Showing posts with label Obesity. Show all posts
Showing posts with label Obesity. Show all posts

Wednesday, January 28, 2015

Scientists zero in on obesity pill 'that could replace the treadmill'

Scientists at Harvard University have created a way of screening potential drugs that turn white fat cells – which are "bad" – into the brown fat cells that are healthier. They have already identified two compounds that work on human cells growing in the laboratory.

Researchers believe it may be possible to lower the levels of white fat, which is linked with diabetes and heart disease, by increasing the proportion of brown fat, which burns off excess energy. It could lead to a “pill that can replace the treadmill” for the control of obesity, they said.
Meanwhile, Imperial College researchers in London have identified an enzyme that drives the craving for sugar in the brain’s hypothalamus, which regulates food intake. The scientists believe the enzyme, called glucokinase, could be a viable target for an anti-obesity drug.

“This is the first time anyone has discovered a system in the brain that responds to a specific nutrient, rather than energy intake in general. It suggests that when you’re thinking about diet, you have to think about different nutrients, not just count calories,” said James Gardiner of Imperial College, who led the study published in the Journal of Clinical Investigation.

Tests on rats showed that boosting the activity of the enzyme within the brain caused the animals to consume more glucose in preference to normal food. A drug targeting glucokinase or its metabolic pathway could potentially prevent obesity by lowering the desire for sugary foods, the scientists suggest.

Wednesday, March 6, 2013

Grape seed and skin extract: A weapon in the fight against kidney disease caused by high-fat diets

Researchers examined the effect of GSSE processed from a grape cultivar ('Carignan') of Vitis vinifera from northern Tunisia on rats. Rats were fed a high-fat diet that induced a low-grade reno-lipotoxicity, that is, kidney damage associated with lipids. This was characterized by elevations in plasma urea and protein in the urine. The researchers found increased deposits of triglycerides (TG) (especially saturated fatty acids), increased signs of oxidative stress and depleted copper levels in the kidneys. There was also histological evidence of disturbance in the kidney structure. When the animals received GSSE at 500 mg/kg bw (which corresponds to 35g/day for a 70 kg human adult) along with the high-fat diet there was a partial reversal of the TG deposition as well as the histological damage. The authors suggest polyphenols including resveratrol are likely the components in GSSE responsible for the positive effects. Furthermore the GSSE prevented the oxidative stress and copper depletion.

"In our research, obesity-induced leaky kidney and proteinuria are shown to be prevented by GSSE, which suggests the use of GSSE as a preventive nutriceutical for high-risk patients," said co-author Kamel Charradi, a researcher with the Laboratory of Bioactive Substance at the Center of Biotechnology of Borj-Cedria (CBBC) in Tunisia. This research group has previously published work showing the benefits of GSSE in combating obesity, heart dysfunction, brain lipotoxicity and kidney cancer.....

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Tuesday, January 22, 2013

Researchers identify potential sources of medicines derived from plants against diabetes

A group of researchers from the university's School of Science, led by Dr Solomon Habtemariam, believe they have identified potential sources of medicines derived from plants which may have fewer adverse side-effects for diabetes sufferers.

The scientists are investigating the properties of two plants found in south-east Asia which they think could have properties that are not only anti-diabetic, but also lipid- or fat-lowering, and so can help tackle obesity. The researchers at Greenwich aim to isolate and identify certain extracts from the plants Cassia auriculata and Cassia alata, which could have 'active ingredients' for treating diabetes. They discovered that one of the compounds isolated from the plant, kaempferol 3-O-rutinoside, (structure below)  has proved to be more than eight times more potent than the standard anti-diabetic drug, acarbose.  

The team also found the plants have anti-oxidant properties, which is beneficial when treating diabetes.

"Our other most interesting finding is that many of the active ingredients from the Cassia auriculata plant work through a process called 'synergism' - in other words, they work together to produce an effect greater than the sum of their individual effects," Dr Habtemariam says. "Overall, this suggests that the crude plant extract has lots of potential to be used clinically for treating diabetes and associated diseases."

