Pine Bark Extract Research Articles

Editorial: Pine bark extract: nutrition and metabolism

Editorial: Pine bark extract: nutrition and metabolism

Assessing the effects of allelopathic properties of organic mulches on liverwort control in container-grown ornamentals

Liverwort (Marchantia polymorpha) is a problematic weed in ornamental crop production. The major limitation of liverwort control is lack of herbicide options inside greenhouses and their potential to cause injury. The current research was undertaken to study the effectiveness of allelopathic properties of six different organic mulches including rice hull (RH), cocoa hull (CH), pine bark (PB), maple leaf (ML), shredded cypress (SC), and red hardwood (HW) for liverwort control. Mulch extracts were prepared and used to impregnate agar media at an increasing dose at 1X (2 mL mulch extract), 2X (4 mL), 3X (6 mL), and 4X (8 mL) rates, in a randomized complete block design. Ten liverwort gemmae were transferred to each petri dish and they were maintained inside a growth chamber. The number of gemmae germinating in each petri dish after 1 week and gemmae surviving at the end of 2 weeks was recorded. In greenhouse study, mulch extracts were applied to containers filled with substrate for assessing liverwort control. The mulch extracts or no extract (control) were applied to the containers uniformly at 1X (15 mL), 2X (30 mL), 3X (45 mL) or 4X (60 mL) rates, in a randomized complete block design. The percentage of substrate surface covered by liverwort thalli was visually estimated bi-weekly for 10 weeks. Fresh biomass of the thalli and gemmae cup counts in each pot were also recorded. After 1 week in the growth chamber, ML followed by SC, PB and RH extracts showed maximum suppression of liverwort gemmae germination. At 2 weeks, ML applied at either of the rates provided complete inhibition of liverwort growth. In greenhouse, all the mulch extracts were able to provide complete liverwort control for the first two weeks. All the mulches and rates of applications were significantly different from the control after 6, 8, and 10 weeks. PB and HW mulches showed excellent liverwort control and minimum fresh biomass of liverwort after 10 weeks as compared to other mulches. The allelopathic potential of the organic mulches can be a promising option for biopesticidal control of liverwort and a component of integrated liverwort management.

Efficacy and safety of an oral complementary medicine combination in people with symptomatic knee osteoarthritis: Protocol for the double-blind, randomized, placebo-controlled ATLAS trial

ObjectiveTo investigate the efficacy and safety of an oral complementary medicine combination formulation relative to placebo, on changes in pain intensity from baseline to week 12, in people with knee osteoarthritis (OA). DesignA placebo-controlled, double-blind, two-arm, superiority, phase II, Randomized Controlled Trial (RCT) (ACTRN12623000380695). We will recruit 82 participants (∼41 per arm), aged ≥40 years, with a clinical diagnosis of symptomatic knee OA and radiographic change on x-ray (Kellgren-Lawrence Grade ≥2). Participants will be randomly allocated to receive either a complementary medicine formulation containing a daily dose of Boswellia serrata extract (Boswellin® Super, 250 ​mg/day), pine bark extract (Fenoprolic™ 70 Organic 100 ​mg/day), curcumin (500 ​mg/day), piperine (5 ​mg/day), and methylsulfonylmethane (MSM, 1500 ​mg/day), or placebo, for 12-weeks. The primary endpoint will be change from baseline in average knee pain intensity at 12-weeks (visual analogue scale). Secondary endpoints will include change in knee pain from baseline to 12-weeks in the Knee Injury and Osteoarthritis Outcome Score (KOOS), global assessment of disease activity, global rating of change, and health-related quality of life (AQoL-8D). Ethics and disseminationThis protocol has been approved by the University of Sydney Human Research Ethics Committee (#2021/877). Dissemination will occur through lay summaries, infographics, conference abstracts, oral presentations, theses, and scientific publications. ConclusionThis RCT will provide credible evidence about the efficacy and safety of this complementary medicine combination and inform updates to international clinical practice standards on the use of complementary medicines in the management of symptomatic knee OA.

