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https://www.readbyqxmd.com/read/27902917/coccidiosis-in-the-chukar-partridge-alectoris-chukar-a-survey-of-coccidiosis-outbreaks-and-a-test-of-anticoccidial-drugs-against-eimeria-kofoidi
#1
R W Gerhold, A L Fuller, L R McDougald
Field isolates of coccidia from 20 natural outbreaks in the chukar partridge ( Alectoris chukar ) were received from gamebird farms in 10 U.S. states. These were propagated in the laboratory and identified by microscopy and PCR. Of 20 samples, 18 were Eimeria kofoidi, two were Eimeria legionensis only, and one was a mixture of the two species. One isolate of E. kofoidi also contained an unidentified species detected only by PCR, nucleotide sequencing, and phylogenetic analysis. The efficacy of anticoccidial drugs against chukar coccidia was tested with experimental infections in battery cages...
December 2016: Avian Diseases
https://www.readbyqxmd.com/read/27894167/salinomycin-reduces-stemness-and-induces-apoptosis-on-human-ovarian-cancer-stem-cell
#2
Hyun Gyo Lee, So Jin Shin, Hye Won Chung, Sang Hoon Kwon, Soon Do Cha, Jin Eui Lee, Chi Heum Cho
OBJECTIVE: Cancer stem cells (CSCs) represent a subpopulation of undifferentiated tumorigenic cells thought to be responsible for tumor initiation, maintenance, drug resistance, and metastasis. The role of CSCs in drug resistance and relapse of cancers could significantly affect outcomes of ovarian cancer patient. Therefore, therapies that target CSCs could be a promising approach for ovarian cancer treatment. The antibiotic salinomycin has recently been shown to deplete CSCs. In this study, we evaluated the effect of salinomycin on ovarian cancer stem cells (OCSCs), both alone and in combination with paclitaxel (PTX)...
November 14, 2016: Journal of Gynecologic Oncology
https://www.readbyqxmd.com/read/27876192/synthesis-and-biological-evaluation-of-salinomycin-triazole-analogues-as-anticancer-agents
#3
Minjian Huang, Zixin Deng, Jian Tian, Tiangang Liu
Salinomycin, a polyether antibiotic used for treatment of coccidial disease in animal husbandry, has demonstrated promising efficacy for treating different cancers. To enrich structure-activity relationship of salinomycin in tumours, we prepared a series of new triazole derivatives in specific site of salinomycin by click cycloaddition reactions, and assessed their antiproliferative activities on breast cancer cell lines. The screening results indicated that most derivatives modified at the C20 hydroxyl group have potent antitumour activity...
November 2, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27863002/development-of-a-single-run-analytical-method-for-the-detection-of-ten-multi-class-emerging-contaminants-in-agricultural-soil-using-an-acetate-buffered-quechers-method-coupled-with-lc-ms-ms
#4
Young-Jun Lee, Jeong-Heui Choi, A M Abd El-Aty, Hyung Suk Chung, Han Sol Lee, Sung-Woo Kim, Md Musfiqur Rahman, Byung-Jun Park, Jang-Eok Kim, Ho-Chul Shin, Jae-Han Shim
This study was undertaken to develop and validate a single multiresidue method for the monitoring of ten multi-class emerging contaminants, viz. ceftiofur, clopidol, florfenicol, monensin, salinomycin, sulfamethazine, sulfathiazole, sulfamethoxazole, tiamulin, and tylosin in agricultural soil. Samples were extracted using acetate-buffered modified quick, easy, cheap, effective, rugged, and safe method followed by liquid chromatography with tandem mass spectrometric analysis in positive ion mode. Separation on an Eclipse Plus C18 column was conducted in gradient elution mode using a mobile phase of methanol (A) and distilled water (B), each containing 0...
November 10, 2016: Journal of Separation Science
https://www.readbyqxmd.com/read/27855654/salinomycin-inhibits-metastatic-colorectal-cancer-growth-and-interferes-with-wnt-%C3%AE-catenin-signaling-in-cd133-human-colorectal-cancer-cells
#5
Johannes Klose, Jana Eissele, Claudia Volz, Steffen Schmitt, Alina Ritter, Shen Ying, Thomas Schmidt, Ulrike Heger, Martin Schneider, Alexis Ulrich
BACKGROUND: The polyether antibiotic Salinomycin (Sal) is regarded as an inhibitor of cancer stem cells. Its effectiveness on human colorectal cancer (CRC) cells in vitro has been demonstrated before. The aim of this study was to establish a murine model to investigate the effectiveness of Sal in vivo. Furthermore, we investigated the impact of Sal on Wnt/β-catenin signaling in human CD133(+) CRC cells. METHODS: The two murine CRC cell lines MC38 and CT26 were used to analyze the impact of Sal on tumor cell proliferation, viability, migration, cell cycle progression and cell death in vitro...
