Analysis of bitter compounds in traditional preparations of Gentiana purpurea L.

Roots of Gentiana purpurea are known to have an intense bitter taste due to its high content of secoiridoids. In folk medicine roots have commonly been prepared as water decoctions, soaked in ethanol, or boiled with milk, wine, or beer. The aim of this study was to explore how various historical preparation methods influence yields of major bitter compounds in G. purpurea. HPLC-DAD analysis revealed that maceration with 40% and 70% ethanol, boiling with acetic acid (3% and 6%), vinegar and raw milk gave the highest extraction yields of gentiopicrin. Erythrocentaurin was detected when the roots were added to cold water before boiling, possibly because of enzymatic degradation. In contrast, erythrocentaurin was not detected in preparations where roots were added to boiling water, or when they were extracted with acetic acid or alcohol. The results stress the significance of traditional preparation methods to optimize yield of bioactive compounds.

Polyherbal Combinations Used by Traditional Health Practitioners against Mental Illnesses in Bamako, Mali, West Africa.

This study explores the traditional knowledge of plants used by traditional health practitioners (THPs) in the treatment of symptoms or syndromes related to mental illnesses in the district of Bamako in Mali, along with the identification of affiliated traditional treating methods. An exploratory and cross-sectional ethnopharmacological survey was conducted in the district of Bamako. The Malian Federation of Associations of Therapists and Herbalists (FEMATH) assisted in the identification and inclusion of the THPs. Data sampling included semi-structured interviews, questionnaires, and in-depth interviews. Quantitative data were evaluated by analysing reports of the use of different medicinal plants and the number of participants. Fifteen THPs belonging to the district of Bamako participated. In total, 43 medicinal plants belonging to 22 plant families were used by the THPs. The most cited plant species was Securidaca longepedunculata (violet tree), followed by Khaya senegalensis (African mahogany) and Boscia integrifolia (rough-leaved shepherds tree). A great number of herbal combinations, preparation methods, and administration routes were used, often with honey as an adjuvant. To our knowledge, this is the first ethnobotanical survey on the use of medicinal plants in the treatment of all types of mental disorders in Bamako.

Three-tiered authentication of herbal traditional Chinese medicine ingredients used in women's health provides progressive qualitative and quantitative insight.

Traditional Chinese Medicine (TCM) herbal products are increasingly used in Europe, but prevalent authentication methods have significant gaps in detection. In this study, three authentication methods were tested in a tiered approach to improve accuracy on a collection of 51 TCM plant ingredients obtained on the European market. We show the relative performance of conventional barcoding, metabarcoding and standardized chromatographic profiling for TCM ingredients used in one of the most diagnosed disease patterns in women, endometriosis. DNA barcoding using marker ITS2 and chromatographic profiling are methods of choice reported by regulatory authorities and relevant national pharmacopeias. HPTLC was shown to be a valuable authentication tool, combined with metabarcoding, which gives an increased resolution on species diversity, despite dealing with highly processed herbal ingredients. Conventional DNA barcoding as a recommended method was shown to be an insufficient tool for authentication of these samples, while DNA metabarcoding yields an insight into biological contaminants. We conclude that a tiered identification strategy can provide progressive qualitative and quantitative insight in an integrative approach for quality control of processed herbal ingredients.

Inhibition of Seizure-Like Paroxysms and Toxicity Effects of Securidaca longepedunculata Extracts and Constituents in Zebrafish Danio rerio.

