Cuca Luis Enrique, Coy Ericsson David, Alarcón Marlén Andrea, Fernández Andrés, Aristizábal Fabio Ancízar
Laboratorio de Investigación en Productos Naturales Vegetales, Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá, D.C., Colombia.
Biomedica. 2011 Jul-Sep;31(3):335-43. doi: 10.1590/S0120-41572011000300006.
The antiproliferative effect of eleven neolignans, two lignans and one diterpene isolated from three Lauraceae plants, four benzofurans and two bicyclooctanes synthetic derivatives was evaluated in vitro on a set of five human cancer cells from solid tumors with a high incidence in Colombia.
To evaluate the cytotoxic effect of twenty compounds on the tumor cell lines HeLa, A-549, Hep-2, PC-3, and MCF-7. MATERIALS AND METHODS. Fourteen natural compounds were isolated by chromatographic techniques from three native Colombian plants (Pleurothyrium cinereum, Ocotea macrophylla and Nectandra amazonum), whose structures were established by spectroscopic methods; six synthetic derivatives were prepared by oxyarylation and diazomethane methylation. Antiproliferative effect and cell recovery were performed by means of in vitro treatment of tumor cell lines with test compounds, evaluating cell viability by resazurin staining.
Among test compounds, only neolignans ocophyllal A, cinerin D, kaurenoic acid, two benzofuran-derivatives, and synthetic (-)-cinerin A were found to have antiproliferative effect at different levels. Bicyclooctanoids as well as kaurenoic acid exhibited activity against all human cancer cells while benzofuranoids showed selective activity against HeLa. Furthermore, compounds (-)-cinerin A and kaurenoic acid exhibited total lethal effect against all-five cell lines and PC-3, Hep-2, and A549 cell lines, respectively.
Test compounds exhibiting antiproliferative activity showed interesting results, which would promote their use as lead compounds on further studies for anticancer agents development.
从三种樟科植物中分离出的11种新木脂素、2种木脂素和1种二萜，以及4种苯并呋喃和2种双环辛烷合成衍生物的抗增殖作用，在体外对一组来自哥伦比亚高发实体瘤的5种人类癌细胞进行了评估。
评估20种化合物对肿瘤细胞系HeLa、A-549、Hep-2、PC-3和MCF-7的细胞毒性作用。材料与方法。通过色谱技术从三种哥伦比亚本土植物（灰叶苞被木、大叶楠和亚马逊新樟）中分离出14种天然化合物，其结构通过光谱方法确定；通过氧芳基化和重氮甲烷甲基化制备了6种合成衍生物。通过用测试化合物体外处理肿瘤细胞系来进行抗增殖作用和细胞恢复实验，通过刃天青染色评估细胞活力。
在测试化合物中，仅发现新木脂素奥科菲拉尔A、灰绿脂素D、贝壳杉烯酸、两种苯并呋喃衍生物和合成的（-）-灰绿脂素A在不同水平上具有抗增殖作用。双环辛烷类化合物以及贝壳杉烯酸对所有人类癌细胞均表现出活性，而苯并呋喃类化合物对HeLa表现出选择性活性。此外，化合物（-）-灰绿脂素A和贝壳杉烯酸分别对所有五种细胞系以及PC-3、Hep-2和A549细胞系表现出完全致死作用。
表现出抗增殖活性的测试化合物显示出有趣的结果，这将促进它们在进一步开发抗癌药物的研究中用作先导化合物。
