Monday, September 28, 2009

Pralatrexate gets FDA approval....

We did know that Pralatrexate, also known as 10-propargyl- 10-deazaaminopterin, common name PDX, is a drug candidate being studied for the treatment of cancer. PDX is a Folate Anolog Inhibitor of dihydrofolate reductase. As of August 2008, it is undergoing Phase II clinical trials for the treatment of Hodgkin & Nonhodgkin lymphoma (including T -cell lymphoma), non-small cell lung cancer (NSCLC), and bladder cancer.

Now FDA has approved this drug. So at last, patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) will breathe a sigh of relief. FOLOTYN (Pralatrexate) is the first and only drug approved by the FDA for this indication and represents a new treatment option for patients with relapsed or refractory PTCL. This indication is based on overall response rate. Clinical benefit such as improvement in progression free survival or overall survival has not been demonstrated. Allos expects to make FOLOTYN available to patients in the U.S. in October.

More info...

Sunday, September 27, 2009

Novel Mass Spectrometry Application for drug discovery?

In one of my earlier blog, Dec., 28th 2008, ( FBDD- A New Approach Of Drug Discovery) I did mention about the use of a number of biophysical techniques as screening tools including high-throughput x-ray crystallography (the advantage of giving the best picture of how the fragment sits in the target) and when paired with NMR allows you to create a structure-based lead.

With different companies approaching this new route in different ways like :

  1. high-throughput x-ray crystallography
  2. NMR-fragment screening
  3. fluorescence polarization assay and many other interesting ways like Protien-Protein interactions etc., this field I think have important role to play.
The drug discovery field got a momentum and has lead to a new direction.....


While reading Science Daily (Online issue, Sept 21, 2009), I found this interesting (article ) and really innovative finding , which I want to share...

Preliminary studies by the researchers (Dr. Ken & Dr.Rakesh )have shown that the new mass spectrometry tool—known as MALDI-QqQMS (matrix-assisted laser desorption ionization-triple quadruple mass spectrometer)—provides a superior means of measuring the enzyme reactions critical to drug discovery at speeds comparable to currently available high-throughput screening systems at significantly lower costs. As per the claim by the researchers, Dr. Ken Greis, "If introduced broadly, the new generation mass spectrometry-based method the researchers are proposing could significantly reduce the cost of running drug compound screening assays while also saving drug development teams substantial time by improving the accuracy of data collected. As per the claim by these researchers the above mentioned methods are costly.

Dr. Ken Greis and Dr. Rakesh Rathore have developed a custom high-throughput screening method using a generalized platform. Unlike the commercially available systems that analyze byproducts and coupled reactions, their system directly measures and quantifies the substrate and the end product of the reaction. They say using mass spectrometry to measure the mass and quantity of the product gives researchers a direct measure of the assay and more reliable compounds to explore, eliminating the chances for molecular interference common with chemiluminescence and fluorescence-based systems. Its a remarkable achievement and hope in the near future we will have an automated system for commercial use with least expense. Best of luck. For More....

Superheavy Element 114 Confirmed.........

Superheavy Element 114 Confirmed: A Stepping Stone To The 'Island Of Stability'

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Certain Colors More Likely To Cause Epileptic Fits......

Certain Colors More Likely To Cause Epileptic Fits, Researchers Find

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Alternates to pheromones ?

I studied about the pheromones when I was doing my post graduation and the professor, who taught us has worked with Dr. H.C. Brown (Nobel Laureate, for his contribution to the field of Organo Boranes) made us understand what are pheromones, how they are prepared and how actually they attract the insects. I think the field has been widely accepted. As for as my knowledge goes the preparation of pheromones is a costly affair (via , organo boranes). Recently I found this interesting article, where in the researchers claim that with the help of alternate chemicals (other than pheromones) one can send insects off the scent of crops.

