PHYTOMEDICINE
·
2025
·
IF 8.3
Zhirui Du,Xueqiao Yan,Lin Cheng,Haiyu Shen,Guoguo Zhi,Baojie Li,Qian Yu
Background Dry eye disease (DED) is a multifactorial ocular condition marked by tear film instability, inflammation, and oxidative stress. Current therapies, including artificial tears and immunosuppressants, offer limited long-term benefit and potential side effects. Natural flavonoids such as luteolin possess anti-inflammatory and antioxidant properties, yet their therapeutic potential in DED remains underexplored. Purpose This study aimed to evaluate the therapeutic efficacy and mechanisms of luteolin in experimental DED. Methods Flavonoids were initially screened using lipopolysaccharide-stimulated RAW264.7 macrophages. A benzalkonium chloride-induced DED mouse model was treated with topical luteolin or cyclosporine A. Ocular surface evaluations included tear secretion, corneal fluorescein staining, and goblet cell density. Inflammatory and oxidative markers were examined via histology, immunofluorescence, and qPCR. RNA sequencing and network pharmacology were used to identify target pathways. In vitro studies with RAW264.7 cells and hyperosmolarity-stressed human corneal epithelial cells further validated mechanism-specific effects. Target engagement was further validated using pathway-specific pharmacological inhibitors. Ocular safety and pharmacokinetics were also assessed. Results Luteolin showed superior anti-inflammatory activity among tested flavonoids. It improved tear production, reduced epithelial damage, and preserved goblet cells. Mechanistically, it modulated macrophage-driven inflammation through JAK-STAT signaling and mitigated oxidative epithelial damage by suppressing the MAPK pathway. Transcriptomic and pharmacological analyses confirmed its dual immunomodulatory and cytoprotective roles. Combined STAT1/3 and MAPK inhibition mimicked its therapeutic effects. Topical luteolin was well-tolerated and achieved corneal bioavailability. Conclusions Luteolin provides a dual protective effect in DED by targeting inflammation and oxidative stress, supporting its development as a safe and effective disease-modifying therapy.
研究领域:
眼科
·
免疫学
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分子生物学
·
药理学
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炎症性疾病
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氧化应激
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信号转导
·
转化医学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2025
·
IF 9.8
Yafeng Jin,Fangming Han,Didi Tong,Xinyue Song,Di Wang,Tao Wang,Xiangquan Qin,Na Chen,Xiaobo Li,Guangri Xu
High-performance electrode materials are crucial for electrochemical sensing of bioactive food compounds. We report an eco-friendly synthesis of coral-like cobalt/nitrogen-doped porous carbon (Co/N-PC) via hydrothermal-pyrolysis, integrated with MnO₂ to construct a Co/N-PC@MnO₂/GCE sensor for ultrasensitive luteolin (LU) detection. Synergy between the conductive Co/N-PC framework (electron transport) and MnO₂ nanoparticles (Mn 2+ /Mn 3+ /Mn 4+ catalysis) delivers exceptional performance: dual linear ranges (0.01–1 μM; 1–100 μM) and a record-low 4 nM detection limit. Kinetic studies confirm the apparent electron transfer number (n app = 4) arises from MnO₂ mediation. The sensor demonstrated high practicality in complex floral teas (honeysuckle, chrysanthemum), achieving 77.2–103.6 % recoveries. This work provides both a sensitive, green LU detection method and elucidates a MnO₂ catalytic cycle mechanism, revealing new insights into LU's electrochemical pathway.
