Sesquiterpene lactones isolated from Elephantopus scaber L. inhibits human lymphocyte proliferation and the growth of tumour cell lines and induces apoptosis in vitro.
Sesquiterpene lactones isolated from Elephantopus scaber L. inhibits human lymphocyte proliferation and the growth of tumour cell lines and induces apoptosis in vitro.
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DOI：
10.1155/2012/721285
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发表时间：
2012
影响因子：
--
通讯作者：
Remani P
中科院分区：
文献类型：
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作者：
Geetha BS;Nair MS;Latha PG;Remani P
本研究旨在分离南印度象皮细胞毒作用的化合物，并进一步研究其对静止和增殖细胞的影响。从南印度象粗糙皮氯仿提取物中分离得到已知的倍半萜内酯、脱氧象托品和异脱氧象托品，其结构经波谱方法确定。细胞活力测定显示，这些化合物对培养72 h的L-92 9肿瘤细胞(IC50值分别为2.7 μg/m L和3.3 μg/m L)有剂量依赖性的抑制作用。这两个化合物都选择性地作用于静止的和PHA刺激的增殖的人淋巴细胞，并抑制氚胸苷掺入DLA肿瘤细胞的DNA。浓度为3 μg/m L的复方脱氧大象托品诱导的细胞凋亡率最高。它在体内对DLA肿瘤细胞也显示出显著的抗肿瘤效果。结果表明，脱氧象托品和异去氧象托品的抗增殖作用可用于治疗具有广泛增殖潜能的肿瘤。
This study was designed to isolate the compounds responsible for the cytotoxic properties of South Indian Elephantopus scaber L. and further investigate their effects on quiescent and proliferating cells. Bioassay-guided isolation of the whole plant of chloroform extract of South Indian Elephantopus scaber afforded the known sesquiterpene lactone, deoxyelephantopin, and isodeoxyelephantopin whose structures were determined by spectroscopic methods. These compounds caused a dose dependent reduction in the viability of L-929 tumour cells in 72 h culture (IC50 value of 2.7 μg/mL and 3.3 μg/mL) by the cell viability assay. Both the compounds act selectively on quiescent and PHA-stimulated proliferating human lymphocytes and inhibited tritiated thymidine incorporation into cellular DNA of DLA tumour cells. The compound deoxyelephantopin at a concentration of 3 μg/mL caused maximum apoptotic cells. It also exhibited significant in vivo antitumour efficacy against DLA tumour cells. The results, therefore, indicate that the antiproliferative property of deoxyelephantopin and isodeoxyelephantopin could be used in regimens for treating tumors with extensive proliferative potencies.