Arctigenin is a bioactive dibenzylbutyrolactone-type lignan exhibiting various pharmacological activities. The neuroprotective effects of arctigenin were demonstrated to be mediated via inhibition of AMPA and KA type glutamate receptors in the somatosensory cortex of the rat brain. The aim of this study was to compare the effects of arctigenin with matairesinol and trachelogenin on synaptic activity in ex vivo rat brain slices. Arctigenin, matairesinol and trachelogenin were isolated from Arctium lappa, Centaurea scabiosa and Cirsium arvense, respectively, and applied on brain slices via perfusion medium at the concentration range of 0.5-40 µM. The effects of the lignans were examined in the CA1 hippocampus and the somatosensory cortex by recording electrically evoked field potentials. Arctigenin and trachelogenin caused a significant dose-dependent decrease in the amplitude of hippocampal population spikes (POPS) and the slope of excitatory postsynaptic potentials (EPSPs), whereas matairesinol (1 µM and 10 µM) decreased EPSP slope but had no effect on POPS amplitude. Trachelogenin effect (0.5 µM, 10 µM, 20 µM) was comparable to arctigenin (1 µM, 20 µM, 40 µM) (p ˃ 0.05). In the neocortex, arctigenin (10 µM, 20 µM) and trachelogenin (10 µM) significantly decreased the amplitude of evoked potential early component, while matairesinol (1 µM and 10 µM) had no significant effect (p>0.05). The results suggest that trachelogenin and arctigenin act via inhibition of AMPA and KA receptors in the brain and trachelogenin has a higher potency than arctigenin. Thus, trachelogenin and arctigenin could serve as lead compounds in the development of neuroprotective drugs.

This study is aimed at developing novel analytical methods to accurately visualize the spatial distribution of various endogenous components in Arctium lappa L. (A. lappa) roots, and to precisely guide the setting of pre-treatment operations during processing technologies and understand plant metabolism process. The matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) imaging technology was used for visual demonstration of the in situ spatial distribution in A. lappa roots. This work consisted of four steps: matrix selection, section preparation, matrix coating, and MALDI-TOF MS imaging analysis. Consequently, eight saccharides, four caffeoylquinic acids, four flavonoids, six amino acids, one choline, and one phospholipid were imaged and four unidentified components were found. Saccharides were distributed in the center, whereas caffeoylquinic acids and flavonoids were mainly present in the epidermis and cortex. Furthermore, amino acids were mainly detected in the phloem, and choline in the cambium, while phosphatidylserine was found in the secondary phloem and cambium. This study demonstrated that MALDI-TOF MS imaging technology could provide a technical support to understand the spatial distribution of components in A. lappa roots, which would promote the processing technologies for A. lappa roots and help us to understand the plant metabolism process.

Dibenzylbutyrolactone-type lignans are phenolic compounds of medical importance. The purpose of the study was to determine the effects of two such lignans, arctigenin and trachelogenin on the motility of isolated rat ileum and obtain indications on their mechanism of action. They were isolated from Arctium lappa and Cirsium arvense, respectively, which have been used traditionally to treat gastrointestinal disorders. 1-1.5 cm long segments of distal ileum were obtained from adult male Wistar rats. The intestinal segments were suspended vertically in a well-aerated organ-bath according to Magnus mounting method. The intestinal motility was monitored for 30 min before treatment to obtain the baseline, followed by treatment with 1 µM, 10 µM, 20 µM and 40 µM concentrations of arctigenin and 0.5 µM, 1 µM, 10 µM and 20 µM of trachelogenin concentrations. The amplitude, tone, and period of spontaneous contractions were measured after 15 and 30 min of treatment. To investigate their mechanism of action, cholinergic, glutamatergic, adrenergic antagonists and compounds inhibiting nitric oxide synthase and L-type calcium channels were also tested. Arctigenin and trachelogenin decreased the frequency of contractions in a dose-dependent manner. At the concentration of 20 µM and 40 µM of trachelogenin and arctigenin, respectively, there was a marked alteration in spontaneous contraction pattern with an observable increase in the period time. This activity was comparable to 0.5 µM nifedipine (L-type calcium channel blocker) treatment. Our results demonstrate relaxant effect of arctigenin and trachelogenin on the ileum motility that may be mediated by L-type calcium ion channel blockade.

