From aged garlic extract to omega-7, suppliers are targeting ingredients that aid in balancing cholesterol levels.Part II of NIE’s heart health coverage.

Cholesterol performs important functions in the body. This soft, waxy substance is found not only in the bloodstream, but also in every cell, where it helps to produce cell membranes, hormones, vitamin D and bile acids that help digest fat.Cholesterol also helps in the formation of memories and is vital for neurological function.

Conventional medicine has stressed strong downward pressure to keep cholesterol levels low. According to the American Heart Association (AHA), 98.8 million Americans age 20 and older have Total blood cholesterol levels of 200 milligrams per deciliter (mg/dL) or higher (45 million men and 53.8 million women).And of that number, 33.6 million have total blood cholesterol levels of 240 mg/dL or higher (14.6 million men and19. 0 million women). Further, the Centers for Disease Control and Prevention (CDC) reports that people with high total cholesterol have approximately twice the risk of heart disease as people with optimal levels (lower than 200 mg/dL).

However, others recommend an approach not based on cholesterol levels, but heart disease risk. Those at low risk of cardiovascular disease may not benefit much from taking often recommended statin drugs, but are still at risk of suffering from side-effects from treatment. Whichever their school of thought, many Americans concerned with cholesterol levels are turning to natural products as an alternative.

“Heart health has become an increasingly important topic for health care providers and their patients,” said Jay Levy, director of sales for Wakunaga of America Co., Ltd. In California. He noted that, according to market Research conducted between 2003 and 2007, cholesterol lowering supplement sales increased 37 percent in natural foods markets and 20 percent in mainstream sales.

Cholesterol Sources

“The general understanding of cholesterol production that is gaining significant attention is the fact that the liver produces approximately 60 to 70 per- cent of the total cholesterol in our body,” said Bryan See, regional product manager for New Jersey-based Carotech Inc. “The remaining 30 to 40 percent is from diet/foods that one eats.” 

While diet is a factor when it comes to cholesterol levels, research is showing that, in some cases, some people are genetically predisposed to have high cholesterol levels. A study published online in the journal The Lancet showed that a large percentage of people who Have a clinical diagnosis of familial hyper- cholesterolemia (FH) inherit a number of small-effect changes in a number of genes instead of what was previously thought to be a large-effect mutation in one gene. According to Dean Mosca, president of New Jersey-based Proprietary Nutritionals Inc. (PNI), FH is a commonly inherited disorder that causes high levels of LDL (low-density lipoprotein). If this condition is left untreated (about 75 percent of cases are undetected), those people have up to eight times greater risk of early coronary heart disease, he said.

“A primary concern remains ‘cholesterol through diet,’ although more Americans are becoming aware of FH and the liver’s role in cholesterol production, outside of diet,” Mosca said. “But diet is what one can control. This is why supplementation of science-backed ingredients is so attractive; they can help Consumers manage their cholesterol supplements through oral/ingestible administration.” 

It is also understood that increased physical activity, weight loss and a balanced diet can help lower levels.However, cholesterol is very specific to each individual and a full lipid profile is important, according to Christine Beckner, director of Anderson Global Group, LLC in California.

“It is widely accepted that your risk of developing heart disease is linked to healthy LDL/HDL (high-density lipoproteins) levels,” she said. “While everyone should know their cholesterol levels, a recent study demonstrates about half of all strokes and heart attacks occur in individuals with ‘normal’ cholesterol levels.Thus, more focus should be put on ‘total lipid health’ and related inflammation … an increasing number of doctors are tying cholesterol health to the inflammation conundrum. Almost everything ties back to inflammation of some sort.” 

Notable Ingredients 

Cholesterol-lowering supplements work in one of several ways, according to Wakunaga’s Levy. “Phytosterols, for example, occupy cholesterol receptor sites, which prevents cholesterol from being absorbed into the bloodstream,” He explained. “Soluble fiber, on the other hand, binds to cholesterol and helps to carry it out of the body. Herbs like artichoke leaf extract trigger an increase in bile production, which accelerates the body’s ability to rid itself of excess cholesterol. Aged garlic extract (AGE) and red yeast rice (RYR) help inhibit the liver’s ability to produce cholesterol.” 

As many consumers are opting for a natural approach to balance their cholesterol levels, some of the long-standing ingredients with research credibility include plant sterols and niacin. Other ingredients, such as AGE and RYR, have become well known as they has been promoted in the press and mentioned on popular TV shows, such as The Dr. Oz Show and The Doctors. “AGE and RYR have garnered the most attention in the press, especially in light of new research highlighting the side effects of cholesterol-lowering statin drugs,” said Levy. “Lesser known ingredients, such as guggul and artichoke leaf extract, have not been as well studied or publicized. For this reason, they have not gained the market momentum of AGE or RYR.” 

