1. Academic Validation
  2. A dual-functional mitochondrial probe for melanoma visualization and PI3K/AKT/mTOR-EMT signaling axis-mediated antitumor therapy

A dual-functional mitochondrial probe for melanoma visualization and PI3K/AKT/mTOR-EMT signaling axis-mediated antitumor therapy

  • Colloids Surf B Biointerfaces. 2025 Jun 3:254:114847. doi: 10.1016/j.colsurfb.2025.114847.
Tong Xia 1 Hongye Liao 1 Ziyuan Zeng 1 Meili Li 1 Simei Yang 2 Xun Yang 1 Yuanmin He 1 Jie Qing 3 Li Liu 1 Xia Xiong 4 Changzhen Sun 5
Affiliations

Affiliations

  • 1 Department of Dermatology, The Affiliated Hospital, Southwest Medical University, Luzhou 646000, China.
  • 2 School of Public Health, Southwest Medical University, Luzhou 646000, China.
  • 3 Drug Research Center of Integrated Traditional Chinese and Western Medicine, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou 646000, China.
  • 4 Department of Dermatology, The Affiliated Hospital, Southwest Medical University, Luzhou 646000, China. Electronic address: xiongxia789@126.com.
  • 5 Drug Research Center of Integrated Traditional Chinese and Western Medicine, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou 646000, China; Luzhou Key Laboratory of research and development of medical institution preparations and large-scale health products, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou 646000, China. Electronic address: sunchangzhen@swmu.edu.cn.
Abstract

Melanoma is a highly metastatic Cancer with poor treatment outcomes. Mitochondria, regulated by various signaling pathways, are an important target in Cancer therapy. Near-infrared (NIR) fluorescence probes have gained interest due to their properties such as deep tissue penetration, high image sensitivity, and precision targeting. In this study, we developed a novel NIR fluorescent probe IR-545 for melanoma imaging, which demonstrated mitochondrial targeting and antitumor activity in melanoma cells. In vitro experiments showed that IR-545 was taken up by melanoma cells through organic anion-transport polypeptides and targeted tumor cell mitochondria. IR-545 induced Apoptosis by inhibiting the PI3K/Akt/mTOR pathway and epithelial-mesenchymal transition (EMT) and suppressed the proliferation and metastasis of melanoma cells. In vivo, IR-545 significantly inhibited tumor growth in BALB/c nude mice. Immunofluorescence, immunohistochemistry, and H&E staining confirmed that IR-545 induced tumor cell Apoptosis and inhibited proliferation without notable side effects. In conclusion, IR-545 shows significant potential in imaging and treating melanoma, offering a promising new therapeutic approach.

Keywords

Anti-cancer; Apoptosis; Melanoma; Mitochondrial-targeted; Near-infrared fluorescent probe.

Figures
Products