Arena Pharmaceuticals and Eisai Announce FDA Approval of BELVIQ® (lorcaserin HCl) for Chronic Weight Management in Adults who are Overweight with a Comorbidity or Obese (NASDAQ:ARNA)

In continuation of my update on lorcaserin

Arena Pharmaceuticals and Eisai Announce FDA Approval of BELVIQ® (lorcaserin HCl) for Chronic Weight Management in Adults who are Overweight with a Comorbidity or Obese (NASDAQ:ARNA)

Nicotinamide riboside can protect against obesity

A natural ingredient found in milk can protect against obesity even as mice continue to enjoy diets that are high in fat. 

The researchers identified this ingredient, known as nicotinamide riboside (see structure), as they were searching for alternative ways to boost the well-known gene SIRT1, which comes with benefits for both metabolism and longevity. One way to do that is to target SIRT1 directly, as the red wine ingredient resveratrol appears to do, at least at some doses.

Auwerx's team lead by Johan Auwerx, suspected there might be a simpler way to go about it, by boosting levels of one of SIRT1's molecular sidekicks, the cofactor NAD+. 

This milk ingredient does just that in a rather appealing way. Not only is it a natural product, but it also gets trapped within cells, where it can do its magic.

Mice that take nicotinamide riboside in fairly high doses along with their high-fat meals burn more fat and are protected from obesity. They also become better runners thanks to muscles that have greater endurance.

http://www.youtube.com/embed/5YwzyqXzntY

Nicotinamide riboside can protect against obesity

Black pepper compound fights fat

We know the that, black pepper has many medicinal benefits, like  curing illness such as constipation, diarrhea, earache, gangrene, heart disease, hernia, hoarseness, indigestion, insect bites, insomnia, joint pain, liver problems, lung disease, oral abscesses, sunburn, tooth decay, and toothaches. Now Korean researchers report that piperine (see structure below), a pungent compound found in black pepper (Piper nigrum), helps block the formation of new fat cells, a process known as adipogenesis.

"Adipogenesis is a well-organized process regulated by adipogenic transcription factors, such as peroxisome proliferator-activated receptor-gamma (PPAR-gamma), sterol regulatory element binding protein (SREBP) family, and CCAAT-enhancer binding protein (C/EBP) family," the authors write in their introduction. "Of these factors, PPAR-gamma has been focused on its role in adipocyte differentiation. In addition to being induced during adipogenesis, it is both necessary and sufficient for the process."

In addition to other benefits such as enhancing nutrient absorption in the digestive tract, black pepper has been found to reduce blood glucose and lipids. In the current study, Soo-Jong Um, Ji-Cheon Jeong and colleagues tested the effects of black pepper extract and piperine on cultured preadipocytes and found that both inhibited the cells differentiation into mature fat cells. Expression of the genes for PPAR-gamma, SREBP-1c and C/EBP-beta were all found to be decreased, as was the binding of PPAR-gamma to a coactivator known as CREB-binding protein following the administration of either treatment. Piperine was also shown to repress LXR-alpha, another transcriptional factor that is involved in the induction of adipogenesis as well as the synthesis of cholesterol and fatty acids.

"Taken together, our findings suggest that piperine, a major component of black pepper, inhibits fat cell differentiation by down-regulating the transcriptional activity of PPAR-gamma (and LXR-alpha) and suppressing the expression of PPAR-gamma (and LXR-alpha), thus leading to its potential use in the treatment of obesity-related diseases," the authors conclude.

Ref : http://pubs.acs.org/doi/abs/10.1021/jf204514a?prevSearch=%255BContrib%253A%2BSoo-Jong%2BUm%255D&searchHistoryKey=

Grape compound may block the formation of fat cells

Purdue University researchers have come up with the ability of a compound known as piceatannol (see structure)  to help prevent the formation of mature fat cells by blocking the pathways needed for their growth. Piceatannol is an analog of resveratrol, found in grapes and other fruit, which is converted to piceatannol in humans following its consumption.