Dr. Antony Hooper of Rothamsted Research, an institute of BBSRC said, one way in which insects find each other and their hosts is by smell, or more accurately: the detection of chemical signals – pheromones, for example. Insects smell chemicals with their antennae; the chemical actually gets into the antennae of the insect and then attaches to a protein called an odorant-binding protein, or OBP. This then leads to the insect changing its behavior in some way in response to the smell, for example, flying towards a plant or congregating with other insects (that is what we were taught..) But the more interesting part of the research is .....studying an OBP found in the silkworm moth Bombyx mori, Dr Hooper and his team were able to look at how the OBP and a relevant pheromone interact. They also tested the interaction between OBP and other molecules (that are similar to, but not the same as, the pheromone). They actually found that there are other compounds that bind to the OBP much more strongly than the pheromone.

The researchers could potentially apply these compounds, in some way to block the insects’ ability to detect chemical signals – the smell would be overwhelmed by the one they introduced. and by doing so the researchers expect the insects to be less likely to orientate themselves towards the crop plants, or find mates in this case, and therefore could reduce the damage. Though still lot of work has to be done, its a good beginning.

Hope this new and innovative way to prevent and control pests and diseases will be a success in the days to come. I wish every success in their endeavor...

Congrats Dr. Antony Hooper and co-workers..

Ref :
http://www.bbsrc.ac.uk/media/releases/2009/090924_scientists_discover_how_to_send_insects_of_the_scent.html

Saturday, September 26, 2009

Stelara approved by the FDA for treating psoriasis

We know that Stelara (Ustekinumab), is a human monoclonal antibody that binds to the shared p40 protein subunit of human IL-12 and IL-23 with high affinity and specificity, thereby preventing interaction with their surface IL-12Rβ1 receptor. Hope this approval provides an alternative treatment for people with plaque psoriasis, which can cause significant physical discomfort from pain and itching and result in poor self-image for people who are self-conscious about their appearance...

Stelara approved by the FDA for treating psoriasis

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Years of caste system belie Indians' shared ancestry - life - 24 September 2009 - New Scientist

Though there were already some sort of genetic info, regarding the difference in the North & South Indians. This info should be used exclusively for medicinal purpose, but not to differentiate again between North & South Indians. After all human beings all over the world are same. We have already facing racial attacks in Australia and this info shldn't lead to difference amongst Indians !...





Years of caste system belie Indians' shared ancestry - life - 24 September 2009 - New Scientist

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Thursday, September 24, 2009

Water Found on the Moon

I think this article finds some significance with relevance to the presence of water..anyway wait for tomorrow.......



Water Found on the Moon

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Water on the moon? ISRO to announce on Friday

Eagerly waiting for Friday....



Water on the moon? ISRO to announce on Friday

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Wednesday, September 23, 2009

Rethinking of Alzheimer's Disease ?

So for the explanation for the Alzheimer's disease is "amyloid hypothesis", i.e., the disease results from of an accumulation of the peptide amyloid beta, the toxic protein fragments that deposit in the brain and become the sticky plaques that have defined Alzheimer's, this hypothesis has been accepted for 100 years. Something new explanation has been provided by George Bartzokis of UCLA professor of psychiatry and he says that a better working hypothesis is the "myelin model". He explains the model in the following lines :

Like insulation around wires, myelin is a fatty sheath that coats our nerve axons, allowing for efficient conduction of nerve impulses. It is key to the fast processing speeds that underlie our higher cognitive functions and encoding of memories. But the lifelong, extensive myelination of the human brain also makes it uniquely vulnerable to damage. The myelin model's central premise is that it is the normal, routine maintenance and repair of myelin throughout life that ultimately initiates the mechanisms that produce degenerative diseases like Alzheimer's. That is, the amyloid-beta peptide and the tau peptide, which is also implicated in Alzheimer's, as well as the signature clinical signs of the disease, such as memory loss and, ultimately, dementia, are all byproducts of the myelin breakdown and repair processes. The pervasive myelination of our brain is the single most unique aspect in which the human brain differs from other species.

