Early Stage In Vitro Bioprofiling of Potential Low-Molecular-Weight Organoboron Compounds for Boron Neutron Capture Therapy (BNCT)—Proposal for a Guide
Zbigniew J. Leśnikowski,
Filip Ekholm,
Narayan S. Hosmane,
Martin Kellert,
Eiji Matsuura,
Hiroyuki Nakamura,
Agnieszka B. Olejniczak,
Luigi Panza,
Louis M. Rendina,
Wolfgang A. G. Sauerwein
Affiliations
Zbigniew J. Leśnikowski
Laboratory of Medicinal Chemistry, Institute of Medical Biology PAS, Lodowa 106, 93-232 Lodz, Poland
Filip Ekholm
Department of Chemistry, University of Helsinki, P.O. Box 55, FI-00014 Helsinki, Finland
Narayan S. Hosmane
Department of Chemistry and Biochemistry, Northern Illinois University, DeKalb, IL 60115, USA
Martin Kellert
Deutsche Gesellschaft für Bor-Neutroneneinfangtherapie DGBNCT e.V., University Hospital Essen, 45122 Essen, Germany
Eiji Matsuura
Graduate School of Interdisciplinary Science and Engineering in Health Systems, Okayama University, Okayama 700-0005, Japan
Hiroyuki Nakamura
Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, Yokohama 226-8501, Japan
Agnieszka B. Olejniczak
Screening Laboratory, Institute of Medical Biology PAS, 106 Lodowa, 93-232 Lodz, Poland
Luigi Panza
Deutsche Gesellschaft für Bor-Neutroneneinfangtherapie DGBNCT e.V., University Hospital Essen, 45122 Essen, Germany
Louis M. Rendina
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia
Wolfgang A. G. Sauerwein
Deutsche Gesellschaft für Bor-Neutroneneinfangtherapie DGBNCT e.V., University Hospital Essen, 45122 Essen, Germany
Given the renewed interest in boron neutron capture therapy (BNCT) and the intensified search for improved boron carriers, as well as the difficulties of coherently comparing the carriers described so far, it seems necessary to define a basic set of assays and standardized methods to be used in the early stages of boron carrier development in vitro. The selection of assays and corresponding methods is based on the practical experience of the authors and is certainly not exhaustive, but open to discussion. The proposed tests/characteristics: Solubility, lipophilicity, stability, cytotoxicity, and cellular uptake apply to both low molecular weight (up to 500 Da) and high molecular weight (5000 Da and more) boron carriers. However, the specific methods have been selected primarily for low molecular weight boron carriers; in the case of high molecular weight compounds, some of the methods may need to be adapted.