The researchers adds that the research  is ongoing and requires further study and validation, in my opinion it is interesting...

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Friday, January 4, 2013

Drug May Help Women Who Quit Smoking Avoid Weight Gain - MedNews

In continuation of my update on Naltrexone

We know that, Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. It is marketed in generic form as its hydrochloridesalt, naltrexone hydrochloride, and marketed under the trade names Revia andDepade. In some countries including the United States, a once-monthly extended-release injectable formulation is marketed under the trade name Vivitrol. Also in the US, Methylnaltrexone Bromide, a closely related drug, is marketed as Relistor, for the treatment of opioid induced constipation.

Naltrexone should not be confused with naloxone (which is used in emergency cases of overdose rather than for longer-term dependence control) nor nalorphine. Using naloxone in place of naltrexone can cause far worse withdrawal symptoms; conversely, using naltrexone in place of naloxone in an overdose can lead to insufficient opiate antagonism and fail to reverse the overdose.

Wednesday, September 5, 2012

Green coffee beans show potential for losing weight..

In  a  study  presented,  at  the  American  Chemical  Society’s  spring     national meeting in San Diego, 16 over weight young adults took, by turns, a low dose of green coffee bean extract, a high  dose  of  the supplement, and a placebo. Though the study was small, the results were striking: Subjects lost an average of 17.5 pounds in 22 weeks and reduced their overall body weight by 10.5%.If green coffee extract were a medication seeking approval from the Food and Drug Administration, these results would make it a viable candidate — more than 35% of subjects lost more than 5% of their body weight, and weight loss appeared to be greater while subjects were taking the pills than when they were on the placebo.

Joe Vinson, the University of Scranton chemist who conducted the pilot study, said the findings should pave the way for more rigorous research on coffee bean extract’s effects. A larger trial involving 60 people is being planned.Vinson, whose research focuses on plant polyphenols and their effects on human health, said it appears that green coffee bean extract may work by reducing the absorption of fat and glucose in the gut; it may also reduce insulin levels, which would improve metabolic function. There were no signs of ill effects on any subjects, Vinson reported.

The study used a “cross-over” design, which allowed each subject to serve as his or her own comparison group. For six weeks, volunteers swallowed capsules three times a day, ingesting either 700 or 1,050 milligrams of green coffee extract a day or taking a placebo. After a two-week break, they moved, round-robin style, to another arm of the trial.Subjects did not change their calorie intake over the course of the trial. But the more extract they consumed, the more weight and fat they lost. Altogether, they reduced their body fat by 16%, on average.Of the 16 volunteers, six wound up with a body mass index in the healthful range.One downside is that the extract is “extremely bitter.” It would be difficult to take without a lot of water, Vinson reported.....

Ref : Detailed article read at

I found the following link more informative...

Sunday, August 19, 2012

Zafgen announces new data from two Phase 1 studies of beloranib on obesity

Zafgen announces new data from two Phase 1 studies of beloranib on obesity: Zafgen, Inc., the world's first biopharmaceutical company dedicated to addressing the unmet need of severely obese patients, today announced new data from two Phase 1 studies of beloranib, a selective methionine aminopeptidase 2 inhibitor (MetAP2), which showed significant weight loss and improvements in cardiometabolic risk markers in severely obese women.

Treatment with beloranib (see structure) was associated with improvements in weight loss and triglycerides, LDL cholesterol, waist circumference and diastolic blood pressure, with no evidence of major tolerability or safety issues.  Body composition measured in one study indicated a reduction in fat mass with beloranib.  

