Evaluation of the anti-inflammatory and cytotoxic activities of naphthazarine derivatives from Onosma leptantha

• Published in: Phytomedicine (Stuttgart) 2006-03, Vol.13 (4), p.290-294
• Main Authors: Kundakovic, T., Fokialakis, N., Dobric, S., Pratsinis, H., Kletsas, D., Kovacevic, N., Chinou, I.
• Format: Article
• Language: English
• Subjects: Animals; Anthraquinones - chemistry; Anthraquinones - pharmacology; Anthraquinones - toxicity; Anti-inflammatory activity; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - toxicity; Anti-inflammatory drugs; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - toxicity; Biological Assay - methods; Boraginaceae - chemistry; Carrageenan - pharmacology; Cell Line, Tumor; Cyclohexanes - chemistry; Cytotoxicity; Edema - chemically induced; Humans; Indomethacin - pharmacology; Inhibitory Concentration 50; Male; Medicine, Botanic; Medicine, Herbal; Naphthazarines; Naphthoquinones - chemistry; Naphthoquinones - pharmacology; Naphthoquinones - toxicity; Onosma leptantha; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Extracts - toxicity; Plant Roots - chemistry; Plant Roots - toxicity; Rats; Rats, Wistar; Shikonin-derivatives
• ISSN: 0944-7113; 1618-095X
• DOI: 10.1016/j.phymed.2004.10.009

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: β, β-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.