Journal of Functional Foods
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2019
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IF 3.197
Shujie Zhu,Shaowei Lei,Sisi Zhou,Lisha Jin,Su Zeng,Huidi Jiang,Hui Zhou
Luteolin is an important phytoestrogen with antidepressant effects found in many foods. We aimed to clarify the underlying antidepressant mechanisms of luteolin on PMAT associated with the monoamine hypothesis. We found rPmat had high expression in the limbic system, significant differences in mRNA expression between the pregnant and non-pregnant rats and an upward trend in mice with chronic unpredictable mild stress (CUMS). The results in the stably transfected cell models demonstrated that luteolin was the inhibitor of monoamine transporters. Further studies in C6 cells and primary hippocampal neurons revealed luteolin significantly downgraded PMAT mainly through the oestrogen β receptor (ERβ) and upgraded brain-derived neurotrophic factor (BDNF) expression. These results for PMAT have also been demonstrated in ovariectomized depressed rats. In conclusion, luteolin could directly and indirectly inhibit serotonin reuptake, resulting in an increase in monoamine neurotransmitters in the synaptic cleft. These findings manifest the antidepressant mechanisms of luteolin through PMAT.
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高影响因子
PHARMACOLOGICAL RESEARCH
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2021
·
IF 7.658
Jinzhu Zhao,Leilei Li,Zhijia Wang,Linlin Li,Mingjing He,Shuhua Han,Yalong Dong,Xiaojie Liu,Wen Zhao,Yu Ke,Cong Wang
Cancer drug resistance is a formidable obstacle that enhances cancer stem-like cell properties, tumour metastasis and relapse. Luteolin (Lut) is a natural flavonoid with strong antitumor effects. However, the underlying mechanism(s) by which Lut protects against paclitaxel-resistant (PTX-resistant) cancer cell remains unknown. Herein, we found that Lut significantly attenuated the stem-like properties of PTX-resistant cancer cells by downregulating the expression of SOX2 protein. Additionally, further study showed that Lut could inhibit the PI3K/AKT pathway to decrease the phosphorylation level of AKT(S473) and UBR5 expression, which is an ubiquitin E3 ligase that promotes SOX2 degradation. In addition, Lut also inhibited PTX-resistant cancer cell migration and invasion by blocking epithelial-mesenchymal transition (EMT) . Importantly, Lut inhibited the tumorigenic ability of oesophageal PTX-resistant cancer cells and showed no obvious toxicity in vivo. Thus, Lut has potential as a promising agent for drug-resistant oesophageal cancer therapy.
研究领域:
癌症生物学
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药理学
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分子生物学
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PubMed
高影响因子
Materials Today Bio
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2026
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IF 10.2
Xiaowen Zheng,Wenqi Wang,Xiaolong Wei,Jianguo Niu,Wei Zhang,Zhenxun Lin,Wei Wei,Shipeng Ning,Min Wang,Xianwen Wang,Qingjun Wei
Precise spatiotemporal control of inflammation serves as an effective means to regulate the inflammatory microenvironment and promote wound healing. This study constructed strontium‒luteolin (Sr‒Lut) nanoparticles with a spherical morphology, which demonstrated outstanding radical scavenging capacity through synergistic metal‒ligand effects. Specifically, Sr-Lut efficiently scavenges reactive oxygen species, inhibits the TNF-α/NF-κB and JAK-STAT signaling pathways, promotes M2 polarization, and simultaneously reduces the proinflammatory factor IL-1β and increases the anti-inflammatory factor IL-10. Transcriptomic analysis revealed that Sr-Lut reprogrammed macrophages to downregulate Ccl4 and Retnlg while upregulating extracellular matrix remodeling-associated genes. In vivo experiments demonstrated that Sr-Lut accelerated wound closure in a dose-dependent manner, achieving a healing rate of 94.33% by day 11, which was significantly greater than the 58.54% reported in the control group, while also enhancing re-epithelialization and collagen deposition. Wound tissue RNA sequencing revealed that Sr-Lut inhibits the IL-17, Toll-like receptor and NF-κB signaling pathways while promoting the expression of genes associated with epidermal structural components. In summary, a dual-function nanocomposite with both anti-inflammatory and tissue-repair capabilities has been developed, offering a promising immunomodulatory strategy for wound treatment.
