Selective anticancer activity of pure licamichauxiioic-B acid in cultured cell lines

Selective anticancer activity of pure licamichauxiioic-B acid in cultured cell lines
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DOI:
10.1080/13880200600592301
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发表时间:
2006-03-01
影响因子:
3.8
通讯作者:
Walker, EH
Walker, EH
中科院分区:
医学3区
文献类型:
--
作者:
Badisa, RB;Ayuk-Takem, LT;Walker, EH

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评估了来自 Licania michauxii Prance (LMP) 植物的茎和根部分的粗提物和纯 licamichauxiioic-B 化合物对丰年虾幼虫和细胞培养物的细胞毒活性。在体内虾测定中,粗提物和纯化化合物均具有活性,ED50 值分别为 122.5 和 32.1 μg/ml。当在四种人类癌细胞系(即 CL-187(结肠腺癌)、MCF-7(激素依赖性乳腺癌)、MDA-MB-231(激素非依赖性乳腺癌)和 CRL-2547(胰腺癌))中进行测试时,纯化合物表现出比粗提取物高 1.5 至约 3 倍的细胞毒活性。在所有癌细胞系中,粗提物的LD50值范围为33.8+/-0.9至88.1+/-3.6μg/ml,而纯化合物的LD50值范围为21.6+/-1.2至31.8+/-4.2μg/ml。在非癌性正常小鼠脂肪乳晕(CCL-1 NCTC 克隆 929)细胞系中,发现纯化合物的 LD50 值大于 100 μg/ml。细胞培养物的细胞毒性结果的比较表明,纯licamichauxiioic-B化合物在非癌细胞系中相对无活性。在所有测试的癌细胞系中,纯 licamichiioic-B 化合物的选择性指数大于 3.14。
The cytotoxic activities of crude extract and pure licamichauxiioic-B compound from stem and root parts of Licania michauxii Prance (LMP) plant were evaluated against brine shrimp larvae and cell cultures. Under in vivo shrimp assay, both crude extract and the purified compound were active with ED50 values of 122.5 and 32.1 mu g/ml, respectively. When tested in four human cancer cell lines, namely, CL-187 (colon adenocarcinoma), MCF-7 (hormone-dependent breast carcinoma), MDA-MB-231 (hormone-independent breast carcinoma), and CRL-2547 (pancreatic carcinoma), the pure compound exhibited 1.5- to about 3-times greater cytotoxic activity than the crude extract. In all cancer cell lines, the LD50 values of crude extract ranged from 33.8 +/- 0.9 to 88.1 +/- 3.6 mu g/ml, while with pure compound the values ranged from 21.6 +/- 1.2 to 31.8 +/- 4.2 mu g/ml. In a noncancerous normal mouse adipose areolar (CCL-1 NCTC clone 929) cell line, the pure compound was found to have an LD50 value greater than 100 mu g/ml. Comparison of cytotoxic results of cell cultures revealed that the pure licamichauxiioic-B compound was relatively inactive in noncancerous cell line. The selectivity index for the pure licamichauxiioic-B compound is greater than 3.14 in all cancer cell lines tested.