November 17, 2016: BMC Cancer
https://www.readbyqxmd.com/read/27830292/slnr-is-a-positive-pathway-specific-regulator-for-salinomycin-biosynthesis-in-streptomyces-albus
#6
Zhenhong Zhu, Han Li, Pin Yu, Yuanyang Guo, Shuai Luo, Zhongbin Chen, Xuming Mao, Wenjun Guan, Yongquan Li
Salinomycin, a polyether antibiotic produced by Streptomyces albus, is widely used in animal husbandry as an anticoccidial drug and growth promoter. Situated within the salinomycin biosynthetic gene cluster, slnR encodes a LAL-family transcriptional regulator. The role of slnR in salinomycin production in S. albus was investigated by gene deletion, complementation, and overexpression. Gene replacement of slnR from S. albus chromosome results in almost loss of salinomycin production. Complementation of slnR restored salinomycin production, suggesting that SlnR is a positive regulator of salinomycin biosynthesis...
November 9, 2016: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/27822137/axitinib-has-antiangiogenic-and-antitumorigenic-activity-in-myxoid-liposarcoma
#7
Lauren T Kerr, Jacqueline F Donoghue, Alexander L Wilding, Terrance G Johns
Myxoid liposarcoma is a rare form of soft-tissue sarcoma. Although most patients initially respond well to treatment, approximately 21% relapse, highlighting the need for alternative treatments. To identify novel treatment regimens and gain a better understanding of myxoid liposarcoma tumor biology, we screened various candidate and approved targeted therapeutics and chemotherapeutics against myxoid liposarcoma cell lines. Therapeutics that target angiogenesis showed antitumor activity. The small molecule inhibitor axitinib, which targets angiogenesis by inhibiting the VEGFR and PDGFR families and c-Kit, inhibited cell cycle progression and induced apoptosis in vitro, as well as having significant antitumor activity against MLS 1765 myxoid liposarcoma xenografts in mice...
2016: Sarcoma
https://www.readbyqxmd.com/read/27774561/the-breast-cancer-stem-cell-potency-of-copper-ii-complexes-bearing-nonsteroidal-anti-inflammatory-drugs-and-their-encapsulation-using-polymeric-nanoparticles
#8
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
https://www.readbyqxmd.com/read/27765904/identification-of-dna-pkcs-as-a-primary-resistance-factor-of-salinomycin-in-osteosarcoma-cells
#9
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
https://www.readbyqxmd.com/read/27740704/structure-activity-relationships-in-salinomycin-cytotoxicity-and-phenotype-selectivity-of-semi-synthetic-derivatives
#10
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
https://www.readbyqxmd.com/read/27666600/salinomycin-enhances-cisplatin-induced-cytotoxicity-in-human-lung-cancer-cells-via-down-regulation-of-akt-dependent-thymidylate-synthase-expression
#11
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...
December 15, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27647449/codelivery-of-salinomycin-and-doxorubicin-using-nanoliposomes-for-targeting-both-liver-cancer-cells-and-cancer-stem-cells
#12
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
https://www.readbyqxmd.com/read/27612428/low-dose-salinomycin-induces-anti-leukemic-responses-in-aml-and-mll
#13
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
https://www.readbyqxmd.com/read/27587902/enzymology-of-pyran-ring%C3%A2-a-formation-in-salinomycin-biosynthesis
#14
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
https://www.readbyqxmd.com/read/27557629/differences-in-antiproliferative-activity-between-salinomycin-azt-conjugates-obtained-via-click-and-esterification-reactions
#15
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
https://www.readbyqxmd.com/read/27557496/dual-targeting-of-androgen-receptor-and-mtorc1-by-salinomycin-in-prostate-cancer
#16
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
https://www.readbyqxmd.com/read/27536105/combination-of-salinomycin-and-silver-nanoparticles-enhances-apoptosis-and-autophagy-in-human-ovarian-cancer-cells-an-effective-anticancer-therapy
#17
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
https://www.readbyqxmd.com/read/27462592/the-effect-of-salinomycin-on-ovarian-cancer-stem-like-cells
#18
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
https://www.readbyqxmd.com/read/27457761/in-vitro-activity-of-salinomycin-and-monensin-derivatives-against-trypanosoma-brucei
#19
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
https://www.readbyqxmd.com/read/27443201/a-multi-residue-method-for-17-anticoccidial-drugs-and-ractopamine-in-animal-tissues-by-liquid-chromatography-tandem-mass-spectrometry-and-time-of-flight-mass-spectrometry
#20
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
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