Enhancing pediatric attention-deficit hyperactivity disorder treatment: exploring the gut microbiota effects of French maritime pine bark extract and methylphenidate intervention.

The pathogenesis of Attention-Deficit Hyperactivity Disorder (ADHD) is thought to be multifactorial, with a potential role for the bidirectional communication between the gut microbiome and brain development and function. Since the "golden-standard" medication therapy with methylphenidate (MPH) is linked to multiple adverse effects, there is a need for alternative treatment options such as dietary polyphenols. These secondary plant metabolites exert antioxidant and anti-inflammatory effects, but much less is known about their impact on the gut microbiota. Since polyphenols are believed to modulate gut microbial composition, interventions might be advantageous in ADHD therapy. Therefore, intervention studies with polyphenols in ADHD therapy investigating the gut microbial composition are highly relevant. Besides the primary research questions addressed previously, this study explored a potential prebiotic effect of the polyphenol-rich French Maritime Pine Bark Extract (PBE) compared to MPH and a placebo in pediatric ADHD patients by studying their impact on the gut microbiota via amplicon sequencing of the full length 16S rRNA gene ribosomal subunit (V1-V9). One interesting finding was the high relative abundance of Bifidobacteria among all patients in our study cohort. Moreover, our study has identified that treatment (placebo, MPH and PBE) explains 3.94% of the variation in distribution of microbial taxa (adjusted p-value of 0.011). Our small sample size (placebo: n = 10; PBE: n = 13 and MPH: n = 14) did not allow to observe clear prebiotic effects in the patients treated with PBE. Notwithstanding this limitation, subtle changes were noticeable and some limited compositional changes could be observed. doi: 10.1186/S13063-017-1879-6.

Pycnogenol-Assisted Alleviation of Titanium Dioxide Nanoparticle-Induced Lung Inflammation via Thioredoxin-Interacting Protein Downregulation.

Titanium dioxide nanoparticles (TiO2NPs) are used in products that are applied to the human body, such as cosmetics and food, but their biocompatibility remains controversial. Pycnogenol (PYC), a natural extract of pine bark, exerts anti-inflammatory and antioxidant effects. In this study, we investigated whether PYC effectively alleviates pulmonary toxicity induced by airway exposure to TiO2NPs, and the beneficial effects of PYC were explained through the analysis of changes to the mechanism of cytotoxicity. TiO2NPs induced pulmonary inflammation and mucus production, increased the levels of malondialdehyde, and upregulated thioredoxin-interacting protein (TXNIP) and cleaved-caspase 3 (Cas3) in the lungs of mice. However, PYC treatment reduced the levels of all toxicity markers of TiO2NPs and restored glutathione levels. These antioxidant and anti-inflammatory effects of PYC were also demonstrated in TiO2NP-exposed human airway epithelial cells by increasing the mRNA levels of antioxidant enzymes and decreasing the expression of TXNIP, cleaved-Cas3, and inflammatory mediators. Taken together, our results showed that PYC attenuated TiO2NP-induced lung injury via TXNIP downregulation. Therefore, our results suggest the potential of PYC as an effective anti-inflammatory and antioxidant agent against TiO2NP-induced pulmonary toxicity.

A Study Protocol Investigating the Impact of the New Zealand Pine Bark Extract (Enzogenol®) on Sucrose Metabolism and Glycaemic Responses in Healthy Adults – A Randomised, Placebo-Controlled, Crossover Trial

A Study Protocol Investigating the Impact of the New Zealand Pine Bark Extract (Enzogenol®) on Sucrose Metabolism and Glycaemic Responses in Healthy Adults – A Randomised, Placebo-Controlled, Crossover Trial