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.

Arctigenin (AR), extracted from Arctium lappa L. (Burdock), is a folk herbal medicine used to treat diabetes. However, its mechanism of action has remained elusive. In this study, type 2 diabetes mellitus (T2DM) mice received AR orally for 10 weeks to evaluate its therapeutic effect based on changes in glucose and lipid metabolism, histological examination of target tissues, and liver immunohistochemistry. Furthermore, HepG2 insulin-resistant cells were established to verify the mechanism of AR against diabetes. The results showed that AR treatment reduced blood glucose and lipid levels, reversing liver as well as pancreas tissue damage in T2DM mice. AR reduced the levels of pro-inflammatory cytokines in the serum of T2DM mice, as well as those in insulin-resistant HepG2 cell supernatants, while increasing interleukin-10 (IL-10) levels. The levels of p-p65, phospho-c-Jun N-terminal kinase (p-JNK), induced nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) were reduced in the liver tissue of T2DM mice, accompanied by an upregulation of glucose transporter 4 (GLUT4) and insulin receptor substrate 2 (IRS-2). In vitro studies further showed that AR downregulated toll-like receptor 4-mediated inflammation, while upregulating insulin pathway-related proteins and ultimately improving glucose uptake in insulin-resistant HepG2 cells. In conclusion, AR protected mice from insulin resistance, and its therapeutic effect was likely associated with inhibition of toll-like receptor 4 inflammatory signaling to reactivate IRS-2/GLUT4.

Turnip yellows virus (TuYV) is one of the most important pathogens of oilseed rape worldwide. The virus has a large host range including many crop species (e.g., oilseed rape, pea, chickpea) and weeds from more than twenty plant families. Other than oilseed rape, we detected TuYV in many commonly grown weed species that share the fields and vegetation period together with canola crops in Czech and Slovak Republics. TuYV was detected by reverse-transcription polymerase chain reaction (RT-PCR) in at least 26 species including main crop hosts (oilseed rape), intercrops and weeds such as Amaranthus retroflexus, Atriplex patula (Amaranthaceae), Arctium lappa, Lactuca serriola, Taraxacum officinale, Tripleurospermum inodorum (Asteraceae), Phacelia tanacetifolia (Boraginaceae), Brassica napus, Capsella bursa-pastoris, Descurainia Sophia, Raphanus raphanistrum, Sinapis alba, Sisymbrium officinale, Thlaspi arvense (Brassicaceae), Silene alba, Stellaria media (Caryophyllaceae), Euphorbia helioscopia (Euphorbiaceae), Geranium rotundifolium (Geraniaceae), Lamium purpureum (Lamiaceae), Fumaria officinalis, Papaver rhoeas (Papaveraceae), Veronica persica (Plantaginaceae syn. Scrophulariaceae), Fallopia convolvulus (Polygonaceae), Solanum nigrum (Solanaceae), Urtica dioica (Urticaceae) and Viola arvensis (Violaceae). The detection of TuYV was further confirmed by RT-qPCR as well as Sanger sequencing of the PCR fragments. We discovered four new weed species as hosts of TuYV such as T. inodorum, S. alba, G. rotundifolium and E. helioscopia, representing their three respective plant families. The readthrough domain (RTD) gene sequence analysis of the Czech and Slovak TuYV isolates from oilseed rape and weed species showed similar within-group nucleotide divergence (7.1% and 5.6%, respectively) and the absence of geographical- or host-based phylogenetic clustering. The high-throughput sequencing of the P. rhoeas sample enabled the obtention of a nearly complete genome of TuYV and revealed the mixed infection of TuYV with turnip mosaic virus and cucumber mosaic virus. Our results thus show that weed species are an important TuYV reservoir and play a significant role in the spread and incidence of the disease in field crops such as oilseed rape.

