Food Analytical Methods
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2013
·Vol. 7
·期 6
·1256-1262
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IF 1.969
Zhou Nan,Sang Renhao,Zhu XiaShi
Functionalized β-cyclodextrin polymer, mono-6-deoxy-6-imidazole-β-cyclodextrin polymer (β-CDIMCP), was synthesized as a new solid phase adsorbent coupled with UV–visible spectroscopy to separate/analyze trace kaempferol. The results showed that kaempferol was adsorbed rapidly by β-CDIMCP (adsorption efficiency, 94.7 %) and then eluted by methanol (elution efficiency, 93.4 %). Under the optimum conditions, the calibration curve was linear in the concentration range from 0.10 to 14.0 μg/mL, with a correlation coefficient ( R ) of 0.9965. And the limit of detection was 0.028 μg/mL for kaempferol. The preconcentration factor of the method was tenfold. The molecular interaction between β-CDIMCP and kaempferol was studied through inclusion constant and FTIR analysis. The present method had been successfully applied to determine kaempferol in red wine samples.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2019
·
IF 4.213
Qian Du,Jianqiu Chen,Guojun Yan,Fannan Lyu,Jie Huang,Jin Ren,Liuqing Di
This study compared the in vitro and in vivo effects of different aliphatic acid grafted N -trimethyl chitosan (TMC) surface-modified nanostructured lipid carriers (NLC) by oral delivery. Medium-chain fatty acids, decylic acids (DA), and long-chain fatty acids, palmitic acids (PA) were selected as contrasting objects. TMC, DA grafted TMC (DA-TMC), and PA grafted TMC (PA-TMC) were successively synthesized. Kaempferol loaded NLC (KNLC), KNLC coated with DA-TMC (DA-TMC-KNLC) and PA-TMC (PA-TMC-KNLC) were fabricated, respectively. KNLC were subspherical in shape at nano-size limits. The particle size increased from 93.6 to 125.5 nm and the zeta potential changed from negative to positive due to surface-modification. The KNLC surface-modified with different aliphatic acid grafted TMC displayed a diverse release profiles at the simulative physiological environment, which contrasted that of KNLC. Pharmacokinetic studies demonstrated that the nanoparticles all could improve the AUC values and prolong blood retention times compared to that of kaempferol suspensions. Cell uptake and in situ intestinal perfusion experiments revealed that DA-TMC-KNLC and PA-TMC-KNLC could remarkably enhance cellular uptake of kaempferol into Caco-2 cells and drug absorption in each intestinal segment in comparison with KNLC, repectively. Wherein, DA-TMC-KNLC exhibits the greatest uptake and absorption efficiency as compared to kaempferol suspensions, KNLC and PA-TMC-KNLC. Collectively, DA-TMC surface-modified NLC might serve as a potential drug carrier for oral delivery of water-insoluble flavonoid ingredients.
研究领域:
药剂学
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药物递送
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纳米技术
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药代动力学
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胶体与界面科学
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Journal of Traditional Chinese Medicine
·
2022
·
IF 2.547
Kaixuan ZHOU,Dong ZHANG,Huiwei BAO,Lijing LI
OBJECTIVE: To study therapeutic effect of kaempferol on metabolic associated fatty liver disease (MAFLD) by network pharmacology and molecular docking combined with cell experiments. METHODS: First, use the SwissTargetPrediction database to predict the targets of kaempferol, and collect the targets of MAFLD through the Disgenet database and the GeneCards database. Then, the common target of kaempferol and MAFLD was enriched and analyzed by the Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes, and the protein-protein interaction (PPI) network was constructed through the string database to obtain the key targets, and carry out molecular docking of key targets with kaempferol; In cell experiment, oleic acid induced steatosis in HepG2 cells, which was intervened by kaempferol, the level of triglyceride (TG) was detected, the lipid deposition was observed by oil red O staining, and the protein expression was detected by Western blot. RESULTS: The results showed that there are 33 common targets for kaempferol and MAFLD. The biological process of GO is related to the regulation of protein kinase B, cell apoptosis, inflammatory factors, lipoxygenase, etc. Its action pathway is related to the phosphatidylinositol-3-kinase and protein kinase B (PI3K-AKT) signaling pathway, hypoxia-inducible factor 1 signaling pathway, forkhead box protein O signaling pathway, AMP-activated protein kinase signaling pathway, tumor necrosis factor signaling pathway, etc., the key targets are protein kinase B (AKT1), pros-taglandin G/H synthase 2, matrix metalloproteinase-9, epidermal growth factor receptor, and the molecular docking of kaempferol with the four key targets shows good binding properties. Cell experiments show that kaempferol can reduce cell TG levels, reduce lipid deposition, increase the expression of PI3K, AKT, and beclin-1, and reduce the expression of caspase-3 and nuclear factor-kappa B. Kaempferol can treat MAFLD by regulating the PI3K-AKT signaling pathway to regulate cell autophagy, apoptosis, and inflammation. CONCLUSIONS: This study shows that kaempferol can regulate lipid metabolism, reduce apoptosis, regulate inflammation and autophagy in the fatty liver cell model. It reveals the therapeutic mechanism of kaempferol on MAFLD and provides a natural product candidate for the treatment of MAFLD.
