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Luciana G Naso, Iker Badiola, Joana Marquez Clavijo, María Valcarcel, Clarisa Salado, Evelina G Ferrer, Patricia A M Williams
The anticancer and antimetastatic behavior of the flavonoid luteolin and its oxidovanadium(IV) complex [VO(lut)(H2O)2]Na·3H2O (VOlut) has been investigated. Considering that the complex displayed strong anticancer activity on MDAMB231 human breast cancer cell line we herein determined through in vitro assays that the complex would probably reduce breast cancer cell metastasis in a higher extent than the natural antioxidant. In the CT26 colon cancer cell line a stronger anticancer effect has also been determined for the complex (IC50 0...
September 24, 2016: Bioorganic & Medicinal Chemistry
Nuno Mendes, Francisco Tortosa, Andreia Valente, Fernanda Marques, António Matos, Tânia S Morais, Ana Isabel Tomaz, Fátima Gärtner, Maria Helena Garcia
Ruthenium-based anti-cancer compounds are proposed as viable alternatives that might circumvent the disadvantages of platinum-based drugs, the only metallodrugs in clinical use for chemotherapy. Organometallic complexes in particular hold great potential as alternative therapeutic agents since their cytotoxicity involve different modes of action and present reduced toxicity profiles. During the last few years our research group has been reporting on a series of organometallic ruthenium(II)-cyclopentadienyl complexes that showed important cytotoxicity against several cancer cell lines, surpassing cisplatin in activity...
September 22, 2016: Anti-cancer Agents in Medicinal Chemistry
Rashmi Holur Kadirareddy, Sujana Ghanta Vemuri, Uma Maheswari Devi Palempalli
Conjugated linoleic acid, a functional lipid, produced from Lactobacillus plantarum (LPCLA), has been demonstrated to possess apoptotic activity. The antiproliferative and apoptotic potential of LPCLA was here evaluated in vitro using the MDAMB231 human breast cancer cell line as a model system. Proliferation of MDA MB231 cells was inhibited with increasing concentrations of LPCLA with altered morphological features like cell detachment, rounding of cells and oligonucleosomal fragmentation of DNA. Flow cytometry confirmed the apoptotic potential of LPCLA by ANNEXIN V/PI double staining...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
JeongHee Lee, Hana Jin, Won Sup Lee, Arulkumar Nagappan, Yung Hyun Choi, Gon Sup Kim, JinMyung Jung, Chung Ho Ryu, Sung Chul Shin, Soon Chan Hong, Hye Jung Kim
Morin, a flavonoid found in figs and other Moraceae species, displays a variety of biological actions, exerting antioxidant, antiinflammatory and anticarcinogenic effects. Here, we investigated the anticancer activity of morin focusing on antiadhesive influence. We performed experiments with MDAMB231 human breast cancer cells. Morin inhibited TNFinduced cancer cell adhesion to human umbilical vein endothelial cells (HUVECs) without showing any toxicity. It further inhibited the expression of VCAM1 on MDAMB231 cells as well as HUVECs...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Siti Nur Hasyila Muhammad, Noor Fatmawati Mokhtar, Nik Soriani Yaacob
Reports indicate that 15deoxydelta12,14prostaglandinJ2 (15dPGJ2) has anticancer activities, but its mechanisms of action have yet to be fully elucidated. We therefore investigated the effects of 15dPGJ2 on the human breast cancer cell lines, MCF7 (estrogen receptor ERα+/ERβ+) and MDAMB231 (ERα/ERβ+). Cellular proliferation and cytotoxicity were determined using the 3(4,5dimethylthiazol2yl)2,5diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays while apoptosis was determined by fluorescence microscopy and flow cytometry using annexin Vpropidium iodide (PI) staining...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Wojciech G Lesniak, Samit Chatterjee, Matthew Gabrielson, Ala Lisok, Bryan Wharram, Martin G Pomper, Sridhar Nimmagadda
The programmed death protein 1 (PD-1) and programmed death-ligand 1 (PD-L1) pair is a major immune checkpoint pathway exploited by cancer cells to develop and maintain immune tolerance. With recent approvals of anti-PD-1 and anti-PD-L1 therapeutic antibodies, there is an urgent need for noninvasive detection methods to quantify dynamic PD-L1 expression in tumors and to evaluate the tumor response to immune modulation therapies. To address this need, we assessed [(64)Cu]atezolizumab for the detection of PD-L1 expression in tumors...
September 21, 2016: Bioconjugate Chemistry
Bridget T Kreger, Andrew L Dougherty, Kai Su Greene, Richard A Cerione, Marc A Antonyak
Extracellular vesicles (EVs), including exosomes and microvesicles (MVs), have emerged as a major form of intercellular communication, playing important roles in several physiological processes and diseases, including cancer. EVs generated by cancer cells contain a variety of proteins and RNA species that can be transferred between cancer cells as well as between cancer and non-transformed (normal) cells, thereby impacting a number of aspects of cancer progression. Here we show how oncogenic transformation influences the biogenesis and function of EVs using a mouse embryonic fibroblast (MEF) cell line that can be induced to express an oncogenic form of diffuse B cell lymphoma (Dbl)...
