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luteolin
LANGMUIR · 2024 · IF 3.7

Luteolin Functionalized Zinc Oxide Nanoparticles for Cancer Therapy Based on Autophagy Activation and EMT Inhibition

Yan Gao,Jinwen Zhu,Xingye Zheng,Guanghui Lin,Peng Miao

Natural bioactive compounds have become increasingly important antitumor and antimicrobial agents due to their high therapeutic potential and low systemic toxicity. However, they also have significant drawbacks like nontumor targeting and low bioavailability, which limit their wide therapeutic applications. There is an urgent need for a safe and compatible nanoparticle-mediated drug delivery system for the efficient transport of drug candidates into tumor tissues. In this paper, amine-modified zinc oxide nanoparticles are synthesized to load luteolin. The functionalized nanoparticles exhibit good synergistic effects in terms of antitumor and antibacterial activities. They show significant induction of oxidative stress and antitumor effects, while no significant inhibitory effect on normal cells is observed, suggesting that the nanocomposites have good targeting of cancer cells. Autophagy activation and EMT inhibition effects are studied to explain the good antitumor performances. The prepared nanocomposites are demonstrated to be attractive candidates for cancer therapy.

CAS / MDL: 67-68-5
研究领域: 纳米医学 · 肿瘤学 · 药理学
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BIOORGANIC CHEMISTRY · 2024 · IF 4.5

Phenylboronic acid-functionalized copper nanoclusters with sensitivity and selectivity for the ratiometric detection of luteolin

Xingyu Hou,He Zuo,Na Sun,Yongqiang Wang,Rui Jia,Yuguang Lv,Lixin Ding

A desirable ratiometric fluorescent probe was designed by using 3-carboxyphenylboronic acid functionalized polyethyleneimine ethoxylated modified copper nanoclusters (CPBA@PEI-CuNCs) for detecting luteolin (LTL, cis -diols structure) with sensitivity and selectivity. Characterization techniques were carried out with the TEM, PSD, FT-IR, XPS and XRD, confirming its successful formation with a quantum yield of 40.49 %. As the optimal excitation wavelength at 386 nm, the fluorescence intensity was detected by fluorophotometer. Meanwhile, the nanoprobe has two emission wavelengths 396 and 473 nm. According to the fluorescence quenching intensity ratio (F 473 /F 396 ), the LOD reached as low as 1.22 nM within the range from 0.11 to 600 μM. The CPBA@PEI-CuNCs exhibited pH-controlled, covalent, and reversible binding properties. Using PEI capped by CuNCs, cytotoxicity is reduced for potential treatment purposes. Additionally, the developed probe was used for LTL detection, HepG2 cell imaging and pH-responsive drug delivery in real samples with carrot leaves, peanut shells, and perilla leaves samples. CPBA@PEI-CuNCs demonstrated repeatability and reproducibility, making it a cost-effective and practical tool for fluorescence analysis in detection.

研究领域: 分析化学 · 生物医学工程 · 材料科学
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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2024 · IF 2.6

Inhibitory activity of luteolin on α-glucosidase and pancreatic lipase in vitro and in vivo

Hai-Xia Xu,Qiao-Ting Xu,Zhong-Ping Yin,Ji-Guang Chen,Qing-Feng Zhang

Summary Obesity is becoming a top global health problem. Inhibition of digestive enzymes is an effective approach in weight management due to the reduction of energy absorption. In this study, the inhibitory effects of luteolin on α-glucosidase and pancreatic lipase were investigated in vitro and in vivo via enzyme kinetics, fluorescence quenching, molecular docking and rat experiments. The results showed that luteolin inhibited α-glucosidase and pancreatic lipase in a mixed-type and uncompetitive manner with IC 50 values of 29.31 and 42.74 μg mL −1 respectively. The binding of luteolin with the two enzymes caused the quenching of intrinsic fluorescence of protein. Molecular docking simulation revealed that luteolin could be located in the active pocket of α-glucosidase and interact with the key amino acid residues. Moreover, a hydrophobic interaction and a van der Waals force were formed between luteolin and the key amino acid residues of pancreatic lipase (His264 and Ser153). In vivo studies further confirmed that luteolin could significantly decrease the absorption of glucose and triacylglyceride in rats by inhibiting α-glucosidase and pancreatic lipase.

