RESUMO
Lantadenes are pentacyclic triterpenoids of the weed Lantana camara. Five new lantadenes (14-18) and their methyl esters (20-24) were synthesized, characterized, and screened for cytotoxicity against four human cancer cell lines. The parent compound (1) and the four most active compounds (15, 16, 21, and 22) were further studied for their in vivo tumor inhibitory potential on squamous cell carcinogenesis in Swiss albino mice induced by 7,12-dimethylbenz[a]anthracene (DMBA) and promoted by 12-O-tetradecanoylphorbol-13-acetate (TPA). These results were supported by histopathological studies and discussed in terms of structure-activity relationships. The results inferred the importance of the groups attached to C-22 and C-17 in relation to the antitumor activity of these compounds.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lantana/química , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacologia , Plantas Medicinais/química , 9,10-Dimetil-1,2-benzantraceno/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Células HL-60 , Células HeLa , Humanos , Índia , Camundongos , Camundongos Endogâmicos , Ácido Oleanólico/química , Ácido Oleanólico/isolamento & purificação , Folhas de Planta/química , Relação Estrutura-Atividade , Acetato de Tetradecanoilforbol/farmacologiaRESUMO
Eupatorium genus grows wild in many parts of the world. A number of species of Eupatorium are toxic to grazing animals. Milk sickness in humans is caused by ingestion of milk of the animals reared on the pastures infested with Eupatorium rugosum (white snakeroot). While some information is available on the toxins in various species of Eupatorium, ambiguities still persist in extrapolation of the data to field incidence of toxicosis. Eupatorium genus has been used for its medicinal properties for many decades. A number of bioactive natural products have been reported in the extracts of Eupatorium spp. and the genus is a promising bioresource for preparation of drugs and value-added products.