Pycnogenol Overview

1) Conditions Studied

Pycnogenol has been studied for a variety of health conditions, including:

• Chronic venous insufficiency
• Hypertension (high blood pressure)
• Osteoarthritis
• Diabetes
• Erectile dysfunction
• Asthma
• Attention Deficit Hyperactivity Disorder (ADHD)
• Menopausal symptoms
• Skin aging

2) Efficacy in Treating Conditions

Research on Pycnogenol's effectiveness for these conditions has shown mixed results:

• There is some evidence suggesting it may help reduce symptoms of chronic venous insufficiency and osteoarthritis.
• For conditions like hypertension and diabetes, Pycnogenol may contribute to modest improvements in some individuals.
• Studies on ADHD, menopausal symptoms, and skin health indicate potential benefits, but more research is needed to confirm these findings.
• The effectiveness of Pycnogenol for erectile dysfunction and asthma is not well established and needs further investigation.

3) Health Benefits

Pycnogenol is known for its antioxidant properties and may offer several health benefits, including:

• Improving endothelial function and circulation
• Anti-inflammatory effects
• Supporting skin health by protecting collagen and elastin from degradation
• Reducing blood glucose levels
• Enhancing cognitive function

4) Potential Downsides

While Pycnogenol is generally considered safe, there are some potential downsides to consider:

• Some individuals may experience mild side effects such as dizziness, gut problems, or headaches.
• There may be interactions with certain medications, particularly blood thinners and immunosuppressants.
• Pregnant and breastfeeding women should avoid using Pycnogenol as there is insufficient evidence regarding its safety in these populations.

5) Genetic Variations

As of the current knowledge cutoff date, there is limited research on the relationship between genetic variations and the effects of Pycnogenol. However, individual responses to supplements can be influenced by genetic makeup, and certain genetic variations could theoretically impact how well someone responds to Pycnogenol. More research is needed in this area to draw any firm conclusions.

Summary of Research on Pycnogenol

Pycnogenol, a dietary supplement derived from the bark of the maritime pine tree, has been studied for its potential in treating a variety of health conditions. It is known for its antioxidant properties and has been shown to have therapeutic potential in the prevention and treatment of degenerative diseases.

Analysis of Pycnogenol Supplements

High-performance liquid chromatography (HPLC) was used to analyze Pycnogenol supplements, revealing the presence of four key components. Variability was detected among commercially available supplements, with some differing from the standard extract due to additional substances or manufacturing quality control issues.

Binding to Human Plasma Proteins

Pycnogenol compounds, particularly flavonoids like catechin and taxifolin, have high binding affinities to plasma proteins. This binding characteristic contributes to a better understanding of its bioactivity as a complex plant supplement.

Absorption and Metabolism in Humans

Pycnogenol components are quickly absorbed and metabolized in the human body, with various components detectable in plasma over a 14-hour period. This comprehensive analysis of pharmacokinetics provides insights into Pycnogenol's therapeutic potential.

Anti-inflammatory Effects

A metabolite of Pycnogenol, known as M1, demonstrates significant inhibitory effects on nitrite production and iNOS expression, indicating its potential for in vivo anti-inflammatory action despite low plasma concentrations.

Urinary Excretion of Metabolites

Following oral intake of Pycnogenol, metabolites such as ferulic acid and taxifolin are excreted in urine, suggesting that procyanidins are metabolized by humans, with complete excretion within 28-34 hours.

Effects on Chronic Venous Insufficiency (CVI)

Pycnogenol has been found to be more effective than Daflon in reducing symptoms of CVI, indicating rapid clinical efficacy and potential as a treatment for CVI and related microangiopathy.

Vascular Health and Hypertension

Studies indicate that Pycnogenol can stimulate the production of nitric oxide by vascular endothelial cells, enhancing endothelium-dependent vasodilation, and may benefit patients with mild hypertension by allowing a reduction in the dosage of calcium antagonist nifedipine.

Conclusion

The research collectively provides evidence of Pycnogenol's bioavailability, plasma protein binding characteristics, and potential anti-inflammatory and therapeutic effects. These findings support the use of Pycnogenol as a supplement for improving various health outcomes, including endothelial function, CVI, and hypertension management.

References:

