Search results for "Polyamines"
showing 10 items of 89 documents
Development of Polyamine‐Substituted Triphenylamine Ligands with High Affinity and Selectivity for G‐Quadruplex DNA
2019
Currently, significant efforts are devoted to designing small molecules able to bind selectively to guanine quadruplexes (G4s). These noncanonical DNA structures are implicated in various important biological processes and have been identified as potential targets for drug development. Previously, a series of triphenylamine (TPA)-based compounds, including macrocyclic polyamines, that displayed high affinity towards G4 DNA were reported. Following this initial work, herein a series of second-generation compounds, in which the central TPA has been functionalised with flexible and adaptive linear polyamines, are presented with the aim of maximising the selectivity towards G4 DNA. The acid-bas…
Polyaspartamide-Doxorubicin Conjugate as Potential Prodrug for Anticancer Therapy
2015
Purpose To synthesize a new polymeric prodrug based on ?,?- poly(N-2-hydroxyethyl)(2-aminoethylcarbamate)-d,l-aspartamide copolymer bearing amine groups in the side chain (PHEA-EDA), covalently linked to the anticancer drug doxorubicin and to test its potential application in anticancer therapy. Methods The drug was previously derivatized with a biocompatible and hydrophilic linker, leading to a doxorubicin derivative highly reactive with amino groups of PHEA-EDA. The PHEAEDA- DOXO prodrug was characterized in terms of chemical stability. The pharmacokinetics, biodistribution and cytotoxicity of the product was investigated in vitro and in vivo on human breast cancer MCF-7 and T47D cell lin…
Chemical speciation of nucleotide 5′-monophosphates in the presence of biogenic amines
2001
The interaction of adenosine-, uridine-, inosine- and guanosine-5’-monophosphates with protonated ethylenediamine, putrescine, cadaverine, spermidine and spermine, was studied potentiometrically, a...
Biocompatible hydrogels based on hyaluronic acid cross-linked with a polyaspartamide derivative as delivery systems for epithelial limbal cells.
2011
The aim of this work was to evaluate the potential use of hydrogels based on hyaluronic acid (HA) chemically cross-linked with α,β-poly(N-2-hydroxyethyl) (2-aminoethylcarbamate)-D,L-aspartamide (PHEA-EDA) as substitutes for the amniotic membrane able to release limbal cells for corneal regeneration. Hydrogels, shaped as films, with three different molar ratios (X) between PHEA-EDA and HA (X = 0.5, 1.0 and 1.5) have been investigated. First, it has been evaluated their swelling ability, hydrolytic resistance in simulated physiological fluid and cell compatibility by using human dermal fibroblasts chosen as a model cell line. Then adhesion studies in comparison with collagen gel, have been pe…
Interactions between Polyamines and Abiotic Stress Pathway Responses Unraveled by Transcriptome Analysis of Polyamine Overproducers
2011
Plant development and productivity are negatively regulated by adverse environmental conditions. The identification of stress-regulatory genes, networks, and signaling molecules should allow the development of novel strategies to obtain tolerant plants. Polyamines (PAs) are polycationic compounds with a recognized role in plant growth and development, as well as in abiotic and biotic stress responses. During the last years, knowledge on PA functions has been achieved using genetically modified plants with altered PA levels. In this review, we combine the information obtained from global transcriptome analyses in transgenic Arabidopsis plants with altered putrescine or spermine levels. Compa…
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic pha…
2012
The in vitro and in vivo anti- Trypanosoma cruzi activity of the pyrazole-containing macrobicyclic polyamine 1 and N-methyl- and N-benzyl-substituted monocyclic polyamines 2 and 3 was studied. Activity against both the acute and chronic phases of Chagas disease was considered. The compounds were more active against the parasite and less toxic against Vero cells than the reference drug benznidazole, but 1 and 2 were especially effective, where cryptand 1 was the most active, particularly in the chronic phase. The activity results found for these compounds were complemented and discussed by considering their inhibitory effect on the iron superoxide dismutase enzyme of the parasite, the nature…
New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
2018
Abstract Despite the continuous research effort that has been made in recent years to find ways to treat the potentially life threatening Chagas disease (CD), this remains the third most important infectious disease in Latin America. CD is an important public health problem affecting 6–7 million people. Since the need to search for new drugs for the treatment of DC persists, in this article we present a panel of new polyamines based on the tripodal structure of tris(2-aminomethyl)amine (tren) that can be prepared at low cost with high yields. Moreover, these polyamines present the characteristic of being water-soluble and resistant to the acidic pH values of stomach, which would allow their…
Simple high-performance liquid chromatographic assay for polyamines and their monoacetyl derivatives.
1993
A rapid reversed-phase high-performance liquid chromatographic method, using pre-column derivatization with benzoyl chloride and ultraviolet detection at 254 nm, was developed for the simultaneous measurement of polyamines and their monoacetyl derivatives. Calibration curves were linear for concentrations from 1.25 to 25 nmol/ml. The method was employed to assay these compounds in chick embryo retina explants using organic solvent extraction and 1,7-diaminoheptane as an internal standard. This simple and sensitive method can be applied to routine determinations of these compounds in various biological samples.
Rapid and simultaneous high-performance liquid chromatography assay of polyamines and monoacetylpolyamines in biological specimens
2000
A rapid, resolutive and reproducible reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed for polyamines and acetylpolyamines by adopting pre-column derivatization with benzoyl chloride. In a single run lasting less than 15 min ten polyamines were separated as well as traces of benzoic acid, methylbenzoate and benzoic anhydride. These contaminants, produced during the derivatization reaction, were almost all eliminated by washing steps envisaged in the same procedure. This simple and sensitive method can be applied to routine determination of polyamines in biological samples. A fine application of this procedure to the determination of endogenous content of p…
Cascade complex formation by phosphate in the cobalt(II)/[30]aneN10 anaerobic system
1993
Abstract The interaction of phosphate with the mono- and binuclear cobalt(II) complexes of [30]aneN 10 (1,4,7,10,13,16,19,22,25,28-decaazacyclotriacontane) has been studied by potentiometry in 0.15 mol dm −3 NaClO 4 solution at 298.15 K under anaerobic conditions. The stable species [CoH 2 ([30]aneN 10 )PO 4 ] + , [CoH 4 ([30]aneN 10 )PO 4 ] 3+ , [Co 2 H([30]aneN 10 )PO 4 ] 2+ , [Co 2 H 2 ([30]aneN 10 )PO 4 ] 3+ and [Co 2 H 3 ([30]aneN 10 )PO 4 ] 4+ , where the phosphate anion is directly bound to the metal ions or acts as a second sphere ligand, are formed and their stability constants have been determined. The results obtained allowed for the selection of suitable conditions for the study…