Search Results (1,132)

Chrysanthemum × morifolium (Ramat) Hemsl. (Hangbaiju), which has been widely consumed as a herbal tea for over 3000 years, is renowned for its biosafety and diverse bioactivities. This study investigates the impact of polyphenol-rich Hangbaiju extracts (HE) on high-fat diet-induced obesity in mice. HE contains phenolic acids and flavonoids with anti-obesity properties, such as apigenin, luteolin-7-glucoside, apigenin-7-O-glucoside, kaempferol 3-(6″-acetylglucoside), etc. To establish the obesity model, mice were randomly assigned into four groups (n = 8 per group) and administered with either HE or water for 42 days under high-fat or low-fat dietary conditions. Administration of low (LH) and high (HH) doses of HE both significantly suppressed body weight growth (by 16.28% and 16.24%, respectively) and adipose tissue enlargement in obese mice. HE significantly improved the serum lipid profiles, mainly manifested as decreased levels of triglycerides (28.19% in LH and 19.59% in HH) and increased levels of high-density lipoprotein cholesterol (44.34% in LH and 54.88% in HH), and further attenuated liver lipid deposition. Furthermore, HE significantly decreased the Firmicutes/Bacteroidetes ratio 0.23-fold (LH) and 0.12-fold (HH), indicating an improvement in the microecological balance of the gut. HE administration also elevated the relative abundance of beneficial bacteria (e.g., Allobaculum, norank_f__Muribaculaceae), while suppressing harmful pathogenic proliferation (e.g., Dubosiella, Romboutsia). In conclusion, HE ameliorates obesity and hyperlipidemia through modulating lipid metabolism and restoring the balance of intestinal microecology, thus being promising for obesity therapy. Full article

Cynara cardunculus L. subsp. cardunculus (Cynara cardunculus L. var. sylvestris (Lam.) Fiori), the wild cardoon, is known for its culinary applications and potential health benefits. Due to this, and given the growing interest in circular economies, deepening our under-standing of the effects of wild cardoon leaf waste on angiogenesis and collagenase activity represents a valuable opportunity to valorise agricultural byproducts as health-promoting ingredients. In this study, the waste product of wild cardoon leaves was extracted to examine its chemical composition and biological activities. Analytical techniques identified several bioactive compounds, including flavonoids, hydroxycinnamic acids such as dicaffeoyl-succinoylquinic acids, and luteolin-7-O-rutinoside. In vivo tests in zebrafish embryos and the chick chorioallantoic membrane demonstrated dose-dependent antiangiogenic effects, particularly enhanced by the complexation with hydroxypropyl-β-cyclodextrin (HP-β-CD). Considering the link between angiogenesis and collagenase, the potential effects of the extract on collagenase activity was investigated. The extract alone inhibited collagenase with an IC₅₀ value comparable to that of the standard inhibitor while its complexed form exhibited a 4.5-fold greater inhibitory activity. A molecular docking study examined the interaction between the main compounds and collagenase. In conclusion, wild cardoon leaves can represent a valuable source of bioactive compounds. This study demonstrated that the complexation of the extract with cyclodextrin determines an increase in its biological activity. Full article

Biotechnological valorization of Flourensia cernua foliage was carried out using fungal solid-state fermentation; several outcomes of this bioprocess were identified which added value to the plant material. F. cernua leaves placed in aluminum trays were inoculated with Aspergillus niger; extracts of this plant were evaluated and the foliage was tested for in vitro digestibility. The solid bioprocess was carried out at 75% humidity for 120 h and after the fermentation, β-glucosidase activity; phenolics and in vitro digestibility were quantified and measured. Two high β-glucosidase production levels were detected at 42 and 84 h with 3192 and 4092 U/L, respectively. Several phenolics of industrial importance were detected with a HPLC-ESI-MS, such as glycosides of luteolin and apigenin. The other outcome was a substantial improvement in anaerobic digestibility. The unfermented sample registered a 30% in vitro degradability, whereas samples subjected to 84 h of fungal fermentation increased degradability by up to 51%. This bioprocess was designed to detect more than one product, which can contribute to an increase in the added value of F. cernua foliage. Full article

