Pterostilbene

What is Pterostilbene ?

Pterostilbene (terro-still-bean) is a Stilbenoid, an antioxidant produced by plants to protect themselves against viral, bacterial, fungal attack and excessive sunlight much like another in the same family: Resveratrol. Pterostilbene is most abundant in Blueberries.

Reservatrol has been known for being in the skins of red grapes as an active ingredient, thought to be responsible for the French Paradox : The french have heart healthy and healthier lives than most on their type of diet (as whole, they eat an inflammatory, artery clogging, pro diabetes and pro cancer diet. But thanks to their love of red wine and the Resveratrol it contains, they are not prone to these diseases). Reservatrol has also been identified for other properties, including anti-diabetic, anti-inflammatory, and anti-cancer.

Pterostilbene is a very similar molecule to Resveratrol’s, but where Resveratrol has three hydroxyl groups at its extremities, two of them are replaced with methoxy groups in Pterostilbene. This difference makes Pterostilbene far more bioavailable than Resveratrol:
It’s more easily absorbed through the stomach lining and cell membranes and stays in one’s system longer, giving it similar, but more powerful effects.

pterostilbene

Researchers believe pterostilbene and resveratrol work through same pathways biologically. Because of this, pterostilbene and resveratrol supplements are now being offered by several supplement companies.

Pterostilbene’s health effects

Pterostilbene has an uncanny ability to treat many diseases by changing abnormal cellular metabolic pathways to best correct whatever problem is being faced by diseased, aging cells.

In other words what Pterostilbene does varies depending on how cells have deviated from normal, healthy metabolic pathways.
It up- or downregulates these pathways based on the nature of the disease or aging process taking place in ailing cells.
In fact, besides many other supplements and medications, Pterostilbene exhibits effects comparable to the medications:

  • Clofibrate – used to lower cholesterol and triglyceride levels.
  • Metformin – used to treat type 2 diabetes.
  • Tamoxifen – used to treat some types of breast cancer
  • FOLFOX – a chemotherapy regimen for the treatment of colorectal cancer.

Weight control and DNA repair means youth/life extension

Calorie Restriction is presently the de-facto youth extension strategy and causes the expression of a large number of genes that keeps inflammation and the inflammation related diseases of old age, like atherosclerosis and cognitive decline, at a minimum.
Pterostilbene has the same effect on most of these same genes.
Combined with Resveratrol; Pterostilbene covers just about all of the genes positively affected by Calorie Restriction and then some, reducing fat accumulation in the body and liver by reducing lipogenesis in adipose (fat) tissue and elevated fatty acid oxidation in the liver etc.

Keeping DNA in good repair is essential to longevity.
DNA damage due to oxidation dropped by 18% after one large dose of Pterostilbene rich Blueberries in volunteers.
DNA damage from sun exposure is also reduced.

Pterostilbene: an immune booster

Blueberry extracts (pterostilbene rich) upregulated Natural Killer (NK) Cells, while downregulating proinflammatory Nuclear Factor kappa-beta (NFk-b) expression.
NK Cells identify and destroy any abnormal cells such as virus infected and pre-cancerous cells.
Amongst others, two notable pathogens Pterostilbene is adept at inhibiting are Hepatitis C virus and Candida:
Pterostilbene inhibits infectious particles from being assembled and secreted by the Hepatitis C virus.
Candida Albicans is a particularly nasty bacteria as it has the ability to form antibiotic resistant biofilms and is a NAD+ auxotroph this means it decreases NAD+ which is essential for the expression of youth extending SIRT genes and energy levels in general.
Pterostilbene downregulates the expression of Ras, cAMP and related genes in Candida that are involved in the forming of its protective biofilm so that the immune system can get to and fight any Candida infections.

Pterostilbene has powerful anti cancer effects

Currently Pterostilbene has been found to be effective at reducing breast, colon, esophageal, liver, pancreatic, prostate, stomach, cancers to varying degrees.

Research into other cancers is ongoing, but so far it has been found that Pterostilbene:

• Inhibits malignancy. (stops cells from becoming cancerous)
• Reduces the rate at which already cancerous cells proliferate and inhibits metastasis. (Cancer from spreading)
• Induces apoptosis (cell death) in some types of cancers!

