title: In vivo anti-tumour effect of 3'-sulphonoquinovosyl 1'-monoacylglyceride isolated from sea urchin (Strongylocentrotus intermedius) intestine.
abstract: Extracts from sea urchin intestine were screened for new anti-tumour drugs. Four glycolipids, 3'-sulphonoquinovosyl-1', 2'-diacylglyceride (A-4), 3'-sulphonoquinovosyl-1'-monoacylglyceride (2'-lyso A-4, A-5), NeuGc(alpha)2-6Glc(beta)1-1ceramide (A-6) and HSO3-8NeuGc(alpha)2-6Glc(beta)1-1ceramide (A-7), were isolated from the intestine of sea urchin, Strongylocentrotus intermedius, and characterized by means of proton nuclear magnetic resonance spectroscopy and fast atom bombardment mass spectrometry. When tested for cytotoxic activity against tumour cells in vitro, 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 tumours of a human lung adenocarcinoma cell line A-549 were evaluated in vivo using A-4 and -5. As a result, A-5 was found to be significantly effective in suppressing the growth of solid tumours, whereas A-4 had no effect. Pathologically, the solid tumours showed haemorrhagic necrosis areas after treatment with A-5. In this study, we have demonstrated the anti-tumour effect of sulphonoquinovosyl-lysoglyceride (A-5), which provides important information that this sulpholipid could be a useful drug for cancer chemotherapy.
authors.affiliation: Marine Biomedical Institute, Sapporo Medical University School of Medicine, Rishirifuji, Hokkaido, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Sahara
authors.forename: M
authors.initials: M
authors.lastname: Ishikawa
authors.forename: N
authors.initials: N
authors.lastname: Takahashi
authors.forename: S
authors.initials: S
authors.lastname: Ohtani
authors.forename: N
authors.initials: N
authors.lastname: Sato
authors.forename: S
authors.initials: S
authors.lastname: Gasa
authors.forename: T
authors.initials: T
authors.lastname: Akino
authors.forename: K
authors.initials: K
authors.lastname: Kikuchi
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000473:pathology; D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000627:therapeutic use / Q000633:toxicity*; D002236:Carbohydrate Conformation; D002240:Carbohydrate Sequence; D002460:Cell Line; D002471:Cell Transformation, Neoplastic; D011905:Genes, ras; D006017:Glycolipids / Q000302:isolation & purification / Q000627:therapeutic use / Q000633:toxicity*; D006801:Humans; D007422:Intestines; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008819:Mice, Nude; D008969:Molecular Sequence Data; D050178:Monoglycerides; D051381:Rats; D012617:Sea Urchins; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014162:Transfection; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
chemical_list: C104118:3'-sulfonoquinovosyl-1'-monoacylglyceride; D000970:Antineoplastic Agents; D006017:Glycolipids; D050178:Monoglycerides