PTEROSTILBENE

A more highly absorbed and potentially more potent polyphenol than its cousin resveratrol. Often described as a source of beneficial effects in berries, grape extracts and more despite their relatively low levels in dietary sources.

There are very few clinical trials with published results, and even then there are mainly milder effects in vascualr health through lowering of blood pressure, but tendency to increase cholesterol at least in lower doses. A small study in 2018 combined with gymnema sylvestre showed postive influence in diabetes control.

TYPICAL ABSORPTION LEVELS

20 – 30%

EXAMPLES OF IMPROVED OUTCOMES

NO

PRE-DIAGNOSIS OR PREVENTION

NO

Highlighted Studies

LDL increased with pterostilbene monotherapy (17.1 mg/dL; P = 0.001) which was not seen with GE combination (P = 0.47). Presence of a baseline cholesterol medication appeared to attenuate LDL effects. Both systolic (−7.8 mmHg; P < 0.01) and diastolic blood pressure (−7.3 mmHg; P < 0.001) were reduced with high dose pterostilbene. Patients not on cholesterol medication (n = 51) exhibited minor weight loss with pterostilbene (−0.62 kg/m2; P = 0.012). Conclusion. P...

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the “VG” [pterostilbene + gymnema sylvestre] administration to type 2 diabetic patients with varying degrees of glycemia, lipidemia and oxidative stress provide an efficient alternative to conventional antidiabetic drugs… Significant decrease in biochemical markers viz., blood glucose, HbA1c, total cholesterol, triglycerides, LDL-cholesterol, and VLDL-cholesterol and higher values of HDL… Further, the formulation did not show any adverse effects on liver and kidney functions a...

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Growing evidence points to pterostilbene’s strong anti-inflammatory and anti-cancer capabilities, highlighting its potential as a treatment for inflammatory and cancer-related conditions. Its antioxidant and neuroprotective attributes further amplify its therapeutic promise. While preliminary clinical studies are encouraging, comprehensive and rigorous trials are imperative to thoroughly assess its therapeutic benefits and safety

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..our study clarifies that PTE is an effective antitumor agent for glioma cells in vivo and in vitro through inhibiting cell viability…and triggering mitochondria-mediated apoptosis.. In addition…our model demonstrated that intravenous injection of PTE can obviously inhibit tumor growth. Therefore, because of its higher bioavailability and ease of crossing the BBB, PTE offers a potential novel treatment for GBM patients.

