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Pterostilbene is a natural substance found in blueberries, red grapes and almonds and other fruits. Chemically similar to Resveratrol, plants produce it as a defense mechanism against infection and insect attack.
It is interesting healthcare researchers due to its greater bioavailability compared to Resveratrol and its powerful antioxidant and anti-inflammation activity. It was shown to have 80% bioavailability compared to 20% for Resveratrol (1), and its half-life in the blood stream is approximately five times higher than that of Resveratrol (2).
Evidence suggests it has potential to inhibit growth, adhesion, metastatic growth and to be an active anti-cancer agent. Research evidence is growing and it is thought that it could have valuable roles in the following key areas:
Cancer Prevention and Treatment
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Prostate Cancer
A 2010 study found that purified Pterostilbene was effective against prostate cancer lines (3). The researchers noted that Pterostilbene caused DNA fragmentation, formation of apoptotic bodies and membrane distortions in the cancer cells.
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Breast Cancer
A team at the University of Vermont found that Pterostilbene decreased breast cancer cells, triggered mitochondrial depolarization and caused alteration in cell cycle (4).
Interestingly, Pterostilbene treatment produced a synergistic inhibitory effect when combined with the chemotherapy drug Tamoxifen, demonstrating clinical potential in the treatment of breast cancer (5).
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Pancreatic Cancer
In 2012 a team in Connecticut evaluated pancreatic cancer cells after they were treated with Pterostilbene. The team found that in nude mice, oral Pterostilbene inhibited tumor growth rates (6).
The team concluded that Pterostilbene alters gene expression in pancreatic cancer and increases the anti-proliferative markers.
In addition to inhibiting pancreatic cancer, recent research found that Pterostilbene ameliorated inflammation and acinar damage in pancreatitis in vitro (13).
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Melanoma
The University of Vermont again carried out research showing that Pterostilbene inhibits melanoma growth in vitro in association with increased effector caspase activity (7).
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Lung Cancer
The same team treated lung cancer cell lines with increasing doses of Pterostilbene and discovered that Pterostilbene significantly decreased cell viability in lung cancer cells in a concentration- and time-dependent manner (8).
Concentrations greater than 20 microM of pterostilbene produced significant growth inhibition.
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Oral Cancer
In 2015 researchers in Taiwan published results that showed that Pterostilbene effectively inhibited the growth of human oral cancer cells by inducing cell cycle arrest and apoptosis (9).
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Gastric Cancer
Researchers in Montréal and Québec found that that juice from velvet leaf blueberry, low-bush blueberry, and high-bush blueberry, all inhibited cell proliferation of gastric adenocarcinoma cells (20).
Liver Health
Pterostilbene and blueberries exert anti-oxidant, anti-inflammatory, and anti-carcinogenic effects in models of Chronic Liver Disease (CLD) and liver cancer. Researchers are hopeful that Pterostilbene can be effective against a wide range of liver conditions possibly through its ability to reduce oxidative stress.
- South Korean researchers found that that Pterostilbene may be a functional chemo preventative agent and that dietary exposure of it would be helpful for improving liver health (10).
- Research in 2011 showed that its antioxidant effects were found in cancerous and noncancerous hepatic cells. The result of this research show that Pterostilbene’s antioxidant activity is beneficial to normal cells but antagonistic to the growth of cancerous cells (11).
- Protection against hepatic problems has also been shown by Pterostilbene, which is able to thwart cellular dysfunction by inhibiting H2O2-induced inhibition of gap junctional intercellular communication (GJIC), a key facilitator of hepatic tumorigenesis (12).
Cardiovascular Health
Vascular problems occur due to poor lifestyle, mechanical stress and Reactive Oxygen Species (ROS). ROS are chemically reactive chemical structures that contain oxygen. Examples are peroxides and superoxide. They can damage cell structures when ROS levels surge due increased levels of stress. The combination of repeated exposure to ROS and oxidative stress can lead to stress of blood vessels that can be predictive of future adverse cardiovascular events.
Research has suggested that Pterostilbene can have protective effects against cardiovascular disease possibly due to creation of antioxidant enzyme (21).
It is believed that Pterostilbene can have protective effects against cardiovascular disease possibly due to creation of antioxidant enzyme.
- Research in 2009 showed that a blueberry enriched diet protects rat hearts from ischemic (blood supply) damage (14).
