A Dual-Function Indole-Benzimidazole Hybrid: Lipid Droplet Imaging and Anticancer Potential


Acikgoz E., Cakir M., Kuzu B., Tan Uygun M.

ACS OMEGA, 2026 (SCI-Expanded, Scopus) identifier

  • Publication Type: Article / Article
  • Publication Date: 2026
  • Doi Number: 10.1021/acsomega.5c12137
  • Journal Name: ACS OMEGA
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core, Directory of Open Access Journals
  • Van Yüzüncü Yıl University Affiliated: Yes

Abstract

A novel indole-fused benzimidazole fluorescent probe, I-BZ, was designed, synthesized, and characterized for selective imaging of intracellular lipid droplets (LDs) in human breast cancer cells (MDA-MB-231). The probe was prepared via condensation of 3-methyl-1H-indole-2-carbaldehyde with 4-methylbenzene-1,2-diamine and confirmed by 1H/13C NMR and LC-MS/MS. Photophysical studies indicated that I-BZ exhibits ESIPT-based fluorescence, enabling sensitive detection of lipid-rich compartments. Cytotoxicity assays showed that low concentrations (0.5 μM) were biocompatible for live-cell imaging, whereas higher doses exhibited anticancer activity, with IC50 values of 35 μM at 24 h and 15 μM at 48 h. Fluorescence microscopy in fixed and live cells demonstrated selective accumulation of I-BZ in LDs, validated by ethanol disruption and colocalization with Nile Red. Nuclear costaining with DAPI provided spatial context for precise visualization of cytoplasmic LDs. I-BZ shows great potential as a fluorescent probe for lipid droplet imaging, offering a robust tool for investigating lipid-associated processes in cancer biology.