BIOMEDICINE & PHARMACOTHERAPY
·
2016
·
IF 2.326
Qin Tang,Fangling Ji,Jianli Guo,Jingyun Wang,Yachen Li,Yongming Bao
Chrysin , one of natural flavonoid compounds, has recently been found to possess anti-inflammatory, antiallergic and anticancer properties. To increase its anticancer effects, 5 chrysin derivates were synthesized on the base of DNA intercalator structure. The inhibiting effects of chrysin and its derivatives on cancer cells Hela, BGC823, MCF-7, HepG2, and normal cells HEK-293, were evaluated by MTT assays . 5-(2′-amino) phenyl-7-cyclohexanemethylchrysin (Ch-1), a unique chrysin derivate, killed all the cancer cells but kept above 60% survival rate in normal cells HEK-293 at 62.5 μM. Treated with chrysin from 250 μM to 500 μM, those cells were still maintained above 60% survival rate. The result of circular dichroism spectra showed that Ch-1 could intercalate DNA while chrysin had no effects on DNA. Interestingly, Hela cells survival rates were 95% and 10%, after treated with 20 μM and 30 μM of Ch-1, respectively. Both intrinsic and extrinsic apoptotic pathway were identified in regulating the cell death caused by Ch-1 in Hela cells. p53, the upstream regulator of apoptotic pathway were extremely significantly up-regulated in Hela cells treated with 25 μM Ch-1. Moreover, the inhibiting effects and apoptotic related proteins responses to Ch-1 on Hela cells were abolished after pre-treated with Pifithrin-α (Pft-α), a p53 inhibitor. So, p53-depedent apoptosis is the crucial factor governing the inhibiting effects of Ch-1 in Hela cells. Amazingly, Ch-1 at non-toxic concentration (2.5–10 μM) enhanced significantly anti-cancer effect of 10-hydroxy camptothecin (HCPT) on Hela, BGC823, and MCF-7 cells.
研究领域:
癌症研究
·
药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
·
2022
·
IF 5.141
Hongxiang Li,Chunyue Zhao,Zhen Wang,Jinfeng Xing
The application of drug-loaded nanogels in the treatment of cancer has attracted much attention. Here, the stability of chrysin under green LED was investigated, the nanogels loaded with chrysin in situ were prepared and the effect of chrysin in the polymerization reaction was investigated. The morphology, chemical structure, and drug-polymer interactions of the nanogels loaded with chrysin (NG-C) were studied. Moreover, the time of gel point appearance and double bond conversion were also evaluated.
研究领域:
药学
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材料科学
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肿瘤学
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产品关联
DOI
高影响因子
Animal Models and Experimental Medicine
·
2026
·
IF 3.3
Yijia Wang,Xing Feng,Shuhui Zhao,Yuchong Fu,Ao Zhang,Xiaofeng Shen,Bowen Yu,Yihao Wang,Jiahui Lin,Bing Zhang,Weiping Ji,Lianpin Wu,Xiaoling Guo
Background Oxidative stress plays a pivotal role in the pathogenesis of heart failure and is closely linked to myocardial remodeling, which includes myocardial hypertrophy and fibrosis. Chrysin (CHR) has multiple medicinal effects such as antioxidant, anti-inflammatory, and anti-apoptosis. This research seeks to investigate whether CHR can protect against pressure overload–induced myocardial remodeling and to explore the underlying mechanism. Methods Transverse aortic constriction (TAC) surgery was conducted to establish a model of cardiac hypertrophy on male C57BL/6J mice. A model of cardiomyocyte hypertrophy in H9C2 cells induced by angiotensin II (Ang II) was also established. Results The results showed that CHR significantly improved survival and cardiac function, reduced myocardial hypertrophy and fibrosis, inhibited the expression of inflammatory mediators TNF-α and IL-1β, suppressed cell apoptosis rate, downregulated the levels of Bcl-2 Associated X protein (BAX) and Cleaved-Caspase-3, and upregulated B-cell lymphoma/leukemia 2 (BCL-2) expression in TAC surgical mice or Ang II-treated H9C2 cells. CHR could also upregulate the levels of antioxidant enzymes SOD1 and HO-1 by mediating the nuclear translocation and expression of NRF2 to counteract oxidative stress response. The further mechanism investigation utilizing bioinformatics analysis and western blot revealed that the disease of heart failure is associated with the phosphatidylinositol‑3‑kinase (PI3K)/serine/threonine-protein kinase B (AKT) signaling pathway. Conclusions Collectively, our findings demonstrated that CHR might exert the improvement effects on pressure overload–induced myocardial remodeling with hypertrophy and fibrosis through regulating the PI3K/AKT/NRF2 pathway–mediated oxidative stress response to alleviate myocardial cell inflammation and apoptosis, suggesting that CHR may be a promising therapeutic agent for cardiac diseases induced by pressure overload.