研究领域:
分析化学
·
食品科学
·
电化学
·
生物传感
·
材料科学
·
天然产物分析
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Carbohydrate Polymer Technologies and Applications
·
2025
·
IF 6.5
Mubarak G. Bello,Shiyu Huang,Zifan Qiao,Zhenhua Chen,Lihua Chen
Luteolin (LT), a biologically active flavonoid with potent anti-inflammatory properties, faces significant limitations due to its instability, poor absorption, and low bioavailability. To overcome these challenges, this study explores the encapsulation of LT within nanosheet and cubic γ-cyclodextrin-based metal-organic frameworks (N-MOF and CD-MOF). This approach achieved a two-fold improvement in LT loading efficiency compared to previously reported methods. A critical finding was the identification of pH as a key factor in optimizing the loading process, which significantly enhanced encapsulation efficiency. The resulting LT/N-MOF and LT/CD-MOF formulations demonstrated improved photo-stability and thermal stability, alongside significantly enhanced cellular permeation. In vitro studies revealed remarkable anti-inflammatory properties of these formulations. Moreover, the bioavailability of LT was increased by 6-fold compared to pure luteolin. In a rat paw edema model, the optimized LT/CD-MOF and LT/N-MOF formulations exhibited 4.86- and 5.4-fold improvements in anti-inflammatory activity, respectively, over pure luteolin. These results underscore the potential of CD-MOFs as effective delivery systems for enhancing the therapeutic efficacy of luteolin.
研究领域:
药剂学
·
材料科学
·
炎症研究
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2018
·Vol. 19
·期 2
·447
·
IF 3.687
Ze-Qun Jiang,Mu-Han Li,Yue-Mu Qin,Hai-Ying Jiang,Xu Zhang,Mian-Hua Wu
Luteolin (LTL) exerts remarkable tumor suppressive activity on various types of cancers, including non-small cell lung cancer (NSCLC). However, it is not completely understood whether the mechanism of its action against NSCLC is related to microRNAs (miRNAs). In the present study, we investigated the anti-tumor effects of LTL on NSCLC in vitro and in vivo. The results revealed that LTL could inhibit cell proliferation and induce apoptosis in both A549 and H460 cells. In a H460 xenograft tumor model of nude mice, LTL significantly suppressed tumor growth, inhibited cell proliferation, and induced apoptosis. miRNA microarray and quantitative PCR (qPCR) analysis indicated that miR-34a-5p was dramatically upregulated upon LTL treatment in tumor tissues. Furthermore, MDM4 was proved to be a direct target of miR-34a-5p by luciferase reporter gene assay. LTL treatment was associated with increased p53 and p21 protein expressions and decreased MDM4 protein expression in both NSCLC cells and tumor tissues. When miR-34a-5p was inhibited in vitro, the protein expressions of Bcl-2 and MDM4 were recovered, while that of p53, p21, and Bax were attenuated. Moreover, caspase-3 and caspase-9 activation induced by LHL treatment in vitro were also suppressed by miR-34a-5p inhibition. Overall, LTL could inhibit tumorigenesis and induce apoptosis of NSCLC cells by upregulation of miR-34a-5p via targeting MDM4. These findings provide novel insight into the molecular functions of LTL that suggest its potential as a therapeutic agent for human NSCLC.Keywords:luteolin;apoptosis;non-small cell lung cancer;microRNA-34a-5p
研究领域:
肿瘤学
·
分子生物学
·
药理学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2020
·Vol. 11
·期 11
·10033-10046
·
IF 4.171
Xiaodong Ge,Chang'e Wang,Huiling Chen,Tingting Liu,Ligen Chen,Ying Huang,Feng Zeng,Bin Liu
Luteolin (LU) is a flavonoid compound and metformin hydrochloride (MH) is a kind of drug. Studies have shown that both LU and MH have the function of hypoglycemic effect. However, there are few reports indicating that LU cooperated with MH (LU·MH) can relieve lipid metabolism disorders and optimize intestinal flora compositions of high-fat diet mice. In this research, we investigated the effects of LU, MH and LU·MH on lipid metabolism disorders and intestinal flora composition in high-fat diet mice. The study found that compared with high-fat diet (HFD) alone, LU, MH and LU·MH could significantly reduce the lipid metabolism disorder. Furthermore, compared with LU or MH alone, the biochemical indicators of LU·MH were significantly improved and the results of the histopathological section also showed that LU·MH has stronger liver repair ability. It revealed that the potential mechanisms of the LU·MH alleviating lipid metabolism disorders were involved in the simultaneous regulation of SREBP-1c/FAS and SREBP-1c/ACC/Cpt-1. In addition, LU·MH could regulate the intestinal flora compositions. This includes significantly reducing the ratio of Firmicutes and Bacteroidetes(F/B) and at the family level, increasing the relative abundance of Lachnospiraceae, Helicobacteraceae, Marinifilaceae and Peptococcaceae to relieve lipid metabolism disorders. In conclusion, the work found that LU·MH regulates the signal pathway of SREBP-1c/FAS and SREBP-1c/ACC/Cpt-1 simultaneously and decreases the ratio of F/B, as well as increases the relative abundance of certain microbiota to alleviate the lipid metabolism disorders of HFD-fed mice.
