Green synthesis and biological evaluation of novel 5-fluorouracil derivatives as potent anticancer agents

This study reports the formation of 5-FU co-crystals with four different pharmacologically safe co-formers; Urea, Thiourea, Acetanilide and Aspirin using methanol as a solvent. Two fabrication schemes were followed i.e., solid-state grinding protocol, in which API and co-formers were mixed through vigorous grinding while in the other method separate solutions of both the components were made and mixed together. The adopted approaches offer easy fabrication protocols, no temperature maintenance requirements, no need of expensive solvents, hardly available apparatus, isolation and purification of the desired products. In addition, there is no byproducts formation, In fact, a phenomenon embracing the requirements of green synthesis. Through FTIR analysis; for API the Nsingle bondH absorption frequency was recorded at 3409.02 cm−1 and that of single bondCdouble bondO was observed at 1647.77 cm−1. These characteristics peaks of 5-FU were significantly shifted and recorded at 3499.40 cm−1 and 1649.62 cm−1 for 5-FU-Ac (3B) and 3496.39 cm−1 and 1659.30 cm−1 for 5-FU-As (4B) co-crystals for Nsingle bondH and single bondCdouble bondO groups respectively. The structural differences between API and co-crystals were further confirmed through PXRD analysis. The characteristic peak of 5-FU at 2θ = 28.79918o was significantly shifted in the graphs of co-crystals not only in position but also with respect to intensity and FWHM values. In addition, new peaks were also recorded in all the spectra of co-formers confirming the structural differences between API and co-formers. In addition, percent growth inhibition was also observed by all the co-crystals through MTT assay against HCT 116 colorectal cell lines in vitro. At four different concentrations; 25, 50, 100 and 200 µg/mL, slightly different trends of the effectiveness of API and co-crystals were observed. However; among all the co-crystal forms, 5-FU-thiourea co-crystals obtained through solution method (2B) proved to be the most effective growth inhibitor at all the four above mentioned concentrations

Study of a two steps process for the valorization of PVC-containing wastes

Published online 27 November 2012The presence of organic compounds in wastes, namely polymer based compounds, is considered a potential relevant source of energy. However, the presence of polyvinyl chloride (PVC) in their composition, causes recycling problems when a thermal process is considered for the wastes treatment [1] preventing its use on processes which the main goal is the energy recovery (Zevenhoven et al. in Fuel 81:507–510, 2002; Kim in Waste Manag 21:609–616, 2001). A possible solution should consider a first step for chlorine removal, through a pyrolysis process previously to a subsequent thermal treatment, for energetic valorization. The present work assesses a possible process for treating PVC-containing wastes in an environmentally friendly way. It is based on the effective de-chlorination of PVC-containing wastes through a pyrolysis process at low temperature before the carbonaceous residue (chlorine free fraction) being subjected to a subsequent thermal treatment for energetic valorization with the production of a synthesis gas (syngas). In the end of the process concentrated hydrochloric acid or other chlorine solutions and a syngas, with high energetic potential are obtained. The synthesis gas produced can be used in turbines or gas engines, replacing the gases obtained from fossil non-renewable resources. The validation of the proposed treatment of PVC-containing wastes in pilot scale has also been performed

Pyrolysis and combustion of municipal solid wastes:evaluation of synergistic effects using TGA-MS

A thermogravimetric methodology was developed to investigate and semi-quantify the extent of synergistic effects during pyrolysis and combustion of municipal solid waste (MSW). Results from TGA-MS were used to compare the pyrolysis and combustion characteristics of single municipal solid waste components (polyvinyl chloride (PVC), polypropylene (PP), polystyrene (PS), branches (BR), leaves (LV), grass (GR), packaging paper (PK), hygienic paper (HP) and cardboard (CB)) and a mixture (MX) of PP, BR and CB. Samples were heated under dynamic conditions at 20°C/min from 25°C to 1000°C with the continuous record of their main evolved fragments. Synergistic effects were evaluated by comparing experimental and calculated weight losses and relative areas of MS peaks. Pyrolysis of the mixture happened in two stages, with the release of H2, CH4, H2O, CO and CO2 between 200 and 415°C and the release of CH4, CxHy, CO and CO2 between 415 and 525°C. Negative synergistic effect in the 1st stage was attributed to the presence of PP where the release of hydrocarbons and CO2 from BR and CB was inhibited, whereas positive synergistic effects were observed during the 2nd degradation stage. In a second part of the study, synergistic effects were related to the dependency of the effective activation energy (Eα) versus the conversion (α). Higher Eαs were obtained for MX during its 1st stage of pyrolysis and lower Eαs for the 2nd stage when compared to the individual components. On the other hand, mostly positive synergistic effects were observed during the combustion of the same mixture, for which lower Eαs were recorded

