JOURNAL OF MOLECULAR LIQUIDS
·
2024
·
IF 5.3
Qian Zhang,Mingyuan Li,Cui Liu,Yutong Li,Yu Guo,Hanlu Jiang,Jie Liu,Min Hong
The antimicrobial, anticancer, and anti-SARS-CoV-2 activities of cepharanthine (CEP) combined with luteolin (Lut) were compared and analyzed by in vitro bioactivity experiment and molecular docking. CEP shows stronger biological activity than Lut, and their combination shows synergism without antagonism, especially in the fungal inhibition and anticancer activity experiments. It is believed that the antiviral activity is still effective confirmed by the simulation between two drugs and anti-SARS-CoV-2. Further, pepsin (Pep) was chosen for imitative gastroenteric environments to study its protease activity and structure effected by two drugs. The results show that the inhibitory mechanism of Lut/CEP is non-competitive inhibition, the binding mechanism is static quenching driven by enthalpy, the order of drug addition can affect the strength of binding ability, and the strength of binding ability is positively correlated with the inhibitory effect on enzyme activity. The ingestion of CEP before ingestion of Lut is more conducive to the efficient utilization of them. Their combination can not only decrease the dosage and toxicity, but also enhance the anti-inflammatory and anti-virus effects. These results can provide theoretical support for the development and utilization of Lut and CEP, and may supply one of the treatment for deal with the newly appeared viruses.
研究领域:
药理学
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分子生物学
·
病毒学
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产品关联
DOI
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Saif Ullah,Gang Hu,Mati Ur Rahman,Asif Hayat,Ata Ur Rehman,Ijaz Ullah,Akhlaq Ahmad,Waqar Uddin,Wen Ma,Zhaohui Fang,Muhammad Yasir Nawabi,Rooh Ullah,Jimei Song
The macrocyclic complex catalyzed Briggs-Rauscher (BR) oscillator was used to determine the antioxidants activity of natural polyphenolic compounds (tannic acid, chlorogenic acid, and luteolin) in this paper. The complex Ni catalyst is donated by NiL(ClO4)2 where the ligand L in the complex is 5,7,7,12,14,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-4,11-diene. The overall reaction pH was maintained at 2, which is similar to the pH of the human stomach. Experimental results have shown that as per addition of the above antioxidants into the BR system, the temporarily cessation of oscillation was noticed and inhibition time linearly depends on the concentration of antioxidants added. The evaluation of natural polyphenolic compound, antioxidants activity was tested successfully. The three natural polyphenolic compounds tested are tannic acid, chlorogenic acid, and luteolin. In these three natural compounds, the chlorogenic acid was found the most proficient antioxidant. The perturbation mechanism involving HOO● radical based on FCA model was suggested.
研究领域:
化学动力学
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生物化学
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产品关联
DOI
高影响因子
JOURNAL OF CHEMICAL RESEARCH
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2014
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IF 0.697
Ji Zhang,Man Liu,Wei Cui,Jian Yang,Bo Yang
Luteolin is a naturally-occurring polyphenolic flavonoid compound which has received considerable attention because of its wide range of biological and pharmacological properties. Efficient methods are reported for preparing luteolin, based on the acylation of 1,3,5-trimethoxybenzene and condensation with 3,4-dimethoxybenzaldehyde or the reaction of 3,4-dimethoxycinnamic acid with 1,3,5-trimethoxybenzene. The first of these is the better method.
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DOI
高影响因子
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH
·
2023
·
IF 2.3
Wang Yujin,Jiang Hua,Wang Lijun,Gan Huiping,Xiao Xinchun,Huang Liangwu,Li Wenxin,Li Zongrun
Functional constipation (FC) is one of the most common gastrointestinal disorders characterized by hard stools and infrequent bowel movements, which is associated with dysfunction of the enteric nervous system and intestinal motility. Luteolin, a naturally occurring flavone, was reported to possess potential pharmacological activities on intestinal inflammation and nerve injury. This study aimed to explore the role of luteolin and its functional mechanism in loperamide-induced FC mice. Our results showed that luteolin treatment reversed the reduction in defecation frequency, fecal water content, and intestinal transit ratio, and the elevation in transit time of FC models. Consistently, luteolin increased the thickness of the muscular layer and lessened colonic histopathological injury induced by loperamide. Furthermore, we revealed that luteolin treatment increased the expression of neuronal protein HuC/D and the levels of intestinal motility-related biomarkers, including substance P (SP), vasoactive intestinal polypeptide (VIP), and acetylcholine (ACh), as well as interstitial cells of Cajal (ICC) biomarker KIT proto-oncogene, receptor tyrosine kinase (C-Kit), and anoctamin-1 (ANO1), implying that luteolin mediated enhancement of colonic function and contributed to the anti-intestinal dysmotility against loperamide-induced FC. Additionally, luteolin decreased the upregulation of aquaporin (AQP)-3, AQP-4, and AQP-8 in the colon of FC mice. In summary, our data showed that luteolin might be an attractive option for developing FC-relieving medications.
