P-13 海綿Crella (Yvesia) spinulata由来のカテプシンB阻害物質の単離と構造決定(ポスター発表の部)

概要

論文の詳細を見る
Cathepsins, collectively known as a class of lysosomal proteindegrading enzymes, have been shown to possess specific physiological activities including cancer progression. The contribution of cathepsin B in tumor invasion is well documented and the inhibition of its activity resulted in a decreased invasiveness of tumor cells. Therefore, the inhibitors of cathepsin B have a potential as anticancer agents. In our search for anticancer lead compounds from Japanese marine invertebrates, we found activity in the extract of the marine sponge Crella (Yvesia) spinulata. Bioassay-guided fractionation afforded two new sterol dimers named shishicrellastatins A (1) and B (2). The structure of shishicrellastatin A (1) was elucidated by interpretation of spectral data. Relative stereochemistry was elucidated by analysis of the ROESY spectrum. Shishicrellastatin B (2) was a dehydrogenated derivative of 1. Compounds 1 and 2 exhibited cathepsin B inhibitory activity.
天然有機化合物討論会の論文
2008-09-01