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https://www.readbyqxmd.com/read/29144008/a-copper-ii-phenanthroline-metallopeptide-that-targets-and-disrupts-mitochondrial-function-in-breast-cancer-stem-cells
#1
Kristine Laws Laws, Ganka Bineva-Todd, Arvin Eskandari, Chunxin Lu, Nicola O'Reilly, Kogularamanan Suntharalingam
The breast cancer stem cell (CSC) and bulk breast cancer cell potency of a series of metallopeptides, 1-4 containing dichloro(1,10-phenanthroline) copper(II) and various organelle-targeting peptide sequences, is reported. The mitochondrial-targeting metallopeptide, 1 exploits the higher mitochondrial load in breast CSCs over corresponding non-CSCs, and the vulnerability of breast CSCs to mitochondrial damage, to potently and selectivity kill breast CSCs. Strikingly, 1 reduces the formation and size of mammospheres to a better extent than salinomycin, an established CSC-potent agent...
November 16, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/29107689/semi-synthetic-salinomycin-analogs-exert-cytotoxic-activity-against-human-colorectal-cancer-stem-cells
#2
Johannes Klose, Sarah Kattner, Björn Borgström, Claudia Volz, Thomas Schmidt, Martin Schneider, Stina Oredsson, Daniel Strand, Alexis Ulrich
Salinomycin, a polyether antibiotic, is a well-known inhibitor of human cancer stem cells. Chemical modification of the allylic C20 hydroxyl of salinomycin has enabled access to synthetic analogs that display increased cytotoxic activity compared to the native structure. The aim of this study was to investigate the activity of a cohort of C20-O-acyl analogs of salinomycin on human colorectal cancer cell lines in vitro. Two human colorectal cancer cell lines (SW480 and SW620) were exposed to three C20-O-acylated analogs and salinomycin...
October 28, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29075110/polymer-lipid-hybrid-anti-her2-nanoparticles-for-targeted-salinomycin-delivery-to-her2-positive-breast-cancer-stem-cells-and-cancer-cells
#3
Jun Li, Wenqing Xu, Xiaoli Yuan, Huaiwen Chen, Hao Song, Bingquan Wang, Jun Han
PURPOSE: Breast cancer stem cells (CSCs) are responsible for the initiation, recurrence, and metastasis of breast cancer. Sufficient evidence has established that breast cancer cells can spontaneously turn into breast CSCs. Thus, it is essential to simultaneously target breast CSCs and cancer cells to maximize the efficacy of breast cancer therapy. HER2 has been found to be overexpressed in both breast CSCs and cancer cells. We developed salinomycin-loaded polymer-lipid hybrid anti-HER2 nanoparticles (Sali-NP-HER2) to target both HER2-positive breast CSCs and cancer cells...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29050441/the-physiological-response-of-broiler-chickens-to-the-dietary-supplementation-of-the-bacteriocin-nisin-and-ionophore-coccidiostats
#4
B Kieronczyk, M Sassek, E Pruszynska-Oszmalek, P Kolodziejski, M Rawski, S Swiatkiewicz, D Józefiak
The aim of this study was to investigate the effect of dietary supplementation with nisin alone or in combination with salinomycin or monensin on broiler chickens in terms of growth performance, selected blood parameters, digestive enzyme activity, apparent nutrient digestibility, and tibiotarsus mineralization, as well as selected gastrointestinal tract (GIT) organ weights, intestinal length, and central immune organ weights. Two independent experiments, each including 400 one-day-old female Ross 308 chicks differing in ionophore coccidiostats, i...
September 1, 2017: Poultry Science
https://www.readbyqxmd.com/read/29043812/amphiphilic-modulation-of-glycosylated-antitumor-ether-lipids-results-in-a-potent-triamino-scaffold-against-epithelial-cancer-cell-lines-and-bt474-cancer-stem-cells
#5
Temilolu Idowu, Pranati Samadder, Gilbert Arthur, Frank Schweizer
The problems of resistance to apoptosis-inducing drugs, recurrence, and metastases that have bedeviled cancer treatment have been attributed to the presence of cancer stem cells (CSCs) in tumors, and there is currently no clinically indicated drug for their eradication. We previously reported that glycosylated antitumor ether lipids (GAELs) display potent activity against CSCs. Here, we show that by carefully modulating the amphiphilic nature of a monoamine-based GAEL, we can generate a potent triamino scaffold that is active against a panel of hard-to-kill epithelial cancer cell lines (including triple-negative breast) and BT474 CSCs...
