Integrated Mechanism of Immune Response Modulation by Arctium Lappa L. Fructans Based on Microbiome and Metabolomics Technologies.

Arctium lappa L. is widely consumed for its various biological effects, and polysaccharides are its main functional components. The present study aimed to evaluate the immunoregulatory effects of the main polysaccharides from burdock (ALP-1) and reveal the underlying mechanisms. ALP-1 consisted of fructose and glucose (14.57:1) and had a molecular weight of 2757 Da, with typical characteristics of (1 → 2)-linked linear fructans. Oral intake of ALP-1 significantly increased the number of colonic goblet cells, serum immunoglobulin A and immunoglobulin G levels, and fecal secretory immunoglobulin A content as well as up-regulated antioxidant enzymes and increased short chain fatty acid production. In addition, ALP-1 administration regulated pro/anti-inflammatory cytokines (i.e., interleukin (IL)-1ß, IL-6, tumor necrosis factor-α, interferon-γ, and IL-10), intestinal microbiota structure, and the spatial information on key metabolites. Some gut-microbiota-mediated metabolic processes were also significantly altered. These results indicated that ALP-1 could exert beneficial effects on immune responses and intestinal health in healthy mice.

Arctigenin from Arctium lappa L. inhibits chikungunya virus by affecting its entry and replication.

BACKGROUND: Dengue and chikungunya, caused by dengue virus (DENV) and chikungunya virus (CHIKV) respectively, are the most common arthropod-borne viral diseases worldwide, for which there are no FDA-approved antivirals or effective vaccines. Arctigenin, a phenylpropanoid lignan from the seeds of Arctium lappa L. is known for its anti-inflammatory, anti-cancer, antibacterial, and immunomodulatory properties. Arctigenin's antimicrobial and immunomodulatory capabilities make it a promising candidate for investigating its potential as an anti-DENV and anti-CHIKV agent. PURPOSE: The aim of the study was to explore the anti-DENV and anti-CHIKV effects of arctigenin and identify the possible mechanisms of action. METHODS: The anti-DENV or anti-CHIKV effects of arctigenin was assessed using various in vitro and in silico approaches. Vero CCL-81 cells were infected with DENV or CHIKV and treated with arctigenin at different concentrations, temperature, and time points to ascertain the effect of the compound on virus entry or replication. In silico molecular docking was performed to identify the interactions of the compound with viral proteins. RESULTS: Arctigenin had no effects on DENV. Various time- and temperature-dependent assays revealed that arctigenin significantly reduced CHIKV RNA copy number and infectious virus particles and affected viral entry. Entry bypass assay revealed that arctigenin inhibited the initial steps of viral replication. In silico docking results revealed the high binding affinity of the compound with the E1 protein and the nsp3 macrodomain of CHIKV. CONCLUSION: This study demonstrates the in-vitro anti-CHIKV potential of arctigenin and suggests that the compound might affect CHIKV entry and replication. Further preclinical and clinical studies are needed to identify its safety and efficacy as an anti-CHIKV drug.

Arctium lappa L. polysaccharides enhanced the therapeutic effects of nasal ectomesenchymal stem cells against liver fibrosis by inhibiting the Wnt/ß-catenin pathway.

The oxidative microenvironment in fibrotic livers often diminishes the effectiveness of mesenchymal stem cells (MSCs)-based therapy. Recent research suggests that pharmacological pre-treatment could enhance the therapeutic performance of MSCs. In this study, we assessed the impact of Arctium lappa L. polysaccharides (ALP) on the biological properties of nasal ectomesenchymal stem cells (EMSCs) and investigated the augmenting effect of ALP pretreatment on EMSCs (ALP-EMSCs) for the treatment of liver fibrosis. ALP treatment demonstrated multiple biological impacts on EMSC functions regarding liver fibrosis: firstly, it maintained the stemness of the cells while boosting the EMSCs' paracrine effects; secondly, it increased the expression of anti-inflammatory and antioxidant factors; thirdly, it inhibited the activation of hepatic stellate cells (HSCs) and liver collagen build-up by modulating the Wnt/ß-catenin signaling pathways. Collectively, these effects helped to halt the progression of liver fibrosis. Therefore, the use of ALP-EMSCs presents an innovative and promising approach for treating hepatic fibrosis in clinical scenarios.

