57(P-31) 新規抗腫瘍抗生物質FE399(ポスター発表の部)

概要

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Most of clinical anticancer drugs have severe side effects and are not so effective on solid tumor. Therefore, a new drug having high selectivity between cancer and normal cells have been required. Many kinds of malignant tumor are reported to have mutation as p53 gene. We screened for lead compounds of anticancer drugs that induce apoptosis specifically on colon cancer cell mutated as p53 gene from microorganisms extractions. The novel depsipeptide, FE399, is one of our candidates found through the screening and isolated from the extract of cultured Ascochyta sp. The structure of FE399 was deduced by high-resolution MS spectrum and several 2D-NMR methods including COSY, HMQC, HOHAHA and HMBC. FE399 has two conformers due to the steric hindrance of disulfide ring. FE399 indicate strong cytotoxicity due to apoptosis and highly inhibition of tumor growth in vivo but not elongate of life.
2000-10-01