INTERNATIONAL IMMUNOPHARMACOLOGY
·
2025
·
IF 4.7
Li Wang,Tao Gu,Chunguang Yu,Yingying Gao,Tingting Xuan,Kaichun Shen,Guowei Wang,Zhenhai Wang
Kaempferol (Kae) is a flavonoid that has antioxidant, anti-inflammatory and neuroprotective effects. In recent years, there have been increasing reports on viral infection-induced Guillain-Barré syndrome (GBS) with high rates of disability and fatality. Therefore, in order to search for effective peripheral nerve injury repair drugs, we used rats with experimental autoimmune neuritis (EAN) as the typical animal model for GBS, and implemented Kae treatment intervention on EAN rats. Real-time quantitative polymerase chain reaction (qPCR), western blotting (WB) and immunofluorescence (IF) were utilized to detect the changes of inflammatory factors and signaling pathway proteins in peripheral nerve of rats. The impact of Kae on peripheral nerve damage in EAN rats was evaluated in multiple dimensions by clinical symptom score and neuroelectrophysiology examination, and the protective impact and mechanism of Kae on peripheral nerve injury were revealed. Our results showed that Kae increased the expression of sciatic myelin basic protein (MBP), decreased the expression of peripheral nerve macrophage infiltration and inflammatory cytokines, including TNF-α, IL-1β and IL-6, and down-regulated the expression levels of TNFR1. Additionally, it suppressed the activation of the JNK and p38 pathways. It can alleviate sciatic nerve symptoms and pathological injury in EAN rats. Therefore, we believe that Kae can be used as an adjunct drug in the treatment of GBS.
研究领域:
药理学
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神经科学
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免疫学
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产品关联
DOI
PubMed
高影响因子
PREPARATIVE BIOCHEMISTRY & BIOTECHNOLOGY
·
2023
·
IF 2.9
Yi Yang,Yunci Zhang,Dongyu Gu,Chang Liu,Yi Wang,Shanshan Tang,Yuxin Yin,Jing Tian
Robinia pseudoacacia flower is a natural product with many biological activities, including antioxidation. To further develop its antioxidation, the extract was fermented by Aspergillus niger FFCC 3112 in the medium with carbon to nitrogen ratio of 1.4:1 and initial pH of 4.2 for 3.5 days to form the best antioxidant activity of the fermentation product by strain screening, single factor optimization, and response surface methodology. Further analysis, isolation and activity determination showed that a main chemical component, kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-galactopyranosyl-7-O-α-L-rhamnopyranoside, in the extract was completely hydrolyzed to kaempferol-7-O-α-L-rhamnopyranoside and kaempferol with better antioxidant activity through biotransformation, which was the basis for improving the antioxidant activity of fermentation products. Moreover, the mechanism of antioxidant and the contribution of phenolic hydroxyl groups were investigated by density functional theory. The result indicated that the antioxidant capacity of kaempferol-7-O-α-L-rhamnopyranoside and kaempferol increased with the increase of solvent polarity. In high-polarity solvents, they mainly scavenge free radicals through single electron transfer followed by proton transfer.
研究领域:
食品科学
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生物化学
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植物学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2020
·Vol. 11
·期 5
·4356-4362
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IF 4.171
Yunci Zhang,Dongyu Gu,Shuai He,Jing Meng,Jifeng Wang,Yunxiao Wang,Yi Wang,Jing Tian,Yi Yang
The flower of S. japonica is a favorite food and used as traditional medicine. In the present study, a facile and effective method based on the changes in the composition before and after the enzyme reaction was established to screen the active compounds from complex natural products. The separation of an active compound from the ethanolic extracts of Sophora japonica var. violacea, which exhibited the α-amylase inhibitory activity is presented as an example. The analysis of HPLC showed that one component was reduced by 25% after the enzyme reaction. The potential active compound was isolated via LH-20 gel permeation chromatography and identified as kaempferol 3-O-α-L-rhamnopyranosyl-(1 → 6)-β-D-galactopyranosyl-7-O-α-L-rhamnopyranoside by 1H and 13C NMR. The in vitro test indicated that the compound had the α-amylase inhibitory activity, and the IC50 was 88.56 ± 0.60 μg mL−1. The molecular docking study of this compound showed that the compound enfolded in the active sites of α-amylase completely and interacted with the amino acid residues through hydrogen bonds, van der Waals force and hydrophobic interactions.
