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Science China Chemistry 2013年第6期56卷 702-715页

作者： PANG ChunCheng SUN ChuanWen WANG Jing XIAO Di DING Li BU HongFei College of Life and Environment Sciences Shanghai Normal University

A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives （II） have been designed and synthesized. The target com- pounds have been identified by elemental analysis and spectral （1H NMR, IR, and MS） data and the absolute configuration of compound （IIl） was confirmed by single crystal X-ray diffraction. The cytotoxicity of the target compounds have been evalu- ated in vitro against two human breast cancer cell lines MCF-7 and MDA-MB-231 by MTT assay. Most compounds exhibited good inhibition, and compounds II21 （IC50 = 4.7 μM for MCF-7 and IC50 = 9.3 μM for MDA-MB-231）, 1133 （IC50 = 2.4 μM for MCF-7 and IC50 = 4.2 gM for MDA-MB-231） and 114o （IC50 = 3.3 μM for MCF-7 and IC5o =8.6 μM for MDA-MB-231） dis- played better inhibitory activity than 5-fluorouracil （IC50 = 4.8 μM for MCF-7 and IC50 = 9.6 I, tM for MDA-MB-231, respec- tively）. Flow cytometric analysis and DNA fragmentation suggest that II33 is cytotoxic and able to induce the apoptosis of MCF-7 cells. The fluorescence properties of compounds IIl, II6, II11,II16, II23, Il2s, and II3s were also studied and compound Ilzs afforded the highest photoluminescence quantum yield （38%）.

关键词： pyrazolopyridine synthesis crystal structure breast cancer cells cytotoxicity evaluation apoptosis fluorescence prop-erties

Piperine suppresses growth and migration of human breast cancer cells through attenuation of Rac1 expression

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Asian Pacific Journal of Tropical Biomedicine 2022年第1期12卷 39-46页

作者： Benjaporn Buranrat Mutita Junking Faculty of Medicine Mahasarakham UniversityMuang DistrictMaha Sarakham 44000Thailand Division of Molecular Medicine Research DepartmentFaculty of MedicineSiriraj HospitalMahidol UniversityBangkok 10700Thailand

Objective:To investigate the effect of piperine on human breast cancer ***:The effect of piperine on proliferation and migration of human breast cancer cells,MCF-7 and MDA-MB-231,was investigated using colony formation assays,wound healing assays,Matrigel migration assays,flow cytometry,RT-qPCR,and Western blotting ***:Piperine inhibited the growth of MCF-7 and MDA-MB-231 cells and suppressed colony *** reduction at the G_(0)/G_(1) phase and cell arrest at the G_(2)/M phase were observed in breast cancer ***,the significant effect was only demonstrated in MDA-MB-231 ***,cancer cell migration was suppressed by piperine at low ***-qPCR and Western blotting assays showed that piperine downregulated Rac1 gene and protein ***:Piperine could inhibit growth and migration of breast cancer cells by reducing Rac1 gene and protein expression.

关键词： Piperine breast cancer cells Rac1 Cell cycle Cell migration MCF-7 MDA-MB-231

The Influence of Phorbol Ester on the Effect of Tamoxifen in breast cancer cells

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2001年第2期21卷 138-139页

作者：蔡开琳陈道达王国斌卢晓明张锦辉田元 Department of General Surgery Xiehe Hospital Tongji Medical College Huazhong University of Science and Technology Wuhan

To investigate the correlation between the activity of kinases in the growth factor signal transduction pathway and the development of resistance of breast cancer to tamoxifen, reporter gene regulated by the regulating fragment of CCD1 was transfected into the MCF 7 cells, and the influence of tamoxifen on the reporter gene expression was examined under different conditions of TPA treatment. Our results showed that the reporter gene expression was inhibited by tamoxifen and promoted by TPA. Furthermore, tamoxifen exerts an agonist effect on the reporter gene expression when the cells was treated by TPA previously for 12 h. It is concluded that TPA could induce estrogen like effect of tamoxifen on estrogen receptor positive breast cancer cells and it may be one of the mechanisms responsible for the development of tamoxifen resistance.

关键词： tamoxifen phorbol ester breast cancer cells

Extracellular cell matrix stiffness-driven drug resistance of breast cancer cells via EGFR activation

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Mechanobiology in Medicine 2023年第2期1卷 67-76页

作者： Tingting Li Yichao Li Hao Wu Chong Peng Jiawen Wang Shihuan Chen Tian Zhao Shun Li Xiang Qin Yiyao Liu Department of Pharmacy Personalized Drug Therapy Key Laboratory of Sichuan ProvinceSichuan Provincial People's HospitalSchool of Life Science and TechnologyUniversity of Electronic Science and Technology of ChinaChengdu 610054PR China TCM Regulating Metabolic Diseases Key Laboratory of Sichuan Province Hospital of Chengdu University of Traditional Chinese MedicineNo.39 Shi-er-qiao RoadChengdu 610072SichuanPR China Chongqing Engineering Laboratory of Nano/Micro Biomedical Detection Technology Chongqing University of Science and TechnologyChongqing 401331PR China