Purdue assistant professor of food science Kee-Hong Kim and his associates tested piceatannol in cultured preadipocytes, which are immature fat cells. These cells pass through several stages before reaching maturity over a ten day or longer period. "These precursor cells, even though they have not accumulated lipids, have the potential to become fat cells," Dr Kim explained. "We consider that adipogenesis is an important molecular target to delay or prevent fat cell accumulation and, hopefully, body fat mass gain."

Dr Kim's team found that piceatannol bound to the preadipocytes' insulin receptors during their initial stage of fat cell formation, which blocked insulin's ability to control cell cycles and activate genes necessary for the further stages of adipogenesis. "Piceatannol actually alters the timing of gene expressions, gene functions and insulin action during adipogenesis, the process in which early stage fat cells become mature fat cells," Dr Kim stated. "In the presence of piceatannol, you can see delay or complete inhibition of adipogenesis."

"Our study reveals an antiadipogenic function of piceatannol and highlights insulin receptor and its downstream insulin signaling as novel targets for piceatannol in the early phase of adipogenesis," the authors conclude.

Dr Kim hopes to test piceatannol in an animal model as well as find a way to prevent the compound from degrading so that enough is available to the body to prevent fat gain. "We need to work on improving the stability and solubility of piceatannol to create a biological effect," he added.

Ref : http://www.jbc.org/content/287/14/11566.abstract?sid=48fa8a22-7a4d-4561-9585-80d643245a89

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

In continuation of my update on the benefits of nuts...

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

FDA approves Lannett's Diethylproprion HCl Tablets ANDA for anti-obesity treatment

FDA approves Lannett's Diethylproprion HCl Tablets ANDA for anti-obesity treatment

Formoterol drug improves fat burning and protein metabolism in men

We know that, Formoterol  or eformoterol  is a long-acting β₂-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD). It is marketed in four forms: a dry-powder inhaler (DPI), a metered-dose inhaler (MDI), an oral tablet, and an inhalation solution, under various trade names including Foradil/Foradile (Schering-Plough in the U.S., Novartis rest of world), Oxeze (AstraZeneca), Atock (Astellas), Atimos Modulite (Trinity-Chiesi), and Perforomist (Dey).

Now researchers lead by Dr. Paul Lee of  Garvan Institute of Medical Research in Sydney, have for the first time reports that research in animals has shown that formoterol can stimulate the growth of muscle and the burning of fat...

Formoterol drug improves fat burning and protein metabolism in men

Study finds anti-obesity drug reduces brain’s response to appetizing foods

Sibutramine (usually in the form of the hydrochloride monohydrate salt) is an oral anorexiant. Until recently it was marketed and prescribed as an adjunct in the treatment of exogenous obesity along with diet and exercise. It has been associated with increased cardiovascular events and strokes and has been withdrawn from the market in the US, EU, AU etc. 

Sibutramine is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines, although its mechanism of action is distinct.

Now, researchers lead by Prof. Paul Fletcher at the University of Cambridge discovered that the anti-obesity drug sibutramine reduced brain responses in two regions of the brain, the hypothalamus and the amygdala, both of which are known to be important in appetite control and eating behavior.

Using functional magnetic resonance imaging (fMRI), the researchers measured brain activity while obese volunteers viewed pictures of appetising high-calorie foods - like chocolate cake - or pictures of low-calorie foods - like broccoli. The brain scanning was carried out both after two weeks of treatment with the anti-obesity drug, sibutramine (see structure above), and two weeks of placebo treatment. 

On placebo, it was shown that simply seeing pictures of appetising foods caused greater activation of many regions of the brain that are known to be important for reward processing. On sibutramine, however, they found that the anti-obesity drug reduced brain responses to the appetising foods in two regions of the volunteers' brain - the hypothalamus and the amygdala. These two regions are known to be important in appetite control and eating behaviour. Additionally, people who had the greatest reduction of brain activation following drug treatment tended to eat less and to lose more weight.

I quote....

"The most exciting aspect of these results is that they help us to see that brain and behaviour are fundamental to understanding and treating obesity. Simply because obesity involves major changes in body weight and body composition, it is easy to imagine that it is entirely 'a body problem'. These results remind us that the major cause of obesity in the West is over-eating, and this behaviour is regulated by reward and satiety processing circuits in the brain." 

Ref : Paul C. Fletcher et. al., The Journal of Neuroscience, October 27, 2010