title: Studies on the cytotoxicity of cucurbitacins isolated from Cayaponia racemosa (Cucurbitaceae).
abstract: The cytotoxic potential of three cucurbitacins, 2,3,16,20(R),25-pentahydroxy-11,22-dioxo-cucurbita-5-en (cucurbitacin P, 1), 2,3,16,20(R),25-pentahydroxy-22-oxocucurbita-5-en (2) and 2,3,16,20(R),25-pentahydroxy-22-oxocucurbita-5,23(E)-diene (deacetylpicracin, 3), obtained from Cayaponia racemosa was evaluated as their ability to induce brine shrimp lethality, to inhibit the development of sea urchin eggs and tumor cell proliferation, and to lysis mouse erythrocytes. Compounds 1 and 2 were highly toxic with LC50 of (29.6+/-.1) (56.8) and (38.8 +/-.0) (76.6) micro/mL (umicro), respectively, while compound 3 was not effective at the tested concentrations. All tested compounds possessed an inhibitory effect on the proliferation of tumor cell lines, compound 1 being the most active, followed by 2 and 3. Nevertheless, no hemolytic activity or inhibition of the development of sea urchin eggs was observed for these compounds.
authors.affiliation: Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, P.O. Box 3157, 60430-270 Fortaleza, Ceará, Brazil.
authors.forename: Ivana Nogueira Fernandes
authors.initials: IN
authors.lastname: Dantas
authors.forename: Gardenia Carmen Militão
authors.initials: GC
authors.lastname: Gadelha
authors.forename: Davina Camelo
authors.initials: DC
authors.lastname: Chaves
authors.forename: Francisco José Queiroz
authors.initials: FJ
authors.lastname: Monte
authors.forename: Cláudia
authors.initials: C
authors.lastname: Pessoa
authors.forename: Manoel Odorico
authors.initials: MO
authors.lastname: de Moraes
authors.forename: Letícia Veras
authors.initials: LV
authors.lastname: Costa-Lotufo
mesh_terms: D000818:Animals; D001156:Artemia / Q000187:drug effects*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D019662:Cucurbitaceae / Q000737:chemistry*; D006461:Hemolysis; D053878:Hemolytic Agents / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D008938:Mitosis / Q000187:drug effects; D014315:Triterpenes / Q000302:isolation & purification* / Q000633:toxicity
chemical_list: D053878:Hemolytic Agents; D014315:Triterpenes; C041246:cucurbitacin B; C474429:cucurbitacin C