研究领域:
药理学
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植物化学
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DOI
PubMed
高影响因子
POLYMER INTERNATIONAL
·
2023
·Vol. 72
·期 6
·586-596
·
IF 3.2
Fangping Liang,Wurong Li,Mingao Li,Xican Li,Jianfeng He,Quanzhou Wu
In this work, kaempferol molecularly imprinted polymers (MIPs) were screened in detail and were applied to the separation of kaempferol from real complex systems. Kaempferol-MIPs with high affinity and selectivity for kaempferol could be prepared successfully by using kaempferol as the template molecule, 4-vinylpyridine as the functional monomer, ethylene glycol dimethacrylate or divinylbenzene as the crosslinker, acetone or acetonitrile as the solvent. Scanning electron microscopy observation and Brunauer–Emmett–Teller measurement showed that the prepared MIPs had a heterogeneous pore structure and large specific surface area. Static and dynamic adsorption experiments and solid-phase extraction application were performed to evaluate the performance of the prepared MIPs. Only the MIPs with both higher distribution coefficient and higher imprinting factor in the dynamic experiments had better ability to retain kaempferol. Using the screened MIPs as solid-phase extraction sorbents, kaempferol and quercetin were extracted directly from the crude ginkgo leaves hydrolysate with high recovery and purity. Control experiments also showed that the screened MIPs were superior to commercially available adsorbents in terms of the separation of kaempferol from crude extracts. © 2023 Society of Industrial Chemistry.
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DOI
高影响因子
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
·
2024
·
IF 3.8
Peiyu Xue,Xinyong You,Li Ren,Weiming Yue,Zheng Ma
Kaempferol can exert biological functions by regulating various signaling pathways. This study evaluated the ameliorative effect of kaempferol on lipid accumulation using oleic acid and palmitic acid-treated HepG2 cells and high-fat diet mice. In vitro oil red O staining showed that kaempferol treatment improved lipid accumulation ( p < 0.001 for TG content and p < 0.05 for TC content). Immunofluorescence, Western blot analysis and RT-qPCR showed that kaempferol could promote nuclear translocation of PPARγ and reduce the expression of PPARγ, C/EBPβ, and SREBP-1c. Dietary intervention with kaempferol could reduce the lipid accumulation in hepatocytes and inflammatory cell infiltration, as well as attenuated serum levels of IL-6 and TNF-α in HFD-fed mice ( p < 0.001 for IL-6 and p < 0.01 for TNF-α at kaempferol 60 mg/kg/d). Meanwhile, histopathological examination revealed that there was no substantial damage or distinct inflammation lesions in organs at the experimental dose, including the heart, lung, kidney, and spleen. The aforementioned research findings can serve as references for further preclinical investigations on the potential of kaempferol to mitigate lipid accumulation.
研究领域:
药理学
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分子生物学
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营养学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2015
·
IF 3.391
Xi Peng,Guowen Zhang,Yijing Liao,Deming Gong
α-Glucosidase is a therapeutic target for diabetes mellitus, and α-glucosidase inhibitors play a vital role in the treatments for the disease. As a kind of potentially safer α-glucosidase inhibitor, flavonoids have attached much attention currently. In this study, kaempferol was found to show a notable inhibition activity on α-glucosidase in a mixed-type manner with IC 50 value of (1.16 ± 0.04) × 10 −5 mol L −1 . Analyses of fluorescence, circular dichroism and Fourier transform infrared spectra indicated that kaempferol bound to α-glucosidase with high affinity which was mainly driven by hydrogen bonds and van der Waals forces, and this binding resulted in conformational alteration of α-glucosidase. Further molecular docking study validated the experimental results. It was proposed that kaempferol may interact with some amino acid residues located within the active site of α-glucosidase, occupying the catalytic center of the enzyme to avoid the entrance of p-nitrophenyl-α- d -glucopyranoside and ultimately inhibiting the enzyme activity.
