A new antitumour substance, 7-oxabicyclo (2.2.1)-5-heptene-2,3-dicarboxylic anhydride.
7-Oxabicyclo(2.2.1)-5-heptene-2,3-dicarboxylic anhydride has been found to possess antitumour activity against Ehrlich ascites carcinoma cells. The tumour cells incubated with the drug showed a decrease in the viable counts and cell proliferation. These effects were confirmed by in vivo studies in Swiss albino mice. The compound has a direct cytotoxic effect on the tumour cells. Vacuolization and disruption of the cytoplasm accompanied by unequal nuclear division and scattered chromosomes were recorded. In addition, 250 and 10 mg/kg were found to be the MTD and MED respectively. A dose of 25 mg/kg injected i.p. for 5 consecutive days in the tumour-transplanted animals caused a significant increase in their survival period. The compound has been shown to have a significant inhibitory effect on the DNA and RNA biosynthesis of EAC cells after 3 hr of administration; the protein biosynthesis was less affected. Meanwhile, the cellular contents of these metabolites were significantly reduced.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001835:Body Weight / Q000187:drug effects; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology / Q000627:therapeutic use*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds / Q000627:therapeutic use*; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004273:DNA, Neoplasm / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D005260:Female; D008055:Lipids / Q000096:biosynthesis; D051379:Mice; D009363:Neoplasm Proteins / Q000096:biosynthesis; D010796:Phthalic Anhydrides; D012334:RNA, Neoplasm / Q000096:biosynthesis
D000970:Antineoplastic Agents; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds; D004273:DNA, Neoplasm; D008055:Lipids; D009363:Neoplasm Proteins; D010796:Phthalic Anhydrides; D012334:RNA, Neoplasm; C035993:7-oxabicyclo(2.2.1)-5-heptene-2,3-dicarboxylic anhydride