Cytotoxic, cytostatic and HIV-1 PR inhibitory activities of the soft coral Litophyton arboreum

Show simple item record Ellithey, M.S. (Mona) Lall, Namrita Hussein, Ahmed A. Meyer, Debra 2014-03-04T11:41:58Z 2014-03-04T11:41:58Z 2013-12
dc.description.abstract Bioassay-guided fractionation using different chromatographic and spectroscopic techniques in the analysis of the Red Sea soft coral Litophyton arboreum led to the isolation of nine compounds; sarcophytol M (1), alismol (2), 24-methylcholesta-5,24(28)-diene-3β-ol (3), 10-O-methyl alismoxide (4), alismoxide (5), (S)-chimyl alcohol (6), 7β-acetoxy-24-methylcholesta-5-24(28)-diene-3,19-diol (7), erythro-N-dodecanoyl-docosasphinga-(4E,8E)-dienine (8), and 24-methylcholesta-5,24 (28)-diene-3β,7β,19-triol (9). Some of the isolated compounds demonstrated potent cytotoxic- and/or cytostatic activity against HeLa and U937 cancer cell lines and inhibitory activity against HIV-1 protease (PR). Compound 7 was strongly cytotoxic against HeLa cells (CC50 4.3 ± 0.75 μM), with selectivity index of SI 8.1, which was confirmed by real time cell electronic sensing (RT-CES). Compounds 2, 7, and 8 showed strong inhibitory activity against HIV-1 PR at IC50s of 7.20 ± 0.7, 4.85 ± 0.18, and 4.80 ± 0.92 μM respectively. In silico docking of most compounds presented comparable scores to that of acetyl pepstatin, a known HIV-1 PR inhibitor. Interestingly, compound 8 showed potent HIV-1 PR inhibitory activity in the absence of cytotoxicity against the cell lines used. In addition, compounds 2 and 5 demonstrated cytostatic action in HeLa cells, revealing potential use in virostatic cocktails. Taken together, data presented here suggest Litophyton arboreum to contain promising compounds for further investigation against the diseases mentioned. en_US
dc.description.librarian hb2014 en_US
dc.description.sponsorship Medical Research Council, the Technology Innovation Agency and the University of Pretoria, South Africa. en_US
dc.description.uri en_US
dc.identifier.citation Ellithey, MS, Lall, N, Hussein, AA & Meyer, D 2013, 'Cytotoxic, cytostatic and HIV-1 PR inhibitory activities of the soft coral Litophyton arboreum', Marine Drugs , vol. 11, no.12, pp. 4917-4932. en_US
dc.identifier.issn 1660-3397 (print)
dc.identifier.issn 1660-3397 (online)
dc.identifier.other 10.3390/md11124917
dc.language.iso en en_US
dc.publisher MDPI en_US
dc.rights © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( en_US
dc.subject Red sea en_US
dc.subject Litophyton arboreum en_US
dc.subject HIV-1 protease en_US
dc.subject HIV-1 reverse transcriptase en_US
dc.subject Cytotoxicity en_US
dc.subject Real time cell analysis en_US
dc.title Cytotoxic, cytostatic and HIV-1 PR inhibitory activities of the soft coral Litophyton arboreum en_US
dc.type Article en_US

Files in this item

This item appears in the following Collection(s)

Show simple item record