Saturday, April 30, 2011

Friday, April 29, 2011

Melatonin can help fight obesity and risks associated with it

Melatonin can help fight obesity and risks associated with it

Wednesday, April 20, 2011

Scientists Exploit Ash Tree Pest's Chemical Communication....

A newly identified chemical sex attractant, or pheromone, of the emerald ash borer could mean improved traps for monitoring and controlling the tree-killing beetle. That's the goal of U.S. Department of Agriculture (USDA) entomologist Allard Cossé and his colleagues. 


More recently, the team discovered a macrocyclic lactone (3z-dodecan-12-olide -see structure), a compound that female borers release while feeding. Large-scale field tests conducted in Canada and the United States showed that the compound attracts male borers and has potential for use in traps either alone or combined with ash-tree-based attractants, reports Cossé, at the ARS National Center for Agricultural Utilization Research in Peoria, Ill........


Details in a book 

Monday, April 18, 2011

New substance (Benzothiazin derivative) to tackle drug resistant tuberculosis...

Project NM4TB which gathers 18 research teams from 13 countries, discovered a novel class of substances, called benzothiazinones (BTZ-see structure), that could be used in the treatment of tuberculosis and drug resistant tuberculosis.

Prof Stewart Cole, Dr Vadim Makarov, Dr Ute Möllmann, Prof Giovanna Riccardi, and their colleagues have identified a novel class of compounds called benzothiazinones (BTZ) that act by preventing the TB bacterium from constructing its cell wall. In particular, one member of the class, BTZ043 was extremely potent, killing the TB agent, both in test tube experiments and in mouse models of the disease. BTZ043 is as effective as the two main drugs (Isoniazid and Rifampicin) in reducing the bacterial levels in the lungs and spleens of infected mice. The target of the new class of compounds is a component of Mycobacterium’s cell-wall-building machinery that has never before been used as a drug target. The most advanced compound of this new class, BTZ043, is a candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB. 

These substances act by preventing the bacteria that cause tuberculosis from constructing their cell wall. This discovery represents an important breakthrough in the battle against tuberculosis as the most advanced compound of this new class, BTZ043, is also effective against extensively drug resistant tuberculosis (XDR-TB).

More... : 

Tuesday, April 12, 2011

Friday, April 1, 2011

Researchers identify drug candidate that can treat prostate cancer

Drug candidate, developed from a naturally occurring anti-cancer agent found in cruciferous vegetables such as cabbages and broccoli, for prostate cancer...
Researchers identify drug candidate that can treat prostate cancer

Boceprevir drug can help cure hard-to-treat hepatitis C

Thursday, March 31, 2011

Wednesday, March 30, 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 et.al.,

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".......


Wednesday, January 12, 2011

Monday, January 10, 2011

Thursday, January 6, 2011

Platinum and Blue Light Combine to Combat Cancer...

Research led by the University of Warwick, along with researchers from Ninewells Hospital Dundee, and the University of Edinburgh, have found a new light-activated platinum-based compound that is up to 80 times more powerful than other platinum-based anti-cancer drugs and which can use “light activation” to kill cancer cells in a much more targeted way than similar treatments. 

The University of Warwick team had already found a platinum-based compound that they could activate with ultra-violet light but that narrow wave length of light would have limited its use. Their latest breakthrough has discovered a new platinum based compound known as trans,trans,trans-[Pt(N3)2(OH)2(py)2] (see structure)  that can be activated by normal visible blue, or even green, light. It is also stable and easy to work with, and it is water soluble so it can simply dissolve and be flushed out of the body after use. Tests show that once activated by blue light the compound was highly effective requiring a concentration of just 8.4 micro moles per litre to kill 50% of the cancer cells. The researchers are also beginning to examine the compound’s effectiveness against ovarian and liver cancer cells. Early results there are also excellent but that testing work is not yet complete.

“This compound could have a significant impact on the effectiveness of future cancer treatments. Light activation provides this compound’s massive toxic power and also allows treatment to be targeted much more accurately against cancer cells...claims Prof.  Peter Sadler...