Plants used in traditional medicine in the management of epilepsy could potentially yield novel drug compounds with antiepileptic properties. The medicinal plant Securidaca longepedunculata is widely used in traditional medicine in the African continent, and epilepsy is among several indications. Limited knowledge is available on its toxicity and medicinal effects, such as anticonvulsant activities. This study explores the potential in vivo inhibition of seizure-like paroxysms and toxicity effects of dichloromethane (DCM) and ethanol (EtOH) extracts, as well as isolated xanthones and benzoates of S. longepedunculata. Ten phenolic compounds were isolated from the DCM extract. All of the substances were identified by nuclear magnetic resonance spectroscopy. Assays for toxicity and inhibition of pentylenetetrazole (PTZ)-induced seizure-like paroxysms were performed in zebrafish larvae. Among the compounds assessed in the assay for maximum tolerated concentration (MTC), benzyl-2-hydroxy-6-methoxy-benzoate (MTC 12.5 µM), 4,8-dihydroxy-1,2,3,5,6-pentamethoxyxanthone (MTC 25 µM), and 1,7-dihydroxy-4-methoxyxanthone (MTC 6.25 µM) were the most toxic. The DCM extract, 1,7-dihydroxy-4-methoxyxanthone and 2-hydroxy-1,7-dimethoxyxanthone displayed the most significant inhibition of paroxysms by altering the locomotor behavior in GABAA receptor antagonist, PTZ, which induced seizures in larval zebrafish. The EtOH extract, benzyl benzoate, and benzyl-2-hydroxy-6-methoxy-benzoate unexpectedly increased locomotor activity in treated larval zebrafish and decreased locomotor activity in nontreated larval zebrafish, seemingly due to paradoxical excitation. The results reveal promising medicinal activities of this plant, contributing to our understanding of its use as an antiepileptic drug. It also shows us the presence of potentially new lead compounds for future drug development.

Apolar Extracts of St. John's Wort Alleviate the Effects of ß-Amyloid Toxicity in Early Alzheimer's Disease.

Hypericum perforatum (St. John's wort) has been described to be beneficial for the treatment of Alzheimer's disease (AD). Different extractions have demonstrated efficiency in mice and humans, esp. extracts with a low hypericin and hyperforin content to reduce side effects such as phototoxicity. In order to systematically elucidate the therapeutic effects of H. perforatum extracts with different polarities, APP-transgenic mice were treated with a total ethanol extract (TE), a polar extract obtained from TE, and an apolar supercritical CO2 (scCO2) extract. The scCO2 extract was formulated with silicon dioxide (SiO2) for better oral application. APP-transgenic mice were treated with several extracts (total, polar, apolar) at different concentrations. We established an early treatment paradigm from the age of 40 days until the age of 80 days, starting before the onset of cerebral ß-amyloid (Aß) deposition at 45 days of age. Their effects on intracerebral soluble and insoluble Aß were analyzed using biochemical analyses. Our study confirms that the scCO2H. perforatum formulation shows better biological activity against Aß-related pathological effects than the TE or polar extracts. Clinically, the treatment resulted in a dose-dependent improvement in food intake with augmentation of the body weight, and, biochemically, it resulted in a significant reduction in both soluble and insoluble Aß (-27% and -25%, respectively). We therefore recommend apolar H. perforatum extracts for the early oral treatment of patients with mild cognitive impairment or early AD.

Bioactive polysaccharides in different plant parts of Aconitum carmichaelii.

BACKGROUND: Aconitum carmichaelii is an industrially cultivated medicinal plant in China and its lateral and mother roots are used in traditional Chinese medicine due to the presence of alkaloids. However, the rootlets and aerial parts are discarded after collection of the roots, and the non-toxic polysaccharides in this plant have attracted less attention than the alkaloids and poisonous features. In this study, five neutral and 14 acidic polysaccharide fractions were isolated systematically from different plant parts of A. carmichaelii, and their structural features and bioactivity were studied and compared. RESULTS: The neutral fraction isolated from the rootlets differed from those isolated from the lateral and mother roots. It consisted of less starch and more possible mannans, galactans, and/or xyloglucans, being similar to those of the aerial parts. Pectic polysaccharides containing homogalacturonan and branched type-I rhamnogalacturonan (RG-I) were present in all plant parts of A. carmichaelii. However, more arabinogalactan (AG)-II side chains in the RG-I backbone were present in the aerial parts of the plants, while more amounts of arabinans were found in the roots. Various immunomodulatory effects were observed, determined by complement fixation activity and anti-inflammatory effects on the intestinal epithelial cells of all polysaccharide fractions. CONCLUSION: This study highlighted the diversity of polysaccharides present in A. carmichaelii, especially in the unutilized plant parts, and showed their potential medicinal value. © 2023 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Complementary authentication of Chinese herbal products to treat endometriosis using DNA metabarcoding and HPTLC shows a high level of variability.