Myelin is produced by oligodendrocytes, specialized glial cells that themselves become more vulnerable with age. Myelination of the brain follows an inverted U-shaped trajectory, growing strongly until our 50s, when it very slowly begins to unravel as we age. The myelin that is deposited in adulthood ensheaths increasing numbers of axons with smaller axon diameters and so spreads itself thinner and thinner. As a result, it becomes more susceptible to the ravages of age in the form of environmental and genetic insults and slowly begins to break down faster than it can be repaired.

The exclusive targeting of the amyloid-beta peptide for many years is understandable because the same genes and enzymes involved in controlling myelination and myelin repair are, ironically, also involved in the production of amyloid-beta proteins. Bartzokis' point is that the amyloid beta may actually develop as a result of the natural process of the repair and maintenance of myelin. So the breakdown that leads to Alzheimer's and other age-related brain diseases, such as Parkinson's, may begin much earlier, before the formation of the protein deposits that are used to define these diseases," Bartzokis said. Hope this explanation will lead to new innovative ideas for drug discoverers like rather than targeting amyloid-beta peptide !. Hoping for the better results....

Ref : http://newsroom.ucla.edu/portal/ucla/new-target-for-alzheimer-s-102065.aspx

Gene Therapy Trial To Treat Alzheimer's Disease !

The first study of its kind for the treatment of patients : the phase II study examines the safety and possible benefits of CERE-110. CERE-110 contains a gene and is injected during surgery into a part of the brain affected by Alzheimer's disease.

The gene will instruct brain cells to produce more of a protein, called Nerve Growth Factor or NGF, which helps nerve cells survive and function properly. The transfer of this gene into the brain is a medical technique called gene therapy. Though the goal is to to stop the progression of Alzheimer's disease, its a good move because still there are drugs to be innovated for the complete cure. Congrats Dr. Chris Kalhorn.


Ref : http://explore.georgetown.edu/news/?ID=44677&PageTemplateID=295

Naked mole rats may help cure cancer - health - 22 September 2009 - New Scientist


Naked mole rats may help cure cancer - health - 22 September 2009 - New Scientist

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Monday, September 21, 2009

Chandrayaan-1 X-ray Spectrometer Success To Provide New Understanding Of Lunar Surface

When I read about the news about the loss of contact with Chandrayaan-1 last month, I thought its huge loss and a set back to ISRO. At least some important info it has provided makes us feel oats. The data finds its significance because of the fact that the science team will be able to determine the geochemistry of new areas of the lunar surface, adding some vital pieces to the jigsaw of the mineralogy of the lunar surface. More....

Chandrayaan-1 X-ray Spectrometer Success To Provide New Understanding Of Lunar Surface

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Valturna gets FDA approval .....



FDA, has approved Valturna (valsartan & aliskiren respective structures above) tablets, the first and only medicine to target two key points within the renin system, also known as the renin angiotensin aldosteronesystem (RAAS), an important regulator of blood pressure. This is the first approval for Valturna, which is indicated for the treatment of Hypertension (high blood pressure) in patients not adequately controlled on aliskiren or angiotensin receptor blocker (ARB) monotherapy and as initial therapy in patients likely to need multiple drugs to achieve their blood pressure goals. This unique combination brings together the powerful blood pressure lowering effects of valsartan and aliskiren. Valturna combines in a single pill valsartan, the active ingredient in Diovan((R)), the number one selling branded Hypertension medicine worldwide, and aliskiren, the active ingredient in Tekturna((R)), the only approved direct renin inhibitor (DRI). Valturna offers significantly greater blood pressure reduction than either valsartan or aliskiren alone. Now for the first time, patients have a treatment option in one pill that targets two key points of the RAAS, which may be overactive in many hypertensive patients. The important fact about the combination is - by targeting two key points within the RAAS, Valturna helps blood vessels relax and widen so blood pressure is lowered. Research suggests that up to 85% of hypertensive patients may need multiple medications to help control their blood pressure, underscoring the need for effective combination treatments, hope this combined drugs will help the patients to a large extent. But those people with stroke, heart attack, heart failure, kidney failure or eye problems resulting from hypertension will have to wait for some more time....

Ref : http://www.novartis.com/newsroom/media-releases/en/2009/1342100.shtml

Sunday, September 20, 2009

Monolaurin as a microbial agent ?

