Phytochemicals and Biological Activities of Burdock (Arctium lappa L.) Extracts: A Review.

Arctium lappa L., also known as burdock, is an edible wild plant which has the ability to grow in distinct environments and is considered a weed in several parts of the world. This species has great value in the biological and medical fields with its major secondary components being phenolic compounds and terpenes, substances rich in desired biological activities as antioxidant, antimicrobial, antitumor and anti-inflammatory. In addition, burdock leaves extracts have shown a modulatory effect on the complement system, which plays an important role in the development of inflammatory diseases, with an inhibitory effect on all complement pathways. Thus, natural products with those relevant activities are promising agents for healthcare applications. Therefore, the species A. lappa may represent an interesting asset for researching and developing new therapies for inflammatory afflictions.

Otimização de método extrativo para raízes de Arctium lappa L / Extractive method optimization for Arctium lappa l. Roots / Optimización de un método de extracción de raíces de Arctium lappa L

Arctium lappa L. é indicada no Formulário de Fitoterápicos da Farmacopeia Brasileira para o tratamento de distúrbios urinários leves. Estudos já demonstraram o potencial antioxidante, anti-inflamatório e antidiabético deste extrato, onde foram identificados fenóis, lignanas, taninos e flavonoides. O objetivo deste trabalho foi otimizar o método extrativo de raízes de A. lappa. Realizou-se o preparo de extratos por diferentes métodos: Ultrassom, Soxhlet, maceração e turbo extração. A otimização foi realizada por turbo extração seguindo um planejamento fatorial 23, empregando como fatores: teor alcoólico, concentração da matéria prima e tempo de extração. Os extratos foram avaliados quanto ao resíduo seco, teores de fenóis e flavonoides, e atividade antioxidante. Com relação ao resíduo seco, e aos teores de fenóis e flavonoides, os métodos de ultrassom e turbo extração demonstraram melhor poder extrativo. Devido ao menor tempo e custo operacional, a otimização foi realizada por turbo extração, e o extrato otimizado foi obtido utilizando álcool 60%, em proporção matéria prima solvente 1:10 e tempo de extração de 15 minutos. Estas análises poderão nortear futuros testes de transposição de método para escala industrial, diminuindo mão de obra, tempo e custos, visando obter produtos fitoterápicos mais eficientes, com valor acessível à população.

Arctium lappa L. is indicated in the Brazilian Pharmacopeia Herbal Medicines Form for the treatment of mild urinary disorders. Studies have already demonstrated the antioxidant, anti-inflammatory and antidiabetic potential of this extract, where phenols, lignans, tannins and flavonoids were identified. The objective of this work was to optimize the extractive method of A. lappa roots. Extracts were prepared by different methods: Ultrasound, Soxhlet, maceration and vortical extraction. The optimization was performed by vortical extraction following a 23 full factorial design, using as factors: alcohol content, drug concentration and extraction time. The extracts were evaluated for dry residue, phenols and flavonoids contents, and antioxidant activity. Regarding the dry residue, and the phenols and flavonoids contents, the ultrasound and vortical extraction methods showed better extractive power. Due to the lower operating time and cost, the optimization was performed by vortical extraction, and the optimized extract was obtained using 60% alcohol, in a 1:10 drug solvent ratio and extraction time of 15 minutes. These assessments guide the future tests of transposition of the method to an industrial scale, reducing manpower, time and costs, aiming to obtain more efficient phytotherapic products, with affordable value for the population.

Arctium lappa L. está indicado en la Formulacao de Fitoterápicos da Farmacopeia Brasileira para el tratamiento de trastornos urinarios leves. Los estudios han demostrado el potencial antioxidante, antiinflamatorio y antidiabético de este extracto, donde se identificaron fenoles, lignanos, taninos y flavonoides. El objetivo de este trabajo fue optimizar el método extractivo de las raíces de A. lappa. Los extractos se prepararon por diferentes métodos: Ultrasonido, Soxhlet, maceración y turboextracción. La optimización se realizó mediante turboextracción siguiendo una planificación factorial de 23, empleando como factores: tenor alcohólico, concentración de materia prima y tiempo de extracción. Se evaluaron los extractos para determinar el residuo seco, el contenido de fenoles y flavonoides y la actividad antioxidante. En cuanto al contenido de residuo seco, fenoles y flavonoides, los métodos de extracción por ultrasonidos y turbo demostraron un mejor poder de extracción. Debido al menor tiempo y coste operativo, la optimización se realizó mediante turboextracción, y el extracto optimizado se obtuvo utilizando alcohol 60%, en proporción disolvente-materia 1:10 y tiempo de extracción de 15 minutos. Estos análisis podrán orientar futuros ensayos de transposición del método para escala industrial, reduciendo mano de obra, tiempo y costes, con el objetivo de obtener productos fitoterapéuticos más eficientes, con valor accesible para la población.