An ethanolic extract of Arctium lappa L. leaves ameliorates experimental atherosclerosis by modulating lipid metabolism and inflammatory responses through PI3K/Akt and NF-κB singnaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Atherosclerosis (AS), a lipid-induced inflammatory condition of the arteries, is a primary contributor to atherosclerotic cardiovascular diseases including stroke. Arctium lappa L. leaf (ALL), an edible and medicinal herb in China, has been documented and commonly used for treating stroke since the ancient times. However, the elucidations on its anti-AS effects and molecular mechanism remain insufficient. AIM OF THE STUDY: To investigate the AS-ameliorating effects and the underlying mechanism of action of an ethanolic extract of leaves of Arctium lappa L. (ALLE). MATERIALS AND METHODS: ALLE was reflux extracted using with 70% ethanol. An HPLC method was established to monitor the quality of ALLE. High fat diet (HFD) and vitamin D3-induced experimental AS in rats were used to determine the in vivo effects; and oxidized low-density lipoprotein-induced RAW264.7 macrophage foam cells were used for in vitro assays. Simvatatin was used as positive control. Biochemical assays were implemented to ascertain the secretions of lipids and pro-inflammatory mediators. Haematoxylin-eosin (H&E) and Oil red O stains were employed to assess histopathological alterations and lipid accumulation conditions, respectively. CCK-8 assays were used to measure cytotoxicity. Immunoblotting assay was conducted to measure protein levels. RESULTS: ALLE treatment significantly ameliorated lipid deposition and histological abnormalities of aortas and livers in AS rats; improved the imbalances of serum lipids including total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C) and high-density lipoprotein cholesterol (HDL-C); notably attenuated serum concentrations of inflammation-associated cytokines/molecules including TNF-α, IL-6, IL-1ß, VCAM-1, ICAM-1and MMP-9. Mechanistic studies demonstrated that ALLE suppressed the phosphorylation/activation of PI3K, Akt and NF-κB in AS rat aortas and in cultured foam cells. Additionally, the PI3K agonist 740Y-P notably reversed the in vitro inhibitory effects of ALLE on lipid deposition, productions of TC, TNF-α and IL-6, and protein levels of molecules of PI3K/Akt and NF-κB singnaling pathways. CONCLUSIONS: ALLE ameliorates HFD- and vitamin D3-induced experimental AS by modulating lipid metabolism and inflammatory responses, and underlying mechanisms involves inhibition of the PI3K/Akt and NF-κB singnaling pathways. The findings of this study provide scientific justifications for the traditional application of ALL in managing atherosclerotic diseases.

Immune regulation and inflammation inhibition of Arctium lappa L. polysaccharides by TLR4/NF-κB signaling pathway in cells.

Arctium lappa L. polysaccharides (ALP) are important active ingredients of burdocks with various bioactivities. In the present study, a crude polysaccharide was extracted from A. lappa L. roots and purified using DEAE-52 and Sephacryl™ S-400 columns to reach 99 % purity. This neutral polysaccharide contained fructose, glucose, galactose and arabinose in a ratio of 0.675:0.265:0.023:0.016 and had a Mw of 4256 Da. The immunomodulatory activity and intestinal inflammation inhibitory effects of ALP were investigated in in vitro models, including lipopolysaccharide-induced macrophage RAW264.7 and interleukin (IL)-1ß-induced colon Caco-2 cells. The results revealed that ALP possessed both antioxidant and anti-inflammatory effects by decreasing nuclear factor-E2-related factor 2 mRNA expression and reactive oxygen species. Furthermore, ALP was found to have inhibitory effects on pro-inflammatory cytokines, including IL-8, IL-6, IL-1ß, and tumor necrosis factor-α, as well as inflammatory cytokines, such as intercellular adhesion molecule-1, vascular cell adhesion molecule-1, and monocyte chemoattractant protein-1 by down-regulating the Toll-like receptor 4 (TLR4)/NF-κB (nuclear factor-kappa B signaling) pathway. It indicated that A. lappa L. was an ideal source of bioactive polysaccharides having potential to be developed as functional foods or nutraceuticals to improve immune system and prevent/treat intestinal inflammation.

Chlorogenic Acid from Burdock Roots Ameliorates Oleic Acid-Induced Steatosis in HepG2 Cells through AMPK/ACC/CPT-1 Pathway.