The impact of exogenous melatonin treatment on the postharvest quality and storability of blue honeysuckle fruit was investigated. Fruits were immersed in melatonin solutions at concentrations of 0 (control), 0.01, 0.05, and 0.25 mM for 5 min and subsequently stored at –1 °C for 63 d. Among all treatments, the combination of two-week storage without fruit puncturing and 0.05 mM melatonin application significantly delayed fruit softening and decay even at the initial stage of storage, while also increasing the concentration of phenolic compounds and enhancing antioxidant activity. During the later storage period (28–63 d), melatonin-treated fruits maintained higher levels of maltose, fructose, and sucrose, contributing to improved flavor retention. In contrast, both lower (0.01 mM) and higher (0.25 mM) concentrations were less effective or even detrimental to fruit quality. HPLC-ESI-QTOF-MS² analysis revealed that 0.05 mM melatonin effectively preserved several functional phenolics, including p-coumaroylquinic acid, caffeoyl glucose, 5-O-caffeoylquinic acid, 3-O-caffeoylquinic acid, luteolin-7-O-glucoside, and hydroxytyrosol. Thus, 0.05 mM melatonin is effective in delaying senescence and maintaining the postharvest quality of blue honeysuckle fruit. Full article

Cadmium (Cd)-induced pulmonary toxicity is closely associated with ferroptosis, a regulated form of cell death characterized by iron-dependent lipid peroxidation (LPO). Luteolin (Lut) is a natural flavonoid compound that exists in many plants. In this study, we used human bronchial epithelial BEAS-2B cells to explore the impact of ferroptosis in the inhibition of Cd-induced BEAS-2B cells proliferation. BEAS-2B cells were exposed to Cd (5 μM) with/without Lut (10 μM), ferroptosis modulators (Ferrostatin-1 (Fer-1)/Erastin), or nuclear factor erythroid 2-related factor 2 (Nrf2) regulators (tert-butylhydroquinone (TBHQ)/ML385). Viability, iron content, reactive oxygen species (ROS), LPO, mitochondrial membrane potential (MMP), and glutathione peroxidase (GSH-PX) activity were assessed. Exposure to Cd significantly decreased cell viability, increased intracellular iron levels, ROS production, and LPO activity, while simultaneously reducing MMP and GSH-PX activity. Fer-1 mitigated Cd-induced cytotoxicity, but Erastin intensified these effects. Mechanistically, Cd exposure suppressed the Nrf2/Solute Carrier Family 7 Member 11 (SLC7A11)/glutathione peroxidase 4 (GPX4) signaling pathway, which plays a crucial role in maintaining redox homeostasis. Activation of Nrf2 using TBHQ mitigated oxidative stress and upregulated the expression of key proteins within this pathway, while inhibition of Nrf2 with ML385 exacerbated cellular damage. Notably, Lut treatment could significantly alleviate Cd-induced cytotoxicity, oxidative stress, and downregulation of Nrf2/SLC7A11/GPX4 proteins. These findings demonstrate that ferroptosis is a critical mechanism underlying Cd-mediated lung epithelial injury and identify Lut as a promising therapeutic candidate via its activation of Nrf2-driven antioxidant defense mechanisms. This study provides novel insights into molecular targets for the prevention and treatment of Cd-associated pulmonary disorders. Full article

