Abstract

AbstractPhenylboronic acids and their conjugates as well as methods for their preparation and use have been the subject of several US patents. A novel phenylboronic acid derivative, 2-(bromoacetamido) phenylboronic acid (2-BAPBA), which may be useful in treatment of the human or animal diseases, has recently been prepared. Questions that need to be answered include: whether 2-BAPBA has any potential cytogenotoxic effects; and if so, whether they are commensurate with a reasonable risk/benefit ratio for its intended use. In this study, a well-established in vivo assessment bioassay, the Allium cepa test, was used to examine the effect of a dimethyl sulfoxide (DMSO) solution of 2-BAPBA at doses equivalent to 1/4, 1/2, 1 EC50 (half maximal effective concentration) and 2 EC50 (2.23, 4.45, 8.90, or 17.8 mg l–1, respectively) for 24 or 48 h. The EC50 of 2-BAPBA was 8.9 mg l–1. The compound was found to be cytotoxic, causing statistically significant reductions in root growth and mitotic index in a dose- and tim...

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