- Narrowing of the heart arteries was reduced by increasing the release of the antioxidant enzyme after blueberry supplementation (15).
- Pterostilbene has shown numerous protective benefits against narrowing of the arteries through regulation of vascular smooth muscle cells (VSMCs) and vascular endothelial cells (VECs) (16).
- It has been shown to supress numerous harmful proteins and signalling of damaging processes that contribute to atherosclerosis (16, 17, 18).
- Pterostilbene modulates antioxidant enzymes and this effect has been shown in heavy smokers (19).
Diabetes
The rise of diabetes is causing concern throughout the developed world. Linked to the epidemic of obesity, the implications for the health for a sizeable percentage of the population are predicted to be significant with commensurate strains on health services and an increasing financial burden.
Standard treatments have side effects and have to be tailored to patient’s needs and circumstances stretching limited resources yet further.
These factors have spurred the search for a more natural and efficient alternative to counteract the effects of sedentary lifestyles, low quality diet and issues such as harmful alcohol levels and smoking. It is suggested that the glucose and lipid-lowering effects of the dietary compound Pterostilbene may contribute to its clinical potential for prevention or treatment of diabetes.
- Researchers found in an animal model that oral dosing of 20 mg/kg Pterostilbene significantly decreased plasma glucose levels by 42% and body weight by 20% (22).
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Further research showed that treatment with oral 40 mg/kg of Pterostilbene for six weeks produced a notable decrease in plasma glucose levels by 56.54% and an increase in plasma insulin levels (23).
The authors concluded that the effects of Pterostilbene were comparable to the experimental effects of 500 mg/kg oral metformin in a streptozocin induced Diabetes mellitus model.
- A possible suggested mechanism for the antidiabetic effects exerted by Pterostilbene is through the reduction of oxidative stress. Research has indicated that Pterostilbene significantly increased the activity of five key antioxidant enzymes (24).
- Pterostilbene demonstrated anti-obesity properties by upregulating adiponectin and downregulating leptin, indicating an anti-lipogenic effect (25).
Neurological Disorders
Studies show that consumption of berries rich in antioxidants may effectively slow neurological deterioration associated with aging (26, 27).
- Research at Tufts University, Boston showed that Pterostilbene fed aged rats performed better on cognitive and motor tasks compared to controls in a dose-dependent manner. Specifically, aged rats treated with Pterostilbene had higher level water maze test performance (28).
- Pterostilbene fed mice showed improved performance in arm water maze test and significant changes in factors such as tau that play an important role in the pathology of Alzheimer’s Disease (29).
- Pterostilbene-induced upregulation of brain receptors may have potential clinical benefits since theseagonists have been shown to confer central nervous system protection and be therapeutic after stroke (30).
It is unclear whether these results can be replicated in humans with regards to Alzheimer’s, Parkinson’s and strokes. However, researchers are encouraged by Pterostilbene’s potential to ameliorate the effects of free radicals and oxidative stress.
In summary it can be said that Pterostilbene exhibits notable anticancer mechanisms which include reduction of proliferation rates, induction of apoptosis, alteration of the cell cycle, and inhibition of metastasis in breast, esophageal, stomach, colon, liver, pancreatic, and prostate cancer studies (31).
Further areas of research include neuroprotection, inhibition of malignancy, attenuation of atherosclerosis, protection against hemolysis and liver disease, and metabolic regulation of diabetes and hyperlipidemia, however larger human trials are needed for more a more conclusive understanding of its effectiveness, safety and applicability to these wide ranging conditions.
References:
1. Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethylether analog, pterostilbene, in rats
2. Association between pterostilbene and quercetin inhibits metastatic activity of B16 melanoma. Neoplasia
3. In vitro evaluation of the cytotoxic, anti-proliferative and anti-oxidant properties of pterostilbene isolated from Pterocarpus marsupium.
https://www.ncbi.nlm.nih.gov/pubmed/20152895
4. Pterostilbene inhibits breast cancer in vitro through mitochondrial depolarization and induction of caspase-dependent apoptosis.
https://www.ncbi.nlm.nih.gov/pubmed/20031172
5. Pterostilbene and tamoxifen show an additive effect against breast cancer in vitro
https://www.ncbi.nlm.nih.gov/pubmed/21056131
6. Genomic analysis of pterostilbene predicts its antiproliferative effects against pancreatic cancer in vitro and in vivo.