Mechanisms and modelling of phosphorus solid-liquid transformation during the hydrothermal processing of swine manure

Phosphorus (P) recovery from swine manure by hydrothermal processes has recently attracted considerable interest; however, research has been limited by knowledge gaps and challenges in understanding the mechanisms of soluble and insoluble P transformations and the evaluation of the effects of the reaction conditions. In this study, the transformation mechanisms were investigated and the soluble and insoluble phosphorus distributions in swine manure during the hydrothermal processes were modelled. By increasing the severity of the exogenous conditions, P transformed from insoluble to soluble, and then polymerized with the formation of orthophosphates; meanwhile, the formation of hydrochar was enhanced thereby facilitating further P reclamation. The effects of the endogenous conditions showed there may be a threshold of calcium content, which limited the combination of Ca and P. Calcium ions mainly reacted with P in the form of hydroxyapatite and octacalcium phosphate. The modelling and prediction results showed that a coalification model gives a good fit (RSP2= 0.9205 andRIP2= 0.8559) for changes in the concentrations of solid total P and liquid inorganic P. The prediction level of mean absolute error was good as well (MAESP= 0.74 mg g−1and MAEIP= 0.62 mg g−1). These findings provide a range of scientific opportunities for achieving a comprehensive understanding of the basis of sustainable utilisation of P

SAUDI PHARMACEUTICAL JOURNAL

5-Fluorouracil is one of the first line drugs for the systemic therapy of solid tumors like breast, colorectal, oesophageal, stomach, pancreatic, head and neck. It could be shown that sugars can improve the absorption across cell membranes and can help to bypass some pharmacokinetic problems. Carbohydrates as most common organic molecules are an important issue of plant and animal metabolisms. They are non toxic and have important duties in the body like participating in DNA and RNA synthesis and being responsible for energy production. In addition, they have many hydroxyl, aldehyde and ketone groups that attract attention for synthesis as a potential drug derivative. 1,2,3,-Triazole compounds have also important role in heterocyclic chemistry because of their pharmaceutical properties and their high reactivity, which could be used as a building block for complex chemical compounds. In this study, following the Click Reaction of 5-FU and tetra-O-acetylglycose the 5-fluorouracil derivative 1-[{1'-(2 '',3 '',4 '',6 ''-tetra-O-acetyl-beta-D-glycopyronosyl)-1'H-1',2',3'-triazole-4'-yl} methyl] 5-fluorouracil was synthesized. Following, a micellar formulation of 5-Fluorouracil derivative was prepared and characterized in terms of particle size, polydispersity index, zeta potential, refractive index and pH. Furthermore, the cytotoxicity and mutagenicity of the 5-fluorouracil derivative was investigated using an in vitro cell culture model and the AMES test. According to the results of this study, the novel 5-fluorouracil derivative could be a drug candidate for the therapy of cancer and needs further in vivo investigations. (C) 2018 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University

Liquefaction of Municipal Waste Plastics over Acidic and Nonacidic Catalysts

This chapter contains sections titled: Introduction Catalytic Liquefaction of MWP Conclusions References. © 2006 John Wiley & Sons, Ltd

