Ursolic Acid

Fighting Fat While Sparing Precious Muscle

• Supports Fat Loss*
• Supports Lean Muscle*
• Supports Cardiovascular Health*

When it comes to getting in shape, do you ever find yourself in a “catch 22”? Coined in the early 1960s, this expression refers to a no-win situation – one where solving one part of a problem only creates another. Picture this as an example: You clean out the junk in your diet, you begin hitting the gym, and you lose 15 pounds. Great! Mission accomplished, right? Maybe not. In your effort to lose unwanted weight, you’ve also lost a precious commodity – muscle. Your waistline may be smaller, but your body is soft, lacking definition. You’ve solved one part of the problem (the number on your scale), only to encounter another (loss of muscle tone). This is the reality for many – having to choose between fat loss and muscle growth. If only there was a way to achieve both...

Trust the Old Adage

As it turns out, an apple a day does more than keep the doctor away. A naturally occurring ingredient found in apple peels (ursolic acid) has actually been shown to support fat loss and muscle growth… and not just one or the other. People who are especially concerned about sparing – and ultimately building – muscle can be confident knowing that Labrada’s new Ursolic Acid Lean Muscle Optimizer has their goals for a lean, defined body in mind. That’s because ursolic acid has been shown to affect molecular pathways that could actually prevent muscle loss and weakness. In studies involving both humans and mice, ursolic acid was proven to help counteract the catabolic effects of fasting/dieting. Meanwhile, in studies with just mice, this natural ingredient was found to protect against muscle atrophy (or decrease in muscle mass). In fact, when ursolic acid was added to the food of normal, non-fasted mice, their muscles grew*.

While ursolic acid as a dietary supplement has only recently come into the spotlight, early findings are extremely promising and human clinical trials continue. Because medicinal plants containing ursolic acid have been used in folk medicine for centuries, you can be confident this ingredient has been proven natural, safe, and effective.*

Fat Loss Anyone?

In the previously mentioned study where mice experienced muscle growth when given ursolic acid, it was also found that the mice became leaner and had lower blood levels of glucose, cholesterol, and triglycerides. This, again, is that coveted combination that many of us strive for – muscle growth and fat loss rolled into one. Supplementing with Labrada’s Ursolic Acid could make all the difference. As further shown in studies, mice that were fed ursolic acid and a high-fat diet had significantly decreased body weights, abdominal (visceral) adiposity, and levels of blood glucose and plasma lipids compared to mice on the same diet but without the ursolic acid supplement. Diet and activity levels were the same for both groups; the only “edge” was the ursolic acid. The question then remains: What could Ursolic Acid do for you?*

It All Comes Back to Better Health

Labrada’s Ursolic Acid hasn’t just been designed to help you look better. It even supports cardiovascular health, making it a beneficial supplement for dieters and athletes of all ages. Because Ursolic Acid can help reduce bodyfat and blood sugar levels, it provides nutritional support that may be beneficial for both obesity and diabetes. It also plays a role in bone and joint health.*

Want to Dig Deeper Into the Science?

While studies continue on ursolic acid and its role in fat loss, muscle sparing, and the prevention of various health conditions, you can view some of the current research by Monica Mollica BSc , MSc. below.

Digging Deeper Into the Science

Ursolic acid is a newly discovered substance, which is a component of apple peels. Ursolic acid has generated a lot of scientific interest lately, because it has been found to affect molecular pathways that could prevent muscle loss and weakness, promote fat loss, and have a beneficial effect on multiple chronic diseases.*

What is it?

Ursolic acid, also known as urson, prunol, micromerol, and malol, is a pentacyclic triterpenoid compound which naturally occurs in a large number of vegetarian foods, medicinal herbs, and other plants, including apples and rosemary.^1,2

Anti-catabolic - Preservation of Muscle Mass

The anti-catabolic effect of ursolic acid was recently discovered in a study that looked at what happens to gene activity in muscles during catabolic situations like fasting.³ It was found that fasting in both people and mice changes gene expression in many genes. These gene expression changes were then compared to those seen in muscle fibers that had been exposed to a wide array of bioactive molecules. Of all the tested bioactive molecules, ursolic acid turned out to be a unique substance that induced a gene expression pattern that counteracted the catabolic effects of fasting.

Next, ursolic acid was given to fasted mice, and found to protect against muscle atrophy. When ursolic acid was added to the food of normal (non-fasted) mice for five weeks, their muscles grew. These effects were mediated by enhanced insulin signaling in muscle and counteracting of the gene expression pattern causing muscle atrophy.

Fat loss

In the same study,³ it was further shown that mice given ursolic acid also became leaner and had lower blood levels of glucose, cholesterol and triglycerides.

