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Treatment of cancer withs salts

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https://www.readbyqxmd.com/read/28438781/transporter-mediated-disposition-clinical-pharmacokinetics-and-cholestatic-potential-of-glyburide-and-its-primary-active-metabolites
#1
Rui Li, Yi-An Bi, Anna Vildhede, Renato J Scialis, Sumathy Mathialagan, Xin Yang, Lisa D Marroquin, Jian Lin, Manthena V S Varma
Glyburide is widely used for the treatment of type 2 diabetes mellitus. We studied the mechanisms involved in the disposition of glyburide and its pharmacologically active hydroxy metabolites, M1 and M2b; and evaluated their clinical pharmacokinetics and the potential role in glyburide-induced cholestasis employing physiologically based pharmacokinetic (PBPK) modeling. Transport studies of parent and metabolites in human hepatocytes and transfected cell systems imply hepatic uptake mediated by organic anion transporting polypeptides...
April 24, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28433659/carbonic-anhydrase-xii-functions-in-health-and-disease
#2
REVIEW
Abdul Waheed, William S Sly
Human CAXII was initially identified as a cancer marker in different cancers and tumors. Expression of CAXII is regulated by hypoxia and estrogen receptors. CAXII expression has been also detected in several tissues, whereas in cancer and tumor tissues its expression is several fold higher. In brain tumors, an alternatively spliced form of CAXII is expressed. Higher expression of CAXII in breast cancer is indicative of lower grade disease. CAXII plays a key role in several physiological functions. Mutation in the CAXII gene causes cystic fibrosis-like syndrome and salt wasting disease...
April 19, 2017: Gene
https://www.readbyqxmd.com/read/28419960/preferentially-enhancing-anti-cancer-isothiocyanates-over-glucosinolates-in-broccoli-sprouts-how-nacl-and-salicylic-acid-affect-their-formation
#3
Azadeh Esfandiari, Ali Saei, Marian J McKenzie, Adam J Matich, Mesbah Babalar, Donald A Hunter
Broccoli (Brassica oleracea L. var. italica) sprouts contain glucosinolates (GLs) that when hydrolysed yield health promoting isothiocyanates such as sulforaphane (SF). SF content can be increased by salt (NaCl) stress, although high salt concentrations negatively impact plant growth. Salicylic acid (SA) treatments can attenuate the negative effects of salt on growth. To test whether sprout isothiocyanate content could be elevated without sprout growth being compromised, broccoli seed were germinated and grown for seven days in salt (0, 80 and 160 mM) alone and in combination with 100 μM SA...
April 7, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28403964/-can-new-molecular-profiles-in-epithelial-ovarian-cancer-modify-therapeutics
#4
REVIEW
V Lavoué, A Rousselin, S Delplanque, M Pinsard, S Henno, F Foucher, J Levêque, T de la Motte Rouge
Epithelial ovarian cancer (EOC) affects 4500 women a year in France, with a survival of 30% at 5 years. Treatment is based on extensive surgery and chemotherapy. Around 15% of EOCs are due to genetic mutation predisposition essentially with mutated BRCA1 and BRCA2 genes. Four histological subtypes are described (serous, endometrioid, and mucinous cells to clear), corresponding to different carcinogenesis and distinct molecular mutations. High-grade serous EOCs have a mutation of the BRCA genes in 20-30% of cases...
February 2017: J Gynecol Obstet Hum Reprod
https://www.readbyqxmd.com/read/28396011/suppression-of-nfat5-mediated-inflammation-and-chronic-arthritis-by-novel-%C3%AE%C2%BAb-binding-inhibitors
#5
Eun-Jin Han, Hyun Young Kim, Naeun Lee, Nam-Hoon Kim, Seung-Ah Yoo, H Moo Kwon, Dae-Myung Jue, Yune-Jung Park, Chul-Soo Cho, Tran Quang De, Dae Young Jeong, Hee-Jong Lim, Woo Kyu Park, Ge Hyeong Lee, Heeyeong Cho, Wan-Uk Kim
Nuclear factor of activated T cells 5 (NFAT5) has been implicated in the pathogenesis of various human diseases, including cancer and arthritis. However, therapeutic agents inhibiting NFAT5 activity are currently unavailable. To discover NFAT5 inhibitors, a library of >40,000 chemicals was screened for the suppression of nitric oxide, a direct target regulated by NFAT5 activity, through high-throughput screening. We validated the anti-NFAT5 activity of 198 primary hit compounds using an NFAT5-dependent reporter assay and identified the novel NFAT5 suppressor KRN2, 13-(2-fluoro)-benzylberberine, and its derivative KRN5...
