scholarly journals In-Vitro Hemocompatibility of Polyaniline Functionalized by Bioactive Molecules

Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1861 ◽  
Author(s):  
Skopalová ◽  
Capáková ◽  
Bober ◽  
Pelková ◽  
Stejskal ◽  
...  

Hemocompatibility is an essential prerequisite for the application of materials in the field of biomedicine and biosensing. In addition, mixed ionic and electronic conductivity of conducting polymers is an advantageous property for these applications. Heparin-like materials containing sulfate, sulfamic, and carboxylic groups may have an anticoagulation effect. Therefore, sodium dodecylbenzenesulfonate, 2-aminoethane-1-sulfonic acid and N-(2-acetamido)-2-aminoethanesulfonic acid were used for modification of the representative of conducting polymers, polyaniline, and the resulting products were studied in the context of interactions with human blood. The anticoagulation activity was then correlated to surface energy and conductivity of the materials. Results show that anticoagulation activity is highly affected by the presence of suitable functional groups originating from the used heparin-like substances, and by the properties of polyaniline polymer itself.

1974 ◽  
Vol 32 (02/03) ◽  
pp. 266-276
Author(s):  
Carl D. Jacobsen ◽  
John C. Hoak ◽  
Kenneth K. WU ◽  
Glenna L. Fry
Keyword(s):  

SummaryIn serum from patients with DIC at least 3 different FR-antigenic components could be found. It was difficult to demonstrate these components in the corresponding plasma samples. It is possible that a portion of these antigens formed as a result of in vitro clotting despite the presence of proteolytic inhibitors. These results suggest that the interpretation of “increased split products in serum” may be more complex than current concepts indicate.


1973 ◽  
Vol 30 (03) ◽  
pp. 494-498 ◽  
Author(s):  
G de Gaetano ◽  
J Vermylen

SummaryThrombelastograms of both native blood and re-calcified platelet-rich plasma samples taken from subjects given a single oral dose of aspirin (1 gram) were not significantly different from the pretreatment recordings. Aspirin also did not modify the thrombelastogram when preincubated in vitro with platelet-rich plasma at concentrations inhibiting the platelet “release reaction” by collagen. Thrombelastography therefore cannot evaluate the effect of aspirin on platelet function.


1973 ◽  
Vol 29 (03) ◽  
pp. 694-700 ◽  
Author(s):  
Paul L. Rifkin ◽  
Marjorie B. Zucker

SummaryDipyridamole (Persantin) is reported to prolong platelet survival and inhibit embolism in patients with prosthetic heart valves, but its mechanism of action is unknown. Fifty jxM dipyridamole failed to reduce the high percentage of platelets retained when heparinized human blood was passed through a glass bead column, but prolonged the inhibition of retention caused by disturbing blood in vitro. Possibly the prostheses act like disturbance. Although RA 233 was as effective as dipyridamole in inhibiting the return of retention, it was less effective in preventing the uptake of adenosine into erythrocytes, and more active in inhibiting ADP-induced aggregation and release. Thus there is no simple relation between these drug effects.


2019 ◽  
Vol 15 (2) ◽  
pp. 257-267 ◽  
Author(s):  
Paritosh Shukla ◽  
Ashok Sharma ◽  
Leena Fageria ◽  
Rajdeep Chowdhury

Background: Cancer being a deadly disease, many reports of new chemical entities are available. Pyranopyrazole (PPZ) compounds have also been disclosed as bioactive molecules but mainly as antimicrobial agents. Based on one previous report and our interest in anticancer drug design, we decided to explore PPZs as anticancer agents. To the best of our knowledge, we found that a comprehensive study, involving synthesis, in-vitro biological activity determination, exploration of the mechanism of inhibition and finally in-silico docking studies, was missing in earlier reports. This is what the present study intends to accomplish. Methods: Ten spiro and eleven non-spiro PPZ molecules were synthesized by environment-friendly multicomponent reaction (MCR) strategy. After subjecting each of the newly synthesized molecules to Hep3b hepatocellular carcinoma cell lines assay, we selectively measured the Optical Density (OD) of the most active ones. Then, the compound exhibiting the best activity was docked against human CHK- 1 protein to get an insight into the binding affinities and a quick structure activity relationship (SAR) of the PPZs. Results: The two series of spiro and non-spiro PPZs were easily synthesized in high yields using microwave assisted synthesis and other methods. Among the synthesized compounds, most compounds showed moderate to good anticancer activity against the MTT assay. After performing the absorbance studies we found that the non-spiro molecules showed better apoptosis results and appeared to bind to DNA causing disruption in their structures. Finally, the docking results of compound 5h (having N,Ndimethylamino substituted moiety) clearly showed good binding affinities as predicted by our experimental findings. Conclusion: The paper describes a comprehensive synthesis, in-vitro and docking studies done on new PPZs. The newly synthesized series of spiro and non-spiro PPZs were found to possess antineoplasmic activity as evinced by the studies on hep3b cells. Also, the UV visible absorbance study gave clues to the possible binding of these molecules to the DNA. Docking studies corroborated well with the experimental results. Thus, these new molecules appear to be potential anticancer agents, but further studies are required to substantiate and elaborate on these findings.


