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新型含天然氨基酸的 25-羟基原人参二醇类似物的合成及抗肿瘤活性评价。

Synthesis and anti-tumor evaluation of novel 25-hydroxyprotopanaxadiol analogs incorporating natural amino acids.

机构信息

School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

出版信息

Steroids. 2013 Feb;78(2):203-9. doi: 10.1016/j.steroids.2012.09.012. Epub 2012 Nov 22.

Abstract

In the current study, derivatives of 25-hydroxyprotopanaxadiol (25-OH-PPD) were prepared and their in vitro anti-tumor activities were tested on six different human tumor cell lines by standard MTT assay. The results showed that combining an ester group combined with the presence of an amino acid moiety led to a 10-fold improved anti-tumor activity. Compound 1c exhibited the best anti-tumor activity in the in vitro assays. Compounds 2c, 3c, 4c, 5c, 6c and 8b showed better anti-tumor activities compared to the parent compound 25-OH-PPD. The current results may provide useful data for researching and developing new anti-cancer agents.

摘要

在本研究中,制备了 25-羟基原人参二醇(25-OH-PPD)的衍生物,并通过标准 MTT 测定法在六种不同的人肿瘤细胞系上测试了它们的体外抗肿瘤活性。结果表明,酯基与氨基酸部分的结合导致抗肿瘤活性提高了 10 倍。化合物 1c 在体外试验中表现出最好的抗肿瘤活性。与母体化合物 25-OH-PPD 相比,化合物 2c、3c、4c、5c、6c 和 8b 显示出更好的抗肿瘤活性。目前的结果可能为研究和开发新型抗癌药物提供有用的数据。

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