Abstract
The root extracts of Onosma leptanhtha were evaluated for their anti-iflammatory and cytotoxic activities. The cyclohexane extract, which appeared as the most active in both assays, has been further subjected to bioassay-directed fractionation to afford the naphthazarine derivatives: beta,beta-dimethylacrylshikonin (1), isovalerylshikonin (2) and acetylshikonin (3). The evaluation of the anti-inflammatory activity was performed on carrageenan-induced rat paw edema test. All the tested compounds proved to be active, while compound 3 showed the best anti-inflammatory effect. In addition, the cytotoxic activity of the extracts and isolated compounds, was also assayed against L1210 murine lymphoblastic leukemia cell line, and human fibrosarcoma HT-1080 cells. Compound 1 exhibited remarkable cytotoxic activity (390 nM for L1210 cells), which is superior to that of shikonin, which was used as control.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anthraquinones / chemistry
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Anthraquinones / pharmacology
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Anthraquinones / toxicity
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Anti-Inflammatory Agents / toxicity
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / toxicity
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Biological Assay / methods
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Boraginaceae / chemistry*
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Carrageenan / pharmacology
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Cell Line, Tumor
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Cyclohexanes / chemistry
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Edema / chemically induced
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Humans
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Indomethacin / pharmacology
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Inhibitory Concentration 50
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Male
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Naphthoquinones / chemistry
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Naphthoquinones / pharmacology*
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Naphthoquinones / toxicity
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Plant Extracts / chemistry
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Plant Extracts / pharmacology*
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Plant Extracts / toxicity
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Plant Roots / chemistry
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Plant Roots / toxicity
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Rats
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Rats, Wistar
Substances
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Anthraquinones
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Anti-Inflammatory Agents
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Antineoplastic Agents
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Cyclohexanes
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Naphthoquinones
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Plant Extracts
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shikonin
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beta, beta-dimethylacrylshikonin
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Carrageenan
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acetylshikonin
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Indomethacin