October 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28956164/trypanosoma-brucei-trypanocidal-and-cell-swelling-activities-of-lasalocid-acid
#6
Dietmar Steverding, Adam Huczyński
Chemotherapeutic treatment of human and animal trypanosomiasis is unsatisfactory because only a few drugs are available. As these drugs have poor efficacy and cause adverse reactions, more effective and tolerable medications are needed. As the polyether ionophore antibiotic lasalocid acid is used as medicated feed additive in cattle, the compound was tested for its trypanocidal and cytotoxic activity against bloodstream forms of Trypanosoma brucei and human myeloid HL-60 cells. The concentrations required of lasalocid acid to reduce the growth rate of trypanosomes by 50% and to kill the parasites were 1...
November 2017: Parasitology Research
https://www.readbyqxmd.com/read/28937680/salinomycin-kills-cancer-stem-cells-by-sequestering-iron-in-lysosomes
#7
Trang Thi Mai, Ahmed Hamaï, Antje Hienzsch, Tatiana Cañeque, Sebastian Müller, Julien Wicinski, Olivier Cabaud, Christine Leroy, Amandine David, Verónica Acevedo, Akihide Ryo, Christophe Ginestier, Daniel Birnbaum, Emmanuelle Charafe-Jauffret, Patrice Codogno, Maryam Mehrpour, Raphaël Rodriguez
Cancer stem cells (CSCs) represent a subset of cells within tumours that exhibit self-renewal properties and the capacity to seed tumours. CSCs are typically refractory to conventional treatments and have been associated to metastasis and relapse. Salinomycin operates as a selective agent against CSCs through mechanisms that remain elusive. Here, we provide evidence that a synthetic derivative of salinomycin, which we named ironomycin (AM5), exhibits a more potent and selective activity against breast CSCs in vitro and in vivo, by accumulating and sequestering iron in lysosomes...
October 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28933990/influence-of-salinomycin-treatment-on-division-and-movement-of-individual-cancer-cells-cultured-in-normoxia-or-hypoxia-evaluated-with-time-lapse-digital-holographic-microscopy
#8
Sofia Kamlund, Daniel Strand, Birgit Janicke, Kersti Alm, Stina Oredsson
Most studies on new cancer drugs are based on population-derived data, where the absence of response of a small population may pass unnoticed. Thus, individual longitudinal tracking of cells is important for the future development of efficient cancer treatments. We have used digital holographic microscopy to track individual JIMT-1 human breast cancer cells and L929 mouse fibroblast cultivated in normoxia or hypoxia. In addition, JIMT-1 cells were treated with salinomycin, a cancer stem cell targeting compound...
September 21, 2017: Cell Cycle
https://www.readbyqxmd.com/read/28927939/autophagy-inhibition-enhances-antiproliferative-effect-of-salinomycin-in-pancreatic-cancer-cells
#9
Sho Endo, Kohei Nakata, Akiko Sagara, Kazuhiro Koikawa, Yohei Ando, Shin Kibe, Shin Takesue, Hiromichi Nakayama, Toshiya Abe, Takashi Okumura, Taiki Moriyama, Yoshihiro Miyasaka, Kenoki Ohuchida, Takao Ohtsuka, Kazuhiro Mizumoto, Masafumi Nakamura
BACKGROUND: Salinomycin has cytotoxic effects on various types of malignancy and induces autophagy. However, it has not been clarified whether autophagy induced by salinomycin treatment has a protective or cytotoxic role. We investigated whether salinomycin affects autophagy in pancreatic cancer cells and whether autophagy induced by salinomycin treatment has a protective or cytotoxic role in these cells. METHODS: We investigated the effect of salinomycin using three pancreatic cancer cell lines...
August 25, 2017: Pancreatology: Official Journal of the International Association of Pancreatology (IAP) ... [et Al.]
https://www.readbyqxmd.com/read/28832761/salinomycin-enhances-doxorubicin-sensitivity-through-reversing-the-epithelial-mesenchymal-transition-of-cholangiocarcinoma-cells-by-regulating-ark5
#10
Z Yu, H Cheng, H Zhu, M Cao, C Lu, S Bao, Y Pan, Y Li
Chemotherapy response rates in patients with cholangiocarcinoma remain low, primarily due to the development of drug resistance. Epithelial-mesenchymal transition (EMT) of cancer cells is widely accepted to be important for metastasis and progression, but it has also been linked to the development of chemoresistance. Salinomycin (an antibiotic) has shown some potential as a chemotherapeutic agent as it selectively kills cancer stem cells, and has been hypothesized to block the EMT process. In this study, we investigated whether salinomycin could reverse the chemoresistance of cholangiocarcinoma cells to the chemotherapy drug doxorubicin...
