The behavior of dihydropyrazine with DNA strand-breakage activity in vivo

Abstract

The effects on the viability of cell lines treated with 2,3-dihydro-5,6-dimethylpyrazine and its derivatives, which revealed DNA strand-breakage activity by the generation of radicals in vitro, were recognized from certain morphological changes and the detection of apoptosis-related proteins: cleaved PARP and SAPK/JNK. These results would suggest that sugar-derived dihydropyrazines induce changes in the cells of certain organs and cause various internal injuries in vivo. The biodistribution of 14C-labelled 2,3-dihydro-5,6-dimethylpyrazine was studied in mouse and the autoradiograms showed highly contrasting results. Radioactivity was high in the brain, spinal cord, salivary gland, and thymus and low in the heart, stomach, and blood. The result was supported by the activity (% dose per organ). © 2003 Pharmaceutical Society of Japan.