Hepatic steatosis can cause liver dysfunction and cell injury, on which natural functional factors are expected to be an effective approach for long-term intervention. However, the cellular molecular mechanisms are unclear. Chlorogenic acid is a phenolic compound, which can regulate lipid metabolism and is abundant in burdock root. The aim of this study was to investigate the potential molecular mechanism of the effect of chlorogenic acid from burdock root (ACQA) on steatosis in HepG2 cells. In this study, we found that ACQA reduced the number of lipid droplets and lipid levels in oleic acid-treated HepG2 cells. Molecular mechanistic results showed that ACQA enhanced CPT-1 expression by activating AMPK-related signaling pathways, and the concentrations of Ca2+ and cAMP were increased with the intervention of ACQA. In addition, ACQA enhanced the ß-oxidation of fatty acids, reduced alanine transaminase and aspartate transaminase, and inhibited apoptosis in oleic acid-treated HepG2 cells. Our studies elucidate a novel mechanism that ACQA enhances the ß-oxidation of fatty acids through the AMPK/ACC/CPT-1 pathway to protect against steatosis in HepG2 cells, which provides insight into its molecular mechanism as well as intervention strategies for chlorogenic acid against fatty liver diseases.

Effect of arctigenin on neurological diseases: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Arctium lappa L. is a common specie of Asteraceae. Its main active ingredient, Arctigenin (AG), in mature seeds exerts pharmacological effects on the Central Nervous System (CNS). AIM OF THE STUDY: To review studies on the specific effects of the AG mechanism on various CNS diseases and elucidate signal transduction mechanisms and their pharmacological actions. MATERIALS AND METHODS: This investigation reviewed the essential role of AG in treating neurological disorders. Basic information on Arctium lappa L. was retrieved from the Pharmacopoeia of the People's Republic of China. The related articles from 1981 to 2022 on the network database (including CNKI, PubMed, and Wan Fang and so on) were reviewed using AG and CNS diseases-related terms such as Arctigenin and Epilepsy. RESULTS: It was confirmed that AG has a therapeutic effect on Alzheimer's disease, Glioma, infectious CNS diseases (such as Toxoplasma and Japanese Encephalitis Virus), Parkinson's disease, Epilepsy, etc. In these diseases, related experiments such as a Western blot analysis revealed that AG could alter the content of some key factors (such as the reduction of Aß in Alzheimer's disease). However, in-vivo AG's metabolic process and possible metabolites are still undetermined. CONCLUSION: Based on this review, the existing pharmacological research has indeed made objective progress to elucidate how AG prevents and treats CNS diseases, especially senile degenerative disease such as Alzheimer's diseases. It was revealed that AG could be used as a potential nervous system drug as it has a wide range of effects in theory with markedly high application value, especially in the elder group. However, the existing studies are limited to in-vitro experiments; therefore, little is known about how AG metabolizes and functions in-vivo, limiting its clinical application and requiring further research.

Genomic characterization of a novel torradovirus infecting Arctium lappa L. in China.

Burdock (Arctium lappa L.) is not only a popular vegetable crop but also an important medicinal plant. In burdock plants with symptoms of leaf mosaic, a novel torradovirus tentatively named "burdock mosaic virus" (BdMV) was identified by high-throughput sequencing. The complete genomic sequence of BdMV was further determined using RT-PCR and the rapid amplification of cDNA ends (RACE) method. The genome is composed of two positive-sense single-stranded RNAs. RNA1 (6991 nt) encodes a polyprotein of 2186 aa, and RNA2 (4700 nt) encodes a protein of 201 aa and a polyprotein of 1212 aa that is predicted to be processed into one movement protein (MP) and three coat proteins (CPs). The Pro-Pol region of RNA1 and the CP region of RNA2 shared the highest amino acid sequence identity of 74.0% and 70.6%, respectively, with the corresponding sequences of lettuce necrotic leaf curl virus (LNLCV) isolate JG3. Phylogenetic analysis based on the amino acid sequences of the Pro-Pol and CP regions showed that BdMV clustered with other non-tomato-infecting torradoviruses. Taken together, these results suggest that BdMV is a new member of the genus Torradovirus.

A systematic review on botany, ethnopharmacology, quality control, phytochemistry, pharmacology and toxicity of Arctium lappa L. fruit.

