70(P-59) 海綿由来イソプレノイド化合物、ステレッタマイドA誘導体の生理活性作用(ポスター発表の部)

概要

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We isolated a novel isoprenoid, stellettamide-A (ST-A), from a marine sponge of the genus Stelletta (Hirota, 1990), which has been found to be a CaM antagonist (Abe et al., 1997). In addition, many isoprenoids derivatives (ST-family) were purified from marine sponge (Shin et al. 1997, Matsunaga et al., 1999). In contrast, there are some endogenous isoprenoids in mammalian cells such as farnesol and vitamine E. These endogenous isoprenoids have an important role in cell functions. In the present study, we examined effects of marine sponge derived isoprenoid compounds and farnesol on calmodulin activity and L-type Ca^<2+> channel activity to analyze of relationship between chemical structure and bioactivity in these compounds. In the present study, we found that ST-A inhibits both calmodulin ability and L-type Ca^<2+> channel activity. In contrast, farnesol inhibited L-type Ca^<2+> channel activity without affecting on calmodulin ability. The chemical structure-bioactivity relationship analysis in the ST-family lead the hypothesis to us that charge number in alkaloid part and configuration between isoprenoid chain and alkaloid may be important for onset of calmodulin antagonistic action. In contrast, isoprenoid chain may be important for the direct inhibitory action of L-type Ca^<2+> channel activity. In addition, the inhibitory action for the channels may be dependent on length of isoprenoids side-chain.
天然有機化合物討論会の論文
2004-10-01