March 31, 2017: EBioMedicine
https://www.readbyqxmd.com/read/28379541/resistance-to-apoptosis-and-autophagy-leads-to-enhanced-survival-in-sertoli-cells
#6
Ferial Aslani, Tim Sebastian, Miguel Keidel, Suada Fröhlich, Hans-Peter Elsässer, Hans-Christian Schuppe, Jörg Klug, Poornima Mahavadi, Monika Fijak, Martin Bergmann, Andreas Meinhardt, Sudhanshu Bhushan
STUDY QUESTION: What is the underlying mechanism of Sertoli cell (SC) resistance to cell death? SUMMARY ANSWER: High expression of pro-survival B cell lymphoma-2 (BCL2) proteins and inhibition of apoptosis and autophagy prolongs SC survival upon exposure to stress stimuli. WHAT IS KNOWN ALREADY: In human and in experimental models of orchitis, tolerogenic SC survive stress conditions, while germ cells undergo massive apoptosis. In general, non-dividing highly differentiated cells tend to resist stress conditions for a longer time by favoring activation of pro-survival mechanisms and inhibition of cell death pathways...
April 3, 2017: Molecular Human Reproduction
https://www.readbyqxmd.com/read/28353361/enhancement-of-the-antitumor-effect-of-methotrexate-on-colorectal-cancer-cells-via-lactate-calcium-salt-targeting-methionine-metabolism
#7
Young-Kwon Jo, Min Hee Park, Hyunju Choi, HooKeun Lee, Jong-Moon Park, Jae Jun Sim, Chonghwan Chang, Keun-Yeong Jeong, Hwan Mook Kim
Methionine (Met) is involved in one-carbon de novo nucleotide synthesis and is an essential amino acid for cell survival. The impact of lactate calcium salt (CaLa) on the Met metabolism was investigated to evaluate the enhanced antitumor effect of methotrexate (MTX) on colorectal cancer (CRC) cells. Met dependency relating to homocysteine (Hcy) and betaine was investigated in human CRC cells (HCT-116 and HT-29) using a viability assay and liquid chromatography-mass spectrometry. Expression of betaine transporter-1 (BGT-1) following treatment with MTX alone or with CaLa was determined by Western blot...
March 29, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28326665/preparation-and-application-of-solid-salt-stabilized-zinc-amide-enolates-with-enhanced-air-and-moisture-stability
#8
Yi-Hung Chen, Mario Ellwart, Georgios Toupalas, Yusuke Ebe, Paul Knochel
The treatment of various N-morpholino amides with TMPZnCl⋅LiCl (TMP=2,2,6,6-tetramethylpiperidyl) and Mg(OPiv)2 in THF at 25 °C provides solid zinc enolates with enhanced air and moisture stability (t1/2 in air: 1-3 h) after solvent evaporation. These enolates undergo Pd- and Cu-catalyzed cross-couplings with (hetero)aryl bromides as well as allylic and benzylic halides. The arylated N-morpholino amides were converted into various ketones by LaCl3 ⋅2 LiCl mediated acylation with Grignard reagents...
March 22, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28284790/ulmus-davidiana-nakai-induces-apoptosis-and-autophagy-on-non-small-cell-lung-cancer-cells
#9
Soon-Oh Hong, In Keun Choi, Wonsik Jeong, Se Ryeon Lee, Hwa Jung Sung, Seong Su Hong, Jae Hong Seo
ETHNOPHARMACOLOGICAL RELEVANCE: Ulmus davidiana Nakai (UDN) is frequently used in the treatment of cancer in traditional oriental medicine. Although several reports indicate that UDN has inhibitory effects in some cancers, there has been no report on the inhibitory effects of UDN via both autophagy and apoptosis. MATERIALS AND METHODS: Cytotoxicity induced by UDN in human non-small cell lung cancer (NSCLC) H-1299 and H-460 cell lines was evaluated using the 2, 3-Bis (2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide inner salt (XTT) assay and trypan blue exclusion assay...
March 8, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28255808/euvolemic-hyponatremia-in-cancer-patients-report-of-the-hyponatremia-registry-an-observational-multicenter-international-study
#10
Volker Burst, Franziska Grundmann, Torsten Kubacki, Arthur Greenberg, Despina Rudolf, Abdulla Salahudeen, Joseph Verbalis, Christian Grohé
PURPOSE: Hyponatremia secondary to SIADH is frequent in cancer patients and potentially deleterious. The aim of this sub-analysis of the Hyponatremia Registry database is to analyze current diagnostic and therapeutic management practices in cancer patients with SIADH. METHODS: We analyzed 358 cancer patients who had serum sodium concentration ([Na(+)]) ≤ 130 mEq/L and a clinical diagnosis of SIADH from 225 sites in the USA and EU. RESULTS: Precise diagnostic testing was performed in only 46%...