ETHNOPHARMACOLOGICAL RELEVANCE: Arctium lappa L., is a biennial plant that grows around the Eurasia. Many parts of Arctium lappa L. (roots, leaves and fruits, etc.) are medically used in different countries. Arctium lappa L. fruit, also called Arctii Fructus, is traditionally applied to dispel wind-heat, ventilate lung to promote eruption, remove toxicity substance and relieve sore throat. THE AIM OF THE REVIEW: The review aims to integrate the botany, ethnopharmacology, quality control, phytochemistry, pharmacology, derivatives and toxicity information of Arctii Fructus, so as to facilitate future research and explore the potential of Arctii Fructus as an agent for treating diseases. MATERIALS AND METHODS: Related knowledge about Arctii Fructus were acquired from Science Direct, GeenMedical, PubMed, China National Knowledge Infrastructure (CNKI), Web of Science, Pharmacopoeia of the People's Republic of China, Doctoral and Master's thesis, ancient books, etc. RESULTS: Arctii Fructus as an herb used for medicine and food was pervasively distributed and applicated around the world. It was traditionally used to treat anemopyretic cold, dyspnea and cough, sore throat, etc. To date, more than 200 compounds have been isolated and identified from Arctii Fructus. It contained lignans, phenolic acids and fatty acids, terpenoids, volatile oils and others. Lignans, especially arctigenin and arctiin, had the extensive pharmacological effects such as anti-cancer, antiviral, anti-inflammatory activities. The ester derivatives of arctigenin had the anti-cancer, anti-Alzheimer's disease and immunity enhancing effects. Although Arctii Fructus extract had no toxicity, arctigenin was toxic at a certain dose. The alleviating effects of Arctii Fructus on chronic inflammation and ageing have been demonstrated by clinical studies. CONCLUSION: Arctii Fructus is regarded as a worthy herb with many chemical components and various pharmacological effects. Several traditional applications have been supported by modern pharmacological research. However, their action mechanisms need to be further studied. Although many chemical components were isolated from Arctii Fructus, the current research mainly focused on lignans, especially arctiin and arctigenin. Therefore, it is very important to deeply clarify the pharmacological activities and action mechanism of the compounds and make full medicinal use of the resources of Arctii Fructus.

Arctium lappa (Burdock): Insights from ethnopharmacology potential, chemical constituents, clinical studies, pharmacological utility and nanomedicine.

Arctium lappa L. is a medicinal edible homologous plant, commonly known as burdock or bardana, which belongs to the Asteraceae family. It is widely distributed throughout Northern Asia, Europe, and North America and has been utilized for hundreds of years. The roots, fruits, seeds, and leaves of A. lappa have been extensively used in traditional Chinese Medicine (TCM). A. lappa has attracted a great deal of attention due to its possession of highly recognized bioactive metabolites with significant therapeutic potential. Numerous pharmacological effects have been demonstrated in vitro and in vivo by A. lappa and its bioactive metabolites, including antimicrobial, anti-obesity, antioxidant, anticancer, anti-inflammatory, anti-diabetic, anti-allergic, antiviral, gastroprotective, hepatoprotective, and neuroprotective activities. Additionally, A. lappa has demonstrated considerable clinical efficacies and valuable applications in nanomedicine. Collectively, this review covers the properties of A. lappa and its bioactive metabolites, ethnopharmacology aspects, pharmacological effects, clinical trials, and applications in the field of nanomedicine. Hence, a significant attention should be paid to clinical trials and industrial applications of this plant with particular emphasis, on drug discovery and nanotechnology.

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.

Arctigenin: pharmacology, total synthesis, and progress in structure modification.

Arctium lappa L. is a prevalent medicinal herb and a health supplement that is commonly used in Asia. Over the last few decades, the bioactive component arctigenin has attracted the attention of researchers because of its anti-inflammatory, antioxidant, immunomodulatory, multiple sclerosis fighting, antitumor, and anti-leukemia properties. After summarising the research and literature on arctigenin, this study outlines the current status of research on pharmacological activity, total synthesis, and structural modification of arctigenin. The purpose of this study is to assist academics in obtaining a more comprehensive understanding of the research progress on arctigenin and to provide constructive suggestions for further investigation of this useful molecule.