Rice bacterial leaf blight caused by Xanthomonas oryzae pv. oryzae (Xoo) is responsible for a significant reduction in rice production. Due to the small impact on the environment, biogenic nanomaterials are regarded as a new type of antibacterial agent. In this research, three colloids of silver nanoparticles (AgNPs) were synthesized with different biological materials such as Arctium lappa fruit, Solanum melongena leaves, and Taraxacum mongolicum leaves, and called Al-AgNPs, Sm-AgNPs and Tm-AgNPs, respectively. The appearance of brown colloids and the UV-Visible spectroscopy analysis proved the successful synthesis of the three colloids of AgNPs. Moreover, FTIR and XRD analysis revealed the formation of AgNPs structure. The SEM and TEM analysis indicated that the average diameters of the three synthesized spherical AgNPs were 20.18 nm, 21.00 nm, and 40.08 nm, respectively. The three botanical AgNPs had the strongest bacteriostatic against Xoo strain C2 at 20 μg/mL with the inhibition zone of 16.5 mm, 14.5 mm, and 12.4 mm, while bacterial numbers in a liquid broth (measured by OD600) decreased by 72.10%, 68.19%, and 65.60%, respectively. Results showed that the three AgNPs could inhibit biofilm formation and swarming motility of Xoo. The ultrastructural observation showed that Al-AgNPs adhered to the surface of bacteria and broke the bacteria. Overall, the three synthetic AgNPs could be used to inhibit the pathogen Xoo of rice bacterial leaf blight.

Arctium minus (Hill) Bernh. (Asteraceae), which has a wide distribution area in Turkey, is a medicinally important plant. Eighty percent methanol extracts of the leaf, flower head, and root parts of A. minus were prepared and their sub-fractions were obtained. Spectrophotometric and chromatographic (high-performance liquid chromatography) techniques were used to assess the phytochemical composition. The extracts were evaluated for antioxidant activity by diphenyl-2-picrylhydrazil radical (DPPH●), 2,2'-Azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS●+) radical scavenging, and β-carotene linoleic acid bleaching assays. Furthermore, the extracts were subjected to α-amylase, α-glucosidase, lipoxygenase, and tyrosinase enzyme inhibition tests. The cytotoxic effects of extracts were investigated on MCF-7 and MDA-MB-231 breast cancer cell lines. The richest extract in terms of phenolic compounds was identified as the ethyl acetate sub-fraction of the root extract (364.37 ± 7.18 mgGAE/gextact). Furthermore, chlorogenic acid (8.855 ± 0.175%) and rutin (8.359 ± 0.125%) were identified as the primary components in the leaves' ethyl acetate sub-fraction. According to all methods, it was observed that the extracts with the highest antioxidant activity were the flower and leaf ethyl acetate fractions. Additionally, ABTS radical scavenging activity of roots' ethyl acetate sub-fraction (2.51 ± 0.09 mmol/L Trolox) was observed to be as effective as that of flower and leaf ethyl acetate fractions at 0.5 mg/mL. In the β-carotene linoleic acid bleaching assay, leaves' methanol extract showed the highest antioxidant capacity (1422.47 ± 76.85) at 30 min. The enzyme activity data showed that α-glucosidase enzyme inhibition of leaf dichloromethane extract was moderately high, with an 87.12 ± 8.06% inhibition value. Lipoxygenase enzyme inhibition was weakly detected in all sub-fractions. Leaf methanol extract, leaf butanol, and root ethyl acetate sub-fractions showed 99% tyrosinase enzyme inhibition. Finally, it was discovered that dichloromethane extracts of leaves, roots, and flowers had high cytotoxic effects on the MDA-MB-231 cell line, with IC50 values of 21.39 ± 2.43, 13.41 ± 2.37, and 10.80 ± 1.26 µg/mL, respectively. The evaluation of the plant extracts in terms of several bioactivity tests revealed extremely positive outcomes. The data of this study, in which all parts of the plant were investigated in detail for the first time, offer promising results for future research.

