Journal
NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
Volume 23, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.nano.2019.102087
Keywords
Mitochondria; Delocalized lipophilic cations; Fluorescence imaging; Human serum albumin
Funding
- Office of Science (BER), U.S. Department of Energy [DE-SC0008397]
- National Natural Science Foundation of China [81571812]
- Jiangsu Higher Education Institutions [1107047002]
- Jiangsu provincial government [KYCX17_0135]
- Graduated School of Southeast University [YBJJ1787]
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Small molecule 5BMF is a novel mitochondria-targeted delocalized lipophilic cation (DLC) with good anti-tumor activity and fluorescence emission suitable for bioimaging. In this study, human serum albumin (HSA) complexed with 5BMF (5BMF@HSA) has been developed to further improve its solubility (from 1.61 to 5.41 mg/mL), and the fluorescent intensity of 5BMF@HSA was improved over 2 times. Nearly 10-fold 5BMF was released from 5BMF@HSA complex in acidic condition when compared with neutral/basic environment. Intracellular distribution of 5BMF was altered by HSA as its signals were observed in lysosomes where free 5BMF barely localized. Both 5BMF@HSA and 5BMF showed selective toxicity toward tumor cells in mu M and nM range and effectively inhibited tumor growth in mice model. In summary, 5BMF@HSA shows improved solubility in aqueous buffer and enhanced fluorescence emission, and maintains tumor inhibition capability. It is a promising protein complex for tumor cell imaging and tumor treatment. (c) 2019 Elsevier Inc. All rights reserved.
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