Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies

Sumit Kumar; Dharmender Kumar; Charu Upadhyay; Meenakshi Bansal; Brijesh Rathi; Priyamvada Singh

doi:10.1016/j.ijbiomac.2024.136660

Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies

Int J Biol Macromol. 2024 Dec;282(Pt 1):136660. doi: 10.1016/j.ijbiomac.2024.136660. Epub 2024 Oct 19.

Authors

Sumit Kumar¹, Dharmender Kumar¹, Charu Upadhyay¹, Meenakshi Bansal², Brijesh Rathi³, Priyamvada Singh⁴

Affiliations

¹ Department of Chemistry, Miranda House, University of Delhi, Delhi, India.
² Laboratory for Translational Chemistry and Drug Discovery, Department of Chemistry, Hansraj College University Enclave, University of Delhi, Delhi, India.
³ Laboratory for Translational Chemistry and Drug Discovery, Department of Chemistry, Hansraj College University Enclave, University of Delhi, Delhi, India. Electronic address: [email protected].
⁴ Department of Chemistry, Miranda House, University of Delhi, Delhi, India. Electronic address: [email protected].

PMID: 39427789
DOI: 10.1016/j.ijbiomac.2024.136660

Abstract

Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the resulting CNC-CXN nano-conjugate. Elemental analysis, powder X-ray, SEM, AFM, Infrared, and solid-state NMR spectroscopic techniques confirmed the composition of novel CNC-CXN nano-conjugate. Next, CNC-CXN nano-conjugate did not exhibit apparent cytotoxic effects on the sensitive Vero E6 cell line up to a concentration of 4.66 μg/μl. The CNC-CXN nano-conjugate was also evaluated for its preliminary efficacy on Plasmodium falciparum (3D7) malaria parasite and showed a 50 % inhibitory concentration value of 0.02 μg/μl. Overall, the selectivity index (SI) of the CNC-CXN nano-conjugate significantly improved to 233, indicating its suitability for further validation studies in animal models.

Keywords: Cellulose nanocrystals; Click chemistry; Functionalization; Nano-conjugate.

MeSH terms

Animals
Antimalarials* / chemical synthesis
Antimalarials* / chemistry
Antimalarials* / pharmacology
Cellulose* / chemistry
Cellulose* / pharmacology
Chlorocebus aethiops
Nanoparticles* / chemistry
Plasmodium falciparum* / drug effects
Vero Cells

Substances

Antimalarials
Cellulose