Fabrication of folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles for folate receptor targeting breast cancer cells.

Autor: Kunjiappan S; Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil 626126, Tamilnadu, India. Electronic address: selvaraj.k@kl.ac.in., Panneerselvam T; Department of Pharmaceutical Chemistry, Swamy Vivekanandha College of Pharmacy, Elayampalayam, Namakkal 637205, Tamilnadu, India., Pavadai P; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bengaluru 560054, Karnataka, India., Balakrishnan V; Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil 626126, Tamilnadu, India., Pandian SRK; Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil 626126, Tamilnadu, India., Palanisamy P; School of Mechanical Engineering, Vellore Institute of Technology, Vellore 632014, Tamilnadu, India., Sankaranarayanan M; Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science-Pilani, Pilani Campus, Pilani-333031, Rajasthan, India., Kabilan SJ; Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil 626126, Tamilnadu, India., Sundaram GA; Department of Research Analytics, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Poonamallee High Road, Chennai 600 077, Tamilnadu, India., Tseng WL; Department of Chemistry, National Sun Yat-sen University, No. 70, Lien-hai Road, Gushan District, Kaohsiung city 80424, Taiwan; School of Pharmacy, Kaohsiung Medical University, No. 100, Shiquan 1st Road, Sanmin District, Kaohsiung city 80708, Taiwan., Kumar ASK; Department of Chemistry, National Sun Yat-sen University, No. 70, Lien-hai Road, Gushan District, Kaohsiung city 80424, Taiwan. Electronic address: krishnakumar@mail.nsysu.edu.tw.
Jazyk: angličtina
Zdroj: International journal of biological macromolecules [Int J Biol Macromol] 2024 Oct; Vol. 277 (Pt 3), pp. 134406. Date of Electronic Publication: 2024 Aug 03.
DOI: 10.1016/j.ijbiomac.2024.134406
Abstrakt: In this study 5-((2-((3-methoxy benzylidene)-amino)-phenyl)-diazenyl)-4,6-diphenyl pyrimidine-2(5H)-thione was synthesized. The pharmacological applications of pyrimidine analogs are restricted due to their poor pharmacokinetic properties. As a solution, a microbial exopolysaccharide (curdlan gum) was used to synthesize folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles (FA-Py-CG-PEGamine NPs). The results of physicochemical properties revealed that the fabricated FA-Py-CG-PEGamine NPs were between 100 and 400 nm in size with a majorly spherical shaped, crystalline nature, and the encapsulation efficiency and loading capacity were 79.04 ± 0.79 %, and 8.12 ± 0.39 % respectively. The drug release rate was significantly higher at pH 5.4 (80.14 ± 0.79 %) compared to pH 7.2. The cytotoxic potential of FA-Py-CG-PEGamine NPs against MCF-7 cells potentially reduced the number of cells after 24 h with 42.27 μg × mL -1 as IC 50 value. The higher intracellular accumulation of pyrimidine-2(5H)-thione in MCF-7 cells leads to apoptosis, observed by AO/EBr staining and flow cytometry analysis. The highest pyrimidine-2(5H)-thione internalization in MCF-7 cells may be due to folate conjugated on the surface of curdlan gum nanoparticles. Further, internalized pyrimidine-2(5H)-thione increases the intracellular ROS level, leading to apoptosis and inducing the decalin in mitochondrial membrane potential. These outcomes demonstrated that the FA-Py-CG-PEGamine NPs were specificity-targeting folate receptors on the plasma membranes of MCF-7 Cells.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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