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Arvin Eskandari, Janine N Boodram, Paul B Cressey, Chunxin Lu, Peter M Bruno, Michael T Hemann, Kogularamanan Suntharalingam
We report the cancer stem cell (CSC) potency of a novel series of copper(ii)-phenanthroline complexes bearing nonsteriodial anti-inflammatory drugs: naproxen, tolfenamic acid, and indomethacin (2a-3c). Two of the complexes, 2a and 3c, kill breast CSC-enriched HMLER-shEcad cells (grown in both monolayer and three-dimensional cell cultures) to a significantly better extent than salinomycin, a well-established CSC toxin. The most potent complex in the series, 3c induces its cytotoxic effect by generating intracellular reactive oxygen species (ROS) and inhibiting cyclooxgenase-2 (COX-2) activity...
October 24, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Yun-Fang Zhen, Song-Tao Li, Yun-Rong Zhu, Xiao-Dong Wang, Xiao-Zhong Zhou, Lun-Qing Zhu
Malignant osteosarcoma (OS) is still a deadly disease for many affected patients. The search for the novel anti-OS agent is extremely urgent and important. Our previous study has proposed that salinomycin is a novel anti-OS agent. Here we characterized DNA-dependent protein kinase catalytic subunit (DNA-PKcs) as a primary salinomycin resistance factor in OS cells. DNA-PKcs inhibitors (NU7026, NU7441 and LY294002) or DNA-PKcs shRNA knockdown dramatically potentiated salinomycin-induced death and apoptosis of OS cells (U2OS and MG-63 lines)...
October 17, 2016: Oncotarget
Björn Borgström, Xiaoli Huang, Cecilia Hegardt, Stina Oredsson, Daniel Strand
The ionophore salinomycin has attracted attention for its exceptional ability to selectively reduce the proportion of cells with stem-like properties in cancer cell populations of varying origin. Targeting the tumorigenicity of such cells is of interest as they are implicated in recurrence, metastasis, and drug resistance. Structural derivatives of salinomycin are thus sought after, both as tools for probing the molecular mechanism(s) underlying the observed phenotype effects, and for improving selectivity and activity against cancer stem cells...
October 14, 2016: Chemistry: a European Journal
Jen-Chung Ko, Hao-Yu Zheng, Wen-Ching Chen, Yi-Shuan Peng, Chia-Hung Wu, Chia-Li Wei, Jyh-Cheng Chen, Yun-Wei Lin
Salinomycin, a polyether antibiotic, acts as a highly selective potassium ionophore and has anticancer activity on various cancer cell lines. Cisplatin has been proved as chemotherapy drug for advanced human non-small cell lung cancer (NSCLC). Thymidylate synthase (TS) is a key enzyme in the pyrimidine salvage pathway, and increased expression of TS is thought to be associated with resistance to cisplatin. In this study, we showed that salinomycin (0.5-2μg/mL) treatment down-regulating of TS expression in an AKT inactivation manner in two NSCLC cell lines, human lung adenocarcinoma A549 and squamous cell carcinoma H1703 cells...
September 22, 2016: Biochemical Pharmacology
Zhirong Gong, Dazhong Chen, Fangyuan Xie, Junjie Liu, He Zhang, Hao Zou, Yuan Yu, Yan Chen, Zhiguo Sun, Xinxia Wang, Hai Zhang, Guoqing Zhang, Chuan Yin, Jie Gao, Yanqiang Zhong, Ying Lu
AIM: To develop salinomycin-loaded nanoliposomes (SLN), doxorubicin-loaded nanoliposomes (DLN) and nanoliposomes codelivering salinomycin and doxorubicin (SDLN) to target both liver cancer cells and cancer stem cells. MATERIALS & METHODS: The characterization and antitumor activity of SLN, DLN and SDLN were evaluated. RESULTS & CONCLUSION: The doxorubicin/salinomycin sodium mole ratio of 1:1 had the best synergistic combination index value, and was chosen as the drug ratio in SDLN...
September 20, 2016: Nanomedicine
Gary D R Roulston, Charlotte L Burt, Laura M J Kettyle, Kyle B Matchett, Heather L Keenan, Nuala M Mulgrew, Joanne M Ramsey, Caoifa Dougan, John McKiernan, Ivan V Grishagin, Ken I Mills, Alexander Thompson
Development of anti-cancer drugs towards clinical application is costly and inefficient. Large screens of drugs, efficacious for non-cancer disease, are currently being used to identify candidates for repurposing based on their anti-cancer properties. Here, we show that low-dose salinomycin, a coccidiostat ionophore previously identified in a breast cancer screen, has anti-leukemic efficacy. AML and MLLr cell lines, primary cells and patient samples were sensitive to submicromolar salinomycin. Most strikingly, colony formation of normal hematopoietic cells was unaffected by salinomycin, demonstrating a lack of hemotoxicity at the effective concentrations...