August 17, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28812299/conversion-of-the-high-yield-salinomycin-producer-streptomyces-albus-bk3-25-into-a-surrogate-host-for-polyketide-production
#11
Xiaojie Zhang, Chenyang Lu, Linquan Bai
An ideal surrogate host for heterologous production of various natural products is expected to have efficient nutrient utilization, fast growth, abundant precursors and energy supply, and a pronounced gene expression. Streptomyces albus BK3-25 is a high-yield industrial strain producing type-I polyketide salinomycin, with a unique ability of bean oil utilization. Its potential of being a surrogate host for heterologous production of PKS was engineered and evaluated herein. Firstly, introduction of a three-gene cassette for the biosynthesis of ethylmalonyl-CoA resulted in accumulation of ethylmalonyl-CoA precursor and salinomycin, and subsequent deletion of the salinomycin biosynthetic gene cluster resulted in a host with rich supplies of common polyketide precursors, including malonyl-CoA, methylmalonyl-CoA, and ethylmalonyl-CoA...
August 14, 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/28792977/determination-of-regulatory-ionophore-coccidiostat-residues-in-feedstuffs-at-carry-over-levels-by-liquid-chromatography-mass-spectrometry
#12
Loredana Annunziata, Pierina Visciano, Arianna Stramenga, Maria Novella Colagrande, Guido Campana, Giampiero Scortichini, Giacomo Migliorati, Dario Compagnone
In this study samples of feedstuffs were collected from different feed mills and animal farms located in central Italy and analyzed for ionophore coccidiostat residues at carry-over levels by liquid chromatography-mass spectrometry. Since unavoidable cross-contamination of feedstuffs may occur during their production as well as distribution and storage, the collection of samples covered all these different stages. Residues of lasalocid, monensin, salinomycin and maduramicin were detected in 32.4% of samples, both at production and storage level...
2017: PloS One
https://www.readbyqxmd.com/read/28766685/salinomycin-s-potential-to-eliminate-glioblastoma-stem-cells-and-treat-glioblastoma-multiforme-review
#13
Justin W Magrath, Yonghyun Kim
Glioblastoma multiforme (GBM) is the most common and deadliest form of primary brain tumor. Despite treatment with surgery, radiotherapy, and chemotherapy with the drug temozolomide, the expected survival after diagnosis remains low. The median survival is only 14.6 months and the two-year survival is a mere 30%. One reason for this is the heterogeneity of GBM including the presence of glioblastoma cancer stem cells (GSCs). GSCs are a subset of cells with the unique ability to proliferate, differentiate, and create tumors...
September 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28766151/anticoccidial-effects-of-artemisia-annua-ethanolic-extract-prevention-simultaneous-challenge-medication-and-treatment
#14
Ahmadreza Fatemi, Keramat Asasi, Seyed Mostafa Razavi
The effect of Artemisia annua ethanolic extract (AE) as a potential source of herbal anticoccidial activity was investigated on experimental coccidiosis in chicken. One hundred ninety-two one-day-old chicks were divided in to 8 groups (n = 24) including AE prevention group, AE-treated group, simultaneously challenged AE-medicated group, challenged-untreated group (positive control), unchallenged-untreated group (negative control), salinomycine prevention group, salinomycine-treated group, and simultaneously challenged salinomycine-medicated group, in a completely randomized design...
August 1, 2017: Parasitology Research
https://www.readbyqxmd.com/read/28748373/novel-combination-of-salinomycin-and-resveratrol-synergistically-enhances-the-anti-proliferative-and-pro-apoptotic-effects-on-human-breast-cancer-cells
#15
Jayant Dewangan, Divya Tandon, Sonal Srivastava, Ajeet Kumar Verma, Ashok Yapuri, Srikanta Kumar Rath
Resveratrol (RES) is a natural polyphenol having anti-proliferative activity against breast cancer cells. RES in combination with other chemo modulatory agents, minimizes toxicity and increases efficacy of the treatment. Salinomycin (SAL), a monocarboxylic polyether ionophore is known for selectively targeting breast cancer stem cells. Purpose of the present study was to investigate whether RES in combination with SAL exerts synergistic anti-proliferative activity on breast cancer cells. We further evaluated the molecular mechanism behind SAL and RES mediated cell death...