Electrospray Ionization—Mass Spectrometry Characterization of Pine Bark Extracts

Electrospray Ionization—Mass Spectrometry Characterization of Pine Bark Extracts

Effects of Pycnogenol® in people with post-COVID-19 condition (PYCNOVID): study protocol for a single-center, placebo controlled, quadruple-blind, randomized trial

BackgroundA significant proportion of the global population has been infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at some point since the onset of the pandemic. Although most individuals who develop coronavirus disease 2019 (COVID-19) recover without complications, about 6% have persistent symptoms, referred to as post-COVID-19 condition (PCC). Intervention studies investigating treatments that potentially alleviate PCC-related symptoms and thus aim to mitigate the global public health burden and healthcare costs linked to PCC are desperately needed. The PYCNOVID trial investigates the effects of Pycnogenol®, a French maritime pine bark extract with anti-inflammatory and antioxidative properties, versus placebo on patient-reported health status in people with PCC.MethodsThis is a single-center, placebo-controlled, quadruple blind, randomized trial. We aim to randomly assign 150 individuals with PCC (1:1 ratio) to receive either 200 mg Pycnogenol® or placebo daily for 12 weeks. Randomization is stratified for duration of PCC symptoms (≤ 6 months versus > 6 months) and presence of symptomatic chronic disease(s). The primary endpoint is perceived health status at 12 weeks (EuroQol—Visual Analogue Scale) adjusted for baseline values and stratification factors. Secondary endpoints include change in self-reported PCC symptoms, health-related quality of life, symptoms of depression and anxiety, cognitive function, functional exercise capacity, physical activity measured with accelerometry, and blood biomarkers for endothelial health, inflammation, coagulation, platelet function, and oxidative stress. Investigators, study participants, outcome assessors, and data analysts are blinded regarding the intervention assignment. Individuals with PCC were involved in the design of this study.DiscussionThis is the first trial to investigate the effects of Pycnogenol® versus placebo on patient-reported health status in people with PCC. Should the trial proof clinical effectiveness, Pycnogenol® may serve as a therapeutic approach to mitigate symptoms associated with PCC.Trial registrationThe study is registered at ClinicalTrials.gov. :NCT05890534, June 6, 2023.

Review of the pharmacokinetics of French maritime pine bark extract (Pycnogenol®) in humans.

The French maritime pine bark extract Pycnogenol® is a proprietary product from Pinus pinaster Aiton. It complies with the quality specifications in the United States Pharmacopeia monograph "Pine extract" in the section of dietary supplements. Pycnogenol® is standardized to contain 65-75% procyanidins which are a variety of biopolymers consisting of catechin and epicatechin monomeric units. The effects of Pycnogenol® have been researched in a multitude of human studies. The basis for any in vivo activity is the bioavailability of constituents and metabolites of the extract. General principles of compound absorption, distribution, metabolism and elimination as well as specific data from studies with Pycnogenol® are summarized and discussed in this review. Based on plasma concentration profiles it can be concluded that low molecular weight constituents of the extract, such as catechin, caffeic and ferulic acid, taxifolin are readily absorbed from the small intestine into systemic circulation. Procyanidin oligomers and polymers are subjected to gut microbial degradation in the large intestine yielding small bioavailable metabolites such as 5-(3',4'-dihydroxyphenyl)-γ-valerolactone. After intake of Pycnogenol®, constituents and metabolites have been also detected in blood cells, synovial fluid and saliva indicating a substantial distribution in compartments other than serum. In studies simultaneously investigating concentrations in different specimen, a preferential distribution of individual compounds has been observed, e.g., of ferulic acid and 5-(3',4'-dihydroxyphenyl)-γ-valerolactone into synovial fluid compared to serum. The main route of elimination of constituents and metabolites of the French pine bark extract is the renal excretion. The broad knowledge accumulated regarding the pharmacokinetics of compounds and metabolites of Pycnogenol® constitute a rational basis for effects characterized on a cellular level and observed in human clinical studies.

