Search Results (32)

Burdock (Arctium lappa L., Asteraceae) seeds, a rich source of dietary fibre, proteins, essential and fatty acids, also contain high levels of polyphenols and lignans, especially arctigenin and arctiin. This study investigated the incorporation of native and supercritical CO₂-defatted burdock seed flour into gingerbread cookies formulated with sweetener xylitol compared to burdock seeds’ free sugar-based and xylitol-based cookies as a control. Arctiin was the dominant lignan in both native and defatted seed flours (68.30 and 75.16 mg/g, respectively), while isochlorogenic acid was the most abundant phenolic acid (7.01 and 7.86 mg/g, respectively). Among enriched formulations, xylitol cookies with defatted burdock seed flour exhibited the highest soluble dietary fibre content (0.29 g/100 g) and reduced hardness, comparable to the xylitol control. All samples achieved “good” sensory quality (18.33–19.65 points), with no significant differences among formulations (p > 0.05). Storage studies (60 days) under varying temperature and light conditions revealed a significant decline in sensory quality only for sucrose-based control cookies stored at 40 °C. The concentrations of major phenolic compounds remained stable under all storage conditions. These results demonstrate the technological and nutritional potential of defatted burdock seed flour as a functional ingredient in bakery products. Full article

Diabetes mellitus is a chronic disease requiring multifunctional natural agents. Arctium lappa is traditionally used in Eastern and European medicine to address metabolic disorders. This comprehensive narrative review, conducted between 2000 and 2025 using international databases (Scopus, PubMed, Web of Science Core Collection, and Google Scholar), evaluates the species through its ethnomedicine, phytochemistry, preclinical evidence, and safety. The available evidence suggests that A. lappa exerts antidiabetic effects via multi-layered mechanisms, including AMPK activation, insulin signaling modulation, and increased GLUT4 translocation. Key bioactives (arctigenin, arctiin, and inulin) collectively improve insulin sensitivity and lipid metabolism. However, preclinical studies confirm these effects in animal models, while limited clinical data in non-diabetic cohorts focus on systemic inflammation. This highlights a significant gap in randomized controlled trials targeting glycemic control in diabetic populations. In this context, while A. lappa shows promise as a potential metabolic regulator; this evidence is currently derived primarily from in vitro and animal models. Systematic clinical trials are urgently required to establish glycemic efficacy in humans, validate its therapeutic potential, and determine the optimal dosage and safety profile. This review evaluates the multi-targeted biological potential of A. lappa to guide future research and evidence-based application. Full article

Background: Hepatocellular carcinoma (HCC) is a highly lethal malignancy with limited therapeutic options. Arctigenin (ARC), a natural lignan derived from Saussurea medusa, exhibits anti-cancer activity, but its mechanism against HCC remain incompletely elucidated. Methods: This study integrated network pharmacology, molecular docking, molecular dynamics, in vitro, and in vivo experiments to investigate ARC’s anti-HCC effects. Results: Seventy-five potential targets shared between ARC and HCC were identified, with KEGG analysis highlighting the PI3K/AKT pathway as central. ARC showed strong binding to key proteins, and molecular dynamics indicated stable interactions with PIK3CA and GSK3B. In HepG2 cells, ARC inhibited proliferation in a dose- and time-dependent manner (IC50: 11.17 μM at 24 h, 4.888 μM at 48 h), induced apoptosis at high concentrations, suppressed PIK3CA phosphorylation, and increased GSK3B (Ser9) phosphorylation. In H22 tumor-bearing mice, ARC dose-dependently inhibited tumor growth (high dose: 50.6% vs. 63.0% for CTX) with minimal weight loss. Conclusions: These findings suggest ARC suppresses HCC by modulating the PI3K/AKT pathway, providing evidence for its development as a plant-derived therapeutic agent. Full article

Coronavirus can cause various diseases, from mild symptoms to the recent severe COVID-19. The coronavirus RNA genome is frequently mutated due to its RNA nature, resulting in many pathogenic and drug-resistant variants. Therefore, many medicines should be prepared to respond to the various coronavirus variants. In this report, we demonstrated that Forsythia viridissima fruit ethanol extract (FVFE) effectively reduces coronavirus replication. We attempted to identify the active compounds and found that actigenin from FVFE effectively reduces human coronavirus replication. Arctigenin treatment can reduce coronavirus protein expression and coronavirus-induced cytotoxicity. These results collectively suggest that arctigenin is a potent natural compound that prevents coronavirus replication. Full article

