IN-VIVO ANTITUMOR EFFECT OF 3'-SULPHONOQUINOVOSYL 1'-MONOACYLGLYCERIDE ISOLATED FROM SEA-URCHIN (STRONGYLOCENTROTUS-INTERMEDIUS) INTESTINE

Extracts from sea urchin intestine were screened for new anti-tumour d rugs. Four glycolipids, 3'-sulphonoquinovosyl-1', 2'-diacylglyceride ( A-4), 3'-sulphonoquinovosyl-1'-monoacylglyceride (2'-lyso A-4, A-5), N euGco2-6Glc beta 1-1ceramide (A-6) and HSO3-8NeuGc alpha 2-6Glc beta 1 -1ceramide (A-7), were isolated from the intestine of sea urchin, Stro ngylocentrotus intermedius, and characterized by means of proton nucle ar magnetic resonance spectroscopy and fast atom bombardment mass spec trometry. When tested for cytotoxic activity against tumour cells in v itro, A-5 showed significant activity, but A-4, -6 and -7 did not. In addition, the hydrophilic derivatives of A-4 or -5 had no cytotoxicity . Furthermore, the anti-tumour effects on nude mice bearing solid tumo urs of a human lung adenocarcinoma cell line A-549 were evaluated in v ivo using A-4 and -5. As a result, A-5 was found to be significantly e ffective in suppressing the growth of solid tumours, whereas A-4 had n o effect. Pathologically, the solid tumours showed haemorrhagic necros is areas after treatment with A-5. In this study, we have demonstrated the anti-tumour effect of sulphonoquinovosyl-lysoglyceride (A-5), whi ch provides important information that this sulpholipid could be a use ful drug for cancer chemotherapy.