scholarly journals Candidate Polyurethanes Based on Castor Oil (Ricinus communis), with Polycaprolactone Diol and Chitosan Additions, for Use in Biomedical Applications

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 237 ◽  
Author(s):  
Yomaira Uscátegui ◽  
Luis Díaz ◽  
José Gómez-Tejedor ◽  
Ana Vallés-Lluch ◽  
Guillermo Vilariño-Feltrer ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Cell Line ◽  
Castor Oil ◽  
Sessile Drop ◽  
Colorimetric Assay ◽  
Biological Properties ◽  
Wound Dressings ◽  
Cytotoxicity Test ◽  
Wide Range

Polyurethanes are widely used in the development of medical devices due to their biocompatibility, degradability, non-toxicity and chemical versatility. Polyurethanes were obtained from polyols derived from castor oil, and isophorone diisocyanate, with the incorporation of polycaprolactone-diol (15% w/w) and chitosan (3% w/w). The objective of this research was to evaluate the effect of the type of polyol and the incorporation of polycaprolactone-diol and chitosan on the mechanical and biological properties of the polyurethanes to identify the optimal ones for applications such as wound dressings or tissue engineering. Polyurethanes were characterized by stress-strain, contact angle by sessile drop method, thermogravimetric analysis, differential scanning calorimetry, water uptake and in vitro degradation by enzymatic processes. In vitro biological properties were evaluated by a 24 h cytotoxicity test using the colorimetric assay MTT and the LIVE/DEAD kit with cell line L-929 (mouse embryonic fibroblasts). In vitro evaluation of the possible inflammatory effect of polyurethane-based materials was evaluated by means of the expression of anti-inflammatory and proinflammatory cytokines expressed in a cellular model such as THP-1 cells by means of the MILLIPLEX® MAP kit. The modification of polyols derived from castor oil increases the mechanical properties of interest for a wide range of applications. The polyurethanes evaluated did not generate a cytotoxic effect on the evaluated cell line. The assessed polyurethanes are suggested as possible candidate biomaterials for wound dressings due to their improved mechanical properties and biocompatibility.

scholarly journals The influence of chromone based hydrazones on lipid peroxidation and bFGF concentration in the HL-60 cell line.

2013 ◽  
Vol 60 (2) ◽  
Author(s):  
Andrzej Łazarenkow ◽  
Marta Michalska ◽  
Anna Gorąca ◽  
Marek Mirowski ◽  
Jolanta Nawrot-Modranka ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Cell Line ◽  
Significant Influence ◽  
Biological Properties ◽  
Synthetic Analogues ◽  
Wide Range ◽  
Synthetic Derivatives ◽  
Derivatives Of

Natural and synthetic derivatives of benzo-γ-pyrones (i.e. flavones, chromones, and coumarins) and their synthetic analogues possess a wide range of biological properties in vitro and in vivo. In this paper we investigated the influence of two hydrazone compounds of chromones, 3-{[(2-dimethoxytiophosphoryl)-2-methylhydrazono]-methyl}-chromen-4-one (CH-3) and 2-amino-6-chloro-3-[(2-hydroxyethyl)-hydrazonomethyl]-chromen-4-one (A-12), on lipid peroxidation and bFGF concentration in the HL-60 cells. Both of the studied compounds had a significant influence on bFGF and TBARS in ranges -137.20 ~ 380.26% and -81.66 ~ -28.68%, respectively, in comparison with the control (counted as 0%).