Effectiveness of different methods for the extraction of principle actives and phytochemicals content in medicinal herbals / Efectividad de diferentes métodos para la extracción de principios activos y contenido de fitoquímicos en hierbas medicinales

In this present study, we investigated the influence of various extraction methods including maceration, sonication, infusion, decoction, and microwave extraction, on the chemical and biological potential of phytochemicals extracted from three medicinal plants (Ageratum conyzoides, Plantago majorand Arctium lappa L). The results were subsequently analyzed by variance analysis. Our results suggested that sonication is the most effective extraction method among the five methods tested herein, for the extraction of phytochemicals that have a high antioxidant potential and high phenolic content. The three plants employed for this study had a high concentration of flavonoids and phenolics which was compatible with the chemosystematics of the species. All the samples possessed a Sun Protection Factor (SPF) of less than 6. Interestingly, a maximum reaction time of approximately 20 min was noted for the complexation of AlCl3 with the flavonoids present in the phytochemical extract during analyses of the kinetic parameters. We finally identified that the Ageratum conyzoides extract, prepared by sonication, possessed a significant pharmacological potential against hepatocarcinoma tumour cells, whose result can guide further studies for its therapeutic efficacy.

En el presente estudio, investigamos la influencia de varios métodos de extracción, incluyendo maceración, sonicación, infusión, decocción y extracción por microondas, sobre el potencial químico y biológico de los fitoquímicos extraídos de tres plantas medicinales (Ageratum conyzoides, Plantago majory Arctium lappa L). Los resultados se analizaron posteriormente mediante análisis de varianza. Nuestros resultados sugieren que la sonicación es el método de extracción más eficaz entre los cinco métodos aquí probados, para la extracción de fitoquímicos que tienen un alto potencial antioxidante y un alto contenido fenólico. Las tres plantas empleadas para este estudio tenían una alta concentración de flavonoides y fenólicos que era compatible con la quimiosistemática de las especies. Todas las muestras poseían un factor de protección solar (SPF) menor a 6. Curiosamente, se observó un tiempo máximo de reacción de aproximadamente 20 min para la complejación de AlCl3con los flavonoides presentes en el extracto fitoquímico durante los análisis de los parámetros cinéticos. Finalmente, identificamos que el extracto de Ageratum conyzoides, elaborado por sonicación, posee un importante potencial farmacológico frente a las células tumorales del hepatocarcinoma, cuyo resultado puede orientar nuevos estudios sobre su eficacia terapéutica.

Burdock (Arctium lappa L) roots as a source of inulin-type fructans and other bioactive compounds: Current knowledge and future perspectives for food and non-food applications.

The roots and tubers of the Asteraceae family are known as a source of various oligosaccharides, and chicory roots and Jerusalem artichoke have stood out for its commercial viability. However burdock root (Arctium lappa L.), which is adapted to temperate climate, moist, and sandy soil, is still unknown as health food in the western world. This review showed the potential of burdock roots as a source of prebiotic fibers, chlorogenic acids, cinnarine, lignans, and quercetin. The extraction methods of burdock functional compounds are made with water, temperature and time variations only. Biological assays showed antioxidant activity, anti-inflammatory, and hypolipidemic properties, and gastric mucosal defense mechanisms, among others. Therefore, the use of burdock roots as functional food should be encouraged in countries that have imported products derived from other roots of the same family for health benefits.

Burdock (Arctium lappa L.) root attenuates preneoplastic lesion development in a diet and thioacetamide-induced model of steatohepatitis-associated hepatocarcinogenesis.

Nonalcoholic steatohepatitis (NASH) is considered growing risk factor for hepatocellular carcinoma development in high-income countries. Diet- and chemically induced rodent models have been applied for the translational study of NASH-associated hepatocarcinogenesis due to their morphological and molecular similarities to the corresponding human disease. Arctium lappa L. (burdock) root tea has been extensively consumed in Traditional Chinese Medicine due to its potential therapeutic properties. Indeed, the bioactive compounds of A. lappa root, as the polyphenols, have already showed antioxidant and anti-inflammatory properties in different in vivo and in vitro bioassays. In this study, we investigated whether burdock root ethanolic extract (BRE) administration attenuates NASH-associated hepatocarcinogenesis. Eight-week-old male Wistar rats received choline-deficient high-fat diet for 8 weeks and multiple thioacetamide doses for 4 weeks in order to induce NASH and preneoplastic glutathione-S-transferase pi (GST-P)+ preneoplastic foci. Subsequently, rats were treated with BRE (100 or 200 mg/kg body weight) or vehicle by oral gavage for 2 weeks. BRE displayed high levels of chlorogenic and caffeic acids and BRE administration reduced total fatty acid and lipid hydroperoxide levels, while increasing the activities of antioxidant superoxide dismutase and catalase enzymes in the liver. Furthermore, burdock intervention diminished the size of GST-P+ remodeling preneoplastic lesions (PNLs) and displayed a trend on reducing hepatocyte proliferation (Ki-67) inside them. These findings suggest that short-term exposure to BRE alleviated remodeling PNL development in NASH-associated hepatocarcinogenesis.

