53(P15) Ornitho galum saundersiaeより単離されたコレスタン配糖体の構造とそれらの各種悪性腫瘍細胞に対する強力な細胞毒性(ポスター発表の部)

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Ornithogalum saundersiae (Liliaceae) is a perennial plant which is native to Natal, Swaziland and the eastern Transvaal. We have found that the MeOH extract of Ornithogalum saundersiae bulbs exhibited extremely potent cytotoxic activity toward human promyelocytic leukemia HL-60 cells with an LC_<50> value of 0.031μg/ml. Bioassay-guided fractionation of the MeOH extract led to the isolation of a series of cholestane glycosides (1-7) with potent cytotoxic activities toward HL-60 cells and human Tlymphocytic leukemia MOLT-4 cells. The structures of 1-7 were determined by two-dimensional NMR techniques, ^1H-^1H COSY, phase-sensitive NOESY, HMQC and HMBC spectra, and acid- and alkaline catalyzed hydrolysis. Cytotoxic activities of 1 and 3 - 7, which possess an acetyl group and an aromatic acyl group linked to the saccharide moiety, on HL-60 and MOLT-4 cells were much more potent than those of the clinically applied anticancer agents, etoposide, adriamycin (ADM) and methotrexate. Further detail examination of 1, which was obtained as a main constituent, discovered that 1 exhibited potent cytotoxic activities against various malignant tumor cells such as mouse mastrocarcinoma, human pulmonary adenocarcinoma and human pulmonary large cell carcinoma including ADM-resistant mouse leukemia (P388) and camptothecin (CPT)-resistant P388; the activities are about 10-100 times more potent than those of the clinically applied anticancer agents, miiomycin C, AMD, cisplatin, CPT and taxol (TAX). Compound 1 has little toxicity to normal human pulmonary cells. In in vivo evaluation made up to the present, 1 was remarkably effective to mouse P388 (increased life span: 59%) by one time administration of 0.01mg/kg. Accordingly, 1 could be expected to be a new anticancer agent from a higher plant next to CPT and TAX.
天然有機化合物討論会の論文
1996-09-02

53(P15) Ornitho galum saundersiaeより単離されたコレスタン配糖体の構造とそれらの各種悪性腫瘍細胞に対する強力な細胞毒性(ポスター発表の部)

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