Pycnogenol® French maritime pine bark extract in randomized, double-blind, placebo-controlled human clinical studies.

Pycnogenol® French maritime pine bark extract is a well-known and thoroughly studied patented extract from the bark of Pinus pinaster Ait. ssp. Atlantica. In 39 randomized double-blind, placebo-controlled (RDP) human clinical trials including 2,009 subjects, Pycnogenol® French maritime pine bark extract supplementation for two weeks to six months has been shown to beneficially affect cardiovascular health, chronic venous insufficiency, cognition, joint health, skin health, eye health, women's health, respiratory health and allergies, oral health and sports performance. The mechanisms of action that can explain the respective effects on different conditions in the human body are discussed as well. As investigated in several in vitro, in vivo and in clinical studies, Pycnogenol® French maritime pine bark extract showed antioxidative effects, anti-inflammatory abilities, beneficial effects on endothelial function and reinforcing effects on the extracellular matrix. The present review aims to give a comprehensive overview of currently available "gold standard" RDP trials of Pycnogenol®'s benefits across various health domains compared to placebo. In addition, some of the processes on which the presented effects of Pycnogenol® French maritime pine bark extract are based will be elucidated and discussed. This broad overview of RDP studies on Pycnogenol® in different health domains can be used as a basis for further research on applications and mechanisms of this unique French maritime pine bark extract.

A Review on Green Chemistry and Its Applications

Green Chemistry is most investigated subject these days. It is also known as sustainable chemistry. Green Chemistry and sustainable chemistry are equals that helps to save and conserve resources. It decreases the effect of chemical products on human and atmospheric health. Green Chemistry gives 12 principles that reduce and prevent the utilization and manufacture of hazardous substance. These principles of green chemistry inform about the various issues related to production of chemical compound. Green Chemistry concept started approximately three decades ago. Green chemistry concept for the chemical synthesis and application launched in 1990. This review article purpose to study about Green chemistry and its application and how green chemistry connect to the phytochemistry. By establishing Green Aspiration Level (GAL) that is a quantifiable descriptor, process greenness becomes measurable. Green house gases and global warming are the problem that affected the human and environment health. Green chemistry is used in daily life mainly in medicines. Tree bark and Pine bark extracts are mostly used in anti-microbial, antioxidant and anticancer drugs. The matter that present in environment gives applicable things to the researchers and engineers for the changing and developing a sustainable culture. The word “Green chemistry” is given by the IUPAC which means: the invention, design and utilization of chemical product and process to reduce or to eliminate the use and production of unsafe substance.

Comparative Evaluation of Various Antioxidants on the Shear Bond Strength of Composite Resin to Bleached Enamel - An In Vitro Study.

To evaluate and compare the effect of various antioxidants on the shear bond strength of composite resin to bleached enamel. Labial enamel surfaces of 90 extracted human maxillary central incisors were randomly divided into five groups based on the antioxidant used as follows: Group I ( n = 20): Bleaching with 40% hydrogen peroxide gel for 10 min, without the use of an antioxidant; Group II ( n = 20): Bleaching followed by the use of 10% sodium ascorbate solution; Group III ( n = 20): Bleaching followed by the use of 5% grape seed extract solution; Group IV ( n =20): Bleaching followed by the use of 5% pine bark extract solution; and Group V ( n =20): Control group in which no bleaching was done. Groups I-IV were further subdivided into two subgroups of 10 teeth each, whether the antioxidant application and composite build-up was done immediately (subgroup A) or after 2 weeks of postbleaching (subgroup B). Shear bond strength of the specimens was tested under a universal testing machine. One-way analysis of variance followed by Mann-Tukey posthoc multiple comparison test was used to analyse the data. The level of significance was established at P < 0.05. Within the limitations of this study, it was observed that the use of antioxidants effectively reversed the compromised bond strength of bleached enamel. Among the antioxidants, 5% pine bark extract application after bleaching showed better bond strength.

