Pine Bark Extract Research Articles

Nutraceutical composition of three pine bark extracts and their antiproliferative effect on Caco-2 cells

The use of vegetal materials that go unused or by-products of the food industry, for the development of functional foods is very interesting. Pine bark extracts have been useful in medicine and in functional foods, yet, little is known about its antiproliferative properties. In this work, the activity of bark extracts from different Pinus species on human colorectal adenocarcinoma (Caco-2) cells was studied. All these extracts induce cell-cycle arrest and apoptosis in Caco-2 cells through alteration of the mitochondrial membrane potential, release of cytochrome c to cytoplasm and caspase 3 activation. In addition, a significant decrease in ROS generation was also observed in the presence of the extracts tested. The results obtained in this work show that these extracts could be interesting in order to elaborate functional foods and not only for improving their antioxidant properties but also for playing an important role in the treatment of colorectal carcinoma.

Exterior grade plywood adhesives based on pine bark polyphenols and hexamine

The aim of this work was to formulate environmental friendly adhesives for plywood production. This adhesive is based on polyphenol extracts from Pinus radiata D. Don bark, the most important by-product from the Chilean forest industry. We focused on a bio-based formulation free of formaldehyde, phenol, and isocyanates. Hexamethylenetetramine was used as hardener. The influence of pH on gel time, rheological behaviour, and pot life was evaluated. The curing process was evaluated by differential scanning calorimetry, Fourier transform infrared spectroscopy, and automatic bonding evaluation system (ABES). For the first time, exterior grade plywood (EN 314) was manufactured with pine bark extracts obtained at pilot scale. Two alternatives for adhesive application were studied: (1) wood veneers activation using a diluted solution of the bio-adhesive, and (2) pine bark extract application as dry powder on the wood veneers. Both alternatives were not reported before and demonstrated an increase in the final plywood quality, as measured by the internal bond strength (IB). On basis of this research, pine bark from Chilean forest industry is an interesting polyphenolic source for the development of adhesives free of formaldehyde and phenol.

The effect of different solvents on extraction yield, total phenolic content and antioxidant activity of extracts from pine bark (pinus pinaster subsp. atlantica)

Pine bark extracts are a rich source of natural polyphenols with potential beneficial antioxidant properties. The extraction yield, antioxidant activity, as well the type of polyphenols recovered not only depend on the extraction method but also on the solvent used for extraction.Thus, the aim of the present study was to ascertain the effect of different solvents on extraction yield, total phenolic content and antioxidant activity of extracts from Pinus pinaster subsp. atlantica, the major forest biomass of Northwest of Portugal.Soxhlet extractions with water, water/ethanol (1/1) and just ethanol, as solvents, were performed for 4 hours. Best results were obtained with the water/ethanol mixture. Overall, the solvent’s performance was as follows: water/ethanol> ethanol> water.

Immediate-release methylphenidate for attention deficit hyperactivity disorder (ADHD) in adults

Immediate-release methylphenidate for attention deficit hyperactivity disorder (ADHD) in adults

Neuroprotective Effects of Korean Red Pine (Pinus densiflora) Bark Extract and Its Phenolics.

Korean red pine (Pinus densiflora) is one of the major Pinus species in Korea. Red pine bark is removed prior to the chipping process in the wood industry and discarded as waste. However, red pine bark contains a considerable amount of naturally occurring phenolics, including flavonoids, and therefore may have a variety of biological effects. In this study, we investigated if Korean red pine bark extract (KRPBE) could protect neuronal PC-12 cells from oxidative stress and inhibit cholinesterase activity. Analysis of reversed-phase high-performance liquid chromatography results revealed four phenolics in KRPBE: vanillin, protocatechuic acid, catechin, and taxifolin. The total phenolic and flavonoid contents of KRPBE were 397.9 mg gallic acid equivalents/g dry weight (DW) and 248.7 mg catechin equivalents/g DW, respectively. The antioxidant capacities of KRPBE measured using ABTS, DPPH, and ORAC assays were 697.3, 521.8, and 2,627.7 mg vitamin C equivalents/g DW, respectively. KRPBE and its identified phenolics protected against H₂O₂-induced oxidative cell death in a dose-dependent manner. Acetylcholinesterase and butyrylcholinesterase, which degrade the neurotransmitter acetylcholine to terminate neurotransmission in synaptic clefts, were inhibited by treatment with KRPBE and its identified phenolics. Taken together, these results suggest that KRPBE and its constituent antioxidative phenolics are potent neuroprotective agents that can maintain cell viability under oxidative stress and inhibit cholinesterase activity.