研究领域: 药理学 · 营养学 · 生物化学 · 分子生物学
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Heliyon · 2024 · IF 3.4

Improved anti-cancer effects of luteolin@ZIF-8 in cervical and prostate cancer cell lines

Linlin Ding,Hao Chen,Guoli Bi,Wenqi Wang,Rui Li

Luteolin, a naturally occurring pharmaceutical compound with significant antitumor properties, faces challenges in clinical applications due to its low solubility in water and limited bioavailability. To address these issues, a one-step synthesis method was employed to encapsulate luteolin within ZIF-8. The successful preparation of luteolin@ ZIF-8 nanoparticles was confirmed through various analytical techniques, including fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), laser size distribution analysis, X-ray diffraction (XRD), and release curve assessment. Results indicate that the formulated luteolin@ ZIF-8 nanoparticles exhibited high drug loading (1360 mg/g) and demonstrated selective drug release in acidic microenvironments. Furthermore, the encapsulation of luteolin increased the size of ZIF-8 from 168.4 ± 0.2 nm to 384.7 ± 1.4 nm, but did not change its crystalline structure significantly. Notably, the results of in vitro anti-cervical and prostate cancers experiments revealed that luteolin@ ZIF-8 had better efficacy in inhibiting the proliferation and migration of HeLa and PC3 cells than free luteolin. The antitumor activity of luteolin@ ZIF-8 was sustained for 72 h, with a particularly pronounced inhibitory effect on HeLa cells as compared to PC3 cells. This study underscores the effective enhancement of luteolin's antitumor activity through encapsulation in ZIF-8, offering substantial implications for improving its clinical applications.

CAS / MDL: 9005-65-6 7664-38-2
研究领域: 药学 · 纳米技术 · 肿瘤学
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FOOD RESEARCH INTERNATIONAL · 2026 · IF 8.8

Chitosan composite packaging film loaded with luteolin-superoxide dismutase nano-micelles: Enhancing food preservation performance

Pei Wu,Yilin Che,Rui Zhou,Yixin Tang,Lei Guo,Baiqiao Chen,Xinran Yan,Shanli Wu,Chang Liu,Mujie Kan,Jizhou Zhang,Xi Yang,Xin Jiang,Zhanxin Wang,Erlei Wang,Tianhao Yan,Caina Xu

Novel chitosan-based composite film with Luteolin-SOD nano-micelles via nano-encapsulation for food preservation. • This composite film outperforms conventional packaging: superior inhibition of oxidation, delays spoilage, biodegradable. • Natural-ingredient film: promising substitute for traditional packaging, meeting eco-friendly and sustainable demands. Chitosan-based films are promising alternatives to petroleum-based food packaging materials but suffer from insufficient mechanical strength, poor water resistance, and limited antioxidant capacity. To address these issues, we synthesized chitosan-based nano-polymers loaded with luteolin (Lut) and superoxide dismutase (SOD) (CLS nano-micelles). We then incorporated these nano-micelles into a chitosan-based film to produce a CLS film. The results showed that, compared with the pure chitosan film, the mechanical properties of CLS film significantly improved, with tensile strength increasing from 6.14 MPa to 37.50 MPa and elongation at break increasing from 17.4% to 34.6%. The barrier properties of the CLS film were also enhanced, as both water vapor permeability and solubility decreased. Notably, the CLS film also exhibited excellent antioxidant properties (with DPPH inhibition rates increasing from 4.4% to 48.3% and ABTS inhibition rates rising from 7.2% to 74.6%) and demonstrated potent antibacterial activity against E. coli , S. aureus , and B. subtilis . It also exhibited excellent biocompatibility and demonstrated favorable biodegradability in soil. Grape preservation assays further confirmed its efficacy in maintaining fruit freshness. These results demonstrate that integrating CLS nano-micelles into a chitosan matrix significantly improves its mechanical, barrier, antioxidant, and antibacterial properties. This makes the CLS film a promising eco-friendly alternative for sustainable food packaging applications, offering an efficient and environmentally friendly solution. Download: Download high-res image (125KB) Download: Download full-size image

✓ 已验证 DOI PubMed 高影响因子
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ULTRASONICS SONOCHEMISTRY · 2025 · IF 9.7

Ultrasonic-Assisted extraction of luteolin from peanut shells using supramolecular solvents and its molecular mechanism

Yuhan Fang,Ping Zhang,Shuang Wang,Lulu Li,Zunlai Sheng

This study innovatively employs ultrasound-assisted extraction (UAE) in conjunction with supramolecular solvents (SUPRAS) for the extraction of luteolin from peanut shells, while also investigating the potential mechanism underlying this extraction process. Initially, the formation mechanism of SUPRAS was characterized using Fourier-transform infrared spectroscopy (FTIR). Based on the results of single-factor experiments, the extraction process was optimized using response surface methodology (RSM), resulting in the determination of optimal conditions: an ultrasound temperature of 67 °C, a SUPRAS/equilibrium solution (EqS) volume ratio of 5:1, and a solid-to-liquid ratio of 1:36 g/mL. Under these conditions, the maximum luteolin yield reached 1.645 mg/g. Furthermore, through independent gradient model (IGMH) calculations, molecular orbital theory, interaction energy analysis, and molecular dynamics simulations, it was revealed that the predominant interaction force between the supramolecular solvent and the target compound is hydrogen bonding. Notably, this study also compares the SUPRAS-UAE extraction method with the traditional extraction in terms of efficiency, economic costs, and environmental impact. The results indicate that the SUPRAS-UAE technique demonstrates significant advantages in terms of its green and high-efficiency characteristics. It provides a new sustainable strategy for the efficient recovery of natural active ingredients in chemical engineering and related fields.

