Pterostilbene Overview

1) Conditions Studied for Pterostilbene Treatment

Pterostilbene has been studied for a range of conditions including high cholesterol, hypertension (high blood pressure), diabetes, cognitive decline, and oxidative stress-related diseases. It has also been researched for its potential anti-inflammatory and anticancer properties.

2) Effectiveness in Treating Conditions

While some studies suggest potential health benefits, the effectiveness of pterostilbene in treating specific medical conditions remains inconclusive. Some small-scale studies and animal research indicate possible benefits, but there is a need for more robust clinical trials to establish its efficacy in humans.

3) Health Benefits of Pterostilbene

• Antioxidant properties that may help in reducing oxidative stress and inflammation.
• Potential to improve cholesterol levels and cardiovascular health.
• May help regulate blood sugar levels and improve diabetes management.
• Could potentially enhance cognitive function and protect against age-related decline.

4) Downsides of Pterostilbene

Although pterostilbene is generally considered safe when consumed in amounts found in food, there can be downsides when taken in supplement form, such as:

• Potential interactions with medications, particularly those that are metabolized by the liver.
• Limited human studies on long-term safety and potential side effects.
• High doses may lead to undesirable effects such as gastrointestinal distress.

5) Pterostilbene and Genetic Variations

Research on pterostilbene and genetic variations is still emerging. Certain genetic polymorphisms may affect how individuals respond to pterostilbene, potentially influencing its metabolism and efficacy. However, more research is needed to fully understand these interactions and to determine if pterostilbene is particularly beneficial or harmful for specific genetic variations.

Pterostilbene Research Summary

Antioxidant Properties and Health Benefits

Pterostilbene, found predominantly in blueberries, exhibits potent antioxidant properties with high bioavailability. It is effective in cancer prevention, neurological disease modulation, anti-inflammatory actions, reduction of vascular disease, and improvement of diabetes. The compound's clinical potential for various disease mechanisms is significant.

Presence in Vaccinium Berries

Among Vaccinium berries, pterostilbene was identified in rabbiteye blueberry and deerberry, suggesting that these berries could be beneficial to health due to their content of bioactive compounds.

Anti-inflammatory Effects

Pterostilbene, a component of Pterocarpus marsupium (PM) extract, inhibits COX-2 without affecting COX-1, reducing the production of the pro-inflammatory molecule PGE2. Although human serum levels post-oral consumption were lower than the effective in vitro concentration, no adverse effects were observed, indicating safety and encouraging further research for inflammatory condition treatment.

Detection and Measurement

A new reversed phase high-performance liquid chromatography (RP-HPLC) method was developed to enhance the analysis of pterostilbene using cyclodextrins, successfully applied to analyze blueberries for pterostilbene content.

Pharmacokinetics and Bioavailability

Compared to resveratrol, pterostilbene demonstrated greater oral bioavailability and higher plasma levels, suggesting more potent biological activity in vivo.

Chemoprevention in Cancer Treatment

Structural factors of stilbene-based compounds, like pterostilbene, influence their cancer-chemopreventive properties, providing insights for new drug designs.

Cytotoxic and Antioxidant Activities

The cytotoxic and antioxidant activities of methoxylated stilbene analogues, such as pterostilbene, are attributed to their specific chemical structures, which have implications for liver cancer treatment.

Antioxidative Properties Against LDL Oxidation

Synthesized resveratrol analogues, including trans-stilbene derivatives, showed more effective antioxidative properties against LDL peroxidation than resveratrol itself, suggesting potential for cardiovascular disease prevention.

Metabolic Stability and Absorption

Methylated polyphenols like pterostilbene have improved metabolic stability and absorption, leading to higher oral bioavailability and potential as cancer chemopreventive agents.

Anticancer Potential

Pterostilbene inhibits the growth of prostate cancer cells, activates AMPK, induces cell cycle arrest, and promotes cell death, demonstrating its potential as a chemopreventive agent.

Neuroprotective Effects

Pterostilbene and other compounds found in blueberries reduce the release of inflammatory molecules in mouse microglia cells, suggesting a synergistic effect in combating inflammation.

Effective Dosages and Synergistic Effects

Higher concentrations of individual compounds like pterostilbene are needed to match the protective effects of blueberry extract, indicating the importance of the combined action of various compounds.

Anxiolytic Effects

Pterostilbene reduces anxiety-like behavior in mice and is associated with the down-regulation of certain kinases in the hippocampus, revealing its potential as a therapeutic agent for anxiety disorders.