Bio-based films prepared with soybean by-products and pine (Pinus densiflora) bark extract

The increasing awareness of environmental protection associated to plastic waste has promoted the developments of biopackaging in food industry. Pine (Pinus densiflora) bark extract (PBE) obtained from waste dry bark from lumber processing is a good source of oligomeric procyanidins and has excellent antioxidant activity. In this study, bio-based antioxidant films were prepared by incorporating different concentrations of PBE (0 20, 50, and 80 g kg−1) into soy protein isolate (SPI) matrix and analyzed in terms of structure, as well as physical, mechanical, and antioxidant properties. Scanning electron microscopy results suggested that the structures of the films with PBE were rougher. X-ray diffraction analysis indicated cross-linking interactions formed between the phenolic hydroxyl group in PBE and the amino groups in the SPI matrix. Thermogravimetric analysis indicated that PBE enhanced the thermal stability of the films. Moreover, the addition of 50 g kg−1 PBE decreased the moisture content, water vapor permeability, and oxygen permeability of the SPI films by 30.7%, 9.1%, and 31.6%, respectively. The PBE-containing films exhibited good light-barrier property. They also exhibited high tensile strength and low elongation at break. Furthermore, PBE markedly increased the antioxidant activity of the SPI films. Antioxidant SPI films with PBE have potential application in food packaging.

Inhibitory effects of Pycnogenol\xae, a pine bark extract, in a rat model of testosterone propionate-induced benign prostatic hyperplasia

Benign prostate hyperplasia (BPH) is a male reproductive disease that has gained increasing importance in recent years. The present study investigated whether Pycnogenol® (PYC), a standardized French maritime pine bark extract, could prevent BPH induced by testosterone propionate (TP) in rats. Male Sprague-Dawley rats were randomly divided into five groups of six rats. One group was used as a normal control rats and the other groups received subcutaneous injections of TP for 4 weeks to induce BPH. In the two treatment groups, PYC (20 or 40 mg/kg) was administered daily for 4 weeks by oral gavage concurrently with the induction of TP. All rats were sacrificed at the scheduled termination time, the prostates were weighed, and histopathologic examinations were conducted. Dihydrotestosterone (DHT) levels in serum and the prostate were measured, and the expression of proliferating cell nuclear antigen (PCNA) and Ki-67 proteins was investigated. BPH-treated animals showed increases in the relative weight of the prostate, higher concentrations of DHT in serum and the prostate, and higher expression of PCNA and Ki-67 in the prostate; in contrast, PYC-treated animals had significant reductions in these factors compared with the BPH animals. These findings indicated that PYC inhibited the development of BPH and that this was closely associated with a reduction in DHT concentration.

Review on Sustained Relief of Osteoarthritis Symptoms with a Proprietary Extract from Pine Bark, Pycnogenol.