Traditional Chinese Medicine (TCM) is popular for the treatment of endometriosis, a complex gynecological disease that affects 10% of women globally. The growing market for TCMs has yielded a significant incentive for product adulteration, and although emerging technologies show promise to improve their quality control, many challenges remain. We tested the authenticity of two traditional Chinese herbal formulae used in women's healthcare for the treatment of endometriosis, known as Gui Zhi Fu Ling Wan (FL) and Ge Xia Zhu Yu Tang (GX). Dual-locus DNA metabarcoding analysis coupled with high-performance thin-layer chromatography (HPTLC) were used to authenticate 19 FL and six GX commercial herbal products, as well as three ad hoc prepared artificial mixtures. HPTLC was able to detect most of the expected ingredients via comparative component analysis. DNA metabarcoding was able to detect an unexpected species diversity in the products, including 38 unexpected taxa. Chromatography has a resolution for all species indirectly through the identification of marker compounds for the different species ingredients. Metabarcoding on the other hand yields an overview of species diversity in each sample, but interpretation of the results can be challenging. Detected species might not be present in quantities that matter, and without validated quantification, some detected species can be hard to interpret. Comparative analysis of the two analytical approaches also reveals that DNA for species might be absent or too fragmented to amplify as the relevant chemical marker compounds can be detected but no amplicons are assigned to the same species. Our study emphasizes that integrating DNA metabarcoding with phytochemical analysis brings valuable data for the comprehensive authentication of Traditional Chinese Medicines ensuring their quality and safe use.

Phytochemical characterization and anti-inflammatory activity of a water extract of Gentiana purpurea roots.

ETHNOPHARMACOLOGICAL RELEVANCE: Gentiana purpurea was one of the most important medicinal plants in Norway during the 18th and 19th centuries, and the roots were used against different types of gastrointestinal and airway diseases. AIM OF THE STUDY: To explore the content of bioactive compounds in a water extract from the roots, a preparation commonly used in traditional medicine in Norway, to assess the anti-inflammatory potential, and furthermore to quantify the major bitter compounds in both roots and leaves. MATERIALS AND METHODS: G. purpurea roots were boiled in water, the water extract applied on a Diaion HP20 column and further fractionated with Sephadex LH20, reverse phase C18 and normal phase silica gel to obtain the low molecular compounds. 1D NMR, 2D NMR, and ESI-MS were used for structure elucidation. HPLC-DAD analysis was used for quantification. The inhibition of TNF-α secretion in ConA stimulated peripheral blood mononuclear cells (PBMCs) was investigated. RESULTS: Eleven compounds were isolated and identified from the hot water extract of G. purpurea roots. Gentiopicrin, amarogentin, erythrocentaurin and gentiogenal showed dose-dependent inhibition of TNF-α secretion. Gentiopicrin is the major secondary metabolite in the roots, while sweroside dominates in the leaves. CONCLUSIONS: The present work gives a comprehensive overview of the major low-molecular weight compounds in the water extracts of G. purpurea, including metabolites produced during the decoction process, and show new anti-inflammatory activities for the native bitter compounds as well as the metabolites produced during preparation of the crude drug.

Pectic polysaccharides from Aconitum carmichaelii leaves protects against DSS-induced ulcerative colitis in mice through modulations of metabolism and microbiota composition.