Remarkably, many of Pterostilbene’s anti cancer effects are due to the upregulation of oxidation and the downregulation of telomerase in pre cancerous, malignant and cancerous cells, yet:

“…It was found that the telomerase inhibitory activity exhibited by pterostilbene was dependent of the cell viability and has the potential to be a new drug candidate against breast and lung cancers…”

The circulatory system, Diabetes , Atherosclerosis and Hemolysis

While Pterostilbene increase oxidative stress in many cancers, it has the opposite effect in in arteries and veins where it decreases oxidative stress; reducing the death of the Vascular endothelial cells that line the entire circulatory system.

Pterostilbene is comparable to the drug Metformin in its ability to improve insulin sensitivity and reduce blood glucose levels via to the metabolic regulation of Diabetes.

Pterostilbene is also a “…potent peroxisome proliferator activated receptor alpha (PPARα) agonist…”
Which means it’s better than drugs such as Ciprofibrate at lowering the high lipid (fat) and cholesterol levels in the bloodstream that cause atherosclerosis and blocked arteries.

High lipid and cholesterol, along with high blood sugar, are associated with Dementia, Liver Disease and the general decline of the circulatory system that should be keeping bodies well nourished, oxygenated, energetic and young.

Pterostilbene also has the remarkable ability to protect red blood cells against bacteria, parasites and drugs that would normally kill them and synergises with Resveratrol to protect them from oxidative stress.

Neuroprotection, Alzheimer’s and Dementia

Pterostilbene showed a remarkable ability to reverse cognitive deficits by reducing the oxidation and inflammation that stress brain cells and are a major cause of Alzheimer’s disease and age related cognitive decline.
It also increases the levels of Insulin-like Growth Factor 1 (IGF-1) and Dopamine in the brain.
IGF-1 is integral to the growth of blood vessels and neurons in the Hippocampus, while Dopamine is integral to learning and memory.

Pterostilbene: market and method of production

In the most recent months, pterostilbene has quickly become a promising natural compound in the nutrition and health supplement marketplace. There are several reasons for this sudden increase in the popularity of the product and the supplements within the market.

First, there have been a number of scientific studies published on the topic since 2004. As more promising studies are released, it promotes scientists to release even more to show how popular a product is and what the research is that they have experience with.

Next, enhanced technology allows pterostilbene to be produced at lower costs and in larger quantities.

Pterostilbene was isolated first from a red sandalwood tree which is endangered and found only in southern India. Due to the endangered status of the tree (and other species containing pterostilbene) and the extraction process (it is labor intensive and expensive), obtain large quantities of the pterostilbene from this source is not practical.

Luckily, another source also contain pterostilbene. The main one from where it is today extracted / purified is blueberries.

pterostilbene blueberries

Technologies such as fermentation make it possible for 99% pure pterostilbene to be manufactured low costs and in larger quantities. The technologies also encourage several endangered species to be protected.

As more positive studies increase and more inexpensive and high quality pterostilbene is produced, more pterostilbene supplements are sold in stores and online, allowing more people to take advantage of the many health benefits.

References:

