scholarly journals Structure–Activity Relationship of Graphene-Based Materials: Impact of the Surface Chemistry, Surface Specific Area and Lateral Size on Their In Vitro Toxicity

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2963
Author(s):  
Salma Achawi ◽  
Bruno Feneon ◽  
Jérémie Pourchez ◽  
Valérie Forest

Predictive toxicity and structure–activity relationships (SARs) are raising interest since the number of nanomaterials has become unmanageable to assess their toxicity with a classical case-by-case approach. Graphene-based materials (GBMs) are among the most promising nanomaterials of this decade and their application might lead to several innovations. However, their toxicity impact needs to be thoroughly assessed. In this regard, we conducted a study on 22 GBMs to investigate their potential SARs by performing a complete physicochemical characterization and in vitro toxicity assessment (on RAW264.7 cells). We used GBMs of variable lateral size (0.5–38 µm), specific surface area (SSA, 30–880 m²/g), and surface oxidation (2–17%). We observed that reduced graphene oxides (RGOs) were more reactive than graphene nanoplatelets (GNPs), potentially highlighting the role of GBM’s surface chemistry and surface defects density in their biological impact. We also observed that for GNPs, a smaller lateral size caused higher cytotoxicity. Lastly, GBMs showing a SSA higher than 200 m²/g were found to induce a higher ROS production. Mechanistic explanations are proposed in the discussion. In conclusion, pairing a full physicochemical characterization with a standardized toxicity assessment of a large set of samples allowed us to clarify SARs and provide an additional step toward safe-by-design GBMs.

Author(s):  
Agnieszka Wróbel ◽  
Danuta Drozdowska

Background: Dihydrofolate reductase (DHFR) has been known for decades as a molecular target for antibacterial, antifungal and anti-malarial treatments. This enzyme is becoming increasingly important in the design of new anticancer drugs, which is confirmed by numerous studies including modelling, synthesis and in vitro biological research. This review aims to present and discuss some remarkable recent advances on the research of new DHFR inhibitors with potential anticancer activity. Methods: The scientific literature of the last decade on the different types of DHFR inhibitors has been searched. The studies on design, synthesis and investigation structure-activity relationship were summarized and divided into several subsections depending on the leading molecule and its structural modification. Various methods of synthesis, potential anticancer activity and possible practical applications as DHFR inhibitors of new chemical compounds were described and discussed. <p> Results: This review presents the current state of knowledge on the modification of known DHFR inhibitors and the structures and searching for over eighty new molecules, designed as potential anticancer drugs. In addition, DHFR inhibitors acting on thymidylate synthase (TS), carbon anhydrase (CA) and even DNA-binding are presented in this paper. <p> Conclusion: Thorough physicochemical characterization and biological investigations it is possible to understand structure-activity relationship of DHFR inhibitors. This will enable even better design and synthesis of active compounds, which would have the expected mechanism of action and the desired activity.


2013 ◽  
Vol 27 (3) ◽  
pp. 1049-1056 ◽  
Author(s):  
Mélanie Pailleux ◽  
Delphine Boudard ◽  
Jérémie Pourchez ◽  
Valérie Forest ◽  
Philippe Grosseau ◽  
...  

2019 ◽  
Vol 31 (4) ◽  
pp. 131-146 ◽  
Author(s):  
Lisa Kobos ◽  
Seyedeh Mahboobeh Teimouri Sendesi ◽  
Andrew J. Whelton ◽  
Brandon E. Boor ◽  
John A. Howarter ◽  
...  

2015 ◽  
Vol 2 ◽  
pp. 27-39 ◽  
Author(s):  
Sudeep Shukla ◽  
Alka Jadaun ◽  
Vikas Arora ◽  
Raj Kumar Sinha ◽  
Neha Biyani ◽  
...  

2010 ◽  
Vol 196 ◽  
pp. S284 ◽  
Author(s):  
L. Garza-Ocañas ◽  
M. Ramirez-Cabrera ◽  
M.T. Zanatta-Calderon ◽  
R. Lujan-Rangel ◽  
D.A. Ferrer ◽  
...  

2016 ◽  
Vol 93 ◽  
pp. 51-57 ◽  
Author(s):  
Isabelle Séverin ◽  
Krystelle Lionti ◽  
Laurence Dahbi ◽  
Catherine Loriot ◽  
Bérangère Toury ◽  
...  

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