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高影响因子
Frontiers in Nutrition
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2026
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IF 5.5
Quanyong Wu,Boya Ouyang,Hui Cao,Min Zhang,Mohamed A. Farag,Thomas Efferth,Jesus Simal-Gandara,Jianbo Xiao
IntroductionLuteolin is a dietary flavonoid widely distributed in fruits, vegetables, and medicinal plants and is recognized for its antioxidant and health-promoting properties. However, its effects on physiological aging and the influence of developmental stage and biological sex remain poorly understood.MethodsIn this study, Drosophila melanogaster was exposed to luteolin during either adulthood or embryonic development and evaluated for lifespan, healthspan, metabolic regulation, and aging-related molecular changes.ResultsAdult supplementation exerted pronounced female-specific benefits, increasing median lifespan by 11.6%, improving locomotor activity and stress resistance, with little effect on body weight, whereas males showed little response. Notably, short-term supplementation during early adulthood produced sustained protective effects later in life. Mechanistically, luteolin enhanced antioxidant defenses, suppressed IIS/PI3K–mTOR signaling, activated AMPK/MAPK pathways, promoted autophagy and immune homeostasis, and induced metabolic remodeling associated with reduced mitochondrial stress and favorable histone modifications. In contrast, embryonic exposure shortened lifespan and disrupted endocrine and metabolic homeostasis, as evidenced by elevated juvenile hormone levels, reduced catalase activity, and dysregulated IIS signaling.DiscussionThese findings suggest that the biological effects of luteolin on aging are highly dependent on developmental stage and biological sex in Drosophila. The beneficial effects observed in adult females were associated with coordinated changes in nutrient-sensing pathways, metabolism, mitochondrial function, and epigenetic regulation, whereas developmental exposure produced adverse outcomes. Collectively, this study provides new insights into the context-dependent actions of dietary flavonoids in Drosophila and highlights the importance of developmental stage and biological sex when evaluating nutritional interventions for healthy aging.
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CURRENT MICROBIOLOGY
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2024
·Vol. 82
·期 1
·1-16
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IF 2.3
Wang Zhibin,Shen Wanxia,Li Yuejiao,Wang Xiaoyun,Zhong Xiaolin,Wang Xing
The emergence of pathogenic bacteria resistant to conventional antibiotics is becoming increasingly challenging. Plant-derived flavonoids are potential alternatives to antibiotics, owing to their antimicrobial properties. However, the molecular mechanisms through which they inhibit the growth of pathogenic microorganisms remain unclear. Therefore, Klebsiella pneumoniae ATCC700603 was separately incubated in two flavonoids to elucidate their inhibitory mechanism. Metabolomic and transcriptomic analyses were performed after 4-h incubation. In total, 5483 genes and 882 metabolites were identified. Compared to the untreated control, rutin and luteolin activated 507 and 374 differentially expressed genes (DEGs), respectively. However, the number of differential abundant metabolites (DAMs) remained the same. The top 10 correlated DEGs and DAMs were identified within each comparative group after a correlation analysis. Rutin induced the accumulation of unique metabolites and suppressed gene expression whereas luteolin did not. Our results explain the disparate effects of these two flavonoids and demonstrate the inhibitory mechanism of rutin on strain growth.
研究领域:
微生物学
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药理学
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分子生物学
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
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IF 7.7
Weiwei Feng,Xinyu Guo,Guang Yang,Yao Yao,Lixia Zhao,Shuang Gao,Fei Ye,Ying Fu
Hydroxypropyl-gamma-cyclodextrin (HP γ CD) inclusion complex nanofibers (Lut/HP γ CD-IC-NF) containing Luteolin (Lut) were prepared by electrospinning technology. Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) spectra confirmed the formation of Lut/HP γ CD-IC-NF. Scanning electron microscopy (SEM) images showed that the morphology of Lut/HP γ CD-IC-NF was uniform and bead-free, suggesting that self-assembled aggregates, macromolecules with higher molecular weights , were formed by strong hydrogen bonding interactions between the cyclodextrin inclusion complexes. Confocal laser scanning microscopy (CLSM) images showed that Lut was distributed in Lut/HP γ CD-IC-NF. Proton nuclear magnetic resonance ( 1 H NMR) spectroscopy revealed the change in chemical shift of the proton peak between Lut and HP γ CD, confirming the formation of inclusion complex. Thermogravimetric analysis (TGA) proved that Lut/HP γ CD-IC-NF had good thermal stability . The phase solubility test confirmed that HP γ CD had a solubilizing effect on Lut . When the solubility of HP γ CD reached 10 mM, the solubility of Lut increased by 15-fold. The drug loading test showed that the content of Lut in fibers reached 8.57 ± 0.02 %. The rapid dissolution experiment showed that Lut/HP γ CD-IC-NF dissolved within 3 s. The molecular simulation provides three-dimensional evidence for the formation of inclusion complexes between Lut and HP γ CD. Antibacterial experiments showed that Lut/HP γ CD-IC-NF had enhanced antibacterial activity against S. aureus . Lut/HP γ CD-IC-NF exhibited excellent antioxidant properties with a free radical scavenging ability of 89.5 ± 1.1 %. In vitro release experiments showed Lut/HP γ CD-IC-NF had a higher release amount of Lut. In conclusion, Lut/HP γ CD-IC-NF improved the physicochemical properties and bioavailability of Lut, providing potential applications of Lut in the pharmaceutical field.
