JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2021
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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
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炎症研究
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DOI
高影响因子
MACROMOLECULAR BIOSCIENCE
·
2021
·Vol. 21
·期 12
·2100269
·
IF 4.979
Chuanjin Yin,Yalu Liu,Xueju Qi,Chuanlong Guo,Xiaochen Wu
The possibility of using drug loaded bovine serum albumin (BSA) porous films as therapeutic contact lenses is investigated. Kaempferol (KAE), a hydrophobic antioxidant and anti-inflammatory agent, is incorporated into BSA porous films to form BSA/KAE films. The BSA/KAE films are transparent in the visible wavelength range of the human eye, possessing high water content and good cytocompatibility. A prolonged and sustained drug release is observed, and the in vivo efficacy of BSA/KAE films is better than the individual KAE. BSA/KAE films promoted the corneal re-epithelialization, inhibited neovascularization, and reduced the inflammation of an alkali burn induced corneal injury model. The study demonstrates the promising potential of BSA/KAE films as therapeutic contact lenses for the treatment of corneal injury, builds an available ocular drug delivery platform for ocular diseases.
研究领域:
眼科
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药剂学
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生物材料
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DOI
PubMed
高影响因子
Frontiers in Bioscience-Landmark
·
2023
·Vol. 28
·期 11
·311
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IF 3.1
Qing Zhu,Yuanshan Han,Ying He,Yilan Fu,Hui Yang,Yun Chen,Yingrui Shi
Background: Breast cancer-related depression (BCRD) is strongly associated with BC and increases recurrence and mortality. This study investigated the role of kaempferol in the pathogenesis of BCRD and its underlying mechanism. Methods: 4T1 mouse BC cells were treated with corticosterone (Cort) in vitro to develop a neuronal injury model, and a BCRD mouse model was established by injecting 4T1 cells and Cort. The effects of kaempferol on 4T1 cells and BCRD models were measured by behavioral tests, Cell Counting Kit-8 assay, wound healing assay, colony formation assay, Western blot analysis, quantitative real-time PCR, hematoxylin and eosin staining, enzyme-linked immunosorbent assay, and immunofluorescence. BCRD cells were transfected with the cyclo-oxygenase-2 (COX-2) overexpression plasmid to study the role of the COX-2/prostaglandin E2 (PGE2) axis in the anti-BCRD activity of kaempferol. The connection between kaempferol and COX-2 was analyzed by molecular docking. Results: Kaempferol reduced the viability, migration, and clones of 4T1 cells and inhibited BC growth and depression-like behavior in mice. Kaempferol alleviated inflammation in BCRD, decreased interleukin 1 beta (IL-1β) and IL-6 levels, and increased transforming growth factor beta 1 (TGF-β1) and IL-10 levels. In addition, kaempferol elevated the levels of serotonin, dopamine, and norepinephrine and the amount of 5-Bromo-2′-deoxyuridine/neuronal nuclei-positive cells. Kaempferol downregulated COX-2 and PGE2, and kaempferol could dock with the protein structure of COX-2. Overexpression of COX-2 reduced BCRD viability, upregulated IL-1β and IL-6 levels, and downregulated TGF-β1 and IL-10 expression. Overexpression of COX-2 reversed the protective effects of kaempferol. Conclusion: Kaempferol exerted anti-BCRD effects, at least in part by inhibiting the COX-2/PGE2 pathway, which regulates neuroinflammation, neurotransmitter imbalance, and defective neurogenesis. Therefore, kaempferol may be a promising candidate active ingredient for treating BCRD.
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PubMed
高影响因子
Food Bioscience
·
2023
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IF 5.2
Wenli Shi,Guowen Zhang,Yijing Liao,Xiaoyun Fei,Deming Gong,Xing Hu
Kaempferol , a natural flavonoid compound, was found to suppress the activity of AChE in a reversible mixed-inhibition with an IC 50 value of 12.43 ± 0.19 μM. Fluorescence spectra showed that the fluorescence burst mechanism of kaempferol on AChE was of static burst type, and it was coupled with AChE to form a complex with a moderate binding affinity driven mainly by hydrogen bonding and hydrophobic interactions. The analysis of circular dichroism spectra found that kaempferol induced structural relaxation of AChE with a decrease in α-helix content (from 19.64% to 18.02%). Computer simulation showed that kaempferol was a two-site inhibitor that bound to both the catalytic active site (Trp86, Glu202, Tyr337) and peripheral anionic site (Tyr72, Asp74, Tyr124 and Tyr341) of AChE, inducing the enzyme structure to become more stable, then the substrate was prevented from binding to the active site of AChE, and the catalytic activity of AChE was inhibited. Moreover, kaempferol binding at the PAS-AChE site induced a conformational change of AChE that may increase the binding affinity of galanthamine to the enzyme, and thus kaempferol and galanthamine synergistically inhibited the activity of AChE. This work may offer novel insights into the development of kaempferol as a food functional factor for the cure of AD.
