Friday, November 18, 2011

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."

Tuesday, November 15, 2011

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.

Sunday, November 13, 2011

Tuesday, November 8, 2011

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......

Friday, November 4, 2011

In continuation of my update on usefulness of benzodiazepine derivatives

Lundbeck Inc. presented interim data from its long-term, open-label extension study evaluating ONFI™ (clobazam see structure below) CIV for the adjunctive treatment of drop seizures associated with Lennox-Gastaut syndrome (LGS). Company claims that, these interim results support the reductions in drop seizure rates associated with ONFI when used as add-on therapy for adult and pediatric patients, two years of age or older, with a current or previous diagnosis of LGS. ....



More....

Thursday, November 3, 2011

Biogen’s Multiple Sclerosis pill succeeds at a late phase clinical trial

Biogen Idec Inc. has reported success in a late stage clinical trial of its oral multiple sclerosis drug BG-12 (see below structure), a competitor's of Teva Pharmaceutical Industries’ Laquinimod. A 240-milligram dose of BG-12 administered two or three times a day significantly reduced the proportion of patients who relapsed by 49% and 50%, respectively, after two years compared with a placebo....

Company adds that, in addition to significantly reducing ARR, BG-12 met all secondary relapse and MRI endpoints for both dose regimens.....


Wednesday, November 2, 2011

Leafy greens (broccoli and cabbage) protect the gut’s immune system

In continuation of my update on Broccoli and its usefulness 

Research from the Babraham Institute and the Medical Research Council (MRC), were able to prove that leafy greens protect a certain type of immune cell known as intra-epithelial lymphocytes (IELs). IELs play a crucial role in keeping the gut lining healthy and preventing ‘bad’ bacteria from entering the gut while maintaining the balance of ‘good’ bacteria which help us to break down our food. Researchers studied mice fed a diet containing many vitamins and minerals known to be essential for good health, but which lacked vegetables. Over three weeks the mice lost 70 to 80 per cent of IELs.


The research showed for the first time that mice fed a diet low in vegetables rapidly lose these specialised immune cells lining the intestinal tract, but not other immune cells. The team discovered that IELs depend on chemical signals from the digestive breakdown products of a substance called Indole-3-carbinol, high levels of which are found in vegetables like broccoli and cabbage.......

Ref :1. http://www.mrc.ac.uk/Newspublications/News/MRC008231
2.  http://www.sciencedirect.com/science/article/pii/S0092867411011366