The genomes of chicory, endive, great burdock and yacon provide insights into Asteraceae palaeo-polyploidization history and plant inulin production.

Inulin is an important reserve polysaccharide in Asteraceae plants, and is also widely used as a sweetener, a source of dietary fibre and prebiotic. Nevertheless, a lack of genomic resources for inulin-producing plants has hindered extensive studies on inulin metabolism and regulation. Here, we present chromosome-level reference genomes for four inulin-producing plants: chicory (Cichorium intybus), endive (Cichorium endivia), great burdock (Arctium lappa) and yacon (Smallanthus sonchifolius), with assembled genome sizes of 1.28, 0.89, 1.73 and 2.72 Gb, respectively. We found that the chicory, endive and great burdock genomes were shaped by whole genome triplication (WGT-1), and the yacon genome was shaped by WGT-1 and two subsequent whole genome duplications (WGD-2 and WGD-3). A yacon unique whole genome duplication (WGD-3) occurred 5.6-5.8 million years ago. Our results also showed the genome size difference between chicory and endive is largely due to LTR retrotransposons, and rejected a previous hypothesis that chicory is an ancestor of endive. Furthermore, we identified fructan-active-enzyme and transcription-factor genes, and found there is one copy in chicory, endive and great burdock but two copies in yacon for most of these genes, except for the 1-FEH II gene which is significantly expanded in chicory. Interestingly, inulin synthesis genes 1-SST and 1-FFT are located close to each other, as are the degradation genes 1-FEH I and 1-FEH II. Finally, we predicted protein structures for 1-FFT genes to explore the mechanism determining inulin chain length.

A synergistic strategy to remove hazardous water pollutants by mimicking burdock flower morphology structures of iron oxide phases.

Artificially mimicking structures/morphologies available in the nature to develop multifunctional materials for catalysis is receiving greater attention. Particularly, the burdock flower morphology, which has a hollow-globe surrounded by spiky sheets, represents a multifunctional structure helpful in adsorption as well as intercalation of molecules. Given this, we have strategically developed a robust microwave (MW) bubble-template process to achieve highly uniform α-Fe2O3 and carbon-enriched Fe3O4 (Fe3O4@C) phases resembling the characteristics of spiky hollow burdock morphologies. The utilization of the MW bubble-templates as a pretreatment to the iron-based precursor solution helps in producing hollowed open-space ferrous glycolate burdock flower morphology with rapid production rate and without any addition of extra agents. Such burdock flower structures remain intact even after annealing in air/N2 ambiance providing highly photoactive α-Fe2O3 or magnetic Fe3O4@C, respectively. Utilizing the hollow burdock flower structures together with the individual photo/magnetic properties of iron oxide phases, a dual-layer filter was designed to remove hazardous dye molecules from water, which efficiently photodegraded (99.2 %) in natural sunlight as well as showed excellent adsorption (99.7 %) within minutes. Comparatively, a lower catalytic activity using simple iron oxide nanoparticles, closed, and faded burdock morphologies were seen. Hence, the high catalytic activity in removing the dye molecules, retention of structural phases after repeated use, and strong durability were a result of the synergetic effect of photo/magnetic properties, activated surface/spiky open burdock structure.

Polyphenols from Arctium lappa L ameliorate doxorubicin-induced heart failure and improve gut microbiota composition in mice.

In this study, the ameliorative effect of purified polyphenols from Arctium lappa L (ALPP) on doxorubicin (DOX)-induce heart failure was investigated. Results indicated that ALPP pretreatment significantly reduced the activities of casein kinase and lactate dehydrogenase, lowered the levels of inflammatory indexes (TNF-α and NO), and alleviated antioxidant stress in DOX-induce mice, thus leading to a reduced heart failure syndrome. In addition, according to 16s high-throughput sequencing, the increased abundance of Lactobacillaceae,Muribaculaceae, and Ruminococcaceae and the decreased abundance of Proteobacteria,Enterobacteriaee, and Escherichia_Shigella were observed in ALPP treatment group. ALPP could significantly enhance the abundance of bacteria producing short chain fatty acids (SCFAs) and then promote the increase of SCFAs. Consequently, ALPP might be a therapeutic alternative in the treatment of DOX-induced heart failure. PRACTICAL APPLICATIONS: The effect of Arctium lappa L (ALPP) on doxorubicin (DOX)-induced heart failure was investigated. It provided experimental basis for further studies on the biological activity of polyphenols from ALPP. The results demonstrated that ALPP could significantly ameliorate DOX-induced heart failure and improve the gut microbiota composition. The obtained results could provide the potential application of ALPP as an alternative therapy for heart failure in the functional food industry.

