Diterpenes from Alomia myriadenia (Asteraceae) with cytotoxic and trypanocidal activity.
Further investigation of the aerial parts of Alomia myriadenia revealed an halimane diterpene identified as ent-8S,12S-epoxy-7R,16-dihydroxyhalima-5(10),13-dien-15,16-olide along with the known ent-16-hydroxylabda-7,13-dien-15,16-olide, ent-12R-hydroxylabda-7,13-dien-15,16-olide, 6,7-methylenedioxycoumarin (ayapin), and kaempferol-7-methylether (rhamnocitrin). Evaluated in a panel of human cancer cell lines, the 16-hydroxylabade diterpene was the most active, showing an ED(50) value of 0.3 mug/ml against Lu1 (human lung cancer) cells. Tested in vitro against Trypanosoma cruzi in infected murine blood, this compound caused lysis of 100% of the parasites at 250 mug/ml.
Laboratório de Química de Produtos Naturais, CPqRR-FIOCRUZ, Av. Augusto de Lima, 1715, Belo Horizonte, MG 30190-002, Brazil.
Elita
E
Scio
Antônia
A
Ribeiro
Tânia M A
TM
Alves
Alvaro J
AJ
Romanha
José
J
Dias de Souza Filho
Geoffrey A
GA
Cordell
Carlos L
CL
Zani
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D035261:Plant Components, Aerial / Q000737:chemistry; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; D014344:Trypanocidal Agents