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• Ellithey, MS.
• Lall, N
• Hussein, AA.
• Meyer, D
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• Ellithey, MS.
• Lall, N
• Hussein, AA.
• Meyer, D
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• Lall, N
• Hussein, AA.
• Meyer, D

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Mar. Drugs 2013, 11(12), 4917-4936; doi:10.3390/md11124917

Article

Cytotoxic, Cytostatic and HIV-1 PR Inhibitory Activities of the Soft Coral Litophyton arboreum

Mona S. Ellithey ¹, Namrita Lall ², Ahmed A. Hussein ³ and Debra Meyer ^1,*

¹ Department of Biochemistry, University of Pretoria, Pretoria 0002, South Africa ² Department of Plant Science, University of Pretoria, Pretoria 0002, South Africa ³ Department of Chemistry, University of the Western Cape, Private Bag X17, Belleville 7535, South Africa

* Author to whom correspondence should be addressed.

Received: 24 September 2013; in revised form: 18 November 2013 / Accepted: 19 November 2013 / Published: 10 December 2013

(This article belongs to the Special Issue Bioactive Compounds from Marine Invertebrates)

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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.

Keywords: red sea; Litophyton arboreum; HIV-1 protease; HIV-1 reverse transcriptase; cytotoxicity; real time cell analysis

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