Friday, February 25, 2011

Thursday, February 24, 2011

2-Aminothiazoles as Therapeutic Leads for Prion Diseases............

Adam Renslo, Stanley B. Prusiner (Nobel Laureate) and colleagues,  explain that prion diseases include conditions like mad cow disease in animals and Creutzfeldt-Jakob Disease in humans, result from deposits of abnormal prion protein in brain tissue. Prion diseases are invariably fatal and no treatments are yet available.  Scientists who examined more than 10,000 chemical compounds during the last year in search of potential new drugs for a group of untreatable brain diseases, are reporting that one substance (a 2-Aminothiazole see structure) shows unusual promise. The early positive signs for so-called prion diseases come from research in laboratory mice and cell cultures.

As per the claim by the researchers,  the new compound can reach the brain and reach high concentrations when taken orally and do not appear toxic. Researchers also claims that, tests on prion-infected mouse brain cells showed that the compounds reduced the amount of the abnormal prion protein. The compounds appear to be among the most promising potential treatments for prion diseases yet discovered, the report suggests…..

Ref : 2-Aminothiazoles as Therapeutic Leads for Prion Diseases…

Wednesday, February 23, 2011

Allegra Approved for Over-the-Counter Sale

Sanofi-Aventis' prescription non-drowsy antihistamine, Allegra (fexofenadine), has been approved by the U.S. Food and Drug Administration for over-the-counter sale. The drug will be available in its original prescription strengths starting in March for people two years and older, according to a news release from Sanofi and its U.S. consumer division, Chattem Inc. A version that combines Allegra with a decongestant, Allegra-D, will be available at the same time for people 12 and older without a prescription at the pharmacy counter, the companies said. 

Monday, February 14, 2011

Small Molecule c-jun-N-Terminal Kinase Inhibitors Blocks Brain Cell Destruction in Parkinson's Disease - a new hope !

Scientists from the Florida campus of The Scripps Research Institute have produced the first known compound to show significant effectiveness in protecting brain cells directly affected by Parkinson's disease, a progressive and fatal neurodegenerative disorder.  Although the findings were in animal models of the disease, the effectiveness of the compound, combined with its potential to be taken orally, offers the tantalizing possibility of a potentially useful future therapy for Parkinson's disease patients.  As per the claim by the lead researcher, Prof. Philip LoGrasso,   the compelling data on the first oral, brain-penetrating inhibitor to show significant efficacy in preventing neurodegeneration in both mouse and rat models of Parkinson's disease.
The new small molecule labeled SR-3306  is aimed at inhibiting a class of enzymes called c-jun-N-terminal kinases (JNK). Pronounced "junk," these enzymes have been shown to play an important role in neuron (nerve cell) survival. As such, they have become a highly viable target for drugs to treat neurodegenerative disorders such as Parkinson's disease.
The SR-3306 compound, which has been in development at Scripps Florida for several years, performed well in both cell culture and animal models. In cell culture, the compound showed greater than 90 percent protection against induced cell death of primary dopaminergic neurons, while in mouse models of induced neuron death, the compound showed protective levels of approximately 72 percent.
 "It was a surprise that level of neuroprotection reduced the behavioral impact so strongly," LoGrasso said, "but it's indicative of how it might perform in human patients. While SR-3306 doesn't represent a cure, it does appear to have the potential of stopping the progression of the disease."….

Monday, February 7, 2011

Tautomycetin Antibiotic Offers Potential for Anti-Cancer Activity.....

Tautomycetin-antibiotic((1R*,2S*)-16-Ethyl-3,7-dihydroxy-1, 2,6,10,12-pentamethyl-5,14-dioxo- 15,17-octadecadienyl 2,5-dihydro-β-hydroxy-4-methyl-2,5-dioxo-3-furanpro panoic acid estersee structure) known for its immunosuppressive functions could also point the way to the development of new anti-cancer agents, researchers at the Indiana University School of Medicine have reported. 

Study determined that the compound, tautomycetin, targets an enzyme called SHP2, which plays an important role in cell activities such as proliferation and differentiation. Interestingly, SHP2 mutations are also known to cause several types of leukemia and solid tumors.

The finding is encouraging because SHP2 is a member of a large family of enzymes called protein tyrosine phosphotases (PTPs), which are important in the signaling processes that control all essential cellular functions. Dysregulation of PTP activity has been linked to several human diseases, including cancer, diabetes, and immune dysfunctions. But their makeup has made it difficult to find potential drugs to act on them.

Authors conclude that,  the  research will serve as a foundation for the development of therapeutic agents for a large family of protein tyrosine phosphotase targets…..

Sijiu Liu, Zhihong Yu,

Thursday, February 3, 2011

Maillard reaction is the principle contributor to the antioxidant capacity of coffee brews ......

