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Treatment of cancer withs salts

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https://www.readbyqxmd.com/read/28326665/preparation-and-application-of-solid-salt-stabilized-zinc-amide-enolates-with-enhanced-air-and-moisture-stability
#1
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
#2
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
#3
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
#4
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...
March 2, 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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/27998076/microwave-triggered-smart-drug-release-from-liposomes-co-encapsulating-doxorubicin-and-salt-for-local-combined-hyperthermia-and-chemotherapy-of-cancer
#14
Yushen Jin, Xiaolong Liang, Yunkun An, Zhifei Dai
The microwave and temperature sensitive liposomes were fabricated successfully from 1,2-dipalmityol-sn-glycero-3-phosphocholine (DPPC), cholesterol, and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000 (DSPE-PEG2000) with a molar ratio of 4:1:0.26 by co-encapsulating NaCl and doxorubicin (DOX) through the thin-film hydration method to externally manipulate drug release at a predetermined location in the body at a desired time in the right dosage for combination microwave hyperthermia and chemotherapy of cancer to afford a synergistic therapeutic effect...
December 21, 2016: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/27989629/-50th-anniversary-of-cisplatin
#15
REVIEW
Chloé Rancoule, Jean-Baptiste Guy, Alexis Vallard, Majed Ben Mrad, Amel Rehailia, Nicolas Magné
We have just celebrated the 50th anniversary of cisplatin cytotoxic potential discovery. It is time to take stock… and it seems mainly positive. This drug, that revolutionized the treatment of many cancer types, continues to be the most widely prescribed chemotherapy. Despite significant toxicities, resistance mechanisms associated with treatment failures, and unresolved questions about its mechanism of action, the use of this cytotoxic agent remains unwavering. The interest concerning this "old" invincible drug has not yet abated...
February 2017: Bulletin du Cancer
https://www.readbyqxmd.com/read/27987939/chitosan-nanoparticles-for-combined-drug-delivery-and-magnetic-hyperthermia-from-preparation-to-in-vitro-studies
#16
Vanessa Zamora-Mora, Mar Fernández-Gutiérrez, Álvaro González-Gómez, Beatriz Sanz, Julio San Román, Gerardo F Goya, Rebeca Hernández, Carmen Mijangos
Chitosan nanoparticles (CSNPs) ionically crosslinked with tripolyphosphate salts (TPP) were employed as nanocarriers in combined drug delivery and magnetic hyperthermia (MH) therapy. To that aim, three different ferrofluid concentrations and a constant 5-fluorouracil (5-FU) concentration were efficiently encapsulated to yield magnetic CSNPs with core-shell morphology. In vitro experiments using normal cells, fibroblasts (FHB) and cancer cells, human glioblastoma A-172, showed that CSNPs presented a dose-dependent cytotoxicity and that they were successfully uptaken into both cell lines...
February 10, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/27920624/neoadjuvant-chemotherapy-with-docetaxel-carboplatin-and-weekly-trastuzumab-is-active-in-her2-positive-early-breast-cancer-results-after-a-median-follow-up-of-over-4-years
#17
Hans-Christian Kolberg, Leyla Akpolat-Basci, Miltiades Stephanou, Bahriye Aktas, Carla Verena Hannig, Cornelia Liedtke
INTRODUCTION: Most patients with HER2-positive breast cancer receive chemotherapy and trastuzumab. Data from adjuvant trials have shown that the combination of docetaxel, carboplatin and weekly trastuzumab (TCH) is well tolerated and as effective as anthracycline-containing regimes. Previous investigations on neoadjuvant treatment with taxanes, platinum salts and trastuzumab showed pathological complete remission (pCR) rates between 43.3 and 76%. To date, the longest published follow-up in this indication is 3 years...
October 2016: Breast Care
https://www.readbyqxmd.com/read/27920523/pegylated-and-nanoparticle-conjugated-sulfonium-salt-photo-triggers-necrotic-cell-death
#18
Alaa A Fadhel, Xiling Yue, Ebrahim H Ghazvini Zadeh, Mykhailo V Bondar, Kevin D Belfield
Photodynamic therapy (PDT) processes involving the production of singlet oxygen face the issue of oxygen concentration dependency. Despite high oxygen delivery, a variety of properties related to metabolism and vascular morphology in cancer cells result in hypoxic environments, resulting in limited effectiveness of such therapies. An alternative oxygen-independent agent whose cell cytotoxicity can be remotely controlled by light may allow access to treatment of hypoxic tumors. Toward that end, we developed and tested both polyethylene glycol (PEG)-functionalized and hydrophilic silica nanoparticle (SiNP)-enriched photoacid generator (PAG) as a nontraditional PDT agent to effectively induce necrotic cell death in HCT-116 cells...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/27916693/comparison-of-2-strategies-to-enhance-pyridoclax-solubility-nanoemulsion-delivery-system-versus-salt-synthesis
#19
A-C Groo, M De Pascale, A-S Voisin-Chiret, S Corvaisier, M Since, A Malzert-Fréon
Pyridoclax is an original oligopyridine lead, very promising in treatment of chemoresistant cancers. However, from solubility measurement and permeability evaluation, it appeared that this compound can be considered as a BCS II drug, with a poor water solubility. To overcome this unfavorable property, two strategies were proposed and compared: pyridoclax di-hydrochloride salt synthesis and formulation of pyridoclax-loaded nanoemulsions (PNEs) efficiently performed by transposing the spontaneous emulsification process previously developed by our team...
January 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27822040/raspberry-like-poly-%C3%AE-glutamic-acid-hydrogel-particles-for-ph-dependent-cell-membrane-passage-and-controlled-cytosolic-delivery-of-antitumor-drugs
#20
Sun-Hee Cho, Ji Hyeon Hong, Young-Woock Noh, Eunji Lee, Chang-Soo Lee, Yong Taik Lim
In this research, we synthesized bioderived poly(amino acid) hydrogel particles that showed pH-dependent membrane-disrupting properties and controlled cytosolic delivery of antitumor drugs. Poly(γ-glutamic acid) (γ-PGA) that has been produced extensively using bacteria, especially those of Bacillus subtilis species, was modified with cholesterol (γ-PGA/Chol), and the γ-PGA/Chol conjugates were used to form polymeric nanoparticles the size of 21.0±1.1 nm in aqueous solution. When the polymeric nanoparticles were mixed with doxorubicin (Dox), raspberry-like hydrogel particles (RBHPs) were formed by the electrostatic interaction between the cationically charged Dox and the anionically charged nanoparticles...
2016: International Journal of Nanomedicine
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