研究领域:
药理学
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胃肠病学
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神经科学
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产品关联
DOI
PubMed
高影响因子
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
·
2022
·Vol. 92
·期 8
·1534-1538
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IF 0.779
Tao Yanzhi,Yu Xiang,Wu Sini,Nong Guangzai
Abstract Selenium is an essential trace element for human body. Flavonoids have been well characterized as antioxidant, antibacterial, anticancer, and immunomodulatory agents. Therefore, a luteolin–selenium complex has been synthesized from selenium dioxide and a flavonoid luteolin. Studies of the structure of the generated complex and mechanism of its formation have indicated that the generated complex contained two luteolin units and one selenium oxide group attached to the two sixth-position carbons of luteolin units. Conversion rate for the complex is determined to be 25.3% of the mass of luteolin, and the selenium content is 11.88% of the mass of the complex.
研究领域:
化学
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药理学
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营养学
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DOI
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2025
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IF 2.5
Miao Wang,Linlin Zhao,Yujiao Liu,Deyong Tian,Aijiao Jiang,Qianqi Cai,Yucheng Xiang,Lie Zhang,Yan Chen,Jing Ye,Aikebaier Reheman,Quan Zhang
Hyperuricemia, a prevalent metabolic disorder, severely impacts life quality. Luteolin (LUT), a natural flavonoid compound, demonstrates potential anti-hyperuricemic effects along with a high safety profile. However, its clinical application is greatly limited by poor oral bioavailability, mainly due to low permeability and inadequate gastrointestinal stability. To address this, we developed a chylomicron-mimicking supramolecular nanoemulsion (LUT-CMSN) composed of soybean oil and a supramolecular aggregate formed between LUT and Kolliphor® HS 15 (HS 15). LUT-CMSN exhibited a near-spherical morphology with an average particle size of approximately 14.2 nm. With CMSN encapsulation, LUT exhibited notably improved permeability and stability in the gastrointestinal tract. After oral administration, LUT-CMSN could be absorbed by lymphatic transport into blood circulation, consequently achieving 4.63-fold higher Cmax and 2.59-fold greater AUC(0–t) compared with free LUT. Additionally, LUT-CMSN showed markedly enhanced distribution in the liver and kidney relative to free LUT. In the acute and chronic hyperuricemia animal model, LUT-CMSN effectively reduced serum uric acid levels through inhibition of xanthine oxidase (XOD) activity and observably alleviated the renal injury induced by hyperuricemia. Taken together, LUT-CMSN represents a promising oral delivery platform for enhancing the bioavailability of LUT and a potential therapeutic strategy for the treatment of hyperuricemia.
研究领域:
药剂学
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纳米医学
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药物递送
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代谢性疾病
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药代动力学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2026
·
IF 5.4
Niu Niu,Ying Zhang,Dong Sun,Jialong Zhang,Chuqi Zhang,Xiumin Li,Weiliang Tian,Feng Gao
The interfacial state of electrode materials critically governs catalytic analyte detection. This study introduces single-atom platinum (Pt) decorated tungsten trioxide (Pt-WO 3 ) nanomaterials for the ultrasensitive electrochemical detection of luteolin, a pharmacologically significant flavonoid. The atomic dispersion of Pt within the WO 3 lattice, achieved via oxygen vacancy anchoring, optimizes the interfacial state and catalytic performance, overcoming Pt nanoparticle agglomeration limitations. The optimized Pt-WO 3 modified electrode demonstrates exceptional performance with an ultra-low detection limit (0.13 nM), superior sensitivity (10.1 μA μM −1 ), and a broad linear range (0.0001–5.6 μM). Systematic mechanistic studies reveal a two-electron/double-proton reaction pathway for luteolin oxidation, with Pt single atoms synergistically accelerating interfacial electron transfer. The sensor exhibits outstanding selectivity, long-term stability, and reproducibility. Successful application in detecting luteolin in complex matrices (apple juice, lemon juice) validates its practical utility. This work highlights the significant potential of single-atom synergistic catalysis in advancing electrochemical sensor performance for pharmaceutical analysis and functional food quality control.