This review summarizes the effects of the standardized proprietary bark extract of the French maritime pine (Pycnogenol®) in mild osteoarthritis (OA), stage 1 and 2. The extract exerts antioxidative, anti-inflammatory, and chondroprotective effects in vitro and in vivo. Its phenolic acids as well as catechin and taxifolin are quickly absorbed. Active metabolites, produced by gut microbiota in the intestinal tract from oligomeric procyanidins, appear in blood 6 h following ingestion and remain for at least 14 h, providing a long-lasting flow of anti-inflammatory substances for relief of OA symptoms. These constituents of Pycnogenol could be detected in serum, blood cells, and synovial fluid of OA patients. The resulting inhibition of cartilage-destructing proteases and pain-producing cyclo-oxygenases provides the basis for relief from pain, improvement of stiffness, enhanced mobility, and well-being in three clinical studies with the pine bark extract as an adjunct supplement. Sparing the use of nonsteroidal anti-inflammatory drugs, supplementation with the pine bark extract reduced gastric complications and hospital admissions of OA patients. Because of its favorable safety profile and sustained anti-inflammatory action, Pycnogenol represents an option as an add-on supplement for OA patients.

Corrigendum to "Inhibitory Effect of a French Maritime Pine Bark Extract-Based Nutritional Supplement on TNF-α-Induced Inflammation and Oxidative Stress in Human Coronary Artery Endothelial Cells".

[This corrects the article DOI: 10.1155/2015/260530.].

Effects of French Pine Bark Extract Chewing Gum on Oral Malodor and Salivary Bacteria.

Frequent or persistent malodor (halitosis) represents a considerable embarrassment to those affected. French pine bark extract, Pycnogenol® (PYC), has displayed antibacterial activity against a broad range of bacterial species. In the present study, anticipated benefits of PYC on diminishing halitosis were investigated. Ten healthy males and 11 females, aged 40.1±12.3 y, were recruited based on threshold breath sulfur compounds presence, diagnosed by portable gas chromatography. Subjects were randomly assigned to either sugar-free gums, or gums bearing an additional 2.5 mg PYC per piece. The subjects were required to consume two pieces of PYC or placebo gum six times daily for 15 min. The levels of volatile sulfur compounds (VSCs), measured by OralChromaTM, and tongue-coating score were recorded at baseline, 2, and 4 wk. Hydrogen sulfide-producing bacteria in saliva were cultured on Brucella blood agar plates containing 0.05% cysteine, 0.12% glutathione, and 0.02% lead acetate. The group consuming PYC chewing gum reduced exhaled hydrogen sulfide, methyl mercaptan and dimethyl sulfide significantly (p<0.01) after 2 wk versus baseline. Continuation of daily PYC-gum consumption for 4 wk remarkably lowered the tongue-coating score and exhaled hydrogen sulfide was significantly decreased compared to the placebo group. PYC chewing gum significantly reduced hydrogen sulfide-producing bacteria in saliva after 4 wk (p<0.01), with no effects observed in the placebo control. The results suggest that PYC chewing gum is effective in reducing oral malodor by decreasing the accumulation of tongue coating and the number of hydrogen sulfide-producing bacteria in saliva.

Evaluation of the systemic toxicity and mutagenicity of OLIGOPIN®, procyanidolic oligomers (OPC) extracted from French Maritime Pine Bark extract.

The potential systemic toxicity of Oligopin®, a French Maritime Pine Bark extract (FMPBE) rich in procyanidolic oligomers, was evaluated in an acute oral limit test and a 90-day repeated dose oral toxicity study with Sprague Dawley rats. The potential mutagenicity was assessed in a bacterial reverse mutation assay and in vitro mammalian chromosome aberration assay with human lymphocytes. The results indicate that Oligopin® was nongenotoxic in both bacterial and human cell assays, was not acutely toxic via oral administration at up to 2000 mg/kg and was well tolerated following 90 days of oral administration to SD rats, with a no observed adverse effect level of 1000 mg/kg/day. The lack of significant adverse systemic effects in the 90 day study is concordant with findings from several human clinical trials. The acute toxicity and mutagenicity data are consistent with data reported by AFSSA in a summary of FMPBE safety, in which a NOAEL of 100 mg/kg/day was established. In contrast, the NOAEL derived from the 90-day study with Oligopin® was 1000 mg/kg/day, suggesting that it is less systemically toxic than other FMPBE previously evaluated in subchronic studies, and comparable to proanthocyanidins extracted from grape seeds, which are widely used as nutritional supplement ingredients.

