Estrogen receptor α (ERα) ligand; potent antiestrogen. Metabolite of tamoxifen (Cat. No. 0999). Primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer...
Med-Chemist : "Quintessential Medicinal Chemistry"
Friday, December 13, 2013
Compound in grapes, red wine could help treat multiple types of cancer
In continuation of my update on resveratrol
A recent study by a University of Missouri researcher shows that resveratrol, a compound found in grape skins and red wine, can make certain tumor cells more susceptible to radiation treatment. This research, which studied melanoma cells, follows a previous MU study that found similar results in the treatment of prostate cancer. The next step is for researchers to develop a successful method to deliver the compound to tumor sites and potentially treat many types of cancers.
"Our study investigated how resveratrol and radiotherapy inhibit the survival of melanoma cells," said Michael Nicholl, MD, assistant professor of surgery at the MU School of Medicine and surgical oncologist at Ellis Fischel Cancer Center in Columbia, Mo. "This work expands upon our previous success with resveratrol and radiation in prostate cancer. Because of difficulties involved in delivery of adequate amounts of resveratrol to melanoma tumors, the compound is probably not an effective treatment for advanced melanoma at this time."
The study found that melanoma cells become more susceptible to radiation if they were treated first with resveratrol. The MU researcher found that when the cancer was treated with resveratrol alone, 44 percent of the tumor cells were killed. When the cancer cells were treated with a combination of both resveratrol and radiation, 65 percent of the tumor cells died.
Nicholl said his findings could lead to more research into the cancer-fighting benefits of the naturally occurring compound.
"We've seen glimmers of possibilities, and it seems that resveratrol could potentially be very important in treating a variety of cancers," Nicholl said. "It comes down to how to administer the resveratrol. If we can develop a successful way to deliver the compound to tumor sites, resveratrol could potentially be used to treat many types of cancers. Melanoma is very tricky due to the nature of how the cancer cells travel throughout the body, but we envision resveratrol could be combined with radiation to treat symptomatic metastatic tumors, which can develop in the brain or bone."Ref : http://dx.doi.org/10.1016/j.jss.2013.02.037
Broccoli compound protects rats from lethal radiation....
In continuation of my update on 3,3′-Diindolylmethane...
We know that, 3,3′-Diindolylmethane or DIM is a compound derived from the digestion of indole-3-carbinol, found in cruciferous vegetables such as broccoli, Brussels sprouts, cabbage and kale. The reputation of Brassica vegetables as healthy foods rests in part on the activities of diindolylmethane. Also DIM has the biological properties listed in the chart below....
Now researchers, have found that, DIM compound protected rodents from lethal doses of radiation in recent experiments....
Tuesday, December 10, 2013
Toxicity limits benefits of bevacizumab–erlotinib NSCLC maintenance therapy
Two targeted anticancer drugs used together after first-line chemotherapy for advanced stage non-small-cell lung cancer (NSCLC) improve progression-free survival (PFS), the results of a large, prospective study show.
Median PFS was 4.8 months for patients treated with bevacizumab plus erlotinib versus 3.7 months for those treated with bevacizumab plus placebo (hazard ratio [HR] = 0.71). There was no overall survival (OS) advantage, however, and the two-drug combination was associated with more adverse events than bevacizumab alone, say the study investigators.
Monday, December 9, 2013
A potential new class of fast-acting antidepressant
Scientists from the University of Chicago have discovered that selectively blocking a serotonin receptor subtype induces fast-acting antidepressant effects in mice, indicating a potential new class of therapeutics for depression. The work was published Oct. 29 in Molecular Psychiatry.
Of the subtypes, serotonin 2C receptors stood out. Selectively blocking these receptors in mice significantly reduced depression-like behaviors in only five days, compared to a minimum of two weeks for a control antidepressant medication.
"We observed fast-acting therapeutic effects in multiple behavioral tasks after we administered compounds that selectively block serotonin 2C receptors," said Mark Opal, a graduate student at the University of Chicago and lead author of the paper. "We began our measurements at five days, but we think there's a possibility it could be effective even sooner than that."