In Vivo Evaluation of Wound Healing Efficacy of Gel-Based Dressings Loaded with Pycnogenol™ and Ceratothoa oestroides Extracts.

Ceratothoa oestroides and French maritime pine bark (Pycnogenol™) extracts are considered promising therapeutic agents in wound healing. This study explores the healing efficacy of composite dressings containing these extracts, aiming to enhance their stability and effectiveness, utilizing a low-temperature vacuum method for producing Sodium Alginate-Maltodextrin gel dressings. Surgical wounds were inflicted on SKH-hr2 hairless mice. Dressings were loaded with Pycnogenol™ and/or C. oestroides extracts and assessed for their efficacy. Wound healing was primarily evaluated by clinical and histopathological evaluation and secondarily by Antera 3D camera and biophysical measurements. Dressings were stable and did not compromise the therapeutic properties of C. oestroides extract. All interventions were compared to the C. oestroides ointment as a reference product. Most of the wounds treated with the reference formulation and the C. oestrodes dressing had already closed by the 15th day, with histological scores of 7 and 6.5, respectively. In contrast, wounds treated with Pycnogenol™, either alone or in combination with C. oestroides, did not close by the end of the experiment (16th day), with histological scores reaching 15 in both cases. Furthermore, treatment with 5% Pycnogenol™ dressing appeared to induce skin thickening and increase body temperature. The study underscores the wound healing potential of C. oestroides extracts and highlights the need for further research to optimize Pycnogenol™ dosing in topical applications.

Effect of pine bark extract and its phenolic compounds on selected pathogenic and probiotic bacterial strains.

Inflammatory bowel disease (IBD) comprises a heterogeneous group of chronic diseases as ulcerative colitis (UC) and Crohn's disease (CD). IBD is the result of a dysregulation of intestinal homeostasis with a host's loss of tolerance toward normal enteric microflora. Plant-based extracts as phenolic compounds can play a role by modulating the intestinal inflammation response. The in vitro antimicrobial activity of French maritime pine bark extract (PBE) and its phenolic constituents has been investigated in this study. Furthermore, the ability of PBE and phenolic compounds (caffeic acid, chlorogenic acid, ferulic acid, gallic acid and taxifolin) to modulate the microbiota has been assessed. Phenolic compounds and PBE showed a great inhibitory effect on the pathogens growth at the highest concentration assessed (1.25 mg/mL). The growth of E. sakazakii and E. faecalis were affected by the effect of caffeic acid and ferulic acid. Taxifolin showed a very strong activity against Listeria sp. (with a reduction ~98%). Gallic acid revealed antibacterial effect on S. aureus at different concentrations. The inhibitory effect of PBE was highly significant on the growth of E. coli O157:H7. PBE, caffeic acid and chlorogenic acid seem to provide the greatest beneficial effect on the probiotic bacteria. However, the highest concentrations of taxifolin may have impaired the growth of beneficial microbiota. Present findings could be of interest for considering PBE and/or its phenolic constituents as protectors against gastrointestinal disturbances which lead to ulcerative colitis and Crohn's disease.

Laccase‐mediated polymerization of tannins from a pine bark extract: Toward an eco‐friendly valorization of forest wastes

AbstractThe valorization of tannins from forest by‐products is a major opportunity for the sustainable development of the forestry industry. Herein we report the laccase‐mediated polymerization of tannins obtained from an aqueous pine bark extract. The reaction was conducted under an oxygen atmosphere at 50°C for 60 min and followed by UV–Vis, fluorescence intensity, phenol content, and viscosity measurements. An insoluble polymer was obtained after 45 min, which was attributed to coupling reactions triggered by phenoxyl radicals within the tannins mixture. The polymer showed a marked increase in thermal stability compared with the precursor pine bark extract, with a total mass loss of less than 12% at temperatures up to 500°C, suggesting potential practical applications in flame retardant materials. Additionally, the polymer showed an 85% DPPH activity and a 60% attenuation of singlet oxygen release upon light irradiation, which supports antioxidant and photoprotective properties for the prepared material. To the best of our knowledge, this is the first report to describe the formation of an insoluble polymer by direct enzymatic reaction of an aqueous tannin extract. In this case, soluble tannins are the sole reactants used to produce a promising versatile material for forest waste valorization.

