Association Behavior of the Synthetic Protein-Lipid Complex Analogues

2012 ◽  
Vol 506 ◽  
pp. 134-137
Author(s):  
P. Punyamoonwongsa ◽  
B.J. Tighe

Hypercoiling poly (styrene-alt-maleic anhydride) (PSMA) is known to undergo conformational transition in response to environmental stimuli. This behavior allows it to associate with the phospholipid,2-dilauryl-sn-glycero-3-phosphocholine (DLPC) to produce nanostructures analogous to lipoproteins. The complex represents a new bio-mimetic delivery vehicle with applications in the cosmetic and pharmaceutical industries. This study investigates, for the first time, the association behavior of PSMA and DLPC through the combination of different analytical techniques. The results indicate that the association is primarily driven by hydrophobic interactions and depends on various factors including the polymer/lipid ratio, the polymer molecular weight and the pH of the aqueous environment. The conformational transition of PSMA leads to the formation of discrete micellar complexes involving anisotropic-to-isotropic lipid phase transformation. As the number of hydrophobic moieties in the polymer is increased, the pH-dependent conformational transition of the polymer plays less important part in achieving this phase transition of the lipid.

Author(s):  
Jorge A. Ramos-Hernández ◽  
Montserrat Calderón-Santoyo ◽  
Armando Burgos-Hernández ◽  
Joel S. García- Romo ◽  
Arturo Navarro-Ocaña ◽  
...  

Background: Cancer is a disease characterized by the invasion and uncontrolled growth of cells. One of the best ways to minimize the harmful effects of mutagens is through the use of natural antimutagens. In this regard, the search for new antimutagens that act in the chemoprevention could represent a promising field in this area. Objective: In this study biological potential of 11 fractions from Coccoloba uvifera L. leaf hexane extract was evaluated by several in vitro tests. Methods: Leaves were lyophilized and hexane extraction was performed. The extract was fractionated by column chromatography with hexane, ethyl acetate, and methanol. The antimutagenic (Ames test), antiproliferative (MTT test), and antioxidant capacity (DPPH, ABTS, and ferrous ion chelation) of the fractions were evaluated. Results: Fractions 4, 6, 8, and 9 have antimutagenic activity (against sodium azide in strain TA100), fraction 11 showed antiproliferative capacity (IC50 of 24 ± 9 μg/mL in cells of HCT 116). The fractions with the highest activity were analyzed by HPLC-MS and lupeol, acacetin, and β-sitosterol were identified. Conclusion: This study demonstrates, for the first time, the bioactivity of C. uvifera leaf as a new source of high biological value compounds (HBVC), which can be of interest to the food and pharmaceutical industries.


Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4735
Author(s):  
Maša Knez Hrnčič ◽  
Darija Cör ◽  
Jana Simonovska ◽  
Željko Knez ◽  
Zoran Kavrakovski ◽  
...  

Phytochemical research based on ethnopharmacology is gaining interest in industries such as functional food, nutraceuticals, cosmetics and pharmaceutical industries. Plants and plant extracts are a rich source of bioactive secondary metabolites. These compounds are often involved in plant protection against biotic or abiotic stresses. The exploitation of available technologies should be oriented and intensified to extend and enhance the continued usefulness of the plants as renewable sources of chemicals, especially medicinal compounds. This current contribution is focused on extraction and analytical techniques for their isolation from the oregano species, their characterization and their potential antioxidative, as well as their antimicrobial, antifungal and anticarcinogenic properties. The work is structured rendering to the different steps involved in the research; starting with extraction and sample preparation, followed by discussing the analytical techniques employed for the isolation and identification of compound/s responsible for the biological activity and methods and techniques for biological activity assessment.


Marine Drugs ◽  
2020 ◽  
Vol 19 (1) ◽  
pp. 2
Author(s):  
Gina De La Fuente ◽  
Marco Fontana ◽  
Valentina Asnaghi ◽  
Mariachiara Chiantore ◽  
Serena Mirata ◽  
...  