Serotonin 2C receptors normally inhibit the release of dopamine, another neurotransmitter commonly associated with mood, from certain neurons. When 2C is blocked, the researchers believe, more dopamine is released into regions of the brain such as the prefrontal cortex. The team also observed the induction of biomarkers that indicate antidepressant action.
This is the first new biological mechanism that has shown the ability to rapidly alleviate symptoms of depression since ketamine and scopolamine, and it potentially represents a much safer alternative. Some current antidepressants on the market already affect serotonin 2C receptors, although not selectively, and Dulawa believes the safety profile is favorable for human use. The team is now investigating compounds suitable for clinical trials.
"One of the primary advantages to our discovery is that this is much more of an innocuous target than others that have been identified," Dulawa said.
Friday, December 6, 2013
Olysio (simeprevir) Approved By FDA To Treat Hepatitis C Virus | MediMoon
We know that, Simeprevir (see structure below, formerly TMC435; trade name Olysio) is a drug for the treatment and cure of hepatitis C. It was developed by Medivir and Johnson & Johnson's pharmaceutical division Janssen Pharmaceutica. In the United States, simeprevir is approved by the Food and Drug Administration for use in combination withpeginterferon-alfa and ribavirin. Simeprevir has been approved in Japan for the treatment of chronic hepatitis C infection, genotype 1
Health Benefits of Ragi | Medindia
Finger millet (Eleusine coracana L.) also known as Ragi in India is one of the important cereals which occupies the highest area under cultivation among the small millets. The state of Karnataka is the largest producer of ragi in India. Ragi is a crop which can withstand severe drought conditions and can be easily grown throughout the year. Nutritionally, when ragi is used as a whole grain, it is higher in protein and minerals in comparison to all other cereals and millets. It is a remarkable source of protein, making it perfect for vegetarian diets.....
Finger millet contains important amino acids viz., isoleucine, leucine, methionine and phenyl alanine which are not present in other starchy meals. It has the highest amount of calcium (344 mg %) and potassium (408 mg %). Ragi is a great source of iron making it beneficial for individuals with low hemoglobin levels.
Millets also contains B vitamins, especially niacin, B6 and folic acid. Some of the health benefits of ragi are attributed to its polyphenol and dietary fiber contents. Due to its high content of polyphenols and dietary fiber ragi exhibits anti-diabetic and antioxidant and antimicrobial properties; it protects against tumors and atherosclerosis (narrowing and hardening of blood vessels). Being low in fat and gluten free, ragi is easy to digest. It is therefore, given as first foods to babies in the form of ragi porridge.
Malted ragi grains are ground and consumed, mixed with milk, boiled water or yogurt. In southern parts of India, it is a recommended food, by doctors, for infants of six months and above because of its high nutritional content. Homemade ragi malt is one of the most popular infant foods till date. Malting characteristics of finger millet are superior to other millets. On malting the vitamin-C is elaborated, phosphorus availability is increased, digestion is easier and amino acids are synthesized. In south India, the malted ragi flour is extensively used in preparation of weaning foods, instant mixes and beverages.
Despite finger millet's rich nutrient profile, low cost and easy availability recent studies indicate its lower consumption in general by urban Indians. Obesity has become a matter of health concern in India. Unhealthy foods have increasingly become a part of the food choices made by youth. Large populations of children in the country are malnourished and are deficient in calcium and protein. The millet ragi then could be the answer to all the above problems relating to nutrient deficiencies. Ragi is truly a wonder cereal grain and should be consciously incorporated in the diets in one way or the other.
Thursday, December 5, 2013
New Drug Shows Early Promise in Treating Parkinson's Psychosis
We know that, Pimavanserin (ACP-103) is a drug developed by Acadia Pharmaceuticals which acts as an inverse agonist on the serotonin receptorsubtype 5-HT2A, with 40x selectivity over 5-HT2C, and no significant affinity or activity at 5-HT2B or dopamine receptors. As of September 3 2009, pimavanserin has not met expectations for Phase III clinical trials for the treatment of Parkinson's disease psychosis, and is in Phase II trials for adjunctive treatment of schizophrenia alongside an antipsychotic medication. It is expected to improve the effectiveness and side effect profile of antipsychotics...
Now a study published in the Nov. 1 online issue of The Lancet and funded by Acadia Pharmaceuticals, the makers of pimavanserin.
