title: Anti-tumour activity of two 19-nor-clerodane diterpenes, trans-dehydrocrotonin and trans-crotonin, from Croton cajucara.
abstract: The effects of two nor-diterpenes, trans-dehydrocrotonin (DCTN) and trans-crotonin (CTN) from Croton cajucara (Euphorbiaceae), on the survival of mice bearing Sarcoma 180 and Ehrlich carcinoma ascitic tumours, on the proliferation of cultured Ehrlich cells and TNF alpha activity were determined. When the mice were treated with 80 and 120 mg/kg of DCTN or 38 mg/kg of 5-FU a significant anti-tumour activity was obtained (%T/C of 128-140). The cytotoxicity against Ehrlich carcinoma was 16 microM for DCTN and CTN whereas the flavonoid quercetin was cytotoxic at 44 microM in 48 h cell culture. No apoptosis was seen on in vitro electrophoresis of DNA extracted from the tumour cells treated with DCTN and CTN. A significant TNF alpha activity was detected in Ehrlich tumour-bearing mice treated with DCTN suggesting an enhanced immune function.
authors.affiliation: Departamento de Química, Universidade Federal Rural do Rio de Janeiro, Brazil. echevarr@ufrrj.br
authors.forename: N F
authors.initials: NF
authors.lastname: Grynberg
authors.forename: A
authors.initials: A
authors.lastname: Echevarria
authors.forename: J E
authors.initials: JE
authors.lastname: Lima
authors.forename: S S
authors.initials: SS
authors.lastname: Pamplona
authors.forename: A C
authors.initials: AC
authors.lastname: Pinto
authors.forename: M A
authors.initials: MA
authors.lastname: Maciel
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology*; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism / Q000473:pathology; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D045785:Diterpenes, Clerodane; D004354:Drug Screening Assays, Antitumor; D019665:Euphorbiaceae / Q000737:chemistry*; D005260:Female; D051379:Mice; D010946:Plants, Medicinal / Q000737:chemistry*; D014407:Tumor Cells, Cultured; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D045785:Diterpenes, Clerodane; D014409:Tumor Necrosis Factor-alpha; C103060:dehydrocrotonin; C403585:trans-crotonin