研究领域:
药理学
·
营养学
·
微生物学
·
代谢性疾病
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY A
·
2019
·
IF 3.858
Nan Li,Jing Qiu,Huiying Liu,Zhijun Chen,Yongzhong Qian
Oligo(ethylene glycol)-based thermoresponsive polymers with Wulff-type boronate affinity were anchored on magnetic nanoparticles . The resultant magnetic nanoparticles were used as sorbents for extracting luteolin, a cis -diol-containing model analyte. By exploiting the thermoresponsive properties and Wulff-type boronate affinity of the sorbents, target adsorption at room temperature (25 °C) and target release at high temperature (40 °C) were achieved under neutral conditions without pH alteration. The proposed thermoregulated extraction method was favorable for automated boronate affinity extraction, preventing degradation of the target and avoiding acidic elution for breaking Wulff-type boronate sites. Compared to reported sorbents for extracting luteolin, the sorbents possessed higher maximum adsorption capacity (98.7 mg g −1 ) with acceptable sensitivity, simplified operation procedure, and mild extraction condition. Furthermore, the sorbents were applied in thermoregulated extraction of luteolin from honey samples. Satisfactory recoveries in the range of 83.2% ˗ 89.1% with RSD ranging from 2.2% to 4.6% were achieved. The results demonstrated that this work provided a new research direction to design and synthesize efficient thermoresponsive materials for recognition and release of cis -diol compounds under neutral conditions.
研究领域:
分析化学
·
材料科学
·
纳米技术
·
药学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2023
·Vol. 103
·期 13
·6440-6451
·
IF 4.1
Haiyun Yang,Zhiqing Peng,Liuming Xie,Jianhua Xie,Zhibing Huang
BACKGROUND Chinese yam fermented by Monascus , namely red mold dioscorea (RMD), has the potential of treating diseases. However, the production of citrinin limits the application of RMD. In the present study, the fermentation process of Monascus was optimized by adding genistein or luteolin to reduce citrinin yield. RESULTS The results showed that citrinin in 25 g of Huai Shan yam was reduced by 48% and 72% without affecting the pigment yield by adding 0.2 g of luteolin or genistein, respectively, to a 250-mL conical flask after fermentation for 18 days at 28 °C, whereas the addition of luteolin increased the content of yellow pigment by 1.3-fold. Under optimal conditions, citrinin in 20 g of iron bar yam decreased by 55% and 74% after adding 0.2 g of luteolin or genistein. Luteolin also increased yellow pigment content by 1.2-fold. Ultra HPLC coupled to quadrupole time-of-flight mass spectrometry was used for the preliminary analysis of Monascus fermentation products. It was found that the amino acid types in RMD are similar to those in yams, but there are fewer polysaccharides and fatty acids. CONCLUSION The results obtained in the present study showed that the addition of genistein or luteolin could reduce citrinin on the premise of increasing pigment yield, which laid a foundation for the better use of yams in Monascus fermentation. © 2023 Society of Chemical Industry.
