In vitro 12(S)-HETE inhibitory activities of naphthoquinones isolated from the root bark of Euclea racemosa ssp. schimperi

Wube, Abraham Abebe, Streit, Bernhard, Gibbons, Simon, Asres, Kaleab and Bucar, Franz (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). pp. 191-196. ISSN 0378-8741

Full text not available from this repository. (Request a copy)

Abstract

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 μg/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 IC50 values ranging from 4 to 58 μg/ml (22.2–155.7 μM). Of these the most abundant compound, 7-methyljuglone displayed a potent inhibitory activity with an IC50 value of 4.18 μg/ml (22.2 μM), which was comparable to the positive control baicalein with an IC50 value of 5 μg/ml (18.5 μM). 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 μg/ml.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 30 Jun 2020 00:20
Last Modified: 30 Jun 2020 00:20
URI: https://ueaeprints.uea.ac.uk/id/eprint/75829
DOI: 10.1016/j.jep.2005.06.009

Actions (login required)

View Item View Item