Unconventional food plants (UFPs) are increasingly valued for their nutritional composition and bioactive potential. This study proposes a comprehensive characterization of the chemical and bioactive properties of Pereskia aculeata Miller (Cactaceae) (PA); Xanthosoma sagittifolium (L.) Schott (Araceae) (XS); Stachys byzantina K. Koch (Lamiaceae) (SB); and inflorescences from three cultivars of Musa acuminata (Musaceae) var. Dwarf Cavendish, var. BRS Platina, and var. BRS Conquista (MAD, MAP, and MAC), including the assessment of physical, nutritional, phytochemical, and biological parameters. Notably, detailed phenolic profiles were established for these species, many of which are poorly documented in the literature. XS was characterized by a unique abundance of C-glycosylated flavones, especially apigenin and luteolin derivatives, rarely described for this species. SB exhibited high levels of phenylethanoid glycosides, particularly verbascoside and its isomers (up to 21.32 mg/g extract), while PA was rich in O-glycosylated flavonols such as quercetin, kaempferol, and isorhamnetin derivatives. Nutritionally, XS had the highest protein content (16.3 g/100 g dw), while SB showed remarkable dietary fiber content (59.8 g/100 g). Banana inflorescences presented high fiber (up to 66.5 g/100 g) and lipid levels (up to 7.35 g/100 g). Regarding bioactivity, PA showed the highest DPPH radical scavenging activity (95.21%) and SB the highest reducing power in the FRAP assay (4085.90 µM TE/g). Cellular antioxidant activity exceeded 2000% in most samples, except for SB. Cytotoxic and anti-inflammatory activities were generally low, with only SB showing moderate effects against Caco-2 and AGS cell lines. SB and PA demonstrated the strongest antimicrobial activity, particularly against Yersinia enterocolitica, methicillin-resistant Staphylococcus aureus (MRSA), and Enterococcus faecalis, with minimum inhibitory concentrations ranging from 0.156 to 0.625 mg/mL. Linear discriminant analysis revealed distinctive chemical patterns among the species, with organic acids (e.g., oxalic up to 7.53 g/100 g) and fatty acids (e.g., linolenic acid up to 52.38%) as key discriminant variables. Overall, the study underscores the nutritional and functional relevance of these underutilized plants and contributes rare quantitative data to the scientific literature regarding their phenolic signatures. Full article

The health benefits of extra virgin olive oil (EVOO), including improved cardiovascular health and metabolic function, are linked to its phenolic content. This study evaluated how storage duration and packaging affect the phenolic composition and sensory quality of Corbella EVOO. Oils were analyzed at production and after 6 and 12 months of storage in two types of packaging: bag-in-box; stainless steel containers with a nitrogen headspace. UPLC-MS/MS profiling quantified 23 phenolic compounds, predominantly secoiridoids such as oleuropein and ligstroside aglycones. Oleuropein aglycone increased over time, whereas ligstroside aglycone peaked mid-storage before declining, likely converting to oleocanthal. Lignans and flavonoids degraded during storage, although luteolin increased, potentially due to glucoside hydrolysis. Bag-in-box packaging better preserved phenolic content than stainless steel. A sensory analysis corroborated the chemical findings, with oils stored in stainless steel showing greater reductions in pungency and astringency. A Pearson correlation linked bitterness with oleuropein aglycone (r = 0.44) and oleacein (r = 0.66), pungency with oleocanthal (r = 0.81), and astringency with oleacein (r = 0.86) and oleocanthal (r = 0.71). These findings highlight the importance of packaging in preserving the phenolic composition responsible for the sensory qualities of EVOO over time. Full article

The capitula of Chrysanthemum indicum Linné or C. morifolium Ramatuelle (Kikuka in Japanese) are included in several formulae of Kampo medicines (traditional Japanese medicines), such as Chotosan, which is used for headache and dizziness. Luteolin, the principal constituent of C. indicum, has antioxidant and anti-inflammatory activities. However, the effects of other flavonoids on this crude drug have not yet been thoroughly investigated. To evaluate and compare anti-inflammatory effects, we used primary cultured rat hepatocytes, which produce proinflammatory mediators, such as nitric oxide (NO) and proinflammatory cytokines, in response to interleukin (IL)-1β. Eight derivatives of 5,7-dihydroxyflavone were purified and identified in the ethyl acetate-soluble fraction of a C. indicum capitulum extract: luteolin (Compound 1), apigenin (2), diosmetin (3), 5,7-dihydroxy-3′,4′,5′-trimethoxyflavone (4), acacetin (5), eupatilin (6), jaceosidin (7), and 6-methoxytricin (8). Luteolin is the most abundant compound in this fraction. All compounds significantly suppressed NO production in hepatocytes, with apigenin and acacetin showing the greatest efficacy. The comparison of the IC₅₀ values of the inhibition of NO production suggests that substitutions by hydroxyl and methoxy groups at the C-3′ and C-4′ positions of 5,7-dihydroxyflavone may be at least essential for the suppression of NO production. In hepatocytes, acacetin and luteolin decreased the levels of mRNAs encoding inducible nitric oxide synthase (iNOS), proinflammatory cytokines, including tumor necrosis factor, IL-6, and type 1 IL-1 receptor, which regulates inflammatory responses. Based on the comparison of the IC₅₀ values and the content, luteolin, jaceosidin, and diosmetin may be responsible for the anti-inflammatory effects of C. indicum capitula. Full article

