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Gonzalo J Diaz, Yandy Aguillón, Amparo Cortés
A study was conducted to evaluate the effects of feeding salinomycin at the recommended prophylactic level, and at 2 and 3 times this level, to finishing male broilers (d 21 to 38). Four treatment groups were given the experimental diets containing 0, 60, 120, or 180 parts per million (ppm) salinomycin from d 21 to 38. Performance, relative organ weights, selected serum enzymes, and salinomycin residues in liver, muscle, and serum were determined. Salinomycin supplementation had no effect on body weight, feed intake, or feed conversion, and caused no overt signs of toxicity...
March 15, 2018: Poultry Science
Yun-Jung Choi, Sangiliyandi Gurunathan, Jin-Hoi Kim
The use of graphene to target and eliminate cancer stem cells (CSCs) is an alternative approach to conventional chemotherapy. We show the biomolecule-mediated synthesis of reduced graphene oxide-silver nanoparticle nanocomposites (rGO-Ag) using R-phycoerythrin (RPE); the resulting RPE-rGO-Ag was evaluated in human ovarian cancer cells and ovarian cancer stem cells (OvCSCs). The synthesized RPE-rGO-Ag nanocomposite (referred to as rGO-Ag) was characterized using various analytical techniques. rGO-Ag showed significant toxicity towards both ovarian cancer cells and OvCSCs...
March 1, 2018: International Journal of Molecular Sciences
Francesca Perut, Francesca Vittoria Sbrana, Sofia Avnet, Angelo De Milito, Nicola Baldini
Chondrosarcoma (CS) is a cartilage malignancy of adulthood that is treated by surgery alone, since chemotherapy is considered ineffective. Unfortunately, a large proportion of patients with CS develop lung metastases, and several die of the disease. In this study, we compared 3D-spheroid cultures and conventional cell monolayer models in order to identify the best way to select anticancer agents that could be effective for the systemic control of CS. Using SW1353 cells, we developed a three-dimensional (3D) in vitro culture model to mimic in vivo features of CS microenvironment and evaluated the efficacy of different drugs to modulate CS cell proliferation and survival in 2D vs...
February 22, 2018: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
Yu Li, Qiuyan Shi, Jiajia Shao, Yaping Yuan, Zhigang Yang, Shizhen Chen, Xin Zhou, Shijun Wen, Zhong-Xing Jiang
To improve the druggability of salinomycin, a 20-epi-amino-20-deoxysalinomycin derivatives library was synthesized with high efficacy from which a few salinomycin derivatives with high potency and selectivity were identified through comprehensive cytotoxicity assay, including a fluorine-19 magnetic resonance sensitive tool molecule. Using a K-ras cellular model, salinomycin and its derivatives showed different molecular mode of action from literature reports. These results would be valuable for developing salinomycin-based cancer therapy...
February 5, 2018: European Journal of Medicinal Chemistry
Dewen Leng, Jun Hu, Xiaolong Huang, Wei He, Yuan Wang, Mei Liu
Initiation and recurrence of lung cancer, the most fatal cancer worldwide, are attributed to lung cancer stem cells (CSCs). Evidence suggests that cancer cells can be turned into CSCs in a spontaneous way, and therefore simultaneous elimination of lung CSCs and cancer cells is crucial to achieve effective therapy of lung cancer. In lung cancer, epidermal growth factor receptor (EGFR) is overexpressed in both CSCs and cancer cells. The present study developed salinomycin poly(ethylene glycol) 2000-distearoylphosphatidylethanolamine nanomicelles conjugated with EGFR aptamers (M-SAL-EGFR) to kill lung CSCs and cancer cells...
August 1, 2018: Journal of Nanoscience and Nanotechnology
Małgorzata Olejnik, Lidia Radko, Piotr Jedziniak
RATIONALE: Salinomycin is an ionophore antibiotic with potential anti-cancer activity. The history of its use in veterinary medicine show large differences in species susceptibility to its toxicity. At the same time, the results of so-far research suggest the correlation between the extent and pathways of ionophore biotransformation and its toxicity. The biotransformation pattern of salinomycin has not been studied so far. METHODS: The extracts from culture media of human hepatoma cells (HepG2) exposed to salinomycin were analysed with two mass spectrometry techniques...
