Synthesis, characterizzation, in vitro antimicrobial and anticancer studies of new platinum N-heterocyclic carbene (NHC) complexes and unexpected nickel complexes

Publication date: Available online 16 July 2019Source: Journal of Organometallic ChemistryAuthor(s): Kar Bee Choo, Sui Mae Lee, Wai Leng Lee, Yuen Lin CheowAbstractA series of bidendate pyridine-functionalized metal N-heterocyclic carbene (NHC) complexes with various wingtip substituents (R = methyl, phenyl and tert-butyl) had been prepared from silver oxide-mediated transmetalation method. The basic backbone of the NHC ligands were prepared in two stepwise reactions: reduction of the commercially available 2-benzoylpyridine, followed by halogenation to yield 2-(chloro(phenyl)methyl)pyridine. Subsequent reactions with different imidazoles gave the desired imidazolium salts (or NHC precursors) with different R groups at the N wingtip (R = Me, Ph, t-Bu). Transmetalation of the imidazolium salts into platinum NHC complexes were achieved by using Ag2O mediated method with Pt(cod)Cl2 as the transmetalating agent. On the other hand, nickel NHC complexes were obtained via one pot synthesis method with nickel chloride as the transmetalating agent and reflux in the presence of a base. Following recrystallisation, the molecular structure of Pt NHC complex ( ± )-5a had been successfully elucidated via single crystal X ray diffraction (XRD) analysis. The six-membered ring of the platinum NHC complexes adopted a boat conformation with the phenyl ring arranged at the axial position. Meanwhile, two unexpected nickel complexes, i.e. a simple nickel coordination complex and a n...
Source: Journal of Organometallic Chemistry - Category: Chemistry Source Type: research

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WEDNESDAY, Aug. 21, 2019 -- Oral antibiotic use is associated with an increased risk for colon cancer and a reduced risk for rectal cancer, according to a study published online Aug. 20 in Gut. Jiajia Zhang, M.D., M.P.H., from the Bloomberg-Kimmel...
Source: Drugs.com - Pharma News - Category: Pharmaceuticals Source Type: news
Abstract The aim of this study was to determine the efficacy of oral recombinant methioninase (o-rMETase) on a colon cancer primary tumor using a patient-derived orthotopic xenograft (PDOX) nude mouse model. Forty colon cancer primary tumor PDOX mouse models were divided into 4 groups of 10 mice each (total 40 mice) by measuring the tumor size. The groups were as follows: untreated control; 5-fluorouracil (5-FU) (50 mg/kg, once a week for two weeks, N = 10 mice) and oxaliplatinum (OXA) (6 mg/kg, once a week for two weeks, N = 10 mice); o-rMETase (100 units/day, oral 14 consecutive days, N = 1...
Source: Biochemical and Biophysical Research communications - Category: Biochemistry Authors: Tags: Biochem Biophys Res Commun Source Type: research
Abstract Due to the decrease of the drugs side effects in controlled drug delivery systems, today's many research has been focused on designing the new controlled drug delivery systems. The main aim of the present work was the improving of the layered double hydroxide (LDH) properties as a drug delivery system through the encapsulation with carboxymethyl cellulose (CMC). In the first section, 5-fluorouracil (5-Fu) as a colon anticancer drug was loaded in LDH(Zn/Al) (about 87%). The FT-IR, SEM, and XRD analysis were used to probe the successful synthesis of LDH(Zn/Al) and 5-Fu loading in it. In the following, the n...
Source: International Journal of Biological Macromolecules - Category: Biochemistry Authors: Tags: Int J Biol Macromol Source Type: research
ConclusionsOverall risk of cancer in our MS cohort did not significantly differ from the controls. However, the age at diagnosis of breast cancer was statistically significantly higher among the MS patients in comparison with a control population from the same patient pool. Further population-based larger studies spanning longer follow-up periods and longer exposure to emerging MS therapies are needed to evaluate cancer risk related to MS treatments and breast cancer risk in particular.