We know that Coconut oil contains about 40 to 55 percent lauric acid. Lauric acid is the main saturated fatty acid found in coconut fat and in palm kernel oil. Lauric acid is also known as n-dodecanoic acid, which is a saturated medium chain C12-fatty acid, hence the Greek name “dodeca”, meaning twelve. A certain biochemical derivative of lauric acid, monolaurin (see right structure), has proven to be anti-viral, anti-bacterial, and anti-protozoal, both in vitro and in vivo experiments — and monolaurin can destroy lipid-coated viruses, including influenza. Lauric acid, however does not have these properties as strongly as monolaurin. When ingesting coconut oil, only a small percentage—an estimated 3%--of the lauric acid will be transformed by the body into the active monolauric acid. This has been shown to elevate the body’s overall immunity to some degree.

Though there were many companies selling this as a dietery suppliment, now monolaurin has been recognized as safe by the U.S. Food and Drug Administration (FDA) and is known for its antimicrobial properties. If used in combination with other antimicrobial agents, monolaurin can present an effective barrier to microorganisms.

Thanx to the researchers from Zhejiang University in China, who studied the use of monolaurin as a nontraditional preservative in food products by combining it with commonly used antimicrobials in various concentrations and testing it on bacterial strains including Esherichia coli and on food components such as soy protein and water-soluble starch.

The findings are really interesting :

1. Monolaurin combined with ethylenediaminetetraacetic acid (EDTA),a binding agent, was effective against Esherichia coliand Bacillus subtilis but not Staphylococcus aureus.

2. When combined with the antimicrobial nisin, monolaurin was synergistically effective against all three bacteria.

3. Antibacterial effectiveness was reduced by fat or starch but was not affected by protein.

Congrats for this achievement...

Ref : http://www.ift.org/cms/?pid=1002122

Podophyllotoxin in American Mayapple ?


A common plant called American mayapple (see the picture) may soon offer an alternative to an Asian cousin that's been harvested almost to extinction because of its anti-cancer properties. The near-extinct Asian plant, Podophyllyum emodi, produces podophyllotoxin (see the structure), a compound used in manufacturing etoposide, the active ingredient in a drug used for treating lung and testicular cancer. Podophyllyum emodi is a cousin of the common mayapple, sometimes considered a weed, found in the United States.

Podophyllotoxin and its derivatives are used in several commercially available pharmaceutical products such as the anticancer drugs etoposide, teniposide, and etopophos, which are used in the treatment of small-cell lung cancer, lymphoblastic leukemia, testicular cancer, and brain tumors. Podophyllotixin derivatives are also used for the treatment of psoriasis and malaria, and some are being tested for the treatment of rheumatoid arthritis. Currently, podophyllotoxin is produced commercially using the roots and rhizomes of Indian mayapple, an endangered species harvested from the wild in India, Pakistan, Nepal, and China.

Now the researchers from the US, found that mayapple colonies in the eastern part of the United States can be used for the development of high podophyllotoxin cultivars, which could subsequently provide the base for commercial production of podophyllotoxin in the United States.

Ref : http://hortsci.ashspublications.org/cgi/content/abstract/44/2/349



Link Between Protein And Lung Disease Found

Link Between Protein And Lung Disease Found

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House plants to cut Indoor Ozone !

We know that ozone, the main component of air pollution or smog, is a highly reactive, colorless gas formed when oxygen reacts with other chemicals. And ozone pollution is most often associated with outdoor air, the gas also infiltrates indoor environments like homes and offices. And that is why those who have allergy like 'morning sneeze' will be advised by doctors to avoid going outside early in the morning and one can follow this advise sincerely. But when I read in an article that ozone can be released by ordinary copy machines (xerox machines), laser printers, ultraviolet lights, and some electrostatic air purification systems, all of which contribute to increased indoor ozone levels, I got an answer for one of my freind's problem.

We are aware that the extensive list of toxic effects of ozone on humans are pulmonary edema, hemorrhage, inflammation, and reduction of lung function. So I was wondering how one can take care of themselves even by staying in house (avoiding morning walk) ?.

Recently I found this interesting fact that three common indoor houseplants (see pictures), snake plant (Sansevieria trifasciata), spider plant (Chlorophytum comosum), and golden pothos (Epipremnum aureum) can reduce the ozone concentrations effectively.

Hope plants as a mitigation method could serve as a cost-effective tool, where expensive pollution mitigation technology may not be economically feasible in the days to come....

Ref : http://horttech.ashspublications.org/cgi/content/abstract/19/2/286

Current Hepatitis C Treatments................

Current Hepatitis C Treatments Work Equally Well, Researchers Report

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Saturday, September 19, 2009

Necklace For Long-term And Robust Cardiac Monitoring In Daily Life

Necklace For Long-term And Robust Cardiac Monitoring In Daily Life

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New Antituberculosis Compounds ?

We all know how TB has become a pandemic and several attempts to eradicate the disease have been tried and scientists are still finding new ways. However the most disadvantage part for the scientists lies in the fact that "the disease-causing bacteria have a sophisticated mechanism for surviving dormant in infected cells". i.e., TB bacteria have a sophisticated way to remove the damaged proteins — a protein-cleaving complex known as a proteasome — identified in earlier research by the Nathan lab. By breaking down damaged proteins, the proteasome allows the bacteria to remain dormant, and possibly go on to cause active TB. And hence finding drugs to disable the proteasome would be a new way to fight TB.

In developing proteasome-inhibitor drugs, scientists face several hurdles. A significant one is the fact that human cells also possess proteasomes, which are essential to their survival. To be effective, the drugs would have to specifically target the TB proteasome without adversely affecting the human protein-cleanup complex.

This study represents a shift in strategy for designing antibiotics that treat TB, says Dr. Lin (Assistant Research professor of Microbiology and Immunology at Weill Cornell Medical College). All the groups who tried focused on developing drugs that attacked the bacterium in its active phase, but this group has found a compound that may help to destroy it in its dormant stage.

The Weill Cornell team screened 20,000 compounds for TB proteasome inhibition activity. They identified and synthesized a group of inhibitors, which they then tested for their ability to inhibit the proteasome inside the mycobacteria. They also tested the compounds' effect on monkey epithelial cells and human immune system cells in culture. After reading this article, I could recollect the High Throughput Screening of my compounds (Southern Research Institute, Birmingham).  The newly synthesized compounds are specific, less toxic, more active and more over the inhibition of the TB proteasome is irreversible and about 1,000-fold more effective than the minor inhibition observed against human proteasomes.

The structural studies revealed that the inhibitor molecules block the proteasome's ability to degrade proteins in more than one way: by producing a direct chemical change to the proteasome active site, and by altering the conformation of the "pocket" into which protein fragments bind before being degraded. Congrats for this efforts and all the best for their future endeavor.... More....

New Material For Nanoscale Computer Chips

We already use various organic materials for example, flat screens, such as OLED (Organic Light Emitting Diode). The new results show how small and advanced devices made of organic materials can become. I read recently about an article in a blog titled Cell phone TV ? and was amused by the use of OLED and it may overtake the usage of LCDs. I would say the following findings are really interesting and are a step ahead - nanochemists from the Chinese Academy of Sciences and the Nano-Science Center, Department of Chemistry have developed nanoscale electric contacts out of organic and inorganic nanowires. In the contact they have crossed the wires like Mikado sticks and coupled several contacts together in an electric circuit. In this way they have produced prototype computer electronics on the nanoscale and by doing so they have succeeded in placing several transistors consisting of nanowires together on a nano device. Though it is a first step towards realisation of future electronic circuitry based on organic materials – a possible substitute for today’s silicon-based technologies. Hope this step will lead to the possibility of making computers in different ways in the near future...

Ref : http://www.ku.dk/english/news/?content=http://www.ku.dk/english/news/danish_chinese_nano_science.htm

New Marker For Alzheimer's Discovered

New Marker For Alzheimer's Discovered

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Genetic Hint For Ridding The Body Of Hepatitis C

Genetic Hint For Ridding The Body Of Hepatitis C

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Ways To Quiet Ordinary Snoring

Ways To Quiet Ordinary Snoring

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A Chip For The Eye? Artificial Vision Enhancers Being Put To The Test

A Chip For The Eye? Artificial Vision Enhancers Being Put To The Test

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New Rabies Vaccine May Require Only A Single Shot... Not 6 !

People were really scared about the number of injections (it used to varies from 12 to 6) rather than the real pain of the dog's bite. Now thanks to Dr. McGettigan according to the researchers, a replication-deficient rabies virus vaccine that lacks a key gene called the matrix (M) gene induced a rapid and efficient anti-rabies immune response in mice and non-human primates.

The M gene is one of the central genes of the rabies virus, and its absence inhibits the virus from completing its life cycle. The virus in the vaccine infects cells and induces an immune response, but the virus is deficient in spreading. The immune response induced with this process is so substantial that only one inoculation may be sufficient enough both pre-exposure and post-exposure settings. The details will be published in the forth coming journal of infectious disease (J Infect Dis.).

Congrats, Dr.McGettigan and co-workers.

Thursday, September 17, 2009

Survey Concludes Telaprevir a Winner for HCV Genotype 1 | Hepatitis Central News, Updates and Commentary

I did mention in my earlier blog about this drug and one person did (Dawn - Blog Name) mention she was happy about the info. I am sure the following update will help her. All the best...(Dawn, U can mail me at dr.umesh1969@gmail.com-if u find this info useful). I am happy something I did blog and that helped a needy & this encourages me to do spend more time with my blog.....

Survey Concludes Telaprevir a Winner for HCV Genotype 1 | Hepatitis Central News, Updates and Commentary

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FDA Okays Vaccines for 2009 H1N1 Influenza Virus !

At last one can breathe a sigh of relief from the H1N1 pandemic.....


FDA's approval of the Vaccine for H1N1.........


News: FDA Okays Vaccines for 2009 H1N1 Influenza Virus.

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Tuesday, September 15, 2009

Tuberculosis Patients Can Reduce Transmissability By Inhaling Interferon Through A Nebulizer

As for as my knowledge goes "Interferons" - (glycoproteins - natural cell-signaling proteins produced by the cells of the immune system of most vertebrates in response to challenges such as viruses, parasites and tumor cells).

1.  assist the immune response by inhibiting viral replication within host cells, activating natural killer cells and macrophages, increasing antigen presentation to T lymphocytes.

2. increasing the resistance of host cells to viral infection.

And are said to possess the antiviral and antitumour activity.   

But this finding is really interesting.................."Tuberculosis Patients Can Reduce Transmissability By Inhaling Interferon Through A Nebulizer

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New look at Alzheimer's could revolutionise treatment - health - 09 September 2009 - New Scientist

New look at Alzheimer's could revolutionise treatment - health - 09 September 2009 - New Scientist

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Tigecycline- as antimalarial drug ?


                As for my knowledge goes,  'Tigecycline'  is being used  as  drug for the antibiotic resistant strain 'Staphylococcus aureus'.  And this drug belongs to the class of "glycylcyclines" (similar to tetracyclines : central four-ring carbocyclic skeleton).  The broad spectrum activity is attributed to the  D-9 position substitution. It is a bacteriostatic and acts by the inhibition of protein synthesis. It has been found to be active against both Gram positive and Gram negative bacterii. 

Now thanx to the researchers from the Medical University of Vienna, Austria, who have achieved something interesting feat, i.e.,  Tigecycline has significant antimalarial activity on its own and may also be effective against multi drug-resistant malaria when administered in combination with traditional antimalarial drugs

Increasing resistance of Plasmodium falciparum to existing drugs has resulted in the search for new antimalarial therapies and I congratulate the team for this important achievement.  More interestingly the drug is 6 times more active against P. falciparum than doxycycline. As the drug itself is an established one,  its one more addition to the serendepity list. Congrats the team...

Ref : http://www.asm.org/index.php?option=com_content&view=article&id=91042


Monday, September 14, 2009

Novel Drug Screening Method: Informative Swellings

Novel Drug Screening Method: Informative Swellings

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Lurasidone - positive results from phase 3 clinical trials !

I  read about this compound few months back, that it is one of  "atypical antipsychotic" drugs that are being tried and this drug has shown promising results in the phase II and is being studied clinically for phase III  by a Japanese company.  


As per the claims by the company 'Lurasidone,  blocks D2- and 5-HT2A-receptors and the advantage is it causes less extrapyramidal side effects than current antipsychotics.


Yes the phase 3 results are really interesting,  with Lurasidone 40 and 120 mg, taken once-daily, demonstrated significantly greater improvement versus placebo on the primary efficacy measure. A total of 53% of patients on lurasidone 40 mg/day and 47% of patients on lurasidone 120 mg/day demonstrated a 30% or more improvement on the PANSS total score from baseline versus 38% on placebo. Lurasidone was also well-tolerated with an overall discontinuation rate similar to placebo (40% vs. 39% placebo) and few adverse event-related discontinuations (9% for both the overall lurasidone group and placebo). Adverse events seen in the trial were generally mild.

Congrats for this achievement. 

Ref : http://dsp-america.com/pdf/news/LurasidonePh3Results.pdf

Tigecycline- as antimalarial drug ?


                As for my knowledge goes,  'Tigecycline'  is being used  as  drug for the antibiotic resistant strain 'Staphylococcus aureus'.  And this drug belongs to the class of "glycylcyclines" (similar to tetracyclines : central four-ring carbocyclic skeleton).  The broad spectrum activity is attributed to the  D-9 position substitution. It is a bacteriostatic and acts by the inhibition of protein synthesis. It has been found to be active against both Gram positive and Gram negative bacterii. 

Now thanx to the researchers from the Medical University of Vienna, Austria, who have achieved something interesting feat, i.e.,  Tigecycline has significant antimalarial activity on its own and may also be effective against multi drug-resistant malaria when administered in combination with traditional antimalarial drugs

Increasing resistance of Plasmodium falciparum to existing drugs has resulted in the search for new antimalarial therapies and I congratulate the team for this important achievement.  More interestingly the drug is 6 times more active against P. falciparum than doxycycline. As the drug itself is an established one,  its one more addition to the serendepity list. Congrats the team...

Ref : http://www.asm.org/index.php?option=com_content&view=article&id=91042

Sunday, September 13, 2009

How one can prepare for the H1N1 flu ......

We all should be thankful to the U.S. Department of Health and Human Services (HHS), for there effort in educating about the health problems.  I find these webcasts very useful in understanding the H1N1 flu and how one  can prepare for this pandemic.  The efforts by the govt., is  highly appreciable as there are many myths about this virus !.

Those interested can go through the webcast archives   about the H1N1 flu.

Saturday, September 12, 2009

Doxorubicin granted orphan drug designation by the FDA

Doxorubicin granted orphan drug designation by the FDA

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Increase in Rifampicin dosage shortens tuberculosis treatment duration !

Increase in Rifampicin dosage shortens tuberculosis treatment duration

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A single dose vaccine for Swine flu !.....

I am reading anything and everything about this H1N1, since it started in Mexico and there were so many different names (many names  like - swine flu !, Mexican flu, ....).   The deadly virus has caused panic in each and every country, where there are reports of infection of H1N1.  The real concern is the use of antibiotics and the real black market  for Tamiflu and so many falsely claimed  drugs. Now thanx to Dr. Russell Basser and group who have found that a single 15-µg dose of 2009 H1N1 vaccine was immunogenic in adults, with mild-to-moderate vaccine-associated reactions. Congrats for for this important  achievement. 