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DOI
PubMed
高影响因子
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
·
2019
·
IF 1.17
Yun-Mei Liu,Yang Li,Jie Xiao,Qi-Zhi Zhang,Jian-Xin Song
Amino acid derivatives containing chrysin were synthesized for evaluating their anticancer effects. Among them, compound N-(7-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)heptanoyl)-L-isoleucine (6e) displayed the most potent antiproliferative activity against MGC-803 cells with IC50 value of 20.0 μM. Preliminary mechanistic studies showed that compound 6e could inhibit the colony formation and migration of MGC-803 cells. Flow cytometry analysis demonstrated that compound 6e mediated cell apoptosis of MGC-803 cells and arrested cell cycle in G2/M-phase. Moreover, 6e treatment in MGC-803 cells downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic gene Bax in a concentration-dependent manner. Our studies suggest that compound 6e may sever as an effective chemotherapeutic candidate.
研究领域:
药理学
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肿瘤学
·
化学
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DOI
PubMed
高影响因子
LUMINESCENCE
·
2021
·Vol. 37
·期 1
·72-81
·
IF 2.464
Haonan Zhao,Junfeng Zhang,Xiaolian Lin,Huihui Li,Qinhe Pan
Cr(VI) is a type of dangerous effluent that has caused great harm to human health and the environment. Recognition and perception of Cr(VI) by artificial receptors has attracted extensive attention. A novel fluorescent chemical sensor based on the 5,7-dihydroxyflavone skeleton was designed and synthesized for the selective recognition of Cr(VI). As confirmed by fluorescence technology, the fluorescent probe 4-dimethylaminobenzyl chrysin ester–Zn (DBC–Zn) showed high sensitivity and selectivity for dichromate and a fast response (less than 30 sec) recognition. The fluorescence intensity of DBC–Zn varies linearly with the concentration of Cr(VI) in the range 0.1–1 μM. The detection limit of Cr 2 O 7 2− by DBC–Zn is 2.3 nM, which is far lower than the national safe drinking water standard stipulated by the US Environmental Protection Agency (1.9 μM). The quenching mechanism of the probe can be attributed to the interaction of the dynamic quenching effect and the fluorescence internal filtration effect. In addition, the probe has good stability in both neutral and alkaline environments, and the accuracy of quantitative analysis of Cr 2 O 7 2− in lake water or tap water is more than 80%. The test paper based on DBC–Zn can effectively detect Cr 2 O 7 2− at the concentration of 100 ppb. This shows that the probe has a certain practical application value.