September 16, 2016: Journal of Biological Chemistry
Luciana Naso, Valeria R Martínez, Luis Lezama, Clarisa Salado, María Valcarcel, Evelina G Ferrer, Patricia A M Williams
The natural antioxidant flavonoid diosmin, found in citric fruits, showed low antioxidant properties among other flavonoids due to its structural characteristics and low cytotoxicity against lung (A549) and breast (T47D, SKBR3 and MDAMB231) cancer cell lines. The anticancer behavior has been improved by the metal complex generated with the flavonoid and the oxidovanadium(IV) ion. This new complex, [VO(dios)(OH)3]Na5·6H2O (VOdios), has been synthesized and characterized both in solid and solution states. The interaction of the metal ion through the sugar moiety of diosmin precluded the improvement of the antioxidant effects...
September 15, 2016: Bioorganic & Medicinal Chemistry
C Fourgeaud, S Derieux, S Mirshahi, S Besbes, J Chidiac, I Mahé, G Contant, M Pocard, J Soria, M Mirshahi
INTRODUCTION: Gastric signet ring cell carcinoma (GSRC) is a distinct entity among of other gastric cancer. With unknown etiopathology, their incidence is increasing and it presents a low sensitivity to chemotherapy. AIM: Here, we studied the expression of the heparanase (HPA) in cancer tissues from GSRC patients and several cancer cell lines. HPA is an endo-β-D-glucuronidase, capable of cleaving the lateral chains of heparan sulfate on cell surfaces and the extracellular matrix at acidic pH...
April 2016: Thrombosis Research
H Shaker, A S Rothmeier, C C Kirwan, W Ruf
INTRODUCTION: Tissue Factor (TF) promotes apoptosis-resistance and facilitates haematogenous metastasis. Cancer cells release TF-bearing microparticles (TF-MP) which have pro-coagulant activity. TF-MPs from cancer cells induce increase in TF expression and procoagulant activity of recipient endothelial cells. Drug resistance microparticles transfer between cancer cells, resulting in induction of recipient cell drug resistance, however transfer of TF-MPs between cancer cells has not been demonstrated...
April 2016: Thrombosis Research
Célia Fernandes, Sofia Monteiro, Ana Belchior, Fernanda Marques, Lurdes Gano, João D G Correia, Isabel Santos
INTRODUCTION: Radiolabeled bisphosphonates (BPs) have been used for bone imaging and delivery of β(-) emitting radionuclides for bone pain palliation. As a β(-) emitter, (188)Re has been considered particularly promising for bone metastases therapy. Aimed at finding innovative bone-seeking agents for systemic radiotherapy of bone metastases, we describe herein novel organometallic compounds of the type fac-[(188)Re(CO)3(k(3)-L)], (L=BP-containing chelator), their in vitro and in vivo stability, and their cellular damage in MDAMB231 cells, a metastatic breast cancer cell line...
February 2016: Nuclear Medicine and Biology
Samit Chatterjee, Wojciech G Lesniak, Matthew Gabrielson, Ala Lisok, Bryan Wharram, Polina Sysa-Shah, Babak Behnam Azad, Martin G Pomper, Sridhar Nimmagadda
Antibodies targeting the PD-1/PD-L1 immune checkpoint lead to tumor regression and improved survival in several cancers. PD-L1 expression in tumors may be predictive of response to checkpoint blockade therapy. Because tissue samples might not always be available to guide therapy, we developed and evaluated a humanized antibody for non-invasive imaging of PD-L1 expression in tumors. Radiolabeled [111In]PD-L1-mAb and near-infrared dye conjugated NIR-PD-L1-mAb imaging agents were developed using the mouse and human cross-reactive PD-L1 antibody MPDL3280A...
March 1, 2016: Oncotarget
Luciana G Naso, Luis Lezama, María Valcarcel, Clarisa Salado, Patricia Villacé, Danel Kortazar, Evelina G Ferrer, Patricia A M Williams
Chemotherapy using metal coordination compounds for cancer treatment is the work of the ongoing research. Continuing our research on the improvement of the anticancer activity of natural flavonoids by metal complexation, a coordination compound of the natural antioxidant flavone luteolin (lut) and the oxidovanadium(IV) cation has been synthesized and characterized. Using different physicochemical measurements some structural aspects of [VO(lut)(H2O)2]Na·3H2O (VOlut) were determined. The metal coordinated to two cis-deprotonated oxygen atoms (ArO(-)) of the ligand and two H2O molecules...
April 2016: Journal of Inorganic Biochemistry
Devesh S Agarwal, Hasitha Shilpa Anantaraju, Dharmarajan Sriram, Perumal Yogeeswari, Shankara H Nanjegowda, P Mallu, Rajeev Sakhuja
A series of bile acid (Cholic acid and Deoxycholic acid) aryl/heteroaryl amides linked via α-amino acid were synthesized and tested against 3 human cancer cell-lines (HT29, MDAMB231, U87MG) and 1 human normal cell line (HEK293T). Some of the conjugates showed promising results to be new anticancer agents with good in vitro results. More specifically, Cholic acid derivatives 6a (1.35 μM), 6c (1.41 μM) and 6m (4.52 μM) possessing phenyl, benzothiazole and 4-methylphenyl groups showed fairly good activity against the breast cancer cell line with respect to Cisplatin (7...
