Prototype Nutrition Ketoforce

Sep

17

Breaking new research on ursolic acid shows increases in brown fat production and confirms muscle building potential

By Patrick

The most interesting health and fitness related natural compound to come around within the last decade or so has got to be ursolic acid. I have been aware of its benefits for quite some time but it wasn’t until last year that I really became excited. It was then that a landmark study was released by some University of Iowa researchers showing that ursolic acid blocked the muscle wasting effects of nerve injury and starvation, as well as increased muscle mass in healthy animals while simultaneously reducing body fat stores. I reviewed this study in a previous blog entry in case you want to refer back to it http://patrickarnoldblog.com/new-natural-anabolic-discovered/

It’s been over a year since then and another study on ursolic acid has been released by these same researchers http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3379974/. The data confirm some of the original findings as well as shed more light on how ursolic acid works in the body to build muscle and burn fat. In contrast to the first study, where normal mice were used, this study used mice fed a high fat diet. This mouse model is used to induce obesity. Since obesity is an enormous health concern in our society, any drug or natural substance that can help treat the causes or effects of obesity would be of tremendous value. In other words, researchers aren’t so interested in developing stuff for athletes and healthy people because that’s not where the bucks are at. Still, studies that utilize the mouse obesity model can be of interest and have applicability to non-obese active folks as well.

To gauge the effects of ursolic acid, the mice were split up into groups. One group just ate the high fat diet alone while the other groups ate the high fat diet supplemented with 0.14 or 0.27 percent ursolic acid. They then examined the rats after 6 weeks. Here are some of the interesting things that they saw

Muscle and Exercise

Ursolic acid increased the size of both slow and fast twitch muscle fibers. This was associated with increased Akt signalling (Akt has vital roles in biological processes such as protein synthesis and glucose uptake and metabolism). These rats had greater grip strength than control rats and could run significantly farther on a treadmill. They had slightly lower resting heart rate than controls while demonstrating no differences in blood pressure. Another interesting find is that a substance called vascular endothelial growth factor – A was substantially more active in the ursolic mice, indicating that new blood vessels were being formed to feed the growing muscle tissue.

Bodyfat and Glucose Tolerance

The mice fed the high fat diet supplemented with ursolic acid gained less weight then the control rats and had substantially less stored body fat. Their fasting blood glucose stayed normal compared to the control mice (average 74 mg/dl versus average 109 mg/dl), and their blood glucose levels after a glucose challenge also was substantially lower.

Brown Fat and Energy Expenditure
There are two types of body fat – brown fat and white fat. White fat is more or less metabolically inactive, and its purpose is mostly to store calories. Brown fat on the other hand is full of an enzyme called UCP-1 which stimulates thermogenesis (this is the same enzyme turned on by DNP). Brown fat is rich in blood supply and essentially burns calories and keeps you warm. The researchers found that the ursolic supplement mice had a lot more brown fat, and not surprisingly they were much more resistant to the cold then the control rats.

The ursolic supplemented mice had higher levels of energy expenditure. Even though they ate more food than the control mice, the ursolic mice weighed less – with the difference in weight made up in body fat. This was not an acute effect however and was only seen after chronic administration of ursolic acid. This is entirely consistent with the fact that it required time for the growth of muscle and brown fat to burn the extra calories, and was not due to some immediate stimulant effect.

Ursolic Acid Supplementation

This latest study just adds to the impressive evidence behind the amazing bodybuilding and overall health potential of ursolic acid. Ursolic acid as a supplement has become more and more popular over the last year or so since the evidence first started pouring in on the stuff. It is usually sold in the form of an extract from herbs such as rosemary or loquat leaf. This form has proven to be less than stellar however in the feedback users have been giving. Results have been hit or miss for the most part.

I noticed this high variability in results and less than anticipated feedback early on, and I was quite certain it was due to the terrible solubility of the compound. It basically repels water and is very insoluble in the sort of solvent systems that are similar to the properties of the lining of your gastrointestinal system. If you couple that with the likelihood it is metabolized extensively upon liver first pass, you end up with very poor bioavailabilty. In fact, research suggests that less than one percent of orally ingested ursolic acid actually gets into your system.

I solved this problem however. For the past several months I have synthesized and played with derivatives of ursolic acid that have solubility and dispersability properties magnitudes better than straight ursolic acid. I have found that delivering these derivatives (which simple break down quickly in the body to ursolic acid after being absorbed) via a topical formulation leads to the sort of body fat loss and muscle mass increases in human subjects that we would expect to see from the published mice studies.

The compound I have settled on as the best has absolutely amazing solubility compared to straight ursolic acid. It is called Arginine Ursolic Acetate and this is its chemical structure.

In the body this compound breaks down rapidly to acetic acid (a dietary fatty acid), l-arginine (a dietary amino acid), and ursolic acid. Although I have never (yet) measured blood levels of ursolic acid to prove that this method delivers the compound way better than regular extract capsules, the fact that almost everyone that has tried when formulated topically gets amazing results sort of speaks for itself.

So there you go. If you weren’t excited about ursolic acid before then you should be now. And if you want to try the patent pending form that I worked my butt off to perfect then you can by clicking here

http://www.prototypenutrition.com/ProductDetails.asp?ProductCode=UR

5 Responses so far

I might be persuaded to actually buy this and I’m seriously considering it, but I really need to know some ballpark idea of how long this bottle will last and how much to use. You know: How many ml total in the bottle? Looks like 240ml, but the pic is too blurry to be sure. Is there a spray pump included? How many ml per spray (approx)? How many sprays per day/bottle? Thanks!

Pat,
I remember some of the old resveratrol studies that gave mice ridiculously high doses (300 mg/kg) to great avail. But then the recent human study showed that 1 mg/kg produced similar blood levels of resveratrol (but no good results due to poor study design imo).
Can you comment on the dose used in Ur Spray (besides its superior bioavailability)?

It is a 240mL bottle. It has 30mg of active per mL. If you do 50 sprays a day the bottle will last you a month. sprayer is included.

I was looking at a study that says ursolic acid causes DNA- damage in the medical journal Atheriosclerosis December 2011 issue. have you heard of it??…https://www.ncbi.nlm.nih.gov/portal/utils/pageresolver.fcgi?recordid=1352204392730301

Patrick,

All results seem very promising, however, I was hoping you could shed some light on the only serious side effect noted – DNA damage. Specifically from the following:

Ursolic acid causes DNA-damage, P53-mediated, mitochondria- and caspase-dependent human endothelial cell apoptosis, and accelerates atherosclerotic plaque formation in vivo
by B Messner; I Zeller; C Ploner; S Frotschnig; T Ringer; A Steinacher-Nigisch; A Ritsch; G Laufer; C Huck; D Bernhard
Article : Peer-reviewed
Language: English
Publication: Atherosclerosis, v219 n2 (201112): 402-408

The only other side i’m aware of (decreased sperm motility) returned to normal when use was discontinued, so this would not be a factor in my consideration of use.

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