OncoTargets and Therapy
·
2019
·
IF 3.046
Zheng-Hong Liu,Cheng-Xi Yang,Lei Zhang,Cong-Ying Yang,Xiu-Quan Xu
Background Baicalein, a natural flavonoid derived from traditional Chinese herb Scutellaria baicalensis Georg (known as Huang Qin in Chinese), has been reported to exhibit notable antitumor activity in various cancer cells, including breast cancer. However, the detailed mechanisms underlying its induced apoptosis as a prooxidant in breast cancer cells are still unknown. Materials and methods In this study, we investigated the effect of endogenous copper on cytotoxic activity of baicalin against human breast cancer MCF-7 cells in vitro. Results Baicalein could remarkably reduce the cell viability in both dose- and time-dependent manners in MCF-7 cells but with lower cytotoxic effects on normal breast epithelial cells, MCF-10A. Such cell death could be prevented by pretreatment with Cu (I)-specific chelator neocuproine (Neo) and reactive oxygen species (ROS) scavengers. Meanwhile, baicalein could induce MCF-7 cell morphological changes, promote apoptotic cell death and increase the apoptotic cell number. Moreover, DCHF-DA staining, flow cytometry and Western blotting analyses proved that baicalein triggered the mitochondrial-dependent apoptotic pathway, as indicated by enhancement the level of intracellular ROS, disruption of mitochondrial membrane potential (ΔΨm), downregulation of anti-apoptotic protein Bcl-2, upregulation of pro-apoptotic protein Bax, release of cytochrome C and activation of caspase-9 and caspase-3 in MCF-7 cells. The pretreatment with Neo remarkably weakened these effects of baicalein. Furthermore, we confirmed that the prooxidant action of baicalein involved the direct production of hydroxyl radicals through redox recycling of copper ions. Conclusion These findings suggested that baicalein, acting as a prooxidant, could trigger apoptosis in MCF-7 cells occurs via the ROS-mediated intrinsic mitochondria-dependent pathway.
研究领域:
肿瘤学
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药理学
·
细胞生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
STEROIDS
·
2017
·
IF 2.282
Xiao-Long He,Yajing Xing,Xiang-Zhong Gu,Jie-Xin Xiao,Ying-Ying Wang,Zhengfang Yi,Wen-Wei Qiu
In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.
研究领域:
药理学
·
有机合成化学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 66
·53835-53845
·
IF 3.84
Weihua Jiang,Lei Yang,Lipeng Qiu,Jingwen Xu,Xiuchun Yang,Ju Wang,Hui Zhou,Dongkai Wang
Multifunctional hybrid nanoparticles (NPs) based on sodium carboxymethylcellulose-graft-histidine (CMH) and TPGS were designed for effective delivery and overcoming multidrug resistance (MDR) of docetaxel (DTX). An amphiphilic CMH copolymer with excellent biocompatibility, pH-sensitivity, and solubilizing capacity for poorly soluble drugs was firstly synthesized and characterized. TPGS incorporated into CMH copolymer facilitated lower critical aggregation concentration (CAC) (0.0074 mg mL−1), smaller particle size (147.8 ± 3.14 nm), higher drug encapsulation (88.3 ± 3.33%), and better controlled release rate. The NPs based on CMH copolymer showed a pH-dependent drug release manner. The DTX-loaded CHT-1.5 NPs could significantly enhance cytotoxicity against both MCF-7 and MCF-7/ADR cells when compared to DTX-loaded CMH NPs and free DTX. Furthermore, cellular uptake and P-gp inhibition assays confirmed that the enhanced MDR reversal effect of DTX-loaded CHT-1.5 NPs was caused by the combination of increased drug accumulation and inhibition of P-glycoprotein mediated drug efflux in drug-resistant MCF-7/ADR cells. Consequently, CHT-1.5 NPs can act as an effective nanocarrier for delivering antitumor drugs and overcoming P-gp overexpressing tumor cells.