https://www.ncbi.nlm.nih.gov/pubmed/22450950
7. Effects of pterostilbene on melanoma alone and in synergy with inositol hexaphosphate.
https://www.ncbi.nlm.nih.gov/pubmed/19887199
8. Pterostilbene inhibits lung cancer through induction of apoptosis.
https://www.ncbi.nlm.nih.gov/pubmed/20031166
9. Pterostilbene induce autophagy on human oral cancer cells through modulation of Akt and mitogen-activated protein kinase pathway.
https://www.ncbi.nlm.nih.gov/pubmed/25883032
10. Pterostilbene from Vitis coignetiae protect H2O2-induced inhibition of gap junctional intercellular communication in rat liver cell line.
https://www.ncbi.nlm.nih.gov/pubmed/19101604
11. Cytotoxic and antioxidant effects of methoxylated stilbene analogues on HepG2 hepatoma and Chang liver cells: implications for structure activity relationship
https://www.ncbi.nlm.nih.gov/pubmed/20385705
12. Pterostilbene from Vitis coignetiae protect H2O2-induced inhibition of gap junctional intercellular communication in rat liver cell line.
https://www.ncbi.nlm.nih.gov/pubmed/19101604/
13. Pterostilbene ameliorates tumor necrosis factor alpha-induced pancreatitis in vitro.
https://www.ncbi.nlm.nih.gov/pubmed/22954523/
14. Blueberry-enriched diet protects rat heart from ischemic damage
https://www.ncbi.nlm.nih.gov/pubmed/19536295/
15. Dietary blueberries attenuate atherosclerosis in apolipoprotein E-deficient mice by upregulating antioxidant enzyme expression
https://www.ncbi.nlm.nih.gov/pubmed/20660283/
16. The autophagy-lysosome pathway: a novel mechanism involved in the processing of oxidized LDL in human vascular endothelial cells
https://www.ncbi.nlm.nih.gov/pubmed/20223224/
17. Endothelial apoptosis induced by oxidative stress through activation of NF-kappaB: antiapoptotic effect of antioxidant agents on endothelial cells.
https://www.ncbi.nlm.nih.gov/pubmed/11463759/
18. Pterostilbene protects vascular endothelial cells against oxidized low-density lipoprotein-induced apoptosis in vitro and in vivo
https://www.ncbi.nlm.nih.gov/pubmed/21928089/
19. Effect of daily fruit ingestion on angiotensin converting enzyme activity, blood pressure, and oxidative stress in chronic smokers
https://www.ncbi.nlm.nih.gov/pubmed/16298751/
20. Inhibition of cancer cell proliferation and suppression of TNF-induced activation of NFkappaB by edible berry juice
https://www.ncbi.nlm.nih.gov/pubmed/17465224/
21. Biological/chemopreventive activity of stilbenes and their effect on colon cancer
https://www.ncbi.nlm.nih.gov/pubmed/18843589/
22. Antihyperglycemic activity of phenolics from Pterocarpus marsupium.
https://www.ncbi.nlm.nih.gov/pubmed/9214733/
23. The antioxidant role of pterostilbene in streptozotocin-nicotinamide-induced type 2 diabetes mellitus in Wistar rats
https://www.ncbi.nlm.nih.gov/pubmed/17132211/
24. Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters.
https://www.ncbi.nlm.nih.gov/pubmed/15853379/
26. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging.
https://www.ncbi.nlm.nih.gov/pubmed/18954071/
27. Blueberry supplementation enhances signaling and prevents behavioral deficits in an Alzheimer disease model
https://www.ncbi.nlm.nih.gov/pubmed/12793519/
28. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging.
https://www.ncbi.nlm.nih.gov/pubmed/18954071/
29. Low-dose pterostilbene, but not resveratrol, is a potent neuromodulator in aging and Alzheimer’s disease
https://www.ncbi.nlm.nih.gov/pubmed/21982274/
30. Anti-apoptotic actions of PPAR-gamma against ischemic stroke
https://www.ncbi.nlm.nih.gov/pubmed/20127524/
31. Pterostilbene and cancer: current review
https://www.ncbi.nlm.nih.gov/pubmed/22099605/