Title

Design, synthesis and analysis of charged RGD derivatives

Authors

Bonaventure Mujyambere¹, Subasri Mohanakrishnan¹, Shoufia Jabeen Mubarak², Hemamalini Vedagiri², Sivasamy Ramasamy³ & Suja Samiappan¹*

Affiliation

¹Department of Biochemistry & ²Department of Bioinformatics & ³Department of Human Genetics and Molecular Biology, Bharathiar University, Coimbatore, Tamilnadu, India; *Corresponding author

Email

Bonaventure Mujyambere – E-mail: mubona@gmail.com

Subasri Mohanakrishnan - E-mail: subamohan025@gmail.com

Shoufia Jabeen – E-mail: shoufiamdu@gmail.com

Hemamalini Vedagiri – E-mail: hemamalini@buc.edu.in

Sivasamy Ramasamy – E-mail: rshgmb@buc.edu.in

Suja Samiappan – E-mail: suja.s@buc.edu.in

Article Type

Research Article

Date

Received September 1, 2023; Revised September 30, 2023; Accepted September 30, 2023, Published September 30, 2023

In the present study, negatively charged N-Biotin-RGD and positively charged C-Biotin-RGD were designed, synthesized, and characterized with docking analysis. The fixation of MDA-MB-231 cells with formalin made their cell surface neutrally charged thus removing the electrostatic interactions between charged biotinylated RGD derivatives and MDA-MB-231 cells. The results of the binding affinity of biotinylated RGD derivatives against MDA-MB-231 cells showed that N-Biotin-RGD had higher binding affinity than C-Biotin-RGD. The cytotoxic effect was analyzed by incubating charged biotinylated RGD derivatives with live MDA-MB-231 cells. MDA-MB-231 cell surface is negatively charged due to high hypersialyliation of polyglycans and Warburg effect. The results of their cytotoxic activities against live MDA-MB-231 cells were found to be electrostatic in nature. C-Biotin-RGD had an attractive interaction with the MDA-MB-231 cell surface resulting in a higher cytotoxic effect. In comparison, N-Biotin-RGD had a repulsive interaction with the MDA-MB-231 cell surface resulting in a lower cytotoxic effect. Hence, positively charged C-Biotin-RGD is a better cytotoxic agent than a negatively charged N-Biotin-RGD against MDA-MB-231 cells.

Keywords

Design, synthesis, analysis, charged RGD derivatives

Citation

Mujyambere et al. Bioinformation 19(9): 918-924 (2023)

Edited by

P Kangueane

ISSN

0973-2063

Publisher

Biomedical Informatics

License

This is an Open Access article which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. This is distributed under the terms of the Creative Commons Attribution License.