Tumor progression is accompanied by complex structural changes in the extracellular matrix(ECM),which decrease the effective exposure of tumors to *** cancer are highly heterogeneous with a typically high degree of ECM remodeling and ***,it is especially important to explore the influence of ECM stiffness on breast cancer ***,we fabricated 3D Methacrylate Gelatin(GelMA)hydrogels with varying stiffness by photo-crosslinking to simulate the change of tissue stiffness during the development of breast *** 3D hydrogels were used to evaluate how MDA-MB-231 cells responded to the chemotherapy drug doxorubicin(DOX),the mechanical regulatory mechanism involved has also been *** findings demonstrated that 15%GelMA hydrogel(9 kPa)increased the activity of EGFR to block the Hippo signaling pathway and activate Yes-associated protein(YAP).Activated YAP allowed cytosolic EGFR transport into the nucleus via binding with it,up-regulated the expression of their respective transcriptional targets,and thus generates drug ***,our study implicates that stiffness-dependent EGFR activation plays an important role in breast cancer drug resistance,indicating that targeting of both YAP and EGFR signals may present a promising therapeutic strategy for ECM stiffness-induced drug resistance.

关键词： breast cancer cells ECM stiffness Drug resistance EGFR YAP

Effect of Estrogen on Telomerase Activity in Human breast cancer cells

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2003年第3期23卷 286-287,293页

作者：高金波陈道达田元张锦辉蔡开琳 Department of General Surgery

To investigate the effects of estrogen(E 2) on telomerase activity and its mechanism in human breast cancer cells, estrogen receptor positive MCF-7 cells were treated with different concentrations of E 2 Telomerase activity was measured by using TRAP-ELISA method, the cell cycle phases analyzed by using flow cytometry, and the expression of Cyclin D 1 detected by using immunohistochemistry method The results showed that telomerase activity levels were increased in MCF-7 cells treated with 10 -8 mol/L E 2 during the observed period ( P cells treated with 10 -8 mol/L E 2 were changed significantly: G 0/G 1 phase decreased from 60 52% to 50 93%, S phase increased from 29 03% to 30 83%; However, the expression of Cyclin D 1 was decreased It was concluded that estrogen can upregulate telomerase activity of MCF-7 cells, and the effect can be blocked by antiestrogen tamoxifen Its mechanism may be closely associated with modulation of cell cycle phases

关键词： breast cancer cells telomerase estrogen Cyclin D 1

In Vivo Selection of Phage Sequences and Characterization of Peptide-specific Binding to breast cancer cells

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Chinese Journal of Clinical Oncology 2008年第2期5卷 128-131页

作者： Rui Wang Lin Zhang Hongkai Zhang Xiyin Wei Yi Yang Shiwu Zhang Jing Wu Min Wu Youjia Cao Ruifang Niu Central Laboratory of Oncology Key Laboratory of Breast Cancer Prevention and Therapy Tianjin Medical University Ministry of Education. Tianjin Medical University Cancer Institute and Hospital Tianjin 300060 China. College of Life Sciences Nankai University Tianjin 300060 China. Molecular pathology Laboratory Tianjin Medical University Cancer Institute and Hospital Tianjin 300060 China.

OBJECTIVE To screen specific polypeptide target binding to breast cancer xenografts in vivo from a phage-displayed peptide library in order to provide peptide sequences for breast cancer tumor-targeting diagnosis and therapy. METHODS A mouse model for carrying breast cancer xenografts was established using Tientsin Albinao Ⅱ mice （TA Ⅱ）. A 12-peptide library was biopanned through 4 rounds. Phages were recovered and titrated from tumor xenografts and control tissue （liver）. The distribution of phages was detected by immunohistochemical staining. RESULTS Phage homing to breast cancer was enriched through 4 rounds of biopanning, being 14-fold of that recovered from liver tissue. A peptide sequence, ASANPFPTKALL was characterized by randomly picked-up clones which appeared most frequently. Immunohistochemical staining revealed phage localization in cancer xenografts 40 min after injection of the enriched phages. When a specific phage was tested individually, the phage reclaimed from breast cancer xenografts was 14 times as those from control tissues. CONCLUSION Tumor-specific homing peptides may provide an effective tool for breast cancer target therapy. The in vivo phage display selection technique employed in this study was feasible and applicable to screening peptides that home to breast cells.

关键词： phage display breast cancer cells in vivo selection.