研究领域:
环境科学
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分析化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF LUMINESCENCE
·
2023
·
IF 3.6
Zhifeng Cai,Yi Zhang,Yiming Zhang,Yongjie Bai,Jiayue Huang,Zijing Guo,Huangjing Bao,Jiayi Zhang
Chrysin has carried out intensive interest in medicine areas due to its excellent influences for human health. Precise determination of chrysin is fairly necessary for pharmaceutical quality control and clinical study. Herein, water soluble fluorescent copper nanoclusters (Cu NCs) were developed through one-pot itinerary by utilizing polyvinylpyrrolidone as the stabilizer and ascorbic acid as the reducing agent. The as-obtained Cu NCs emitted bright blue fluorescence and suggested good optical features and outstanding photostability with the quantum yield of 9.27%. The inner filter effect (IFE) should be the main cause of the fluorescence quenching of Cu NCs. For this, a fluorescent system for chrysin determination was carried out by utilizing the Cu NCs as a nanoprobe. The fluorescence weakening efficiency of Cu NCs had a linear relationship to chrysin amounts in the range of 0.5–300 μM, and detection limit of 0.093 μM was obtained. This as-established system was effectively utilized to measure chrysin in real samples.
研究领域:
分析化学
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医学
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DOI
高影响因子
ELECTROANALYSIS
·
2016
·Vol. 29
·期 3
·835-842
·
IF 2.471
Zhengkun Xie,Yongmei Wu,Sheng Kai,Gaiping Li,Baoxian Ye
A novel electrochemically activated doped Ta 2 O 5 particles modified carbon paste electrode (EA-Ta 2 O 5 -CPE) was prepared and applied for selective and sensitive determination of chrysin. X-ray diffraction (XRD), scanning electron microscopy (SEM), electrochemical impedance spectroscopy (EIS) techniques and cyclic voltammetry (CV) were used to characterize the Ta 2 O 5 particles and investigate the electrochemical response of the sensor. Compared with bare CPE, the doped Ta 2 O 5 modified electrode got much more porous by electrochemical treatment and exhibited larger effective surface area, more reactive site and excellent electrochemical catalytic activity toward the oxidation of chrysin. Under optimum conditions by LSV, the oxidation peak currents responded to chrysin linearly over a concentration range from 5.0×10 −8 to 7.0×10 −6 mol L −1 with a detection limit of 2.0×10 −8 mol L −1 (5.08 ng mL −1 ). The fabricated sensor showed anti-interference ability against the biological common interferents (i.e. baicalein, baicalin) and provided to be reliable for the determination of chrysin in Chinese medicinal herb Oroxylum indicum and chrysin capsules samples with satisfactory results.
研究领域:
分析化学
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药物分析
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产品关联
DOI
高影响因子
Frontiers in Pharmacology
·
2022
·
IF 5.988
Zuoxing Wu,Chen Li,Yu Chen,Qian Liu,Na Li,Xuemei He,Weibin Li,Rong Shen,Li Li,Chenming Wei,Siyuan Shao,Fangsheng Fu,Jiaxin Ding,Xiaochen Sun,Dairong Wang,Guixin Yuan,Yiji Su,Jinmin Zhao,Jiake Xu,Ren Xu,Xin Xu,Feng Xu
Bone homeostasis only exists when the physical function of osteoblast and osteoclast stays in the balance between bone formation and resorption. Bone resorption occurs when the two processes are uncoupled, shifting the balance in favour of bone resorption. Excessive activation of osteoclasts leads to a range of osteolytic bone diseases including osteoporosis, aseptic prosthesis loosening, rheumatoid arthritis, and osteoarthritis. Receptor activator of nuclear factor kappa-B ligand (RANKL) and its downstream signaling pathways are recognized as key mediators that drive the formation and activation of osteoclastic function. Hence, osteoclast formation and/or its function remain as dominant targets for research and development of agents reaching the treatment towards osteolytic diseases. Chrysin (CHR) is a flavonoid with a wide range of anti-inflammatory and anti-tumor effects. However, its effect on osteoclasts remains unknown. In this study, we found the effects of CHR on inhibiting osteoclast differentiation which were assessed in terms of the number and size of TRAcP positive multinucleated osteoclasts (OCs). Further, the inhibitory effects of CHR on bone resorption and osteoclast fusion of pre-OC were assessed by hydroxyapatite resorption pit assay and F-actin belts staining; respectively. Western blotting analysis of RANKL-induced signaling pathways and immunofluorescence analysis for p65 nuclear translocation in response to RANKL-induced osteoclasts were used to analyze the mechanism of action of CHR affecting osteoclasts. Lastly, the murine calvarial osteolysis model revealed that CHR could protect against particle-induced bone destruction in vivo . Collectively, our data strongly suggested that CHR with its promising anti-tumor effects would also be a potential therapeutic agent for osteolytic diseases.