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Journal of Functional Foods
·
2021
·
IF 4.451
Jie Gao,Manqian Zhang,Ruixue Niu,Xue Gu,Erwei Hao,Xiaotao Hou,Jiagang Deng,Gang Bai
Nutrients in diets, especially functional foods, are beneficial in metabolism-related diseases, such as diabetes. Cinnamaldehyde (CA), a natural flavorant, inhibits glycolysis while enhancing glucose storage. Kaempferol (KP), a flavonol in edible plants, inhibits amino acid metabolism and gluconeogenesis. Whether the combination of CA and KP exerts stronger effects in diabetes needs further investigation. In this work, nontargeted metabolomics results confirmed the simultaneous obstruction of glucose and amino acid metabolism by CA and KP. The falling status of the energy supply, demonstrated by the increased ratio of adenosine monophosphate (AMP) /adenosine triphosphate (ATP), was sensed by AMP-activated protein kinase (AMPK). The activation of AMPK in turn enhanced lipolysis and inhibited fatty acid synthesis both in vivo and in vitro. In conclusion, this study indicated that the CA and KP combination ameliorated glucose and lipid metabolism disorders by enhancing lipid metabolism via the activation of AMPK.
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Food & Function
·
2020
·Vol. 11
·期 9
·7925-7934
·
IF 4.171
Yi-Chao Du,Li Lai,Hao Zhang,Fu-Rui Zhong,Huan-Li Cheng,Bao-Lin Qian,Peng Tan,Xian-Ming Xia,Wen-Guang Fu
Acetaminophen (APAP) is one of the safest and most effective over-the-counter (OTC) analgesics and antipyretics, but excessive doses of APAP will induce hepatotoxicity with high morbidity and mortality worldwide. Kaempferol (KA), a flavonoid compound derived from the medicinal and edible plant of Penthorum chinense Pursh, has been reported to exert a profound anti-inflammatory and antioxidant activity. In this study, we explored the protective effect and novel mechanism of KA against APAP-induced hepatotoxicity. The results revealed that KA pretreatment significantly reduced the levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT), relieved hepatocellular damage and apoptosis, attenuated the exhaustion of glutathione (GSH) and accumulation of malondialdehyde (MDA), increased the expression of antioxidative enzymes (e.g., heme oxygenase 1 (HO-1) and NADPH quinone oxidoreductase 1 (NQO1)), and thus restrained APAP-induced oxidative damage in the liver. KA suppressed the expression of NLRP3 and reduced the levels of pro-inflammatory factors, including interleukin-1 beta (IL-1β), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6). Moreover, KA remarkably inhibited high-mobility group box 1 (HMGB1) and toll-like receptor 4 (TLR4) expression as well as nuclear factor kappa-B (NF-κB) activation for liver protection against APAP-induced inflammatory responses and apoptosis. Taken together, our findings suggested that KA could effectively protect hepatocytes from APAP hepatotoxicity through the up-regulation of HO-1 and NQO1 expression, the down-regulation of NLRP3 expression, and the inhibition of the HMGB1/TLR4/NF-κB signaling pathway.