Ref : http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2980786/

Saturday, January 1, 2011

Ginseng just got better -- not as bitter

Ginseng just got better -- not as bitter

HAPPY NEW YEAR - 2011

WISHING ONE AND ALL "A HAPPY,  PROSPEROUS AND PEACEFUL NEW YEAR-2011.

Tuesday, December 28, 2010

Almonds can help treat, prevent type 2 diabetes and cardiovascular disease

We know that the sweet almond contains about 26% carbohydrates (12% dietary fiber, 6.3% sugars, 0.7% starch and the rest miscellaneous carbohydrates), and may therefore be made into flour for cakes and cookies (biscuits) for low-carbohydrate diets or for patients suffering from diabetes mellitus or any other form of glycosuria.

Now the same has been further substantiated by the researchers from Nutrition at Loma Linda University's School of Public Health and Principal Investigator for this study, which was conducted at the University of Medicine and Dentistry of New Jersey.

The study looked at the effects of consuming an almond-enriched diet as it relates to the progression of type 2 diabetes and cardiovascular disease in adults with pre-diabetes. After 16 weeks of consuming either an almond-enriched or regular diet, both of which conformed with American Diabetes Association (ADA) recommendations, the group that consumed an almond-enriched diet showed significantly improved LDL cholesterol levels and measures of insulin sensitivity, risk factors for heart disease and type 2 diabetes.

Researchers conclude that, overall, consuming an ADA-recommended diet consisting of 20% of the total calories from almonds for 16 weeks is effective in improving LDL cholesterol levels and measures of insulin sensitivity in individuals with pre-diabetes. Nutrients in almonds, such as fiber and unsaturated fat, have been shown to help maintain healthy cholesterol levels and increase insulin sensitivity, both of which help to prevent the development of type 2 diabetes and reduce the risk of cardiovascular disease.   It also provides evidence that suggests almonds contribute to heart health. However, it adds a new dimension to the existing research because it shows almond consumption not only aids in disease management, but may also help reduce the risk  of certain chronic diseases. Almonds offer 3.5 grams of fiber, 13 grams of unsaturated fat and only 1 gram of saturated fat per one-ounce serving.

Ref : http://www.almondboard.com/InTheNews/Pages/ArticleDetails.aspx?aID=97

Thursday, December 23, 2010

Wednesday, December 22, 2010

Researchers demonstrate that monensin antibiotic prevents prostate cancer cell growth

We know that, monensin was first described by Agtarap et al. in 1967, and was the first polyether antibiotic to have its structure elucidated in this way. The first total synthesis of monensin was reported in 1979 by Kishi et al. 

Researchers from VTT Technical Research Centre of Finland and the University of Turku have demonstrated that  "monensin" prevents the growth of prostate cancer cells. 

Evidence pointing to the effects of monensin emerged in a project investigating the effects of nearly 5,000 drugs and micromolecules on the growth of prostate cancer cells. The project involved most of the drugs on the market today. Researchers found that small amounts of compounds - disulfiram (Antabus), thiram, tricostatin A, and monensin (see structure) - can prevent the growth of prostate cancer cells without significant effects on the growth of the normal human prostate epithelial cells.  Further studies revealed that monensin caused prostate cancer cell death by reducing the amount of testosterone receptor and by increasing production of reactive oxygen species and inducing DNA damage. In addition, monensin was shown to have combined effects with anti-androgens - the drugs suppressing the effects of androgens - in preventing prostate cancer cell growth. 

"These research findings give rise to a potential new use for the monensin. The results also demonstrate that the effects of anti-androgens in suppressing the growth of cancer cells can be enhanced by using drugs inducing production of reactive oxygen species", say Senior Research Scientist Kristiina Iljin from VTT and Research Scientist Kirsi Ketola from the University of Turku....

Ref : http://www.vtt.fi/index.jsp
http://www.vtt.fi/news/2011/topicals/20111208_eturauhassyovanesto.jsp?lang=fi

Monday, December 20, 2010

Boceprevir drug may cure hepatitis C

In continuation of my update on Boceprevir
Boceprevir drug may cure hepatitis C