Cellular pharmacodynamic effects of Pycnogenol\xae in patients with severe osteoarthritis: a randomized controlled pilot study

BackgroundThe standardized maritime pine bark extract (Pycnogenol®) has previously shown symptom alleviating effects in patients suffering from moderate forms of knee osteoarthritis (OA). The cellular mechanisms for this positive impact are so far unknown. The purpose of the present randomized pilot controlled study was to span the knowledge gap between the reported clinical effects of Pycnogenol® and its in vivo mechanism of action in OA patients.MethodsThirty three patients with severe OA scheduled for a knee arthroplasty either received 100 mg of Pycnogenol® twice daily or no treatment (control group) three weeks before surgery. Cartilage, synovial fluid and serum samples were collected during surgical intervention. Relative gene expression of cartilage homeostasis markers were analyzed in the patients’ chondrocytes. Inflammatory and cartilage metabolism mediators were investigated in serum and synovial fluid samples.ResultsThe oral intake of Pycnogenol® downregulated the gene expression of various cartilage degradation markers in the patients’ chondrocytes, the decrease of MMP3, MMP13 and the pro-inflammatory cytokine IL1B were statistically significant (p ≤ 0.05). Additionally, protein concentrations of ADAMTS-5 in serum were reduced significantly (p ≤ 0.05) after three weeks intake of the pine bark extract.ConclusionsThis is the first report about positive cellular effects of a dietary supplement on key catabolic and inflammatory markers in patients with severe OA. The results provide a rational basis for understanding previously reported clinical effects of Pycnogenol® on symptom scores of patients suffering from OA.Trial registrationISRCTN10754119. Retrospectively registered 08/10/2015.

Influence of solvent additives on the aqueous extraction of tannins from pine bark: potential extracts for leather tanning

AbstractBACKGROUNDPine bark, which represents approximately 10 to 20% in weight of the tree trunk, is an abundant and low cost agro‐industrial waste. In order to obtain condensed tannin‐rich pine bark extracts (for future application in leather tanning/retanning processes), conventional aqueous extractions were performed, varying the type and amount of the solvent additive: sodium hydroxide (0.5, 1.0 and 1.5%, w/v), formic acid (0.5, 1.0 and 1.5%, v/v) and ethanol (5, 10 and 15%, v/v). Extractions were performed with and without the addition of sodium sulfite (1.0%, w/v).RESULTSThe most favorable solvent additive in terms of total phenolics and condensed tannins was ethanol: extracts achieved 34.8% of gallic acid equivalents and 62.8% of catechin monohydrate equivalents. Moreover, the favorable pH values (∼3.5) of the resultant aqueous solutions and their relatively low viscosities are suitable for subsequent tanning applications.CONCLUSIONSThe results of this study suggest that the high added‐value aqueous extracts of Pinus pinaster bark, which were achieved with small amounts of ethanol, have appropriate characteristics for leather tanning, and therefore they may be used as eco‐friendly tanning agents to partially replace chromium salts, thus reducing some of the environmental impacts typically associated with the leather industry. © 2017 Society of Chemical Industry

Cardioprotective effect of Pycnogenol in ischemic-reperfusion injury (IRI) in rats.

