Med-Chemist : "Quintessential Medicinal Chemistry"
Saturday, September 17, 2011
Tuesday, September 13, 2011
Biologists identify mechanism of H. pylori that damages DNA of gastric mucosal cells
In continuation of my update on H.Pylorihttp://www.med-chemist.com/search?q=pylori..
We know that, stomach bacterium Helicobacter pylori is one of the biggest risk factors for the development of gastric cancer, the third most common cause of cancer-related deaths in the world. Molecular biologists from the University of Zurich have now identified a mechanism of Helicobacter pylori that damages the DNA of cells in the gastric mucosa and sets them up for malignant transformation.
More at :
Biologists identify mechanism of H. pylori that damages DNA of gastric mucosal cells
Monday, September 12, 2011
Saturday, September 10, 2011
Researchers rethink fenretinide for prevention of oral cancer
In continuation of my update on fenretinide...
For more than two decades, researchers have studied and used fenretinide, a synthetic vitamin A
derivative. Fenretinide's capacity to induce both terminal
differentiation and cell death yielded highly promising results with
cultured human cancer cells. Likewise, studies in lung, breast skin, prostate and bladder animal cancer models re-enforced fenretinide's cancer-preventing effects at the in vivo level. However, when it came to prevention of oral cancer, fenretinide efficacy wasn't what scientists expected. After multiple studies with lackluster results, oral cancer researchers moved away from fentretinide to look elsewhere for an answer.
Now researchers lead by Dr. Susan Mallery started rethinking about the failure and wanted to find a way to circumvent issues with poor systemic uptake by delivering the compound directly to the lesion.
Mallery found the answer in partnering with two University of Michigan
pharmaceutical chemists (Steven Schwendeman and Kashappa Goud Desai) to
develop a first of its kind patch that sticks to the inside of the
mouth, and delivers a continuous therapeutic dose of fenretinide
directly to the precancerous lesion. The patch consists of three layers:
a disk saturated with fenretinide and polymers that make the lipid
soluble fenretinide better adsorbed in a water-rich environment, a
secondary adhesive ring to hold the disk in place, and a final backing
layer that ensures the medication stays inside the area of the patch.
The research team has just completed a pharmacokinetic study in rabbits.
Subsequent plans include an initial Phase zero study in humans,
followed by a clinical trial to evaluate efficacy
in patients with precancerous oral lesions. A companion formulation
designed to prevent emergence of pre-cancerous cells within the entire
mouth may also be used in the fenretinide patch clinical trial.
Ref : http://cancer.osu.edu/mediaroom/releases/Pages/Oral-Patch.aspx
Friday, September 9, 2011
Redesigned Vancomycin As Potent Antimicrobial Activity Against Vancomycin-Resistant Bacteria...
In continuation of my update on vancomycin....
Vancomycin normally works by grabbing hold of and sequestering the
bacterial cell-wall making machinery, a peptidoglycan (carbohydrate and
peptide containing molecule). Only Gram-positive bacteria have a cell
wall, which is a membrane on the cell's outer surface. Unfortunately, bacteria have found a way to alter the peptidoglycan in such a way that the antibiotic can no longer grab hold. Researchers claim that, the new vancomycin analogue can grab hold of the mutant peptidoglycan,
and again prevent the bacteria from making the cell wall and killing the
resistant bacteria. But what is so remarkable about the design is that
the redesigned antibiotic maintains its ability to bind the wild type
peptidoglycan as well.
New compound has an amidine (an iminium, RC=NH+ linked to a nitrogen,
N) instead of an amide at a key position buried in the interior of the
natural product. I appreciate the idea and the simplicity in achieving the target functional group.
Researchers add that, although it is still at its early stages and there is much work ahead.In my opinion it is a good beginning...
Thursday, September 8, 2011
Monday, September 5, 2011
In continuation of my update on Valproic acid...
New research suggests brain tumor patients who take the seizure drug valproic acid on top of standard treatment may live longer than people who take other kinds of epilepsy medications to control seizures. The research is published in the August 31, 2011, online issue of Neurology®, the medical journal of the American Academy of Neurology.....
Ref : http://www.neurology.org/content/75/24/2229.abstract?sid=49b511a0-d597-4598-865c-297439b6eb39
Saturday, September 3, 2011
Heat in Chili Peppers Can Ease Sinus Problems, Research Shows
In continuation of my update on the usefulness of Casaicin...