Arctium lappa L. is one of the medicinal and food homologous plants in China, which is rich in nutrients and medicinal ingredients. The use of plant growth-promoting (PGP) endophytic bacteria is an alternative to reducing chemical fertilizers in agricultural production. The aim of this study was to analyze the diversity of endophytic bacteria in different cultivars of A. lappa L. collected from two geographical locations in China and evaluate PGP traits of the isolates and their potential PGP ability in greenhouse condition. Endophytic bacterial community was investigated by culture-dependent and culture-independent methods. Isolates were screened and investigated for multiple PGP traits, and representative strains were inoculated host seedlings to evaluate the growth promoting effect. A total of 348 endophytic bacteria were obtained and they were distributed into 4 phyla and 30 genera. In addition, high throughput sequencing revealed more abundant bacterial community, including 17 bacterial phyla and 207 genera. A high proportion of PGP traits were detected, including production of indole acetic acid, siderophore, ammonia and phosphate solubilization. Four representative strains with multiple PGP traits of the most dominant genera (Bacillus, Pantoea, Microbacterium and Pseudomonas) were further selected for host inoculation and growth promoting evaluation, and they significantly increase seedlings length, root length and fresh weight. This study demonstrated that A. lappa L. harbors abundant endophytic bacteria, and some endophytic bacteria showed good potential for the development of microbial fertilizer in the future.

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.

Burdock (Arctium lappa L) root is eaten as a vegetable in many countries and used as an ethnomedicine because of its various pharmacological effects. The objective of this study was to investigate the underlying mechanisms of ethanolic extract of root from Arctium lappa L root (ALE) to lose weight and regulate lipid metabolism. The results showed that ALE can regulate lipid metabolism level and inhibit the weight gain of rats induced by the high-sugar and high-fat diet. The contents of triglyceride and cholesterol in the liver of obese rats significantly reduced, and hepatic steatosis was ameliorated. In addition, this study identified that ALE enhanced hepatic fatty acid β-oxidation and ameliorated hepatic steatosis by activating AMPK/ACC/CPT-1 pathway. These results indicated that ALE has a potential preventive and therapeutic effect on metabolic-associated fatty liver disease and obesity. PRACTICAL APPLICATIONS: Obesity is already a global health problem. Obesity causes accumulation of triglycerides, which leads to hepatic steatosis. Long-term steatosis causes liver damage and metabolic fatty liver disease. Plant-derived functional foods or herbal medicines have better effects on weight loss and liver protection, which are more conducive to long-term use with less toxic side effects. As a medicinal and edible plant material, Arctium lappa L root has the effect in losing weight. Our study showed that ethanolic extract of Arctium lappa L root effectively regulates lipid metabolism and inhibits hepatic steatosis. Arctium lappa L root may be used as a therapeutic drug and functional food raw material for obesity and fatty liver disease.

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.