Inflammation and oxidative stress are part of the complex biological responses of body tissues to harmful stimuli. In recent years, due to the increased understanding that oxidative stress is implicated in several diseases, pharmaceutical industries have invested in the research and development of new antioxidant compounds, especially from marine environment sources. Marine seaweeds have shown the presence of many bioactive secondary metabolites, with great potentialities from both the nutraceutical and the biomedical point of view. In this study, 50%-ethanolic and DMSO extracts from the species C. amentacea var. stricta were obtained for the first time from seaweeds collected in the Ligurian Sea (north-western Mediterranean). The bioactive properties of these extracts were then investigated, in terms of quantification of specific antioxidant activities by relevant ROS scavenging spectrophotometric tests, and of anti-inflammatory properties in LPS-stimulated macrophages by evaluation of inhibition of inflammatory cytokines and mediators. The data obtained in this study demonstrate a strong anti-inflammatory effect of both C. amentacea extracts (DMSO and ethanolic). The extracts showed a very low grade of toxicity on RAW 264.7 macrophages and L929 fibroblasts and a plethora of antioxidant and anti-inflammatory effects that were for the first time thoroughly investigated. The two extracts were able to scavenge OH and NO radicals (OH EC50 between 392 and 454 μg/mL; NO EC50 between 546 and 1293 μg/mL), to partially rescue H2O2-induced RAW 264.7 macrophages cell death, to abate intracellular ROS production in H2O2-stimulated macrophages and fibroblasts and to strongly inhibit LPS-induced inflammatory mediators, such as NO production and IL-1α, IL-6, cyclooxygenase-2 and inducible NO synthase gene expression in RAW 264.7 macrophages. These results pave the way, for the future use of C. amentacea metabolites, as an example, as antioxidant food additives in antiaging formulations as well as in cosmetic lenitive lotions for inflamed and/or damaged skin.


1989 ◽  
Vol 56 (3) ◽  
pp. 427-433 ◽  
Author(s):  
Charles W. Slattery ◽  
Satish M. Sood ◽  
Pat Chang

SummaryThe association of non-phosphorylated (0-P) and fully phosphorylated (5-P) human β-caseins was studied by fluorescence spectroscopy and laser light scattering. The tryptophan fluorescence intensity (FI) level increased between 20 and 35 °C, indicating a change in the environment of that residue. A similar transition occurred when ANS was used as a probe. Transition temperatures were slightly lower in 10 mM-CaCl2 but were not affected by an equivalent increase in ionic strength caused by NaCl. The magnitude of the FI change was less for the 5-P than the 0-P protein but was increased for both by CaCl2 addition. These FI data were characteristic of a conformational change and this was supported by fluorescence polarization which indicated that with CaCl2, tryptophan and ANS mobility increased at the transition temperature even though the extent of protein association also increased. Light scattering suggested that protein association proeeeded with the primary formation of submicellar aggregates containing 20–30 monomers which then associated further to form particles of minimum micelle size (12–15 submicelles), and eventually larger. The temperature of precipitation of the 5-P form in the presence of CaCl2 was lower than the conformational transition and suggested that both hydrophobic interactions and Ca bridges between phosphate esters on adjacent molecules are important in micelle formation.


RSC Advances ◽  
2016 ◽  
Vol 6 (71) ◽  
pp. 66963-66970 ◽  
Author(s):  
Haiguan Yang ◽  
Junqi Zha ◽  
Peng Zhang ◽  
Yuhao Xiong ◽  
Linjing Su ◽  
...  

CoS, which was prepared using a facile solvothermal method, and characterized using various analytical techniques, was demonstrated for the first time to exhibit intrinsic peroxidase-like activity.


Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1163 ◽  
Author(s):  
Walid Hikal ◽  
Brandon Weeks

Non-isothermal sublimation kinetics of low-volatile materials is more favorable over isothermal data when time is a crucial factor to be considered, especially in the subject of detecting explosives. In this article, we report on the in-situ measurements of the sublimation activation energy for 2,4,6-trinitrotoluene (TNT) continuous nanofilms in air using rising-temperature UV-Vis absorbance spectroscopy at different heating rates. The TNT films were prepared by the spin coating deposition technique. For the first time, the most widely used procedure to determine sublimation rates using thermogravimetry analysis (TGA) and differential scanning calorimetry (DSC) was followed in this work using UV-Vis absorbance spectroscopy. The sublimation kinetics were analyzed using three well-established calculating techniques. The non-isothermal based activation energy values using the Ozawa, Flynn–Wall, and Kissinger models were 105.9 ± 1.4 kJ mol−1, 102.1 ± 2.7 kJ mol−1, and 105.8 ± 1.6 kJ mol−1, respectively. The calculated activation energy agreed well with our previously reported isothermally-measured value for TNT nanofilms using UV-Vis absorbance spectroscopy. The results show that the well-established non-isothermal analytical techniques can be successfully applied at a nanoscale to determine sublimation kinetics using absorbance spectroscopy.


