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Wube, A. A., Streit, B., Gibbons, S., Asres, K., & Bucar, F. (2005). In vitro 12(s)-hete inhibitory activities of naphthoquinones isolated from the root bark of euclea racemosa ssp. schimperi. Journal of Ethnopharmacology, 102(2), 191–196. 
Resource type: Journal Article
DOI: 10.1016/j.jep.2005.06.009
ID no. (ISBN etc.): 3788741
BibTeX citation key: Wube2005
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Categories: General
Keywords: 12-Lipoxygenase, 12(S)-HETE, 7-Methyljuglone, Euclea racemosa ssp. schimperi, Naphthoquinones, Neodiospyrin
Creators: Asres, Bucar, Gibbons, Streit, Wube
Collection: Journal of Ethnopharmacology
Platelet 12-lipoxygenase is believed to play a role in cancer and other pathological conditions, such as psoriasis, atherosclerosis and arthritis. The inhibition of 12-LOX is a potential therapeutic approach in the treatment of tumor metastasis. The extracts of Euclea racemosa Murr. ssp. schimperi (A. DC.) F. White (Ebenaceae) obtained by maceration and naphthoquinones isolated from the dichloromethane extract have been investigated for their 12(S)-HETE inhibitory activity using human platelets. At 100 $μ$g/ml, the dichloromethane extract inhibited the formation of 12(S)-HETE by 88.7% and compounds 7-methyljuglone (2), isodiospyrin (3), neodiospyrin (4) and mamegakinone (5), isolated from this extract, exhibited significant activities with IC 50 values ranging from 4 to 58 $μ$g/ml (22.2-155.7 $μ$M). Of these the most abundant compound, 7-methyljuglone displayed a potent inhibitory activity with an IC50 value of 4.18 $μ$g/ml (22.2 $μ$M), which was comparable to the positive control baicalein with an IC50 value of 5 $μ$g/ml (18.5 $μ$M). In contrast, 4(S)-shinanolone (1), the reduced form of compound 2, did not show any significant inhibitory activity even at a concentration of 60 $μ$g/ml. ©2005 Elsevier Ireland Ltd. All rights reserved.