Oxidative stress plays a critical task in the biochemical and pathological alteration linked with myocardial ischemic-reperfusion injury (IRI). This warrants identifying agents with a potential for preventing such damage in an effective way. A novel plant based product, Pycnogenol, obtained from the French maritime pine (Pinus pinaster ssp. atlantica) bark extract was known for its tremendous antioxidant potential (both in vivo, in vitro). It was able to attenuate the symptoms of immune dysfunction through restoring a cellular antioxidant status in low micronutrient-induced immune deficient mice. Consequently, the present study was deals with the determination of protective effect of Pycnogenol in ischemic-reperfusion injury (IRI) in rats via Non-recirculating Langendorff's technique. The effect of Pycnogenol on the level of various key biomarkers in the rat heart homogenate was determined, such as, myocardial thiobarbituric acid reactive substances (TBARS, a marker of lipid peroxidation), lactic dehydrogenase (LDH) (a marker of tissue injury) and effect on endogenous antioxidants, e.g., superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx). The activity of these biomarkers appreciably improved in Pycnogenol-treated group than IRI group (P &lt; 0.05). The effect of Pycnogenol was further confirmed via histopathological examination of cardiac tissues, which suggests that, it considerably improved the injury related to tissue damage through suppression of edema and infiltration of neutrophil compared to IRI group. It also showed modulation of the expression of apoptotic factors, e.g. Bcl-2, bax and caspase-9 as confirmed by western blot analysis.

Downregulation of Hepatic De Novo Lipogenesis and Adipogenesis in Adipocytes by Pinus densiflora Bark Extract.

Korean red pine (Pinus densiflora) bark extract, PineXol (PX), was investigated for its potential antioxidant and anti-inflammation effects in vitro. It was hypothesized that PX treatment (25-150 μg/ml) would reduce the lipid synthesis in HepG2 hepatocytes as well as lipid accumulation in 3T3-L1 adipocytes. Hepatocytes' intracellular triglycerides and cholesterol were decreased in the PX 150 μg/ml treatment group compared with the control (p < 0.05). Consequently, de novo lipogenic proteins (acetyl-CoA carboxylase 1, stearoyl-CoA desaturase 1, elongase of very long chain fatty acids 6, glycerol-3-phosphate acyltransferase 1, and sterol regulatory element-binding protein 1) were significantly decreased in hepatocytes by PX 150 μg/ml treatment compared with the control (p < 0.05). In differentiated 3T3-L1 adipocytes, the lipid accumulation was significantly attenuated by all PX treatments (p < 0.01). Regulators of adipogenesis, including CCAAT-enhancer-binding proteins alpha, peroxisome proliferator-activated receptor gamma, and perilipin, were decreased in PX 100 μg/ml treatment compared with the control (p < 0.05). In conclusion, PX might have anti-obesity effects by blocking hepatic lipogenesis and by inhibiting adipogenesis in adipocytes.

P 154 - Diabetic skin and UV light: protection by Pinus halepensis pine bark extract

Diabetic skin is characterized by great sensitivity when compared to normal skin. Ultraviolet radiation is directly related to the oxidative stress affecting the skin. Diabetic skin, when compared to the normal one, is greatly damaged by ultraviolet radiation resulting in significant photoaging. Despite the fact that the long-term effect of UV light on normal skin has been partially investigated, for the diabetic skin data is missing. Antioxidants, such as Pinus halepensis seem to prevent photoaging. On the skin of hairless male diabetic mice the effects of UV radiation and the possible protection of Pinus halepensis pine bark extract topical application were studied, showing the significant antioxidant role of pine.

Distribution of Constituents and Metabolites of Maritime Pine Bark Extract (Pycnogenol®) into Serum, Blood Cells, and Synovial Fluid of Patients with Severe Osteoarthritis: A Randomized Controlled Trial.

The present randomized controlled study aimed to investigate the in vivo distribution of constituents or metabolites of the standardized maritime pine bark extract Pycnogenol®. Thirty-three patients with severe osteoarthritis scheduled for a knee arthroplasty were randomized to receive either 200 mg per day Pycnogenol® (P+) or no treatment (Co) over three weeks before surgery. Serum, blood cells, and synovial fluid samples were analyzed using liquid chromatography coupled to tandem mass spectrometry with electrospray ionization (LC-ESI/MS/MS). Considerable interindividual differences were observed indicating pronounced variability of the polyphenol pharmacokinetics. Notably, the highest polyphenol concentrations were not detected in serum. Catechin and taxifolin primarily resided within the blood cells while the microbial catechin metabolite δ-(3,4-dihydroxy-phenyl)-γ-valerolactone, ferulic, and caffeic acid were mainly present in synovial fluid samples. Taxifolin was detected in serum and synovial fluid exclusively in the P+ group. Likewise, no ferulic acid was found in serum samples of the Co group. Calculating ratios of analyte distribution in individual patients revealed a simultaneous presence of some polyphenols in serum, blood cells, and/or synovial fluid only in the P+ group. This is the first evidence that polyphenols distribute into the synovial fluid of patients with osteoarthritis which supports rationalizing the results of clinical efficacy studies.