Effect of herbal antioxidants on the shear bond strength of composite resin to bleached enamel at different time intervals.

Anterior tooth discolorations can be treated conservatively and noninvasively through bleaching to achieve the desired esthetic outcomes. However, bleaching along with composite resin is advisable for certain clinical cases for optimum results. However, shear bond strength (SBS) of composite resin to the bleached tooth gets significantly lowered. Before placing the composite restoration, the bleached enamel needs to be treated with antioxidant agents to increase its SBS. The study aims to evaluate and compare the effect of herbal antioxidants on SBS of composite resin to bleached enamel at different time intervals. Sixty extracted single-rooted maxillary incisors postdecoronation, keeping their labial surfaces up were mounted in cold-cure acrylic resin. The samples were randomly divided into: Group I - unbleached; Group II - 10% pine bark extract for 10 min postbleaching; Group III - 10% pine bark extract for 20 min postbleaching; Group IV - application of 10% rosemary extract for 10 min postbleaching, Group V - application of 10% rosemary extract for 20 min postbleaching; Group VI - no application of antioxidant. 35% hydrogen peroxide was used for bleaching all the samples except those which served as negative control. Later composite cylinder 4 mm in diameter and length were built on prepared enamel. The maximum load at failure was recorded using the universal testing machine. Data were analyzed using the analysis of variance and Tukey's t-test with significance level of P < 0.05. Highest load was exhibited by Group I. Group V showed satisfactory shear strength followed by Groups IV, III, II, and VI. Both 10% rosemary and 10% pine bark extracts showed better results when applied for 20 min as compared to 10 min application. Increased duration of antioxidant application increases the SBS.

Protocol of a Randomised Controlled Trial to Assess the Efficacy and Safety of a Oral Complementary Medicine Combination in People with Knee Osteoarthritis

Background Osteoarthritis (OA) is a leading cause of pain and disability in middle-aged or older adults worldwide. The prevalence of symptomatic knee OA has been increasing over the past several decades, indicating the need for the deployment of innovative prevention and treatment strategies for knee OA. The aim of this study is to investigate the efficacy and safety of an oral complementary medicine formulation in people with symptomatic knee OA. Methods This is a randomised, placebo-controlled, double-blinded (participants and investigators), two-arm, superiority, parallel, phase II trial. The study will recruit 82 ([Formula: see text]41 per arm) community-based participants with knee OA living in Australia. Participants aged [Formula: see text] 40 years with a clinical diagnosis of symptomatic knee OA and radiographic change on X-ray (Kellgren-Lawrence Grade [Formula: see text] 2) will be recruited. Participants will be randomly allocated to receive either a complementary medicine formulation containing a daily dose of Boswellia serrata extract (Boswellin[Formula: see text]Super, 250 mg/day), pine bark extract (Fenoprolic™70 Organic 100mg/day), curcumin (500mg/day), piperine (5mg/day), and methylsulfonylmethane (MSM, 1500mg/day), or placebo, for 12 weeks. The primary endpoint is change from baseline in average index knee pain at 12 weeks (visual analogue scale). Secondary endpoints include change in knee pain at other timepoints, the Knee Injury and Osteoarthritis Outcome Score (KOOS), global assessment of disease activity, global rating of change, health-related quality of life (AQoL-8D), and adverse events. Ethics, trial registration and dissemination: The study protocol has been approved by the University of Sydney Human Research Ethics Committee (#2021/877). The trial has been prospectively registered on the Australian New Zealand Clinical Trials Registry (ACTRN12623000380695, 14/04/2023). Dissemination will occur through lay summaries, scientific publications, conference abstracts, poster or oral presentations, infographics, and theses. Conclusion The outcomes of this study will provide high-quality evidence guiding the clinical use of the complementary medicine combination and will inform updates on international OA clinical practice standards on the use of complementary medicines.