Arctium lappa (A. lappa) leaves are widely used in various traditional Chinese herbal formulae to ameliorate atherosclerosis (AS) and its complications such as stroke; however, there is no literature reporting the anti-atherosclerotic effect and mechanism of A. lappa leaves thus far. In the present study, we used network pharmacology and molecular docking approaches to examine the protective effect and potential mechanism of A. lappa leaves against AS in vivo and in vitro. From the network pharmacology, PPARG, HMGCR and SREBF2 were identified as the core targets of A. lappa leaves against AS. Further enrichment analyses of GO and KEGG pathways suggested that A. lappa leaves might play an anti-AS role by regulating metabolic processes and PPAR signalling pathways. The results of molecular docking experiment revealed that the major components of A. lappa leaves interacted with cholesterol efflux-regulating core proteins (PPARG, LXRα, ABCA1, and ABCG1), AMPK and SIRT1. Both in vivo and in vitro experimental results demonstrated that treatment with A. lappa leaves significantly lowered TC and LDL-C, increased HDL-C, and reduced cholesterol accumulation in the liver and aorta of the AS rat model and the foam cell model. Importantly, both in vivo and in vitro experimental results demonstrated that A. lappa leaves regulate the activity of the PPARG/LXRα signalling and AMPK/SIRT1 signalling pathways. Moreover, after treatment with the AMPK inhibitor Compound C in vitro, the improvement induced by A. lappa leaves was significantly reversed. In conclusion, A. lappa leaves attenuated AS-induced cholesterol accumulation by targeting the AMPK-mediated PPARG/LXRα pathway and promoting cholesterol efflux.

Phenolic acids are now receiving a great deal of interest as pervasive human dietary constituents that have various therapeutic applications against chronic and age-related diseases. One such phenolic acid that is being utilized in traditional medicine is chlorogenic acid (CGA). It is one of the most readily available phytochemicals that can be isolated from the leaves and fruits of plants such as coffee beans (CoffeaarabicaL.), apples (Malus spp.), artichoke (Cynara cardunculus L.), carrots (Daucus carota L.), betel (Piper betle L.), burdock (Arctium spp.) and so on. Despite its low oral bioavailability (about 33%), CGA has drawn considerable attention due to its wide range of biological activities and numerous molecular targets.Several studies have reported that the antioxidant and antiinflammatory potential of CGA mainly account for its broad-spectrum pharmacological attributes. CGA has been implicated in exerting beneficial role against dysbiosis by encouraging the growth of beneficial GUT microbes. At biochemical level its therapeutic action is mediated by free radical scavenging efficacy, modulation of glucose and lipid metabolism, down-regulation of proinflammatory cytokines such as tumor necrosis factor alpha (TNF-α),interleukin-6 (IL-6), IL-1β, and interferon gamma (IFN-γ), upregulation of nuclear factor erythroid 2-related factor 2 (Nrf-2) and inhibition ofthe activity of nuclear factor- κβ (NF-κβ) and thus help inmanagement of diabetes, cardiovascular diseases, neurodegenerative disorder, cancer, hypertension etc. This review highlights the natural sources of CGA, its bioavailability, metabolism, pharmacotherapeutic potential and underlying mechanisms of action for clinical usefulness of CGA in the management of health disorders.

In this study, the anti-inflammatory and antioxidant activities and mechanism of burdock leaf flavonoids (BLF) on LPS-stimulated inflammation in RAW264.7 macrophage cells were explored. We have observed that BLF and main effective components morin and quercetin 3-O-rhamnoside pretreatment significantly inhibited LPS-stimulated inflammatory activation of RAW264.7 cells by lowering the levels of NO, PGE2, TNF-α, and IL-6 production (p < .05). At the same time, BLF not only had potent free radical scavenging ability in vitro (DPPH: 2025.33 ± 84.15 μmol Trolox/g, ABTS: 159.14 ± 5.28 μmol Trolox/g, and ORAC: 248.72 ± 9.74 μmol Trolox/g) but also effectively ameliorated cellular oxidative stress status by restoring the decreased activity of antioxidant enzymes (SOD, CAT, and GSH-Px) and decreasing the elevated levels of ROS and TBARS in LPS-stimulated macrophages (p < .05). The western blot analysis indicated that BLF and main components morin and quercetin 3-O-rhamnoside mainly inhibited LPS-stimulated inflammation by reducing the iNOS and COX-2 protein expression, decreasing cellular ROS, and blocking the activation of NF-κB signaling pathway in macrophages. Our results collectively imply that BLF could be used as a new type of functional factor for the development of antioxidant and anti-inflammatory foods.