Inhibitory Effect of Supercritical Extracts from Arctium lappa L. on the Lectin Pathway of the Complement System.

The complement system participates in host defense by eliminating microorganisms and triggering inflammation. However, insufficient control or exacerbated complement activation contributes to inflammatory diseases. Since promising antioxidant and anti-inflammatory activities have been identified in Arctium lappa L. extracts, this study aims to explore the effect of A. lappa extracts on the lectin pathway (LP) of complement activation. Four extracts were obtained by supercritical extraction using scCO2 with or without ethanol as co-solvent, at different temperatures and pressures (E1: 2.2 mg/mL, E2: 2.6 mg/mL and E3: 2.0 mg/mL, E4: 1.5 mg/mL). To evaluate the effect of A. lappa extracts on the LP activation, an ELISA assay using mannose binding lectin pathway of complement was carried out with C4 detection. All extracts showed a concentration-dependent inhibitory effect on the activation of complement by the LP. The following IC50 were observed for E1, E2, E3 and E4: 179.4 µg/mL, 74.69 µg/mL, 119.1 µg/mL and 72.19 µg/mL, respectively. Our results suggest that A. lappa extracts are potential candidates for the treatment of inflammatory disorders that are complement-related.

Enzymatic preparation of fructooligosaccharides-rich burdock syrup with enhanced antioxidative properties

Background: Burdock (Arctium lappa L.) is a fructan-rich plant with prebiotic potential. The aim of this study was to develop an efficient enzymatic route to prepare fructooligosaccharides (FOS)-rich and highly antioxidative syrup using burdock root as a raw material. Results: Endo-inulinase significantly improved the yield of FOS 2.4-fold while tannase pretreatment further increased the yield of FOS 2.8-fold. Other enzymes, including endo-polygalacturonase, endo-glucanase and endo-xylanase, were able to increase the yield of total soluble sugar by 11.1% (w/w). By this process, a new enzymatic process for burdock syrup was developed and the yield of burdock syrup increased by 25% (w/w), whereas with FOS, total soluble sugars, total soluble protein and total soluble polyphenols were enhanced to 28.8%, 53.3%, 8.9% and 3.3% (w/w), respectively. Additionally, the scavenging abilities of DPPH and hydroxyl radicals, and total antioxidant capacity of the syrup were increased by 23.7%, 51.8% and 35.4%, respectively. Conclusions: Our results could be applied to the development of efficient extraction of valuable products from agricultural materials using enzyme-mediated methods.

New phytochemicals as potential human anti-aging compounds: Reality, promise, and challenges.

Aging is an inevitable process influenced by genetic, lifestyle, and environmental factors. Indirect evidence shows that several phytochemicals can have anti-aging capabilities, although direct evidence in this field is still limited. This report aims to provide a critical review on aspects related to the use of novel phytochemicals as anti-aging agents, to discuss the obstacles found when performing most anti-aging study protocols in humans, and to analyze future perspectives. In addition to the extensively studied resveratrol, epicatechin, quercetin, and curcumin, new phytochemicals have been reported to act as anti-aging agents, such as the amino acid L-theanine isolated from green tea, and the lignans arctigenin and matairesinol isolated from Arctium lappa seeds. Furthermore, this review discusses the application of several new extracts rich in phytochemicals with potential use in anti-aging therapies. Finally, this review also discusses the most important biomarkers to test anti-aging interventions, the necessity of conducting epidemiological studies and the need of clinical trials with adequate study protocols for humans.

Arctium minus crude extract presents antinociceptive effect in a mice acute gout attack model.