Central possible antinociceptive mechanism of naringin

Background and Aims: The object of this study was the investigation of the central antinociceptive effects of naringin as well as the association of stimulation of opioidergic, serotonergic, adrenergic, and cholinergic (muscarinic and nicotinic) receptors to the central analgesia of mice due to naringin. Methods: Several intraperitoneal doses (20, 40, and 80 mg/kg) were injected into mice models and analyzed via hot-plate (integrated supraspinal response) and tail-immersion (spinal reflex) for the possible antinociceptive effects of naringin. Moreover, the involved action mechanism was investigated using 80 mg/kg naringin (i.p.) administered to the mice which were previously pre-treated with opioid antagonist naloxone (5 mg/kg, i.p.), serotonin 5-HT2A/2C receptor antagonist ketanserin (1 mg/kg, i.p.), alpha 2-adrenoceptor antagonist yohimbine (1 mg/kg, i.p.) and muscarinic antagonist atropine (5 mg/kg, i.p.), as well as nicotinic antagonist mecamylamine (1 mg/kg, i.p.). Results: It can be claimed that a dose-dependant antinociceptive effect of naringin was noticed for 40 and 80 mg/kg doses in tail-immersion and hot-plate tests, respectively. Furthermore, the improvement of inactivity of naringin-induced response to thermal stimuli was counteracted by mecamylamine and naloxone when tested with the tail-immersion test, and hot-plate analyses. Conclusion: From the data, it was confirmed that naringin presents central antinociceptive effects which may be coordinated by supraspinal/spinal mediated opioidergic and nicotinic (cholinergic) inflection. Nevertheless, it is unclear how naringin organizes the interactions of the aforementioned modulatory systems. To conclude, naringin could be a possible candidate for pain relief management.University of Health Sciences Scientific Research Projects Fund [2020/033]This study was supported by University of Health Sciences Scientific Research Projects Fund with the project number 2020/033

Synthesis of egonol derivatives and their antimicrobial activities

WOS: 000287419000021PubMed ID: 21251840Eighteen derivatives of egonol (A-R) were synthesized and evaluated for their antimicrobial activities against Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC 6633, Candida albicans ATCC 10231 and Escherichia coli ATCC 8739 microorganisms comparing with egonol. The obtained data reported that compound B exhibited improved activities against all tested bacteria than egonol, others have shown different range of activities. (C) 2010 Elsevier Ltd. All rights reserved.TUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [105T226]; Ege University Research FoundationEge University [2005 Fen 047]; Ege University ScienceEge University; Technology Application and Research Center [2007 Bil 036]This work was supported by TUBITAK (105T226), Ege University Research Foundation (2005 Fen 047) and Ege University Science, Technology Application and Research Center (2007 Bil 036). The authors thank Professor Dr. Misir Ahmedzade for his valuable suggestions for synthetic routes and also Assoc. Professor Dr. Yurdanur AKGUL for her assistance in some of the NMR analyses

Char and Coke Formation as Unwanted Side Reaction of the Hydrothermal Biomass Gasification

WOS: 000261134400002The hydrothermal biomass gasification is a promising technology, to produce hydrogen and/or methane from wet biomass with a water Content of >= 80% (g/g). In the process, the coke formation usually is very low, but already low amounts problems like, e.g., fouling in the heat exchanger. To learn more about the product formation, the results of the hydrothermal treatment (at 400, 500, 600 degrees C and 1 h) of different biomass feedstocks (artichoke stalk, pinecone, sawdust, and cellulose as model biomass) in a microreactor are compared. The gas composition and the total organic carbon content of the aqueous phase were determined after reaction. The gas formation rises with increasing temperature. The formation of carbon deposits and their characterization has been investigated by scanning electron microscopy (SEM). The variation of the solid morphology during the hydrothermal conversion is discussed based on chemical pathways occurring during hydrothermal biomass degradation.DAAD (German Academic Exchange Service)Deutscher Akademischer Austausch Dienst (DAAD)The authors gratefully acknowledge A. Bohm and A. Lauten-bach for TOC analysis. Our special thanks are to F. Schubel and J. Lamla for mechanical Support and to W. Habicht for SEM analysis. The authors Would also like to acknowledge DAAD (German Academic Exchange Service) for financially Supporting Dr. Ali Sinag and Dr. Tainer Karayildirim through the re-invitation program