Aging is often accompanied by irreversible decline in body function, which causes a large number of age-related diseases and brings a huge economic burden to society and families. Many traditional Chinese medicines have been known to extend lifespan, but it has still been a challenge to isolate a single active molecule from them and verify the mechanism of anti-aging action. Drugs that inhibit senescence-associated secretory phenotypes (SASPs) are called “senomorphics”. In this study, arctigenin (ATG), a senomorphic, was screened from the Chinese medicine Fructus arctii using K6001 yeast replicative lifespan. Autophagy, oxidative stress, and telomerase activity are key mechanisms related to aging. We found that ATG may act through multiple mechanisms to become an effective anti-aging molecule. In exploring the effect of ATG on autophagy, it was clearly observed that ATG significantly enhanced autophagy in yeast. We further verified that ATG can enhance autophagy by targeting protein phosphatase 2A (PP2A), leading to an increased lifespan. Meanwhile, we evaluated the antioxidant capacity of ATG and found that ATG increased the activities of the antioxidant enzymes, thereby reducing reactive oxygen species (ROS) and malondialdehyde (MDA) levels to improve the survival of yeast under oxidative stress. In addition, ATG was able to increase telomerase activity by enhancing the expression of EST1, EST2, and EST3 genes in yeast. In conclusion, ATG exerts anti-aging effects through induction of autophagy, antioxidative stress, and enhancement of telomerase activity in yeast, which is recognized as a potential molecule with promising anti-aging effects, deserving in-depth research in the future. Full article

The fruit of Forsythia suspensa (Thunb.) Vahl has been used in traditional Chinese medicine as “Forsythiae fructus”. The species is also grown in parks and gardens, and on streets and building lots, as an ornamental plant, but it requires pruning. In this study, the allelopathic activity and allelopathic substances in the leaves of pruned branches of F. suspensa were investigated to determine any potential application. The leaf extracts of F. suspensa showed growth inhibitory activity against three weed species; Echinochloa crus-galli, Lolium multiflorum, and Vulpia myuros. Two allelopathic substances in the extracts were isolated through the bioassay-guided purification process, and identified as (-)-matairesinol and (-)-arctigenin. (-)-Matairesinol and (-)-arctigenin, which showed significant growth inhibitory activity at concentrations greater than 0.3 mM in vitro. The inhibitory activity of (-)-arctigenin was greater than that of (-)-matairesinol. However, both compounds were more active than (+)-pinolesinol which is their precursor in the biosynthetic pathway. The investigation suggests that F. suspensa leaves are allelopathic, and (-)-matairesinol and (-)-arctigenin may contribute to the growth inhibitory activities. Therefore, the leaves of the pruned branches can be applied as a weed management strategy in some agricultural practices such as using the leaf extracts in a foliar spray and the leaves in a soil mixture, thereby reducing the dependency on synthetic herbicides in the crop cultivation and contributing to developing eco-friendly agriculture. Full article

The low bioavailability of most phytochemicals limits their anticancer effects in humans. The present study was designed to test whether combining arctigenin (Arc), a lignan mainly from the seed of Arctium lappa, with green tea (GT) and quercetin (Q) enhances the chemopreventive effect on prostate cancer. We performed in vitro proliferation studies on different cell lines. We observed a strong synergistic anti-proliferative effect of GT+Q+Arc in exposing androgen-sensitive human prostate cancer LNCaP cells. The pre-malignant WPE1-NA22 cell line was more sensitive to this combination. No cytotoxicity was observed in normal prostate epithelial PrEC cells. For an in vivo study, 3-week-old, prostate-specific PTEN (phosphatase and tensin homolog) knockout mice were treated with GT+Q, Arc, GT+Q+Arc, or the control daily until 16 weeks of age. In vivo imaging using prostate-specific membrane antigen (PSMA) probes demonstrated that the prostate tumorigenesis was significantly inhibited by 40% (GT+Q), 60% (Arc at 30 mg/kg bw), and 90% (GT+Q+Arc) compared to the control. A pathological examination showed that all control mice developed invasive prostate adenocarcinoma. In contrast, the primary lesion in the GT+Q and Arc alone groups was high-grade prostatic intraepithelial neoplasia (PIN), with low-grade PIN in the GT+Q+Arc group. The combined effect of GT+Q+Arc was associated with an increased inhibition of the androgen receptor, the PI3K/Akt pathway, Ki67 expression, and angiogenesis. This study demonstrates that combining Arc with GT and Q was highly effective in prostate cancer chemoprevention. These results warrant clinical trials to confirm the efficacy of this combination in humans. Full article