Food scientists at the University of British Columbia have been able to pinpoint more of the complex chemistry behind coffee's much touted antioxidant benefits, tracing valuable compounds to the roasting process.  Yazheng Liu and Prof. David Kitts found that the prevailing antioxidants present in dark roasted coffee brew extracts result from the green beans being browned under high temperatures.

Liu and Kitts analyzed the complex mixture of chemical compounds produced during the bean's browning process, called the "Maillard reaction (a chemical reaction between an amino acid and a reducing sugar, usually requiring heat). The term refers to the work by French chemist Louis-Camille Maillard who in the 1900s looked at how heat affects the carbohydrates, sugars and proteins in food, such as when grilling steaks or toasting bread. Previous studies suggested that antioxidants in coffee could be traced to caffeine or the chlorogenic acid (see structures above and below respectively)  found in green coffee beans, but the present results clearly show that the Maillard reaction is the main source of antioxidants claims the researchers.  Researchers conclude that that coffee beans lose 90 per cent of their chlorogenic acid during the roasting process, LFS food science professor and director of the Food, Nutrition and Health program.

Ref : Yazheng Liu and David D. Kitt, Food Research International.

Monday, January 31, 2011

Taxol reduces cell regeneration obstacles after spinal cord injury...

Scientists of the Max Planck Institute of Neurobiology in Martinsried and their colleagues from the Kennedy Krieger Institute and University of Miami in the United States, and the University of Utrecht in the Netherlands, have now shown that the cancer drug Taxol (see structure)  reduces both regeneration obstacles. Frank Bradke and his team at the Max Planck Institute of Neurobiology in Martinsried study the mechanisms inside CNS nerve cells responsible for stopping their growth. As per the claim by the researchers,  protein tubes (micro tubules) have a parallel arrangement in the tip of growing nerve cells, stabilizing cells and actively pushing the cell end forward. This arrangement is lost in injured CNS cells. So how can the order of the microtubule be kept or regained in these cells? And once the cells start growing, how can they overcome the barrier of the scar tissue? Together with their colleagues from the United States and the Netherlands, the Max Planck scientists have now found a common solution for both problems. Taxol, the trade name of a drug currently used for cancer treatment, has now been shown to promote regeneration of injured CNS-nerve cells.

Researchers claim that,  Taxol promotes regeneration of injured CNS-nerve cells in two ways: Taxol stabilizes the microtubules so that their order is maintained and the injured nerve cells regain their ability to grow. In addition, Taxol prevents the production of an inhibitory substance in the scar tissue. The scar tissue, though reduced by Taxol, will still develop at the site of injury and can thus carry out its protective function. Yet growing nerve cells are now better able to cross this barrier. 
"This is literally a small breakthrough", says Bradke.
Experiments in rats performed by this group verified the effects of Taxol. These researchers supplied the injury site after a partial spinal cord lesion with Taxol via a miniature pump. After just a few weeks, animals showed a significant improvement in their movements. So far researchers  tested the effects of Taxol immediately after a lesion.  Researchers next plan  is to investigate whether Taxol is as effective when applied onto an existing scar several months after the injury.  As the research is still in the state of basic research and a variety of obstacles remain  and eventually, pre-clinical trials will need to be done,  "however,  researchers believe that this is a very promising path........

Sunday, January 30, 2011

Protective properties of green tea uncovered

In continuation of my up date on the benefits of green tea...

Protective properties of green tea uncovered

Iniparib Phase III study in metastatic triple-negative breast cancer does not meet primary goal

A randomized Phase III trial evaluating iniparib (BSI-201) in patients with metastatic triple-negative breast cancer (mTNBC) did not meet the pre-specified criteria for significance for co-primary endpoints of overall survival and progression-free survival......

Iniparib Phase III study in metastatic triple-negative breast cancer does not meet primary goal

Friday, January 28, 2011

Discovery of a Biochemical Basis for Broccoli's Cancer-Fighting Ability

Fung-Lung Chung and colleagues showed in previous experiments that substances called isothiocyanates (or ITCs)  found in broccoli, cauliflower, watercress, and other cruciferous vegetables appear to stop the growth of cancer. But nobody knew exactly how these substances work, a key to developing improved strategies for fighting cancer in humans. The tumor suppressor gene p53 appears to play a key role in keeping cells healthy and preventing them from starting the abnormal growth that is a hallmark of cancer. When mutated, p53 does not offer that protection, and those mutations occur in half of all human cancers. ITCs might work by targeting this gene, the report suggests.

Scientists studied the effects of certain naturally-occurring ITCs on a variety of cancer cells, including lung, breast and colon cancer, with and without the defective tumor suppressor gene. They found that ITCs are capable of removing the defective p53 protein but apparently leave the normal one alone. Drugs based on natural or custom-engineered ITCs could improve the effectiveness of current cancer treatments or lead to new strategies for treating and preventing cancer.