Lobelia nummularia Lam. is a traditional medicinal herb of which the anticancer mechanisms remain largely unexplored. Here, we demonstrated that its ethanolic extract (LNE) exerts potent anti-breast cancer activity by inducing ROS-dependent mitochondrial apoptosis in MDA-MB-231 cells, a mechanism confirmed via rescue experiments with the antioxidant N-acetylcysteine (NAC). This pro-apoptotic program is driven by a dual mechanism: potent suppression of the pro-survival EGFR/PI3K/AKT signaling pathway and simultaneous activation of the TP53-mediated apoptotic cascade, culminating in the cleavage of executor caspase-3. Phytochemical analysis identified numerous flavonoids, and quantitative HPLC confirmed that key bioactive compounds, including luteolin and apigenin, are substantially present in the extract. These mechanisms translated to significant in vivo efficacy, where LNE administration suppressed primary tumor growth and lung metastasis in a 4T1 orthotopic model in BALB/c mice. Furthermore, a validated molecular docking protocol provided a plausible structural basis for these multi-target interactions. Collectively, this study provides a comprehensive, multi-layered validation of LNE’s therapeutic potential, establishing it as a mechanistically well-defined candidate for natural product-based anticancer drug discovery. Full article

Background: Herbal medicine represents a rich yet complex source of bioactive compounds, offering both therapeutic potential and toxicological risks. Methods: In this study, we systematically evaluated the biological effects of three traditional herbal extracts—Mentha longifolia, Scrophularia orientalis, and Echium biebersteinii—using Caenorhabditis elegans as an in vivo model. Results: All three extracts significantly reduced worm survival, induced larval arrest, and triggered a high incidence of males (HIM) phenotypes, indicative of mitotic failure and meiotic chromosome missegregation. Detailed analysis of germline architecture revealed extract-specific abnormalities, including nuclear disorganization, ectopic crescent-shaped nuclei, altered meiotic progression, and reduced bivalent formation. These defects were accompanied by activation of the DNA damage response, as evidenced by upregulation of checkpoint genes (atm-1, atl-1), increased pCHK-1 foci, and elevated germline apoptosis. LC-MS profiling identified 21 major compounds across the extracts, with four compounds—thymol, carvyl acetate, luteolin-7-O-rutinoside, and menthyl acetate—shared by all three herbs. Among them, thymol and carvyl acetate significantly upregulated DNA damage checkpoint genes and promoted apoptosis, whereas thymol and luteolin-7-O-rutinoside contributed to antioxidant activity. Notably, S. orientalis and E. biebersteinii shared 11 of 14 major constituents (79%), correlating with their similar phenotypic outcomes, while M. longifolia exhibited a more distinct chemical profile, possessing seven unique compounds. Conclusions: These findings highlight the complex biological effects of traditional herbal extracts, demonstrating that both beneficial and harmful outcomes can arise from specific phytochemicals within a mixture. By deconstructing these extracts into their active components, such as thymol, carvyl acetate, and luteolin-7-O-rutinoside, we gain critical insight into the mechanisms driving reproductive toxicity and antioxidant activity. This approach underscores the importance of component-level analysis for accurately assessing the therapeutic value and safety profile of medicinal plants, particularly those used in foods and dietary supplements. Full article