研究领域:
药理学
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神经科学
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DOI
高影响因子
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
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2024
·Vol. 27
·期 11
·1611-1628
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IF 1.6
Pan Chengzhen,Zhang Chi,Lin Zonghan,Liang Zhou,Cui Yinhang,Shang Zhihao,Wei Yuanxun,Chen Feng
Background: Osteoporosis (OP) is an age-related skeletal disease. Kaempferol can regulate bone mesenchymal stem cells (BMSCs) osteogenesis to improve OP, but its mechanism related to disulfidptosis, a newly discovered cell death mechanism, remains unclear. Objective: The study
aimed to investigate the biological function and immune mechanism of disulfidptosis- related ribophorin I (RPN1) in OP and to experimentally confirm that RPN1 is the target for the treatment of OP with kaempferol. Methods: Differential expression analysis was conducted on disulfide-related
genes extracted from the GSE56815 and GSE7158 datasets. Four machine learning algorithms identified disease signature genes, with RPN1 identified as a significant risk factor for OP through the nomogram. Validation of RPN1 differential expression in OP patients was performed using the GSE56116
dataset. The impact of RPN1 on immune alterations and biological processes was explored. Predictive ceRNA regulatory networks associated with RPN1 were generated via miRanda, miRDB, and TargetScan databases. Molecular docking estimated the binding model between kaempferol and RPN1. The targeting
mechanism of kaempferol on RPN1 was confirmed through pathological HE staining and immunohistochemistry in ovariectomized (OVX) rats. Results: RPN1 was abnormally overexpressed in the OP cohort, associated with TNF signaling, hematopoietic cell lineage, and NF-kappa B pathway. Immune
infiltration analysis showed a positive correlation between RPN1 expression and CD8+ T cells and resting NK cells, while a negative correlation with CD4+ naive T cells, macrophage M1, T cell gamma delta, T cell follicular helper cells, activated mast cells, NK cells, and dendritic cells, was
found. Four miRNAs and 17 lncRNAs associated with RPN1 were identified. Kaempferol exhibited high binding affinity (-7.2 kcal/mol) and good stability towards the RPN1. The experimental results verified that kaempferol could improve bone microstructure destruction and reverse the abnormally
high expression of RPN1 in the femur of ovariectomized rats. Conclusion: RPN1 may be a new diagnostic biomarker in patients with OP, and may serve as a new target for kaempferol to improve OP.
研究领域:
医学研究
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药理学
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分子生物学
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免疫学
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生物信息学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
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IF 5.2
Dazhen Zhang,Xinzhe Qu,Fuchao Chu,Zhenxin Wang,Jie Mou,Feng Yuan
Background Heterotopic ossification (HO) is characterized by abnormal bone formation outside the skeleton following injury or inherited disease, leading to limb dysfunction and neurological deficits. Current treatment options for HO are largely ineffective. Methods A network pharmacological analysis was conducted to identify the active ingredients and protein targets in Astragalus and Cinnamon Twig Five-Substance Decoction (ACTFSD) on HO. Protein-protein interaction analysis and Gene Ontology Enrichment Analysis were used to investigate the key genes associated with the target proteins. Molecular docking was employed to validate the interactions between the core components and targets of ACTFSD. Kaempferol was encapsulated in liposomes synthesized via the thin-film dispersion method. In vitro and in vivo experiments were conducted to evaluate the therapeutic effects of kaempferol liposomes. Results Kaempferol, an active ingredient in ACTFSD, effectively inhibits the PTGS2\ NF-κB pathway, regulates macrophage immune responses, and reduces cytokine released by macrophages induce abnormal osteogenesis in tendon stem cells (TDSCs), thereby slowing the formation of HO. Kaempferol liposomes demonstrate better therapeutic effect than kaempferol alone. Conclusion This study indicates that targeting macrophages may represent an effective therapeutic strategy for HO. Furthermore, kaempferol liposomes appear to be a promising treatment for trauma-induced HO. These findings provide potential new directions for future HO treatment strategies.