October 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28746279/thy1-cd90-expression-is-elevated-in-radiation-induced-periprosthetic-capsular-contracture-implication-for-novel-therapeutics
#16
Trevor C Hansen, Collynn F Woeller, Shannon H Lacy, Peter F Koltz, Howard N Langstein, Richard P Phipps
BACKGROUND: Capsular contracture is a devastating complication of postmastectomy implant-based breast reconstruction. Unfortunately, capsular contracture rates are drastically increased by targeted radiotherapy, a standard postmastectomy treatment. Thy1 (also called CD90) is important in myofibroblast differentiation and scar tissue formation. However, the impact of radiotherapy on Thy1 expression and the role of Thy1 in capsular contracture are unknown. METHODS: The authors analyzed Thy1 expression in primary human capsular tissue and primary fibroblast explants by real-time quantitative polymerase chain reaction, Western blotting, and immunohistochemistry...
August 2017: Plastic and Reconstructive Surgery
https://www.readbyqxmd.com/read/28693187/salinomycin-inhibits-canine-mammary-carcinoma-in-vitro-by-targeting-cancer-stem-cells
#17
Hongchao Du, Bin Zhou, Hong Zhang, Yipeng Jin, Di Zhang, Degui Lin
Salinomycin (SAL), a polyether ionophore antibiotic, has been demonstrated to selectively kill cancer stem cells (CSCs) in various types of human tumor. The aim of the present study was to investigate the effects of SAL on canine mammary CSCs. CSCs in canine mammary carcinoma cell lines (CMT7364 and CIPp) were identified using a sphere formation assay and flow cytometry. The chemoresistance, invasive potential and expression of stem cell-associated proteins of these spheres was then analyzed. This demonstrated that the spheres exhibited characteristics of CSCs, including a cluster of differentiation (CD)44(+)/CD24(-/low) phenotype, upregulation of Wnt/β-catenin signaling pathway-associated proteins and chemoresistance...
July 2017: Oncology Letters
https://www.readbyqxmd.com/read/28692437/codelivery-of-salinomycin-and-docetaxel-using-poly-d-l-lactic-co-glycolic-acid-poly-ethylene-glycol-nanoparticles-to-target-both-gastric-cancer-cells-and-cancer-stem-cells
#18
Lan Li, Dejun Cui, Limin Ye, Yu Li, Liyi Zhu, Lanqun Yang, Banjun Bai, Zhao Nie, Jie Gao, Yu Cao
Cancer stem cells (CSCs) in gastric cancer (GC) have been established recently as key therapeutic targets for the successful treatment of GC. Emerging evidence suggests that both CSCs and cancer cells should be eradicated to achieve optimal therapeutic efficacy. In the present study, salinomycin, which has been reported to kill CSCs, was used in combination with docetaxel, a chemotherapeutic drug that is used as first-line therapy in GC, to eradicate both GC stem cells (SCs) and cancer cells. Salinomycin and docetaxel were loaded separately into poly(D,L-lactic-co-glycolic acid)-poly(ethylene glycol) nanoparticles of ∼140 nm with a narrow size distribution, high drug loading, and sustained drug release...
July 7, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28688275/design-and-synthesis-of-conformationally-constrained-salinomycin-derivatives
#19
Wenxuan Zhang, Jun Wu, Bo Li, Xu Lian, Jie Xia, Qi Zhou, Song Wu
Two conformationally restricted salinomycin derivatives by tethering the hydroxyl groups at C1 and C20 with different chain length were designed and synthesized. The cyclic derivatives showed better biological activities than C1/C20 modified derivatives, indicating the importance of the compact conformation for the ion binding capacity. In addition, the length of the connective chain plays critical role in the biological activities, thus cyclic the derivative 7 preserved some pharmacological activity but derivative 5 with two carbon atom shorter chain showed significantly reduced activity...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28676857/salinomycin-exerts-anticancer-effects-on-pc-3-cells-and-pc-3-derived-cancer-stem-cells-in-vitro-and-in-vivo
#20
Yunsheng Zhang, Luogen Liu, Fang Li, Tao Wu, Hongtao Jiang, Xianxun Jiang, Xiaobo Du, Yi Wang
Salinomycin is an antibiotic isolated from Streptomyces albus that selectively kills cancer stem cells (CSCs). However, the antitumor mechanism of salinomycin is unclear. This study investigated the chemotherapeutic efficacy of salinomycin in human prostate cancer PC-3 cells. We found that cytotoxicity of salinomycin to PC-3 cells was stronger than to nonmalignant prostate cell RWPE-1, and exposure to salinomycin induced G2/M phage arrest and apoptosis of PC-3 cells. A mechanistic study found salinomycin suppressed Wnt/β-catenin pathway to induce apoptosis of PC-3 cells...
2017: BioMed Research International
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