研究领域: 化学工程 · 天然产物化学 · 绿色化学 · 分子模拟
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SEPARATION AND PURIFICATION TECHNOLOGY · 2025 · IF 9

Covalent organic frameworks-based microspheres with precisely designed recognition sites for selective adsorption of luteolin

Na Su,Hongxiang Ou,Shucheng Liu,Fang Zhu,Honglai Xue,Xuan Zhang

Global agricultural activities generate substantial flavonoid-rich waste streams, which presents both resource recovery opportunities and environmental challenges. The selective separation of high-value luteolin (LTL) from such complex matrices remains difficult due to structural similarities among flavonoids. Covalent organic frameworks (COFs) are promising separation materials due to their tunable structures and functionalities. However, COFs face limitations in accurately recognizing LTL within complex environmental matrices. Key issues include insufficient specific binding sites and low functionalization density. To overcome these challenges, we developed molecularly imprinted COFs microspheres (COFs-DVA-SH MIPMCs) through a novel emulsion-based synthesis and post-modification strategy. This approach involved constructing hollow vinyl-functionalized COFs microspheres via emulsion polymerization, followed by dithiol linker grafting through thiol-ene click reaction, and culminating in boronic acid affinity site imprinting. This yielded COFs microspheres with precise recognition capabilities. The COFs-DVA-SH MIPMCs combine boronate affinity with molecular imprinting advantages to enable selective LTL extraction. They demonstrate significant recognition capacity (67.97 mg g −1 ), rapid mass transfer (180 min), and high selectivity ( IF  = 2.89) under alkaline conditions. The adsorbent also exhibits excellent stability, maintaining 93.7 % capacity after 5 cycles and robust thermal stability. This work provides a new strategy for specific separation of natural flavonoids using COFs, supporting sustainable valorization of agricultural waste through advanced separation technologies.

研究领域: 分析化学 · 材料科学 · 环境科学 · 天然产物化学 · 分离科学
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JOURNAL OF NANOBIOTECHNOLOGY · 2025 ·Vol. 23 ·期 1 ·1-17 · IF 12.6

Quadruple synergistic amplification of ferroptosis for precision glioblastoma therapy: a luteolin-coordinated ferric ion nanoplatform

Liu Suyi,Sun Kunhui,Li Mengnan,Liu Xinyue,Wang Ping,Li Meifang,Peng Bo,Wang Bing,Chang Yan-xu,Yu Xie-an

Ferroptosis is emerging as a promising therapeutic strategy for glioblastoma (GBM). However, insufficient lipid peroxidation levels and blood-brain barrier (BBB) pose a significant challenge for GBM treatment. Here, we present natural product luteolin (Lut)-coordinated Fe3+ nanoparticles loaded with dihydroartemisinin (DHA), designated as FLD NPs, which can cross the BBB and induce quadruple amplified ferroptosis. Specifically, FLD NPs leverage four mechanisms to enhance ferroptosis: (1) Lut upregulates heme oxygenase 1 (HO-1), promoting heme degradation and recruiting endogenous Fe2+. (2) exogenous Fe3+ depletes glutathione (GSH), increasing Fe2+ levels and catalyzing H2O2 to generate ·OH via the Fenton reaction; (3) Fe2+ facilitates the cleavage of DHA’s peroxide bridge, further elevating ·OH production; and (4) Lut-coordinated Fe3+ acts as a photothermal agent, accelerating the Fenton reaction under light irradiation. Furthermore, FLD NPs enable multimodal imaging capabilities, including photoacoustic and photothermal imaging, for precise tumor targeting. It demonstrates satisfactory antitumor efficacy in GBM models, highlighting its potential as a novel ferroptosis-amplifying nanotherapeutic. Importantly, this study reveals that Lut modulates tight junction protein expression in vascular endothelial cells, facilitating BBB penetration. This work highlights a novel strategy for GBM therapy, leveraging natural product-mediated nanoparticles to amplify ferroptosis.