1. Chromatographic fingerprint analysis of Pycnogenol dietary supplements
2. Plasma protein binding of polyphenols from maritime pine bark extract (USP)
3. Single and multiple dose pharmacokinetics of maritime pine bark extract (pycnogenol) after oral administration to healthy volunteers
4. Facilitated cellular uptake and suppression of inducible nitric oxide synthase by a metabolite of maritime pine bark extract (Pycnogenol)
5. Urinary metabolites of French maritime pine bark extract in humans
6. Green tea flavan-3-ols: colonic degradation and urinary excretion of catabolites by humans
7. A comparison of the in vitro biotransformation of (-)-epicatechin and procyanidin B2 by human faecal microbiota
8. Studies on flavonoid metabolism. Absorption and metabolism of (+)-catechin in man
9. Bioavailability of dietary flavonoids and phenolic compounds
10. Antioxidant activity and inhibition of matrix metalloproteinases by metabolites of maritime pine bark extract (pycnogenol)
11. The role of natural antioxidants in preserving the biological activity of endothelium-derived nitric oxide
12. Endothelium-dependent vascular effects of Pycnogenol
13. Pycnogenol, French maritime pine bark extract, augments endothelium-dependent vasodilation in humans
14. Pycnogenol, French maritime pine bark extract, improves endothelial function of hypertensive patients
15. Synthesis and biological activity of the tea catechin metabolites, M4 and M6 and their methoxy-derivatives
16. Grape-seed procyanidins act as antiinflammatory agents in endotoxin-stimulated RAW 264.7 macrophages by inhibiting NFkB signaling pathway
17. Effects of naturally occurring flavonoids on nitric oxide production in the macrophage cell line RAW 264.7 and their structure-activity relationships
18. Inhibitory effects of anthocyanins and other phenolic compounds on nitric oxide production in LPS/IFN-gamma-activated RAW 264.7 macrophages
19. Modulatory effects of Pycnogenol in a rat model of insulin-dependent diabetes mellitus: biochemical, histological, and immunohistochemical evidences
20. Pycnogenol attenuates the inflammatory and nitrosative stress on joint inflammation induced by urate crystals
21. Single and multiple dose pharmacokinetics of maritime pine bark extract (pycnogenol) after oral administration to healthy volunteers
22. Ferulic acid excretion as a marker of consumption of a French maritime pine (Pinus maritima) bark extract
23. Anaerobic degradation of flavonoids by Clostridium orbiscindens
24. Glucose and blood pressure lowering effects of Pycnogenol® are inefficient to prevent prolongation of QT interval in experimental diabetic cardiomyopathy
25. Effects of Pycnogenol on endothelial function in patients with stable coronary artery disease: a double-blind, randomized, placebo-controlled, cross-over study
26. Chronic venous insufficiency and varicose veins of the lower extremities
27. Comparison of Pycnogenol and Daflon in treating chronic venous insufficiency: a prospective, controlled study
28. Pycnogenol in chronic venous insufficiency
29. PYCNOGENOL in chronic venous insufficiency
30. Comparative study of Venostasin and Pycnogenol in chronic venous insufficiency
31. Venous ulcers: microcirculatory improvement and faster healing with local use of Pycnogenol
32. Pycnogenol for chronic venous insufficiency
33. Improvement in cochlear flow with Pycnogenol® in patients with tinnitus: a pilot evaluation
34. Improvement in symptoms and cochlear flow with pycnogenol in patients with Meniere's disease and tinnitus
35. Pycnogenol, French maritime pine bark extract, improves endothelial function of hypertensive patients
36. Reduction of cardiovascular risk factors in subjects with type 2 diabetes by Pycnogenol supplementation
37. Effects of Pycnogenol on endothelial function in patients with stable coronary artery disease: a double-blind, randomized, placebo-controlled, cross-over study
38. Effects of melatonin and Pycnogenol on small artery structure and function in spontaneously hypertensive rats
39. Reduction of myeloperoxidase activity by melatonin and pycnogenol may contribute to their blood pressure lowering effect
40. Does pycnogenol intensify the efficacy of acetylsalicylic acid in the inhibition of platelet function? In vitro experience
41. Supplementation with a pine bark extract rich in polyphenols increases plasma antioxidant capacity and alters the plasma lipoprotein profile
42. Comparative study of Venostasin and Pycnogenol in chronic venous insufficiency
43. Pycnogenol inhibits macrophage oxidative burst, lipoprotein oxidation, and hydroxyl radical-induced DNA damage
44. Compulsory psychiatric treatment in the community. I. A controlled study of compulsory community treatment with extended leave under the Mental Health Act: special characteristics of patients treated and impact of treatment
45. Impact of plant extracts tested in attention-deficit/hyperactivity disorder treatment on cell survival and energy metabolism in human neuroblastoma SH-SY5Y cells
46. Treatment of ADHD with French maritime pine bark extract, Pycnogenol
47. Urinary catecholamines in children with attention deficit hyperactivity disorder (ADHD): modulation by a polyphenolic extract from pine bark (pycnogenol)
48. Pycnogenol® supplementation improves cognitive function, attention and mental performance in students
49. An experimental comparison of Pycnogenol and methylphenidate in adults with Attention-Deficit/Hyperactivity Disorder (ADHD)