March 2, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28251822/tolvaptan-use-in-cancer-patients-with-hyponatremia-due-to-the-syndrome-of-inappropriate-antidiuretic-hormone-a-post-hoc-analysis-of-the-salt-1-and-salt-2-trials
#11
Richard J Gralla, Fatima Ahmad, Jaime D Blais, Joseph Chiodo, Wen Zhou, Linda A Glaser, Frank S Czerwiec
Hyponatremia is a common electrolyte disorder in cancer patients and has been associated with poor prognosis. A frequent cause of cancer-related hyponatremia is the syndrome of inappropriate antidiuretic hormone (SIADH). This study was a post hoc subgroup analysis of the SALT-1 (Study of Ascending Levels of Tolvaptan in Hyponatremia) and SALT-2 clinical trials. Hyponatremic subjects with SIADH and cancer received the oral selective vasopressin V2-receptor antagonist tolvaptan (n = 12) or matching placebo (n = 16) once-daily for 30 days...
April 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28250648/the-influence-of-pluronic-f68-and-f127-nanocarrier-on-physicochemical-properties-in-vitro-release-and-antiproliferative-activity-of-thymoquinone-drug
#12
Salwa Shaarani, Shahrul Sahul Hamid, Noor Haida Mohd Kaus
BACKGROUND: This study reports on hydrophobic drug thymoquinone (TQ), an active compound found in the volatile oil of Nigella sativa that exhibits anticancer activities. Nanoformulation of this drug could potentially increase its bioavailability to specific target cells. OBJECTIVE: The aim of this study was to formulate TQ into polymer micelle, Pluronic F127 (5.0 wt %) and Pluronic F68 (0.1 wt %), as a drug carrier to enhance its solubility and instability in aqueous media...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28217276/synthesis-and-biological-evaluation-of-benzocyclooctene-based-and-indene-based-anticancer-agents-that-function-as-inhibitors-of-tubulin-polymerization
#13
Christine A Herdman, Tracy E Strecker, Rajendra P Tanpure, Zhi Chen, Alex Winters, Jeni Gerberich, Li Liu, Ernest Hamel, Ralph P Mason, David J Chaplin, Mary Lynn Trawick, Kevin G Pinney
The natural products colchicine and combretastatin A-4 (CA4) have been inspirational for the design and synthesis of structurally related analogues and spin-off compounds as inhibitors of tubulin polymerization. The discovery that a water-soluble phosphate prodrug salt of CA4 (referred to as CA4P) is capable of imparting profound and selective damage to tumor-associated blood vessels paved the way for the development of a new therapeutic approach for cancer treatment utilizing small-molecule inhibitors of tubulin polymerization that also act as vascular disrupting agents (VDAs)...
December 1, 2016: MedChemComm
https://www.readbyqxmd.com/read/28216890/evaluate-the-antigenotoxicity-and-anticancer-role-of-%C3%AE-sitosterol-by-determining-oxidative-dna-damage-and-the-expression-of-phosphorylated-mitogen-activated-protein-kinases-c-fos-c-jun-and-endothelial-growth-factor-receptor
#14
Ramalingam Sharmila, Ganapathy Sindhu
BACKGROUND: Plant sterols are the major source of micronutrients and have not shown any obvious side effects in human. β-sitosterol is one of the most prevalent phytosterols which have been recorded in ancient medicinal history for its use in the treatment of many chronic diseases, especially cancer. The modulations of mitogen-activated protein kinases' (MAPKs') play a crucial role in the development of human renal cell carcinoma. OBJECTIVE: The aim of the current study is to evaluate the antigenotoxic and anticancer role of β-sitosterol against renal carcinogen...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28123543/increased-chemosensitivity-and-radiosensitivity-of-human-breast-cancer-cell-lines-treated-with-novel-functionalized-single-walled-carbon-nanotubes
#15
Yijun Jia, Ziyi Weng, Chuanying Wang, Mingjie Zhu, Yunshu Lu, Longlong Ding, Yongkun Wang, Xianhua Cheng, Qing Lin, Kejin Wu
Hypoxia is a major cause of treatment resistance in breast cancer. Single-walled carbon nanotubes (SWCNTs) exhibit unique properties that make them promising candidates for breast cancer treatment. In the present study, a new functionalized single-walled carbon nanotube carrying oxygen was synthesized; it was determined whether this material could increase chemosensitivity and radiosensitivity of human breast cancer cell lines, and the underlying mechanisms were investigated. MDA-MB-231 cells growing in folic acid (FA) free medium, MDA-MB-231 cells growing in medium containing FA and ZR-75-1 cells were treated with chemotherapy drugs or radiotherapy with or without tombarthite-modified-FA-chitosan (R-O2-FA-CHI)-SWCNTs under hypoxic conditions, and the cell viability was determined by water-soluble tetrazolium salts-1 assay...