Tuesday, June 5, 2012

Lorcaserin Receives Positive Vote From FDA Advisory Committee

In continuation of my update on Lorcaserin

(FDA) Endocrinologic and Metabolic Drugs Advisory Committee voted 18 to 4, with one abstention, that the available data demonstrate that the potential benefits of lorcaserin outweigh the potential risks when used long-term in a population of overweight and obese individuals. Lorcaserin is an investigational drug candidate intended for weight management, including weight loss and maintenance of weight loss, in patients who are obese (BMI greater than or equal to 30) or patients who are overweight (BMI greater than or equal to 27) and have at least one weight-related co-morbid condition.
"The advisory committee's positive vote supports our belief in lorcaserin as a potential new treatment option for the medical management of overweight and obesity," said Jack Lief, Arena's President and Chief Executive Officer. "We will continue to work with the FDA as the agency completes its review of the lorcaserin new drug application."

Tuesday, May 1, 2012

New drug to tackle body fat problems

Leptin regulates energy homeostasis, fertility, and the immune system, making it an important drug target. However, due to a complete lack of structural data for the obesity receptor (ObR), leptin's mechanism of receptor activation remains poorly understood. Researchers have crystallized the Fab fragment of a leptin-blocking monoclonal antibody (9F8), both in its uncomplexed state and bound to the leptin-binding domain (LBD) of human ObR. They describe the structure of the LBD-9F8 Fab complex and the conformational changes in 9F8 associated with LBD binding. A molecular model of the putative leptin-LBD complex reveals that 9F8 Fab blocks leptin binding through only a small (10%) overlap in their binding sites, and that leptin binding is likely to involve an induced fit mechanism. This crystal structure of the leptin-binding domain of the obesity receptor will facilitate the design of therapeutics to modulate leptin signaling.
New drug to tackle body fat problems

Friday, April 13, 2012

Weight loss pill Qnexa wins panel vote and awaits approval

We know that, The combination of the drugs phentermine (see structure-1) and topiramate (structure -2) (trade name Qnexa) is an investigational medication for the treatment ofobesity and related conditions such as type 2 diabetes and has been found to lower blood pressure and cholesterol.  Qnexa is being developed by Vivus, a California pharmaceutical company.  Phentermine is an appetite suppressant and stimulant of the amphetamine andphenethylamine class. Topiramate is an anticonvulsant that has weight loss side effects.

Structure 1
Weight loss pill Qnexa wins panel vote and awaits approval: The drug was rejected in a 10-6 vote the first time it came before a Food and Drug Administration (FDA) advisory panel, in 2010, due to safety concerns. However when the medication returned for another review in February, the advisory committee gave it near-unanimous approval (20-2). Because the FDA often follows the advisory panel's advice, Qnexa is likely to get FDA approval, probably by mid-April.

Tuesday, November 9, 2010

Chillies for diabetes: Study

In continuation of my update on diabetes and its treatment,  I find the following study interesting.  In fact, I had a blog article  , where in the authors claim that Capsaicin may cause weight loss and I think these findings are of great significance........


Wednesday, August 4, 2010

Scientists develop obesity drug without neurological side effects....

We know the side effects of Rimonabant, (see structure) the first selective CB1 receptor blocker to be approved for use anywhere in the world. In Europe, it was indicated for use in conjunction with diet and exercise for patients with a body mass index greater than 30 kg/m², or patients with a BMI greater than 27 kg/m² with associated risk factors, such as type 2 diabetes or dyslipidaemia. In the UK, it was available beginning in July 2006. As of 2008, the drug was available in 56 countries. On October 23, 2008, the European Medicines Agency (EMEA) issued a press release stating that its Committee for Medical Products for Human Use (CHMP) had concluded that the benefits of Acomplia no longer outweighed its risks and subsequently recommended that the product be suspended from the UK market. Sanofi-Aventis later released a press statement stating that the drug had been suspended. Approval of the drug was officially withdrawn by the EMEA on January 16, 2009. But never approved for use in the US because of serious neurological side effects including depression and anxiety.

Now researchers from National Institutes of Health, Bethesda, and Alexandros Makriyannis, at Northeastern University, Boston lead by Dr. George Kunos, have developed a drug (see structure AM6545)  that has the same positive effects in mice on levels of glucose and fats in the blood as rimonabant but none of the neurological side effects.