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2013
·
IF 2.596
Jiakai Yan,Guowen Zhang,Junhui Pan,Yajie Wang
α-Glucosidase is a critical associated enzyme with type 2 diabetes mellitus in humans. Inhibition of α-glucosidase is important due to the potential effect of down regulating glucose absorption in patients. In this study, the inhibitory activity of flavone luteolin on α-glucosidase and their interaction mechanism were investigated by multispectroscopic methods along with molecular docking technique. It was found that luteolin reversibly inhibited α-glucosidase in a noncompetitive manner with an IC 50 value of (1.72 ± 0.05) × 10 −4 mol L −1 , and the inhibition followed a multi-phase kinetic process with a first-order reaction. Luteolin had a strong ability to quench the intrinsic fluorescence of α-glucosidase through a static quenching procedure. The positive values of enthalpy and entropy change suggested that the binding of luteolin to α-glucosidase was driven mainly by hydrophobic interactions, and the binding distance was estimated to be 4.56 nm. Analysis of synchronous fluorescence, circular dichroism, and Fourier transform infrared spectra demonstrated that the binding of luteolin to α-glucosidase induced rearrangement and conformational changes of the enzyme. Moreover, the results obtained from molecular docking indicated that luteolin had a high affinity close to the active site pocket of α-glucosidase and indirectly inhibited the catalytic activity of the enzyme.
研究领域:
生物化学
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分子生物学
·
酶学
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药物代谢
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糖尿病研究
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天然产物药理学
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DOI
高影响因子
MATERIALS CHEMISTRY AND PHYSICS
·
2026
·
IF 4.7
Sheng Lin,Yuting Wang,Chunxiang Huang,Yu Niu,Yongming Liu,Wangchuan Xiao,Fenghua Chen,Rongrong Xue
Co-amorphous systems, including co-amorphous and co-amorphous salts, can enhance the solubility of poorly water-soluble small molecules. It is important to identify them because co-amorphous and co-amorphous salts have different physicochemical properties. Co-amorphous system of luteolin (LUT, a well-known poorly soluble flavonoid) and amino acids at a molar ratio of 1:1 was prepared using neat ball milling. Only amorphous luteolin-arginine (LUT-Arg) and luteolin-lysine (LUT-Lys) exhibit significant solubility enhancements in the media of water and PBS. The Δ p K a rule suggests that LUT-Arg (Δ p K a , 2.8) and LUT-Lys (Δ p K a , 2.9) are close to co-amorphous salts. Diffuse reflectance spectroscopy and Raman spectroscopy confirmed that LUT-Arg and LUT-Lys are co-amorphous salts, while IR spectroscopy, the most common used method, cannot distinguish them. Comprehensive multiple characterizations (>2) are essential to confirm the formation of co-amorphous or co-amorphous salts, such as applying the Δ p K a rule, diffuse reflectance spectroscopy, and Raman spectroscopy for LUT-Arg and LUT-Lys.
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产品关联
DOI
高影响因子
Analytical Methods
·
2023
·Vol. 15
·期 7
·925-936
·
IF 3.1
Li-xin Ding,Yong-qiang Wang,Xue Sun,Zhao-qi Jiang,Xiao-yu Wang,Yan-fen Zhou,Xing-yu Hou
In this study, 3-carboxyphenylboronic acid (CP)-functionalized amino-modified Fe3O4 (Fe3O4@NH2-CP, FNC) magnetic molecularly imprinted polymers (FNC@MIPs) were synthesized and applied for the quick identification and selective separation of luteolin (LTL). The structure and morphology were characterized in detail by Fourier transform-infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), dynamic light scattering (DLS), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and vibrating specimen magnetometry (VSM) methods. The FNC@MIPs had a homogeneous shape, excellent magnetic characteristics, quick binding kinetics, a high adsorption capacity, acceptable selectivity, and stable reusability. The solid-phase extraction parameters and preparation conditions were both optimized. Under optimized conditions, the maximal adsorption capacity was 14.26 mg g−1 and the imprinting factor was 3.62. Furthermore, the experimental kinetics data were best fitted with the pseudo-first-order model (R2 = 0.9877), and the Langmuir model could describe the adsorption process (R2 = 0.9979), suggesting a monolayer covering. The practical application of the sorbent for LTL detection in Lonicera japonica Thunb samples showed recoveries in the range of 84.5–108.7%. Therefore, the strategy offers a fresh avenue for the extraction and purification of LTL.