Gout is a disorder that triggers a severe inflammatory reaction which generates episodes of intense pain and discomfort to the patient. Arctium minus (Hill) Bernh. (Asteraceae) is known as "burdock" and displays anti-inflammatory, antinociceptive, against rheumatic pain and radical-scavenging activities. Species of the genus Arctium have been used in assistant therapy of gout and other inflammatory processes. We investigated the antinociceptive and anti-edematogenic effects of the crude extract of A. minus seeds in an acute gout attack model induced by intra-articular injection of monosodium urate (MSU) crystals in adult male Swiss mice (25-30 g). The crude extract of A. minus (100 mg/kg, p.o.) reduced the mechanical allodynia induced by the injection of MSU (1.25 mg/site, i.a.) from 4 until 8 h after its administration. A. minus seeds crude extract prevented mechanical allodynia at doses of 30 and 100 mg/kg, but not 10 mg/kg. Allopurinol (10 µg/mL) and A. minus crude extract (10-300 µg/mL) inhibited the xanthine oxidase activity in vitro. The A. minus seeds crude extract did not cause adverse effects since did not change the toxicological parameters evaluated. A. minus crude extract can be used as an assistant therapy of gout pain, supporting its traditional use, without causing adverse effects.

Acid-gastric antisecretory effect of the ethanolic extract from Arctium lappa L. root: role of H+, K+-ATPase, Ca2+ influx and the cholinergic pathway.

BACKGROUND: Arctium lappa L., popularly known as burdock, is a medicinal plant used worldwide. The antiulcer and gastric-acid antisecretory effects of ethanolic extract from roots of Arctium lappa (EET) were already demonstrated. However, the mechanism by which the extract reduces the gastric acid secretion remains unclear. Therefore, this study was designed to evaluate the antisecretory mode of action of EET. MATERIALS AND METHODS: The effects of EET on H+, K+-ATPase activity were verified in vitro, whereas the effects of the extract on cholinergic-, histaminergic- or gastrinergic-acid gastric stimulation were assessed in vivo on stimulated pylorus ligated rats. Moreover, ex vivo contractility studies on gastric muscle strips from rats were also employed. RESULTS: The incubation with EET (1000 µg/ml) partially inhibited H+, K+-ATPase activity, and the intraduodenal administration of EET (10 mg/kg) decreased the volume and acidity of gastric secretion stimulated by bethanechol, histamine, and pentagastrin. EET (100-1000 µg/ml) did not alter the gastric relaxation induced by histamine but decreased acetylcholine-induced contraction in gastric fundus strips. Interestingly, EET also reduced the increase in the gastric muscle tone induced by 40 mM KCl depolarizing solution, as well as the maximum contractile responses evoked by CaCl2 in Ca2+-free depolarizing solution, without impairing the effect of acetylcholine on fundus strips maintained in Ca2+ -free nutritive solution. CONCLUSION: Our results reinforce the gastric antisecretory properties of preparations obtained from Arctium lappa, and indicate that the mechanisms involved in EET antisecretory effects include a moderate reduction of the H+, K+-ATPase activity associated with inhibitory effects on calcium influx and of cholinergic pathways in the stomach muscle.

In vitro schistosomicidal and antiviral activities of Arctium lappa L. (Asteraceae) against Schistosoma mansoni and Herpes simplex virus-1.

Schistosomiasis and herpes diseases represent serious issues to the healthcare systems, infecting a large number of people worldwide, mainly in developing countries. Arctium lappa L. (Asteraceae), known as "bardana" and "burdock", is a medicinal plant popularly used for several purposes, including as antiseptic. In this study, we evaluated the in vitro schistosomicidal and antiherpes activities of the crude extract of A. lappa, which have not yet been described. Fruits of A. lappa L. were extracted by maceration with ethanol: H2O (96:4 v/v) in order to obtain the hydroalcoholic extract of A. lappa (AL). In vitro schistosomicidal assays were assessed against adult worms of Schistosoma mansoni, while the in vitro antiviral activity of AL was evaluated on replication of Herpes simplex virus type-1 (HSV-1). Cell viability was measured by MTT assay, using Vero cells and chemical composition of AL was determined by qualitative UPLC-ESI-QTOF-MS analysis. UPLC-ESI-QTOF-MS analysis of AL revealed the presence of dibenzylbutyrolactone lignans, such as arctiin and arctigenin. Results showed that AL was not cytotoxic to Vero cells even when tested at 400µg/mL. qPCR results indicated a significant viral load decreased for all tested concentrations of AL (400, 50, and 3.125µg/mL), which showed similar antiviral effect to acyclovir (50µg/mL) when tested at 400µg/mL. Also, AL (400, 200, and 100µg/mL) caused 100% mortality and significantly reduction on motor activity of all adult worms of S. mansoni. Confocal laser scanning microscopy showed tegumental morphological alterations and changes on the numbers of tubercles of S. mansoni worms in a dose-dependent manner after treatment with AL. This report provides the first evidence for the in vitro schistosomicidal and antiherpes activities of AL, opening the route to further schistosomicidal and antiviral studies with AL and their compounds, especially lignans.