研究领域:
药学
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纳米技术
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癌症研究
·
药物递送系统
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产品关联
DOI
高影响因子
MICROCHIMICA ACTA
·
2018
·Vol. 185
·期 10
·1-9
·
IF 5.705
Wang Lude,Chen Yang
A colorimetric and fluorescent pH probe was designed by doping carbon dots (C-dots) with Eu(III), Tb(III) and 2,6-pyridinedicarboxylic acid (DPA). The resulting nanoparticles were applied as fluorescent indicators for pH values (best detected at excitation/emission wavelengths of 272/545, 614 nm). The pH induced optical effects are due to pH induced variations in energy transfer. The fluorescence of the probe shows a continuous color variation, and a linear change with pH values in the range from 3.0 to 10.0 can be established by using a Commission Internationale de L’Eclairage (CIE) chromaticity diagram. This new kind of pH nanoprobe is more accurate than previously reported pH indicator probes because the pH value can be calculated by using chromaticity coordinates that only depend on the chromaticity. The pH nanoprobe was applied to visualize pH values in human breast adenocarcinoma cells (MCF-7).
Carbon dots modified with Eu(III) and Tb(III) complexes of 2,6-pyridinedicarboxylic acid (DPA) were prepared. The doped carbon dots were used as a pH-sensitive nanosensor. The fluorescence chromaticity of the nanoparticles changes with the variation of pH value.
研究领域:
生物化学
·
材料科学
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医学检测
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF INTERNATIONAL MEDICAL RESEARCH
·
2026
·
IF 1.8
Enyuan Chen,Yu Yin,Xiaoyun Miao,Bin Yu,Jun Yang,Mingming Li,Xiaoyun Wang,Caifang Ni
Objective: To develop S1-4 aptamer-conjugated citric acid-coated Fe3O4 nanoparticles and evaluate their targeting ability and magnetic hyperthermia effect against MCF-7 breast cancer cells.Methods: Citric acid-coated Fe3O4 nanoparticles were synthesized by chemical co-precipitation and subsequently conjugated with the S1-4 aptamer to fabricate S1-4 aptamer-conjugated citric acid-coated Fe3O4 nanoparticles. The nanoparticles were characterized by X-ray diffraction, transmission electron microscopy, dynamic light scattering, zeta potential analysis, Fourier transform infrared spectroscopy, and vibrating sample magnetometry. Biocompatibility was assessed in MCF-7 and MEF cells; cellular targeting was examined by Prussian blue staining; and the magnetic hyperthermia effect under an alternating magnetic field was evaluated by cell viability, live/dead staining, and apoptosis assays.Results: Compared with citric acid-coated Fe3O4 nanoparticles, S1-4 aptamer-conjugated citric acid-coated Fe3O4 nanoparticles exhibited a larger hydrodynamic diameter (17 ± 4 nm vs. 8 ± 3 nm) and a more negative surface charge (−26.7 ± 0.3 mV vs. −19.7 ± 0.5 mV). Fourier transform infrared spectroscopy confirmed successful aptamer conjugation. Both nanoparticles demonstrated good biocompatibility in MCF-7 and MEF cells. Prussian blue staining demonstrated stronger cellular uptake of S1-4 aptamer-conjugated citric acid-coated Fe3O4 nanoparticles in MCF-7 cells. Under alternating magnetic field exposure, S1-4 aptamer-conjugated citric acid-coated Fe3O4 nanoparticles produced a significantly greater hyperthermia effect than the controls, resulting in reduced cell proliferation and increased apoptosis in MCF-7 cells (P < 0.01).Conclusions: S1-4 aptamer-mediated Fe3O4 nanoparticles demonstrated active targeting ability and enhanced the antitumor effect of alternating magnetic field–mediated magnetic hyperthermia in breast cancer cells and maintained low cytotoxicity under the tested conditions, suggesting that they may be a feasible platform for targeted magnetic hyperthermia.
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DOI
PubMed
高影响因子
Scientific Reports
·
2017
·Vol. 7
·期 1
·1-8
·
IF 4.259
Yang Yufang,Shen Dongjun,Long Yijuan,Xie Zhixiong,Zheng Huzhi
Ficin is classified as a sulfhydryl protease isolated from the latex of fig trees. In most cases, a particular enzyme fits a few types of substrate and catalyzes one type of reaction. In this investigation, we found sufficient proofs for the intrinsic peroxidase-like activity of ficin and designed experiments to examine its effectiveness in a variety of scenarios. Ficin can transform peroxidase substrates to colored products in the existence of H 2 O 2 . Our results also indicate that the active sites of peroxidase-like activity of ficin are different from that of protease, which reveals that one enzyme may catalyze more than one kind of substrate to perform different types of reactions. On the basis of these findings, H 2 O 2 releasing from MCF-7 cells was detected successfully. Our findings support a wider application of ficin in biochemistry and open up the possibility of utilizing ficin as enzymatic mimics in biotechnology and environmental monitoring.
