The heart health market has surged during the past 10 years, largely due to the aging of the Baby Boomer generation. This is the first generation that has stressed education and knowledge, and Boomers are using this knowledge to research ways to maintain their health as they age. During the most recent recession, as health care costs rose and health benefits were cut, people started looking to nutraceuticals as an alternative and less expensive means of combating and preventing illnesses. In short, this target audience is receptive to nutraceuticals that target specific diseases (e.g., cholesterol and blood pressure).
Antioxidants are among the nutraceutical solutions to help target specific diseases. Many have heard of the grape antioxidant, resveratrol, but the less-famous blueberry antioxidant, pterostilbene, has shown key advantages over resveratrol. Although they are both stilbenes and belong to the same class of compounds, the structure of pterostilbene provides added health benefits over resveratrol. For example, pterostilbene:
- has 80-percent bioavailability (can more easily enter into the blood stream) while resveratrol has just 20 percent;1
- lasts longer in the blood stream, for more prolonged use by cells,2 as pterostilbenes half-life in the blood is 105 minutes while resveratrols is just 14 minutes3,4; and
- is effective at activating good" proteins such as PPAR-alpha, which helps lower cholesterol levels.5,6
First Clinical Data Supporting Pterostilbene
Numerous animal studies have shown the positive benefits of pterostilbene, and recently the first clinical trial evaluated its impact in humans. The study, conducted by the University of Mississippi Medical Center, evaluated pTeroPure® pterostilbene (from ChromaDex Inc.) for multiple health benefits, including its impact on blood pressure, body weight and cholesterol.7 The study, a double blind, placebo-controlled trial, included 80 adults averaging 54 years of age with high cholesterol (total cholesterol of 200 or greater and/or low-density lipoprotein (LDL) cholesterol of 100 or greater). Most participants were women (71 percent), and some participants (55 percent) had been diagnosed with high blood pressure. Participants were randomized to receive either pTeroPure, with or without a grape extract, or placebo for six to eight weeks.
At the conclusion of the study, participants who took a high dose of pterostilbene (250 mg/d) achieved significant reductions in blood pressure compared to placebo: 7.8 mmHg in systolic blood pressure (P<0.01) and 7.3 mmHg in diastolic blood pressure (p<0.001), without serious adverse events. The only change in lipids was an increase in LDL cholesterol with pTeroPure pterostilbene (24.9 mg/dL, P<0.001), which was less among participants on cholesterol-lowering medication and was not seen in those who also received grape extract with pterostilbene. The presence of a baseline cholesterol medication appeared to lessen the LDL effects. Additionally, those not on cholesterol medication had a minor average reduction in body weight (reduced body mass index [BMI] of 0.59 kg/m2) with pterostilbene.
Developing a Commercially Viable Supply
As with any ingredient, it is essential to have supportive data as well as a commercially viable way to produce the ingredient. Method and cost are the two main challenges to manufacturing and supplying pterostilbene.
The two main sources of natural pterostilbene are:
- berries, which include only a tiny fraction of the amount of pterostilbene needed to realize the benefits shown in studies,8 and are not a viable source due to low natural levels and the implied cost of the starting materials; and
- the Indian kino tree (Pterocarpus marsupium), which includes higher levels of pterostilben,e but is also not a viable source because extracting the pterostilbene would require the harvesting of the International Union for Conservation of Nature-listed threatened species.
Therefore, pTeroPure pterostilbene is manufactured as a nature-identical, but chemically-synthesized ingredient. However, because of the complicated method of manufacturing, the average cost for a clinically relevant dose (50 mg) of pterostilbene remains approximately $0.06 to $0.08, still higher than the penny or less to manufacture the majority of vitamins, minerals and herbs.
Despite these challenges, pterostilbene is now affordable and accessible through multiple products sold throughout the United States. With pterostilbene shaping up to be one of the most exciting new ingredients in recent years, additional clinical studies are planned to explore additional health benefits beyond heart health, including cognitive function ,9,10 anti-aging,11,12 weight loss and other metabolic disorders.
Tanushree Bose, Ph.D., is the clinical development senior manager at ChromaDex Inc.
References listed on the next page.
Learn more about this ingredient, view the whitepaper, " Blueberries and Pterostilbene ."
1. Kapetanovic IM, Muzzio M, Huang Z, Thompson TN, McCormick DL. Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethylether analog, pterostilbene, in rats; Cancer ChemotherPharmacol. 68, 593 (2011).
2. W Nutakul et al. Inhibitory Effects of Resveratrol and Pterostilbene on Human Colon Cancer Cells: A Side-by-Side Comparison. J Agric Food Chem. [Epub ahead of print] (2011).
3. Rimando AM, Nagmani R, Feller DR, and Yokoyama W. Pterostilbene, a new agonist for the peroxisome proliferatoractivated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters. J. Agric. Food Chem. 53, 3403 (2005)
4. Satheesh AM, and Pari L. Effect of pterostilbene on lipids and lipid profiles in streptozotocin-nicotinamide induced type 2 diabetes mellitus. J. Appli. Biomed. 6, 31 (2008)
5. Rimando AM, Nagmani R, Feller DR, and Yokoyama W. Pterostilbene, a new agonist for the peroxisome proliferatoractivated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters. J. Agric. Food Chem. 53, 3403 (2005).
6. Joseph JA, Fisher DR, Cheng V, Rimando AM, and Shukitt-Hale B. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging. J. Agric. Food Chem. 56, 10544 (2008).
7. Riche DM, Deschamp D, Griswold ME, McEwen CL Riche KD, Sherman JJ, Wofford MR. Impact of pterostilbene on metabolic parameters in humans. Poster presentation at: American Heart Association 2012 Scientific Sessions on High Blood Pressure Research, September 20, 2012.
8. Rimando AM, Kalt W, Magee JB, Dewey J, and Ballington JR. Resveratrol, pterostilbene, and piceatannol in Vaccinium berries. J. Agric. Food Chem. 52, 4713 (2004).
9. Joseph JA, Fisher DR, Cheng V, Rimando AM, and Shukitt-Hale B. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging. J. Agric. Food Chem. 56, 10544 (2008).
10. Shukitt-Hale B, Lau FC, Joseph JA. Berry Fruit Supplementation and the Aging Brain. J. Agric. Food Chem. 56, 636 (2008).
11. Joseph JA, Fisher DR, Cheng V, Rimando AM, and Shukitt-Hale B. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging. J. Agric. Food Chem. 56, 10544 (2008).
12. Shukitt-Hale B, Lau FC, Joseph JA. Berry Fruit Supplementation and the Aging Brain. J. Agric. Food Chem. 56, 636 (2008).