"There are no first-line approved treatments for psychosis in people with Parkinson's disease," said lead researcher Dr. Clive Ballard, a professor of age-related diseases at King's College, London.
"Existing antipsychotics are either ineffective or not tolerated. Pimavanserin is not yet licensed, but could potentially offer a change in the treatment of these distressing and impactful symptoms," he said.
An expert not involved with the study talked about the need for a medication alternative.
"The Parkinson's disease community has been waiting for a potentially new approach for the treatment of psychosis and hallucinations," said Dr. Michael Okun, national medical director of the National Parkinson Foundation.
Wednesday, December 4, 2013
Researchers identify potential way to combat TB
Researchers have identified a potential way to manipulate the immune system to improve its ability to fight off tuberculosis (TB).
TB is a major problem for both humans and cattle and the new findings could help scientists to create better drugs to combat the disease in both.
The disease is caused by the bacterium Mycobacterium tuberculosis, which infects the lungs. The mycobacteria are able to establish persistent TB infections by taking up residence in macrophages - cells of the immune system that would normally destroy invading microorganisms.
Now, in early stage research published in the Journal of Biological Chemistry, researchers from Imperial College London and Stanford University have revealed precisely how unusual sugars on the surface of the mycobacteria that cause TB are able to latch onto the macrophages and disarm them. They now hope that scientists at Imperial and elsewhere can use this knowledge to develop small molecule drugs that latch tightly onto the same site.
These drugs could potentially fight tuberculosis in a number of ways, say the researchers. They could create a barrier to prevent the mycobacteria from attaching to the macrophages; they could transport drugs to kill the mycobacteria; or they could change how the macrophages behave, so that they destroy the mycobacteria rather than harbouring them.
Professor Kurt Drickamer, a lead author of the research from the Department of Life Sciences at Imperial College London, said: "TB is hard to fight effectively because it can hide inside the cells of the immune system that should be able to destroy it. We were surprised to find that there is an extensive interaction between the macrophage and one particular type of molecule on the surface of the mycobacteria. The nature of the interaction gives us hope that we can make simple molecules that block the ability of the mycobacteria to subvert the macrophages.
Tuesday, December 3, 2013
New drug cuts risk of deadly transplant side effect in half
The study, the first to test this treatment in people, combined the drug vorinostat (see structure) with standard medications given after transplant, resulting in 22 percent of patients developing graft-vs.-host disease compared to 42 percent of patients who typically develop this condition with standard medications alone. Results of the study appear in The Lancet Oncology.
"Graft-vs.-host disease is the most serious complication from transplant that limits our ability to offer it more broadly. Current prevention strategies have remained mostly unchanged over the past 20 years. This study has us cautiously excited that there may be a potential new way to prevent this condition," says lead study author Sung Choi, M.D., assistant professor of pediatrics at the U-M Medical School.
Vorinostat is currently approved by the U.S. Food and Drug Administration to treat certain types of cancer. But U-M researchers, led by senior study author Pavan Reddy, M.D., found in laboratory studies that the drug had anti-inflammatory effects as well -- which they hypothesized could be useful in preventing graft-vs.-host disease, or GVHD, a condition in which the new donor cells begin attacking other cells in the patient's body.
The study enrolled 61 older adults from the University of Michigan and Washington University in St. Louis who were undergoing a reduced-intensity bone marrow transplant with cells donated from a relative. Patients received standard medication used after a transplant to prevent GVHD. They also received vorinostat, which is given as a pill taken orally. Fifty of the 61 participants completed the full 21-day course of vorinostat.
Plant Sterols prove to be better cholesterol in Alzheimer`s disease
"Plant sterols are present in various combinations in nuts, seeds and plant oils. As plant sterols are the equivalents of animal cholesterol, they can in principal influence metabolic processes, where cholesterol is involved," explained Marcus Grimm, Head of the Experimental Neurology Laboratory at Saarland University. "Because they also lower cholesterol levels, they are extensively used in the food industry and as dietary supplements."
High cholesterol levels have long been discussed to increase the risk of developing Alzheimer's disease. "Studies have already shown that cholesterol promotes the formation of so-called senile plaques," said Grimm. These plaques, which are composed of proteins, particularly beta-amyloid proteins, deposit at nerve cells within the brain and are regarded as one of the main causes of Alzheimer's disease.
