Diterpenes from Alomia myriadenia (Asteraceae) with cytotoxic and trypanocidal activity

被引:44
|
作者
Scio, E
Ribeiro, A
Alves, TMA
Romanha, AJ
de Souza, JD
Cordell, GA
Zani, CL
机构
[1] Fiocruz MS, CPqRR, Lab Quim Prod Nat, BR-30190002 Belo Horizonte, MG, Brazil
[2] Univ Fed Juiz de Fora, ICB, Dept Bioquim, BR-36036030 Juiz de Fora, MG, Brazil
[3] Fiocruz MS, CPqRR, Lab Parasitol Celular & Mol, BR-30190002 Belo Horizonte, MG, Brazil
[4] Univ Fed Minas Gerais, ICEx, Dept Quim, Belo Horizonte, MG, Brazil
[5] Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, Chicago, IL 60612 USA
关键词
Ageratum myriadenium; Alomia myriadenia; Compositae; halimane; labdane; Trypanosoma cruzi; human cancer cell line;
D O I
10.1016/S0031-9422(03)00529-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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-12Rhydroxylabda-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 ED50 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. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1125 / 1131
页数:7
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