Fructus arctii: an overview on its traditional uses, pharmacology and phytochemistry.

OBJECTIVES: Fructus arctii (F. arctii) is the dried ripe fruit of Arctium lappa Willd (Asteraceae). It is being used as a traditional medicine in China, Japan, Iran, Europe, Afghanistan, India, etc. for cough, inflammation, clearing the heat, detoxification, cancer and diabetes. This review summarized the botanical description, distribution, ethnopharmacology, bioactive constituents and pharmacological actions of F. arctii including methods to assess its quality. In addition, this review also provides insights into future research directions on F. arctii to further explore its bioactive constituents, mechanism involved in pharmacological activity, and clinical use including the development of new analytical methods for assessing the quality. KEY FINDINGS: The comprehensive analysis of the literature revealed that F. arctii contains lignans, volatile oil, flavonoids, sesquiterpenoids, triterpenes, phenolic acids, etc. Experimental studies on various extracts and drug formulations showed that it has antioxidant, antimicrobial, hypoglycaemic, lipid-lowering, anti-inflammatory, analgesic, antiviral, anti-tumour activity, etc. SUMMARY: The pharmacological activity of a few major constituents in F. arctii have been identified. However, there are still need more studies and more new technologies to prove the pharmacological activity and the effective mechanism of the other constituents that undergoing uncertain. Except for the animal experiments, clinical studies should be carried out to provide the evidence for clinical application.

Antiallergic activities of Japanese leaf burdock extract in a rat basophilic leukemia cell line.

Although primarily cultivated for its edible root, the leaves and stems of "Japanese leaf burdock (Arctium lappa L)" are also edible. This study determined the antiallergic activity of root, leaf, and stem extracts of Japanese leaf burdock using the rat basophilic leukemia cell line. We demonstrate that the hot water extract of Japanese leaf burdock stems has a strong inhibitory effect on antigen-stimulated degranulation. This extract was further fractionated into five fractions using a glass column. The fraction obtained with 99% ethanol extracts (99% EtEx) elicits a concentration-dependent increase in degranulation inhibition. One of antiallergic compounds from the separation of components of the 99% EtEx fraction using high-performance liquid chromatography and mass spectrometry analyses had a value of m/z 393.16. From these results and those of previous studies, one of the antiallergic components was hypothesized to be onopordopicrin. Our findings demonstrate that the extract of Japanese leaf burdock exerts a strong antiallergic activity. PRACTICAL APPLICATIONS: "Japanese leaf burdock (Arctium lappa L)" is a traditional Japanese vegetable with edible leaves and stems. The antiallergic activity of the hot water extracts has been shown in vitro. One of the antiallergic components was hypothesized to be onopordopicrin. Therefore, "Japanese leaf burdock" could serve as a functional food for patients with allergic disorders, such as allergic rhinitis.

Discovery of quality control ingredients in burdock root by combining anti-tumor effects and UHPLC-QqQ-MS/MS.

Burdock root is the root of Arctium lappa L., a plant of the Compositae family, which has the effects of dispersing wind and heat, detoxifying and reducing swelling. In order to better control the quality of burdock root, a screening study of quality control indicators was carried out. The current research combines biological activity evaluation with chemical analysis to screen and identify the biologically active compounds of burdock root as chemical components for the quality control of herbal medicine. The efficacy of 10 batches of ethanol extracts of burdock roots was evaluated by a tumor inhibition experiment in S180 tumor-bearing mice. The five main chemical components of these extracts were simultaneously quantitatively measured by ultra-high performance liquid chromatography combined with triple quadrupole mass spectrometry. Pearson correlation analysis was used to establish the relationship between these extracts' biological activity and chemical properties. The results showed that chlorogenic acid, caffeic acid and cynarin were positively correlated with the effect of inhibiting tumor growth, and further bioassays confirmed this conclusion. In conclusion, chlorogenic acid, caffeic acid and cynarin can be used as quality control markers for burdock root's antitumor effect.

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.