Binding properties of polyamidoamine dendrimers

ABSTRACT: Dendrimers are globular, hyperbranched polymers possessing a high concentration of surface functional groups and internal cavities. These unique features make them good host molecules for small ligands. To reveal relationships between dendrimer size and its encapsulating properties, the interactions of the fourth and the sixth generations of polyamidoamine dendrimers (PAMAM G4 and PAMAM G6) with a fluorescent dye 1-anilinonaphthalene-8-sulfonate (ANS) were studied. Because ANS is a fluorescent molecule and its fluorescence is very sensitive to changes in its microenvironment, it was possible to use spectrofluorometric methods to evaluate the interactions with dendrimers. A double fluorometric titration method was used to estimate a binding constant and the number of binding centers. There were two types of dendrimer binding centers characterized by different affinity towards ANS. For PAMAM G4, the values of K b and n for low-affinity and high-affinity sites equaled to 2.6 Â 10 5 , 0.60 and 3.70 Â 10 6 , 0.34, respectively, whereas in the case of PAMAM G6, these values equaled to 1.2 Â 10 5 , 76.34 and 1.38 Â 10 6 , 22.73. It was observed that the size of the dendrimer had a strong impact on the number of ANS molecules that interacted with dendrimers and their location within the macromolecule

Ultrasonic Formation of Fe3O4‑Reduced Graphene Oxide−Salicylic Acid Nanoparticles with Switchable Antioxidant Function

We demonstrate a single-step ultrasonic in situ complexation of salicylic acid during the growth of Fe3O4-reduced graphene oxide nanoparticles (∼10 nm) to improve the antioxidant and antiproliferative effects of pristine drug molecules. These nanoparticles have a precisely defined electronic molecular structure with salicylic acid ligands specifically complexed to Fe(III)/Fe(II) sites, four orders of magnitude larger electric surface potential, and enzymatic activity modulated by ascorbic acid molecules. The diminishing efficiency of hydroxyl radicals by Fe3O4-rGO-SA nanoparticles is tenfold higher than that by pristine salicylic acid in the electro-Fenton process. The H+ production of these nanoparticles can be switched by the interaction with ascorbic acid ligands and cause the redox deactivation of iron or enhanced antioxidation, where rGO plays an important role in enhanced charge transfer catalysis. Fe3O4-rGO-SA nanoparticles are nontoxic to erythrocytes, i.e., human peripheral blood mononuclear cells, but surpassingly inhibit the growth of three cancer cell lines, HeLa, HepG2, and HT29, with respect to pristine salicylic acid molecules

Biological properties of water-soluble phosphorhydrazone dendrimers

1984-8250Dendrimers are hyperbranched and perfectly defined macromolecules, constituted of branches emanating from a central core in an iterative fashion. Phosphorhydrazone dendrimers constitute a special family of dendrimers, possessing one phosphorus atom at each branching point. The internal structure of these dendrimers is hydrophobic, but hydrophilic terminal groups can induce the solubility of the whole structure in water. Indeed, the properties of these compounds are mainly driven by the type of terminal groups their bear; this is especially true for the biological properties. For instance, positively charged terminal groups are efficient for transfection experiments, as drug carriers, as anti-prion agents, and as inhibitor of the aggregation of Alzheimer's peptides, whereas negatively charged dendrimers have anti-HIV properties and can influence the human immune system, leading to anti-inflammatory properties usable against rheumatoid arthritis. This review will give the most representative examples of the biological properties of water-soluble phosphorhydrazone dendrimers, organized depending on the type of terminal groups they bear

Nitric oxide releasing-dendrimers: an overview

Platforms able to storage, release or scavenge NO in a controlled and specific manner is interesting for biological applications. Among the possible matrices for these purposes, dendrimers are excellent candidates for that. These molecules have been used as drug delivery systems and exhibit interesting properties, like the possibility to perform chemical modifications on dendrimers surface, the capacity of storage high concentrations of compounds of interest in the same molecule and the ability to improve the solubility and the biocompatibility of the compounds bonded to it. This review emphasizes the recent progress in the development and in the biological applications of different NO-releasing dendrimers and the nitric oxide release pathways in these compounds

Activation of ibuprofen via ultrasonic complexation with silver in N-doped oxidized graphene nanoparticles for microwave chemotherapy of cervix tumor tissue

An ultrasonic method (20 kHz) is introduced to activate pristine ibuprofen organic molecular crystals via complexation with silver in nitrogen-doped oxidized graphene nanoplatforms (∼50 nm). Ultra9 sonic complexation occurs in a single-step procedure through the binding of the carboxylic groups with Ag, H-bond formation, involving noncovalent πC=C → πC=C* transitions in the altered phenyl ring and πPY → πCO* in ibuprofen occurring between the phenyl ring and C−O bonds as a result of interaction with hydroxyl radicals. The ibuprofen−silver complex in ≪NrGO≫ exhibits a ∼42 times higher acceleration rate than free ibuprofen of the charge transfer between hexacyanoferrate and thiosulfate ions. The increased acceleration rate can be caused by electron injection/ejection at the interface of the ≪Ag-NrGO≫ nanoplatform and formation of intermediate species (Fe(CN)5(CNSO3)x− with x = 4 or 5 and AgHS2O3) at the excess of produced H+ ions. Important for microwave chemotherapy, ibuprofen−silver complexes in the ≪NrGO≫ nanoplatform can produce H+ ions at ∼12.5 times higher rate at the applied voltage range from 0.53 to 0.60 V. ≪Ibu-Ag-NrGO≫ NPs develop ∼105 order higher changes of the electric field strength intensity than free ibuprofen in the microwave absorption range of 100−1000 MHz as revealed from the theoretical modeling of a cervix tumor tissue