Esters of betulin and betulinic acid with amino acids have improved water solubility and are selectively cytotoxic toward cancer cells

被引：123

作者：

Drag-Zalesinska, Malgorzata ^{[1
]}

Kulbacka, Julita ^{[1
]}

Saczko, Jolanta ^{[1
]}

Wysocka, Teresa ^{[1
]}

Zabel, Maciej ^{[1
,2
]}

Surowiak, Pawel ^{[1
,3
]}

Drag, Marcin ^{[4
]}

机构：

[1] Univ Sch Med, PL-50356 Wroclaw, Poland

[2] Med Univ Poznan, Dept Histol & Embryol, Poznan, Poland

[3] Lower Silesian Oncol Ctr, PL-53413 Wroclaw, Poland

[4] Wroclaw Univ Technol, Fac Chem, Div Med Chem & Microbiol, PL-50370 Wroclaw, Poland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Betulin; Betulinic acid; Cytotoxicity; Apoptosis; HUMAN-MELANOMA; DRUG-RESISTANT; LINES; DERIVATIVES;

D O I：

10.1016/j.bmcl.2009.06.046

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Betulin and betulinic acid are naturally occurring pentacyclic triterpenes showing cytotoxicity towards a number of cancer cell lines. Unfortunately they are practically insoluble in aqueous media and therefore their overall absorption index is not satisfactory. We have modified structures of both compounds by simple transformation to mono-and disubstituted esters of L-amino acids. This allowed us to achieve better water solubility without loss of the observed earlier anticancer properties. Comet assay on various cancer cell lines demonstrate that these compounds act via an apoptotic mechanism. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4814 / 4817

页数：4

共 13 条

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