The industrial processing of Aconitum carmichaelii roots for use in Traditional Chinese Medicine generates a high amount of waste material, especially leaves. An acidic polysaccharide fraction isolated from these unutilized leaves, AL-I, was in our previous work shown to contain pectic polysaccharides. This study aimed to investigate the protective effect of AL-I on ulcerative colitis for the possible application of A. carmichaelii leaves in the treatment of intestinal inflammatory diseases. AL-I was found to alleviate symptoms and colonic pathological injury in colitis mice, and ameliorate the levels of inflammatory indices in serum and colon. The production of short- and branched-chain fatty acids was also restored by AL-I. The observed protective effect could be due to the inhibition of NOD1 and TLR4 activation, the promotion of gene transcription of tight-junction proteins, and the modulation of gut microbiota composition like Bacteroides, Dubosiella, Alistipes and Prevotella,. A regulation of serum metabolomic profiles being relevant to the bacterial change, such as D-mannose 6-phosphate, D-erythrose 4-phosphate and uric acid, was also observed.

The discovery of novel immunomodulatory medicinal plants by combination of historical text reviews and immunological screening assays.

ETHNOPHARMACOLOGICAL RELEVANCE: With the advent of immunotherapies against cancers, autoimmune diseases and infections, there is a steady demand for novel medicines. New sources for discovery of potentially novel immunomodulatory compounds are therefore needed. Nature contains a large and diverse reservoir of novel compounds that can be exploited for their potential as new drugs, and exploring the pharmaceutical potential of medicinal plants used in traditional medicine is highly relevant. AIM OF THE STUDY: We aimed with this study to explore usage of medicinal plants in Scandinavian folk medicine against diseases interpreted to involve the immune system, and to further screen water extracts from previously overlooked medicinal plants in order to discover potential new sources of immunomodulatory compounds. MATERIALS AND METHODS: We systematically investigated historical records dating back to the 1800s with an emphasis on plants used as treatment for wounds or diseases interpreted to be inflammatory. Of 74 candidate plants, 23 pharmacologically under-studied species were selected for further characterization. The plants were collected from their natural habitats in Southern Norway, air-dried, and subjected to boiling water and accelerated solvent extraction. The crude extracts were separated into polysaccharide-enriched fractions and C-18 solid phase extracted fractions. Immunological screenings were performed with all extracts and fractions. Monosaccharide composition and total phenolic content were determined and compared across all species. RESULTS: We identified 10 species with clear immune activating effects and 8 species with immune inhibitory effects by comparing cytokine production by human peripheral blood mononuclear cells, primary human T- and NK-cell proliferation, and nitric oxide production from macrophages. CONCLUSIONS: With this study, we provide a comprehensive overview of Scandinavian medicinal plants and their usage, and our findings support an approach of combining historical sources with modern pharmacology in the discovery of plant sources containing potentially new pharmacological compounds.

Aconitum carmichaelii Debeaux: A systematic review on traditional use, and the chemical structures and pharmacological properties of polysaccharides and phenolic compounds in the roots.

