Abrantes Marta, Mil-Homens Tânia, Duarte Noélia, Lopes Dinora, Cravo Pedro, Madureira Maria do, Ferreira Maria-José U
iMed.UL, Faculdade de Farmácia, Universidade de Lisboa, Lisboa, Portugal.
Planta Med. 2008 Sep;74(11):1408-12. doi: 10.1055/s-2008-1081317. Epub 2008 Jul 31.
The dichloromethane, methanol and aqueous ethanol extracts of the stem bark of Pycnanthus angolensis were evaluated for their in vitro activity against the 3D7 Plasmodium falciparum strain. The CH (2)Cl (2) extract was the most active showing an IC (50) = 1.6 microg/mL. From this extract, a new dibenzylbutane lignan, threo-4,4'-dihydroxy-3-methoxylignan ( 1) named pycnantolol, together with the known lignans (-)-dihydroguaiaretic acid ( 2), heliobuphthalmin ( 3), talaumidin ( 4), hinokinin ( 5), the labdane-type diterpene ozic acid ( 6), and the steroids stigmast-4-en-6beta-ol-3-one ( 7), beta-sitosterol ( 8) and stigmasterol ( 9) were isolated. Their structures were established on the basis of physical and spectroscopic methods, including 2 D NMR experiments (COSY, HMQC, HMBC and NOESY). The antimalarial activity of compounds 1 - 7 was evaluated against 3D7 and Dd2 P. falciparum strains. Despite the significant activity displayed by the crude CH (2)Cl (2) extract, the isolated compounds showed weaker antiplasmodial activity. The lowest IC (50) value was obtained for talaumidin ( 4) (IC (50) = 20.7 microg/mL against the Dd2-chloroquine resistant P. falciparum strain).
对安哥拉锥花茎皮的二氯甲烷、甲醇和乙醇水提取物进行了体外抗恶性疟原虫3D7株活性评估。二氯甲烷提取物活性最强，IC50 = 1.6μg/mL。从该提取物中分离出一种新的二苄基丁烷木脂素，即苏式-4,4'-二羟基-3-甲氧基木脂素（1），命名为锥花醇，同时还分离出了已知的木脂素（-）-二氢愈创木酸（2）、日光补骨脂素（3）、他劳米定（4）、日桧素（5）、拉丹烷型二萜奥齐酸（6）以及甾体化合物豆甾-4-烯-6β-醇-3-酮（7）、β-谷甾醇（8）和豆甾醇（9）。通过包括二维核磁共振实验（COSY、HMQC、HMBC和NOESY）在内的物理和光谱方法确定了它们的结构。评估了化合物1 - 7对恶性疟原虫3D7和Dd2株的抗疟活性。尽管粗二氯甲烷提取物显示出显著活性，但分离出的化合物显示出较弱的抗疟原虫活性。他劳米定（4）获得了最低的IC50值（对Dd2氯喹耐药恶性疟原虫株的IC50 = 20.7μg/mL）。
