Anti-proliferation activity of synthetic ajoene analogues on cancer cell-lines.
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| Abstract |
The ability of garlic preparations to inhibit cancer cell-growth has been attributed to a group of structurally-related organosulfur compounds found in the crushed clove. Historically, interest has centred on three such compounds as allicin, diallyl disulfide and diallyl trisulfide, with less interest on E- and Z-ajoene. A recently developed synthetic route from our laboratory for preparing ajoene analogues allows access to derivatives containing the sulfoxide / vinyl disulfide core whilst varying the terminal end-group functionality. A small library has been synthesized and an advanced lead with p-methoxybenzyl end groups (8) identified. Data on the in vitro anti-proliferation activity of compound (8) is presented here against six cancer cell-lines in comparison with that of Z- and E-ajoene to reveal an enhancement in activity of up to twelvefold. In addition, a modest selectivity is observed for tumour over normal cell-lines of up to threefold. Data on ajoene and its derivatives is presented in the context of chemosensitization in drug-resistance, and ideas on ajoene's mode of action at the molecular level are presented and discussed.
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| Authors | Catherine H Kaschula, Roger Hunter, Hassan T Hassan, Nashia Stellenboom, Jonathan Cotton, Xiao Q Zhai, M Iqbal Parker |
| Journal | Anti-cancer agents in medicinal chemistry (Anticancer Agents Med Chem) Vol. 11 Issue 3 Pg. 260-6 (Mar 2011) ISSN: 1875-5992 [Electronic] Netherlands |
| PMID | 21269251 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review) |
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