Source: Multiple Sclerosis and Related Disorders - Category: Neurology Source Type: research
Publication date: September 2019Source: Colloid and Interface Science Communications, Volume 32Author(s): Rayan Sabra, Clive J. Roberts, Nashiru BillaAbstractWe aimed to probe the carrier properties of a colon-targeted curcumin-containing modified pectinate-chitosan nanoparticulate carrier system (MCPCNPs), in simulated colonic condition. The MCPCNPs were prepared via ionic gelation. There was a reduction in zeta potential (ZP) of the MCPCNPs at pH 1.2 and a more significant reduction at pH 7.0, both mucin concentration-dependent. A reduction in ZP correlates mucoadhesive propensity. Nanoparticle tracking analyses (NTA...
Source: Colloids and Interface Science Communications - Category: Nanotechnology Source Type: research
CONCLUSION: This is the first report of bilateral sensorineural hearing loss induced by regorafenib. PMID: 31381817 [PubMed - as supplied by publisher]
Source: Clinical Colorectal Cancer - Category: Cancer & Oncology Authors: Tags: J Clin Pharm Ther Source Type: research
Publication date: Available online 3 August 2019Source: Colloids and Surfaces B: BiointerfacesAuthor(s): Heyu Li, Brenda Sanchez-Vazquez, Rita P. Trindade, Qiaobei Zou, Yang Mai, Liu Dou, Li-Min Zhu, Gareth R. WilliamsAbstractIn this work, we report new formulations for the combined photo-chemotherapy of colon cancer. Fibers were fabricated via coaxial-electrospinning with the intent of targeting delivery of the anti-cancer drug carmofur (CAR) and the photosensitizer rose bengal (RB) selectively to the colon site. The fibers comprised a hydroxypropyl methylcellulose (HPMC) core loaded with the active ingredients, and a pH-...
Source: Colloids and Surfaces B: Biointerfaces - Category: Biochemistry Source Type: research
Publication date: Available online 30 July 2019Source: Nanomedicine: Nanotechnology, Biology and MedicineAuthor(s): Ruoning Wang, Jinyu Huang, Jian Chen, Mengmeng Yang, Honglan Wang, Hongzhi Qiao, Zhipeng Chen, Lihong Hu, Liuqing Di, Junsong LiAbstractColon adenocarcinoma is the third most common cause of cancer-related deaths worldwide owing to its aggressive nature. Here, we developed a novel oral drug delivery system (DDS) that comprised active targeted nanoparticles made from gelatin and chitosan (non-toxic polymers). The nanoparticles were fabricated using a complex coacervation method, which was accompanied by conjug...
Source: Nanomedicine: Nanotechnology, Biology and Medicine - Category: Nanotechnology Source Type: research
In this study we established a new animal model of spleen deficiency and cancer cachexia in mice and evaluated the therapeutic effects of atractylenolide I, an active component of tonifying TCM BaiZhu, in the mouse model. Cancer cachexia was induced in male BALB/c mice by inoculation of mouse C26 colon adenocarcinoma cells, whereas spleen deficiency syndrome was induced by treating the mice with spleen deficiency-inducing factors, including limited feeding, fatigue, and purging. The mouse model was characterized by both cachexia and spleen deficiency characteristics, including significant body weight loss, cancer growth, m...
Source: Acta Pharmacologica Sinica - Category: Drugs & Pharmacology Authors: Tags: Acta Pharmacol Sin Source Type: research
Publication date: 15 October 2019Source: Journal of Organometallic Chemistry, Volume 898Author(s): Kar Bee Choo, Sui Mae Lee, Wai Leng Lee, Yuen Lin CheowAbstractA series of bidendate pyridine-functionalized metal N-heterocyclic carbene (NHC) complexes with various wingtip substituents (R = methyl, phenyl and tert-butyl) had been prepared from silver oxide-mediated transmetalation method. The basic backbone of the NHC ligands were prepared in two stepwise reactions: reduction of the commercially available 2-benzoylpyridine, followed by halogenation to yield 2-(chloro(phenyl)methyl)pyridine. Subsequent reactions with di...
Source: Journal of Organometallic Chemistry - Category: Chemistry Source Type: research
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