Prebiotic effects of inulin extracted from burdock (Arctium lappa) in broilers / Efeito prebiótico da inulina extraída da bardana (Arctium lappa) em frangos de corte

The aim of this study was to evaluate the prebiotic effect of burdock (Arctium lappa) in commercial poultry. Four experiments were conducted to evaluate the performance parameters and the protection after challenge with Salmonella Enteritidis and Salmonella Kedougou, with and without Bifidobacterium probiotic. In two trials, the chickens were fed with flour burdock 1% during 42 days. In the other two, the chickens were fed with fructan extracted from burdock (inulin), by gavage, at a concentration of 100 mg/bird, during the first three days of life. The results showed that the broilers treated with burdock flour showed underperformed, with less weight gain from the second week, and the worst results in the fattening stage. The treated birds had diarrhea and impaired intestinal integrity. However, the groups treated with the flour had a lower rate of intestinal colonization by Salmonella Kedougou, after challenge. No statistically significant differences were detected in the performance parameters of broilers receiving the inulin, and the morphometric analysis showed no lesions in the intestinal villi. However, there was no protection in the challenge with Salmonella Enteritidis, regardless of association with probiotic. These results demonstrated that the manner of administration has influence on the prebiotic effect of burdock. The burdock flour was administered for 42 days, which may have influenced intestinal mucosal injury. Instead, the inulin was given only in the first three days, which may have been insufficient for protection against Salmonella. New experiments are needed to determine an able formulation for a protective effect, without negative impact on growth, weight gain and feed conversion of the supplemented animals.(AU)

Este projeto teve por objetivo avaliar o efeito prebiótico da bardana (Arctium lappa) em aves comerciais. Foram realizados quatro experimentos para avaliar os parâmetros zootécnicos e o grau de proteção após o desafio com Salmonella Kedougou e Salmonella Enteritidis, com e sem a adição de probióticos à base de Bifidobacterium. Em dois experimentos, as aves receberam a farinha de bardana 1% na ração, durante 42 dias. Nos outros dois, as aves receberam o frutano extraído da bardana (inulina), por gavagem, na concentração de 100 mg/ave, nos três primeiros dias de vida. Os resultados demonstraram que os frangos tratados com farinha de bardana apresentaram desempenho zootécnico inferior ao controle, com menor ganho de peso a partir da segunda semana e piores resultados na fase de engorda. As aves tratadas apresentaram diarreia e comprometimento da integridade intestinal. Em contrapartida, os grupos tratados com a farinha tiveram menor taxa de colonização intestinal por Salmonella Kedougou, após o desafio. Não foram detectadas diferenças estatisticamente significativas nos parâmetros zootécnicos dos frangos que receberam a inulina, e a análise morfométrica não evidenciou lesões nas vilosidades intestinais. No entanto, não houve proteção no desafio por Salmonella Enteritidis, independentemente da associação com probiótico. Esses resultados demonstraram que o modo de administração tem influência sobre o efeito prebiótico da bardana. A farinha de bardana foi administrada por 42 dias, o que pode ter causado a lesão da mucosa intestinal. Em contrapartida, a inulina foi administrada apenas nos primeiros três primeiros dias, o que pode ter sido insuficiente para proteção contra Salmonella. Novos experimentos são necessários para determinar uma formulação capaz de promover efeito protetor, sem impacto negativo no crescimento, ganho de peso e conversão alimentar dos animais suplementados.(AU)

Prebiotic effects of inulin extracted from burdock (Arctium lappa) in broilers / Efeito prebiótico da inulina extraída da bardana (Arctium lappa) em frangos de corte

The aim of this study was to evaluate the prebiotic effect of burdock (Arctium lappa) in commercial poultry. Four experiments were conducted to evaluate the performance parameters and the protection after challenge with Salmonella Enteritidis and Salmonella Kedougou, with and without Bifidobacterium probiotic. In two trials, the chickens were fed with flour burdock 1% during 42 days. In the other two, the chickens were fed with fructan extracted from burdock (inulin), by gavage, at a concentration of 100 mg/bird, during the first three days of life. The results showed that the broilers treated with burdock flour showed underperformed, with less weight gain from the second week, and the worst results in the fattening stage. The treated birds had diarrhea and impaired intestinal integrity. However, the groups treated with the flour had a lower rate of intestinal colonization by Salmonella Kedougou, after challenge. No statistically significant differences were detected in the performance parameters of broilers receiving the inulin, and the morphometric analysis showed no lesions in the intestinal villi. However, there was no protection in the challenge with Salmonella Enteritidis, regardless of association with probiotic. These results demonstrated that the manner of administration has influence on the prebiotic effect of burdock. The burdock flour was administered for 42 days, which may have influenced intestinal mucosal injury. Instead, the inulin was given only in the first three days, which may have been insufficient for protection against Salmonella. New experiments are needed to determine an able formulation for a protective effect, without negative impact on growth, weight gain and feed conversion of the supplemented animals.(AU)

