P-51 新規非ペプチド性レニン阻害剤Naphthostatin類の構造決定(ポスター発表の部)

概要

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In the course of our screening program of renin inhibitors, we isolated novel ansa-macrolides, naphthostatins A(1), B(2), C(3) and D(4) from the cultured broth of an actinomycete, Streptomyces sp. NR0640. The molecular formula of the naphthostatins were determined to be C_<51>H_<60>O_<11>N_2, (1 and 2), C_<80>H_<93>O_<18>N_3S(3) and C_<39>H_<46>O_9N_2(4) respectively, on the basis of HRFAB-MS and ^<13>C NMR. The structure determination of the naphthostatins was performed by various 2D NMR techniques, including HMBC, NOESY and deuterium-induced shift experiments of ^<13>C nuclei. Naphthostatins A(1) and B(2), which are epimers at C44 each other and have a diazatricyclo[4.3.3.0] ring systems in their molecules, showed selective activity against human plasma renin with IC_<50>s of 1.7 to 3.3μg/ml and no significant cytotoxicity against HeLa cells at 40μg/ml concentration.
天然有機化合物討論会の論文
1994-09-20