Effect of brassinosteroid esters with salicylic, succinic, and indolylacetic acids on the tumor cell growth

Alesia V. Panibrat, Alina R. Tryfanava, A. Savachka, R. Litvinovskaya, N. M. Chashchina, Corresponding Member, Vladimir N. Zhabinskii Academician, V. Khripach, О. В. Панибрат, А. Р. Трифонова, О. П. Савочка, Р. П. Литвиновская, Н. М. Чащина, Владимир Николаевич Жабинский, В. А. Хрипач
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Abstract

The aim of this work is to study the effect of new derivatives of brassinosteroids – their esters with salicylic, succinic, and indolylacetic acids on the growth of tumor cells, on their distribution by cell cycle phases and determination of the type of cell death. It was shown that the activity of the new synthesized compounds differed significantly depending on the substitution nature in the steroid nucleus, amounting to <10 µM in the case of epibrassinolide and epicastasterone salicylates, simultaneously causing the cycle arrest in the G0/G1 phase, a mitochondrial potential decrease, and apoptosis of tumor cells. The results obtained indicate the high activity of salicylates, which effectively suppress the growth of the all studied types of tumors, and the prospects of finding new antitumor agents in this series of compounds.
含水杨酸、琥珀酸和吲哚乙酸的类固醇酯对肿瘤细胞生长的影响
这项工作的目的是研究黄铜类固醇的新衍生物--它们与水杨酸、琥珀酸和吲哚乙酸的酯类--对肿瘤细胞生长、细胞周期阶段分布和细胞死亡类型的影响。结果表明,新合成化合物的活性因甾体核中的取代性质不同而有显著差异,表巴西内酯和表司他酮水杨酸酯的活性小于 10 µM,同时导致肿瘤细胞周期停滞在 G0/G1 期、线粒体电位降低和凋亡。研究结果表明,水杨酸盐具有很高的活性,能有效抑制所有研究类型肿瘤的生长,并有望在这一系列化合物中发现新的抗肿瘤药物。
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