研究领域:
药学
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材料科学
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PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2025
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IF 4.6
Xiangrong Li,Wanqing Xu,Xianfei Liu,Zhizhi Song,Zheng Li,Zihan Jia
In this study, the interaction mechanism of papain and bromelain with apigenin and luteolin in binary and ternary systems was compared and analyzed by spectroscopic methods, molecular docking, and molecular dynamics simulation. Additionally, the effects of apigenin and/or luteolin on the conformational changes and enzymatic activity of papain and bromelain were investigated. The results show that apigenin and/or luteolin exhibit a moderate binding affinity with papain/bromelain, with the binding constants K a in the range of 10 4 –10 5 L mol −1 . The order of addition of apigenin and luteolin significantly influenced their binding affinities to the enzymes. The main non-covalent forces of the papain-luteolin (first)-apigenin ternary system are hydrogen bonds and Van der Waals forces. Hydrophobic interactions, electrostatic forces and hydrogen bonds are the main non-covalent forces of other binary and ternary systems. These systems differentially alter the microenvironment of Trp and Tyr residues, secondary and tertiary structures, and enzymatic activity. Molecular docking and dynamics simulations identified specific binding sites of apigenin and/or luteolin on papain/bromelain, corroborating experimental findings. Notably, the ternary system exhibits a stronger inhibitory effect on papain activity compared to binary systems.
研究领域:
生物化学
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分子生物学
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PubMed
高影响因子
DYES AND PIGMENTS
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2025
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IF 4.2
Di Wu,Chengpei Du,Lingyan Ma,Rui Xiao,Long Tan,Wenjing Qi
Owing to Zn 2+ -sensitized fluorescent effect, boric acid functionalized zinc-europium binuclear metal-organic frameworks ( Zn-Eu-MOFs ) are synthesized and applied in fluorescent quenching detection of luteolin in Chrysanthemum tea for the first time. Eu 3+ /Zn 2+ and 5-boronobenzene-1,3-dicarboxylic acid (BBDC) are utilized via a fast one-pot microwave process at 120 °C for 1 h. Due to energy transfer efficiency change by “antenna” effect and better effective energy transfer of Zn 2+ than Eu 3+ , Zn 2+ increases fluorescence of Zn-Eu-MOFs nearly 3.5 times. Different ligands and different metal ions are compared to synthesize Zn-Eu-MOFs . Highly specific binding affinity of boric acid towards cis-diol structure in luteolin and chelating of Zn 2+ with luteolin achieves fluorescent quenching detection of luteolin with low limit of detection of 16 nΜ and high selectivity. When it is utilized in fluorescent detection of luteolin in water and Chrysanthemum tea, mean recoveries are obtained from 99.5 % to 102.7 % and from 99.3 % to 100.6 %, respectively.
