scholarly journals A Comprehensive Analysis of the Thrombin Binding Aptamer Containing Functionalized Pyrrolo-2’-deoxycytidines

2021 ◽  
Vol 14 (12) ◽  
pp. 1326
Author(s):  
Weronika Kotkowiak ◽  
Zofia Jahnz-Wechmann ◽  
Anna Pasternak
Keyword(s):  
Targeted Therapy ◽  
Spatial Arrangement ◽  
Biological Properties ◽  
Comprehensive Analysis ◽  
Hela Cell Line ◽  
Chemical Modifications ◽  
Quadruplex Structure ◽  
G Quadruplex ◽  
Physicochemical And Biological Properties ◽  
Therapy Development

Aptamers constitute an answer for the growing need for targeted therapy development. One of the most well-known representatives of this group of compounds is thrombin binding aptamers (TBA) targeted towards thrombin. The TBA inhibitory activity is determined by its spatial arrangement, which consists of two G-tetrads linked by two shorter TT loops and one longer TGT loop and folds into a unimolecular, antiparallel G-quadruplex structure. Interesting properties of the aptamer can be further improved via the introduction of a number of chemical modifications. Herein, a comprehensive analysis of the influence of pyrrolo-2’-deoxycytidine (Py-dC) and its derivatives on TBA physicochemical and biological properties has been presented. The studies have shown that the presence of modified residues at the T7 position of the TGT loop has only minor effects on TBA thermodynamic stability without affecting its folding topology. All analyzed oligomers exhibit anticoagulant properties, but only aptamer modified with a decyl derivative of Py-dC was able to inhibit thrombin activity more efficiently than unmodified, parental compounds. Importantly, the same compound also possessed the potential to effectively restrain HeLa cell line growth.

scholarly journals Antiviral Activity of Carrageenans and Processing Implications

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 437
Author(s):  
Milena Álvarez-Viñas ◽  
Sandra Souto ◽  
Noelia Flórez-Fernández ◽  
Maria Dolores Torres ◽  
Isabel Bandín ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antiviral Activity ◽  
Drug Delivery Systems ◽  
Biological Properties ◽  
Red Seaweed ◽  
Processing Conditions ◽  
Chemical Modifications ◽  
Viral Attachment ◽  
Extraction Stage ◽  
Composition Structure

Carrageenan and carrageenan oligosaccharides are red seaweed sulfated carbohydrates with well-known antiviral properties, mainly through the blocking of the viral attachment stage. They also exhibit other interesting biological properties and can be used to prepare different drug delivery systems for controlled administration. The most active forms are λ-, ι-, and κ-carrageenans, the degree and sulfation position being determined in their properties. They can be obtained from sustainable worldwide available resources and the influence of manufacturing on composition, structure, and antiviral properties should be considered. This review presents a survey of the antiviral properties of carrageenan in relation to the processing conditions, particularly those assisted by intensification technologies during the extraction stage, and discusses the possibility of further chemical modifications.

scholarly journals The Influence of Bloom Index, Endotoxin Levels and Polyethylene Glycol Succinimidyl Glutarate Crosslinking on the Physicochemical and Biological Properties of Gelatin Biomaterials

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1003
Author(s):  
Zhuning Wu ◽  
Stefanie H. Korntner ◽  
Jos Olijve ◽  
Anne Maria Mullen ◽  
Dimitios I. Zeugolis
Keyword(s):  
Elastic Modulus ◽  
Polyethylene Glycol ◽  
Enzymatic Degradation ◽  
Structural Integrity ◽  
Biological Response ◽  
Biological Properties ◽  
Compression Stress ◽  
Free Amine ◽  
Amine Content ◽  
Physicochemical And Biological Properties

In the medical device sector, bloom index and residual endotoxins should be controlled, as they are crucial regulators of the device’s physicochemical and biological properties. It is also imperative to identify a suitable crosslinking method to increase mechanical integrity, without jeopardising cellular functions of gelatin-based devices. Herein, gelatin preparations with variable bloom index and endotoxin levels were used to fabricate non-crosslinked and polyethylene glycol succinimidyl glutarate crosslinked gelatin scaffolds, the physicochemical and biological properties of which were subsequently assessed. Gelatin preparations with low bloom index resulted in hydrogels with significantly (p < 0.05) lower compression stress, elastic modulus and resistance to enzymatic degradation, and significantly higher (p < 0.05) free amine content than gelatin preparations with high bloom index. Gelatin preparations with high endotoxin levels resulted in films that induced significantly (p < 0.05) higher macrophage clusters than gelatin preparations with low endotoxin level. Our data suggest that the bloom index modulates the physicochemical properties, and the endotoxin content regulates the biological response of gelatin biomaterials. Although polyethylene glycol succinimidyl glutarate crosslinking significantly (p < 0.05) increased compression stress, elastic modulus and resistance to enzymatic degradation, and significantly (p < 0.05) decreased free amine content, at the concentration used, it did not provide sufficient structural integrity to support cell culture. Therefore, the quest for the optimal gelatin crosslinker continues.

scholarly journals Applications of Radiolabelled Curcumin and Its Derivatives in Medicinal Chemistry

2021 ◽  
Vol 22 (14) ◽  
pp. 7410
Author(s):  
Matteo Mari ◽  
Debora Carrozza ◽  
Erika Ferrari ◽  
Mattia Asti
Keyword(s):  
Nuclear Medicine ◽  
Early Diagnosis ◽  
Clinical Application ◽  
Medicinal Chemistry ◽  
Biological Properties ◽  
Present Review ◽  
Chemical Modifications ◽  
Technetium 99M ◽  
Curcumin Derivatives ◽  
Gallium 68

Curcumin is a natural occurring molecule that has aroused much interest among researchers over the years due to its pleiotropic set of biological properties. In the nuclear medicine field, radiolabelled curcumin and curcumin derivatives have been studied as potential radiotracers for the early diagnosis of Alzheimer’s disease and cancer. In the present review, the synthetic pathways, labelling methods and the preclinical investigations involving these radioactive compounds are treated. The studies entailed chemical modifications for enhancing curcumin stability, as well as its functionalisation for the labelling with several radiohalogens or metal radionuclides (fluorine-18, technetium-99m, gallium-68, etc.). Although some drawbacks have yet to be addressed, and none of the radiolabelled curcuminoids have so far achieved clinical application, the studies performed hitherto provide useful insights and lay the foundation for further developments.

scholarly journals Identification of targeted therapy options for gastric adenocarcinoma by comprehensive analysis of genomic data

2020 ◽  
Vol 23 (4) ◽  
pp. 627-638
Author(s):  
Daniel A. Hescheler ◽  
Patrick S. Plum ◽  
Thomas Zander ◽  
Alexander Quaas ◽  
Michael Korenkov ◽  
...  
Keyword(s):  
Targeted Therapy ◽  
Gastric Adenocarcinoma ◽  
Genomic Data ◽  
Comprehensive Analysis ◽  
Therapy Options

The depolymerization of chitosan: effects on physicochemical and biological properties

2004 ◽  
Vol 281 (1-2) ◽  
pp. 45-54 ◽  
Author(s):  
Shirui Mao ◽  
Xintao Shuai ◽  
Florian Unger ◽  
Michael Simon ◽  
Dianzhou Bi ◽  
...  
Keyword(s):  
Biological Properties ◽  
Physicochemical And Biological Properties
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