Pine Bark Extract Protects Against Oxidative Stress Induced By Recurrent Hypoglycemia In Rats.

Pine Bark Extract Protects Against Oxidative Stress Induced By Recurrent Hypoglycemia In Rats.

Pine bark extract (Pycnogenol\xae) suppresses cigarette smoke-induced fibrotic response via transforming growth factor-\u03b21/Smad family member 2/3 signaling

Chronic obstructive pulmonary diseases (COPD) is an important disease featured as intense inflammation, protease imbalance, and air flow limitation and mainly induced by cigarette smoke (CS). In present study, we explored the effects of Pycnogenol® (PYC, pine bark extract) on pulmonary fibrosis caused by CS+lipopolysaccharide (LPS) exposure. Mice were treated with LPS intranasally on day 12 and 26, followed by CS exposure for 1 h/day (8 cigarettes per day) for 4 weeks. One hour before CS exposure, 10 and 20 mg/kg of PYC were administered by oral gavage for 4 weeks. PYC effectively reduced the number of inflammatory cells and proinflammatory mediators caused by CS+LPS exposure in bronchoalveolar lavage fluid. PYC inhibited the collagen deposition on lung tissue caused by CS+LPS exposure, as evidenced by Masson’s trichrome stain. Furthermore, transforming growth factor-β1 (TGF-β1) expression and Smad family member 2/3 (Smad 2/3) phosphorylation were effectively suppressed by PYC treatment. PYC markedly reduced the collagen deposition caused by CS+LPS exposure, which was closely involved in TGF-β1/Smad 2/3 signaling, which is associated with pulmonary fibrotic change. These findings suggest that treatment with PYC could be a therapeutic strategy for controlling COPD progression.

Ameliorative effects of pine bark extract on cisplatin-induced acute kidney injury in rats

Objective: This study investigated the dose–response effects of pine bark extract (PBE, pycnogenol®) on oxidative stress-mediated apoptotic changes induced by cisplatin (Csp) in rats.Materials and methods: The ameliorating potential of PBE was evaluated after orally administering PBE at doses of 10 or 20 mg/kg for 10 days. Acute kidney injury was induced by a single intraperitoneal injection of Csp at 7 mg/kg on test day 5.Results: Csp treatment caused acute kidney injury manifested by elevated levels of serum blood urea nitrogen (BUN) and creatinine (CRE) with corresponding histopathological changes, including degeneration of tubular epithelial cells, hyaline casts in the tubular lumen, and inflammatory cell infiltration (interstitial nephritis). Csp also induced significant apoptotic changes in renal tubular cells. In addition, Csp treatment induced high levels of oxidative stress, as evidenced by an increased level of malondialdehyde, depletion of the reduced glutathione (GSH) content, and decreased activities of glutathione S-transferase, superoxide dismutase, and catalase in kidney tissues. On the contrary, PBE treatment lowered BUN and CRE levels and effectively attenuated histopathological alterations and apoptotic changes induced by Csp. Additionally, treatment with PBE suppressed lipid peroxidation, prevented depletion of GSH, and enhanced activities of the antioxidant enzymes in kidney tissue.Conclusions: These results indicate that PBE has a cytoprotective effect against oxidative stress-mediated apoptotic changes caused by Csp in the rat kidney, which may be attributed to both increase of antioxidant enzyme activities and inhibition of lipid peroxidation.