研究领域:
化学
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食品科学
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高影响因子
PHYTOMEDICINE
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2024
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IF 6.7
Shuang Chai,Yanbing Yang,Liwei Wei,Yuju Cao,Jiangtao Ma,Xuxia Zheng,Junyan Teng,Na Qin
Background Recently, osteoblast pyroptosis has been proposed as a potential pathogenic mechanism underlying osteoporosis, although this remains to be confirmed. Luteolin (Lut), a flavonoid phytochemical, plays a critical role in the anti-osteoporosis effects of many traditional Chinese medicine prescriptions. However, its protective impact on osteoblasts in postmenopausal osteoporosis (PMOP) has not been elucidated. Purpose This research aimed to determine the effect of Lut in ameliorating PMOP by alleviating osteoblast pyroptosis and sustaining osteogenesis. Study design This research was designed to investigate the novel mechanism of Lut in alleviating PMOP both in cell and animal models. Methods Ovariectomy-induced PMOP models were established in mice with/without daily gavaged of 10 or 20 mg/kg body weight Lut. The impact of Lut on bone microstructure, metabolism and oxidative stress was evaluated with 0.104 mg/kg Estradiol Valerate Tablets daily gavaged as positive control. Network pharmacological analysis and molecular docking were employed to investigate the mechanisms of Lut in PMOP treatment. Subsequently, the impacts of Lut on the PI3K/AKT axis, oxidative stress, mitochondria, and osteoblast pyroptosis were assessed. In vitro, cultured (MC3T3-E1(14) cells were exposed to H 2 O 2 with/without Lut to examine its effects on the PI3K/AKT signaling pathway, osteogenic differentiation, mitochondrial function, and osteoblast pyroptosis. Results Our findings demonstrated that 20 mg/kg Lut, similar to the positive control drug, effectively reduced systemic bone loss and oxidative stress, and enhanced bone metabolism induced by ovariectomy. Network pharmacological analysis and molecular docking indicated that the PI3K/AKT axis was a potential target, with oxidative stress response and nuclear membrane function being key mechanisms. Consequently, the effects of Lut on the PI3K/AKT axis and pyroptosis were investigated. In vivo data revealed that the PI3K/AKT axis was deactivated following ovariectomy, and Lut restored the phosphorylation of key proteins, thereby reactivating the axis. Additionally, Lut alleviated osteoblast pyroptosis and mitochondrial abnormalities induced by ovariectomy. In vitro, Lut intervention mitigated the inhibition of the PI3K/AKT axis and osteogenesis, as well as H 2 O 2 -induced pyroptosis. Furthermore, Lut attenuated ROS accumulation and mitochondrial dysfunction. The effects of Lut, including osteogenesis restoration, anti-pyroptosis, and mitochondrial maintenance, were all reversed with LY294002 (a PI3K/AKT pathway inhibitor). Conclusion In summary, Lut could improve mitochondrial dysfunction, alleviate GSDME-mediated pyroptosis and maintain osteogenesis via activating the PI3K/Akt axis, offering a new therapeutic strategy for PMOP.
研究领域:
药理学
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骨生物学
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细胞信号传导
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骨质疏松研究
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高影响因子
Journal of Integrative Neuroscience
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2024
·Vol. 23
·期 10
·185
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IF 2.5
Yangzhi Xie,Hao Zhang,Jiacheng Chen,Sicong Xu,Yan Luo
Background: Luteolin is a natural flavonoid and its neuroprotective and anti-inflammatory effects have been confirmed to mitigate neurodegeneration. Despite these findings, the underlying mechanisms responsible for these effects remain unclear. Toll-like receptor 4 (TLR4) is widely distributed in microglia and plays a pivotal role in neuroinflammation and neurodegeneration. Here studies are outlined that aimed at determining the mechanisms responsible for the anti-inflammatory and neuroprotective actions of luteolin using a rodent model of Parkinson's disease (PD) and specifically focusing on the role of TLR4 in this process. Methods: The mouse model of PD used in this experiment was established through a single injection of lipopolysaccharide (LPS). Mice were then subsequently randomly allocated to either the luteolin or vehicle-treated group, then motor performance and dopaminergic neuronal injury were evaluated. BV2 microglial cells were treated with luteolin or vehicle saline prior to LPS challenge. MRNA expression of microglial specific marker ionized calcium-binding adapter molecule 1 (IBA-1) and M1/M2 polarization markers, as well as the abundance of indicated pro-inflammatory cytokines in the mesencephalic tissue and BV2 were quantified by real time-polymerase chain reaction (RT-PCR) and Enzyme-linked Immunosorbent Assay (ELISA), respectively. Cell viability and apoptosis of neuron-like PC12 cell line co-cultured with BV2 were detected. TLR4 RNA transcript and protein abundance in mesencephalic tissue and BV2 cells were detected. Nuclear factor kappa-gene binding (NF-κB) p65 subunit phosphorylation both in vitro and in vivo was evaluated by immunoblotting. Results: Luteolin treatment induced functional improvements and alleviated dopaminergic neuronal loss in the PD model. Luteolin inhibited apoptosis and promoted cell survival in PC12 cells. Luteolin treatment shifted microglial M1/M2 polarization towards an anti-inflammatory M2 phenotype both in vitro and in vivo. Finally, it was found that luteolin treatment significantly downregulated both TLR4 mRNA and protein expression as well as restraining NF-κB p65 subunit phosphorylation. Conclusions: Luteolin restrained dopaminergic degeneration in vitro and in vivo by blocking TLR4-mediated neuroinflammation.