March 2016: Steroids
Irene Filippi, Fabio Carraro, Antonella Naldini
Inflammation and tumor hypoxia are intimately linked and breast cancer provides a typical example of an inflammation-linked malignant disease. Indeed, breast cancer progression is actively supported by inflammatory components, including IL-1β, and by the hypoxia-inducible factor- (HIF-) 1α. In spite of many attempts where the role of either IL-1β or HIF-1α was evaluated, detailed mechanisms for their effects on breast cancer cell migration under hypoxia are still unclear. We here report that IL-1β increased MDAMB231 cell migration under hypoxic conditions along with HIF-1α accumulation and upregulation of CXCR1, which is transcriptionally regulated by HIF-1α, as well as an increased expression of CXCL8 and NFκB...
2015: Mediators of Inflammation
Mariko Kikuchi, Keishi Yamashita, Mina Waraya, Naoko Minatani, Hideki Ushiku, Ken Kojo, Akira Ema, Yoshimasa Kosaka, Hiroshi Katoh, Norihiko Sengoku, Takumo Enomoto, Hirokazu Tanino, Masakazu Sawanobori, Masahiko Watanabe
Phenylbutyrate (PB) is a histone deacetylase antagonist that also exhibits antitumor activity. In this study, we used 7 breast cancer cell lines to identify biomarker candidates that predict PB sensitivity in breast cancer.Comprehensive gene expression profiles were compared using microarrays, and the importance of the identified genes to PB sensitivity was confirmed in gene transfection experiments. CRL and MDAMB453 cells were identified as PB-sensitive, while MDAMB231 cells were PB-resistant.RAB25 and ESRP1 were identified as key regulators of PB sensitivity, while ANKD1, ETS1, PTRF, IFI16 and KIAA1199 acted as PB resistance-related genes...
January 12, 2016: Oncotarget
Sreeraj G Pillai, Nupur Dasgupta, Chidananda M Siddappa, Mark A Watson, Timothy Fleming, Kathryn Trinkaus, Rebecca Aft
The presence of disseminated tumor cells (DTCs) in the bone marrow (BM) of breast cancer patients is prognostic for early relapse. In the present study, we analyzed the gene expression profiles from BM cells of breast cancer patients to identify molecular signatures associated with DTCs and their relevance to metastatic outcome. We analyzed BM from 30 patients with stage II/III breast cancer by gene expression profiling and correlated expression with metastatic disease development. A candidate gene, PITX2, was analyzed for expression and phenotype in breast cancer cell lines...
October 2015: Breast Cancer Research and Treatment
Tadanobu Nagaya, Kazuhide Sato, Toshiko Harada, Yuko Nakamura, Peter L Choyke, Hisataka Kobayashi
AIM: Triple-negative breast cancer (TNBC) is considered one of the most aggressive subtypes of breast cancer. Near infrared photoimmunotherapy (NIR-PIT) is a cancer treatment that employs an antibody-photosensitizer conjugate (APC) followed by exposure of NIR light for activating selective cytotoxicity on targeted cancer cells and may have application to TNBC. In order to minimize the dose of APC while maximizing the therapeutic effects, dosing of the APC and NIR light need to be optimized...
2015: PloS One
Yan-hong Wang, Wen-jie Zhao, Wei-juan Zheng, Li Mao, Hong-zhen Lian, Xin Hu, Zi-chun Hua
Intracellular metal elements exist in mammalian cells with the concentration range from picomoles per litre to micromoles per litre and play a considerable role in various biological procedures. Element provided by different species can influence the availability and distribution of the element in a cell and could lead to different biological effects on the cell's growth and function. Zinc as an abundant and widely distributed essential trace element, is involved in numerous and relevant physiological functions...
March 2016: Biological Trace Element Research
Leonor Côrte-Real, M Paula Robalo, Fernanda Marques, Guilherme Nogueira, Fernando Avecilla, Tiago J L Silva, Filipa C Santos, A Isabel Tomaz, M Helena Garcia, Andreia Valente
A new family of eight ruthenium(II)-cyclopentadienyl bipyridine derivatives, bearing nitrogen, sulfur, phosphorous and carbonyl sigma bonded coligands, has been synthesized. Compounds bearing nitrogen bonded coligands were found to be unstable in aqueous solution, while the others presented appropriate stabilities for the biologic assays and pursued for determination of IC50 values in ovarian (A2780) and breast (MCF7 and MDAMB231) human cancer cell lines. These studies were also carried out for the [5: HSA] and [6: HSA] adducts (HSA=human serum albumin) and a better performance was found for the first case...
September 2015: Journal of Inorganic Biochemistry
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