研究领域:
医学
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药理学
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2026
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IF 10.4
Haowei Yang,Xiufang Bi,Ruifeng Ying,Khizar Hayat,Xiaohong Sun,Chunlei Ni,Quan "Sophia" He,Meigui Huang
Kaempferol, a plant flavonoid with antioxidant, anti-inflammatory, and anti-allergenic bioactivities, has limited use in functional foods due to its bitterness and low bioavailability. This study compared two zein-based modification strategies, insertion and coating, for kaempferol-loaded liposomes in terms of bitterness masking, stability, and bioaccessibility. At 0.2 mg/mL zein, insertion showed 4.67% higher encapsulation efficiency than coating. ( P < 0.05 ). E -tongue analysis showed coating reduced bitterness more effectively than insertion. Raman spectroscopy revealed coating involved electrostatic interactions, while insertion involved hydrophobic ones. Fluorescence probing indicated insertion expanded liposome internal space, whereas coating resulted in a compact structure. TG and DSC analyses confirmed coating provided greater thermal stability. Additionally, coated liposomes exhibited superior environmental stability, antioxidant activity, and bioaccessibility. In vitro tests showed zein-coated liposomes released 62.98 ± 1.35% kaempferol, while zein-inserted liposomes released 50.32 ± 0.59%. These findings offer new insights for integrating bitter bioactives into functional foods.
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PubMed
高影响因子
Frontiers in Microbiology
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2026
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IF 5.8
Yinhui Lin,Yufei Jiang,Shan Zhang,Ziyuan Zhang,Shaoya Liu,Jinru Lin,Xiaoxiao Chen,Yuchen Zhang,Yonghui Yu,Wenbo Wei,Xuan OuYang,Xinan Huang,Yajun Song,Jun Jiao
Chlamydia psittaci is an obligate intracellular pathogen that poses a significant threat to both human and animal health. The current therapeutic strategies are limited by the emergence of potential drug resistance, underscoring the urgent need for novel anti-chlamydial agents. In this study, we evaluated the anti-chlamydial activity of kaempferol, a natural occurring flavonoid. Potential targets of kaempferol and C. psittaci infection-related targets were identified through in silico screening. In cellular assays using both HeLa and THP-1 cells, kaempferol treatment significantly inhibits the intracellular growth of C. psittaci in a dose-dependent manner, while showing no host cell cytotoxicity at effective concentrations. Based on prior in silico virtual screening and our group’s systematic evaluation of the anti-chlamydial activity of flavonoids, kaempferol (40 μM) was selected as the target compound for this study due to its potent antimicrobial effects and its potential to modulate key host–pathogen interaction pathways. Mechanistic investigations revealed that kaempferol interferes with the trafficking of host-derived lipid to the bacterial inclusion, thereby depriving the pathogen of essential nutrients. Moreover, kaempferol treatment severely disrupted the normal differentiation of reticulate bodies (RBs) into infectious elementary bodies (EBs), resulting in an aberrant developmental cycle and a reduction in the production of new infectious progeny. This study demonstrates that kaempferol exerts anti-chlamydial activity by targeting two key processes of C. psittaci infection: lipid trafficking to inclusions and RB-EB conversion. These results highlight kaempferol as a promising lead compound for developing new therapeutic approaches against C. psittaci infections.
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PubMed
高影响因子
CRYSTENGCOMM
·
2021
·Vol. 23
·期 12
·2367-2375
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IF 3.545
Yuntian Xiao,Wenchao Yang,Ling Zhou,Hongxun Hao,Ying Bao,Qiuxiang Yin,Chuang Xie
As an emerging technology that can simultaneously improve the powder performance and bioavailability of drugs, spherulitic cocrystallization has increasingly shown its unique advantages. In this study, we reported a new case of a propylthiouracil/kaempferol (PTU–KA) spherulitic cocrystal and explored its growth mechanism. The morphological evolution process and growth kinetics of spherulites were studied using an in situ stereomicroscope and scanning electron microscope. The growth of the PTU–KA spherulitic cocrystal was discovered to have three stages: single crystal growth, non-crystallographic branching, and surface nucleation. It was found that increasing temperature can strengthen the surface nucleation process, and the increasing degree of supersaturation is beneficial to the formation of dense spherulites. An appropriate kinetic model has been established, which has demonstrated that the growth rate curve is not monotonical but has a maximum. Subsequent modeling analysis shows that different stages involve different control steps. Specifically, the non-crystallographic branching process is mainly dominated by interface control, while the surface nucleation process is mainly determined by diffusion control. The results of this work may provide a useful reference for the design and manufacture of spherulitic cocrystals.