Background: Metabolic syndrome (MetS) is characterized by chronic inflammation, oxidative stress, and mitochondrial dysfunction. MetS is associated with increased intestinal permeability and dysbiosis. The objective of this study was to investigate the effects of peanut shell extract (PSE) and luteolin (LUT) on the kidneys, colon, and ileum in a MetS-like murine model. Methods: Thirty-six male Slc6a14^y/− mice were divided into four groups: low-fat diet (LFD), high-fat diet (HFD), HFD + 200 mg PSE/kg BW (PSE, p.o.), and HFD + 100 mg LUT/kg BW (LUT, p.o.) for 4 months. Outcome measures included glucose homeostasis, intestinal permeability, gut microbiome composition, and mRNA gene expression of mitochondrial homeostasis and inflammation/oxidative stress in the kidneys, colon, and ileum. Results: HFD resulted in glucose dysregulation with hyperglycemia and insulin resistance. PSE and LUT improved insulin tolerance and beta-cell function. PSE and LUT mitigated HFD-increased serum lipopolysaccharide-binding protein concentration. Perturbations in the gut microbiome were associated with HFD, and PSE or LUT reversed some of these changes. Specifically, Phocaeicola vulgatus was depleted by HFD and reverted by PSE or LUT. Relative to the LFD group, the HFD group (1) upregulated mitochondrial fusion (MFN1, MFN2, OPA1), mitophagy (TLR4, PINK1, LC3B), and inflammation (NFκB, TNFα, IL6), and (2) downregulated mitochondrial fission (FIS1, DRP1), biosynthesis (PGC1α, NRF1, NRF2, TFAM), electron transport chain (complex I), and antioxidant enzyme (SOD1) in the kidneys, colon, and ileum. Conclusions: PSE and LUT reversed such HFD-induced changes in the aforementioned gene expression levels. Full article

Lactate dehydrogenase (LDH) catalyzes the reversible interconversion of pyruvate and lactate, coupled with the redox cycling of NADH and NAD⁺. While LDHA has been extensively studied as a therapeutic target, particularly in cancer, due to its role in the Warburg effect, LDHB remains underexplored, despite its involvement in the metabolic reprogramming of specific cancer types, including breast and lung cancers. Most known LDH inhibitors are designed against the LDHA isoform and act competitively at the active site. In contrast, LDHB exhibits distinct kinetic properties, substrate preferences, and structural features, warranting isoform-specific screening strategies. In this study, 115 natural compounds previously reported as LDHA inhibitors were systematically evaluated for LDHB inhibition using an integrated in silico and in vitro approach. Virtual screening identified 16 lead phytochemicals, among which luteolin and quercetin exhibited uncompetitive inhibition of LDHB, as demonstrated by enzyme kinetic assays. These findings were strongly supported by molecular docking analyses, which revealed that both compounds bind at an allosteric site located at the dimer interface, closely resembling the binding mode of the established LDHB uncompetitive inhibitor AXKO-0046. In contrast, comparative docking against LDHA confirmed their active-site binding and competitive inhibition, underscoring their isoform-specific behavior. Our findings highlight the necessity of assay conditions tailored to LDHB’s physiological role and demonstrate the application of a previously validated colorimetric assay for high-throughput screening. This work lays the foundation for the rational design of selective LDHB inhibitors from natural product libraries. Full article

Mao Jian Green Tea flavonoids (MJGT_F) contain luteolin, luteolin-7-O-glucoside, eriodictyol, and eriodictyol-7-O-glucoside, among which the first three components have hypoglycemic effects; however, the overall hypoglycemic potential of MJGT_F remains unclear. This study demonstrated that MJGT_F inhibited α-glucosidase in vitro and improved metabolic parameters in a dose-dependent manner in T2DM (type 2 diabetes mellitus) rats (reducing blood glucose, triglyceride, total cholesterol, low-density lipoprotein, insulin, and the homeostatic model assessment of insulin resistance; increasing high-density lipoprotein, insulin sensitivity index, and glucagon-like peptide-1). High-dose MJGT_F (MJGT_F_H) showed optimal efficacy. Mechanistically, MJGT_F_H activated the AMPK pathway, evidenced by a significant increase in the p-AMPK/AMPK ratio and downregulation of hepatic gluconeogenic enzymes G6Pase and PEPCK. These coordinated effects collectively suggest enhanced hepatic glucose utilization and suppression of glucose overproduction. MJGT_F_H also modulated gut microbiota by enriching beneficial taxa (e.g., Akkermansia muciniphila, 11.17-fold vs. metformin) and reducing pathogens like Enterobacteriaceae. These findings highlight MJGT_F’s dual regulatory roles in glucose metabolism and microbiota, supporting its potential for diabetes management. Full article