ETHNOPHARMACOLOGICAL RELEVANCE: Aconitum carmichaelii, belonging to the Ranunculaceae family, is a widely used traditional herbal plant in Asian countries, especially in China. The lateral ("Fuzi") and mother ("Chuanwu") roots are the two main plant parts used in Traditional Chinese Medicine (TCM), where they are used in the treatment of acute myocardial infarction, heart failure, rheumatoid arthritis, and as analgesics. AIM OF THE STUDY: In order to further guide the research direction and application of A. carmichaelii, this study aims to give a systematic and in-depth overview on the phytochemical and pharmacological studies of non-alkaloid natural products with focus on polysaccharides and phenolic compounds. MATERIALS AND METHODS: A comprehensive search in the literature was conducted based on the databases Google Scholar, SciFinder (American Chemical Society), Springer Link, PubMed Science, Science Direct and China National Knowledge Internet, Wanfang Data, in addition to books, doctoral and master's dissertations, and official website. The main keywords were: "Aconitum carmichaelii", "Aconiti Lateralis Radix Praeparata", "Fuzi", "Chuanwu", "Aconiti Radix", "monkshood" and "Bushi". RESULTS: A. carmichaelii is known for the use of its different root parts, including "Fuzi" and "Chuanwu". Different types of polysaccharides, both neutral and acidic, and 39 phenolic compounds like flavonoids, phenylpropanoids, lignans, neolignans, and benzoic acid derivatives have been isolated and identified from the roots. Pharmacological studies of the isolated polysaccharides have demonstrated various biological effects such as hypoglycemic, hypolipidemic, cardiovascular, immunomodulatory, anti-tumor, and neuropharmacological activities. Studies on pharmacological effects of the phenolic compounds isolated from the roots are however limited. CONCLUSIONS: This review shows that polysaccharides could be one of the active components in the roots of A. carmichaelii, and they are promising for future applications due to their pharmacological properties. In addition, polysaccharides are generally non-toxic, biocompatible, and biodegradable. This review also sheds light on new research directions for A. carmichaelii. A more detailed structural characterization of polysaccharides from different root parts of A. carmichaelii, and their structure-activity relationships are required. Additionally, their pharmacological properties as immunomodulators in the intestinal system should be investigated. Further, more knowledge about the pharmacological effects and molecular mechanisms of the phenolic compounds that have been identified are needed.

Ethnopharmacology, biological activities and chemical compounds of Canarium strictum: An important resin-yielding medicinal tree in India.

The resin of Canarium strictum Roxb. is used for rheumatism and asthma; the bark is used as a mosquito repellent. The major compounds in the resin are triterpenoids, but as no studies have been performed on the bark, this study investigated this economically important resource. Ten folk healers were interviewed about their medicinal uses of C. strictum. Resin and bark were extracted with dichloromethane followed by methanol using accelerated solvent extraction. The extracts were fractionated using different chromatographic methods, and isolated compounds were identified by NMR spectroscopy and GC-MS. Resin and bark extracts were investigated for DPPH radical scavenging, 15-lipoxygenase inhibition, effects on nitric oxide (NO) production in LPS-activated dendritic D2SC/I cells and toxicity against Artemia salina nauplii. Traditional healers used resin to treat colds, airway afflictions and rheumatoid arthritis. α-Amyrin and ß-amyrin were identified as the major constituents in the dichloromethane resin extract. From the stem bark, procyanidins, gallic acid, methyl gallate, scopoletin, 3,3'-di-O-methylellagic acid 4-O-α-arabinofuranoside and elephantorrhizol (3,3',4',5,6,7,8-heptahydroxyflavan) were isolated and identified. By GC-MS, α-amyrin and ß-amyrin and their acetates, lupeol, and taraxasterol were identified. Radical scavenging, 15-lipoxygenase inhibitory activity and inhibition of NO production was observed from resin and bark extracts, and no toxicity towards Artemia salina nauplii was found. Triterpenoids and procyanidins are the major compounds in C. strictum resin and stem bark, respectively. The high content of triterpenoids might contribute to anti-inflammatory effects and give a rationale for the widespread usage of the resin in India.

Anti-plasmodial Effects of Zanthoxylum zanthoxyloides.

