Resveratrol (3,5,4′-trihydroxy-trans-stilbene) is a polyphenol found in various plants, especially in the skin of red grapes. The effect of resveratrol on human health is the topic of numerous studies. In fact this molecule has shown anti-cancer, anti-inflammatory, blood-sugar-lowering ability and beneficial cardiovascular effects. However, for many polyphenol compounds of natural origin bioavailability is limited by low solubility in biological fluids, as well as by rapid metabolization in vivo. Therefore, appropriate carriers are required to obtain efficient therapeutics along with low administration doses.Liposomes are excellent candidates for drug delivery purposes, due to their biocompatibility, wide choice of physico-chemical properties and easy preparation.In this paper liposome formulations made by a saturated phosphatidyl-choline (DPPC) and cholesterol (or its positively charged derivative DC-CHOL) were chosen to optimize the loading of a rigid hydrophobic molecule such as resveratrol.Plain and resveratrol loaded liposomes were characterized for size, surface charge and structural details by complementary techniques, i.e. Dynamic Light Scattering (DLS), Zeta potential and Small Angle X-ray Scattering (SAXS). Nuclear and Electron Spin magnetic resonances (NMR and ESR, respectively) were also used to gain information at the molecular scale.The obtained results allowed to give an account of loaded liposomes in which resveratrol interacted with the bilayer, being more deeply inserted in cationic liposomes than in zwitterionic liposomes. Relevant properties such as the mean size and the presence of oligolamellar structures were influenced by the loading of RESV guest molecules.The toxicity of all these systems was tested on stabilized cell lines (mouse fibroblast NIH-3T3 and human astrocytes U373-MG), showing that cell viability was not affected by the administration of liposomial resveratrol.
In the presence of poly(ethylene glycol) (PEG),
α-cyclodextrin forms a molecular adduct called
“molecular
necklace” that belongs to the class of polyrotaxanes. The
condensation of α-cyclodextrin with epichlorohydrin
results in the formation of the so-called “molecular tube” (MT), a
rodlike rigid molecule with an empty
hydrophobic cavity that can behave as a host for ions or small organic
molecules. MT has been obtained
from PEG3350, considerably longer than the chain used in
previous works. This paper reports an NMR
investigation of the dynamic properties, via carbon spin−lattice
relaxation technique, of α-cyclodextrin, the
molecular necklace, and the molecular tube. The results show that
the molecular tube is really formed by a
linear thread of condensed α-cyclodextrin molecules and that MT
possesses a faster reorientational motion
than all the other compounds. UV spectroscopy shows that the
molecular tube forms a host−guest system
with iodine (I3
-) in aqueous
solution.
Proton NMR selective and non-selective spin-lattice relaxation rate measurements were used to monitor the strength of the overall complexation behaviour of a ligand (carbamazepine) toward a macromolecular receptor (albumin). The 'affinity index,' a quantitative parameter related to the strength of the ligand-macromolecule interaction, was determined from the experimental contribution of the bound ligand molar fraction to the observed selective spin-lattice relaxation rate. The effect of a second ligand (lamotrigine) on the carbamazepine-albumin interaction was also investigated and was found to have a modulation effect on the carbamazepine-albumin interaction.
We investigated whether static electromagnetic fields (EMFs) at a flux density of 4.75 T, generated by an NMR apparatus (NMRF), could promote movements of Ca2+, cell proliferation, and the eventual production of proinflammatory cytokines in human peripheral blood mononuclear cells (PBMC) as well as in Jurkat cells, after exposure to the field for 1 h. The same study was also performed after activation of cells with 5 mg/ml phytohaemagglutinin (PHA). Our results clearly demonstrate that static NMRF exposure has neither proliferative, nor activating, nor proinflammatory effects on both normal and PHA activated PBMC. Moreover, the concentration of interleukin-1beta, interleukin-2, interleukin-6, interferon, and tumour necrosis factor alpha (TNFalpha) remained unvaried in exposed cells. Exposure of Jurkat cells statistically decreased the proliferation and the proliferation indexes, which 24 and 48 h after exposure were 0.7 +/- 0.29 and 0.87 +/- 0.12, respectively. Moreover, in Jurkat cells the [Ca2+]i was higher than in PBMC and was reduced significantly to about one half after exposure. This is consistent with the decrease of proliferation and with the low levels of IL-2 measured. On the whole, our data suggest that NMRF exposure failed to affect the physiologic behaviour of normal lymphomonocytes. Instead in Jurkat cells, by changing the properties of cell membranes, NMRF can influence Ca2+ transport processes, and hence Ca2+ homeostasis with improvement of proliferation.
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