研究领域:
生物化学
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酶学
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生物技术
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环境监测
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产品关联
DOI
PubMed
高影响因子
Biosensors-Basel
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2021
·Vol. 11
·期 10
·378
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IF 5.519
Jinfeng Quan,Yihan Wang,Jialei Zhang,Kejing Huang,Xuemei Wang,Hui Jiang
Arch-cruciform DNA are self-assembled on AuNPs/VS2scaffold as a highly sensitive and selective electrochemical biosensor for michigan cancer foundation-7 (MCF-7) breast cancer cells. In the construction, arch DNA is formed using two single-strand DNA sequences embedded with the aptamer for MCF-7 cells. In the absence of MCF-7 cells, a cruciform DNA labeled with three terminal biotin is bound to the top of arch DNA, which further combines with streptavidin-labeled horseradish peroxidase (HRP) to catalyze the hydroquinone-H2O2reaction on the electrode surface. The presence of MCF-7 cells can release the cruciform DNA and reduce the amount of immobilized HRP, thus effectively inhibiting enzyme-mediated electrocatalysis. The electrochemical response of the sensor is negatively correlated with the concentration of MCF-7 cells, with a linear range of 10~1 × 105cells/mL, and a limit of detection as low as 5 cells/mL (S/N = 3). Through two-dimensional materials and enzyme-based dual signal amplification, this biosensor may pave new ways for the highly sensitive detection of tumor cells in real samples.Keywords:MCF-7 cells;electrochemistry;2-D materials;signal amplification;DNA assembly
研究领域:
生物传感
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肿瘤检测
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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 BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Jie Liu,Xinyu Li,Yushu Wu,Xinpeng Zhang,Xiangtai Wang,Lixia Yuan,Yanna Zhao,Min Liu
Imaging, silencing cancer-related microRNA, and chemotherapy-phototherapy (CTPT) combination therapy are crucial for cancer diagnosis and drug resistance overcoming. In this study, we designed a multifunctional DNA tetrahedron (MB-MUC1-TD) for the targeted delivery of combined daunorubicin (DAU) + toluidine blue O (TBO). The detection limit of miRNA-21 was determined to be 0.91 nM. The intercalation of DAU and TBO into MB-MUC1-TD was proved by spectroscopic and calorimetric methods. The thermodynamic parameters for the interactions of DAU and/or TBO with MB-MUC1-TD confirmed high drug loading. The first addition of TBO in the ternary system achieved a higher loading of both drugs and a more stable complex structure. Deoxyribonuclease I (DNase I) accelerated the release of DAU and/or TBO loaded in MB-MUC1-TD. Confocal laser scanning microscope demonstrated that MB-MUC1-TD exhibited good imaging ability for miRNA-21 to accurately identify cancer cells, and DAU/TBO was predominantly distributed within the nucleus of cancer cells. In vitro cytotoxicity showed better gene therapy efficacy of MB on MCF-7 cells, better biocompatibility of loaded DAU and TBO on LO2 cells, and stronger synergistic cytotoxicity of DAU + TBO on MCF-7/ADR cells. This study may establish a theoretical foundation for co-loading CTPT combination drugs based on multifunctional DNA nanostructures.
研究领域:
癌症研究
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纳米技术
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药学
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分子生物学
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治疗学
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产品关联
DOI
PubMed
高影响因子
BIOCHEMICAL PHARMACOLOGY
·
2025
·
IF 5.6
Mi Zhou,Jiahuan Hong,Xiaofeng Qiu,Zixian Xiong,Xiaoyong Liu,Zhuan Qin,Zhesi Luo,Qi Chen,Mianjie Lin,Ling Min,Xiaorong Yang,Xinmin Guo,Bin Xu,Jianwen Mao
Multidrug resistance (MDR) in tumor cells presents a significant challenge in cancer therapy. This study investigates the role of serum-derived extracellular vesicles (EVs) in mediating MDR during chemotherapeutic exposure. The findings indicate that short- or long-term co-incubation of doxorubicin (Dox)-pretreated serum derived EVs (EVs(S-PT)) caused drug-sensitive MCF-7 breast cancer cells to develop a MDR phenotype. In addition, serum EVs contain a high concentration of unglycosylated P-glycoprotein (P-gp). Chemotherapy treatment of tumor patients or exposure to chemotherapeutic drugs in vitro activates serum glycosyltransferases, inducing glycosylation of EVs P-gp and giving it drug-pumping activity. Furthermore, damage caused by Dox to the vascular endothelial barrier facilitates the crossing of serum EVs into the tumor microenvironment. These EVs are then taken up by tumor cells, providing them with access to a significant quantity of glycosylated P-gp proteins that possess transporter activity and the ability to evade degradation by the ubiquitin proteasome system. The results indicate that EVs(S-PT) transfers glycosylated P-gp across the damaged vascular endothelial barrier into MCF-7 cells and that these glycosylated P-gp remain intracellular for a long period of time, inducing MDR in the cells. Our study highlights a novel mechanism of acquired MDR and provides a potential avenue for therapeutic interventions targeting the serum EVs pathway in cancer therapy.