September 6, 2016: Oncotarget
Hanna Luhavaya, Marcio V B Dias, Simon R Williams, Hui Hong, Luciana G de Oliveira, Peter F Leadlay
Tetrahydropyran rings are a common feature of complex polyketide natural products, but much remains to be learned about the enzymology of their formation. The enzyme SalBIII from the salinomycin biosynthetic pathway resembles other polyether epoxide hydrolases/cyclases of the MonB family, but SalBIII plays no role in the conventional cascade of ring opening/closing. Mutation in the salBIII gene gave a metabolite in which ring A is not formed. Using this metabolite in vitro as a substrate analogue, SalBIII has been shown to form pyran ring A...
November 9, 2015: Angewandte Chemie
Michał Antoszczak, Ewa Maj, Natalia Kleczewska, Joanna Wietrzyk, Lech Celewicz, Adam Huczyński
BACKGROUND: Pharmacophore hybridization by bioconjugation, in which two bioactive moieties are covalently linked, is one of the current strategies in drug discovery for the development of new compounds with improved affinity and efficacy relative to those of the parent molecules. Prompted by the idea that cancer cells may be effectively killed by 3'-azido-3'-deoxythymidine (AZT) and salinomycin (SAL) individually, we synthesized hybrids of these compounds. The development of this type of derivatives, which can easily penetrate the lipid-rich cell membranes and then undergo hydrolysis inside the cancer cells, is an important research area...
August 23, 2016: Medicinal Chemistry
Nooshin Mirkheshti, Sulgi Park, Shoulei Jiang, Jodie Cropper, Sherry L Werner, Chung S Song, Bandana Chatterjee
Androgen receptor (AR) and PI3K/AKT/mTORC1 are major survival signals that drive prostate cancer to a lethal disease. Reciprocal activation of these oncogenic pathways from negative cross talks contributes to low/limited success of pathway-selective inhibitors in curbing prostate cancer progression. We report that the antibiotic salinomycin, a cancer stem cell blocker, is a dual-acting AR and mTORC1 inhibitor, inhibiting PTEN-deficient castration-sensitive and castration-resistant prostate cancer in culture and xenograft tumors...
August 19, 2016: Oncotarget
Xi-Feng Zhang, Sangiliyandi Gurunathan
Ovarian cancer is one of the most important malignancies, and the origin, detection, and pathogenesis of epithelial ovarian cancer remain elusive. Although many cancer drugs have been developed to dramatically reduce the size of tumors, most cancers eventually relapse, posing a critical problem to overcome. Hence, it is necessary to identify possible alternative therapeutic approaches to reduce the mortality rate of this devastating disease. To identify alternative approaches, we first synthesized silver nanoparticles (AgNPs) using a novel bacterium called Bacillus clausii...
2016: International Journal of Nanomedicine
Hyewon Chung, Yu-Hwan Kim, Myoung Kwon, So-Jin Shin, Sang-Hoon Kwon, Soon-Do Cha, Chi-Heum Cho
OBJECTIVE: The identification of cancer stem-like cells is a recent development in ovarian cancer. Compared to other cancer cells, cancer stem-like cells present more chemo-resistance and more aggressive characteristics. They play an important role in the recurrence and drug resistance of cancer. Therefore, the target therapy of cancer stem-like cell may become a promising and effective approach for ovarian cancer treatment. It may also help to provide novel diagnostic and therapeutic strategies...
July 2016: Obstetrics & Gynecology Science
Dietmar Steverding, Michał Antoszczak, Adam Huczyński
BACKGROUND: African trypanosomes are the causative agents of sleeping sickness in humans and nagana disease in livestock animals. As the few drugs available for treatment of the diseases have limited efficacy and produce adverse reactions, new and better tolerated therapies are required. Polyether ionophores have been shown to display anti-cancer, anti-microbial and anti-parasitic activity. In this study, derivatives of the polyether ionophores, salinomycin and monensin were tested for their in vitro activity against bloodstream forms of Trypanosoma brucei and human HL-60 cells...
2016: Parasites & Vectors
Johanna L Matus, Joe O Boison
A new and sensitive multi-residue liquid chromatography-tandem mass spectrometry (LC-MS/MS) and liquid chromatography-quadrupole time-of-flight-mass spectrometry (LC-QToF-MS) method was developed and validated for the determination and confirmation of residues of 17 anticoccidials, plus free ractopamine in poultry muscle and liver, and bovine muscle, liver, and kidney tissues. The 17 anticoccidials are lasalocid, halofuginone, narasin, monensin, semduramicin, ethopabate, robenidine, buquinolate, toltrazuril as its sulfone metabolite, maduramicin, salinomycin, diclazuril, amprolium, decoquinate, dinitolmide, clopidol, and the nicarbazin metabolite DNC (N,N1-bis(4-nitrophenyl)urea)...
