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

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dc.contributor.authorEllithey, Mona S.
dc.contributor.authorLall, Namrita
dc.contributor.authorHussein, Ahmed A.
dc.contributor.authorMeyer, Debra
dc.date.accessioned2017-02-28T11:37:22Z
dc.date.available2017-02-28T11:37:22Z
dc.date.issued2013
dc.description.abstractBioassay-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.accreditationISI
dc.identifier.citationEllithey, M.S. et al. (2013). Cytotoxic, Cytostatic and HIV-1 PR Inhibitory Activities of the Soft Coral Litophyton arboreum. Marine Drugs, 11, 4917-4936.en_US
dc.identifier.issn1660-3397
dc.identifier.urihttp://hdl.handle.net/10566/2579
dc.identifier.urihttp://dx.doi.org/10.3390/md11124917
dc.language.isoenen_US
dc.publisherMDPIen_US
dc.rightsAll articles published by MDPI are made immediately available worldwide under an open access license
dc.subjectRed seaen_US
dc.subjectLitophyton arboreumen_US
dc.subjectHIV-1 proteaseen_US
dc.subjectHIV-1 reverse transcriptaseen_US
dc.subjectCytotoxicityen_US
dc.subjectReal time cell analysisen_US
dc.titleCytotoxic, cytostatic and HIV-1 PR inhibitory activities of the soft coral litophyton arboreumen_US
dc.typeArticleen_US

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