Este projeto teve por objetivo avaliar o efeito prebiótico da bardana (Arctium lappa) em aves comerciais. Foram realizados quatro experimentos para avaliar os parâmetros zootécnicos e o grau de proteção após o desafio com Salmonella Kedougou e Salmonella Enteritidis, com e sem a adição de probióticos à base de Bifidobacterium. Em dois experimentos, as aves receberam a farinha de bardana 1% na ração, durante 42 dias. Nos outros dois, as aves receberam o frutano extraído da bardana (inulina), por gavagem, na concentração de 100 mg/ave, nos três primeiros dias de vida. Os resultados demonstraram que os frangos tratados com farinha de bardana apresentaram desempenho zootécnico inferior ao controle, com menor ganho de peso a partir da segunda semana e piores resultados na fase de engorda. As aves tratadas apresentaram diarreia e comprometimento da integridade intestinal. Em contrapartida, os grupos tratados com a farinha tiveram menor taxa de colonização intestinal por Salmonella Kedougou, após o desafio. Não foram detectadas diferenças estatisticamente significativas nos parâmetros zootécnicos dos frangos que receberam a inulina, e a análise morfométrica não evidenciou lesões nas vilosidades intestinais. No entanto, não houve proteção no desafio por Salmonella Enteritidis, independentemente da associação com probiótico. Esses resultados demonstraram que o modo de administração tem influência sobre o efeito prebiótico da bardana. A farinha de bardana foi administrada por 42 dias, o que pode ter causado a lesão da mucosa intestinal. Em contrapartida, a inulina foi administrada apenas nos primeiros três primeiros dias, o que pode ter sido insuficiente para proteção contra Salmonella. Novos experimentos são necessários para determinar uma formulação capaz de promover efeito protetor, sem impacto negativo no crescimento, ganho de peso e conversão alimentar dos animais suplementados.(AU)

Prebiotic effects of inulin extracted from burdock (Arctium lappa) in broilers / Efeito prebiótico da inulina extraída da bardana (Arctium lappa) em frangos de corte

The aim of this study was to evaluate the prebiotic effect of burdock (Arctium lappa) in commercial poultry. Four experiments were conducted to evaluate the performance parameters and the protection after challenge with Salmonella Enteritidis and Salmonella Kedougou, with and without Bifidobacterium probiotic. In two trials, the chickens were fed with flour burdock 1% during 42 days. In the other two, the chickens were fed with fructan extracted from burdock (inulin), by gavage, at a concentration of 100 mg/bird, during the first three days of life. The results showed that the broilers treated with burdock flour showed underperformed, with less weight gain from the second week, and the worst results in the fattening stage. The treated birds had diarrhea and impaired intestinal integrity. However, the groups treated with the flour had a lower rate of intestinal colonization by Salmonella Kedougou, after challenge. No statistically significant differences were detected in the performance parameters of broilers receiving the inulin, and the morphometric analysis showed no lesions in the intestinal villi. However, there was no protection in the challenge with Salmonella Enteritidis, regardless of association with probiotic. These results demonstrated that the manner of administration has influence on the prebiotic effect of burdock. The burdock flour was administered for 42 days, which may have influenced intestinal mucosal injury. Instead, the inulin was given only in the first three days, which may have been insufficient for protection against Salmonella. New experiments are needed to determine an able formulation for a protective effect, without negative impact on growth, weight gain and feed conversion of the supplemented animals.

