Lignans from Dysosma versipellis with inhibitory effects on prostate cancer cell lines
Lignans from Dysosma versipellis with inhibitory effects on prostate cancer cell lines
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DOI：
10.1021/np060430o
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发表时间：
2007-02-01
影响因子：
5.1
通讯作者：
But, Paul Pui-Hay
中科院分区：
文献类型：
--
作者：
Jiang, Ren-Wang;Zhou, Jin-Rong;But, Paul Pui-Hay
一种新的单环氧木脂素地苦参醇 (1)，以及八种已知化合物：鬼臼毒素 (2)、4'-去甲基鬼臼毒素 (3)、脱氧鬼臼毒素 (4)、4'-去甲基脱氧鬼臼毒素 (5)、二茶素 (6)、山柰酚、槲皮素和 β-谷甾醇， 是从八角莲的根中分离出来的。通过光谱方法阐明了1的结构。 Aryltetralin 木脂素 2-4 对雄激素敏感 (LNCaP) 和雄激素非依赖性 (PC-3) 人前列腺癌细胞系的生长表现出最有效的抑制活性，IC50 值分别在 0.030-0.056 和 0.032-0.082 muM 范围内。定量 HPLC 分析显示，化合物 2 在植物中的浓度最高 (37.21 mg/g)，其次是化合物 4 (5.01 mg/g) 和化合物 3 (2.75 mg/g)。此外，与木酚素的商业来源鬼臼草的根茎和根相比，D. versipellis 根含有相似含量的化合物 2。因此，在合适的地点培养 D. versipellis 可以作为鬼臼毒素 (2) 生产的替代来源。
A new monoepoxylignan, dysosmarol (1), along with eight known compounds, podophyllotoxin (2), 4'-demethylpodophyllotoxin (3), deoxypodophyllotoxin (4), 4'-demethyldeoxypodophyllotoxin (5), diphyllin (6), kaempferol, quercetin, and beta-sitosterol, were isolated from the roots of Dysosma versipellis. The structure of 1 was elucidated by spectroscopic methods. Aryltetralin lignans 2-4 showed the most potent inhibitory activities against the growth of androgen-sensitive (LNCaP) and androgen-independent (PC-3) human prostate cancer cell lines, with IC50 values in the ranges 0.030-0.056 and 0.032-0.082 mu M, respectively. A quantitative HPLC analysis showed that compound 2 occurred at the highest concentration in the plant (37.21 mg/g) followed by compound 4 (5.01 mg/g) and compound 3 (2.75 mg/g). Furthermore, D. versipellis roots contain a similar content of compound 2 as compared with the rhizomes and roots of Podophyllum hexandrum, a commercial source of the lignan. Thus, cultivation of D. versipellis in suitable locations may serve as an alternative source for podophyllotoxin (2) production.