Arctigenin (ATG) is a broad-spectrum antitumor drug with an excellent inhibitory effect on malignant tumors such as breast cancer, glioblastoma, liver cancer, and colon cancer. However, the clinical application of ATG is limited by its poor water solubility and quick hydrolysis in the liver, intestine, and plasma, which might hinder its application. Sialic acid (SA) recognizes selectin receptors overexpressed on the surface of tumor-associated macrophages. In this study, SA was conjugated with octadecylamine (ODA) to prepare SA-ODA, which was employed to prepare SA functionalized nanoliposomes (SA-Lip) to achieve breast cancer targeting. The formulations were finely optimized using the Box–Behnken design to achieve higher ATG loading. The size, ζ potential, entrapment efficiency, drug loading, and release behavior of ATG@SA-Lip were fully investigated in comparison with conventional ATG@Lip. The ATG@SA-Lip displayed more potent cytotoxicity and higher cellular internalization compared to ATG@Sol and ATG@Lip in both MCF7 and 4T1 cells. Notably, ATG@SA-Lip showed the lowest impact on the immune system. Our study demonstrates that SA-Lip has strong potential as a delivery system for the targeted delivery of ATG. Full article

This research aimed to determine the target protein and molecular mechanism of trans-(±)-kusunokinin (KU) derivatives ((±)-arctigenin (ARC) and trans-(±)-TTPG-B). Molecular docking was used to predict potential synthesized (±)-KU targets among 22 proteins. The (+)-TTPG-B bound HSP90α better than EC44, native (±)-KU and trans-(±)-ARC. In contrast, (−)-ARC bound PI3K more strongly than any other test compound. CSF1R and AKR1B1 were not supposed to be the target of (±)-TTPG-B and (±)-ARC, unlike native (±)-KU. The (+)-TTPG-B bound Tyr139 and Trp162 of HSP90α. Moreover, (−)-ARC bound PI3K via hydrogen bonds and π-π stacking at distinct amino acids, which was different from the other tested compounds. Using half of the IC₅₀ concentration, (±)-TTPG-B, (±)-KU and (±)-ARC enhanced cell cycle arrest at the G0/G1 phase after 12 h and 24 h on KKU-M213 (CCA) cells. The (±)-TTPG-B showed a stronger inhibitory effect than (±)-ARC and (±)-KU on HSP90α, PI3K, HSP90β, c-Myc, AKT, MEK1, CyclinB1, CyclinD1, and CDK1 for 24 and 48 h after treatment with the same concentration (0.015 µM). Thus, trans-(±)-TTPG-B, a newly synthesized compound, has pharmacological potential for development as a target therapy for CCA treatment. Full article

The poor oral bioavailability of arctiin caused by its low water solubility is the biggest obstacle in developing it as a drug. In this work, a new water-soluble glucuronide derivative of arctiin (arctigenin-4′-O-glucuronide) was synthesized through 2,2,6,6-tetramethylpiperidine 1-oxyl mediated oxidation reaction. Subsequently, its anti-inflammatory effect was evaluated by mice acute lung injury model in vivo. The results showed that the glucuronide derivative of arctiin not only had better water solubility but also displayed improved anti-inflammatory activity in vivo, thus serving as an innovative compound in the drug development of arctiin. Full article

Fish rhabdoviruses are harmful single-stranded RNA viruses with high mortality rates which cause considerable economic losses in aquaculture. It is imperative to explore and develop new antiviral compounds against them. In recent years, in addition to inorganic antiviral substances, more than 50 different organic compounds have been confirmed to be effective in the prevention and treatment of rhabdovirus infection and its dissemination in fish. The main types of extracts or agents and their trial designs are here considered for review. This review reveals the reported antiviral activities of extracts from organisms, proteins, lipids, polysaccharides, nucleic acids, coumarin derivatives, arctigenin derivatives, and other antiviral organic molecules against fish rhabdoviruses, respectively. Additionally, their antiviral mechanisms of action include direct virucidal effects, inhibiting virus-induced host cell apoptosis, the blocking of the viral replication cycle, affecting gene expression and innate antiviral immune responses, and so on. This review also gives perspectives on how to comprehensively explore the potential applications of the candidate molecules, which lay the foundation for the future development of new compounds or strategies for the prevention and control of fish rhabdoviruses in aquaculture. Full article