Este projeto teve por objetivo avaliar o efeito prebiótico da bardana (Arctium lappa) em aves comerciais. Foram realizados quatro experimentos para avaliar os parâmetros zootécnicos e o grau de proteção após o desafio com Salmonella Kedougou e Salmonella Enteritidis, com e sem a adição de probióticos à base de Bifidobacterium. Em dois experimentos, as aves receberam a farinha de bardana 1% na ração, durante 42 dias. Nos outros dois, as aves receberam o frutano extraído da bardana (inulina), por gavagem, na concentração de 100 mg/ave, nos três primeiros dias de vida. Os resultados demonstraram que os frangos tratados com farinha de bardana apresentaram desempenho zootécnico inferior ao controle, com menor ganho de peso a partir da segunda semana e piores resultados na fase de engorda. As aves tratadas apresentaram diarreia e comprometimento da integridade intestinal. Em contrapartida, os grupos tratados com a farinha tiveram menor taxa de colonização intestinal por Salmonella Kedougou, após o desafio. Não foram detectadas diferenças estatisticamente significativas nos parâmetros zootécnicos dos frangos que receberam a inulina, e a análise morfométrica não evidenciou lesões nas vilosidades intestinais. No entanto, não houve proteção no desafio por Salmonella Enteritidis, independentemente da associação com probiótico. Esses resultados demonstraram que o modo de administração tem influência sobre o efeito prebiótico da bardana. A farinha de bardana foi administrada por 42 dias, o que pode ter causado a lesão da mucosa intestinal. Em contrapartida, a inulina foi administrada apenas nos primeiros três primeiros dias, o que pode ter sido insuficiente para proteção contra Salmonella. Novos experimentos são necessários para determinar uma formulação capaz de promover efeito protetor, sem impacto negativo no crescimento, ganho de peso e conversão alimentar dos animais suplementados.

Polysaccharides from Arctium lappa L.: Chemical structure and biological activity.

The plant Arctium lappa L. is popularly used to relieve symptoms of inflammatory disorders. A crude polysaccharide fraction (SAA) resulting of aqueous extraction of A. lappa leaves showed a dose dependent anti-edematogenic activity on carrageenan-induced paw edema, which persisted for up to 48h. Sequential fractionation by ultrafiltration at 50kDa and 30kDa cut-off membranes yielded three fractions, namely RF50, RF30, and EF30. All these maintained the anti-edematogenic effect, but RF30 showed a more potent action, inhibiting 57% of the paw edema at a dose of 4.9mg/kg. The polysaccharide RF30 contained galacturonic acid, galactose, arabinose, rhamnose, glucose, and mannose in a 7:4:2:1:2:1 ratio and had a Mw of 91,000g/mol. Methylation analysis and NMR spectroscopy indicated that RF30 is mainly constituted by a type I rhamnogalacturonan branched by side chains of types I and II arabinogalactans, and arabinan.

Effects of Arctium lappa on Cadmium-Induced Damage to the Testis and Epididymis of Adult Wistar Rats.

The protective role of Arctium lappa (AL) on the testes of rats acutely exposed to cadmium (Cd) was tested. The rats were randomly divided into a control group (C-group) and three major experimental groups, which were further subdivided into minor groups (n = 6) according to the experimental period (7 or 56 days). The C-group was subdivided into C-7 and C-56 [receiving a single saline solution, intraperitoneal (i.p.), on the first day]; the AL-group, AL-7, and AL-56, received AL extract (300 mg/kg/daily); the Cd group, Cd-7 and Cd-56, received a single i.p. dose of CdCl2 (1.2 mg/kg body weight (BW)) on the first day; the CdAL group, CdAL-7 and CdAL-56, received the same Cd dose, followed by AL extract. Water or AL extract was administered daily by gavage. After either 7 or 56 days, the testis and accessory glands were removed after whole-body perfusion. Exposure to Cd and CdAL decreased the weight of the testis and epididymis, the gonadosomatic index, seminiferous tubular (ST) diameter, and ST volumetric proportion, and increased the volumetric proportion of interstitium after 56 days. In the epididymis caput, the tubular volumetric proportion decreased along with an increase of interstitial volumetric proportion and epithelium height after 56 days. The alterations observed were less severe only after 7 days. A progressive testicular damage resulted mainly in tubules lined only by Sertoli cells. The sperm number and cell debris decreased in the epididymis. We demonstrated that the testicular damage induced by single acute i.p. exposure to Cd occurred despite the daily oral intake of AL extract.

Identification of a dicaffeoylquinic acid isomer from Arctium lappa with a potent anti-ulcer activity.

Leaves of Arctium lappa contain several mono- and dicaffeoylquinic acids, as evaluated by liquid chromatography-mass spectrometry. In order to investigate the protection on gastric mucosa against ulcers, rats were treated with fractions from leaf extract prior to ethanol-induced ulcers. The original fraction obtained as ethanol soluble fraction from hot aqueous extract was able to protect de gastric mucosa, and this effect was retained in the ethyl acetate fraction, obtained from liquid/liquid fractionation. The main compound in this fraction was isolated and chemically characterized by nuclear magnetic resonance and mass spectrometry, assisted by isopropylidene derivatization which gave rise a mass increment of 40 units. Therefore, the underivatized compound that had m/z 515.119 [M-H](-) was shifted to m/z 555.151, being confirmed as 1,3-O-dicaffeoylquinic acid, which presented an ED50 of 57 µg kg(-1) on gastric protection, lesser than the therapeutic concentration of omeprazole (40 mg kg(-1)).

