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.
Department of Pharmacognosy, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia. chinou@pharm.uoa.gr
T
T
Kundakovic
N
N
Fokialakis
S
S
Dobric
H
H
Pratsinis
D
D
Kletsas
N
N
Kovacevic
I
I
Chinou
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