环 A 修饰的 11-酮-β-乳香酸衍生物的合成及抗肿瘤活性。
Synthesis and antitumor activity of ring A modified 11-keto-β-boswellic acid derivatives.
机构信息
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D-06120 Halle (Saale), Germany.
Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str.2, D-06120 Halle (Saale), Germany.
出版信息
Eur J Med Chem. 2015 Mar 6;92:700-11. doi: 10.1016/j.ejmech.2015.01.039. Epub 2015 Jan 20.
Beta-boswellic acids are interesting triterpenoic acids that show different biological activities. Their cytotoxic potential, as well as that of their derivates remained unexploited so far. In this study we were able to prepare derivatives of 11-keto-β-boswellic acid that showed lower IC50 values as determined by a sulphorhodamine B (SRB) assay using several different human tumour cell lines. Thus, the introduction of an amino group at position C-2 led to a significantly improved cytotoxic activity of amine 18. An apoptotic effect of compound 18 was determined using DNA laddering and trypan blue staining experiments.
β-乳香酸是一类具有多种生物活性的三萜酸，其细胞毒性及其衍生物的细胞毒性至今尚未得到充分开发。在本研究中，我们通过使用几种不同的人肿瘤细胞系进行磺基罗丹明 B（SRB）测定，成功制备了 11-酮-β-乳香酸的衍生物，其 IC50 值较低。因此，在 C-2 位引入氨基会显著提高化合物 18 的细胞毒性。通过 DNA 梯状电泳和台盼蓝染色实验确定了化合物 18 的凋亡作用。
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