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.