February 14, 2018: Rapid Communications in Mass Spectrometry: RCM
Thomas Gehrke, Stephan Hackenberg, Bülent Polat, Gisela Wohlleben, Rudolf Hagen, Norbert Kleinsasser, Agmal Scherzad
The antibiotic drug salinomycin has been reported to mediate cancer cell-specific cytotoxicity, especially regarding cancer stem cells. Since salinomycin has also been reported to arrest cancer cells in the G2 phase, it may have possible radiosensitizing effects. Radiotherapy is a common therapeutic strategy for head and neck squamous cell carcinoma (HNSCC). The aim of the present study was to evaluate a possible influence of salinomycin on the radiosensitivity of the HNSCC cell line HLaC-78 in vitro. HLaC-78 cells were incubated with 5 µM salinomycin or control medium for 24 h and then received 5-Gy irradiation...
February 13, 2018: Oncology Reports
Jiang Jiang, Hailong Li, Eskandar Qaed, Jing Zhang, Yushu Song, Rong Wu, Xinmiao Bu, Qinyan Wang, Zeyao Tang
Since Salinomycin (Sal) emerged its ability to target breast cancer stem cells in 2009, numerous experiments have been carried out to test Sal's anticancer effects. What deserve to be mentioned is that Sal can efficiently induce proliferation inhibition, cell death and metastasis suppression against human cancers from different origins both in vivo and in vitro without causing serious side effects as the conventional chemotherapeutical drugs on the body. There may be novel cell death pathways involving the anticancer effects of Sal except the conventional pathways, such as autophagic pathway...
February 13, 2018: Journal of Experimental & Clinical Cancer Research: CR
Johannes Klose, Engin Guerlevik, Tina Trostel, Florian Kühnel, Thomas Schmidt, Martin Schneider, Alexis Ulrich
Introduction: Cholangiocarcinoma is characterized by aggressive tumor growth, high recurrence rates, and resistance against common chemotherapeutical regimes. The polyether-antibiotic Salinomycin is a promising drug in cancer therapy because of its ability to overcome apoptosis resistance of cancer cells and its selectivity against cancer stem cells. Here, we investigated the effectiveness of Salinomycin against cholangiocarcinoma in vivo, and analyzed interference of Salinomycin with autophagic flux in human cholangiocarcinoma cells...
January 9, 2018: Oncotarget
Zuochong Yu, Fangyi Chen, Xiaoxia Qi, Yinmei Dong, Yingying Zhang, Zhe Ge, Guoping Cai, Xinchao Zhang
Osteosarcoma is a common childhood bone cancer with a poor survival rate. Osteosarcoma cancer stem cells (CSCs) contribute to the recurrence, drug resistance and metastasis of this disease. Previous evidence suggested that cancer cells are able to spontaneously turn into CSCs, thus it is crucial to simultaneously target osteosarcoma cells and CSCs. Our previous studies have demonstrated that salinomycin preferably eliminated osteosarcoma CSCs. In addition, amplification of the epidermal growth factor receptor (EGFR) is a common genetic aberration in osteosarcoma, and thus EGFR is a promising target in osteosarcoma...
February 2018: Experimental and Therapeutic Medicine
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No abstract text is available yet for this article.
February 2018: Acta Pharmacologica Sinica
Yi-Bin Zeng, Zuo-Chong Yu, Yan-Ni He, Tong Zhang, Ling-Bo Du, Yin-Mei Dong, Huai-Wen Chen, Ying-Ying Zhang, Wu-Qing Wang
Melanoma is the deadliest type of skin cancer. CD20+ melanoma stem cells (CSCs) are pivotal for metastasis and initiation of melanoma. Therefore, selective elimination of CD20+ melanoma CSCs represents an effective treatment to eradicate melanoma. Salinomycin has emerged as an effective drug toward various CSCs. Due to its poor solubility, its therapeutic efficacy against melanoma CSCs has never been evaluated. In order to target CD20+ melanoma CSCs, we designed salinomycin-loaded lipid-polymer nanoparticles with anti-CD20 aptamers (CD20-SA-NPs)...