研究领域:
药理学
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骨科
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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
Advanced Composites and Hybrid Materials
·
2024
·Vol. 7
·期 6
·1-16
·
IF 23.2
Jiang Youwei,Sima Yingyu,Alomar Taghrid S.,AlMasoud Najla,El-Bahy Zeinhom M.,Feng Jinxia,Wan Kun,Toktarbay Zhexenbek,He Quanguo,Ding Jianhua,Wang Jingfeng,Wang Wu
The pursuit of rapid and sensitive detection methods for bioactive compounds in traditional Chinese medicine (TCM) is a continuous quest in the field of natural product chemistry. Herein, we report the development of a novel nanocomposite material comprising bismuth molybdate (Bi 2 MoO 6 ) and multi-walled carbon nanotubes (MWCNTs), which has been successfully applied to the ultrasensitive and simultaneous detection of the bioactive flavonoids baicalein and chrysin. These compounds, known for their potent anticancer and antioxidant properties, are prevalent in TCM and nutraceuticals. The Bi 2 MoO 6 -MWCNTs nanocomposite was meticulously characterized using X-ray diffraction (XRD), scanning electron microscopy (SEM), electrochemical impedance spectroscopy (EIS), and cyclic voltammetry (CV), revealing its structural and functional attributes. The optimized electrochemical sensor, based on a glassy carbon electrode modified with the nanocomposite, demonstrated remarkable sensitivity with a linear response range of 0.001–5.0 μmol·L −1 for baicalein and 0.007–3.0 μmol·L −1 for chrysin, alongside impressively low detection limits of 0.2 nmol·L −1 and 1.4 nmol·L −1 , respectively. The sensor’s performance was further validated through its application in the analysis of human serum and Scutellaria baicalensis extracts, showcasing its robust repeatability, selectivity, and stability. This work not only advances the field of TCM analysis but also opens new horizons for the integration of hollow bimetallic oxides with carbon-based materials in electrochemical sensing, offering a strategic approach to the rapid assessment of bioactive constituents in complex matrices.
研究领域:
中药分析
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材料科学
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生物医学工程
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产品关联
DOI
高影响因子
BIOCHEMICAL PHARMACOLOGY
·
2015
·
IF 5.009
Wan Li,Hua Sun,Xingwang Zhang,Huan Wang,Baojian Wu
Efflux transport is a critical determinant to the pharmacokinetics of sulfate conjugates. Here we aimed to establish SULT1A3 stably transfected HEK293 cells, and to determine the contributions of BCRP and MRP transporters to excretion of chrysin and apigenin sulfates. The cDNA of SULT1A3 was stably introduced into HEK293 cells using a lentiviral vector , generating a sulfonation active cell line (i.e., SULT293 cells). Identification of sulfate transporters was achieved through chemical inhibition (using chemical inhibitors) and biological inhibition (using short-hairpin RNAs (shRNAs)) methods. Sulfated metabolites were rapidly generated and excreted upon incubation of SULT293 cells with chrysin and apigenin. Ko143 (a selective BCRP inhibitor) did not show inhibitory effects on sulfate disposition, whereas the pan-MRP inhibitor MK-571 caused significant reductions (38.5–64.3%, p < 0.001) in sulfate excretion and marked elevations (160–243%, p < 0.05) in sulfate accumulation. Further, two efflux transporters (BCRP and MRP4) expressed in the cells were knocked-down by shRNA-mediated silencing. Neither sulfate excretion nor sulfate accumulation was altered in BCRP knocked-down cells as compared to scramble cells. By contrast, MRP4 knock-down led to moderate decreases (17.1–20.6%, p < 0.05) in sulfate excretion and increases (125–135%, p < 0.05) in sulfate accumulation. In conclusion, MRP4 was identified as an exporter for chrysin and apigenin sulfates. The SULT1A3 modified HEK293 cells were an appropriate tool to study SULT1A3-mediated sulfonation and to characterize BCRP/MRP4-mediated sulfate transport.
