Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

UMass Amherst Researchers Test a Drug-Exercise Program Designed to Prevent Type 2 Diabetes

In continuation of my update on Metformin...

Kinesiology researcher Barry Braun of the University of Massachusetts Amherst and colleagues recently reported unexpected results of a study suggesting that exercise and one of the most commonly prescribed drugs for diabetes, metformin, each improves insulin resistance when used alone, but when used together, metformin blunted the full effect of a 12-week exercise program in pre-diabetic men and women.

Ref : http://www.umass.edu/newsoffice/newsreleases/articles/142505.php

Editorial: An apple a day keeps colitis away

In continuation on my update on the benefits of apple

Editorial: An apple a day keeps colitis away:

More : http://msuextension.org/publications/AgandNaturalResources/MT200812AG.pdf

'via Blog this'

European Commission approves Vyndaqel® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP)

We know that, Tafamidis (see structure) or Vyndaqel was discovered in the Jeffery W. Kelly Laboratory at The Scripps Research Institute using a structure-based drug design strategy and was developed at FoldRx pharmaceuticals, a biotechnology company led by Richard Labaudiniere that was acquired by Pfizer in 2010.

Tafamidis or Vyndaqel functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. In patients with FAP, this protein dissociates in a process that is rate limiting for aggregation including amyloid fibril formation, causing neurodegeneration and failure of the autonomic nervous system and/or the peripheral nervous system and/or the heart.

Now, European Commission has approved Vyndaqel^® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy.

More...

HSC NEWS - Bat plant could give some cancers a devil of a time

In a new study published this month in the Journal of the American Chemical Society, researchers with The University of Texas Health Science Center at San Antonio have pinpointed the cancer-fighting potential in the bat plant, or Tacca chantrieri......

HSC NEWS - Bat plant could give some cancers a devil of a time

FDA Approves Intermezzo.....

The U.S. Food and Drug Administration today approved Intermezzo (zolpidem tartrate sublingual tablets) for use as needed to treat insomnia characterized by middle-of-the-night waking followed by difficulty returning to sleep.

This is the first time the FDA has approved a drug for this condition. Intermezzo should only be used when a person has at least four hours of bedtime remaining. It should not be taken if alcohol has been consumed or with any other sleep aid....

More....

Coffee may protect against womb cancer: Study

 In continuation of my update on the benefits of coffee

A new study shows that regular intake of coffee may significantly lower risk for endometrial or womb cancer.

For the study the researchers looked at coffee consumption and endometrial cancer risk in more than 67,000 women aged between 34 and 59 enrolled in the long-running Nurses' Health Study. The researchers found that women who took more than four cups of coffee a day over a 26-year period were 25 percent less likely to get the cancer. Women who drank two to three cups a day were 7 percent less likely to get it. Drinking less than four cups a day was not associated with reduced risk. Furthermore drinking tea did not reduce the risk. Additionally drinking more than two cups of decaffeinated coffee a day was tied to a 22 percent reduced risk for endometrial cancer.

The benefit wasn't a complete surprise, since coffee has been shown to lower estrogen and insulin levels, and higher levels of these hormones have been associated with an increased risk of endometrial cancer. But the new findings do help to clarify how obesity, estrogen and coffee might interact in triggering tumors.

“It would be premature to make a recommendation that women drink coffee to lower their endometrial cancer risk,” study author Dr. Edward Giovannucci, professor of nutrition and epidemiology at Harvard School of Public Health...

Ref : http://cebp.aacrjournals.org/content/early/2011/10/03/1055-9965.EPI-11-0766.abstract?sid=d8d229ed-e4b4-4b7a-bc6a-f3f86cba4c0e

Cisplatin anti-cancer drug binds pervasively to RNA....

In continuation of my update on Cisplatin.....

An anti-cancer drug used extensively in chemotherapy binds pervasively to RNA -- up to 20-fold more than it does to DNA, a surprise finding that suggests new targeting approaches might be useful, according to University of Oregon researchers, lead by Victoria J. DeRose

Ref : http://uonews.uoregon.edu/archive/news-release/2011/11/cancer-drug-cisplatin-found-bind-glue-cellular-rna

Old drugs find new target for treating brain tumor

In continuation of erlotinib ................................