The research team based at Saarland University's medical campus in Homburg collaborated with scientists from Bonn, Finland and the Netherlands to examine how the sterols that we ingest influence the formation of these plaque proteins. It was found that one sterol in particular, stigmasterol, actually inhibited protein formation. "Stigmasterol has an effect on a variety of molecular processes: it lowers enzyme activity, it inhibits the formation of proteins implicated in the development of Alzheimer's disease, and it alters the structure of the cell membrane," explained Dr Grimm. "Together, these effects synergistically reduce the production of beta-amyloid proteins." The research team has been able to confirm the positive effect of stigmasterol in tests on animals.
Overall, the researchers were able to demonstrate that the various plant sterols influence different cellular mechanisms and therefore have to be assessed individually. "Particularly in the case of Alzheimer's disease, it seems expedient to focus on the dietary intake of specific plant sterols rather than a mixture of sterols," explained Dr Grimm. In future studies, the research team wants to determine which other cellular processes in the brain are affected by phytosterols.
Monday, December 2, 2013
Research brings hope of new treatment for asthma patients resistant to corticosteroids
New research from Japan brings hope of a new treatment for asthma patients resistant to corticosteroids. In a study published today in the journal Nature Communications, researchers from the RIKEN Center for Integrative Medical Sciences and Keio University in Japan report that a type of lymphocytes called natural helper (NH) cells plays a critical role in corticosteroid resistance and demonstrate that the anti-psychotic drug Pimozide can be used to overcome resistance to steroids in severe asthma patients.
Friday, November 29, 2013
Cinnamon May Help Ease Common Cause of Infertility, Study Says...
A small study by researchers from Columbia University Medical Center in New York City found that women with polycystic ovary syndrome who took inexpensive daily cinnamon supplements experienced nearly twice the menstrual cycles over a six-month period as women with the syndrome given an inactive placebo. Two of the women in the treated group reported spontaneous pregnancies during the trial.
"There is a lot of interest in homeopathic or natural remedies for this condition," said study author Dr. Daniel Kort, a postdoctoral fellow in reproductive endocrinology at the medical center. "This may be something we can do using a totally natural substance that can help a large group of patients."
The study was scheduled for presentation Wednesday at a meeting of the International Federation of Fertility Societies and American Society for Reproductive Medicine in Boston.
An estimated 5 percent to 10 percent of women of childbearing age have polycystic ovary syndrome, with up to 5 million Americans affected. Polycystic ovary syndrome, which involves many of the body's systems, is thought to be caused by insensitivity to the hormone insulin. Typical symptoms include menstrual irregularity, infertility, acne, excess hair growth on the face or body, and thinning scalp hair.
Treatment for polycystic ovary syndrome currently includes weight loss, ovulation-inducing drugs such as clomiphene (brand name Clomid) and diabetes medications such as metformin, said Dr. Avner Hershlag, chief of the Center for Human Reproduction at North Shore University Hospital in Manhasset, N.Y.
Kort said that it's not yet clear exactly why cinnamon may work to regulate menstrual cycles in those with polycystic ovary syndrome, but it may improve the body's ability to process glucose and insulin. Prior research among diabetic patients suggested the spice can reduce insulin resistance.
Of the 16 patients who completed Kort's trial, 11 were given daily 1,500-milligram cinnamon supplements and five were given placebo pills. Diet and activity levels were monitored, and patients completed monthly menstrual calendars.
After six months, women receiving cinnamon had significant improvement in menstrual cycle regularity, having an average of nearly four menstrual periods over that time compared to an average of 2.2 periods among the placebo group. Two women reported spontaneous pregnancies after three months of cinnamon treatment, meaning they became pregnant without additional help.
Polycystic ovary syndrome "is one of the most common causes why women don't have regular menstrual cycles," Kort said. "But the clinical consequences later in life are truly great from an increased risk of diabetes and glucose intolerance to endometrial cancer. Many women can go their whole lives without regular menstrual cycles, and it doesn't necessarily bother them until they want to have children."