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EXPERIMENTAL CELL RESEARCH
·
2023
·
IF 3.7
Hong Liu,Yang Huang,Jing Yang,Xuejiao Xu,Qiaomei Dai,Yuwei Zhang,Li Zhao,Mengdi Zhang,Jing Zhang,Tonghui Liu,Lili Zhong
Estrogens have been demonstrated to inhibit age-related cognitive decline via binding to estrogen receptors (ERs). As a natural flavonoid component of Cuscuta Chinensis Lam. , Kaempferol-3- O -glucoside (K-3-G) not only possesses anti-neuroinflammatory potential but also functions as an agonist for ERα and ERβ. This study aimed to determine whether K-3-G improved cognition during the aging process, with an emphasis on its effect on microglial inflammation. In vivo , K-3-G (5 or 10 mg/kg/day) was orally given to the senescence-accelerated mouse prone 8 (SAMP8) mice from six to eight-month old. In addition to mitigating the memory and learning deficits of SAMP8 mice, K-3-G upregulated the expression of ERα and ERβ in their hippocampal CA1 region, with the higher dose being more effective. Less Iba-1 + microglial cells presented in SAMP8 mice treated with K-3-G. The formation of NLR Family Pyrin Domain Containing 3 (NLRP3) complex, production of pro-inflammatory cytokines and oxidative stress-related markers, as well as expression of pro-apoptotic proteins were reduced by K-3-G. In vitro , BV2 microglial cells exposed to oligomeric amyloid beta (Aβ) 1-42 were treated with 100 μM K-3-G. K-3-G showed similar anti-inflammatory effects on BV2 cells as in vivo . K-3-G-induced alterations were partly diminished by fulvestrant, an ER antagonist. Moreover, dual-luciferase reporter system demonstrated that K-3-G induced ER expression by activating the transcription of estrogen-response elements (EREs). Collectively, these findings demonstrate that K-3-G may be a novel therapeutic agent for senescence-related cognitive impairment by inhibiting microglial inflammation through its action on ERs.
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JOURNAL OF FOOD ENGINEERING
·
2023
·
IF 5.5
Chuye Ji,Muhammad Aslam Khan,Kaiwen Chen,Li Liang
Zein particles are potential for the encapsulation of bioactive compounds . Deoxyribonucleic acid (DNA) shows good pH stability and can complex with antioxidants. In this study, DNA and DNA-quercetin complexes was used as the coating layer of zein particles. Zein particles had a size of 85.10 nm and ζ-potential of −30.73 mV at 1 mg/mL DNA. Zein/DNA particles were stable at pH 4–9. Encapsulation efficiency of kaempferol and α-tocopherol in complex particles reached 92.90% and 97.02%, respectively. The potential use of zein/DNA particles was evaluated for protecting kaempferol. Moreover, DNA-quercetin complex coating was investigated to discuss the protection of α-tocopherol in zein particles. The DNA coating improved the storage stability of kaempferol or α-tocopherol by strengthening physical barrier. DNA-quercetin complexes further improved the stability of α-tocopherol by acting as antioxidant barrier. The retention of kaempferol and α-tocopherol was about 58% in zein/DNA and zein/DNA-quercetin particles at 45 °C after 28 days.
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FOOD CHEMISTRY
·
2026
·
IF 10.4
Shi-Ye Luo,Xiao-Tong Fan,Na-Li,Lei-Li,Yan-Xiang Bi,Li-Peng Du,Guang-Gang Xiang,Xiang-Xin Li,Xiao-Ming Fang
Kaempferol-3-O-sophoroside was a marker of Gentiana macrophylla Pall. • monofloral honey (GH). • SEM and UHPLC–DAD-QTOF-MS/MS enabled reliable botanical authentication of GH. • GH was enriched in flavonoids and phenolics compared with common honeys. • GH exhibited significant antioxidant and antibacterial activities. As a medicinal plant–derived honey, Gentiana macrophylla Pall. monofloral honey (GH) remains insufficiently characterized in terms of botanical authentication and characteristic chemical markers. The objective of this study was to identify a marker compound for GH and to evaluate the physicochemical characteristics and bioactive properties. The botanical origin of GH was verified by SEM observation, revealing that Gentiana macrophylla Pall. pollen grains are monad, isopolar, radially symmetrical, with a tricolporate aperture system. Kaempferol-3-O-sophoroside was identified as a potential characteristic compound by UHPLC–DAD-QTOF-MS/MS, with a content of 331.06 ± 19.96 μg/kg in GH. Due to the abundant total flavonoid (34.98 ± 0.31 mg Rutin/kg) and total phenolic contents (283.68 ± 3.07 mg GAE/kg) compared with other common commercial honeys, GH exhibited significant antioxidant capacity and antibacterial activity against E. coli MG1655 and S. aureus 23,923. Consequently, kaempferol-3-O-sophoroside, as a potential authentication marker for GH, contributes to the improvement of bioactivity. Download: Download high-res image (207KB) Download: Download full-size image
