A novel antitumour compound from the mucus of a coral, Galaxea fascicularis, inhibits topoisomerase I and II.
S2 isolated from the mucus of G. fascicularis contains anti-topoisomerase activity, causing cytotoxicity to a multiple-drug resistant leukaemia cell line, P388/VCR. It inhibits DNA relaxation catalysed by topoisomerase I and II. S2 stabilised the topoisomerase I-DNA cleavable complex, thereby inhibiting the DNA replication machinery, leading to cell death. The active centre of S2 probably contains a Gal beta(1-4)GlcNAc dissacharide linkage. S2 has potentials of being developed into a new anticancer therapeutic.
Fung
F M
FM
Marine Biotechnology Laboratory, School of Biological Sciences, National University of Singapore, Singapore.
Ding
J L
JL
D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D003063:Cnidaria / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D051379:Mice; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors