S-methylmethionine (Vitamin U) as antiulcer agent .......

About S-methylthionine :

S-Methylmethionine, or S-methyl-L-methionine, is a derivative of methionine In plants, it is produced from methionine by the enzyme methionine S-methyltransferase. S-Methyl- methionine is sometimes called vitamin U in naturopathic medicine, but it is not recognized as a vitamin by mainstream nutrition science. Methionine in itself has not been demonstrated as effective for treating peptic and duodenal ulcers. Its proponents claim that sources of methionine are limited, or claim it can be found only in raw cabbage; however, these claims are incorrect. Methionine is a common amino acid found in a wide variety of fruits, vegetables, and legumes.

More interesting results by the researchers from the Stanford University, have further substantiated the claim that it can be used to treat peptic and duodenal ulcers.

Acetaminophen is a pain reliever present in many over-the-counter cold and flu medicines. It is broken down, or metabolized, in the body into byproducts , one of which can be very toxic to the liver. At normal, therapeutic levels, this byproduct is easily deactivated when it binds to a naturally occurring, protective molecule called glutathione. But the body's glutathione stores are finite, and are quickly depleted when the recommended doses of acetaminophen are exceeded. Acetaminophen overdose is the most common cause of liver transplantation and the only effective antidote is an unpalatable compound called NAC that can induce nausea and vomiting, and must be administered as soon as possible after the overdose.

As per the claim by the authors, an enzyme called Bhmt2 helped to generate more glutathione. Bhmt2 works by converting the diet-derived molecule S-methylmethionine, or SMM, into methionine, which is subsequently converted in a series of steps into glutathione. The researchers confirmed the importance of the pathway by showing that SMM conferred protection against acetaminophen-induced liver toxicity only in strains of mice in which the Bhmt2 pathway was functional.

By administering SMM, which is found in every flowering plant and vegetable, we were able to prevent a lot of the drug’s toxic effect,” said Peltz. He and his colleagues are now working to set up clinical trials at Stanford to see whether it will have a similar effect in humans. In the meantime, though, he cautions against assuming that dosing oneself with SMM will protect against acetaminophen overdose....

Source : http://med.stanford.edu/ism/2009/november/peltz.html

Top 10 Amazing Chemistry Videos

Top 10 Amazing Chemistry Videos

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Mode of action of tetrathiomolybdate (a drug for Wilson's disaese) established ?

We know that Ammonium tetrathiomolybdate ([NH₄]₂MoS_4), was first used therapeutically in the treatment of copper toxicosis in animals. It was then introduced as a treatment in Wilson's disease, a hereditary copper metabolism disorder, in humans; it acts both by competing with copper absorption in the bowel and by increasing excretion. It has also been found to have an inhibitory effect on angiogenesis, potentially via the inhibition of Cu ion dependent membrane translocation process invovling a non-classical secretion pathway. This makes it an interesting investigatory treatment for cancer, age-related macular degeneration, and other diseases featuring excessive blood vessel deposition. Though the activity was established mode of action was to be established. Now researchers from Northwestern University , have achieved something which was eluding so for. As per the claim by the researchers, the three-dimensional structure of TM bound to copper-loaded metallochaperones. The drug sequesters the chaperone and its bound copper, preventing both from carrying out their normal functions in the cell. For patients with Wilson disease and certain cancers whose initial growth is helped by copper-dependent angiogenesis, this is very promising. O'Halloran and his research team studied the copper chaperone protein Atx1, which provides a good model of copper metabolism in animal cells.

The drug brings three copper chaperones into close quarters, weaving them together through an intricate metal-sulfur cluster in a manner that essentially shuts down the copper ferrying system.

The nest-shaped structure of the metal-sulfur cluster discovered by the researchers was completely unanticipated. The sulfur atoms in the tetrathiomolybdate bound to the copper atoms to form an open cluster that bridged the chaperone proteins. In this manner, three copper proteins were jammed onto one thiomolybdate. More interestingly the structure of the complex has been concluded by X-ray studies. Based on the structure and additional experiments, the scientists propose that the drug inhibits the traffic of copper within the cell because of its ability to sequester copper chaperones and their cargo in clusters, rendering the copper inactive.

Copper also is an important cofactor for tumor angiogenesis, the process of growing new blood vessels to feed the tumor. Researchers believe this is why tetrathiomolybdate has shown promise as an anti-cancer drug. Hope the clinical trials (phase II) of tetrathiomolybdate (as anticancer drug) a success and wide applications of this drug (as amyotrophic lateral sclerosis (ALS), Parkinson's disease, multiple sclerosis and Alzheimer's disease, primary pulmonary hypertension and left ventricular hypertrophy) will help patients to breathe a sigh of relief...

Ref : http://www.northwestern.edu/newscenter/stories/2009/11/crystal.html

Palmitoylethanolamide - a natural body fat as antiinflammatory agent !

About Palmitoylethanolamide : Palmitoylethanolamide, is an endogenous fatty acid amide which has been demonstrated to bind to peroxisome proliferator-activated receptor alpha (PPAR-α) , GPR55 and GPR119. PEA has been shown to have anti-inflammatory and anti-nociceptive properties. PEA is metabolized by fatty acid amide hydrolase (FAAH) and N-acylethanolamine-hydrolyzing acid amidase (NAAA), the latter of which has more specificity towards PEA over other fatty acid amides.

For decades, it has been known that palmitoylethanolamide (PEA), is a potent anti-inflammatory substance that reduces both allergic symptoms and occurrences of rheumatic fever, but researchers understood little about how PEA works. But now Daniele Piomelli, the Louise Turner Arnold (Chair in Neurosciences at UCI), and colleagues found that levels of PEA are tightly regulated by immune system cells. In turn, PEA helps control the activity of these cells, which are called into action to fight infection, disease and injury in the body. In addition, they found that PEA - also present in foods like eggs and peanuts , is deactivated by a protein called N-acylethanolamine-hydrolyzing acid amidase, which is an enzyme that breaks down molecules controlling cell inflammation.

When given to rodents, the compound increased the levels of PEA in their immune cells and reduced the amount of inflammation elicited by an inflammatory substance. Furthermore, when administered to the spinal cords of mice after spinal cord injury, the compound decreased inflammation associated with the trauma and improved the recovery of motor function.

As most of the antiinflammatory drugs available these days have side effects, this drug may be a boon to the sufferers....

Ref : http://today.uci.edu/news/nr_PEA_091116.php

Generating electricity from air flow

A group of researchers at the City College of New York is developing a new way to generate power for planes and automobiles based on materials known as piezoelectrics, which convert the kinetic energy of motion into electricity

Details ..........Generating electricity from air flow

siRNA for pachyonychia congenita treatment...

In continuation of my update on siRNAs, I found this recent development an interesting finding in the field of RNAi class of compounds. Dr. Sancy Leachman and co workers found that siRNA derivative can be a new treatment for pachyonychia congenita, an ultra-rare genetic skin condition caused by mutations in a gene called keratin.

As per the claim by the authors, siRNA, works by preventing the gene with the mutation from being expressed but permitting the healthy keratin genes to function normally. The study marked the first time that the skin of a human subject was treated with this type of drug. Researchers say that in this single patient trial the drug worked, had no serious side effects, and has vast potential because of its ability to specifically and potently target single molecules, making it an option for many other genetic diseases, including cancer.

The patient was treated with siRNA on her right foot and with placebo on the left foot. The callus on the right foot that received the siRNA fell off at the site of injection, but this did not happen on the left foot. Congrats for this remarkable achievement...

Source : http://healthcare.utah.edu/dermatology/about/faculty/sancyleachman.html

Molecule discovered that makes obese people develop diabetes

Molecule discovered that makes obese people develop diabetes

New Drug Application for Tramadol....

About Tramadol :

Tramadol is a centrally acting analgesic, used for treating moderate to severe pain. Tramadol was developed by the German pharmaceutical company Grünenthal GmbH in the late 1970.

Tramadol possesses agonist actions at the μ-opioid receptor and affects reuptake at the noradrenergic and serotonergic systems. Tramadol is a compound with mild and delayed μ-agonist activity.

Tramadol is a synthetic stripped-down analog of Codeine and, as such, is an opioid. The opioid agonistic effect of tramadol and its major metabolite(s) almost exclusively effects the μ-opioid receptor. This characteristic is notable, because even morphine is not exclusive to the μ-receptor, although it manifests the preponderance of its opioid agonistic effects here. Tramadol is used to treat moderate to moderately severe pain and most types of neuralgia, including trigeminal neuralgia.

Recently, Par Pharmaceutical Companies, Inc received FDA approval for the abbreviated New Drug Application for the 100mg and 200mg strengths of tramadol ER.....

Source : http://www.parpharm.com/media/NR_20091116.jsp

Oncolytics Biotech's REOLYSIN combined with paclitaxel and carboplatin well tolerated for advanced cancers

In continuation of my follow up on cisplatin derivatives, I find this article interesting to share with.....

Oncolytics Biotech's REOLYSIN combined with paclitaxel and carboplatin well tolerated for advanced cancers

Green tea prevents the development of hepatic fibrosis in rat model of DMN-induced liver fibrosis

Green tea prevents the development of hepatic fibrosis in rat model of DMN-induced liver fibrosis

Nicardipine Hydrochloride injection is back !

About Nicardipine :

We know that Nicardipine hydrochloride (Cardene) is a medication used to treat high blood pressure and angina. It belongs to the class of calcium channel blockers.

Nicardipine is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders such as chronic stable angina, hypertension, and Raynaud's phenomenon. It is available in oral and intravenous formulations. Its mechanism of action and clinical effects closely resemble those of nifedipine and the other dihydropyridines (amlodipine, felodipine), except that nicardipine is more selective for cerebral and coronary blood vessels. Furthermore, nicardipine does not intrinsically decrease myocardial contractility and may be useful in the management of congestive heart failure. Nicardipine also has a longer half-life than nifedipine. Nicardipine was approved by the FDA in December 1988. The patent for both Cardene and Cardene SR expired in October 1995.