研究领域:
神经科学
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药理学
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免疫学
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分子生物学
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PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
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2021
·Vol. 46
·期 5
·2360-2367
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IF 3.591
Xiaoyan Wang,Xiaona Hu,Shiqing Li,Wenhui Shi,Shujing Li,Yuxi Zhang
Sustained-release antimicrobial nanofibers (PVA-Lut-IC-NF) were prepared by incorporating a luteolin-hydroxypropyl-β-cyclodextrin inclusion complex (Lut-IC) into polyvinyl alcohol (PVA) via the electrospinning technique. PVA-Lut-IC-NF exhibits excellent water solubility and thermal stability. The results also showed significant antibacterial effects of PVA-Lut-IC-NF against Staphylococcus aureus, Candida albicans and Escherichia coli. Moreover, because of the sensitivities of different cytoderms to Lut, PVA-Lut-IC-NF was more effective against Staphylococcus aureus than Candida albicans and Escherichia coli. Additionally, PVA-Lut-IC-NF showed an appropriate slow release and maintained effective concentration in vitro release. PVA-Lut-IC-NF could have potential applications in food, pharmaceuticals, and healthcare due to its efficient antibacterial activity along with enhanced water solubility and thermal stability.
研究领域:
材料科学
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微生物学
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药剂学
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高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2021
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IF 4.36
Ali Attiq,Juriyati Jalil,Khairana Husain,Hazni Falina Mohamad,Abrar Ahmad
Ethnopharmacological relevance Numerous Alphonsea species including Alphonsea elliptica (mempisang) leaves and fruits are indigenously used in inflammatory conditions such as postpartum swelling and rheumatism in southeast Asian countries. In our previous in-vitro findings, A. elliptica methanol extract exhibited platelet-activating factor inhibition, suggesting the presence of phyto-constituents with anti-inflammatory potential. Aim of the study However, so far there is no literature available on the anti-inflammatory activity of this species. Henceforth, based on the above background and our previous laboratory findings, we hypothesize that phytoconstituents of A. elliptica could possess anti-inflammatory potential against inflammatory mediators including prostaglandin-E 2 (PGE 2 ), cyclooxegenase-2 (COX-2) and cytokines (IL-1β and IL-6). Materials and methods Vacuum and column chromatography techniques were employed for the isolation of phytoconstituents. The structure elucidation was carried out using HRESI-MS, 1 H and 13 C-NMR analysis and compared with the published literature. For cytotoxicity analysis, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was performed on peripheral blood mononuclear cells. In-vitro anti-inflammatory activities were evaluated against the levels of PGE 2 , COX-2, IL-1β and IL-6 in lipopolysaccharide (LPS)-induced human plasma using enzyme-linked immunosorbent assay and radioimmunoassay . Results Unprecedentedly, chromatographic purification of methanolic leaves extract afforded five flavones namely vitexin , isovitexin , orientin, isoorientin , schaftoside with three flavanols ; kaempferol , myricetin and rutin from A elliptica . In cell viability analysis, isolates did not present cytotoxicity up to 50 μM. In anti-inflammatory evaluation, orientin and isoorientin exhibited strong (≥70%), while isovitexin and vitexin produced strong to moderate (50–69%) PGE 2 , COX-2, IL-1β and IL-6 inhibition at 25 and 50 μM. Isoorientin, orientin, isovitexin, and vitexin showed significant (p < 0.05) and concentration-dependent PGE 2 inhibition with IC 50 values (μM) of 11.40, 14.71, 17.70 and 20.58 against indomethacin (8.80). Furthermore, isoorientin, orientin, isovitexin, and vitexin produced significant concentration-dependent inhibition with IC 50 values (μM) of COX-2: 7.13, 9.51, 12.81, 16.61; IL-1β 4.80, 6.20, 10.85, 14.51; IL-6: 4.01, 5.90, 11.51 and 14.88 as compared to dexamethasone : 5.29, 2.93, 3.72, respectively (p < 0.05). Conclusion Conclusively, isolated phytoconstituents are reported for the first time from the A. elliptica. Moreover, isovitexin, vitexin orientin and isoorientin abrogated LPS-induced inflammatory responses in human plasma at non-cytotoxic concentrations.
研究领域:
药理学
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民族药理学
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生物化学
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免疫学
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植物化学
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PubMed
高影响因子
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