阿尔瓦拉多因E-N，来自海地阿尔瓦拉多树树叶的抗肿瘤和细胞毒性蒽酮碳苷。
Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis.
作者信息
Phifer Sharnelle S, Lee Dongho, Seo Eun-Kyoung, Kim Nam-Cheol, Graf Tyler N, Kroll David J, Navarro Hernan A, Izydore Robert A, Jiménez Francisco, Garcia Ricardo, Rose William C, Fairchild Craig R, Wild Robert, Soejarto Djaja D, Farnsworth Norman R, Kinghorn A Douglas, Oberlies Nicholas H, Wall Monroe E, Wani Mansukh C
机构信息
Natural Products Laboratory, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA.
出版信息
J Nat Prod. 2007 Jun;70(6):954-61. doi: 10.1021/np070005a. Epub 2007 Jun 7.
Bioactivity-directed fractionation of an extract of the leaves of Alvaradoa haitiensis, using the KB (human oral epidermoid carcinoma) cell line, led to the isolation and identification of 10 new anthracenone C-glycosides, alvaradoins E-N (1-10), along with the known compound chrysophanol (11). The cytotoxicity of all compounds was evaluated, and preliminary structure-activity relationships are suggested. The most potent compounds in the in vitro assays (1 and 2) were evaluated in vivo versus the P388 (murine lymphocytic leukemia) model, and alvaradoin E (1) showed antileukemic activity (125% T/C) at a dose of 0.2 mg kg-1 per injection when administered intraperitoneally.
采用KB（人口腔表皮样癌）细胞系对海地阿尔瓦拉多树树叶提取物进行生物活性导向分级分离，导致10种新的蒽酮碳苷，阿尔瓦拉多因E-N（1-10）以及已知化合物大黄酚（11）的分离和鉴定。评估了所有化合物的细胞毒性，并提出了初步的构效关系。在体外试验中最具活性的化合物（1和2）在体内针对P388（小鼠淋巴细胞白血病）模型进行了评估，腹腔注射时，阿尔瓦拉多因E（1）以0.2mg kg-1的剂量显示出抗白血病活性（T/C为125%）。
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