• YAKHAK HOEJI
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• v.34 no.4
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• pp.262-266
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• 1990

Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity ($ED_{50}=0.10\;ug/ml$) against L1210 cell and T/C = 182% in ICR mice bearing S-180 at a dose of 5 mg/kg. Administrations of 10 mg/kg and 15 mg/kg reduced the T/C values to 60 and 77% respectively. Higher doses reveal toxicity. Seven naphthazarin derivatives synthesized showed good cytotoxic activities against L1210 cell. Especially, naphthazarin and hydronaphthazarin have strong activities ($ED_{50}=0.05\;ug/ml$ for both). Naphthazarin showed a severe toxic effect on ICR mice bearing S-180; no significant toxic effect was observed at a dose of 1 mg/kg or 2 mg/kg, but a severe toxicity (T/C = 23%) by administration of 5 mg/kg. Alkylation of C-2 of naphthazarin is necessary for reducing the toxic effect on ICR mice bearing S-180.