The 1,500-milligram cinnamon dose was chosen for this trial because it was between the 1,000 to 2,000 mg daily that seemed to have metabolic effects on diabetic patients in earlier research, Kort said. But all doses in that range are cheaply obtained, costing pennies per capsule.
"Compared to most medical therapies these days, the cost is very small," he said.
Although the study suggests a link between cinnamon and improvement of polycystic ovary syndrome, it doesn't establish a direct cause-and-effect relationship.
Still, Hershlag called the study "welcome and interesting" and said he sees no reason women with polycystic ovary syndrome shouldn't use more cinnamon in their food or take cinnamon supplements.
"Any work that's something nutritional in nature and seems to affect the abnormal physiology of polycystic ovaries is welcome," Hershlag said. "If they want to spice up their life and take it, that's fine , but I think the best thing to do when you have polycystic ovaries is to be under the control of a physician."
Wednesday, November 27, 2013
Bacteria-eating viruses 'magic bullets in the war on superbugs'
Dr Martha Clokie, from the University of Leicester's Department of Infection, Immunity and Inflammation has been investigating an alternative approach to antibiotics, which utilizes naturally occurring viruses called bacteriophages, meaning 'eaters of bacteria'.
The work has predominantly been funded by the Medical Research Council (MRC).
Dr Clokie said: "Ever since the discovery of the first antibiotic, penicillin, antibiotics have been heralded as the 'silver bullets' of medicine. They have saved countless lives and impacted on the well-being of humanity.
"But less than a century following their discovery, the future impact of antibiotics is dwindling at a pace that no one anticipated, with more and more bacteria out-smarting and 'out-evolving' these miracle drugs. This has re-energised the search for new treatments.
"One alternative to antibiotics is bacteriophages, known as phages, which unlike antibiotics, are specific in what they kill and will generally only infect one particular species, or even strain, of bacteria -- referred to as the 'host'. Following attachment to their hosts, they inject their DNA into the bacterium, which then replicates many times over, ultimately causing the bacterial cell to burst open. The phages released from the dead bacterium can then infect other host cells."
Dr. Clokie and her team have achieved the remarkable feat of isolating and characterising the largest known set of distinct C. diff phages that infect clinically relevant strains of C. diff. Of these, a specific mixture of phages have been proved, through extensive laboratory testing, to be effective against 90% of the most clinically relevant C. diff strains currently seen in the U.K.
As a testament to their therapeutic potential, these phages, that are the subject of a patent application, have been licensed by AmpliPhi Biosciences Corporation -- a US-based biopharmaceutical company and pioneers in developing phage-based therapeutics. AmpliPhi have already made progress in developing phages targeted against Pseudomonas aeruginosa, a pathogen that causes acute, life-threatening lung infections in cystic fibrosis patients. They were also the first biopharmaceutical company to demonstrate the effectiveness ofPseudomonas phages in controlled and regulated human clinical trials.
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Painkillers May Worsen Headaches Following Concussion
The researchers found that daily headache, female sex, the presence of nausea, throbbing headache versus steady or stabbing pain, irritability following concussion, and a relatively longer interval between the concussive event and neurological evaluation were more common in the 54 patients with probable medication-overuse headache than in the 23 without. Within two months of stopping analgesics, 37 of the 54 in the probable group had improvement in symptoms, i.e., complete resolution or reversion to preconcussion levels of the headache. The study was presented as a poster session at the Child Neurology Society (CNS) annual meeting, held during October-November 2013 in Austin.
“Continued use of analgesics for headache despite lack of efficacy can cause chronification of a headache syndrome. Because withdrawal of painkillers alleviated these patients' headaches, a diagnosis of medication-overuse headache may be made,” concluded study authors Geoffrey Heyer, MD, and Syed Idris, MD. “Management of patients with prolonged postconcussion headache should include analgesic detoxification when medication overuse is suspected.”
“Continued use of analgesics for headache despite lack of efficacy can cause chronification of a headache syndrome. Because withdrawal of painkillers alleviated these patients' headaches, a diagnosis of medication-overuse headache may be made,” concluded study authors Geoffrey Heyer, MD, and Syed Idris, MD. “Management of patients with prolonged postconcussion headache should include analgesic detoxification when medication overuse is suspected.”
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