N-Phthaloyl-glycine-hydroxamic acid as serum iron chelator in rats

Abstract

Major functions of iron, as an essential element for living organisms, are oxygen transport and its role in oxidative-reductive reactions that utilize its alternative ferrous--ferric states. Total body iron has to be strictly controlled because excess iron can be highly toxic, leading, through generation of reactive oxygen species (ROS), to iron overloading disorders (1, 2). Iron chelating therapy has long been the standard care for patients suffering from Thalassemias (anemias caused by mutation of globin genes) and other anemias, caused e.g. by renal dysfunction (lack of erythropoietin (EPO) production), and for patients receiving transfusion iron supplementation. Iron chelators are used to treat dialyzed patients; in kidney transplantation, cardiac diseases, malaria, iron poisoning, and can inhibit tumor cell growth. They are also used to stimulate EPO production (3-5).Various structures of iron chelates have been investigated but the best known and in use for more than 40 years is desferrioxamine (DFO), despite its poor membrane permeability, short shelf life, difficulties in application and expensiveness. DFO is a natural hydroxamic acid (HA) of the microorganism Streptomyces sp. and belongs to sideropho- The aim of this study was to investigate the activity of N-phthaloyl-glycine-hydroxamic acid (Phth-Gly-HA) as a new iron chelator in vivo to be used in iron overload diseases. After intraperitoneal application of Phth-Gly-HA to male rats (1 mg kg -1 body mass) once a day for seven days, iron serum level decreased by 21%, whereas the iron value dropped by 32% in female rats (1.5 mg kg -1 body mass).The results indicate that the tested substance has the ability to bind serum iron by complexation. Besides transferrin iron release, mobilization of ferritin iron is also possible.

Iron chelation and liver disease healing activity of edible mushroom (Cantharellus cibarius), in vitro and in vivo assays

“…They can inhibit tumour cell growth too. 25 In the current work we studied the iron chelating activity of edible mushroom C. cibarius as a natural compound. Among all the body organs, liver is more susceptible to iron overloading damages; therefore we used liver tissue in a pathological study to show the iron overloading damages and to display the potential inhibitory effects of mushroom extract.…”

2-(4-Amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-ylmethyl)isoindoline-1,3-dione

“…For related literature, see: Allen et al (1987); Antunes et al (1998); Barooah et al (2006a,b); Brana & Ramos (2001); Chandrasekhar et al (1999); Eugenio, et al (2004); Gö rner et al (2002); Khan & Ismail (2002); Matijević-Sosa & Cvetnić (2005); Neto et al (1993); Ng (1992); Shariat & Abdollahi (2004); Wang et al (1998); Xu et al (2005), Zhang et al (2004). Hydrogen-bond geometry (Å , ).…”

“…Such phthalimide derivatives undergo photochemical reactions such as photochemical decomposition and decarboxylation (Görner et al, 2002). Moreover N-phthaloylamino acids and their derivatives possess a wide range of biological activities such as hypolipidemic (Neto et al, 1993) analgesic (Antunes et al, 1998) antimicrobial (Matijević-Sosa & Cvetnić, 2005) and DNA cleaving abilities (Brana & Ramos, 2001). Among the N-phthaloylamino acids, N-phthaloylglycine has been the most widely studied.…”

Keto- Enol Tautomerism of 2-Hydroxy Naphthylideneaniline with Lanthanide Shift Reagent Pr(fod)3in Different Solvents

“…mixed solvents, and it was established that the tautomeric equilibrium in 2-hdroxynaphthy lideneaniline schiff-bases depend on the polarity of the solvent, the acidity of the medium, the temperature, and the strength of the hydrogen bond. [6][7][8] Theoretical studies of tautomeric equilibrium in orhto-hydroxy schiff-bases have been reported. [9][10][11] Earlier [12][13][14] we have reported the cistrans isomerization of benzylideneaniline on addition of Eu(fod) 3 .…”