References:

1. A review of pterostilbene antioxidant activity and disease modification
2. Resveratrol, pterostilbene, and piceatannol in vaccinium berries
3. Selective COX-2 inhibition by a Pterocarpus marsupium extract characterized by pterostilbene, and its activity in healthy human volunteers
4. Constituents of Pterocarpus marsupium: an ayurvedic crude drug
5. Development of a reversed phase high performance liquid chromatography method based on the use of cyclodextrins as mobile phase additives to determine pterostilbene in blueberries
6. Stilbene content of mature Vitis vinifera berries in response to UV-C elicitation
7. Simultaneous quantification of five major constituents in stems of Dracaena plants and related medicinal preparations from China and Vietnam by HPLC-DAD
8. Polyphenolic composition of roots and petioles of Rheum rhaponticum L
9. Biological activity of peanut (Arachis hypogaea) phytoalexins and selected natural and synthetic Stilbenoids
10. Structure-activity relationship of trans-resveratrol and its analogues
11. Cytotoxic and antioxidant effects of methoxylated stilbene analogues on HepG2 hepatoma and Chang liver cells: Implications for structure activity relationship
12. Structure-activity relationship studies of resveratrol and its analogues by the reaction kinetics of low density lipoprotein peroxidation
13. Specific structural determinants are responsible for the antioxidant activity and the cell cycle effects of resveratrol
14. Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethylether analog, pterostilbene, in rats
15. Resveratrol: a review of preclinical studies for human cancer prevention
16. Cyclodextrin-based device coatings for affinity-based release of antibiotics
17. Physicochemical study of the complexation of pterostilbene by natural and modified cyclodextrins
18. Pharmacokinetics of pterostilbene in Sprague-Dawley rats: the impacts of aqueous solubility, fasting, dose escalation, and dosing route on bioavailability
19. Methylated flavonoids have greatly improved intestinal absorption and metabolic stability
20. Determination of pterostilbene in rat plasma by a simple HPLC-UV method and its application in pre-clinical pharmacokinetic study
21. Activation of AMPK by pterostilbene suppresses lipogenesis and cell-cycle progression in p53 positive and negative human prostate cancer cells
22. Stilbenes and anthocyanins reduce stress signaling in BV-2 mouse microglia
23. Effects of resveratrol and its derivatives on lipopolysaccharide-induced microglial activation and their structure-activity relationships
24. Anxiolytic action of pterostilbene: involvement of hippocampal ERK phosphorylation
25. The role of the extracellular signal-regulated kinase signaling pathway in mood modulation
26. Cellular and behavioral effects of stilbene resveratrol analogues: implications for reducing the deleterious effects of aging
27. Pterostilbene on metabolic parameters: a randomized, double-blind, and placebo-controlled trial
28. Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters
29. Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha
30. Effect of pterostilbene on hepatic key enzymes of glucose metabolism in streptozotocin- and nicotinamide-induced diabetic rats
31. Antihyperglycemic activity of phenolics from Pterocarpus marsupium
32. Priming of the neutrophil NADPH oxidase activation: role of p47phox phosphorylation and NOX2 mobilization to the plasma membrane
34. The combined luminol/isoluminol chemiluminescence method for differentiating between extracellular and intracellular oxidant production by neutrophils
35. Structure-efficiency relationship in derivatives of stilbene. Comparison of resveratrol, pinosylvin and pterostilbene
36. Effect of stilbene derivative on superoxide generation and enzyme release from human neutrophils in vitro
37. Polyphenol derivatives - potential regulators of neutrophil activity
38. Decreased activity of neutrophils in the presence of diferuloylmethane (curcumin) involves protein kinase C inhibition
39. Suppression of oxidative burst in human neutrophils with the naturally occurring serotonin derivative isomer from Leuzea carthamoides
40. In vivo effect of pinosylvin and pterostilbene in the animal model of adjuvant arthritis
41. Notch-1 activation-dependent p53 restoration contributes to resveratrol-induced apoptosis in glioblastoma cells
42. Resveratrol induces Notch2-mediated apoptosis and suppression of neuroendocrine markers in medullary thyroid cancer
43. gamma-Secretase inhibitors abrogate oxaliplatin-induced activation of the Notch-1 signaling pathway in colon cancer cells resulting in enhanced chemosensitivity
44. Notch-1 signaling facilitates survivin expression in human non-small cell lung cancer cells
45. Pterostilbene exerts antitumor activity via the Notch1 signaling pathway in human lung adenocarcinoma cells
46. Identification of molecular pathways affected by pterostilbene, a natural dimethylether analog of resveratrol
47. Low-dose pterostilbene, but not resveratrol, is a potent neuromodulator in aging and Alzheimer's disease
48. Dietary administration of high doses of pterostilbene and quercetin to mice is not toxic
49. Analysis of safety from a human clinical trial with pterostilbene

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