研究领域: 肿瘤学 · 神经肿瘤学 · 纳米医学 · 分子生物学 · 药理学 · 转化医学 · 生物材料
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ULTRASONICS SONOCHEMISTRY · 2025 · IF 9.7

Ultrasonic-assisted extraction of luteolin from peanut shells using ionic liquid and its molecular mechanism

Liwei Niu,Siwen Zhang,Xiaoyu Si,Yuhan Fang,Shuang Wang,Lulu Li,Zunlai Sheng

This study investigates the potential of ionic liquids (ILs) as sustainable solvents in ultrasonic-assisted extraction (UAE) to efficiently recover luteolin from peanut shells. Among the range of ILs tested, 1-butyl-3-methylimidazolium tetrafluoroborate stood out as the most effective solvent, achieving the highest extraction yield. Single-factor experiments were conducted to analyze the effects of ultrasonic power, extraction time, extraction temperature, IL concentration, and solid-to-liquid ratio on extraction efficiency. Further optimization of the extraction conditions was performed using response surface methodology and neural network analysis, resulting in a significantly enhanced luteolin yield of 3.71 ± 0.06 mg/g. Interaction energy analyses were conducted to elucidate the interactions between ILs and luteolin, confirming the experimental findings and highlighting the strongest interaction energy between 1-butyl-3-methylimidazolium tetrafluoroborate and luteolin. A kinetic model for luteolin extraction was developed, demonstrating that the extraction process follows a second-order rate model, where the extraction rate is directly proportional to the square of the concentration difference between luteolin and the solvent. The outcomes of this research present an efficient protocol for luteolin extraction and provide novel insights into the application of UAE in extracting natural products.

研究领域: 植物化学 · 天然产物开发 · 药用植物学
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npj Science of Food · 2025 ·Vol. 9 ·期 1 ·234 · IF 7.8

Luteolin protects against alcoholic liver injury by restoring NRF2 stability to suppress ACSS2 nuclear accumulation

Cao Lixue,Lei Qi,Dong Yujia,Meng Chuyang,Qi Qianqian,Li Lisi,Liu Hongwei,Liu Xifu,Wang Meng

Alcohol abuse results in alcoholic liver disease which are associated with high morbidity and mortality worldwide. Whereas luteolin has shown potential hepatoprotective effects on ethanol-induced liver damage and the underlying mechanism remains unclear. In this study, a chronic plus a single binge ethanol feeding mouse model was employed to mimic acute-on-chronic alcoholic liver injury in humans, and the primary hepatocytes were isolated for the mechanism investigation. Our study demonstrated that luteolin protects against ethanol-induced liver injury by restoring NRF2 stability, thereby blocking the nuclear accumulation of ACSS2 and histone H3 acetylation. This subsequently led to reduced hepatic lipogenesis, and ultimately ameliorated alcoholic liver damage. Our findings elucidate the protective mechanism of luteolin in alcoholic liver injury and provide a new therapeutic strategy for the treatment of alcoholic liver disease.

CAS / MDL: 491-70-3
研究领域: 肝脏病学 · 分子生物学 · 药理学 · 营养生物化学
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Open Medicine · 2025 ·Vol. 20 ·期 1 ·20251198 · IF 1.6

Luteolin alleviates oxygen-glucose deprivation/reoxygenation-induced neuron injury by regulating NLRP3/IL-1β signaling

Fei Yu,Guangxue Wang,Xingyi Chen,Yanfei Zhang,Cheng Yang,Hui Hu,Liang Wei

We aimed to investigate the protective effect of luteolin against neuron injury induced by oxygen-glucose deprivation/reoxygenation (OGD/R), and to further elucidate the roles of NLRP3 in luteolin-mediated regulation of neuron injury. Using Schwann (SW) 10 cells, an OGD/R-induced neuron injury model was established, and six experimental groups were designated. Subsequently, cell viability and apoptosis were respectively detected by cell counting kit 8 and flow cytometry. Reactive oxygen species (ROS) levels were measured via flow cytometry with a ROS assay kit. Moreover, the expression of interleukin (IL)-6, IL-1β, NLRP3, and MMP9 was examined by real-time quantitative PCR and Western blot. Compared with control cells, OGD/R significantly reduced cell viability and increased apoptosis, ROS levels, and the mRNA levels of IL-6 , IL-1β , NLRP3 , and MMP9 . Luteolin significantly enhanced OGD/R-induced cell viability and alleviated apoptosis in SW10 cells ( P < 0.05). Additionally, luteolin suppressed ROS levels, along with the expression of IL-1β, IL-6, NLRP3, and MMP9 induced by OGD/R. Furthermore, BMS-986299 significantly decreased the cell viability and increased the expression of inflammatory factors in OGD/R-induced SW10 cells treated with luteolin. This inhibitory effect was reversed by NLRP3 knockdown. In conclusion, luteolin may exert a protective effect on OGD/R-induced nerve injury by inhibiting the NLRP3/IL-1β signaling pathway.

CAS / MDL: 7646-79-9
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Functional Foods · 2019 · IF 3.197

Luteolin shows antidepressant-like effect by inhibiting and downregulating plasma membrane monoamine transporter (PMAT, Slc29a4)

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.

CAS / MDL: 56296-78-7
研究领域: 药理学 · 神经科学 · 分子生物学
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