Dibenzylbutyrolactone lignans (DBLs) are a class of natural products with a wide variety of biological activities. Due to their potential for the development of human therapeutic agents, DBLs have been subjected to various SAR studies in order to optimise activity. Previous reports have mainly considered changes on the aromatic rings and at the benzylic carbons of the compounds, whilst the effects of substituents in the lactone, at the C-9′ position, have been relatively unexplored. This position has an unexploited potential for the development of novel dibenzyl butyrolactone derivatives, with previous preliminary findings revealing C-9′-hydroxymethyl analogues inducing programmed cell cycle death. Using the core structure of the bioactive natural product arctigenin, C-9′ derivatives were synthesised using various synthetic pathways and with prepared derivatives providing more potent anti-proliferative activity than the C-9′-hydroxymethyl lead compound. Full article

The Arctium lappa L. plant, commonly known as burdock, has been used therapeutically for hundreds of years. Arctigenin (ATG) is an active ingredient in burdock, albeit at low quantities or mostly in the form of acrtiin (arctigenin-4-glucoside). ATG has been touted for its anti-inflammatory properties in many cell types and disease states; however, its role in skin and melanin production has not been extensively studied. Our aims for this study were to develop a burdock seed extract enriched for ATG that is amenable to quasi-drug development, determine in vitro brightening activity, and evaluate safety and skin brightening efficacy clinically in human subjects. Arctiin and ATG content were measured by high-performance liquid chromatography (HPLC). In vitro studies utilized EpiDerm^TM tissues for skin irritation test, and MelanoDerm^TM tissues for melanin reduction capacity. A 45 subject clinical study was performed in adult subjects ranging in age from 30 to 60 years old (mean = 41.9 ± 6.7) to test the safety and skin brightening potential of 1% ABSO lotion. We demonstrate by HPLC that ABSO is a natural extract that contains ~5-times more arctigenin than BSO. Furthermore, ABSO inhibits melanin production better than BSO and retains the same melanin-reducing capacity as synthetic ATG in vitro in MelanoDerm™ 3D skin cultures. ABSO also adheres to quasi-drug criteria according to the Japanese Standards of Quasi-Drug Ingredients as determined by infrared absorption spectrum method, unsaponifiable matter, heavy metal and arsenic content, and acid, saponification, and iodine value methods. Clinical assessment of 1% ABSO lotion shows it is well-tolerated in human skin and demonstrates improved brightness and skin tone evenness. ABSO is a natural arctigenin-enriched burdock seed extract that reduces melanin content in vitro and clinically improves skin brightness. Full article

Salt-sensitive hypertension is closely related to inflammation, but the mechanism is barely known. Transmembrane member 16A (TMEM16A) is the Ca²⁺-activated chloride channel in epithelial cells, smooth muscle cells, and sensory neurons. It can promote inflammatory responses by increasing proinflammatory cytokine release. Here, we identified a positive role of TMEM16A in vascular inflammation. The expression of TMEM16A was increased in high-salt-stimulated vascular smooth muscle cells (VSMCs), whereas inhibiting TMEM16A or silencing TMEM16A with small interfering RNA (siRNA) can abolish this effect in vitro or in vivo. Transcriptome analysis of VSMCs revealed some differential downstream genes of TMEM16A related to inflammation, such as endothelial cell-specific molecule 1 (ESM1) and CXC chemokine ligand 16 (CXCL16). Overexpression of TMEM16A in VSMCs was accompanied by high levels of ESM1, CXCL16, intercellular adhesion molecule-1 (ICAM-1), and vascular adhesion molecule-1 (VCAM-1). We treated VSMCs cultured with high salt and arctigenin (ARC), T16Ainh-A01 (T16), and TMEM16A siRNA (siTMEM16A), leading to greatly decreased ESM1, CXCL16, VCAM-1, and ICAM-1. Beyond that, silencing ESM1, the expression of VCAM-1 and ICAM-1, and CXCL16 was attenuated. In conclusion, our results outlined a signaling scheme that increased TMEM16 protein upregulated ESM1, which possibly activated the CXCL16 pathway and increased VCAM-1 and ICAM-1 expression, which drives VSMC inflammation. Beyond that, arctigenin, as a natural inhibitor of TMEM16A, can reduce the systolic blood pressure (SBP) of salt-sensitive hypertension mice and alleviate vascular inflammation. Full article