研究领域:
食品科学
·
微生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2016
·
IF 3.994
Jinli Li,Xudong Cheng,Yan Chen,Weiming He,Li Ni,Peihua Xiong,Minggang Wei
Luteolin (LUT) is an active agent in cancer prevention and a potential candidate for clinical chemotherapy. However, poor water solubility and extensive excretion have limited the clinical use of luteolin. Herein, we attempted to develop vitamin E d-α-tocopherol acid polyethylene glycol 1000 succinate (TPGS) coated liposomes to improve the accumulation of luteolin in lung cancer. Luteolin or coumarin-6 loaded liposomes were prepared using film-dispersion methods and characterized according to their particle size, polydispersity, zeta potential , and drug encapsulation efficiency. Cellular uptake properties and cytotoxicities of luteolin or coumarin-6 loaded liposomes were determined in A549 cells. Optical in vivo imaging was employed as a method of assessing tumor targeting. The antitumor effect was evaluated in mice xenotransplanted with A549 cancer cells. The results showed that TPGS coated liposomes are spherical, and are ∼176.2 nm in size. TPGS coated liposomes enhanced cellular uptake and apoptosis by upregulating the Bax/Bcl-2 ratio, resulting in improved cytotoxicity in A549 cells. TPGS coated liposomes significantly accumulated in tumor tissue and enhanced tumor inhibition without altering the structures of other organs. Thereby, TPGS coated liposomes provide an effective strategy in cancer chemotherapy for model drugs with poor water solubility such as luteolin.
研究领域:
药剂学
·
肿瘤学
·
药物递送系统
·
纳米技术
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产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2017
·Vol. 41
·期 9
·3308-3319
·
IF 3.269
Qiang Jia,Yinxian Peng,Jianming Pan,Xiaobin Huang,Xiangheng Niu,Tao Zhang
Magnetic microspheres (Fe3O4@PVIM@Zn(II)) composed of a high magnetic-response Fe3O4 core and a Zn(II)-immobilized cross-linked polyvinyl imidazole (PVIM) shell via reflux-precipitation polymerization and metal-ion affinity strategy were fabricated. Integrating the advantages of specific uptake and fast separation, Fe3O4@PVIM@Zn(II) was adopted as an ideal pathway for luteolin (LTL) recognition. As-prepared Fe3O4@PVIM@Zn(II) possessed core–shell structure, uniform size (200 nm), high magnetic responsiveness (32.6 emu g−1), and a very easy synthesis process. X-ray photoelectron spectroscopy (XPS) suggested a strong interaction between the nitrogen heterocyclic ring of PVIM and Zn(II), which produced abundant binding sites for LTL. The batch mode experiments can be well described by pseudo-first-order kinetic models and a Langmuir isotherm. A rapid binding equilibrium (within 45 min) and large monolayer adsorption capacity (23.92 mg g−1) at 298 K were also observed. In addition, Fe3O4@PVIM@Zn(II) displayed remarkable selectivity to LTL; the purification process using Fe3O4@PVIM@Zn(II) can make purified LTL from approximately 85% to 94.26%. The antibacterial activity of purified LTL was outstanding by means of a Staphylococcus aureus (ATCC29213) resistance experiment. Considering its multiple merits, Fe3O4@PVIM@Zn(II) exhibited great potential for specific binding with natural products, such as flavonoids.
研究领域:
材料科学
·
生物化学
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产品关联
DOI
高影响因子
CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
·
2022
·
IF 1.193
Cong-Jie PAN,Tian-Tian CHEN,Long-Fei MA,Xue-Zhen QIN,Qiao-Qiao WEN,Su-Xiang FENG
Luteolin has gained extensive attention in pharmaceutical and clinical fields owing to their beneficial effects for human health. Accurate detection of luteolin is quite important for drug quality control and clinical medicine research. In this work, novel water dispersible fluorescent silicon nanoparticles (SiNPs) were prepared via one-pot hydrothermal approach by using (3-aminopropyl)trimethoxysilane (APTMS) as silicon source and D -penicillamine as reducing agent. The synthesized SiNPs emitted bright blue fluorescence with a high quantum yield of 44.78% and displayed outstanding optical properties and excellent stability. The fluorescence of the SiNPs could be distinctly quenched by luteolin through inner filter effect (IFE). Based on this, a novel fluorescent method for luteolin detection was developed by using the SiNPs as probe. A linear relationship between the fluorescence quenching efficiency and the concentration of luteolin was obtained from 1 to 100 µM with a limit of detection (LOD) of 0.24 µM. The proposed method was successfully applied to detect luteolin in urine samples.