Background/Objectives: Verbena officinalis L. (common vervain) is a medicinal plant traditionally used and investigated in phytotherapy for its neuroprotective, antioxidant, and anti-inflammatory properties. This study aims to investigate the phytochemical diversity and biological activity of V. officinalis extracts prepared with different ratios of butanol and ethanol. Methods: Aerial parts of V. officinalis were extracted using four solvent systems: 100% butanol (B1), 75:25 (BE7.5), 50:50 (BE5), and 25:75 (BE2.5) butanol:ethanol mixtures. Metabolite profiling was conducted using liquid chromatography–high-resolution tandem mass spectrometry (LC-HRMS/MS). Antioxidant activities were evaluated through six assays: 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), cupric ion-reducing antioxidant capacity (CUPRAC), ferric-reducing antioxidant power (FRAP), metal-chelating ability (MCA), and the phosphomolybdenum assay (PMA). Enzyme inhibition assays targeted acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, and α-amylase. Antibacterial activity against Pseudomonas aeruginosa was tested via microdilution, while dominant phytochemicals were evaluated for binding affinity through molecular docking. Results: Seventy-five compounds, including phenolic acids, flavonoids, iridoids, phenylethanoids, and xanthones, were identified. BE5 extract exhibited the highest total phenolic content and strongest antioxidant capacity, while BE2.5 demonstrated the greatest antibacterial and metal-chelating effects. All extracts showed comparable AChE inhibition, with BE5 achieving the strongest tyrosinase and α-amylase inhibition. Docking studies confirmed high binding affinities of luteolin glucuronides to human and bacterial target enzymes. Conclusions: Solvent composition markedly influenced the chemical and biological profiles of V. officinalis extracts. BE5 and BE2.5 emerged as promising systems for obtaining bioactive fractions with therapeutic potential. Full article

The COVID-19-related long-standing effect or Post-Acute Sequelae of COVID-19 (PASC) is often associated with NLRP3 inflammasome activation in pulmonary inflammation elicited by SARS-CoV-2 spike proteins. Spike proteins engage toll-like receptors (TLRs) in respiratory epithelial cells, leading to excessive cytokine production. Given the need for effective therapeutic strategies to mitigate spike protein-stimulated lung inflammation, we examined the anti-inflammatory properties of luteolin and ethanolic extract from Harrisonia perforata (Blanco) Merr. root. The ethanolic extract of H. perforata root (HPEE) contained a high concentration of luteolin flavonoid (143.53 ± 1.58 mg/g extract). Both HPEE (25–100 μg/mL) and luteolin (4.5–36 μM) significantly inhibited inflammation stimulated by the Wuhan (W) and Omicron (O) spike protein S1, as evidenced by a dose-dependent significant decrease in IL-6, IL-1β, and IL-18 secretion in A549 lung epithelial cells (p < 0.05). Furthermore, pretreatment with HPEE or luteolin prior to spike protein exposure (100 ng/mL) significantly, in a dose-dependent manner, repressed the inflammatory mRNA expression (p < 0.05). Mechanistic study revealed that HPEE and luteolin suppressed NLRP3 inflammasome signaling activation by reducing their machinery protein expressions. Additionally, they inhibited the ERK/JNK/p38 MAPK signaling activation, resulting in decreased inflammatory mRNA expression and cytokine release. These findings suggest that H. perforata root extract and its major flavonoid luteolin exert potent anti-inflammatory effects and may offer therapeutic potential against spike protein-induced lung inflammation. Full article