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TABLE OF REFERENCES

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https://www.hindawi.com/journals/ecam/2014/459165/#resultsHuman study2.5This is the first comparison of pterostilbene on metabolic parameters in humans. There appears to be a direct benefit of pterostilbene on both SBP and DBP [blood pressure]. The reduction in SBP is comparable to other complementary and alternative medicine (CAM) regimens (including garlic, fish oil, and vitamin D). Although direct comparison studies have not been done, the reduction in DBP seems to surpass most CAM therapies (including coenzyme Q10, vitamin C, and melatonin)LDL increased with pterostilbene monotherapy (17.1 mg/dL; ) which was not seen with GE combination (). Presence of a baseline cholesterol medication appeared to attenuate LDL effects. Both systolic (−7.8 mmHg; ) and diastolic blood pressure (−7.3 mmHg; ) were reduced with high dose pterostilbene. Patients not on cholesterol medication () exhibited minor weight loss with pterostilbene (−0.62 kg/m2; ). Conclusion. Pterostilbene increases LDL and reduces blood pressure in adults
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0057542#abstract0Lab study1We demonstrated that pterostilbene (PTER), found in blueberries, had greater increase in MTA1-mediated p53 acetylation, confirming superior potency over resveratrol as dietary epigenetic agent. In orthotopic PCa xenografts, resveratrol and PTER significantly inhibited tumor growth, progression, local invasion and spontaneous metastasis. Furthermore, MTA1-knockdown sensitized cells to these agents resulting in additional reduction of tumor progression and metastasis. The reduction was dependent on MTA1 signaling showing increased p53 acetylation, higher apoptotic index and less angiogenesis in vivo in all xenografts treated with the compounds, and particularly with PTERIn conclusion, we demonstrated that dietary stilbenes are effective regulators of MTA1/NuRD mediated p53 acetylation, apoptosis and angiogenesis in PCa xenografts. This novel epigenetic signaling provides the first mechanistic evidence of MTA1 as a potential therapeutic target in PCa. MTA1 has the additional advantage of being sensitive to pharmacologically safe dietary compounds. We propose, for the first time, on the basis of strong pre-clinical evidence, that PTER is a lead compound for potent target-specific treatment of MTA1-overexpressing advanced PCa. Our findings substantiate new approaches in PCa management with the inclusion of natural product drugs not only for primary chemoprevention [48] but for anticancer and antimetastatic therapy.Screenshot from 2023-11-29 16-40-21
https://www.nature.com/articles/srep15239Lab study1Stilbenes, including resveratrol and pterostilbene (PT), are a class of naturally occurring phenolic compounds that exhibit a wide spectrum of biological functions including anticancer activity9,10,11. Berries are considered a rich source for PT and its abundance varies between different types of berries. Some varieties of blueberries contain up to 15 μg PT per 100 gm (1 cup) of berries12. PT is a structural analogue to resveratrol and is characterized by the presence of 2 methoxy groups instead of the hydroxyl groups of resveratrol13. PT was reported to be superior to resveratrol in suppressing the formation of aberrant foci in a mouse model of azoxymethane-induced colon carcinogenesis14. Moreover, PT surpasses resveratrol in its inhibition for the DNA synthesis as well as suppressing pro-inflammatory mediators (iNOS and COX-2) in colon cancer cellsTreatment of cells with PT increased cleaved PARP levels in Caco-2 to a greater extent compared to HCT-116. Combined treatment significantly increased cleaved PARP levels in Caco-2 compared to 5-FU-alone. This is concordant with the observed effects of PT on the apoptosis markers (Bax/Bcl-2 ratio and the percent of cells at the pre-G phase) in Caco-2 cells. In summary, it could be concluded from these studies that, PT synergizes the cytotoxic effects of 5-FU in Caco-2 colon cancer cells. PT exhibited higher potency in Caco-2 cells, which express higher levels of ER-β, compared to HCT-116. These results provide a rationale for novel combination treatment strategies, especially for patients with 5-FU-resistant tumors expressing ER-β protein.Screenshot from 2023-11-29 16-59-31
https://www.oncotarget.com/article/23390/text/Lab study1To achieve the maximum anti-tumor effect from available Vit. E analogs, a natural compound, PS, was investigated for its synergistic pharmacological effects. In summary, this study shows that α-TOS and PS synergistically suppressed breast cancer cell proliferation and tumor growth in vitro and in vivo through the inhibition of downstream AP1 activation and cell cycle protein regulation. In addition, our recently developed CTC detection assay was used to show that the combination of α-TOS and PS largely suppressed the invasion ability of MDA-MB-231 cells in a xenograft animal model. These results suggest that a combination of Vit. E and PS as dietary supplements may be beneficial during breast cancer treatment.Treatment with blueberry extract significantly decreased signaling transduction of the PI3K/AKT pathway and resulted in the inhibition of breast carcinogenesis. Similar to blueberry extract, in the current study, PS exposure inhibited carcinogenic pathways in breast cancer cells (MDA-MB-231) but not in normal breast epithelial cells (MCF-10A), indicating that PS may be the primary agent responsible for the anti-carcinogenic effects of blueberry extract in several malignancies, especially breast cancer [37]. The daily amount of PS consumption can vary according to fruit intake, and the PS content per blueberry has been estimated to vary from 99 to 520 ng/g depending on the type of berry selected [38].Screenshot from 2023-11-29 17-12-50
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0057542Lab study1we demonstrated that dietary stilbenes are effective regulators of MTA1/NuRD mediated p53 acetylation, apoptosis and angiogenesis in PCa xenografts. This novel epigenetic signaling provides the first mechanistic evidence of MTA1 as a potential therapeutic target in PCa. MTA1 has the additional advantage of being sensitive to pharmacologically safe dietary compounds. We propose, for the first time, on the basis of strong pre-clinical evidence, that PTER is a lead compound for potent target-specific treatment of MTA1-overexpressing advanced PCa. Our findings substantiate new approaches in PCa management with the inclusion of natural product drugs not only for primary chemoprevention .. but for anticancer and antimetastatic therapy.We detected higher serum levels of PTER compared to resveratrol in both EV and MTA1-knockdown groups. Previous studies have also shown higher bioavailability for PTER [40]–[43] which was attributed to the replacement of two hydroxy by methoxy groups making PTER more lipophilic and more stable [44]. In addition, PTER’s half-life is several times longer than resveratrol’s [45]. Better bioavailability of PTER could explain its greater in vivo activity compared to resveratrol observed by us and others [46]. In the latter study, authors compared the anticancer effects of PTER and resveratrol in colon cancer in vivo and found PTER to be a more potent anticarcinogen and anti-inflammatory agent [46]. Pterostilbene has been shown to inhibit micrometastasis in colon, breast, melanoma, pancreatic and hepatocellular carcinoma [43]. In PCa, the anticancer activity of PTER has been shown in vitro using LNCaP and PC3 cells [33], [47]. Our current study is the first to demonstrate in vivo anticancer and antimetastatic effects of PTER in PCa
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3174855/Lab study1Importantly, the dosage used in these studies was nontoxic and may be considered physiologic, because the human equivalent dose of the 5% BB diet (based on body surface area) (59) is 300 g (10.6 oz.) of fresh BB (~ 2 cups/d). Future clinical trials using whole BB powder are planned that will aid in the determination of a suitable human dose. It is our hope that the knowledge gained from this study may aid in the design of future dietary strategies for the prevention of TNBC.In this study, tumor volume was 75% lower in mice fed the 5% BB diet and 60% lower in mice fed the 10% BB diet than in control mice (P ≤ 0.05). Tumor cell proliferation (Ki-67) was lower in the 5 and 10% BB-fed mice and cell death (Caspase 3) was greater in the 10% BB-fed mice compared to control mice (P ≤ 0.05). Gene analysis of tumor tissues from the 5% BB-fed mice revealed significantly altered expression of genes important to inflammation, cancer, and metastasis, specifically, Wnt signaling, thrombospondin-2, IL-13, and IFNγ

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