研究领域:
药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
·
2023
·
IF 4.8
Lei Liu,Yingyu Sima,Jinxia Feng,Shuting Shi,Aiting Chen,Chuanqin Zhou,Quanguo He,Yimin Tan
A bismuth oxide- nitrogen doped reduced graphene oxide/glassy carbon electrode (Bi 2 O 3 -NRGO/GCE) was prepared for the detection of the flavonoid drug chrysin in pharmaceutical capsules, for the first time. Bi 2 O 3 nanosheets synthesized by a hydrothermal method, were ultrasonically mixed with NRGO, and a simple and efficient Bi 2 O 3 -NRGO/GCE composite was prepared. The composites were characterized by various methods. Cyclic voltammetry and electrochemical impedance techniques were used to study the electrochemical sensing performance of the composites-modified electrode surface. The electrochemical performance and optimal detection conditions of chrysin on Bi 2 O 3 -NRGO/GCE were investigated by differential pulse voltammetry (DPV). The oxidation peak current of chrysin has a linear relationship with its concentration, in the range of 0.01–10 μM, with a detection limit of 2.0 nM. Bi 2 O 3 -NRGO/GCE also has good selectivity for chrysin, which is not interfered with by common inorganic salts and common organic substances, or by structurally similar substances. The composite electrode also has good repeatability, reproducibility and stability. It shows that utilizing Bi 2 O 3 and NRGO binary complexes modified electrodes for ultrasensitive chrysin sensing is a simple and convenient detection method, with promising applicability in the development of pharmaceutical component sensing technology.
研究领域:
分析化学
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药物分析
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材料科学
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产品关联
DOI
高影响因子
Chemical Biology & Drug Design
·
2024
·Vol. 104
·期 4
·e70003
·
IF 3.2
Xiang Yu,Di Zhang,Chengming Hu,Zejun Yu,Yang Li,Cheng Fang,Yinsheng Qiu,Zhinan Mei,Lingyun Xu
Hepatocellular carcinoma (HCC) is the sixth most prevalent malignant tumor. Hepatocellular carcinogenesis is closely linked to apoptosis, autophagy, and inflammation. Diosmetin and chrysin, are two flavonoid compounds, exhibit anti-inflammatory and anticancer properties. In this study, the TCGA database was utilized to identify differentially expressed genes between normal subjects and HCC patients. Molecular docking and molecular dynamics analyses were employed to assess the binding affinity of chrysin and diosmetin to key proteins in the PI3K/AKT/mTOR/NF-κB signaling pathway. Western blotting and RT-qPCR were used to measure the protein and gene expression within this pathway. The results indicated that HCC patients had elevated levels of PI3K, AKT, mTOR, and P65 proteins compared to normal subjects, which adversely affected patient survival. Molecular docking and dynamics studies demonstrated that diosmetin and chrysin are effectively bound to these four proteins. In vitro experiments revealed that the combination of diosmetin and chrysin could induce apoptosis, enhance autophagy, reduce inflammatory mediator production, and improve the tumor cell microenvironment by inhibiting the PI3K/AKT/mTOR/NF-κB signaling pathway. Notably, the synergy score for the combination of diosmetin (25 μM) and chrysin (10 μM) was 16. Thus, the diosmetin–chrysin combination shows promise as an effective therapeutic approach for hepatocellular carcinoma due to its strong synergistic effect.
研究领域:
肿瘤学
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）