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1.
Molecules ; 25(24)2020 Dec 09.
Article in English | MEDLINE | ID: mdl-33317120

ABSTRACT

The main objectives of this study were to evaluate the chemical constitution and allergenic potential of red propolis extract (RPE). They were evaluated, using high performance liquid chromatography (HPLC) and the release of ß-hexosaminidase, respectively. A plethora of biologically active polyphenols and the absence of allergic responses were evinced. RPE inhibited the release of ß-hexosaminidase, suggesting that the extract does not stimulate allergic responses. Additionally, the physicochemical properties and antibacterial activity of hydrogel membranes loaded with RPE were analyzed. Bio-polymeric hydrogel membranes (M) were obtained using 5% carboxymethylcellulose (M1 and M2), 1.0% of citric acid (M3) and 10% RPE (for all). Their characterization was performed using thermal analysis, Fourier transform infrared (FTIR), total phenolic content, phenol release test and, antioxidant activity through 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and Ferric Reducing Antioxidant Power (FRAP). The latter appointed to the similar antioxidant capacity of the M1, M2 and M3. The degradation profiles showed higher thermostability to M3, followed by M2 and M1. The incorporation of RPE into the matrices and the crosslinking of M3 were evinced by FTIR. There were differences in the release of phenolic compounds, with a higher release related to M1 and lower in the strongly crosslinked M3. The degradation profiles showed higher thermostability to M3, followed by M2 and M1. The antibacterial activity of the membranes was determined using the disc diffusion assay, in comparison with controls, obtained in the same way, without RPE. The membranes elicited antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis, with superior performance over M3. The hydrogel membranes loaded with RPE promote a physical barrier against bacterial skin infections and may be applied in the wound healing process.


Subject(s)
Propolis/chemistry , Administration, Topical , Allergens/chemistry , Animals , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antioxidants/administration & dosage , Antioxidants/chemistry , Antioxidants/pharmacology , Bandages , Biocompatible Materials/administration & dosage , Biocompatible Materials/chemistry , Biocompatible Materials/pharmacology , Biopolymers/administration & dosage , Biopolymers/chemistry , Biopolymers/pharmacology , Brazil , Cell Line , Chemical Phenomena , Chromatography, High Pressure Liquid , Drug Compounding , Drug Stability , Humans , Hydrogels , In Vitro Techniques , Mast Cells/drug effects , Mast Cells/enzymology , Mast Cells/immunology , Membranes, Artificial , Phenols/chemistry , Propolis/administration & dosage , Propolis/pharmacology , Rats , Spectroscopy, Fourier Transform Infrared , Staphylococcus aureus/drug effects , Staphylococcus epidermidis/drug effects , Thermogravimetry , beta-N-Acetylhexosaminidases/metabolism
2.
Biochim Biophys Acta ; 1808(1): 55-64, 2011 Jan.
Article in English | MEDLINE | ID: mdl-20713019

ABSTRACT

Primaquine (PQ) is a potent therapeutic agent used in the treatment of malaria and its mechanism of action still lacks a more detailed understanding at a molecular level. In this context, we used differential scanning calorimetry (DSC), pressure perturbation calorimetry (PPC), and electron spin resonance (ESR) to investigate the effects of PQ on the lipid phase transition, acyl chain dynamics, and on volumetric properties of lipid model membranes. DSC thermograms revealed that PQ stabilizes the fluid phase of the lipid model membranes and interacts mainly with the lipid headgroups. This result was revealed by the great effect on the pretransition of phosphatidylcholines and the destabilization of the inverted hexagonal phase of a phosphatidylethanolamine bilayer. Spin probes located at different positions along the lipid chain were used to monitor different membrane regions. ESR results indicated that PQ is effective in changing the acyl chain ordering and dynamics of the whole chain of dimyristoylphosphatidylcholine (DMPC) phospholipid in the rippled gel phase. The combined ESR and PPC results revealed that the slight DMPC volume changes at the main phase transition induced by the presence of PQ is probably due to a less dense lipid gel phase. At physiological pH, the cationic amphiphilic PQ strongly interacts with the lipid headgroup region of the bilayers, causing considerable disorganization in the hydrophobic core. These results shed light on the molecular mechanism of primaquine-lipid interaction, which may be useful in the understanding of the complex mechanism of action and/or the adverse effects of this antimalarial drug.


Subject(s)
Antimalarials/pharmacology , Lipid Bilayers/chemistry , Lipids/chemistry , Membranes, Artificial , Primaquine/pharmacology , Calorimetry/methods , Calorimetry, Differential Scanning/methods , Cations , Dimyristoylphosphatidylcholine/chemistry , Electron Spin Resonance Spectroscopy , Hydrogen-Ion Concentration , Phospholipids/chemistry , Temperature
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