研究领域:
肿瘤学
·
细胞生物学
·
药理学
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产品关联
DOI
PubMed
高影响因子
Chemistry-An Asian Journal
·
2014
·Vol. 9
·期 8
·2272-2280
·
IF 3.935
Yan-Jie Guo,Fen Yang,Lu Zhang,Jiang Pi,Ji-Ye Cai,Pei-Hui Yang
Graphical Fighting cancer : Quercetin surface-functionalized germanium nanoparticles (Qu-GeNPs) with enhanced antioxidant and anticancer activity were synthesized by a simple method (see scheme). In vitro drug release of Qu from Qu-GeNPs indicated that Qu could principally be distributed around tumor tissues, and Qu-GeNPs were internalized by MCF-7 cells. A simple method for preparing quercetin surface-functionalized germanium nanoparticles (Qu-GeNPs) with enhanced antioxidant and anticancer activity is reported. Spherical germanium nanoparticles (GeNPs) were capped by quercetin (Qu) with a mean particle size of approximately 33 nm and were characterized by TEM, AFM, UV-visible absorption spectroscopy, FTIR, and XRD measurements. The in vitro drug release of Qu from the Qu-GeNPs indicated that Qu could principally be distributed around tumor tissues rather than in the normal section and Qu-GeNPs were internalized by MCF-7 cells. Their biological activity test results indicated that these Qu-GeNPs possessed stronger hydroxyl-scavenging effects and proliferative inhibition effect on MCF-7 cancer cells than quercetin, thus suggesting that the strategy to use GeNPs as a carrier of Qu could be an efficient way to achieve enhanced antioxidant and anticancer activity. In addition, Qu-GeNPs possessed a high apoptotic induction effect in cancer cells, especially in high dosages, and could arrest MCF-7 cells in the S phase.
研究领域:
纳米医学
·
药物递送
·
肿瘤学
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DOI
高影响因子
NATURAL PRODUCT RESEARCH
·
2018
·
IF 1.928
Jingjing Liang,Xiaogang Peng,Jia Zhou,Ming Zhou,Hanli Ruan
One new diarylheptanoid (3S)-3′, 4″-epoxy-1-(4′-hydroxylphenyl)-7-(3″-hydroxylphenyl) heptane-3-hydroxy (1), together with eleven known ones (2–12), was isolated from the fresh pericarps of Juglans sigillata. Their structures were elucidated on the basis of extensive spectroscopic methods, including HR-ESI-MS, 1D and 2D-NMR. All isolates were evaluated for their cytotoxic activities in vitro against the growth of human cancer cells lines HT-29 and MCF-7 by MTT assay.
研究领域:
植物化学
·
药理学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 21
·15549
·
IF 5.6
Weihong Lai,Jiaxin Chen,Xinjiao Gao,Xiaobao Jin,Gong Chen,Lianbao Ye
Chalcone is a common simple fragment of natural products with anticancer activity. In a previous study, the research group discovered a series of chalcone derivatives with stronger anticancer activities. To find better anticancer drugs, novel chalcone derivativesA1–A14,B1–B14have continuously been designed and synthesized. The antiproliferative activity of these compounds against breast cancer cells (MCF-7) was investigated by the Cell Counting Kit-8 (CCK-8) method with 5-fluorouracil (5-Fu) as the control drug. The results showed that compoundA14exhibited excellent antiproliferative ability compared to the control drug 5-Fu. Scratch experiments and cloning experiments further confirmed that compoundA14could inhibit the proliferation and colony formation activity of MCF-7 cells. In addition, molecular docking primarily explains the interaction between compound and protein. These results suggested that compoundA14could be a promising chalcone derivative for further anti-breast cancer research.Keywords:chalcones;synthesis;anti-breast cancer (MCF-7);molecular docking
研究领域:
药理学
·
肿瘤学
·
药物化学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）