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International Journal of Electrochemical Science
·
2023
·
IF 1.5
Saif Ullah,Rooh Ullah,Rasha M.K. Mohamed,Gang Hu,Ateeq ur rehman,Muhammad Yasir Nawabi,Asif Hayat,Ata Ur Rehman,Mehboob Hassan,Ikram Uddin,Syed Attaullah Shah,Muhammad Zahir Shah,Jimei Song
An appropriate analytical technique for determination of kaempferol (KMF) by its perturbation effect on Belousov-Zhabotinskii (B-Z) oscillating system was reported. The macrocyclic copper (II) complex [CuL] (ClO 4 ) 2 ] was used as a catalyst while malic acid as substrate in B-Z system. The ligand L in the macrocyclic-complex is 5, 7, 7, 12, 14, 14-hexamethyl-1, 4, 8, 11-tetraazacyclotetradeca-4, 11-diene. Experimental outcomes shown the perturbation effect of KMF could cause the change in the amplitude of oscillation (ΔA) which was directly related to its concentration (2.5 × 10 -6 to 3.0 × 10 -4 mol/L) with correlation coefficient of 0.99315. The calculated relative standard deviation (RSD) is 3.1 % by eight samples (1.8 × 10 -5 mol/L) and the observed lower limit of detection is 1.25 × 10 -6 mol/L. The cyclic voltammetry (CV) experiments were used to confirm the redox reaction between kaempferol and sodium bromate. Furthermore, the reaction perturbation mechanism was derived from the well-known FKN (Field-Koros-Noyes) oscillation mechanism.
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DRUG DEVELOPMENT RESEARCH
·
2023
·Vol. 84
·期 3
·582-600
·
IF 3.8
Jiabin Zhou,Yuhan Liu,Jun Chen,Nanxiang Xiong,Dongye Yi
Kaempferol (Kae) is a natural flavonoid that has multiple biological activities, such as anti-inflammatory and antitumor activities. However, few studies have been reported on antiglioma effects of Kae. This study aimed to explore the effects and potential mechanisms of Kae and synergistic antitumor activities with gefitinib (Gef) on glioma. Cell Counting Kit-8 and 5-ethynyl-2'-deoxyuridine assays were used to detect cytotoxicity and cell proliferation. Cell apoptosis and the cell cycle were detected by flow cytometry. Transwell assays were used to detect the migratory and invasive abilities of glioma cells. Network pharmacology and molecular docking analysis were used to screen for core targets of Kae in glioma therapy. Xenograft tumor nude mice were established with U251 cells to verify the antiglioma effects of Kae in vivo. A terminal deoxynucleotidyl transferase dUTP nick end labeling assay was used to detect apoptosis in tumor tissues. The expression of proteins was detected by immunohistochemistry and western blot analysis. Kae inhibited cell proliferation, promoted apoptosis, and induced cell cycle arrest in the G2/M phase of glioma cells in a concentration-dependent manner. Kae inhibited the migration and invasion of glioma cells at low concentrations. Network pharmacology analyses showed that epidermal growth factor receptor (EGFR) and SRC proto-oncogene (SRC) might be direct molecular-binding targets of Kae. Our results showed that Kae inhibited the levels of phosphorylated EGFR, phosphorylated SRC (p-SRC), and phosphorylated signal transducer and activator of transcription 3 (STAT3). In addition, the combination of Kae with Gef significantly inhibited the proliferation of glioma cells. Kae further inhibited EGFR phosphorylation after treatment with Gef. Similarly, Kae further enhanced the inhibition of p-SRC caused by SU6656. Finally, we demonstrated that Kae exerted great antitumor activities and enhanced the antitumor effect of Gef by inhibiting EGFR/SRC/STAT3 signaling pathway in vivo. Kae played a potential role and synergistic antiglioma effects with Gef by inhibiting the phosphorylation of EGFR/SRC dual targets. Kae is expected to be a candidate drug or chemosensitizer in glioma therapy.
