Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity (ED_(50)=0.10 ug/m/) 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 red...
Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity (ED_(50)=0.10 ug/m/) 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/m/ 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.