May 2016: Drug Testing and Analysis
Ann-Katrin Sommer, Adam Hermawan, Frauke Martina Mickler, Bojan Ljepoja, Pjotr Knyazev, Christoph Bräuchle, Axel Ullrich, Ernst Wagner, Andreas Roidl
Luminal A breast cancer is the most common breast cancer subtype which is usually treated with selective estrogen receptor modulators (SERMS) like tamoxifen. Nevertheless, one third of estrogen receptor positive breast cancer patients initially do not respond to endocrine therapy and about 40% of luminal A breast tumors recur in five years. In this study, we investigated an alternative treatment approach by combining tamoxifen and salinomycin in luminal A breast cancer cell lines. We have found that salinomycin induces an additional cytotoxic effect by inhibiting the ligand independent activation of ERα...
July 7, 2016: Oncotarget
Fangyuan Xie, Siyue Zhang, Junjie Liu, Zhirong Gong, Kaixuan Yang, He Zhang, Ying Lu, Hao Zou, Yuan Yu, Yan Chen, Zhiguo Sun, Xinxia Wang, Hai Zhang, Guoqing Zhang, Wei Li, Bohua Li, Jie Gao, Yanqiang Zhong
AIM: To improve the suboptimal therapeutic efficacy of salinomycin (SAL) toward liver cancer cells using chloroquine (CQ) combination by the liposomes co-delivering SAL and CQ (SCNL). MATERIALS & METHODS: The synergy of these two drugs was evaluated in liver cancer cells (HepG2) and liver cancer stem cells (LCSCs) by median-effect analysis. SCNL with optimized ratio were developed. The cytotoxic effect and basal autophagy flux (measure of autophagic degradation activity) of various formulations were evaluated...
July 2016: Nanomedicine
Björn Borgström, Xiaoli Huang, Eduard Chygorin, Stina Oredsson, Daniel Strand
The polyether ionophore salinomycin has recently gained attention due to its exceptional ability to selectively reduce the proportion of cancer stem cells within a number of cancer cell lines. Efficient single step strategies for the preparation of hydroxamic acid hybrids of this compound varying in N- and O-alkylation are presented. The parent hydroxamic acid, salinomycin-NHOH, forms both inclusion complexes and well-defined electroneutral complexes with potassium and sodium cations via 1,3-coordination by the hydroxamic acid moiety to the metal ion...
June 9, 2016: ACS Medicinal Chemistry Letters
Peizhe Sun, Spyros G Pavlostathis, Ching-Hua Huang
Monensin (MON) and salinomycin (SAL), known as polyether ionophore antibiotics (IPAs), are extensively used in livestock industry and can enter the environment via animal manure and agricultural runoff. Although some studies have investigated the environmental fate and transformation of IPAs, the lack of information on IPAs' aqueous-phase chemical properties is a major hindrance for further in-depth research. This study was able to experimentally determine the acidity constants (pKa), metal-complex dissociation constants (Kdiss), and intrinsic aqueous solubility of MON species, and some of these properties of SAL...
September 2016: Environmental Science and Pollution Research International
Samir Djemai, Abdeslam Mekroud, Mark C Jenkins
The present study represents the first description of ionophore resistance in recovered from commercial Algerian (Jijel-Algeria) broiler farms. Microscopy and intervening transcribed sequence 1 PCR (ITS1 PCR) revealed only 2 Eimeria species present in litter from these farms- namely Eimeria acervulina and Eimeria maxima. A pool of these isolates were evaluated in broiler chickens (Cobb 500) for sensitivity to 5 anticoccidial compounds-diclazuril (1ppm), lasalocid (125ppm), monensin (125ppm), narasin (70ppm) and salinomycin (60ppm)...
July 15, 2016: Veterinary Parasitology
Tao Wang, Radhika Narayanaswamy, Huilan Ren, Vladimir P Torchilin
Many types of tumors are organized in a hierarchy of heterogeneous cell populations. The cancer stem-like cells (CSCs) hypothesis suggests that tumor development and metastasis are driven by a minority population of cells, which are responsible for tumor initiation, growth and recurrences. The inability to efficiently eliminate CSCs during chemotherapy, together with CSCs being highly tumorigenic and invasive, may result in treatment failure due to cancer relapse and metastases. CSCs are emerging as a promising target for the development of translational cancer therapies...
June 2, 2016: Cancer Biology & Therapy
G-F Zhang, C-X Li, Z-Q Liu, S Ma, H-B Chen
The varied therapeutic approaches like radiotherapy, chemotherapy, surgery, etc. primarily aimed to target cancer cells specifically. Despite these efforts, they are not completely successful in eliminating this deadly pathological state. These failures ultimately lead to cancer reoccurrence, which is again, another burning problem associated with cancer. The prime reason for the above observation has been found to be the development of resistance by cancer cells towards cancer drugs or cancer-initiating cells (cancer stem cells) remain unaffected by existing treatment procedures...
May 2016: European Review for Medical and Pharmacological Sciences
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