1963 ◽  
Vol 18 (5) ◽  
pp. 955-958 ◽  
Author(s):  
S. H. Blondheim ◽  
Gabriel Neumann ◽  
Edna Kott ◽  
Zena Ben-Ishai

The ability of human blood to acetylate p-aminobenzoic acid, determined in vitro, varied directly with the ambient temperature to which the subject was exposed before the blood was drawn. This was demonstrated by 135 determinations of the acetylating ability of the blood of 49 subjects performed over a period of 3 years, and also in acute experiments in which subjects were exposed to 6 and 37 C for up to 2 hr. Variations in the acetylating ability of blood may reflect the activity of metabolic mechanisms involved in thermal homeostasis. aromatic amines; p-aminobenzoic acid; cold; heat acclimatization; (blood) enzymes; weather; environment Submitted on September 11, 1962


2020 ◽  
pp. 128951
Author(s):  
Nadezhda Frolova ◽  
Alena Soboleva ◽  
Viet Duc Nguyen ◽  
Ahyoung Kim ◽  
Christian Ihling ◽  
...  
Keyword(s):  

Materials ◽  
2021 ◽  
Vol 14 (12) ◽  
pp. 3337
Author(s):  
Sara Hooshmand ◽  
Sahar Mollazadeh ◽  
Negar Akrami ◽  
Mehrnoosh Ghanad ◽  
Ahmed El-Fiqi ◽  
...  

Exploring new therapies for managing skin wounds is under progress and, in this regard, mesoporous silica nanoparticles (MSNs) and mesoporous bioactive glasses (MBGs) offer great opportunities in treating acute, chronic, and malignant wounds. In general, therapeutic effectiveness of both MSNs and MBGs in different formulations (fine powder, fibers, composites etc.) has been proved over all the four stages of normal wound healing including hemostasis, inflammation, proliferation, and remodeling. The main merits of these porous substances can be summarized as their excellent biocompatibility and the ability of loading and delivering a wide range of both hydrophobic and hydrophilic bioactive molecules and chemicals. In addition, doping with inorganic elements (e.g., Cu, Ga, and Ta) into MSNs and MBGs structure is a feasible and practical approach to prepare customized materials for improved skin regeneration. Nowadays, MSNs and MBGs could be utilized in the concept of targeted therapy of skin malignancies (e.g., melanoma) by grafting of specific ligands. Since potential effects of various parameters including the chemical composition, particle size/morphology, textural properties, and surface chemistry should be comprehensively determined via cellular in vitro and in vivo assays, it seems still too early to draw a conclusion on ultimate efficacy of MSNs and MBGs in skin regeneration. In this regard, there are some concerns over the final fate of MSNs and MBGs in the wound site plus optimal dosages for achieving the best outcomes that deserve careful investigation in the future.


Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 28
Author(s):  
Katie Shiels ◽  
Alexandros Tsoupras ◽  
Ronan Lordan ◽  
Constantina Nasopoulou ◽  
Ioannis Zabetakis ◽  
...  

Microalgae are at the start of the food chain, and many are known producers of a significant amount of lipids with essential fatty acids. However, the bioactivity of microalgal lipids for anti-inflammatory and antithrombotic activities have rarely been investigated. Therefore, for a sustainable source of the above bioactive lipids, the present study was undertaken. The total lipids of microalga Chlorococcum sp., isolated from the Irish coast, were fractionated into neutral-, glyco-, and phospho-lipids, and were tested in vitro for their anti-inflammatory and antithrombotic activities. All tested lipid fractions showed strong anti-platelet-activating factor (PAF) and antithrombin activities in human platelets (half maximal inhibitory concentration (IC50) values ranging ~25–200 μg of lipid) with the highest activities in glyco- and phospho-lipid fractions. The structural analysis of the bioactive lipid fraction-2 revealed the presence of specific sulfoquinovosyl diacylglycerols (SQDG) bioactive molecules and the HexCer-t36:2 (t18:1/18:1 and 18:2/18:0) cerebrosides with a phytosphingosine (4-hydrosphinganine) base, while fraction-3 contained bioactive phosphatidylcholine (PC) and phosphatidylethanolamine (PE) molecules. These novel bioactive lipids of Chlorococcum sp. with putative health benefits may indicate that marine microalgae can be a sustainable alternative source for bioactive lipids production for food supplements and nutraceutical applications. However, further studies are required towards the commercial technology pathways development and biosafety analysis for the use of the microalga.


e-Polymers ◽  
2009 ◽  
Vol 9 (1) ◽  
Author(s):  
Chiara Gualandi ◽  
Piotr Wilczek ◽  
Maria Letizia Focarete ◽  
Gianandrea Pasquinelli ◽  
Michal Kawalec ◽  
...  

AbstractElectrospinning technology is used to fabricate sub-micrometric fiber mats made of a random equimolar poly(lactide-co-glycolide) copolymer (PLGA), whose in vitro hydrolytic degradation kinetics is investigated over a period of 49 days in phosphate buffer at 37 °C. The PLGA mats show a decrease of molecular weight (by GPC) from the very beginning of the experiment, whereas a macroscopic weight loss from the samples is appreciated (by gravimetry) only after 20 days of buffer exposure. The molar mass distribution curves remain monomodal during the degradation experiment suggesting that no acid auto-catalyzed hydrolysis, commonly observed in bulk specimens, occurs in sub-micrometric PLGA fibers. PLGA scaffolds containing Endothelial Growth Factor Supplement (ECGS) were also fabricated by electrospinning, from ECGS-containing polymer solutions. Mesenchymal cells derived from human bone marrow mononuclear cells were cultured in the presence of such ECGS-loaded PLGA scaffolds. Flow cytometry and Differential Interference Contrast microscopy were used to characterize the cell cultures over a 7 day period. The results of AnexinV/PI staining and of intranuclear Ki-67 protein expression show, together with concomitant cell morphology modifications, that growth factors released from the scaffolds support the survival, proliferation and growth of the mesenchymal cells. This result demonstrates that ECGS maintains its bioactivity upon release from the electrospun fibers and shows the versatility of the electrospinning technique.


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