环己基二胺部分的存在赋予五环三萜类化合物细胞毒性。
The Presence of a Cyclohexyldiamine Moiety Confers Cytotoxicity to Pentacyclic Triterpenoids.
机构信息
Organic Chemistry, Martin-Luther University Halle-Wittenberg, Kurt-Mothes, Str. 2, D-06120 Halle (Saale), Germany.
Institute of Precision Medicine, Medical and Life Science Faculty, Furtwangen University, Jakob-Kienzle-Str. 17, D-78054 Villigen-Schwenningen, Germany.
出版信息
Molecules. 2021 Apr 6;26(7):2102. doi: 10.3390/molecules26072102.
Pentacyclic triterpenoids oleanolic acid, ursolic acid, betulinic acid, and platanic acid were acetylated and converted into several amides -; the cytotoxicity of which has been determined in sulforhodamine B assays employing seral human tumor cell lines and nonmalignant fibroblasts. Thereby, a betulinic acid/-1,4-cyclohexyldiamine amide showed excellent cytotoxicity (for example, EC = 0.6 μM for HT29 colon adenocarcinoma cells).
五环三萜齐墩果酸、熊果酸、白桦酸和角鲨烷被乙酰化，并转化为几种酰胺 - ；采用一系列人肿瘤细胞系和非恶性成纤维细胞，用磺酰罗丹明 B 测定法测定了它们的细胞毒性。由此，白桦酸/1,4-环己二胺酰胺表现出优异的细胞毒性（例如，对 HT29 结肠腺癌细胞的 EC = 0.6 μM）。
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