Recently, Caraco Pharmaceutical Laboratories, Ltd. has launched Nicardipine Hydrochloride Injection immediately following Sun Pharma's final approval from the US Food and Drug Administration (FDA).

Nicardipine Hydrochloride Injection is indicated for the short-term treatment of hypertension when oral therapy is not feasible or not desirable. These Nicardipine Hydrochloride Injections are available as 25 mg/10ml single use ampuls containing 2.5 mg/ml of the drug....

Source : http://phx.corporate-ir.net/phoenix.zhtml?c=98920&p=irol-newsArticle_Print&ID=1356898&highlight=

Vardenafil (PDE5 inhibitor) as antiulcer agent?

Vardenafil, (Levitra, Bayer) is a PDE5 inhibitor used for treating impotence (erectile dysfunction). Vardenafil's indications and contra-indications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). Structurally, the difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. Vardenafil's relatively short effective time is comparable to but somewhat longer than sildenafil's.

We know that most of the NSAIDs are associated with ulcerogenecity. Though there are many compounds with different mode of action have been tested (and some of them are being used) to treat the peptic ulcer, compounds with phosphodiesterase 5 inhibitor were not tested before Dr. Karakaya of Zonguldak Karaelmas University-who have reported that Vardenafil can be used to treat the NSAID-induced gastric ulcer. As per the claim by the researchers the activity is dose dependent.

Ref : http://www.wjgnet.com/1007-9327/abstract_en.asp?f=5091&v=15

Spineology's Capture Facet Screw System receives FDA clearance

Spineology's Capture Facet Screw System receives FDA clearance

A potassium channel blocker to restore nerve function in patients with spinal cord injuries..

The experimental compound, 4-aminopyridine-3-methyl hydroxide, has been shown to restore function to damaged axons, slender fibers that extend from nerve cells and transmit electrical impulses in the spinal cord.

The researchers subjected spinal cord tissue to stresses that mimic what happens in a compression injury, which stretches nerves. Then they treated the damaged axons with 4-aminopyridine-3-methyl hydroxide. The same drug is used primarily as a research tool and also to manage symptoms of multiple sclerosis.

The axons of each nerve are sheathed in a thick insulating lipid layer, called myelin, which enables the transmission of signals without short circuiting, much like the insulation surrounding electrical wires. Spinal cord trauma damages the myelin sheath, exposing "fast potassium channels" that are embedded in the axons and are critical for transmitting nerve impulses.

The researchers also discovered that 4-aminopyridine-3-methyl hydroxide is a "potassium channel blocker," using a sophistic laboratory technique called "patch clamp" to measure signal conduction. Findings confirmed that the compound prevents the exposed channels from leaking electrical current and enhances nerve conduction in segments of the damaged spinal cord. The compound could make it possible to sidestep spinal cord damage by enabling axons to transmit signals as though they were still sheathed in myelin.

As per the claim by the researchers, the new compound is about 10 times more potent than 4-aminopyridine, meaning lower doses can be used to reduce the likelihood of serious side effects. Because myelin also is damaged in multiple sclerosis, the same drug might be used to restore nerve function in people stricken with the disease. Hope in the days to come patients suffering from Multiple sclerosis and spinal cord injuries will breathe a sigh of relief...

Ref : J Neurophysiol (November 18, 2009). doi:10.1152/jn.00154.2009.

Antioxidant in the vegetables for treating Cystic Fibrosis.....

I did mention in my earlier blogs, about the importance of eating broccoli and how it helps to prevent cancer and the authors claimed that the key ingredient that is responsible for this activity (claimed by the authors) is sulforaphane.

Now researchers from the University of Pennsylvania, have found an interesting fact that the antioxidant thiocyanate normally existing in the body protects lung cells from injuries caused by accumulations of hydrogen peroxide and hypochlorite, the active ingredient in household bleach. These potentially harmful chemicals are made by the body as a reaction to infection and injury. In addition, thiocyanate also protects cells from hypochlorite produced in reactions involving MPO, an enzyme released from germ-fighting white blood cells during inflammation.

The research team demonstrated that in three additional cell types used to extend their ideas to other inflammation-related conditions - cardiovascular disease, neurodegeneration, and diabetes - thiocyanate at blood concentrations of at least 100 micromolar (micromoles per liter) greatly reduces the toxicity of MPO in cells, including those lining blood vessels. Humans naturally derive thiocyanate from some vegetables and blood levels of thiocyanate in the general population vary from 10 to 140 micromolar.

So without an adequate dietary supply of thiocyanate (from broccoli & Cauliflower), hypochlorite produced by the body during inflammation would cause additional collateral damage to cells, thus worsening inflammatory diseases, and predisposing humans to diseases linked to MPO activity, including atherosclerosis. Thus the authors claim that delivering thiocyanate directly to the digestive and respiratory systems might be a therapy for CF disease.

Ref :
http://www.pnas.org/content/early/2009/11/11/0911412106.full.pdf+html?sid=2078aa5c-20d6-4a74-b98a-2a5ef6df93d4