Fluids ◽  
2019 ◽  
Vol 4 (1) ◽  
pp. 17 ◽  
Author(s):  
Prodromos Arsenidis ◽  
Kostas Karatasos

Fully atomistic molecular dynamics simulations are employed to study in detail the interactions between a complex comprised by a PEGylated hyperbranched polyester (HBP) and doxorubicin molecules, with a model dipalmitoylphosphatidylglycerol membrane in an aqueous environment. The effects of the presence of the lipid membrane in the drug molecules’ spatial arrangement were examined in detail and the nature of their interaction with the latter were discussed and quantified where possible. It was found that a partial migration of the drug molecules towards the membrane’s surface takes place, driven either by hydrogen-bonding (for the protonated drugs) or by hydrophobic interactions (for the neutral drug molecules). The clustering behavior of the drug molecules appeared to be enhanced in the presence of the membrane, while the development of a charge excess close to the surface of the hyperbranched polymer and of the lipid membrane was observed. The uneven charge distribution created an effective overcharging of the HBP/drug complex and the membrane/drug surface. The translational motion of the drug molecules was found to be strongly affected by the presence of the membrane. The extent of the observed changes depended on the charge of the drug molecule. The build-up of the observed charge excesses close to the surface of the polymeric host and the membrane, together with the changes in the diffusional behavior of the drug molecules are of particular interest. Both phenomena could be important at the latest stages of the liposomal disruption and the release of the drug cargo in formulations based on relevant liposomal carriers.


2020 ◽  
Vol 10 (17) ◽  
pp. 5737
Author(s):  
Vasilis Kostas ◽  
Maria Baikousi ◽  
Nektaria-Marianthi Barkoula ◽  
Aris Giannakas ◽  
Antonios Kouloumpis ◽  
...  

Carbon into polymer nanocomposite is so far a common additive for the enhancement of the polymer properties. The properties of the polymer, such as thermal, and especially its mechanical properties, are improved by the homogeneously dispersed carbon nanoparticles on the polymer matrix. In this study, carbon wires in nano dimensions are, for the very first time, synthesized via the hard templating method from the silicate matrix MCM-41, and used as nano additives of polystyrene. The carbon nanowires were chemically oxidized, and further modified by attaching octadecylamine molecules, for the development of organic functionalities onto carbon nanowires surface. The nanocomposite materials of polystyrene with the modified carbon nanowires were prepared by a solution-precipitation method at three nano additive to polymer loadings (1, 3 and 5 wt%). The as-derived nanocomposites were studied with a combination of characterization and analytical techniques. The results showed that the thermal and mechanical properties of the polystyrene nanocomposites gradually improved while increasing nano-additive loading until 3 wt%. More specifically, the 3 wt% loading sample showed the best mechanical properties, while the 5 wt% sample was difficult to achieve satisfactory dispersion of carbon nanowires and consequently has a wide range of values.


2019 ◽  
Vol 151 (3) ◽  
pp. 342-356 ◽  
Author(s):  
Ruchi Kapoor ◽  
Thasin A. Peyear ◽  
Roger E. Koeppe ◽  
Olaf S. Andersen

The two major classes of antidepressants, tricyclic antidepressants (TCAs) and selective serotonin reuptake inhibitors (SSRIs), inhibit neurotransmitter reuptake at synapses. They also have off-target effects on proteins other than neurotransmitter transporters, which may contribute to both desired changes in brain function and the development of side effects. Many proteins modulated by antidepressants are bilayer spanning and coupled to the bilayer through hydrophobic interactions such that the conformational changes underlying their function will perturb the surrounding lipid bilayer, with an energetic cost (ΔGdef) that varies with changes in bilayer properties. Here, we test whether changes in ΔGdef caused by amphiphilic antidepressants partitioning into the bilayer are sufficient to alter membrane protein function. Using gramicidin A (gA) channels to probe whether TCAs and SSRIs alter the bilayer contribution to the free energy difference for the gramicidin monomer⇔dimer equilibrium (representing a well-defined conformational transition), we find that antidepressants alter gA channel activity with varying potency and no stereospecificity but with different effects on bilayer elasticity and intrinsic curvature. Measuring the antidepressant partition coefficients using isothermal titration calorimetry (ITC) or cLogP shows that the bilayer-modifying potency is predicted quite well by the ITC-determined partition coefficients, and channel activity is doubled at an antidepressant/lipid mole ratio of 0.02–0.07. These results suggest a mechanism by which antidepressants could alter the function of diverse membrane proteins by partitioning into cell membranes and thereby altering the bilayer contribution to the energetics of membrane protein conformational changes.


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