研究领域:
药理学
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生物化学
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DOI
高影响因子
ARCHIVES OF INSECT BIOCHEMISTRY AND PHYSIOLOGY
·
2024
·Vol. 117
·期 2
·e70001
·
IF 1.5
Qimeng He,Hui Jin,Jie Shen
Short-wavelength blue light is ubiquitous in daily life and has a lasting destructive influence. Its potential harm to biological health is significant. This study used Drosophila as a model organism to investigate the protective effects of kaempferol, a flavonoid, against the toxicity of blue light. It also examined its physiological effects on Drosophila under blue light irradiation. In this experiment, fruit flies were fed with three different concentrations of kaempferol solutions (0.1, 0.01, and 0.001 mol/L) dissolved in food. The survival rate and physiological indexes of Drosophila were investigated under blue light irradiation of 2500 lux. The results showed that 0.1 mol/L kaempferol increased the activity of male flies during the day and significantly extended the male survival time under blue light irradiation. However, the study found that kaempferol did not significantly prolong the survival time of Drosophila in the oxidative stress experiment, and no significant difference was observed in the feeding experiment. In summary, our research found that kaempferol, at the concentration of 0.1 mol/L, has a protective effect on Drosophila under blue light irradiation, potentially achieved through alterations in circadian rhythm. Summary Kaempferol protects Drosophila from blue light damage. The effect of kaempferol on Drosophila exhibits sex-specific responses. Kaempferol enhances daytime activity and extends the lifespan of male Drosophila .
研究领域:
生物学
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毒理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCES AND NUTRITION
·
2013
·
IF 1.257
Hui Cao,Xiaohui Jing,Donghui Wu,Yujun Shi
Methylation of flavonoids appears to be a simple and effective way to improve metabolic resistance and transport of flavonoids. Serum albumins are major soluble proteins serving as transport proteins for many exogenous compounds. This work in here mainly concerns about the effect of methylation of flavonoids on the affinity for human serum albumin (HSA) and ovalbumin. One isoflavone (genistein) and one flavonol (kaempferol) and their monomethylated derivatives at position 4′ (biochanin A and kaempferide) were studied for their affinities for ovalbumin and HSA. The methylation of flavonoids significantly affects the binding process. In general, the methylation of flavonoids improved the affinities for proteins by 2–16 times. This result supports that the methylation of genistein and kaempferol enhanced the transporting ability, which leads to facilitated absorption and greatly increased bioavailability. The methylation increases the hydrophobicity of genistein and kaempferol, and the hydrophobic interaction plays an important role in binding flavonoids to HSA and ovoalbumin.
研究领域:
药理学
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生物化学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2021
·
IF 3.981
Wenjing Yang,Dengchao Xie,Yuqi Liang,Nanxi Chen,Bo Xiao,Lian Duan,Min Wang
Kaempferol is well known for the desirable properties in radical scavenging, oxidation resistance and inflammation resistance. However, the clinical translation of kaempferol for inflammatory disease treatment is still restricted by the poor solubility, undesirable stability and dissatisfied bioavailability. In this manuscript, multi-responsive kaempferol loaded fibroin nanoparticles (KF-NPs) were fabricated to overcome these shortages in biomedical application. The experimental results suggested that the negative charged KF-NPs (−25.2 ± 0.3 mV) had favorable average particle size (151 ± 1.6 nm) with uniform distribution. Noticeably, the accumulative drug release of fibroin nanoparticles dramatically increased in environment with acidity, glutathione (GSH) or reactive oxygen species (ROS), indicating the on-demand intracellular drug release properties. In vitro experiments revealed that the KF-NPs were biocompatible and can be internalized by cells. Moreover, KF-NPs had synergistic effect in downregulating the expression of TNF-α and eliminating the intracellular reactive oxygen. These results suggested that KF-NPs were promising therapeutic platform for anti-inflammatory treatments.