Another study specifically evaluated ursolic acid for its effects on blood glucose, lipids, and abdominal fat deposition in mice fed a high-fat diet. Mice supplemented with ursolic acid and fed a high-fat diet had significantly decreased body weights, abdominal (visceral) adiposity, and levels of blood glucose and plasma lipids compared to mice on the same diet but without the ursolic acid supplement. Also, a significant increase was observed in levels of leptin with a decrease in ghrelin.⁴

Ghrelin is a hormone secreted in the stomach. It has an orexigenic (appetite increasing) effect through its action on the hypothalamic appetite-regulating pathway.^5-8 It also increases adipose tissue accumulation and has a diabetogenic effect on the liver and pancreas.⁶

Leptin, a hormone secreted from fat cells, has wide ranging effects in the body.⁹ Among all, it plays a key role in regulating energy intake and energy expenditure.^9-12

Thus, the increase in leptin and decrease in ghrelin levels most likely contributed to these ursolic acid induced anti-obesity effects. Ursolic acid also has been shown to increase liberation of fatty acids from body fat stores,^13,14 and inhibit fat absorption by reducing the activity of pancreatic lipase (an enzyme that is necessary for fat absorption).¹⁴ Thus, ursolic acid can help to fight off excess body fat via several complementary mechanisms.*

Improved Blood Lipid Profile and Blood Sugar Control

The ability of ursolic acid to lower blood sugar was further demonstrated in another study, which also found that ursolic acid significantly lowers levels of total blood cholesterol and LDL (the bad cholesterol), increases HDL (the good cholesterol), and stimulates liver glycogen synthesis.¹⁵ This study concluded that ursolic acid may be useful for people at risk of developing diabetes and associated cardiovascular complications by improving plasma glucose levels and lipid profile, as well as by promoting liver glycogen deposition.

Anti-Atherogenic and Cardio Protective

The walls of large arteries, when activated, recruit circulating monocytes (a type of white blood cell).¹⁶ This in turn contributes to chronic inflammation and the development and progression of atherosclerosis.¹⁶ A common condition that affects monocytes in a negative way is high blood sugar (hyperglycemia),¹⁷ which can be caused by a high carbohydrate diet and physical inactivity. High blood sugar levels cause a low grade inflammatory state, and monocytes are important in orchestrating these effects.¹⁷ In light of this, it is interesting that ursolic acid is a potent inhibitor of monocyte dysfunction and the development of an inflammatory state, and has anti-atherogenic properties.¹⁸

Ursolic acid also beneficially affects endothelial cells and thereby promotes cardiovascular health via other mechanisms. One of those is via an up-regulation of eNOS expression in endothelial cells and increase in bioactive vascular nitric oxide, and parallel downregulation of eNOS-dependent production of free radicals in human endothelial cells.¹⁹

eNOS stands for endothelial nitric oxide synthase, and is the enzyme in blood vessels that produces nitric oxide. In the body, nitric oxide is an important cellular signaling molecule. Nitric oxide has gained status as one of the most important signaling molecules in the cardiovascular system, and is regarded to be a ubiquitous mediator of cardioprotection.²⁰ The origin of many cardiovascular diseases is associated with reduced nitric oxide production and availability and/or increased endothelial eNOS-dependent free radical formation.^20-22 Therefore, restoring and/or increasing adequate nitric oxide levels and activities in the heart and blood vessels is a promising therapeutic intervention with a high potential for effective prevention and/or treatment of cardiovascular diseases. The fact that several medicines (for ex. nitroglycerine) are active by being precursors to nitric oxide, and that medical drug research is developing medicines that target eNOS to increase its activity,^21,23 proves that this mechanism is very important for cardiovascular health. Thus, ursolic acid holds great potential in being a natural dietary compound that increases eNOS actvity and nitric oxide levels.*

Bone and Joint Health

In the field of osteoporosis there has been growing interest in anabolic agents that enhance bone mass and improve bone architecture. It has been demonstrated that ursolic acid has anabolic effects on the skeleton by stimulating osteoblast differentiation, bone mineralization and enhance new bone formation.²⁴

Ursolic acid also has been found to have anti-arthritic effects comparable with that of ibuprofen, but without causing gastric dmage which is a side effect of ibuprofen treatments.²⁵

Safety

Ursolic acid is a natural dietary substance that only recently has started to generate scientific interest. While most of the studies on ursolic acid have been made in mice and cell cultures, medicinal plants containing ursolic acid have been used in folk medicine for centuries.¹ It has been established that ursolic acid is non-toxic,¹ so we can count on seeing products being developed with ursolic acid as the active ingredient for different health related condition in the near future.

Bottom Line

The presence of ursolic acid in apple peels and many edible plants contributes to their overall health benefits. Ursolic acid not only counteracts muscle breakdown during catabolic conditions like fasting and dieting, but also can help to reduce body fat, and lower sugar and lipid levels in blood. These effects are beneficial for the prevention and/or reduction of the severity of both obesity and diabetes. It is interesting that ursolic acid exerts its potential anti-obesity effects via both hypothalamic and metabolic targets.

In addition, ursolic acid has potent anti-atherogenic and anti-tumor effects that beneficially could influence cardiovascular disease and cancer outcomes. Ursolic acid is generating a lot of scientific interest as being a novel and bioactive molecule for drug discovery.^26-31 Currently ursolic acid is in human clinical trials for treating cancer, tumor, and skin wrinkles.²⁶ With all the recent studies on ursolic acids, the old cliché "an apple a day keeps the doctor away" could more specifically be restated as "an apple a day helps keep muscle wasting and body flab away."