1: Pterostilbene, a dimethyl ether derivative of resveratrol, reduces fat accumulation in rats fed an obesogenic diet. J Agric Food Chem. 2014 Aug 20;62(33):8371-8. doi: 10.1021/jf501318b. Epub 2014 Aug 8.
2: A single portion of blueberry (Vaccinium corymbosum L) improves protection against DNA damage. Nutr Res. 2013 Mar;33(3):220-7. doi: 10.1016/j.nutres.2012.12.009. Epub 2013 Feb 1
3: Pterostilbene and cancer: current review. McCormack D, et al. J Surg Res. 2012.
4: Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging.
J Agric Food Chem. 2008 Nov 26;56(22):10544-51. doi: 10.1021/jf802279h.
5: Pterostilbene, a natural dimethylated analog of resveratrol, inhibits rat aortic vascular smooth muscle cell proliferation by blocking Akt-dependent pathway. Vascul Pharmacol. 2010 Jul-Aug;53(1-2):61-7. doi: 10.1016/j.vph.2010.04.001. Epub 2010 Apr 14.
6: Protective effect of Pterostilbene against free radical mediated oxidative damage. BMC Complement Altern Med. 2013; 13: 238.
7: Identification of molecular pathways affected by pterostilbene, a natural dimethylether analog of resveratrol. BMC Medical Genomics 2008, 1:7 doi:10.1186/1755-8794-1-7
8: Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethyl ether analog, pterostilbene, in rats. Published online 2010 Nov 30. doi: 10.1007/s00280-010-1525-4
9: Analysis of Safety from a Human Clinical Trial with Pterostilbene. Journal of Toxicology. Volume 2013 (2013), Article ID 463595, 5 pages
10: Pterostilbene as a potential novel telomerase inhibitor: molecular docking studies and its in vitro evaluation. Curr Pharm Biotechnol. 2014;14(12):1027-35.
11: Low-dose pterostilbene, but not resveratrol, is a potent neuromodulator in aging and Alzheimer’s disease. Neurobiol Aging. 2012 Sep;33(9):2062-71. doi: 10.1016/j.neurobiolaging.2011.08.015. Epub 2011 Oct 7.
12: Modulation of Hippocampal Plasticity and Cognitive Behavior by Short-term Blueberry Supplementation in Aged Rats Maney Online. Volume 7, Issue 5-6 (01 October 2004), pp. 309-316
13: Protective effect of Pterostilbene against free radical mediated oxidative damage. BMC Complement Altern Med. 2013; 13: 238.
14: Pterostilbene, a natural phytoalexin, effectively protects against UVB-induced skin carcinogenesis by increasing antioxidant cellular defenses and preventing mutagenesis. doi: 10.1158/1538-7445.AM2014-1605 Cancer Res October 1, 2014 74; 1605
15: Pterostilbene protects vascular endothelial cells against oxidized low-density lipoprotein-induced apoptosis in vitro and in vivo. DOI 10.1007/s10495-011-0653-6
16: In vitro and in vivo activities of pterostilbene against Candida albicans biofilms; Antimicrob Agents Chemother. 2014;58(4):2344-55. doi: 10.1128/AAC.01583-13. Epub 2014 Feb 10.
17: Synergistic induction of human cathelicidin antimicrobial peptide gene expression by vitamin D and stilbenoids DOI: 10.1002/mnfr.201300266
18: Stilbene compounds: from the grapevine to wine. Drugs Exp Clin Res. 1999;25(2-3):57-63.
19: Identification of pterostilbene as a phytoalexin from Vitis vinifera leaves. Phytochemistry (Impact Factor: 3.35). 01/1979; 18(6):1025–1027. DOI: 10.1016/S0031-9422(00)91470-5
21: Unbiased probing of the entire hepatitis C virus life cycle identifies clinical compounds that target multiple aspects of the infection. Proc Natl Acad Sci U S A. 2010 Jan 5; 107(1): 291–296. Published online 2009 Dec 29. doi: 10.1073/pnas.0912966107
22: Effect of blueberry ingestion on natural killer cell counts, oxidative stress, and inflammation prior to and after 2.5 h of running. Appl Physiol Nutr Metab. 2011 Dec;36(6):976-84. doi: 10.1139/h11-120. Epub 2011 Nov 23
.23: Pterostilbene, a bioactive component of blueberries, suppresses the generation of breast cancer stem cells within tumor microenvironment and metastasis via modulating NF-κB/microRNA 448 circuit. Mol Nutr Food Res. 2013 Jul;57(7):1123-34. doi: 10.1002/mnfr.201200549. Epub 2013 Mar 15.
24: Dietary intake of pterostilbene, a constituent of blueberries, inhibits the β-catenin/p65 downstream signaling pathway and colon carcinogenesis in rats. Carcinogenesis. 2010 Jul; 31(7): 1272–1278. Published online 2010 Jan 8. doi: 10.1093/carcin/bgq004
25: Immune Exhaustion and Immune Senescence – Two Distinct Pathways for HBV Vaccine Failure during HCV and/or HIV Infection. Arch Immunol Ther Exp (Warsz). 2013 Jun; 61(3): 193–201. Published online 2013 Feb 12. doi: 10.1007/s00005-013-0219-0
26: From French Paradox to cancer treatment: anti-cancer activities and mechanisms of resveratrol. Anticancer Agents Med Chem. 2014;14(6):806-25.
27: Resveratrol: French Paradox Revisited. Front Pharmacol. 2012; 3: 141. Published online 2012 Jul 17. doi: 10.3389/fphar.2012.00141
28: Gene expression profiles induced by cancer chemopreventive isothiocyanate sulforaphane in the liver of C57BL/6J mice and C57BL/6J/Nrf2 (-/-) mice. Cancer Lett. 2006 Nov 18;243(2):170-92. Epub 2006 Mar 3.
29: A Review of Pterostilbene Antioxidant Activity and Disease Modification. Oxidative Medicine and Cellular Longevity; Volume 2013 (2013), Article ID 575482, 15 pages
30: Antioxidant effect of trans-resveratrol, pterostilbene, quercetin and their combinations in human erythrocytes in vitro.
Plant Foods Hum Nutr. 2010 Mar;65(1):57-63. doi: 10.1007/s11130-010-0154-8.