研究领域:
分析化学
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材料科学
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植物化学
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产品关联
DOI
PubMed
高影响因子
AQUACULTURE
·
2024
·
IF 3.9
Guang-shuo Wang,Jia-cheng Qin,Yun-long Qin,Yao Wang,Bin Yang,Xiang Liu,Fei Ling,Gao-xue Wang
Largemouth bass virus (LMBV) poses a serious threat to commercial fish production, resulting in significant economic losses to the aquaculture industry. To date, no approved treatment for LMBV infection exists. In response to this urgent need, we conducted an investigation into the anti-LMBV activity of 15 natural compounds. Among these compounds, luteolin (LUT) was the most effective, with a remarkable inhibition rate of 97.27 % on LMBV replication. In vitro antiviral activity assays further demonstrated that LUT significantly inhibited LMBV replication in epithelioma papulosum cyprini (EPC) cells, and the half maximal inhibitory concentration (IC 50 ) was 2.77 μM. Additionally, viral titers and cytopathic effect (CPE) were reduced in the presence of LUT, suggesting its potential to protect infected cells. Mechanistically, LUT could directly affect LMBV particles and weaken their infectivity. Furthermore, LUT was effective in inhibiting LMBV adsorption to host cells and had preventive effects. In vivo studies revealed that LUT improved the survival rate of largemouth bass infected with LMBV. Real-time quantitative PCR (RT-qPCR) assays demonstrated that LUT significantly decreased viral loads in the liver, spleen, and kidney of largemouth bass at 1, 3, 5, and 7 days after infection. These findings suggest that LUT has the potential as a therapeutic agent to protect economically valuable fish from LMBV infection.
研究领域:
水产养殖
·
病毒学
·
药理学
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DOI
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
·
2025
·
IF 3.3
Zhixin Zhang,Linli Zhao,Jiahui Wang,Hao Chen,Yan Lin,Fangbin Wang,Lu Wang,Juan Chen,Jian Liu,Xian Zhang
In beige adipocytes, UCP1-dependent thermogenesis can be driven by intracellular reactive oxygen species (ROS) generation. While ROS elevation also induces mast cell activation, serotonin synthesis and release from mast cells inhibits beige progenitor cell proliferation and browning. As a natural antioxidant and mast cell stabilizer, luteolin promotes adipocyte thermogenesis and inhibits mast cell activation. Thus, to activate adipocyte thermogenesis, how luteolin regulates ROS level in beige adipocytes and mast cells needs to be further investigated. In this study, mouse subcutaneous stromal vascular fraction (SVF) cells are induced to differentiate into beige adipocytes, and mouse bone marrow-derived mast cells (BMMCs) are activated with hydrogen peroxide (H 2 O 2 ). Intracellular ROS level is augmented in differentiated beige adipocytes and H 2 O 2 -activated BMMCs, and H 2 O 2 -activated BMMCs inhibited brown differentiation of SVF cells and thermogenesis of beige adipocytes. In beige adipocytes, unlike synthetic antioxidant N -acetylcysteine (NAC), luteolin elevates the expression of thermogenic and beige-selective marker genes and intracellular ROS generation. Contrarily, luteolin inhibits H 2 O 2 -induced mast cell activation and ROS generation. Further, luteolin partially reverses the inhibitory effects of H 2 O 2 -activated BMMCs on the brown differentiation of SVF cells and the thermogenesis of beige adipocytes. Molecular mechanistic studies demonstrate that luteolin regulates intracellular ROS level in beige adipocytes and mast cells via the nuclear factor erythroid 2-related factor 2 (Nrf2)/Catalase pathway. Altogether, as a ROS regulator, luteolin contrarily affects intracellular ROS generation in beige adipocytes and mast cells, and hence elevates adipocyte browning.
研究领域:
分子生物学
·
代谢研究
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
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