Sensitive β-galactosidase-targeting fluorescence probe for visualizing small peritoneal metastatic tumours in vivo

• DOI: 10.1038/ncomms7463
• Publication Date: 2015-03-13T10:03:17Z
• Authors: Daisuke Asanuma; Masayo Sakabe; Mako Kamiya; Kyoko Yamamoto; Jun Hiratake; Mikako Ogawa; Nobuyuki Kosaka; Peter L. Choyke; Tetsuo Nagano; Hisataka Kobayashi; Yasuteru Urano
• Keywords: Molecular probe; Fluorescence-lifetime imaging microscopy

Abstract Fluorescence-guided diagnostics is one of the most promising approaches for facile detection cancer in situ . Here we focus on β-galactosidase, which overexpressed primary ovarian cancers, as a molecular target visualizing peritoneal metastases from cancers. As existing fluorescence probes are unsuitable, have designed membrane-permeable HMRef-βGal, optimized intramolecular spirocyclic function affords >1,400-fold enhancement activation. We confirm that HMRef-βGal sensitively detects intracellular β-galactosidase activity several lines. In vivo , this probe visualizes small <1 mm diameter seven mouse models disseminated human (SHIN3, SKOV3, OVK18, OVCAR3, OVCAR4, OVCAR5 and OVCAR8). Because its high brightness, real-time with naked eye possible. Endoscopic also demonstrated. The results clearly indicate preclinical potential value fluorescence-guided diagnosis