Targeted theranostics: Near-infrared triterpenoic acid-rhodamine conjugates as prerequisites for precise cancer diagnosis and therapy

Eur J Med Chem. 2023 Nov 5:259:115663. doi: 10.1016/j.ejmech.2023.115663.

Niels Heise ¹, Florian Lehmann ², René Csuk ³, Thomas Mueller ⁴

Affiliations

1 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany.
2 Martin-Luther-University Halle-Wittenberg, Physical Chemistry, von-Dankelmann-Platz 4, D-06120, Halle (Saale), Germany.
3 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany. Electronic address: [email protected].
4 Martin-Luther-University Halle-Wittenberg, Medical Faculty, University Clinic for Internal Medicine IV, Hematology/Oncology, Ernst-Grube-Str. 40, D-06120, Halle (Saale), Germany.

PMID: 37480713 DOI: 10.1016/j.ejmech.2023.115663

Abstract

Pentacyclic triterpenoic acids have shown excellent potential as starting Materials for the synthesis of highly cytotoxic agents with significantly reduced toxicity for non-malignant cells. This study focuses on the development of triterpenoic acid-rhodamine conjugates with fluorescence shifted to the near-infrared (NIR) region for theranostic applications in Cancer research. Spectral analysis revealed emission wavelengths around λ = 760 nm, enabling stronger signals and deeper tissue penetration. The conjugates were evaluated using SRB assays on tumor cell lines and non-malignant fibroblasts, demonstrating low nanomolar activity and high selectivity, similarly to their known rhodamine B counterparts. Additional staining experiments proved their mode of action as mitocans.

Keywords

Asiatic acid; Changsha dye; Cytotoxicity; NIR-Fluorescence; Theranostics.

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