研究领域:
药剂学
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纳米技术
·
炎症研究
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DOI
高影响因子
Food Science & Nutrition
·
2024
·
IF 3.5
Peiyu Xue,Hongmei Zhao,Xinyong You,Weiming Yue
Lactoferrin and polyphenols are common natural functional compounds. Their interactions and the consequential alterations in functional activity have received widespread attention. The work aimed to investigate the interaction between lactoferrin and kaempferol, as well as evaluate the in vitro anticancer properties of the lactoferrin–kaempferol complex. The results of the spectra experiments revealed that lactoferrin and kaempferol are capable of forming complexes to quench the endogenous fluorescence of lactoferrin. Further insight into the binding mechanism was gained through molecular docking and molecular dynamics simulations. These analyses suggest that both hydrophobic interactions and hydrogen bonding are essential factors in the interaction between lactoferrin and kaempferol. Furthermore, the MTT assay and apoptosis by flow cytometry were conducted, revealing a synergistic effect of kaempferol and lactoferrin on the inhibition of HeLa cell proliferation. The findings from this investigation could improve our understanding of lactoferrin's interaction with polyphenols and the role of the lactoferrin–kaempferol complex in inhibiting cancer cell proliferation.
研究领域:
药理学
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癌症研究
·
分子生物学
·
生物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Chao Hao,Changping Fan,Lanting Gao,Mingyue Yin,Xue Jiang,Chenchen Wang,Xingyin Wang,Chaoyang Yin,Guisen Zhang,Jian Zhang
The present study aimed to prepare and evaluate a sustained-release microsuspension (MSP) of the antischizophrenic drug risperidone (RIS) via cocrystallization with kaempferol (KAE) (RIS-KAE-MSP). Cocrystal solvates of RIS and KAE in solvent systems of ethanol (EtOH), methanol (MeOH) and ethyl acetate (EA) were successfully prepared by solvent evaporation method. Cocrystal solvates prepared from 3 different solvent systems were characterized in detail using single-crystal X-ray diffraction (SCXRD), Hirshfeld surface analysis (HSA), Gas chromatography (GC), Karl Fischer titration (KFT), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and Fourier transform infrared (FT-IR) spectroscopy. SCXRD successfully confirmed that RIS-KAE·0.4EtOH·2.6H₂O and RIS-KAE·MeOH are solvates. The dissolution rates of RIS from cocrystal solvates at pH 6.8 in 12 hours were 9.4-fold (RIS-KAE·0.4EtOH·2.6H₂O), 11.8-fold (RIS-KAE·MeOH) and 7.4-fold (RIS-KAE·EA·H₂O) lower than that of free RIS, showing significant sustained release behaviors. Furthermore, RIS-KAE·0.4EtOH·2.6H 2 O was prepared into microsuspensions (MSP), denoted as RIS-KAE-MSP, for I.M. injection. Pharmacokinetic (PK) results indicated that plasma RIS of RIS-KAE-MSP were still detectable by liquid chromatography-mass spectrometry (LC-MS) for as long as 45 days. In conclusion, cocrystallization with insoluble coformers is a promising strategy for long-term sustained release of RIS.
研究领域:
药剂学
·
药理学
·
晶体工程
·
药物递送
·
分析化学
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产品关联
DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2015
·
IF 2.912
Yajie Wang,Guowen Zhang,Junhui Pan,Deming Gong
Xanthine oxidase (XO), a key enzyme in purine catabolism, is widely distributed in human tissues. It can catalyze xanthine to generate uric acid and cause hyperuricemia and gout. Inhibition kinetics assay showed that kaempferol inhibited XO activity reversibly in a competitive manner. Strong fluorescence quenching and conformational changes of XO were found due to the formation of a kaempferol–XO complex, which was driven mainly by hydrophobic forces. The molecular docking further revealed that kaempferol inserted into the hydrophobic cavity of XO to interact with some amino acid residues. The main inhibition mechanism of kaempferol on XO activity may be due to the insertion of kaempferol into the active site of XO occupying the catalytic center of the enzyme to avoid the entrance of the substrate and inducing conformational changes of XO. In addition, luteolin exhibited a stronger synergistic effect with kaempferol than did morin at the lower concentration.
研究领域:
生物化学
·
酶学
·
药理学
·
天然产物研究
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DOI
高影响因子
危险品化学品经营许可证（带存储）