Zanthoxylum zanthoxyloides, syn. Fagara zanthoxyloides, is a tree growing in West Africa and is used in traditional medicine against a variety of diseases, including malaria. In the work reported here, root bark and stem bark extracts of this tree, as well as compounds isolated from the extracts, have been investigated for activity in vitro against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. In addition, toxicity against nauplii of the brine shrimp Artemia salina has been studied. Dichloromethane extracts of the root bark and stem bark, and a methanol extract of the stem bark, showed anti-parasitic activity towards chloroquine-sensitive as well as chloroquine-resistant P. falciparum, with IC50 values between 1 and 10 µg/mL. Among the isolated compounds, bis-dihydrochelerythrinyl ether, buesgenine, chelerythrine, γ-fagarine, skimmianine, and pellitorine were the most active, with IC50 values of less than 5 µg/mL. The dichloromethane extracts were toxic to brine shrimp nauplii, with LC50 values of less than 1 µg/mL. Methanol extracts were much less toxic (LC50 between 50 and 100 µg/mL). Among the isolated substances, bis-dihydrochelethrinyl ether was the most toxic (LC50 ca. 2 µg/mL).

DNA Metabarcoding Authentication of Ayurvedic Herbal Products on the European Market Raises Concerns of Quality and Fidelity.

Ayurveda is one of the oldest systems of medicine in the world, but the growing commercial interest in Ayurveda based products has increased the incentive for adulteration and substitution within this herbal market. Fraudulent practices such as the use of undeclared fillers and use of other species of inferior quality is driven both by the increased as well as insufficient supply capacity of especially wild plant species. Developing novel strategies to exhaustively assess and monitor both the quality of raw materials and final marketed herbal products is a challenge in herbal pharmacovigilance. Seventy-nine Ayurvedic herbal products sold as tablets, capsules, powders, and extracts were randomly purchased via e-commerce and pharmacies across Europe, and DNA metabarcoding was used to assess the ability of this method to authenticate these products. Our analysis reveals that only two out of 12 single ingredient products contained only one species as labeled, eight out of 27 multiple ingredient products contained none of the species listed on the label, and the remaining 19 products contained 1 to 5 of the species listed on the label along with many other species not specified on the label. The fidelity for single ingredient products was 67%, the overall ingredient fidelity for multi ingredient products was 21%, and for all products 24%. The low level of fidelity raises concerns about the reliability of the products, and detection of threatened species raises further concerns about illegal plant trade. The study highlights the necessity for quality control of the marketed herbal products and shows that DNA metabarcoding is an effective analytical approach to authenticate complex multi ingredient herbal products. However, effort needs to be done to standardize the protocols for DNA metabarcoding before this approach can be implemented as routine analytical approaches for plant identification, and approved for use in regulated procedures.

Authentication of Garcinia fruits and food supplements using DNA barcoding and NMR spectroscopy.

Garcinia L. (Clusiaceae) fruits are a rich source of (-)-hydroxycitric acid, and this has gained considerable attention as an anti-obesity agent and a popular weight loss food supplement. In this study, we assessed adulteration of morphologically similar samples of Garcinia using DNA barcoding, and used NMR to quantify the content of (-)-hydroxycitric acid and (-)-hydroxycitric acid lactone in raw herbal drugs and Garcinia food supplements. DNA barcoding revealed that mostly G. gummi-gutta (previously known as G. cambogia) and G. indica were traded in Indian herbal markets, and there was no adulteration. The content of (-)-hydroxycitric acid and (-)-hydroxycitric acid lactone in the two species varied from 1.7% to 16.3%, and 3.5% to 20.7% respectively. Analysis of ten Garcinia food supplements revealed a large variation in the content of (-)-hydroxycitric acid, from 29 mg (4.6%) to 289 mg (50.6%) content per capsule or tablet. Only one product contained quantifiable amounts of (-)-hydroxycitric acid lactone. Furthermore the study demonstrates that DNA barcoding and NMR could be effectively used as a regulatory tool to authenticate Garcinia fruit rinds and food supplements.

Ethnobotany of dioecious species: Traditional knowledge on dioecious plants in India.