February 2018: Acta Pharmacologica Sinica
Alicja Urbaniak, Magdalena Delgado, Michał Antoszczak, Adam Huczyński, Timothy C Chambers
Salinomycin (SAL) and monensin (MON) are polyether ionophore antibiotics commonly used in veterinary medicine. They are known from their anti-cancer activity against various types of cancer cells, including those that display multi-drug resistance as well as cancer stem cells. In order to increase the biological activity profile and reduce toxicity against normal cells, while retaining the activities in the micromolar range, a library of ester and amide derivatives of SAL was synthesized and previously reported...
January 19, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jerod J Hurst, Josh S Wallace, Diana S Aga
Ionophore antimicrobials are heavily used in the livestock industries, both for preventing animal infection by coccidia protozoa and for increasing feed efficiency. Ionophores are excreted mostly unmetabolized and are released into the environment when manure is land-applied to fertilize croplands. Here, an analytical method was optimized to study the occurrences of five ionophore residues (monensin, lasalocid, maduramycin, salinomycin, and narasin) in dairy manure after solid-liquid separation and further treatment of the liquid manure by a membrane-based treatment system...
January 9, 2018: Chemosphere
Xiuge Gao, Yani Zheng, Xiangchun Ruan, Hui Ji, Lin Peng, Dawei Guo, Shanxiang Jiang
Salinomycin, as a polyether ionophore antibiotic, is extensively used as a feed additive against coccidiosis in poultry and as a growth promoter of ruminants worldwide. Owing to its narrow therapeutic index, numerous intoxication have been reported in target/non-target animals by overdosage, misuse or drug interactions as well as human who consumed salinomycin accidently. Salinomycin-induced cardiotoxicity in chicken and non-target animals is considered as a major contributor to animal death. In the current study, we aim to elucidate the underlying mechanism of its myocardial toxicity using primary chicken myocardial cell as an in vitro model...
January 10, 2018: Chemico-biological Interactions
Yu Zhang, Qi Zhang, Jing Sun, Huijie Liu, Qingfeng Li
Purpose: Lung cancer (LC) is the leading cause of cancer death worldwide. Evidences suggest that both LC cancer stem cells (CSCs) and cancer cells are supposed to be eliminated to achieve superior treatment effect against LC. Salinomycin could eradiate CSCs in various types of cancers, and gefitinib is a first-line therapy in LC. The purpose of the present study was to develop salinomycin-loaded nanoparticles (salinomycin-NPs) combined with gefitinib-loaded nanoparticles (gefitinib-NPs) to eradicate both LC CSCs and cancer cells...
2017: OncoTargets and Therapy
Kalina Kamenova, Yordanka Gluhcheva, Ivelin Vladov, Silviya Stoykova, Juliana Ivanova
This study presents experimental data on the effects of the tetraethylammonium salt of salinomycinic acid (Sal) on Cd-induced hepatotoxicity and renal dysfunction in Cd-treated mice compared to those of meso-2,3-dimercaptosuccinic acid (DMSA). Forty 60-day-old male ICR mice were randomized into five groups: control group (untreated mice), Cd group (Cd(II) acetate 20 mg/kg body weight provided orally once per day for 14 days), Cd + DMSA group (exposed to Cd(II) acetate as the Cd-exposed group followed by DMSA 20 mg/kg body weight provided orally once per day for 14 days), and Cd + Sal group (exposed to Cd(II) acetate as the Cd-exposed group followed by Sal 20 mg/kg body weight once per day for 14 days)...
November 21, 2017: Environmental Science and Pollution Research International
Kristine 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 containing dichloro(1,10-phenanthroline)copper(II) and various organelle-targeting peptide sequences is reported. The mitochondria-targeting metallopeptide 1 exploits the higher mitochondrial load in breast CSCs over the corresponding non-CSCs and the vulnerability of breast CSCs to mitochondrial damage to potently and selectively kill breast CSCs. Strikingly, 1 reduces the formation and size of mammospheres to a greater extent than salinomycin, an established CSC-potent agent...
January 2, 2018: Angewandte Chemie
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
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
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