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首页> 外文期刊>Dhaka University Journal of Pharmaceutical Sciences >Cycloartane and Stigmastane Type Triterpenoids from Pothos scandens Inhibit Estradiol (E2) Induced Proliferations in Breast Cancer Cells
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Cycloartane and Stigmastane Type Triterpenoids from Pothos scandens Inhibit Estradiol (E2) Induced Proliferations in Breast Cancer Cells

机译:来自Pothos scandens的环烷和柱头类三萜类化合物抑制雌二醇(E2)诱导的乳腺癌细胞增殖。

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摘要

Four cycloartane type triterpenoids and three stigmastane type steroids were isolated from the methanolic extract of stem and root part of Pothos scandens L. (Araceae), a Bangladeshi medicinal plant by high performance liquid chromatographic technique. The compounds were characterized as 24-methylenecycloartanol (1), 24-methylenecycloartenone (2), 24-en-cycloartenone (3), 24-methylenecycloartanyl ferulate (4), stigmast-4-en-3-one (5), stigmast-4,22-diene-3-one (6) and β-sitosterol glucoside (7) through extensive 1D and 2D NMR spectroscopic studies. All the isolates were evaluated for their estrogenic/antiestrogenic activity using the estrogen-responsive breast cancer cell lines, MCF-7 and T47D. The results showed that all the compounds possess mild to strong antiestrogenic activity in both cell lines which was compared to positive control tamoxifen. 24- Methylenecycloartanol (1), which contains a hydroxyl group in its C-3 position, inhibited 90% of estradiol (E2)- induced cell proliferation in MCF-7 and T47D cell lines at a concentration of 0.01 μM only. 24- Methylenecycloartanyl ferulate (4) and stigmast-4,22-diene-3-one (6) showed 90% of estradiol (E2)-induced cell proliferation in T47D cell only at a concentration of 0.01 μM whereas 10.0 μM was required for 24- methylenecycloartanyl ferulate (4) for the same activity in MCF-7 cells. This is the first report of isolation of these compounds from the plant along with their antiestrogenic property.
机译:通过高效液相色谱法从孟加拉国药用植物Pothos scandens L.(Araceae)的茎和根部分的甲醇提取物中分离出了四种环戊烷型三萜类化合物和三种柱头甾类类固醇。这些化合物的特征为24-亚甲基环烷醇(1),24-亚甲基环戊烯酮(2),24-环-环戊烯酮(3),阿魏酸24-亚甲基环戊基酯(4),柱头4-en-3-one(5),柱头通过广泛的1D和2D NMR光谱研究了-4,22-二烯-3-酮(6)和β-谷甾醇葡萄糖苷(7)。使用雌激素反应性乳腺癌细胞系MCF-7和T47D评估所有分离物的雌激素/抗雌激素活性。结果表明,与阳性对照他莫昔芬相比,所有化合物在两种细胞系中均具有中等至强的抗雌激素活性。仅在0.01μM的浓度下,在其C-3位置含有羟基的24-亚甲基环戊醇(1)抑制了雌二醇(E2)诱导的MCF-7和T47D细胞系中细胞增殖的90%。 24-亚甲基环戊烷阿魏酸酯(4)和柱头-4,22-二烯-3-酮(6)仅在0.01μM的浓度下显示90%的雌二醇(E2)诱导的T47D细胞增殖,而10.0μM的浓度在MCF-7细胞中具有相同活性的24-亚甲基环戊基阿魏酸酯(4)。这是从植物中分离这些化合物及其抗雌激素特性的首次报道。

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