ETHNOPHARMACOLOGICAL RELEVANCE: More than 15,000 angiosperm species are dioecious, i.e., having distinct male and female individual plants. The allocation of resources between male and female plants is different, and also variation in secondary metabolites and sex-biased herbivory is reported among dioecious plants. However, little is known about the ethnobotany of dioecious species and whether preferences exist for a specific gender, e.g., in food, medicine or timber. AIM OF THE STUDY: The aim of this study was: 1) to study whether Indian folk healers have preference for plant genders, and to document their knowledge and use of dioecious species; 2) to understand the concept of plant gender in Indian systems of medicine and folk medicine, and whether Ayurvedic literature includes any references to gender preference. MATERIALS AND METHODS: Lists of dioecious plants used in Indian systems of medicine and folk medicine were compiled. Ethnobotanical data was collected on perceptions and awareness of dioecious plants, and preferences of use for specific genders of dioecious species using semi-structured interviews with folk healers in Tamil Nadu, India. In addition, twenty Ayurvedic doctors were interviewed to gain insight into the concept of plant gender in Ayurveda. RESULTS: Indian systems of medicine contain 5-7% dioecious species, and this estimate is congruent with the number of dioecious species in flowering plants in general. Informants recognized the phenomenon of dioecy in 31 out of 40 species, and reported gender preferences for 13 species with respect to uses as timber, food and medicine. Among informants different plant traits such as plant size, fruit size, and visibility of fruits determines the perception of a plant being a male or female. Ayurvedic classical literature provides no straightforward evidence on gender preferences in preparation of medicines or treatment of illness, however it contains details about reproductive morphology and sexual differentiation of plants. CONCLUSIONS: A knowledge gap exists in ethnobotanical and ethnopharmacological literature on traditional knowledge of dioecious plants. From this explorative study it is evident that people have traditional knowledge on plant gender and preferential usages towards one gender. Based on this, we propose that researchers conducting ethnobotanical and ethnopharmacological studies should consider documenting traditional knowledge on sexual systems of plants, and test the existence of gender specific usages in their conceptual framework and hypothesis testing. Incorporating such concepts could provide new dimensions of scientific knowledge with potential implications to conservation biology, chemical ecology, ethnoecology and drug discovery.

Metabolic and Performance Effects of Yerba Mate on Well-trained Cyclists.

INTRODUCTION: Yerba Mate (YM) is a South American plant, rich in polyphenols, saponins, and xanthines, of growing scientific interest because of its metabolic effects. YM has been shown to increase fat utilization during exercise in untrained humans, but its effects on well-trained individuals during exercise are unknown. METHODS: We characterized metabolic and physical performance effects of YM in 11 well-trained male cyclists. In a double-blind crossover design, participants ingested 5 g of YM or placebo (PL; maltodextrin) daily for 5 d and 1 h before experimental trials. RESULTS: Ergometer-based tests included a submaximal step test (SST) at 30%-80% of V˙O2max (6 × 5-min stages), followed by a cycloergometer-based time trial (TT) test to complete mechanical work (~30 min; n = 9). Before and during tests, blood and respiratory gas samples were collected. YM increased resting plasma adrenaline concentration (P = 0.002), and fat utilization by 23% at 30%-50% V˙O2max versus PL (Glass effect sizes (ES) ± 95% confidence interval (CI), 0.8 ± 0.55) correlating strongly with post-SST plasma (glycerol; r = 0.758). Treatment effects on rates of perceived exertion, heart rate, and gross efficiency were unclear during SST. Respiratory exchange ratio during TT indicated carbohydrate dependence and did not differ between treatments (PL, 0.95 ± 0.03 (SD); YM, 0.95 ± 0.02). TT performance showed a small (ES = 0.38 ± 0.33) but significant (P = 0.0278) improvement with YM (PL, 30.1 ± 1.8 min (SD); YM, 29.4 ± 1.4 min; 2.2% ± 2% (95% CI)), with an average increase of 7-W power output (ES = 0.2 ± 0.19; P = 0.0418; 2.3% ± 2% (95% CI)) and 2.8% V˙O2 (P = 0.019). Pacing displayed lower power output after 30% of total TT workload in PL vs YM. CONCLUSIONS: YM increased fat utilization during submaximal exercise and improved TT performance, but performance-enhancement effect was unrelated to measures of substrate metabolism during maximal exercise.