According to Levy, AGE is a well- established cholesterol-lowering ingredient backed by more than 700 published studies. Wakunaga of America offers a number of dietary supplements that are designed to promote healthy cholesterol levels including Kyolic Formula 104- Cholesterol. In addition to AGE, this cholesterol-specific supplement contains lecithin, which was shown to significantly reduce total and LDL cholesterol levels in a 2010 study at Camilo Castelo Branco University in Brazil, according to the company.

Wakunaga also offers Kyolic Formula 107-Phytosterols, a formula that pairs AGE with phytosterols. According to Levy, phytosterols are naturally occurring compounds found in many vegetables And legumes. Because they have a chemical structure similar to cholesterol, these plant sterols can block cholesterol absorption in the intestine by more than 10 percent. Additionally, phytosterols also help reign in triglycerides.

“We believe that the phytosterols, which received approval from FDA (U.S. Food and Food Administration) as well as EFSA (European Food Safety Authority), are well recognized and accepted by consumers as the ingredient for cholesterol management,” said Carotech’s See. “The synergistic combination of tocotrienols plus phytosterol will allow a company to differentiate their product from the many phytosterols in the market. And hence, having the marketing edge over competition.” 

According to See, tocotrienol is a nat- ural vitamin E, but it is far more potent (biologically and physiologically) than the conventional vitamin E alphatocopherol.Research has shown that tocotrienols degrades HMG-CoA reductase—an enzyme that catalyzes cholesterol production in the liver, hence lowering the production of LDL- cholesterol, while the regular tocopherol vitamin E does not.

Tocomin SupraBio from Carotech Inc. is a patented, bio-enhanced, self-emulsifying formulation containing natural full-spectrum tocotrienols concentrated from virgin red palm oil. This advanced formulation ensures an increase in oral tocotrienol absorption (each and individual tocotrienols) by an average of 250 percent1 Tocomin SupraBio is patented in the U.S., Europe, Japan, Australia, New Zealand, Malaysia, Singapore, Philippines, China, Hong Kong and Taiwan.

PNI’s ingredient, Sytrinol, is a safe, effective cholesterol- and triglyceride- lowering nutrient that works in 30 days, according to the company. It is made up of a blend of powerful antioxidants including polymethoxylated flavones (PMFs)—tangeretin and nobiletin—and a range of palm tocotrienols (alpha, delta and gamma). Studies have revealed that Sytrinol is able to significantly lower total cholesterol, LDL and triglycerides. In addition, the formula has also been shown to increase HDL levels, according to the company.

In one 12-week, placebo-controlled study, 120 men and women with moderately elevated cholesterol levels.Compared to those in the placebo Group, subjects taking Sytrinol had a 30 percent drop in total cholesterol, 27 percent in LDL cholesterol and 34 percent in triglycerides. In addition, HDL levels increased by four percent, resulting in a significant 29 percent improvement in the LDL/HDL ratio.

According to the AHA, omega fatty acids can supply the body with nutrients that can increase the body’s overall level of cardiovascular functioning. Omega-3 fatty acids can aid in raising HDL levels, while lowering trycglyceride levels. According to a study published in 2011 in the journal International Journal of Hypertension, Japanese researchers investigated the effects of taking 2 g of DHA supplements daily for five weeks on Scottish men with hypertension and high cholesterol. The results revealed that the fish oil significantly boosted HDL and significantly lowered total cholesterol.

Another essential fatty acid, omega-7 fatty acids can also help reduce total cholesterol, triglycerides and LDL levels.Anderson Global Group offers Provinal Purified Omega 7 Oil, an ultra-purified omega-7 fatty acid blend. “The Cleveland Clinic’s findings on the progression of atherosclerosis and the positive impact of purified palmitoleic acid have made Provinal one of the hottest new offerings,” said Beckner. “In a recent preclinical trial conducted by Dr. Luis Martinez, patients consuming 210 mg of Provinal daily saw an average C- reactive protein reduction of 67 percent and an average triglyceride reduction of 36 percent. Additional clinical studies are pending later this year, but the results thus far are very compelling.” 

While some ingredients such as AGE and RYR have gained momentum in the market, others have lost some ground due to under performing. “One supplement that has lost some credibility for its ability to lower cholesterol is policosanol,” said Wakunaga’s Levy. He noted that a 2006 German study did not find policosanol to reduce cholesterol levels. Other research has provided mixed results with some studies showing certain benefits while other studies claiming that policosanol has no benefit in cholesterol management.