A (H1N1) 2009 virus is responsible for the first influenza pandemic in 41 years. This itself shows how important the vaccine is.  The results are really interesting and as per the claim by the researchers : by day 21 after vaccination,  antibody titers of 1:40 or more were observed in 96.7%  those who received the 15-µg dose  and 93.3% who received the 30-µg dose. No deaths, serious adverse events, or adverse events of special interest were reported. Local discomfort (e.g., injection-site tenderness or pain) was reported by 46.3% of subjects, and systemic symptoms (e.g., headache) by 45.0% of subjects. Nearly all events were mild to moderate in intensity.  

Hope the efforts by the Australian drug maker CSL, Ltd. has yielded a novel vaccine that could take care of the H1N1 pandemic. Congrats once again for this achievement. 

Ref : http://content.nejm.org/cgi/content/full/NEJMoa0907413


Sunday, September 6, 2009

Secrets Of Scorpion Venom revealed .....

Genetic Analysis Reveals Secrets Of Scorpion Venom

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New Supercomputer -- Cystorm (Unleashes 28.16 Trillion Calculations Per Second)

New Supercomputer -- Cystorm -- Unleashes 28.16 Trillion Calculations Per Second

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Discovery Of Natural Odors- a new way to develop cheaper mosquito repellents !..

Entomologists at the University of California, Riverside (Anandasankar Ray, an assistant professor in the Department of Entomology, and Stephanie Turner, his graduate student)  working on fruit flies in the lab have discovered a novel class of compounds that could pave the way for developing inexpensive and safe mosquito repellents for combating West Nile virus and other deadly tropica. 

The basis for the 'invention' though looks simple, but this finding is of great importance. As for my knowledge goes most of the mosquito repellents are cyclohalothrins, which are a costly affair to prepare [as a synthetic chemist,  I know how difficult its to prepare cyclohalothrins (pyrethroids)  e.g., Allethrin & Permethrin. When I was working in Rallis India Limited, one of my senior colleague was working on Permethrin and I know how difficult to introduce the halo group that too by using florochlorocarbons CFCs (banned chemicals !)]. Congrats Anandsankar Ray, for this interesting achievement. 

When fruit flies undergo stress, they emit carbon dioxide (CO2) that serves as a warning to other fruit flies that danger or predators could be nearby. The fruit flies are able to detect the CO2 and escape because their antennae are equipped with specialized neurons that are sensitive to the gas.

But fruits and other important food sources for fruit flies also emit CO2 as a by-product of respiration and ripening. If the innate response of the fruit fly is to avoid CO2, how then does it find its way to these foods?. The researchers have have identified a new class of odorants – chemical compounds with smells – present in ripening fruit that prevent the CO2-sensitive neurons in the antennae from functioning. In particular two odors, hexanol and 2,3- butanedione, are strong inhibitors of the CO2-sensitive neurons in the fruit fly.

CO2 emitted in human breath is the main attractant for the Culex mosquito to find people, aiding the transmission of these deadly diseases," Ray said. In their  experiments they  identified hexanol, and a related odor, butanal, as strong inhibitors of CO2-sensitive neurons in Culex mosquitoes. These compounds can now be used to guide research in developing novel repellents and masking agents that are economical and environmentally safe methods to block mosquitoes.
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Fruits better than prviously thought !.......

Polyphenol content in fruits usually refers to extractable polyphenols, but a Spanish scientist working at the Institute of Food Research in Norwich analysed apple, peach and nectarine. She found that nonextractable polyphenol content is up to five times higher than extractable compounds. Its really interesting and that might be the reason why our forefathers used to insist to eat whole fruits (though they might not have studied so exhaustively... !).  

The interesting findings like,  "polyphenols need to be treated with acid to extract them from the cell walls of fruit in the lab" will help at least now onwards to collect all the useful polyphenols (proanthocyanidins, ellagic acid and catechin)  which without this new findings might have gone as waste.  Dr Paul Kroon from IFR explains: “In the human body these compounds will be fermented by bacteria in the colon, creating metabolites that may be beneficial, for example with antioxidant activity. 

Hope these  nonextractable polyphenols, (which mostly escape analysis and are not usually considered in nutritional studies),  will play a major part of bioactive compounds in the diet  in the days to come. Congrats Professor Saura-Calixto, for this  achievement.....