about juicy alkaline diet tips and recipes do visit her blog.....

Two-drug phase I trial shows promise in treating late-stage ovarian cancer

In continuation of my update on carboplatin .....

Researchers from Indiana University School of Medicine, have come up  with interesting finding from a two-Drug Phase I Trial Show, i.e.,  the combination of decitabine (see structure) and carboplatin appears to improve the outcome of women who have late-stage ovarian cancer. Researchers report four of 10 patients who participated in a phase I clinical trial had no disease progression after six months of treatment. One patient experienced complete resolution of tumor tissue for a period of time.

"Carboplatin is the most efficient drug therapy for ovarian cancer,"  unfortunately, patients with recurrent disease become resistant to the drug after one or two rounds claims the lead researcher.."

Decitabine was first used to treat the study patients intravenously daily for five days followed on the eighth day with carboplatin. After a month, the regimen begins again.

Encouraged by the results of the phase I trial, which determined the safety of two different dosing regimens, a phase II trial is now under way with 17 patients already enrolled. Phase II trials are primarily focused on assessing the effectiveness of a drug or treatment protocol.

As per the claim by the researcher, decitabine  (a known methylation inhibitor) can help return tumor suppression genes to an active state, and also improve cells' susceptibility to anti-cancer drugs like carboplatin. Researchers adds that decitabine isn't just targeting active ovarian cancer cells, but also cancer stem cells that seem to survive the first treatments. 

Researchers conclude that, by keeping tumor suppression genes from being methylated, carboplatin and other platinum-based treatments for ovarian cancer have a better chance of success in the late stages.

Ref : http://www3.interscience.wiley.com/journal/123500856/abstract?CRETRY=1&SRETRY=0

Eribulin mesylate drug may help extend lives of women with advanced breast cancer..

We know that, Eribulin (see structure E7389) is an investigational  anticancer drug. Eribulin was previously known as E7389.  Eribulin is currently being investigated by Eisai Co. for the third-line treatment of advanced breast cancer in patients who have been previously treated with anthracyclines, taxanes and capecitabine, as well as a variety of other solid tumors, including non-small cell lung cancer, prostate cancer and sarcoma.

Structurally, eribulin is a fully synthetic macrocyclic ketone analogue of the marine sponge natural product halichondrin B a potent mitotic inhibitor with a unique mechanism of action found in the Halichondria genus of sponges. Eribulin is a mechanistically-unique inhibitor of microtubule dynamics, exerting its anticancer effects by triggering apoptosis of cancer cells following prolonged mitotic blockage. A new synthetic route to E7389 was published in 2009.

Now   research team at the University of Leeds and St James's Institute of Oncology led an international trial of the new chemotherapy drug, eribulin mesylate. As per the claim by the researchers, average survival was typically 25 per cent longer for women who took eribulin mesylate.

In the EMBRACE trial, 762 patients with advanced breast cancer received either eribulin or standard cancer treatment. All of the patients had already been heavily treated with conventional therapies, but their disease had returned or spread to other parts of the body.  Researchers concluded that those who took the new drug lived for 13.1 months, on average, compared with 10.7 months for those on conventional chemotherapy. The drug was also well-tolerated by most patients. Researchers hope that these results may establish eribulin as a new, effective treatment for women with late-stage metastatic breast cancer (either single drug or in combination with other anticancer drug). The drug is not yet available for routine clinical treatment and is awaiting regulatory approval in the European Union, the US and Japan.

"Until now, there hasn't really been a standard treatment for women with such advanced breast cancer. For those women who have already received all of the recognised treatments, these are promising results, claims the lead investigator Professor Christopher Twelves...

Ref : http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=74&abstractID=50309

Polyphenols in red wine and green tea halt prostate cancer growth, study suggests

In continuation of my update on Green Tea and EGCG........

"The profound impact that the antioxidants in red wine and green tea have on our bodies is more than anyone would have dreamt just 25 years ago," Weissmann added. "As long as they are taken in moderation, all signs show that red wine and green tea may be ranked among the most potent 'health foods' we know." ....

Polyphenols in red wine and green tea halt prostate cancer growth, study suggests

New evidence that drinking coffee may reduce the risk of diabetes

In continuation of my update on benefits of coffee....

New evidence that drinking coffee may reduce the risk of diabetes

Carbamazepine Reduces Hepatic Fibrosis.....

We know that Carbamazepine (CBZ see structure), is an  anticonvulsant and mood stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia. It is also used off-label for a variety of indications, including attention-deficit hyperactivity disorder (ADHD), schizophrenia, phantom limb syndrome, paroxysmal extreme pain disorder, and post-traumatic stress disorder.

Now researchers from University of Pittsburgh School of Medicine, have come up with interesting finding about this drug, i.e., the liver scarring of α1-antitrypsin (AT) deficiency, the most common genetic cause for which children undergo liver transplantation, might be reversed or prevented with carbamazepine.  The disease, which affects 1 in 3,000 live births, a gene mutation leads to an abnormal protein, dubbed ATZ, that unlike its normal counterpart is prone to aggregation. As per the claim by the researchers these aggregates of ATZ accumulate in the liver cells and eventually lead to scarring, or fibrosis, of the organ and set the stage for tumor development. The disease sometimes doesn't show itself until adulthood, when the liver starts to fail due to cirrhosis or cancer.