Enhanced Glucose Uptake in Human Liver Cells and Inhibition of Carbohydrate Hydrolyzing Enzymes by Nordic Berry Extracts.

A Western lifestyle with low physical activity and a diet rich in sugar, fat and processed food contribute to higher incidences of diabetes and obesity. Enhanced glucose uptake in human liver cells was observed after treatment with phenolic extracts from different Nordic berries. All berry extracts showed higher inhibition against α-amylase and α-glucosidase than the anti-diabetic agent acarbose. Total phenolic content and phenolic profiles in addition to antioxidant activities, were also investigated. The berries were extracted with 80% methanol on an accelerated solvent extraction system (ASE) and then purified by C-18 solid phase extraction (SPE). Among the ASE methanol extracts, black chokeberry, crowberry and elderberry extracts showed high stimulation of glucose uptake in HepG2 cells and also considerable inhibitory effect towards carbohydrate hydrolyzing enzymes. SPE extracts with higher concentrations of phenolics, resulted in increased glucose uptake and enhanced inhibition of α-amylase and α-glucosidase compared to the ASE extracts. Crowberry and cloudberry were the most potent 15-lipoxygenase inhibitors, while bog whortleberry and lingonberry were the most active xanthine oxidase inhibitors. These results increase the value of these berries as a component of a healthy Nordic diet and have a potential benefit against diabetes.

Elderberry and Elderflower Extracts, Phenolic Compounds, and Metabolites and Their Effect on Complement, RAW 264.7 Macrophages and Dendritic Cells.

Modulation of complement activity and inhibition of nitric oxide (NO) production by macrophages and dendritic cells may have therapeutic value in inflammatory diseases. Elderberry and elderflower extracts, constituents, and metabolites were investigated for their effects on the complement system, and on NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages and murine dendritic D2SC/I cells. The EtOH crude extracts from elderberry and elderflower and the isolated anthocyanins and procyanidins possessed strong complement fixating activity and strong inhibitory activity on NO production in RAW cells and dendritic cells. Phenolic compounds in the range of 0.1-100 µM showed a dose-dependent inhibition of NO production, with quercetin, rutin, and kaempferol as the most potent ones. Among the metabolites, caffeic acid and 3,4-dihydroxyphenylacetic acid showed the strongest inhibitory effects on NO production in both cell lines, without having cytotoxic effect. Only 4-methylcatechol was cytotoxic at the highest tested concentration (100 µM). Elderberry and elderflower constituents may possess inflammatory modulating activity, which increases their nutritional value.

Phenolic Elderberry Extracts, Anthocyanins, Procyanidins, and Metabolites Influence Glucose and Fatty Acid Uptake in Human Skeletal Muscle Cells.

Uptake of glucose and fatty acids in skeletal muscle is of interest for type 2 diabetes treatment. The aim was to study glucose and fatty acid uptake in skeletal muscle cells, antioxidant effects, and inhibition of carbohydrate-hydrolyzing enzymes by elderberries. Enhanced glucose and oleic acid uptake in human skeletal muscle cells were observed after treatment with phenolic elderberry extracts, anthocyanins, procyanidins, and their metabolites. The 96% EtOH and the acidified MeOH extracts were highly active. Of the isolated substances, cyanidin-3-glucoside and cyanidin-3-sambubioside showed highest stimulation of uptake. Phloroglucinol aldehyde was most active among the metabolites. Isolated anthocyanins and procyanidins are strong radical scavengers and are good inhibitors of 15-lipoxygenase and moderate inhibitors of xanthine oxidase. As α-amylase and α-glucosidase inhibitors, they are considerably better than the positive control acarbose. The antidiabetic property of elderberry phenolics increases the nutritional value of this plant and indicates potential as functional food against diabetes.