Wednesday, January 26, 2011

Small Molecules (Isoxazole derivatives) May Prevent Ebola Infection

A new study by University of Illinois at Chicago scientists has uncovered a family of small molecules (isoxazole derivatives), which appear to bind to the virus's outer protein coat and may inhibit its entry into human cells.
The new findings demonstrate that it is possible for a small molecule to bind to the virus before it has a chance to enter the cell and thereby prevent infection. Wardrop collaborated with UIC virologist Lijun Rong, who created a screening system that uses a chimeric HIV-Ebola virus bearing the protein coat of the Ebola virus. The chimera looks like Ebola but isn't life-threatening for scientists to work with.
After screening more than 230 candidate compounds, Wardrop and Rong found two molecules that inhibited cell entry, but only one that demonstrated specificity for the Ebola virus plus a bonus.

We found that our lead compound also inhibits Marburg," Wardrop said, referring to a related virus that, along with Ebola, is one of the deadliest pathogens known. "That was a nice surprise. There's growing evidence the two viruses have the same cell-entry mechanism, and our observations appear to point to this conclusion."
In an effort to find even more potent anti-Ebola agents, Wardrop and Maria Yermolina synthesized a series of derivatives of the lead molecule called isoxazoles. Researchers found that the compounds, displayed increased activity against Ebola infection. Though the mechanism of action of these class of compounds is still to be established, in my opinion its an achievement. More interestingly, the mode of study is being studied by nuclear magnetic resonance spectroscopy, done by Michael Caffrey, associate professor of biochemistry and molecular genetics. While it's too early to predict whether the findings will lead to a new treatment for Ebola or Marburg infections, the positive results so far raise the hope....

Tuesday, January 25, 2011

FDA Panel Backs Amyvid (Florbetapir) Approval

FDA approve a new chemical, Florbetapir, E)-4-(2-(6-(2-(2-(2-([18F]-fluoroethoxy)ethoxy)ethoxy)- pyridin-3-yl)vinyl)-N-methyl benzenamine (see structure) that can highlight the telltale signs of Alzheimer's in brain scans may one day help doctors diagnose the neurodegenerative disease, experts said. Amyvid (trade name), with one critical caveat, however manufacturer Eli Lilly and Co. must demonstrate that standards for interpreting brain scans that show amyloid plaques illuminated by Amyvid can be made consistent enough to routinely guarantee an accurate diagnosis.

Amyvid (florbetapir) is injected into patients who then undergo a PET scan; a negative result can help rule out Alzheimer's, according to Lilly. Experts agreed that the test could become a critical part of spotting Alzheimer's before symptoms have taken hold, but they noted that the clinical reality of that is far from imminent.
    "It may well be that amyloid imaging will join colonoscopy, mammography, etc. as mid-life surveillance tests, and that anti-amyloid interventions are most effective in the pre-symptomatic stages of Alzheimer's disease," said Dr. Sam Gandy, the Mount Sinai Chair in Alzheimer's Disease Research in New York City. However, this possibility is years away, he added..............

Friday, January 21, 2011

Monday, January 17, 2011

Bioactive Compounds (anthocyanins) in Berries Can Reduce High Blood Pressure

We have already seen the benefits of anthocyanins, and also how useful the blue berries are. Now the researchers from University of East Anglia (UEA) and Harvard University, have further substantiated the usefulness of blue berries. As per the claim by the researchers eating blueberries can guard against high blood pressure.

The new findings show that bioactive compounds in blueberries called anthocyanins offer protection against hypertension. Compared with those who do not eat blueberries, those eating at least one serving a week reduce their risk of developing the condition by 10 per cent.

Anthocyanins (see structure) belong to the bioactive family of compounds called flavonoids and are found in high amounts in blackcurrants, raspberries, aubergines, blood orange juice and blueberries. Other flavonoids are found in many fruits, vegetables, grains and herbs. The flavonoids present in tea, fruit juice, red wine and dark chocolate are already known to reduce the risk of cardiovascular disease.

During the study, 35,000 participants developed hypertension. Dietary information identified tea as the main contributor of flavonoids, with apples, orange juice, blueberries, red wine, and strawberries also providing important amounts. When the researchers looked at the relation between individual subclasses of flavonoids and hypertension, they found that participants consuming the highest amounts of anthocyanins (found mainly in blueberries and strawberries in this US-based population) were eight per cent less likely to be diagnosed with hypertension than those consuming the lowest amounts. The effect was even stronger in participants under 60.

The effect was stronger for blueberry rather than strawberry consumption. Compared to people who ate no blueberries, those eating at least one serving of blueberries per week were 10 per cent less likely to become hypertensive.

"Our findings are exciting and suggest that an achievable dietary intake of anthocyanins may contribute to the prevention of hypertension," said lead author Prof Aedin Cassidy of the Department of Nutrition at UEA's Medical School".......