Old drugs find new target for treating brain tumor

Researchers discover new class of antimalarial compounds...

Researchers have discovered a group of chemical compounds that might one day be developed into drugs that can treat malaria infection in both the liver and the bloodstream. The study, which appears in the Nov. 18 issue of Science, was led by Elizabeth A. Winzeler, Ph.D., of the Scripps Research Institute in La Jolla, Calif., and was partially funded by the National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health.

By screening more than 4,000 chemical compounds that had previously shown activity against blood-stage Plasmodium, the investigators searched for a compound that would also inhibit liver-stage parasites and whose protein structure would allow the modification necessary for future drug development. They found that a group of three related compounds, known collectively as the imidazolopiperazine (IP) cluster, fit these criteria. In addition, strains of Plasmodium that had acquired resistance to other malaria drugs were susceptible to the IP cluster.

Using the IP cluster as a foundation, the researchers designed a drug candidate, GNF179, that reduced levels of one Plasmodium species by 99.7 percent and extended survival by an average of 19 days when tested in malaria-infected mice. By examining infected cells, the researchers confirmed that GNF179 (see the structure) was active in the liver stage of infection. Rresearchers note that while additional studies will be needed to fully understand the drug's mechanism of action and its specific targets within the liver, this study provides a potential starting point for developing new dual-stage antimalarial drugs.....

More : http://www.sciencemag.org/content/early/2011/11/16/science.1211936.abstract

New efficient synthesis for Taxol ?

In continuation of my update on taxol....

Baran's group reports erecting that Rockefeller tree and adding the first few ornaments -- a molecule called taxadiene. A conventional taxadiene synthesis is inefficient and involves 26 steps to produce. The Baran group's method involves just 10 steps to produce many times what has been previously synthesized -- more than sufficient for planned research to find a way to efficiently produce Taxol®.

Innovation Leads to Access.....

The taxadiene synthesis is more than just a midway stop on the way to Taxol®. The current commercial Taxol® production method, which involves culturing cells from the yew tree, is more economical than any new synthesis is likely to be. Instead, Baran and his team are aiming to understand the processes used in nature to produce the compound, which are many times more efficient than those used by scientists to date. "It's my opinion that when there's a huge discrepancy between the efficiency of nature and humans, in the space between, there's innovation.

More specifically, lead researcher Phil Baran believes that, while developing an efficient synthesis for Taxol®, they will gain a fundamentally improved understanding of the chemistry involved and develop more widely applicable techniques. Such innovation could allow production of a whole range of taxanes currently inaccessible for drug discovery research either because the quantities researchers can produce are vanishingly small, or because they can't produce them at all. Control of the taxane oxidation process therefore offers the potential for discovering new and important drugs, perhaps even one or more that is better at fighting specific cancers than Taxol®.

Establishing the remaining steps between taxadiene and Taxol® or other more complex taxanes remains a challenging task that Baran estimates will take years.

"Nature has a choreography in the way she decorates the tree," he said. "It's a precise dance she has worked out over millennia. We have to figure out a way to bring that efficiency to the laboratory setting."

More... : http://www.nature.com/nchem/journal/vaop/ncurrent/full/nchem.1196.html

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF

In continuation of my up date on rivaroxaban.....

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF: The U.S. Food and Drug Administration today approved the anti-clotting drug Xarelto (rivaroxaban) to reduce the risk of stroke in people who have abnormal heart rhythm.

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

In continuation of my update on the benefits of nuts...

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

Crocin for multiple sclerosis?

Medical researchers at the University of Alberta have discovered that an active ingredient in the Persian spice saffron may be a potential treatment for diseases involving neuroinflammation, such as multiple sclerosis. Researchers found there is a compound in saffron, known as crocin (see the structure below), that exerts a protective effect in brain cell cultures and other models of MS. It prevented damage to cells that make myelin in the brain.

Lead researcher  Power said. "Myelin is insulation around nerves. MS is characterized by inflamed brain cells that have lost this protective insulation, which ultimately leads to neurodegeneration.......

More......

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Ref : http://www.nature.com/ajg/journal/v106/n10/full/ajg2011201a.html