Lycopene and pine bark extract as nitrite replacers in Egyptian basterma

Lycopene and pine bark extract as nitrite replacers in Egyptian basterma

Comparative Antioxidant and Antimicrobial Activities of Several Conifer Needles and Bark Extracts.

Nowadays, an increased concern regarding using natural products for their health benefits can be observed. The aim of this study was to assess and compare several phenolic compounds found in 15- to 60-year-old Douglas fir, silver fir, larch, pine, and spruce needle and bark extracts and to evaluate their antioxidant and antimicrobial activities. Spectrophotometric assays were used to determine the total polyphenol content and the antioxidant activity that was assessed by using the DPPH• radical scavenging assay (RSA), the ferric reducing antioxidant power assay (FRAP), and the ABTS•+ radical cation scavenging assay (ABTS). The phytochemical content was determined by using high-performance liquid chromatography, and the antimicrobial activity was determined by assessing the minimal inhibition concentration (MIC). The results of the study show a total polyphenol content of 62.45-109.80 mg GAE/g d.w. and an antioxidant activity of 91.18-99.32% for RSA, 29.16-35.74 µmol TE/g d.w. for FRAP, and 38.23-53.57 µmol TE/g d.w. for ABTS. The greatest quantity of phenolic compound for most of the extracts was for (+)-catechin, and it had values between 165.79 and 5343.27 µg/g d.w. for these samples. The antimicrobial inhibition for all the extracts was the strongest for Staphylococcus aureus (MIC 62.5-125 µg/mL). The extracts analyzed could be used for their bioactive potential after further investigations.

Development and validation of a LC–MS/MS method for the quantification of phenolic compounds in human saliva after intake of a procyanidin-rich pine bark extract

Plant-derived phenolic compounds are regularly ingested as food compounds or as food supplements. Concentrations of individual compounds and metabolites are typically measured in serum or urine samples. This, however, allows no conclusion on the distribution into organs and tissues. An easily accessible biofluid is saliva. At this point, it was not clear yet, whether polyphenols circulating in the blood would be secreted or diffuse into saliva. The purpose of the present study was to develop and validate a method using liquid chromatography coupled to electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) for analysis of phenolic compounds in human saliva. Method validation for the quantification of taxifolin, ferulic acid, caffeic acid, gallic acid, para-coumaric acid, and protocatechuic acid and the gut microbial catechin metabolite δ-(3,4-dihydroxyphenyl)-γ-valerolactone (M1) in human saliva was performed according to current guidelines for bioanalytical method validation. The lower limit of quantification ranged from 0.82 ng/ml for M1 to 8.20 ng/ml for protocatechuic acid. The method was successfully applied to an authentic saliva sample of a volunteer after swallowing of procyanidin-rich pine bark extract capsules (dietary supplement Pycnogenol®). All polyphenols except ferulic acid were quantified at concentrations ranging from 1.20 ng/ml (M1) to 10.34 ng/ml (gallic acid). Notably, in contrast to serum samples, all phenolic compounds were present without sulfate or glucuronic acid conjugation in saliva, suggesting an enzymatic deconjugation, e.g., by a β-glucuronidase activity, during compound transfer from serum to saliva. Since M1 is only produced in the gut, its presence in saliva ruled out the possibility of sample contamination by phenolic compounds residing in the oral cavity after food intake. To the best of our knowledge, this is the first time that the gut microbiota-derived metabolite M1 has been detected in saliva. To further investigate the role of phenolic compounds in saliva, the described analytical method can be applied in clinical studies investigating the biodistribution of polyphenols and their metabolites.