Influence of N-Alkynylaminosteroids on Mitochondrial Functioning and Autophagy in Glioma Cells

IF 0.6 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Biochemistry (Moscow), Supplement Series B: Biomedical Chemistry Pub Date : 2022-08-15 DOI:10.1134/S199075082203009X
J. U. Panada, V. A. Klopava, T. A. Kulahava, Y. V. Faletrov, N. S. Frolova, S. V. Koran, E. G. Fomina, V. M. Shkumatov
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引用次数: 1

Abstract

The effect of the synthesized N-alkynyl-17-aminosteroids and N-alkynyl-20-aminosteroids (based on dehydroepiandrosterone and pregnenolone, respectively) on C6 rat glioma cell functions has been investigated. At 10 μM, the compounds had an insignificant effect on C6 glioma mitochondrial membrane potential, but increased cell autophagy by 70–90%; this effect was comparable to the known autophagy inducer dexamethasone. Docking simulations predict a potential high-affinity interaction between N-alkynylaminosteroids and Keap1 and the Hedgehog pathway protein, Smoothened, which are involved in autophagy regulation. The possible mechanisms of observed processes are discussed.

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n -炔酰氨基类固醇对胶质瘤细胞线粒体功能和自噬的影响
摘要:本文研究了合成的n -炔基17-氨基类固醇和n -炔基20-氨基类固醇(分别以脱氢表雄酮和孕烯醇酮为基础)对C6大鼠胶质瘤细胞功能的影响。在10 μM时,化合物对C6胶质瘤线粒体膜电位影响不显著,但使细胞自噬增加70-90%;这种效果与已知的自噬诱导剂地塞米松相当。对接模拟预测了n -炔酰氨基类固醇与Keap1和Hedgehog通路蛋白Smoothened之间潜在的高亲和相互作用,它们参与自噬调节。讨论了观测过程的可能机制。
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期刊介绍: Biochemistry (Moscow), Supplement Series B: Biomedical Chemistry   covers all major aspects of biomedical chemistry and related areas, including proteomics and molecular biology of (patho)physiological processes, biochemistry, neurochemistry, immunochemistry and clinical chemistry, bioinformatics, gene therapy, drug design and delivery, biochemical pharmacology, introduction and advertisement of new (biochemical) methods into experimental and clinical medicine. The journal also publishes review articles. All issues of the journal usually contain solicited reviews.
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