The ultrasound-assisted aqueous extraction of chlorogenic acid (CGA) and cynarin with the impact of inulin from burdock (Arctium lappa L.) roots was investigated. Three extraction modes, ultrasound at 40 kHz/300 W (U-40), ultrasound at 120 kHz/300 W (U-120), and shaking at 120 rpm (S-120), were compared. The effects of process parameters on the extraction of polyphenols, CGA, cynarin, inulin, and antioxidant activity using U-40 were evaluated. In 10 min, 50 °C, and 1/30 (g/mL-water) of solid-to-liquid ratio, the order of CGA content in the dried burdock root powder (DBR) was U-40 (484.65 μg/g-DBR) > U-120 (369.93 μg/g-DBR) > S-120 (176.99 μg/g-DBR), while the order of cynarin content in DBR was U-120 (376.47 μg/g-DBR) > U-40 (341.54 μg/g-DBR) > S-120 (330.44 μg/g-DBR), showing the selective extraction of CGA and cynarin between using 40 and 120 kHz of ultrasound. The profiles of increase and then decrease in free CGA and cynarin concentrations against time revealed their degradation, including their interactions with the abundant inulin. The kinetic model, considering extraction followed by degradation, was proposed to describe the variations of free CGA and cynarin against time. This study provides an effective method using water to extract CGA, cynarin, and inulin from burdock roots.

Diabetes mellitus (DM) type 2 is amongst the most common chronic diseases, being responsible for various problems in humans and contributing to increased mortality rates worldwide. Fructooligosaccharide, which can be produced from the roots of burdock (Arctium lappa L.), has been shown to have a wide range of pharmacological proprieties, including antiviral, anti-inflammatory, hypolipidemic, and antidiabetic effects. Moreover, burdock also contains chlorogenic acid, which has been used in traditional medicine as an antioxidant. Considering its natural origin and minimal toxicity, burdock fructooligosaccharides (BFO) has gained considerable attention from researchers owing its wide, efficient, and beneficial action against DM. Although the effectiveness of fructooligosaccharide and chlorogenic acid has been extensively discussed, limited information is available on the application of burdock for DM treatment. In this review, we discuss the beneficial contributions, and the recent in vitro and in vivo analytical findings on A. lappa extract as DM therapy.

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.

Nine new cadinane-type sesquiterpenoids (1-9) and three new eucalyptane -type sesquiterpenes (10-12) were isolated from the ethyl acetate extract of Burdock leaves, which were commonly used for preventing or treating atherosclerosis in China. Their structures were confirmed by extensive spectroscopic analysis, single-crystal X-ray diffraction analysis and ECD calculations. Compound 1 possessed the rare large conjugated skeleton. All the isolates were evaluated for anti-inflammatory and cholesterol-lowering activities by the LPS- and oxidized-low-density-lipoprotein-stimulated RAW 264.7 cells, respectively. As the results, all isolates could decrease the productions of NO, and down-regulate the accumulation of cholesterol. Among them, 4 showed the most potent cholesterol-lowering effect. For the high content of 4 in the herb, mechanistic study of 4 was performed and the results showed that 4 markedly reduced the release of pro-inflammatory mediators which was probably associated with inhibition of the PI3K/Akt and 5-LOX signaling pathways. The findings of this study demonstrated the anti-inflammatory/cholesterol-lowering effects of the new sesquiterpenes from burdock leaves, which provides chemical basis and scientific evidence for the herb used as anti-atherosclerosis agents for the further study. The sesquiterpene lactones of burdock leaves are expected to become new small molecule inhibitors for the treatment of AS.