A novel anticancer property of Lycium barbarum polysaccharide in triggering ferroptosis of breast cancer cells

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2022年第4期23卷 286-299页

作者： Xing DU Jingjing ZHANG Ling LIU Bo XU Hang HAN Wenjie DAI Xiuying PEI Xufeng FU Shaozhang HOU Key Laboratory of Fertility Preservation and Maintenance of Ministry of Education School of Basic Medical SciencesNingxia Medical UniversityYinchuan 750004China Department of Clinical Pathology School of Basic Medical SciencesNingxia Medical UniversityYinchuan 750004China

breast cancer is one of the most malignant tumors and is associated with high mortality rates among *** barbarum polysaccharide(LBP)is an extract from the fruits of the traditional Chinese herb,*** is a promising anticancer drug,due to its high activity and low *** it has anticancer properties,its mechanisms of action have not been fully ***,which is a novel anticancer strategy,is a cell death mechanism that relies on iron-dependent lipid reactive oxygen species(ROS)*** this study,human breast cancer cells(Michigan cancer Foundation-7(MCF-7)and MD Anderson-Metastatic breast-231(MDA-MB-231))were treated with *** inhibited their viability and proliferation in association with high levels of ***,we aimed to ascertain whether LBP reduced cell viability through *** found that the structure and function of mitochondria,lipid peroxidation,and expression of solute carrier family 7 member 11(SLC7 A11,also known as x CT,the light-chain subunit of cystine/glutamate antiporter system X_(c)^(-))and glutathione peroxidase 4(GPX4)were altered by ***,the ferroptosis inhibitor,Ferrostatin-1(Fer-1),rescued LBP-induced ferroptosis-associated events including reduced cell viability and glutathione(GSH)production,accumulation of intracellular free divalent iron ions and malondialdehyde(MDA),and down-regulation of the expression of x CT and ***(x CT inhibitor)and RSL3(GPX4 inhibitor)inhibited the expression of x CT and GPX4,respectively,which was lower after the co-treatment of LBP with Erastin and *** results suggest that LBP effectively prevents breast cancer cell proliferation and promotes ferroptosis via the x CT/GPX4 ***,LBP exhibits novel anticancer properties by triggering ferroptosis,and may be a potential therapeutic option for breast cancer.

关键词： Lycium barbarum polysaccharide Ferroptosis breast cancer cells xCT Glutathione peroxidase 4(GPX4)

IN SITU IMAGING OF breast cancer cells USING GREEN SEMICONDUCTOR QUANTUM DOTS

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Transactions of Nanjing University of Aeronautics and Astronautics 2010年第1期27卷 13-20页

作者：许恒毅 Zoraida P. Aguilar 苏怀朋 Benjamin J. Jones John. D. Dixon 熊勇华魏华 Andrew Y. Wang 南昌大学食品科学与技术国家重点实验室 Ocean NanoTech LLC 2143 Worth LaneSpringdaleusa72764

The breast cancer is the most common cause of cancer death in women. To establish an early stage in situ imaging of breast cancer cells, green quantum dots （QDs） are used as a fluorescent signal generator. The QDs based imaging of breast cancer cells involves anti-HER2/neu antibody for labeling the over expressed HER2 on the surface of breast cancer cells. The complete assay involves breast cancer cells, biotin labeled antibody and streptavidin conjugated QDs. The breast cancer cells are grown in culture plates and exposed to the biotin labeled antibodies, and then exposed to streptavidin labeled QDs to utilize the strong and stable biotin-streptavidin interaction. Fluorescent images of the complete assay for breast cancer cells are evaluated on a microscope with a UV light source. Results show that the breast cancer cells in the complete assay are used as fluorescent cells with brighter signals compared with those labeled by the organic dye using similar parameters and the same number of cells.

关键词： in situ processing quantum optics breast cancer cells non-specific binding immuno-histochemical imaging

Cu(II) Benzoylpyridine Thiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against breast cancer cells

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Open Journal of Inorganic Chemistry 2016年第2期6卷 146-154页

作者： Jennifer D. Conner Wathsala Medawala Madison T. Stephens William H. Morris Joseph E. Deweese Patrick L. Kent Jeffery J. Rice Xiaohua Jiang Edward C. Lisic Department of Chemistry Tennessee Technological University Cookeville TN USA Department of Pharmaceutical Sciences Lipscomb University Nashville TN USA Department of Biochemistry Vanderbilt University Nashville TN USA Department of Chemical Engineering Tennessee Technological University Cookeville TN USA

The focus of this research is on the study of a series of copper (II) benzoylpyridine thiosemicarbazone complexes. Of the six benzoylpyridine thiosemicarbazone ligands used in this study, two are reported for the first time;2-benzoylpyridine tert-butyl thiosemicarbazone (BZP-tBTSC), and 2-benzoylpyridine benzyl thiosemicarbazone (BZP-BzTSC). Once characterized by NMR, melting point, and MS, these mono-anionic tridentate ligands were then reacted with Cu2+ to form the new square planar metal complexes [Cu(BZP-tBTSC)Cl] and [Cu(BZP-BzTSC)Cl]. All of the copper complexes display marked inhibition of human topoisomerase IIα. The [Cu(BZP-tBTSC)Cl] complex shows marked activity against human breast cancer cell lines.

关键词： Topoisomerase IIα Alpha-(N)-Heterocyclic Thiosemicarbazones breast cancer cells

Gelsolin is a novel coactivator of ERa in Her-2/neu over-expressing breast cancer cells

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Gelsolin is a novel coactivator of ERa in Her-2/neu over-exp...