Encouraged by the fact that carbamazepine could enhance a natural cellular pathway called autophagy  or self-digestion, researchers thought that  it might be able to rid the cells of the toxic aggregated ATZ. For the study researchers treated an ATZ cell line with carbamazepine. They found that carbamazepine did indeed cause a marked decrease in ATZ because the abnormal proteins were degraded more quickly via autophagy, and so they did another experiment in a mouse model of AT deficiency.

The most amazing finding,  as per the claim by the researchers is  that the drug reversed the fibrosis in the livers of the mice and after two weeks of treatment the liver tissue resembled that of a healthy mouse...

The ability of carbamazepine and drugs like it to "soup up" the cell's autophagy machinery might have value in other disorders ― such as Alzheimer's disease, Huntington's disease and Parkinsonism ― that are thought to be caused by toxic effects of protein clumping in the brain. Dr. Perlmutter and his colleagues are now exploring these possibilities in preclinical studies. ....

Ref : http://www.sciencemag.org/cgi/content/abstract/science.1190354v1

Azithromycin as effective as penicillin for early-stage syphilis...

We know that azithromycin (structure) is one of the world's best-selling  antibiotics. It is derived from erythromycin; however, it differs chemically from erythromycin in that a methyl-substituted nitrogen atom is incorporated into the lactone ring, thus making the lactone ring 15-membered.  Azithromycin is being used to treat or prevent certain bacterial infections, most often those causing middle ear infections, tonsillitis, throat infections, laryngitis, bronchitis, pneumonia, Typhoid, certain urinary tract infections and venereal diseases, such as non-gonococcal urethritis, chlamydia, gonorrhea and cervicitis. and sinusitis. In recent years it has primarily been used to prevent bacterial infections in infants and those with weaker immune systems.

Now researchers lead by Dr. Edward W. Hook, III of University of Alabama at Birmingham have come up with an interesting finding, i.e., antibiotic pills (azithromycin) are as effective as penicillin injections in curing early-stage syphilis in HIV-negative volunteers. 

Although long-acting penicillin delivered by injection is recommended as the preferred treatment for early syphilis, the authors note that this therapy has shortcomings, particularly in resource-limited settings. Penicillin injections can cause allergic reactions, and the drug must be refrigerated and administrated by trained personnel. The orally administered azithromycin may provide a good alternative for treating HIV-negative people with early-stage syphilis, the scientists conclude. They note that there is a potential for syphilis-causing bacteria to acquire resistance to macrolide drugs such as azithromycin and they recommend continued research into this possibility..

Ref : http://www.niaid.nih.gov/news/newsreleases/2010/Pages/syphilis.aspx

Telomeres: Size matters when it comes to DNA

In continuation of my update on Telomerase and Telomerase inhibition....

Telomeres: Size matters when it comes to DNA

Lovastatin: A New Weapon Against Plague?

We know that, Lovastatin is a member of the drug class of statins,  used for lowering  cholesterol (hypolipidemic agent) in those with hypercholesterolemia and so preventing cardiovascular disease. Lovastatin is a naturally occurring drug found in food such as oyster mushrooms  and red yeast rice.

Now scientists at the Unité de Recherche sur les Maladies Infectieuses et Tropicales Emergentes (CNRS/Université Aix-Marseille 2), have found that Lovastatin protects animals against the deadly effects of plague.

After inoculating small rodents with the Yersinia pestis bacterium, the team led by Didier Raoult and Michel Drancourt at the URMITE (CNRS/Université Aix-Marseille 2) showed that animals treated with lovastatin presented fewer and less severe infections. Lovastatin therefore has preventive properties against plague mortality in an animal model. This experimental study also reveals that this statin has no direct antibiotic effect against Yersinia pestis but that it prevents the development of septicemia.  

Researchers conclude that Lovastatin had no in-vitro antibiotic effect against Y. pestis. The difference in the mortality between control mice (11/15; 73.5%) and lovastatin-treated mice (3/15; 20%) was significant (P<0.004; Mantel-Haenszel test). Dead mice exhibited Y. pestis septicemia and inflammatory destruction of lung and spleen tissues not seen in lovastatin-treated surviving mice. These data suggest that lovastatin may help prevent the deadly effects of plague, with a caution that field observations are warranted to assess the role of lovastatin in the prophylaxis of human plague....

Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0010928

FDA accepts Orexigen's Contrave NDA for treatment of obesity

Orexigen Therapeutics, Inc., a biopharmaceutical company focused on the treatment of obesity, recently anounced that the U.S. Food and Drug Administration (FDA) has accepted for filing the Company's New Drug Application (NDA) for Contrave(R) (see structrures below ; naltrexone SR   and bupropion SR), its investigational drug for the treatment of obesity. The NDA is based on a substantial body of evidence gathered through the Contrave Obesity Research (COR) clinical program, which included over 4,500 patients.....

"We are pleased the FDA has accepted our NDA for filing and look forward to working with the Agency during the review process," said Michael Narachi, President and CEO of Orexigen. "If approved, we believe Contrave will become an important therapeutic option for obese patients, making weight loss and weight maintenance an achievable cornerstone in the treatment of obesity and its common co-morbidities."

Ref : http://ir.orexigen.com/phoenix.zhtml?c=207034&p=irol-newsArticle&ID=1432740&highlight=