Arctigenin (Arc) is a phenylpropanoid dibenzylbutyrolactone lignan in Arctium lappa L, which has been widely applied as a traditional Chinese herbal medicine for treating inflammation. In the present study, we explored the neuroprotective effect and the potential mechanisms of arctigenin against LPS-evoked neuroinflammation, neurodegeneration, and memory impairments in the mice hippocampus. Daily administration of arctigenin (50 mg/kg per day, i.g.) for 28 days revealed noticeable improvements in spatial learning and memory deficits after exposure to LPS treatment. Arctigenin prevented LPS-induced neuronal/synaptic injury and inhibited the increases in Abeta (Aβ) generation and the levels of amyloid precursor protein (APP) and β-site amyloid precursor protein cleavage enzyme 1 (BACE1). Moreover, arctigenin treatment also suppressed glial activation and reduced the production of proinflammatory cytokines. In LPS-treated BV-2 microglial cells and mice, activation of the TLR4 mediated NF-κB signaling pathway was significantly suppressed by arctigenin administration. Mechanistically, arctigenin reduced the LPS-induced interaction of adiponectin receptor 1 (AdipoR1) with TLR4 and its coreceptor CD14 and inhibited the TLR4-mediated downstream inflammatory response. The outcomes of the current study indicate that arctigenin mitigates LPS-induced apoptotic neurodegeneration, amyloidogenesis and neuroinflammation as well as cognitive impairments, and suggest that arctigenin may be a potential therapeutic candidate for neuroinflammation/neurodegeneration-related diseases.

Dental caries and oral infections have become a widespread issue in the modern world. This study aimed to investigate the antibacterial, antifungal, and cytotoxicity characteristics of the extracts of Echinacea purpura, Arctium lappa, and the essential oil of Zataria multiflora as a potential herbal mouthwash. The essential oil of Z. multiflora leaves and the extracts of E. purpurea and A. lappa roots were prepared. The characterization was carried out by GC-MS and also, total phenol and flavonoid were assed for all three samples. The antimicrobial and anti-biofilm effects were evaluated against Streptococcus mutans, Streptococcus mitis, Streptococcus salivarius, Lactobacillus acidophilus, Escherichia coli, Staphylococcus aureus, and Candida albicans. The cytotoxic effect of the samples was evaluated on HEK 293 and HDFa cells by MTT test. Thymol and carvacrol contents in EO of Z. multiflora were measured at 31% and 42.2%, respectively. A. lappa had the lowest total phenolic and flavonoid value among the samples. On the other hand, the total phenolic content of Z. multiflora and the total flavonoid content of E. purpurea were the highest. The MIC values of Zataria, Arctium, and Echinacea against S. mutans were 0.011% v/v, 187.5 mg/ml, and 93.75 mg/ml, while MBC were 0.011% v/v, 375 mg/ml, and 187.5 mg/ml, respectively. The formulation showed bactericidal activity against S. mutans in the concentration of 5.86 mg/ml for Echinacea and Burdock extracts and 0.08 µl/ml for EO of Zataria. The formulation significantly affected microbial biofilm formation and induced biofilm degradation. The cell viability percentages were higher than 50% during 24 and 48 h. The formulation had a significant antimicrobial effect on cariogenic bacteria and C. albicans, with the lowest cytotoxic effects. Therefore, this formulation can be an appropriate candidate for mouthwash.

Intestinal mucus barrier dysfunction is closely involved in the pathogenesis of inflammatory bowel diseases (IBD). To investigate the protective effect and underlying mechanism of arctigenin, a phytoestrogen isolated from the fruits of Arctium lappa L., on the intestinal mucus barrier under colitis condition. The role of arctigenin on the intestinal mucus barrier and the apoptosis of goblet cells were examined by using both in vitro and in vivo assays. Arctigenin was demonstrated to promote the mucus secretion and maintain the integrity of mucus barrier, which might be achieved by an increase in the number of goblet cells via inhibiting apoptosis. Arctigenin selectively inhibited the mitochondrial pathway-mediated apoptosis. Moreover, arctigenin elevated the protein level of prohibitin 1 (PHB1) through blocking the ubiquitination via activation of estrogen receptor β (ERβ) to competitively interact with PHB1 and disrupt the binding of tripartite motif 21 (TRIM21) with PHB1. ERβ knock down in the colons of mice with DSS-induced colitis resulted in significant reduction of the protection of arctigenin and DPN against the mucosal barrier. Arctigenin can maintain the integrity of the mucus barrier by inhibiting the apoptosis of goblet cells through the ERβ/TRIM21/PHB1 pathway.