Design, Synthesis, In vitro and In silico Evaluation of New Hydrazonebased Antitumor Agents as Potent Akt Inhibitors

2020 ◽  
Vol 17 (11) ◽  
pp. 1380-1392
Author(s):  
Emine Merve Güngör ◽  
Mehlika Dilek Altıntop ◽  
Belgin Sever ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Cell Line ◽  
Anticancer Agents ◽  
In Silico ◽  
Antitumor Agents ◽  
Colorimetric Assay ◽  
Fibroblast Cell ◽  
Lipinski’S Rule ◽  
In Silico Docking ◽  
Embryonic Fibroblast

Background: Akt is overexpressed or activated in a variety of human cancers, including gliomas, lung, breast, ovarian, gastric and pancreatic carcinomas. Akt inhibition leads to the induction of apoptosis and inhibition of tumor growth and therefore extensive efforts have been devoted to the discovery of potent antitumor drugs targeting Akt. Objectives: The objective of this work was to identify potent anticancer agents targeting Akt. Methods: New hydrazone derivatives were synthesized and investigated for their cytotoxic effects on 5RP7 H-ras oncogene transformed rat embryonic fibroblast and L929 mouse embryonic fibroblast cell lines. Besides, the apoptotic effects of the most active compounds on 5RP7 cell line were evaluated using flow cytometry. Their Akt inhibitory effects were also investigated using a colorimetric assay. In silico docking and Absorption, Distribution, Metabolism and Excretion (ADME) studies were also performed using Schrödinger’s Maestro molecular modeling package. Results and Discussion: Compounds 3a, 3d, 3g and 3j were found to be effective on 5RP7 cells (with IC50 values of <0.97, <0.97, 1.13±0.06 and <0.97 μg/mL, respectively) when compared with cisplatin (IC50= 1.87±0.15 μg/mL). It was determined that these four compounds significantly induced apoptosis in 5RP7 cell line. Among them, N'-benzylidene-2-[(4-(4-methoxyphenyl)pyrimidin- 2-yl)thio]acetohydrazide (3g) significantly inhibited Akt (IC50= 0.5±0.08 μg/mL) when compared with GSK690693 (IC50= 0.6±0.05 μg/mL). Docking studies suggested that compound 3g showed good affinity to the active site of Akt (PDB code: 2JDO). According to in silico ADME studies, the compound also complies with Lipinski's rule of five and Jorgensen's rule of three. Conclusion: Compound 3g stands out as a potential orally bioavailable cytotoxic agent and apoptosis inducer targeting Akt.

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

scholarly journals Development of Spanish Broom and Flax Dressings with Glycyrrhetinic Acid-Loaded Films for Wound Healing: Characterization and Evaluation of Biological Properties

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1192
Author(s):  
Angela Abruzzo ◽  
Concettina Cappadone ◽  
Valentina Sallustio ◽  
Giovanna Picone ◽  
Martina Rossi ◽  
...  
Keyword(s):  
Wound Healing ◽  
Drug Loading ◽  
Healing Process ◽  
In Vitro Release ◽  
Sodium Hyaluronate ◽  
Biological Properties ◽  
Glycyrrhetinic Acid ◽  
Wound Dressings ◽  
Biological Studies

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

scholarly journals Brushite cement containing gelatin: evaluation of mechanical strength and in vitro degradation

Cerâmica ◽  
2019 ◽  
Vol 65 (374) ◽  
pp. 261-266 ◽  
Author(s):  
L. P. Silva ◽  
M. D. P. Ribeiro ◽  
E. S. Trichês ◽  
M. Motisuke
Keyword(s):  
Mechanical Properties ◽  
Weight Loss ◽  
Compressive Strength ◽  
Solid Phase ◽  
Setting Time ◽  
Biological Properties ◽  
Solubility In Water ◽  
Ringer’S Solution ◽  
Weight Loss Data

Abstract Calcium phosphate cements (CPCs) are potential materials for repairing bone defects, mainly due to their excellent biocompatibility and osteoconductivity. Nevertheless, their low mechanical properties limit their usage in clinical applications. The gelatin addition may improve the mechanical and biological properties of CPCs, but their solubility in water may increase the porosity of the cement during degradation. Thus, the aim of this work was to investigate the influence of gelatin on the setting time, compressive strength and degradation rate of a brushite cement. CPCs were prepared with the addition of 0, 5, 10 and 20 wt% of gelatin powder in the solid phase of the cement. The results indicated that the setting time increased with gelatin. Furthermore, cement with 20 wt% of gelatin had an initial compressive strength of 14.1±1.8 MPa while cement without gelatin had 4.5±1.2 MPa. The weight loss, morphology and compressive strength were evaluated after degradation in Ringer’s solution. According to the weight loss data, gelatin was eliminated of samples during degradation. It was concluded that the presence of gelatin improved CPCs mechanical properties; however, as degradation in Ringer’s solution evolved, cement compressive strength decreased due to gelatin dissolution and, consequently, an increase in sample porosity.

scholarly journals Cell-Fusing Agent Virus Reduces Arbovirus Dissemination in Aedes aegypti Mosquitoes In Vivo

2019 ◽  
Vol 93 (18) ◽  
Author(s):  
Artem Baidaliuk ◽  
Elliott F. Miot ◽  
Sebastian Lequime ◽  
Isabelle Moltini-Conclois ◽  
Fanny Delaigue ◽  
...  
Keyword(s):  
Aedes Aegypti ◽  
Dengue Virus ◽  
Cell Line ◽  
Content Type ◽  
Cells In Culture ◽  
Mosquito Cells ◽  
Wide Range ◽  
Natural Hosts

ABSTRACT Aedes aegypti mosquitoes are the main vectors of arthropod-borne viruses (arboviruses) of public health significance, such as the flaviviruses dengue virus (DENV) and Zika virus (ZIKV). Mosquitoes are also the natural hosts of a wide range of viruses that are insect specific, raising the question of their influence on arbovirus transmission in nature. Cell-fusing agent virus (CFAV) was the first described insect-specific flavivirus, initially discovered in an A. aegypti cell line and subsequently detected in natural A. aegypti populations. It was recently shown that DENV and the CFAV strain isolated from the A. aegypti cell line have mutually beneficial interactions in mosquito cells in culture. However, whether natural strains of CFAV and DENV interact in live mosquitoes is unknown. Using a wild-type CFAV isolate recently derived from Thai A. aegypti mosquitoes, we found that CFAV negatively interferes with both DENV type 1 and ZIKV in vitro and in vivo. For both arboviruses, prior infection by CFAV reduced the dissemination titer in mosquito head tissues. Our results indicate that the interactions observed between arboviruses and the CFAV strain derived from the cell line might not be a relevant model of the viral interference that we observed in vivo. Overall, our study supports the hypothesis that insect-specific flaviviruses may contribute to reduce the transmission of human-pathogenic flaviviruses. IMPORTANCE The mosquito Aedes aegypti carries several arthropod-borne viruses (arboviruses) that are pathogenic to humans, including dengue and Zika viruses. Interestingly, A. aegypti is also naturally infected with insect-only viruses, such as cell-fusing agent virus. Although interactions between cell-fusing agent virus and dengue virus have been documented in mosquito cells in culture, whether wild strains of cell-fusing agent virus interfere with arbovirus transmission by live mosquitoes was unknown. We used an experimental approach to demonstrate that cell-fusing agent virus infection reduces the propagation of dengue and Zika viruses in A. aegypti mosquitoes. These results support the idea that insect-only viruses in nature can modulate the ability of mosquitoes to carry arboviruses of medical significance and that they could possibly be manipulated to reduce arbovirus transmission.

scholarly journals Fabrication of High-Strength and Porous Hybrid Scaffolds Based on Nano-Hydroxyapatite and Human-Like Collagen for Bone Tissue Regeneration

Polymers ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 61 ◽  
Author(s):  
Yannan Liu ◽  
Juan Gu ◽  
Daidi Fan
Keyword(s):  
Mechanical Properties ◽  
Enzymatic Hydrolysis ◽  
Bone Tissue ◽  
Tissue Regeneration ◽  
Bone Repair ◽  
Three Dimensional ◽  
High Strength ◽  
Biological Properties ◽  
Bone Tissue Regeneration

A novel, three-dimensional, porous, human-like collagen (HLC)/nano-hydroxyapatite (n-HA) scaffold cross-linked by 1,2,7,8-diepoxyoctane (DEO) was successfully fabricated, which showed excellent mechanical and superior biological properties for bone tissue regeneration in this study. The physicochemical characterizations of different n-HA/HLC/DEO (nHD) scaffolds were investigated by determining the morphology, compression stress, elastic modulus, Young’s modulus and enzymatic hydrolysis behavior in vitro. The results demonstrated that nHD-2 and nHD-3 scaffolds showed superior mechanical properties and resistance to enzymatic hydrolysis compared to nHD-1 scaffolds. The cell viability, live cell staining and cell adhesion analysis results demonstrated that nHD-2 scaffolds exhibited low cytotoxicity and excellent cytocompatibility compared with nHD-1 and nHD-3 scaffolds. Furthermore, subcutaneous injections of nHD-2 scaffolds in rabbits produced superior anti-biodegradation effects and histocompatibility compared with injections of nHD-1 and nHD-3 scaffolds after 1, 2 and 4 weeks. In addition, the repair of bone defects in rabbits demonstrated that nHD-2 scaffolds presented an improved ability for guided bone regeneration and reconstruction compared to commercially available bone scaffold composite hydroxyapatite/collagen (HC). Collectively, the results show that nHD-2 scaffolds show promise for application in bone tissue engineering due to their excellent mechanical properties, anti-biodegradation, anti-biodegradation, biocompatibility and bone repair effects.

scholarly journals Pleiotropic Biological Effects of Dietary Phenolic Compounds and their Metabolites on Energy Metabolism, Inflammation and Aging

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 596 ◽  
Author(s):  
María del Carmen Villegas-Aguilar ◽  
Álvaro Fernández-Ochoa ◽  
María de la Luz Cádiz-Gurrea ◽  
Sandra Pimentel-Moral ◽  
Jesús Lozano-Sánchez ◽  
...  
Keyword(s):  
Energy Metabolism ◽  
Phenolic Compounds ◽  
Molecular Mechanisms ◽  
Biological Effects ◽  
Biological Properties ◽  
In Vivo Studies ◽  
Wide Range ◽  
High Prevalence

Dietary phenolic compounds are considered as bioactive compounds that have effects in different chronic disorders related to oxidative stress, inflammation process, or aging. These compounds, coming from a wide range of natural sources, have shown a pleiotropic behavior on key proteins that act as regulators. In this sense, this review aims to compile information on the effect exerted by the phenolic compounds and their metabolites on the main metabolic pathways involved in energy metabolism, inflammatory response, aging and their relationship with the biological properties reported in high prevalence chronic diseases. Numerous in vitro and in vivo studies have demonstrated their pleiotropic molecular mechanisms of action and these findings raise the possibility that phenolic compounds have a wide variety of roles in different targets.

scholarly journals Biocompatibility Evaluation of a New Hydrogel Dressing Based on Polyvinylpyrrolidone/Polyethylene Glycol

2012 ◽  
Vol 2012 ◽  
pp. 1-5 ◽  
Author(s):  
Esmaeil Biazar ◽  
Ziba Roveimiab ◽  
Gholamreza Shahhosseini ◽  
Mohammadreza Khataminezhad ◽  
Mandana Zafari ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Staphylococcus Epidermidis ◽  
Cell Attachment ◽  
Wound Dressings ◽  
Cytotoxicity Test ◽  
Check Sample ◽  
Hydrogel Sample ◽  
Antifungal Effect ◽  
Anti Fungal

The composition of the dressings is based on polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), and agar. The electron beam irradiation technique has been used to prepare hydrogel wound dressings. Thein vitrobiocompatibility of the hydrogel was investigated by check samples (hydrocolloid Comfeel), antibacterial test (Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Escherichia Colik12), anti fungal test (Candida Albicans) and cytotoxicity test (Fibroblast L929). Results have shown cell attachment characteristics and nontoxicity of all samples. Antibacterial testing also showed that the antibacterial effect of the hydrogel sample to the check sample increased to 30%. Also, investigation of antifungal analysis did not show any trace of fungi growth on the surface of the hydrogel, whereas antifungal effect did not observe on the surface of the check sample. Finally, this hydrogel sample showed a goodin vitrobiocompatibility.

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