Partial Molecular Characterization of Arctium minus Aspartylendopeptidase and Preparation of Bioactive Peptides by Whey Protein Hydrolysis.

In this article, we report the cloning of an aspartic protease (AP) from flowers of Arctium minus (Hill) Bernh. (Asteraceae) along with the use of depigmented aqueous flower extracts, as a source of APs, for the hydrolysis of whey proteins. The isolated cDNA encoded a protein product with 509 amino acids called arctiumisin, with the characteristic primary structure organization of typical plant APs. Bovine whey protein hydrolysates, obtained employing the enzyme extracts of A. minus flowers, displayed inhibitory angiotensin-converting enzyme (ACE) and antioxidant activities. Hydrolysates after 3 and 5 h of reaction (degree of hydrolysis 2.4 and 5.6, respectively) and the associated peptide fraction with molecular weight below 3 kDa were analyzed by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, matrix-assisted laser desorption ionization/time of flight mass spectrometry, and reverse phase-high-performance liquid chromatography. The results obtained in this study demonstrate the viability of using proteases from A. minus to increase the antioxidant and inhibitory ACE capacity of whey proteins.

Anti-inflammatory intestinal activity of Arctium lappa L. (Asteraceae) in TNBS colitis model.

ETHNOPHARMACOLOGICAL RELEVANCE: In Brazilian traditional medicine, Arctium lappa (Asteraceae), has been reported to relieve gastrointestinal symptoms. AIM OF THE STUDY: In the present study, we investigated the effects of the lactone sesquiterpene onopordopicrin enriched fraction (ONP fraction) from Arctium lappa in an experimental colitis model induced by 2,4,6 trinitrobenzene sulfonic acid and performed experiments to elucidate the underlying action mechanisms involved in that effect. MATERIALS AND METHODS: ONP fraction (25 and 50 mg/kg/day) was orally administered 48, 24 and 1 h prior to the induction of colitis and 24 h after. The inflammatory response was assessed by gross appearance, myeloperoxidase (MPO) activity, tumor necrosis factor alpha (TNF-α) levels and a histological study of the lesions. We determined cyclooxygenase (COX)-1 and -2 protein expressions by western blotting and immunohistochemistry assays. RESULTS: TNBS group was characterized by increased colonic wall thickness, edema, diffuse inflammatory cell infiltration, increased MPO activity and TNF-α levels. On the contrary, ONP fraction (25 and 50 mg/kg) treatment significantly reduced the macroscopic inflammation scores (p<0.05 and p<0.01, respectively) and morphological alterations associated with an increase in the mucus secretion. Similarly, the degree of neutrophil infiltration and the cytokine levels were significantly ameliorated. Moreover, COX-2 expression was up regulated in TNBS-treated rats. In contrast, ONP fraction (50 mg/kg) administration reduced COX-2 overexpression. CONCLUSIONS: We have shown that the ONP fraction obtained from Arctium lappa exert marked protective effects in acute experimental colitis, confirming and justifying, at least in part, the popular use of this plant to treat gastrointestinal diseases.

Ethanolic extract of roots from Arctium lappa L. accelerates the healing of acetic acid-induced gastric ulcer in rats: Involvement of the antioxidant system.

We evaluate the curative efficacy of the ethanolic extract (EET) of roots from Arctium lappa (bardana) in healing of chronic gastric ulcers induced by 80% acetic acid in rats and additionally studies the possible mechanisms underlying this action. Oral administration of EET (1, 3, 10 and 30mg/kg) reduced the gastric lesion area in 29.2%, 41.4%, 59.3% and 38.5%, respectively, and at 10mg/kg promoted significant regeneration of the gastric mucosa, which was confirmed by proliferating cell nuclear antigen immunohistochemistry. EET (10mg/kg) treatment did not increase the gastric mucus content but restored the superoxide dismutase activity, prevented the reduction of glutathione levels, reduced lipid hydroperoxides levels, inhibited the myeloperoxidase activity and reduced the microvascular permeability. In addition, EET reduced the free radical generation and increased scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals in vitro. Furthermore, intraduodenal EET (10 and 30mg/kg) decreased volume and acidity of gastric secretion. Total phenolic compounds were high in EET (Folin-Ciocalteau assay) and the analysis by liquid chromatography-mass spectrometry revealed that the main compounds present in EET were a serie of hydroxycinnamoylquinic acid isomers. In conclusion, these data reveal that EET promotes regeneration of damaged gastric mucosa, probably through its antisecretory and antioxidative mechanisms.