50. Supplementation with Pycnogenol® improves signs and symptoms of menopausal transition
51. Nuclear factor kappa B--molecular biomedicine: the next generation
52. The involvement of matrix metalloproteinase-9 in airway inflammation of patients with acute asthma
53. Novel and therapeutic effect of caffeic acid and caffeic acid phenyl ester on hepatocarcinoma cells: complete regression of hepatoma growth and metastasis by dual mechanism
54. Relaxin induces matrix metalloproteinase-9 through activation of nuclear factor kappa B in human THP-1 cells
55. Spinal NF-kB activation induces COX-2 upregulation and contributes to inflammatory pain hypersensitivity
56. Inhibition of COX-1 and COX-2 activity by plasma of human volunteers after ingestion of French maritime pine bark extract (Pycnogenol)
57. Toll-like receptor signaling pathways
58. Pycnogenol attenuates atherosclerosis by regulating lipid metabolism through the TLR4-NF-κB pathway
59. Pycnogenol, an extract from French maritime pine, suppresses Toll-like receptor 4-mediated expression of adipose differentiation-related protein in macrophages
60. Pycnogenol Protects Against Rotenone-Induced Neurotoxicity in PC12 Cells Through Regulating NF-κB-iNOS Signaling Pathway
61. Pycnogenol Reduces Toll-Like Receptor 4 Signaling Pathway-Mediated Atherosclerosis Formation in Apolipoprotein E-Deficient Mice
62. Toll-Like Receptor-Dependent Immunomodulatory Activity of Pycnogenol®
63. Treatment of osteoarthritis with Pycnogenol. The SVOS (San Valentino Osteo-arthrosis Study). Evaluation of signs, symptoms, physical performance and vascular aspects
64. A randomized, double-blind, placebo-controlled exploratory study to evaluate the potential of pycnogenol for improving allergic rhinitis symptoms
65. Pycnogenol inhibits immunoglobulin E-mediated allergic response in mast cells
66. Brain-Gut Axis: Clinical Implications
67. Treatment of irritable bowel syndrome
68. Irritable bowel syndrome: the clinical approach
69. Pycnogenol® supplementation improves the control of irritable bowel syndrome symptoms
70. A review of the French maritime pine bark extract (Pycnogenol), a herbal medication with a diverse clinical pharmacology
71. The effect of pycnogenol on patients with dysmenorrhea using low-dose oral contraceptives
72. Clinical and immunological parameters of Sjögren's syndrome
73. Efficacy of Pycnogenol® supplementation in remission phases of Sjögren syndrome
74. Behçet's syndrome: pulmonary vascular disease
75. Behçet syndrome: effects of Pycnogenol® supplementation during regression phases
76. Review on Sustained Relief of Osteoarthritis Symptoms with a Proprietary Extract from Pine Bark, Pycnogenol
77. Treatment of osteoarthritis with Pycnogenol. The SVOS (San Valentino Osteo-arthrosis Study). Evaluation of signs, symptoms, physical performance and vascular aspects
78. Effect of pine bark extract (Pycnogenol) on symptoms of knee osteoarthritis
79. Pycnogenol® inhibits lipid accumulation in 3T3-L1 adipocytes with the modulation of reactive oxygen species (ROS) production associated with antioxidant enzyme responses
80. Stimulation of lipolysis by pycnogenol
81. Pycnogenol stimulates lipolysis in 3t3-L1 cells via stimulation of beta-receptor mediated activity
82. Effect of pycnogenol on glucose transport in mature 3T3-L1 adipocytes
83. Antioxidant activity and biologic properties of a procyanidin-rich extract from pine (Pinus maritima) bark, pycnogenol
84. Hydroxyl and superoxide anion radical scavenging activities of natural source antioxidants using the computerized JES-FR30 ESR spectrometer system
85. Pharmaceutical and nutraceutical effects of Pinus pinaster bark extract
86. The effect of Pycnogenol on the erythrocyte membrane fluidity
87. Ferritin oxidation and proteasomal degradation: protection by antioxidants
88. Pycnogenol protects vascular endothelial cells from t-butyl hydroperoxide induced oxidant injury
89. In vitro testing of antioxidants and biochemical end-points in bovine retinal tissue
90. Pycnogenol and Ginkgo biloba extract: effect on peroxynitrite-oxidized sarcoplasmic reticulum Ca-ATPase
91. Oligomeric procyanidins of French maritime pine bark extract (Pycnogenol) effectively inhibit alpha-glucosidase
92. French maritime pine bark extract Pycnogenol dose-dependently lowers glucose in type 2 diabetic patients
93. Clinical assessment of a supplement of Pycnogenol® and L-arginine in Japanese patients with mild to moderate erectile dysfunction
94. Reduction of cardiovascular risk factors in subjects with type 2 diabetes by Pycnogenol supplementation
95. Pycnogenol((R)) in the Management of Asthma
96. Pycnogenol® improvements in asthma management
97. Hepatoprotective effects of pycnogenol in a rat model of non-alcoholic steatohepatitis
98. Protective effects of Pycnogenol on hyperglycemia-induced oxidative damage in the liver of type 2 diabetic rats
99. Investigation of a complex plant extract for mild to moderate erectile dysfunction in a randomized, double-blind, placebo-controlled, parallel-arm study
100. Treatment of erectile dysfunction with pycnogenol and L-arginine
101. Improvement of erectile function with Prelox: a randomized, double-blind, placebo-controlled, crossover trial
102. Pycnogenol® effects on skin elasticity and hydration coincide with increased gene expressions of collagen type I and hyaluronic acid synthase in women

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