We know that, Capsicum annum contains capsaicin, which is the main component
of chili peppers and produces a hot sensation. Capsaicin is also the
active ingredient in several topical medications used for temporary pain
relief. It is approved for use by the U.S. Food and Drug Administration
and is available over the counter.
Now researchers lead by University of Cincinnati College of Medicine, Cincinnati, Ohio, have come up with an interesting finding about Capsicum annum. As per the claim by the researchers a nasal spray containing an ingredient derived from hot chili peppers (Capsicum annum) may help people "clear up" certain types of sinus inflammation. Researchers add that, study which showed that participants who used a nasal spray with Capsicum reported a faster onset of action or relief, on average within a minute of using the spray, than the control group and the spray is safe and effective on non-allergic rhinitis.
Interestingly, this is the first controlled trial where capsaicin was able to be used
on a continuous basis to control symptoms. It is considered a
significant advance, because of the fact that in the previous trials the ingredient was too hot to administer without anesthesia.
Ref : http://www.annallergy.org/article/S1081-1206%2811%2900383-8/abstract
Thursday, September 1, 2011
Wednesday, August 31, 2011
Medical engineers develop sensor chip to monitor cancerous tumors
A team of medical engineers headed by Prof. Bernhard Wolf at the TUM Heinz Nixdorf Chair of Medical Electronics have now developed a sensor chip that can be implanted close to a tumor. The sensor chip measures the concentration of dissolved oxygen in the tissue and wirelessly transmits this information to a receiver carried by the patient. The receiver forwards the data to the patient's doctor, who can then monitor the tumor's development and arrange for an operation or therapies such as chemotherapy. The tumor is thus continually monitored and the patient does not have to visit the practice or hospital as frequently for check-ups.
Researchers claim that, sensor chip has already passed laboratory tests with cell and tissue cultures. The main challenge for the researchers was developing a sensor that functions entirely autonomously for long periods of time. The sensor must continue to function and deliver correct values even in the presence of protein contamination or cell debris. It also has to be “invisible” to the body so that it is not identified as a foreign object, attacked and encapsulated in tissue.
We designed the sensor chip to self-calibrate to a set dissolved oxygen concentration at measurement intervals," explains engineer and project manager Sven Becker.....
More....
Sunday, August 28, 2011
Saturday, August 27, 2011
Yale scientists synthesize huperzine A to combat Alzheimer's
Scientists at Yale University have developed the first practical method to create a compound called huperzine A (see structure below) in the lab. Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the plant firmoss Huperzia serrata. Huperzine A is also an Acetylcholinesterase inhibitor, which has a mechanism of action similar to donepezil, rivastigmine, and galantamine. In the US, Huperzine A is sold as a dietary supplement for memory support. The botanical has been used in China for centuries for the treatment of swelling, fever and blood disorders. Clinical trials in China have shown it to be effective in the treatment of Alzheimer's disease and enhancing memory in students.
Sunday, August 21, 2011
FDA Approves Zelboraf - Potent New Melanoma Drug
Plexxikon Inc., a member of the Daiichi Sankyo Group, today announced
that applications for market approval for vemurafenib ( PLX4032/RG7204, see below structure)
for the treatment of metastatic melanoma have been submitted to the U.S.
Food and Drug Administration (FDA) and the European Medicines Agency
(EMA). The company had
Phase 2 and 3 trials (BRIM2 and BRIM3) that evaluated vemurafenib in patients with BRAF V600 mutation-positive melanoma, as determined by the cobas 4800 BRAF V600 Mutation
Test.
Earlier this year, the company reported positive data from an
interim analysis of BRIM3 which showed that the study met the
pre-specified criteria for co-primary endpoints for BRIM3 for
progression-free survival and overall survival, and that the safety
profile was generally consistent with the previous vemurafenib studies.
Based on these results, the data safety monitoring board for the trial
recommended early termination of the trial and allowed
dacarbazine-treated patients to immediately cross over to vemurafenib
treatment. BRIM2 results reported earlier showed a 52 percent confirmed
response rate, with tumor shrinkage in the majority of patients,
consistent with results from earlier studies.
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