Quality Assurance

Studies are garnering attention from consumers who are looking for products with proven ingredients that back up the claims on the label. “We observed that consumers are taking charge now in that they are beginning to manage their cholesterol level via dietary supplementation,” said Carotech’s See. “This augurs well for the industry. But in order to Ensure integrity, we need to have good science backed by well-designed, double-blind, placebo-controlled, human clinical studies.” 

In addition to research, checkpoints must include bioavailability of the ingredient. “Along with efficacy and safety, bioavailability and dosage are critical,” explained Levy. “It’s important that consumers receive a clinically effective dose that results in higher serum levels of the cholesterol-lowering nutrient. However, it’s also important that this dosage is available in a convenient delivery system to increase consumer compliance when taking the supplement.” 

“It all begins with us, as a supplier,” added PNI’s Mosca. “We will never put forth any ingredient that does not have a portfolio of credible science, or does not comply with strict manufacturing and processing regulations (cGMPs).” He also noted that PNI heavily engages in social media and consumer marketing to pull consumers to our brand partners.

See offered that finished product manufacturers should consider the source of the ingredients, the research on the ingredients themselves, in addition to learning if they are produced according to approved manufacturing processes, such as implementation and compliance to GMPs.

“This market will remain steady as more people become aware of how unhealthy cholesterol numbers can devastate their health,” concluded Mosca.

“There’s a reason why Cheerios re branded itself as the cholesterol-management cereal, with their homespun commercials featuring active, middle-aged adults concerned about their health and well- being: cholesterol is a top health concern across the board.” NIE 

Reference 

1 D. Ho, et al., “Drug Delivery System: Formulation for Fat-Soluble Drugs,” US Patent 6596306 (2003).

Study: “Good” Cholesterol Could

New research provides early evidence that “good” cholesterol may possess anti-aneurysm forming properties. In laboratory-based investigations, scientists found that increased levels of high-density lipoproteins (HDL), the so-called good cholesterol, blocked the development of aneurysms—dangerous “ballooning” in the wall of a blood vessel in the body’s largest artery, the aorta. According to researchers, the findings, published in the journal Atherosclerosis Thrombosis and Vascular Biology, lay the foundations for further investigations into ways of raising HDL cholesterol as a possible therapeutic intervention for the condition.

Abdominal aortic aneurysms can rupture and kill without warning. There are no therapeutic treatments for aneurysms. Patients are monitored until the aneurysm reaches what is considered to be a critical size where it is at significant risk of rupturing—5 cm in N diameter—and then it is repaired by surgery.

The study, led by researchers from St. George’s University of London, found that elevating the amount of HDL cholesterol in the abdominal area of the aortic artery in mice both reduced the size of aneurysms that had already grown and prevented abdominal aortic aneurysms from forming at all.

The researchers say that while more work is needed to understand the exact mechanism by which HDL cholesterol effects aneurysms, their investigations indicate that raising HDL cholesterol influences the activity of the aortic artery’s cells, which are the building blocks of its structure and function.

Researchers found that elevated levels of HDL had two key influences on the cells. Firstly, it altered the signals sent between cells, which, in turn, reduced the activity of a protein called ERK1/2 that is known for its cell growth properTies. Secondly, it increased levels of HDL cholesterol induced programmed cell death, which is an essential part of the cell life cycle that sees old cells replaced with new ones.

The study focused on mice models of the aorta just above the kidney (the suprarenal region) and the region that is just below the kidney and most commonly associated with aneurysm formation in humans (the infrarenal region). The researchers hope that the effects seen in these specific areas will help explain basic mechanisms of aneurysm formation.

“HDL cholesterol is made up of a complex family of heterogeneous particles that may vary in composition, size and function,” said Dr. Gillian W. Cockerill. “Whilst we have shown that elevating the concentration of the so called ‘good-lipid’ can modulate site specific cellular responses and inhibit aneurysm formation, it is important to Learn more about changes that occur on HDL complexity in addition to the effects in the artery’s responses that influence aneurysm development.” 

The researchers said that, in principle, if raising HDLs can be induced using a drug, it could offer a preventative measure to reduce the chance of an aneurysm developing for individuals considered at high risk of aneurysms. It could also offer a treatment option for patients from early diagnosis that could negate the need for surgery. But they point out that much more research is needed before this becomes a reality. The next phase of the investigations, which the researchers hope to begin this year, will see the researchers conduct laboratory tests with families of drugs that can elevate HDLs and reproduce the observed effects on aneurysms.

For more information, visit www.sgul.ac.uk.