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桦木醇新型乙炔衍生物对G-361人黑色素瘤细胞的抗增殖活性

ANTIPROLIFERATIVE ACTIVITY OF NOVEL ACETYLENIC DERIVATIVES OF BETULIN AGAINST G-361 HUMAN MELANOMA CELLS.

作者信息

Bębenek Ewa, Chodurek Ewa, Orchel Arkadiusz, Dzierżewicz Zofia, Boryczka Stanisław

出版信息

Acta Pol Pharm. 2015 Jul-Aug;72(4):699-703.

Abstract

Acetylenic derivatives of betulin were tested in vitro for their antiproliferative activity against G-361 human melanoma cells. Two types of betulin derivatives were studied: monoesters, obtained by modification of the hydroxyl group at C-28 position, and diesters modified at both C-28 and C-3 positions. To assess cell proliferation, a colorimetric sulforhodamine B based method was used. All the tested monoesters inhibited cellular growth and 28-O-propynoylbetulin showed the strongest cytotoxic effect. Esterification of the C-3 hydroxyl group of the molecule abolished its growth inhibitory activity.

摘要

对桦木醇的乙炔衍生物进行了体外测试,以研究其对G - 361人黑色素瘤细胞的抗增殖活性。研究了两种类型的桦木醇衍生物:通过修饰C - 28位羟基得到的单酯,以及在C - 28和C - 3位均有修饰的二酯。为评估细胞增殖,采用了基于比色法的磺酰罗丹明B法。所有测试的单酯均抑制细胞生长,其中28 - O - 丙炔酰桦木醇表现出最强的细胞毒性作用。分子中C - 3羟基的酯化消除了其生长抑制活性。

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