Search results for "lactone"
showing 10 items of 335 documents
Understanding the role of graphene oxide in the capture and eradication of circulating tumor cells
2016
The capture of circulating cancer cells on functional biomaterials is expected to control metastatic spread of a tumor, which is related to good probability containing the progression of disease burden. (1) The physicochemical characteristics of a biomaterial surface highly affect cell recruitment and adhesion, which is of great importance in such applications. Here, we designed a poly(caprolactone)-based nanocompsite scaffold, henceforth PCLMF-GO, to simultaneously recruit and kill circulating cancer cells by tuning physicochemical features of the scaffold surface through nitrogen plasma activation and hetero-phase graphene oxide (GO) covalent functionalization. Nitrogen plasma activation …
New approach for synthesis of poly(ethylglyoxylate) using Maghnite-H + , an Algerian proton exchanged montmorillonite clay, as an eco-catalyst
2017
International audience; In this works, we have explored a new method for a green synthesis of poly(ethylglyoxylate) (PEtG). This method consists on using a montmorillonite clay called Maghnite-H+ as an eco-catalyst to replace triethylamine which is toxic. Cationic polymerization experiments are performed in bulk conditions at three temperatures (-40 degrees C, 25 degrees C, 80 degrees C) and in THF solutions at room temperature (25 degrees C). At 25 degrees C, an optimum ratio of 5 wt% of catalyst leads to molar masses up to 22000 g/mol in THF solutions. Polymerizations in bulk conditions lead to slightly lower masses than experiments conducted in THF solutions. However, bulk polymerization…
Stereoselective Access to Fluorinated and Non-fluorinated Quaternary Piperidines: Synthesis of Pipecolic Acid and Iminosugar Derivatives
2012
The preparation of optically pure quaternary piperidines, both fluorinated and non-fluorinated, has been achieved from a chiral imino lactone derived from (R)-phenylglycinol. In the case of the fluorinated derivatives, the addition of (trifluoromethyl)trimethylsilane (TMSCF(3)) followed by iodoamination and migration of the CF(3) group allowed access to four derivatives of α-(trifluoromethyl)pipecolic acid. A theoretical study of the CF(3)-group rearrangement has been carried out to help establish the reaction mechanism of this uncommon transformation. Moreover, a route to trifluoromethyl-substituted iminosugars was also developed through the diastereoselective dihydroxylation of suitable s…
Assessment of the Optimum Linker Tethering Site of Alternariol Haptens for Antibody Generation and Immunoassay Development
2021
Immunochemical methods for mycotoxin analysis require antigens with well-defined structures and antibodies with outstanding binding properties. Immunoreagents for the mycotoxins alternariol and/or alternariol monomethyl ether have typically been obtained with chemically uncharacterized haptens, and antigen conjugates have most likely been prepared with mixtures of functionalized molecules. For the first time, total synthesis was performed, in the present study, to obtain two haptens with opposite linker attachment locations. The functionalized synthetic haptens were purified and deeply characterized by different spectrometric methods, allowing the preparation of bioconjugates with unequivoc…
Nanoparticle formulations as recrystallization inhibitors in transdermal patches
2020
Abstract Drug crystallization in transdermal patches is still a major challenge, confronting the formulation development of topical drug delivery systems. Encapsulation of drugs into nanoparticles is proposed here as a promising tool for regulating drug crystallization in transdermal patches. The degree of recrystallization and transdermal permeation of ibuprofen and hydrocortisone loaded in polymeric and lipid nanoparticles from matrix-type transdermal patches were investigated. Ethyl cellulose (EC4), poly (lactide-co-glycolic acid) (PLGA) and polycaprolactone (PCL) were employed for polymeric nanoparticle preparations; while medium chain triglyceride (MCT) and witepsol were used for the p…
Gamma-valerolactone from levulinic acid and its esters: Substrate and reaction media determine the optimal catalyst
2021
13 figures, 7 tables.-- © 2021. This manuscript version is made available under the CC-BY-NC-ND 4.0 license https://creativecommons.org/licenses/by-nc-nd/4.0
Novel Paraoxonase 2-Dependent Mechanism Mediating the Biological Effects of the Pseudomonas aeruginosa Quorum-Sensing Molecule N-(3-Oxo-Dodecanoyl)-l…
2015
ABSTRACT Pseudomonas aeruginosa produces N -(3-oxo-dodecanoyl)- l -homoserine lactone (3OC12), a crucial signaling molecule that elicits diverse biological responses in host cells thought to subvert immune defenses. The mechanism mediating many of these responses remains unknown. The intracellular lactonase paraoxonase 2 (PON2) hydrolyzes and inactivates 3OC12 and is therefore considered a component of host cells that attenuates 3OC12-mediated responses. Here, we demonstrate in cell lines and in primary human bronchial epithelial cells that 3OC12 is rapidly hydrolyzed intracellularly by PON2 to 3OC12 acid, which becomes trapped and accumulates within the cells. Subcellularly, 3OC12 acid acc…
Novel indole alkaloids from cell suspension cultures of aspidosperma quebracho blanco schlecht
1991
Abstract Two novel monoterpenoid indole alkaloids, aspidochibine ( 1 ) and 3-oxo-14,15-dehydrorhazinilam ( 2 ), were isolated from cell suspension cultures of Aspidosperma quebracho blanco Schlecht. Aspidochibine ( 1 ) exhibits a new alkaloid skeleton. The structure of these alkaloids was elucidated by spectroscopic methods.
SYNTHESIS AND PHOTOCHEMIOTHERAPEUTIC ACTIVITY OF THIOPYRANO[2,3-E]INDOL-2-ONES
2004
A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong antiproliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range.
THIOPYRANO[2,3-E]INDOL-2-ONES: ANGELICIN HETEROANALOGUES WITH POTENT PHOTOANTIPROLIFERATIVE ACTIVITY
2008
A new class of compounds, the thiopyrano[2,3-e]indol-2-ones, bioisosters of the angular furocoumarin angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents. In particular 7,8-dimethyl-thiopyranoindolone 6c s showed a remarkable phototoxicity and a great dose UVA dependence reaching IC(50) values at submicromolar level. This latter photoinduced a massive apoptosis and a remarkable photodamage to lipids and proteins. Although it did not intercalate DNA, it was able to cause photooxidation of DNA bases.