研究领域:
分析化学
·
药物分析
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 4
·1-10
·
IF 4.026
Liu Xia,Zhang Mengying,Tian Yuxin,Liu Ruijia,Wang Yunfei,Guo Feifei,Gong Yanling,Yan Meixing
Luteolin (Lu) is a kind of flavonoid that has been proved to treat non-alcoholic fatty liver disease by alleviating intestinal microbiota disorder. In this study, luteolin was coated with methoxy poly(ethylene glycol)–poly(dl-lactide-co-glycolic acid) (mPEG-PLGA) using an emulsion solvent evaporation method, and the optimum preparation process was determined by a single-factor experiment combined with response surface methodology (RSM). Methacrylic acid-methyl methacrylate (1:2) copolymer (Eudragit S100) was then used to coat the surface of Lu/mPEG-PLGA nanoparticles. The physical parameters of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles (Lu-NPs), such as appearance, particle size, potential, particle size distribution and drug release, and stability in vitro, were evaluated. In addition, its cytotoxicity in vitro , pharmacokinetics, tissue distribution, and toxicity in vivo were also studied. The results showed that the prepared Lu-NPs had uniform particle size distribution, high encapsulation efficiency, and good stability. Normal colonic epithelial cells showed good tolerance to Lu-NPs. After oral administration, the blood concentration of luteolin peaked at 8 h, and the main tissue distribution was within the colon, confirming its colon-targeted profile. Safety assessments also indicated that no significant changes were observed in main organs after administration of Lu-NPs. The use of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles is a new strategy for colon-targeted delivery of luteolin that encourages luteolin to fulfill its role in the colon. Graphical abstract
研究领域:
药学
·
纳米技术
·
药物递送系统
·
药理学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF NUTRITIONAL BIOCHEMISTRY
·
2022
·
IF 6.117
Lingli Zhao,Mengfei Zheng,Hao Cai,Juan Chen,Yan Lin,Fangbin Wang,Lu Wang,Xian Zhang,Jian Liu
Mitochondrial reactive oxygen species (ROS)generation plays an essential role in the process of adipocyte differentiation and is involved in the development of obesity and associated metabolic diseases . Various dietary flavonoids possess the substantial anti-adipogenic activity. However, it is unclear whether these flavonoids inhibit adipocyte differentiation by reducing ROS generation. In this study, the effects of six common dietary flavonoids on adipocyte differentiation were assessed in 3T3-L1 cells. The flavonoids with the same backbone of 5,7-dihydroxylflavone, including flavones apigenin , chrysin , luteolin and flavonols kaempferol , myricetin , quercetin , dose-dependently inhibited 3T3-L1 adipocyte differentiation, suggesting an associated hierarchy of inhibitory capability: luteolin > quercetin > myricetin > apigenin/kaempferol > chrysin. Meanwhile, six flavonoids were found to inhibit adipogenic gene expression and the early stage of adipocyte differentiation. Among the tested flavonoids, luteolin significantly reduced both intracellular and mitochondrial ROS generation during adipocyte differentiation. Further, luteolin treatment depressed the elevation of H 2 O 2 concentration in the early stage of 3T3-L1 differentiation and reversed the facilitated effects of exogenous H 2 O 2 on 3T3-L1 adipocyte differentiation and ROS generation. Altogether, the activity comparison of six dietary flavonoids identifies that luteolin inhibits 3T3-L1 adipocyte differentiation through reducing ROS generation, elucidating a new mechanism underlying the anti-adipogenic actions of flavonoids.
研究领域:
药理学
·
细胞生物学
·
营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）