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Studies on Cytotoxic Constituents from the Leaves of Elaeagnus oldhamii Maxim. in Non-Small Cell Lung Cancer A549 Cells

机译:沙枣(Elaeagnus oldhamii Maxim)叶片中细胞毒性成分的研究。非小细胞肺癌A549细胞中的表达

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Elaeagnus oldhamii Maxim. is a commonly used traditional herbal medicine. In Taiwan the leaves of E. oldhamii Maxim. are mainly used for treating lung disorders. Twenty five compounds were isolated from the leaves of E. oldhamii Maxim. in the present study. These included oleanolic acid (1), 3-O-(Z)-coumaroyl oleanolic acid (2), 3-O-(E)-coumaroyl oleanolic acid (3), 3-O-caffeoyl oleanolic acid (4), ursolic acid (5), 3-O-(Z)-coumaroyl ursolic acid (6), 3-O-(E)-coumaroyl ursolic acid (7), 3-O-caffeoyl ursolic acid (8), 3β, 13β-dihydroxyolean-11-en-28-oic acid (9), 3β, 13β-dihydroxyurs-11-en-28-oic acid (10), uvaol (11), betulin (12), lupeol (13), kaempferol (14), aromadendrin (15), epigallocatechin (16), cis-tiliroside (17), trans-tiliroside (18), isoamericanol B (19), trans-p-coumaric acid (20), protocatechuic acid (21), salicylic acid (22), trans-ferulic acid (23), syringic acid (24) and 3-O-methylgallic acid (25). Of the 25 isolated compounds, 21 compounds were identified for the first time in E. oldhamii Maxim. These included compounds 1, 4, 5 and 8–25. These 25 compounds were evaluated for their inhibitory activity against the growth of non-small cell lung cancer A549 cells by the MTT assay, and the corresponding structure-activity relationships were discussed. Among these 25 compounds, compound 6 displayed the best activity against the A549 cell line in vitro (CC50 = 8.56 ± 0.57 μg/mL, at 48 h of MTT asssay). Furthermore, compound 2, 4, 8 and 18 exhibited in vitro cytotoxicity against the A549 cell line with the CC50 values of less than 20 μg/mL at 48 h of MTT asssay. These five compounds 2, 4, 6, 8 and 18 exhibited better cytotoxic activity compared with cisplatin (positive control, CC50 value of 14.87 ± 1.94 μg/mL, at 48 h of MTT asssay). The result suggested that the five compounds might be responsible for its clinical anti-lung cancer effect.
机译:Elaeagnus oldhamii Maxim。是一种常用的传统草药。在台湾,E。oldhamii Maxim的叶子。主要用于治疗肺部疾病。从E.oldhamii Maxim的叶子中分离出二十五种化合物。在目前的研究中。这些包括齐墩果酸(1),3-O-(Z)-香豆酰齐墩果酸(2),3-O-(E)-香豆酰齐墩果酸(3),3-O-咖啡酰齐墩果酸(4),熊果酚酸(5),3-O-(Z)-香豆酰熊果酸(6),3-O-(E)-香豆酰熊果酸(7),3-O-咖啡酰熊果酸(8),3β,13β- dihydroxyolean-11-en-28-oic acid(9),3β,13β-dihydroxyurs-11-en-28-oicacid(10),uvaol(11),betulin(12),lupeol(13),kaempferol(14) ),芳香醛(15),表没食子儿茶素(16),顺式-tiliroside(17),反-tiliroside(18),异十八烷醇B(19),反-对香豆酸(20),原儿茶酸(21),水杨酸(22),反式阿魏酸(23),丁香酸(24)和3-O-甲基没食子酸(25)。在25种分离出的化合物中,首次在E. oldhamii Maxim中鉴定出21种化合物。其中包括化合物1、4、5和8-25。通过MTT法评估了这25种化合物对非小细胞肺癌A549细胞生长的抑制活性,并讨论了其相应的构效关系。在这25种化合物中,化合物6在体外对A549细胞系表现出最佳的活性(MTT分析48 h,CC 50 = 8.56±0.57μg/ mL)。此外,化合物2、4、8和18对A549细胞系表现出体外细胞毒性,MTT分析48 h时CC 50 值小于20μg/ mL。与顺铂相比,这五个化合物2、4、6、8和18表现出更好的细胞毒性活性(阳性对照,MTT分析48 h时CC 50 值为14.87±1.94μg/ mL)。结果表明这五种化合物可能是其临床抗肺癌作用的原因。

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