Several exotic plants (non-native) are used in Brazilian traditional medicine and are known worldwide for their possible diuretic actions. Among the wide variety of plants, standing out Achillea millefolium L., Camellia sinensis L. Kuntze, Crocus sativus L., Hibiscus sabdariffa Linn., Petroselinum crispum (Mill.) A.W. Hill, Taraxacum officinale (L.) Weber, and Urtica dioica L., whose effects have already been the subject of some scientific study. In addition, we also discussed other exotic species in Brazil used popularly, but that still lack scientific studies, like the species Arctium lappa L., Carica papaya L., Catharanthus roseus (L.) G. Don, Centella asiatica (L.) Urb, Citrus aurantium L., and Persea americana Mill. However, generally, clinical studies on these plants are scarce. In this context, different plant species can be designated for further comprehensive studies, therefore, promoting support for developing an effective medicine to induce diuresis.

Osteoporosis is a systemic disorder of bone metabolism. This study aimed to investigate the impacts and possible mechanisms of Arctiin, a lignin isolated from Arctium lappa on MC3T3-E1 osteoblast differentiation. In this study, after treatment with different concentrations of Arctiin, reverse transcription-quantitative polymerase chain reaction (RT-qPCR) and western blotting were used to estimate the expression of osteogenesis markers. Then, the activity of alkaline phosphatase (ALP) was detected by an ALP assay kit and calcium nodules staining was evaluated by alizarin red staining (ARS). Additionally, the regulatory effects of Arctiin on cyclin D1 (Ccnd1) was assessed by measurement of protein expression. Subsequently, the functions of Ccnd1 silencing on the osteogenic differentiation was examined in Arctiin-treated MC3T3-E1 cells. Results indicated that Arctiin dose-dependently upregulated the expression of runt-related transcription factor 2 (RUNX2), collagen type 1 (COL1A1), osteocalcin (OCN) and osteopontin (OPN). Elevated ALP activity and calcification degree was prominently observed in the Arctiin-treated groups. Moreover, Ccnd1 expression was notably enhanced after Arctiin intervention. Importantly, Ccnd1-knockdown abrogated the impacts of Arctiin on osteogenic differentiation of MC3T3-E1. To conclude, findings in this study suggested that Arctiin could regulate MC3T3-E1 osteoblast differentiation via up-regulating Ccnd1, supporting that Arctiin might be a therapeutic target for osteoporosis.

Arctium lappa L., also known as burdock, is a popular medicinal plant in traditional Chinese medicine due to its potential therapeutic properties. Saccharides from Arctium lappa L. root (ALR-S) have been extensively studied for their anti-inflammatory and anti-diabetes effects. Platelets play a pivotal role in thrombosis. The present study describes the effects of ALR-S on platelet activation and thrombosis using a laser injury thrombosis in vivo model. The study also measured the effects of ALR-S on platelet activation by analysing aggregation, ATP release, platelet spreading, adhesion and clot retraction in vitro. Specifically, the effects were ALR-S concentration-dependent inhibition of platelet aggregation and ATP release. Activated platelets pretreated with ALR-S showed diminished CD62P expression levels and fibrinogen binding, as measured by flow cytometry. ALR-S inhibited platelet spreading on fibrinogen and adhesion on collagen under shear. ALR-S attenuated platelet activation by decreasing oxidative stress and thrombus formation. These results demonstrated the antiplatelet effects of ALR-S, suggesting the antithrombotic and cardiovascular protective activities of ALR-S as a functional food.