研究领域:
药学
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晶体学
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材料科学
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DOI
高影响因子
Journal of Functional Foods
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2020
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IF 3.701
Sha Li,Junhui Pan,Xing Hu,Ying Zhang,Deming Gong,Guowen Zhang
Repression of pancreatic lipase activity reduces the excessive absorption of lipids, thereby reducing the risk of being overweight and obese. In the study, the inhibition of kaempferol on pancreatic lipase was studied by various spectroscopy techniques and molecular docking analysis. Kinetic analysis indicated that kaempferol reversibly inhibited pancreatic lipase activity in a competitive manner and showed the synergistic inhibition with orlistat. The fluorescence titrations suggested that kaempferol quenched the fluorescence of pancreatic lipase and the binding process was mainly driven by hydrophobic interactions and hydrogen bonds. The structural compactness of pancreatic lipase was verified by the results of circular dichroism and Fourier transform infrared spectra. Molecular docking and molecular dynamics simulation showed that kaempferol interacted with the residues Lys42 and Tyr404 in the active site of the enzyme by hydrogen bonds, preventing the substrate from binding to the active site. These findings may provide a theoretical basis for the further study of kaempferol as a natural anti-obesity supplement.
研究领域:
药理学
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生物化学
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分子生物学
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营养学
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DOI
高影响因子
MOLECULAR BIOLOGY REPORTS
·
2022
·Vol. 49
·期 6
·4607-4617
·
IF 2.742
Zhang Yimin,Chen Jingqin,Fang Wenxuan,Liang Kaoyun,Li Xiaoning,Zhang Fan,Pang Yuzhou,Fang Gang,Wang Xueni
Purpose Kaempferol is a natural flavonoid that has been reported to be active against many cancers, including prostate cancer, breast cancer and colon cancer. In our previous study, we found kaempferol could act as a selective androgen receptor modulator, thereby suppress development of benign prostatic hyperplasia. This finding inspired us to further explore the effect and the mechanism of action of kaempferol on prostate cancer. Methods Plate clone formation assay was performed to detect the effect of kaempferol on cell proliferation. Flow cytometry was used to detect the impact of kaempferol on cell apoptosis and cell cycle distribution. qPCR, immunofluorescence staining, and enzyme-linked immunosorbent assay were used to detect the expression of gene and protein of Ki67 which is a biomarker of cell proliferation. Results In the present study, we found kaempferol could dramatically suppress androgen-dependent and androgen-independent prostate cancer cells proliferation and induce their apoptosis. Furthermore, we found that kaempferol induced cell cycle to be arrested at G1 phase in 22Rv1 cells but at S and G2 phase in PC-3 cells. In addition, we detected the mRNA and protein of Ki67 which is corresponding to the cell proliferation and found that kaempferol could significantly inhibit Ki67 expression at mRNA level but increase its expression at protein levels in both androgen-dependent and androgen-independent prostate cancer cells. Conclusion Taken together, kaempferol inhibited the proliferation of androgen-dependent and androgen-independent prostate cancer cells by regulating the expression of Ki67. These findings further shed light on the mechanism of action of kaempferol on anti-prostate cancer.
研究领域:
肿瘤学
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药理学
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分子生物学
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细胞生物学
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DOI
PubMed
高影响因子
JOURNAL OF FLUORESCENCE
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2023
·Vol. 33
·期 5
·1971-1979
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IF 2.7
Zeng Hongyan,Peng Huan,He Hongmei,Feng Jinrong,Sun Yiqiang,He Huanyu,Li Li
As a common flavonols, kaempferol (Kae) has a broad market as health food and medicine for its anti-inflammatory, anti-oxidation, and anti-cancer properties. In this study, a novel convenient and simple fluorescent sensor based on carbon dots (CDs) for the detection of Kae was developed. The fluorescent CDs, with excellent photo-luminescence (PL) and up-conversion luminescence (UCPL) properties, were successfully prepared by low-temperature oil bath reaction based on ascorbic acid as carbon source at 90 °C in one pot. Under the optimal conditions, the fluorescence (FL) intensity of CDs was gradually quenched by the increasing addition of Kae with a linear relationship between F 0 /F and Kae concentration in a wide range from 5 µM to 100 µM with a detection limit of 0.38 µM. And this designed sensor was favourably applied for the detection of Kae in actual sample (xin-da-kang tablets). Moreover, the proposed CDs has great application prospects as a drug-sensor for detecting Kae due to its simple operation, economical and green materials, low equipment requirement, and rapid detection.
研究领域:
材料科学
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分析化学
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药学
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生物技术
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产品关联
DOI
PubMed
高影响因子
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