Evaluation of the anti-inflammatory and cytotoxic activities of naphthazarine derivatives from Onosma leptantha.
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.
Kundakovic
T
T
Department of Pharmacognosy, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia. chinou@pharm.uoa.gr
Fokialakis
N
N
Dobric
S
S
Pratsinis
H
H
Kletsas
D
D
Kovacevic
N
N
Chinou
I
I
D000818:Animals; D000880:Anthraquinones / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001681:Biological Assay / Q000379:methods; D028082:Boraginaceae / Q000737:chemistry*; D002351:Carrageenan / Q000494:pharmacology; D045744:Cell Line, Tumor; D003510:Cyclohexanes / Q000737:chemistry; D004487:Edema / Q000139:chemically induced; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D009285:Naphthoquinones / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D018517:Plant Roots / Q000737:chemistry / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar
D000880:Anthraquinones; D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D003510:Cyclohexanes; D009285:Naphthoquinones; D010936:Plant Extracts; C016101:shikonin; C032573:beta, beta-dimethylacrylshikonin; D002351:Carrageenan; C073944:acetylshikonin; D007213:Indomethacin