As per researchers claim AM6545 is a non-brain-penetrant neutral CB1R antagonist. First-generationCB1R antagonists, such as rimonabant, are highly lipid soluble and readily penetrate the blood-brain barrier. In order to reduce brain penetrance, we introduced several modifications into the structure of rimonabant. AM6545 is less lipid soluble than rimonabant (estimated partition coefficient [log P], 3.3 vs. 6.4 for rimonabant) but retains high affinity and selectivity for CB1R. In radioligand displacement assays, AM6545 has a KI of 3.3 nM for CB1R, which is similar to that of rimonabant and greater than 100-fold CB1/CB2 selectivity. Unlike rimonabant, AM6545 does not reduce GTPγS binding in mouse brain membranes and is therefore a neutral antagonist.

As per the claim by the researchers, this drug did not cause weight loss or neurological side effects, which rimonabant does, but did have effects on levels of glucose and fats in the blood that should reduce the risk of the serious health consequences of obesity.

The authors therefore hope that this approach of targeting only peripheral CB1R can be translated into the clinic to reduce health risks in obese patients..

Monday, August 2, 2010

Phenolic compounds (chlorogenic & neo-chlorogenic acids) in peaches, plums kill breast cancer cells..

We know that Peaches and plums are both high in Potassium, Phosphorus, Magnesium, Calcium, and Vitamins A, C, Niacin, and Folate and antioxidant rich. A recent study performed at Texas A&M University revealed that peaches and plums may present an even sweeter, juicier treat in their ability to fight breast cancer. According to research scientists Dr. Luis Cisneros-Zevallos and Dr. David Byrne from AgriLife Research at Texas A&M, extracts found in commercial varieties of peaches and plums have been to kill breast cancer cells while not harming normal cells.
The AgriLife research scientists identified two phenolic compounds (slightly acidic and may be associated with traits such as aroma, taste or color)  within the Rich Lady peach and Black Splendor (commercial varieties) plum that are responsible for killing the cancer cells. Phenols are organic compounds that occur in fruits and may affect traits such as aroma, taste or color. Stone fruits such as peaches and plums have especially high levels of phenols.

Byrne and Dr. Luis Cisneros-Zevallos originally studied the antioxidants and phytonutrients in plums and found them to match or exceed the blueberry which had been considered superior to other fruits in those categories.
"These extracts killed the cancer cells but not the normal cells," Cisneros-Zevallos said...

As per the claim by the researchers,  two specific phenolic acid components - chlorogenic and neochlorogenic ( structures, source :ChemBlink) - were responsible for killing the cancer cells while not affecting the normal cells. Researchers add that the two compounds are very common in fruits, the researchers said, but the stone fruits such as plums and peaches have especially high levels. The team said laboratory tests also confirmed that the compounds prevented cancer from growing in animals given the compounds.
"So this is very, very attractive from the point of view of being an alternative to typical chemotherapy which kills normal cells along with cancerous ones," Byrne claims..

Researchers conclude that,  phenolic acids present (chlorogenic- left above structure and neo-chlorogenic acids-right below structure)  have potential as chemopreventive dietary compounds because of the relatively high growth inhibition exerted on the estrogen-independent MDA-MB-435 breast cancer cell line and low toxicity exerted in the normal MCF-10A cells.

Dr. Byrne plans to examine more fully the lines of the varieties that were tested to see how these compounds might be incorporated into his research of breeding plums and peaches. Dr.  Cisneros-Zevallos will continue testing these extracts and compounds in different types of cancer and conduct further studies of the molecular mechanisms involved. Hope they come up with substantial results to support their claim....

Tuesday, July 27, 2010

New evidence that chili pepper ingredient fights fat..

In continuation of my update on Capsaicin may cause weight loss....
In an effort to find out, the scientists lead by Jong Won Yun of of Daegu University, Kyungsan, Korea,  fed high-fat diets with or without capsaicin to lab rats used to study obesity. The capsaicin-treated rats lost 8 percent of their body weight and showed changes in levels of at least 20 key proteins found in fat. The altered proteins work to break down fats.