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Analytical Methods
·
2013
·Vol. 5
·期 10
·2591-2601
·
IF 1.855
Xiaojie Liu,Xiu Huang,Yuzhi Wang,Songyun Huang,Xiao Lin
An ionic liquid-based microwave-assisted extraction (IL-MAE) technique has been successfully developed for the simultaneous effective extraction of quercetin and kaempferol from Toona sinensis and Rosa chinensis which are Chinese medicinal plants. Twenty different types of ionic liquids (ILs) with different cations and anions have been synthesized and investigated. Several significant operating parameters of IL-MAE were optimized by a series of single factor experiments and orthogonal design L9 (34) experiments, respectively. Compared with ionic liquid-based maceration extraction (IL-ME), ionic liquid-based heat extraction (IL-HE) and ionic liquid-based ultrasound-assisted extraction (IL-UAE), the optimized approach was demonstrated as the optimal technique with the highest extraction efficiency and the shortest extraction time. Reversed phase high performance liquid chromatography (RP-HPLC) with ultraviolet-detection (UV-DAD) was employed for the simultaneous analysis of kaempferol and quercetin. The results indicated that the extraction amounts of quercetin from Toona sinensis extracted using [Bmim]Br and from Rosa chinensis extracted using [Omim]Br were 176.5 mg g−1 with RSD 1.2% and 134.3 mg g−1 with RSD 0.63%. And the extraction amounts of kaempferol from Toona sinensis extracted using [Bmim]Br and from Rosa chinensis extracted using [Omim]Br were 16.12 mg g−1 with RSD 0.24% and 9.070 mg g−1 with RSD 0.15%. The developed approach for analyzing quercetin was linear between the concentrations of 32.10 mg L−1 to 233.3 mg L−1 in Toona sinensis and 25.70 mg L−1 to 160.5 mg L−1 in Rosa chinensis with the regression coefficients (R) of 0.9998 and 0.9999, respectively. And for kaempferol, the developed approach was linear between the concentrations of 0.73 mg L−1 to 23.20 mg L−1 in Toona sinensis and 0.19 mg L−1 to 15.00 mg L−1 in Rosa chinensis with the regression coefficients (R) of 0.9993 and 0.9996, respectively. The recoveries of quercetin extracted by the developed methods were 96.76–104.1% in Toona sinensis and 98.40–103.3% in Rosa chinensis, and the recoveries of kaempferol were 95.75–106.3% in Toona sinensis and 98.55–102.9% in Rosa chinensis with the RSDs of lower than 3.0%. The LODs were 1.87–2.26 μg mL−1. The microstructures and chemical structures of these two researched samples before and after different extraction procedures were also investigated.
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CARBOHYDRATE POLYMERS
·
2024
·
IF 10.7
Xiao Tang,Kun Wang,Zihan Liu,Xu Luo,Ming Wu,Hui Ding,Gang Liu,Qian Du
Ulcerative colitis (UC) remains a major challenge in clinical treatment due to its multivariate pathology. Developing an oral formulation that encapsulates and delivers multiple active ingredients to target colon tissues by suppressing intestinal inflammation and restoring the intestinal barrier is crucial for effectively treating UC. Here, we developed rhubarb-derived nanovesicles (RNs) and a supramolecular hydrogel platform formed by furfural-functionalized chitosan-mannose polymer and synthesized 3-maleimide HP-β-CD, with kaempferol (Kae) integrated into the hydrophobic cavity. The hydrogel's cross-linking network effectively encapsulates RNs, forming the Kae/CMCHD@RNs system. Rheology, SEM, TGA, degradation behavior, in vitro drug release, and a macrophage-targeted permeability test were performed. The results indicate that the hydrogel utilizes pH/enzyme sensitivity to ensure sustained release in the colon, while also facilitating targeted delivery to macrophages. In vivo imaging further reveals a prolonged local drug retention time in the colon. Moreover, both in vitro and in vivo studies demonstrate RNs and Kae exhibit synergistic therapeutic effects for UC, including inflammation reduction, oxidative stress alleviation, M1-to-M2 macrophage repolarization, and restoration of the intestinal barrier. Consequently, this study underscores the potential of Kae/CMCHD@RNs as a promising therapeutic approach for managing UC.
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