January 2017: Oncology Letters
https://www.readbyqxmd.com/read/28117205/synthesis-and-biological-evaluation-of-a-water-soluble-phosphate-prodrug-salt-and-structural-analogues-of-kgp94-a-lead-inhibitor-of-cathepsin-l
#16
Erica N Parker, Samuel O Odutola, Yifan Wang, Tracy E Strecker, Rajeswari Mukherjee, Zhe Shi, David J Chaplin, Mary Lynn Trawick, Kevin G Pinney
The magnitude of expression of cathepsin L, often upregulated in the tumor microenvironment, correlates with the invasive and metastatic nature of certain tumors. Inhibition of cathepsin L represents an emerging strategy for the treatment of metastatic cancer. A potent, small-molecule inhibitor (referred to as KGP94) of cathepsin L, and new KGP94 analogues were synthesized. (3,5-Dibromophenyl)-(3-hydroxyphenyl) ketone thiosemicarbazone (22), with an IC50 value of 202nM, exhibited similar inhibitory activity against cathepsin L compared to KGP94 (IC50=189nM)...
December 21, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28109077/simultaneous-but-not-consecutive-combination-with-folinate-salts-potentiates-5-fluorouracil-antitumor-activity-in-vitro-and-in-vivo
#17
Antonello Di Paolo, Paola Orlandi, Teresa Di Desidero, Romano Danesi, Guido Bocci
The combination of folinate salts to 5-fluoruracil (5-FU)-based schedules is an established clinical routine in the landscape of the colorectal cancer treatment. The aim of this study was to investigate the pharmacological differences between the sequential administration of folinate salts (1 h before, as in clinical routine) followed by 5-FU and the simultaneous administration of both drugs. Proliferation and apoptotic assays were performed on human colon cancer cells exposed to 5-FU, calcium (CaLV) or disodium (NaLV) levofolinate or their simultaneous and sequential combination for 24 and 72h...
January 20, 2017: Oncology Research
https://www.readbyqxmd.com/read/28076666/the-global-incidence-of-lip-oral-cavity-and-pharyngeal-cancers-by-subsite-in-2012
#18
Kevin D Shield, Jacques Ferlay, Ahmedin Jemal, Rengaswamy Sankaranarayanan, Anil K Chaturvedi, Freddie Bray, Isabelle Soerjomataram
By using data from the International Agency for Research on Cancer publication Cancer Incidence in 5 Continents and GLOBOCAN, this report provides the first consolidated global estimation of the subsite distribution of new cases of lip, oral cavity, and pharyngeal cancers by country, sex, and age for the year 2012. Major geographically based, sex-based, and age-based variations in the incidence of lip, oral cavity, and pharyngeal cancers by subsite were observed. Lip cancers were highly frequent in Australia (associated with solar radiation) and in central and eastern Europe (associated with tobacco smoking)...
January 2017: CA: a Cancer Journal for Clinicians
https://www.readbyqxmd.com/read/28039836/structure-based-design-and-synthesis-of-imidazo-1-2-a-pyridine-derivatives-as-novel-and-potent-nek2-inhibitors-with-in%C3%A2-vitro-and-in%C3%A2-vivo-antitumor-activities
#19
Jian-Bei Xi, Yan-Fen Fang, Brendan Frett, Meng-Li Zhu, Tong Zhu, Yan-Nan Kong, Feng-Jie Guan, Yun Zhao, Xiong-Wen Zhang, Hong-Yu Li, Ming-Liang Ma, Wenhao Hu
We present herein the discovery and development of novel and potent Nek2 inhibitors with distinctive in vitro and in vivo antitumor activity based on an imidazo[1,2-a]pyridine scaffold. Our studies identified a nonlinear SAR for activity against both Nek2 and cancer cells. Bioisostere and structure-based design techniques were employed to identify compounds 42c (MBM-17, IC50 = 3.0 nM) and 42g (MBM-55, IC50 = 1.0 nM), which displayed low nanomolar activity and excellent selectivity for Nek2. Both compounds effectively inhibited the proliferation of cancer cells by inducing cell cycle arrest and apoptosis...
January 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28011480/synergistically-anti-metastatic-effect-of-5-flourouracil-on-colorectal-cancer-cells-via-calcium-mediated-focal-adhesion-kinase-proteolysis
#20
Minhee Park, Pasupathi Sundaramoorthy, Jae Jun Sim, Keun-Yeong Jeong, Hwan Mook Kim
AIM: To investigate the possibility of enhancing an anti-metastatic effect of 5-fluorouracil (5-FU) on colorectal cancer (CRC) cells by combining it with continuous calcium supplementation. MATERIALS AND METHODS: Optimal doses of 5-FU with/without lactate salt (CaLa) were determined via clonogenicity and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays using human CRC cells cultured on normal or low-attachment plates. Invasion and migration assays confirmed the enhanced anti-metastatic effect of combining 5-FU and CaLa...
2017: Anticancer Research
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