"These changes provide valuable new molecular insights into the mechanism of the antiobesity effects of capsaicin the scientists say"...

Through secretion of adipokines into the blood, adipose tissue plays a central role in development of these syndromes. In particular, white adipose tissue (WAT) functions as an energy storage organ through formation of triacylglycerol and release of fatty acids into the bloodstream during a shortage of energy. In association with overnutrition, excess WAT play a major role in obesity and obesity-related disorders through dysregulation of adipokine secretion from WAT. Therefore, inhibition of excess WAT can be an efficient strategy for prevention of obesity and metabolic disorders.

Researchers concludes that, thermogenesis and lipid metabolism related proteins were markedly altered upon capsaicin treatment in WAT, suggesting that capsaicin may be a useful phytochemical for attenuation of obesity....

Tuesday, June 8, 2010

FDA accepts Orexigen's Contrave NDA for treatment of obesity

Orexigen Therapeutics, Inc., a biopharmaceutical company focused on the treatment of obesity, recently anounced that the U.S. Food and Drug Administration (FDA) has accepted for filing the Company's New Drug Application (NDA) for Contrave(R) (see structrures below ; naltrexone SR   and bupropion SR), its investigational drug for the treatment of obesity. The NDA is based on a substantial body of evidence gathered through the Contrave Obesity Research (COR) clinical program, which included over 4,500 patients.....

"We are pleased the FDA has accepted our NDA for filing and look forward to working with the Agency during the review process," said Michael Narachi, President and CEO of Orexigen. "If approved, we believe Contrave will become an important therapeutic option for obese patients, making weight loss and weight maintenance an achievable cornerstone in the treatment of obesity and its common co-morbidities."

Ref :

Saturday, June 5, 2010

Chili peppers may cause weight loss and fight fat buildup, says study

In one of my earlier blog article, titled "Peppers may increase energy expenditure in people tying to lose weight"....have mentioned that researchers form UCLA's Center for Human Nutrition in Los Angeles, CA, lead by Dr. David Heber claimed that "peppers may increase energy expenditure in people tying to lose weight". 

Now interestingly, Steven C. Powell, has come up with new evidence that capsaicin (see below structure), the stuff that gives chili peppers their kick, may cause weight loss and fight fat buildup by triggering certain beneficial protein changes in the body. Their study, which could lead to new treatments for obesity, appears in ACS' monthly Journal of Proteome Research........details ...

Ref : Chili peppers may cause weight loss and fight fat buildup, says study  

Tuesday, April 27, 2010

Chokeberry extract reduces weight gain in insulin-resistant animals.....

Chokeberries (Aronia) are a great example of those fruits that both  taste good and show a number of health benefits for the body. Chokeberries' rich antioxidant content may be beneficial as a dietary preventative for reducing the risk of diseases caused by oxidative stress. Among the models under evaluation where preliminary results show benefits of chokeberry anthocyanins are colorectal cancer, chronic inflammation, gastric mucosal disorders (peptic ulcer),eye inflammation (uveitis) and liver failure cardiovascular disease.

Now Drs. Bolin Qin and Richard Anderson from the US Department of Agriculture in Beltsville, MD, have come up with some more interesting info about chokeberries, i.e., "chokeberry extract reduces weight gain in insulin-resistant animals". 

Qin and Anderson found that at the end of the study,  the rats consuming the chokeberry-spiked water weighed less than the controls; both levels of chokeberry had the same effect in this regard. Similar beneficial effects of chokeberry consumption were found for body fat (specifically, that of the lower abdominal region). They also discovered that animals that had been drinking chokeberry extract had lower blood glucose and reduced levels of plasma triglycerides, cholesterol, and low-density lipoprotein (LDL) cholesterol when compared to the control animals. These alterations would theoretically lead to lower risk for diabetes and cardiovascular disease in humans.

To add even more evidence for a healthful impact of this super-berry, the researchers documented numerous alterations in expression of genes that would likely lead to reduced chronic inflammation and perhaps even lower cancer risk. For instance, drinking chokeberry extract lowered expression of the gene coding for interleukin-6 (IL-6), a protein that normally triggers inflammation following trauma or infection. Chronic overproduction of IL-6 has been documented in many diseases such as diabetes, arthritis, and atherosclerosis and is thought to be a partial cause of these conditions.

Researchers conclude that though human trials are essential to further substantiate their claim,  they believe their study "provides evidence that the chokeberry extract inhibits weight gain in insulin-resistant animals and that it modulates multiple genes associated with adipose tissue growth, blood glucose regulation, and inflammatory pathways."....

Ref : Bolin Qin and Richard A Anderson, :  Abstract in FASEB, 

(those interested can read other benefits and other details at the link)

Sunday, February 7, 2010

Metformin helps dieting teens to lose weight....

We know that Metformin  (see structure), is a  biguanide hypoglycemic  agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. Metformin's pharmacologic mechanisms of action are different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. In my earlier blogs, I have covered the recent (findings)  updates on metformin.

Now researchers  lead by Dr. Darrell Wilson (from Division of Pediatric Endocrinology and Diabetes, Stanford University)  have found that metformin appears to help overweight teenagers lose weight when combined with a program designed to help them change their lifestyle habits.

As per the claim by the authors though metformin hydrochloride is  used as a primary or adjunctive treatment in obese  nondiabetic adolescents there are limited short-term data to support this therapy  and also it is unclear whether any observed effects of metformin on body mass index. Therefore  the researchers conducted a 48-week randomized, double-blind, placebo-controlled trial of extended-release (XR) metformin therapy in nondiabetic obese adolescents  followed by a 48-week monitoring period after completion of treatment.

Researchers found that the addition of metformin to a lifestyle change intervention for a period of 12 months resulted in a significant improvement of BMI regardless of baseline fasting insulin levels, that persisted for 12 to 24 weeks after cessation of drug treatment. The mean (SE) reduction in BMI of –1.1 (0.5) at 1 year was comparable with that observed in other randomized controlled trials of metformin treatment in obese adolescents, although these randomized controlled trials involved shorter treatment duration (about 6 months), targeted obese children with additional diabetes risks, and had smaller sample sizes.

The mechanisms of action for these effects have not fully been elucidated but may involve beneficial effects on carbohydrate and lipid metabolism, mediated through adenosine monophosphate kinase.

Researchers conclude that  "metformin  in combination with lifestyle modification, had a small but statistically significant effect to reduce BMI in obese adolescents; this effect waned within 12 to 24 weeks of discontinuing metformin treatment". These results indicate that metformin may have an important role in the treatment of adolescent obesity. Longer-term studies will be needed to define the effects of metformin treatment on obesity-related disease risk in this population....

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Friday, January 15, 2010

Phentermine & Topiramate combination (Qnexa®) for obstructive sleep apnea (OSA)....

In continuation of my update on Qnexa® (combination of Phentermine & Topiramate), a drug by VIVUS, Inc., I found this info really interesting  to share with.

VIVUS, Inc on 7. January 201, announced positive results from a phase 2 study evaluating the safety and efficacy of Qnexa®, an investigational drug, for the treatment of obstructive sleep apnea (OSA). VIVUS recently completed phase 3 development of Qnexa for the treatment of obesity and submitted a New Drug Application (NDA) to the FDA for that indication. The OSA- study announced  demonstrated statistically significant improvement in the apnea/hypopnea index ("AHI" - a measure of the severity of sleep apnea) in patients with OSA treated with Qnexa for 28 weeks.

OSA is a sleep-related breathing disorder that involves a decrease or complete halt in airflow despite an ongoing effort to breathe. OSA is associated with an increased risk of hypertension, diabetes, stroke, sudden cardiac death and all-cause mortality. Currently, there are no approved pharmacologic treatments for OSA and current treatment approaches are limited to devices or surgery, so if approved by the FDA, Qnexa®  not only reduce the weight  but also significantly improve sleep apnea.

Ref :