5'-Noraristeromycin Repurposing：知名的 S-腺苷-L-高半胱氨酸水解酶抑制剂作为抗白血病的潜在药物。

IF 2 4区生物学 Q4 CELL BIOLOGY

Acta Naturae Pub Date : 2024-07-01 DOI:10.32607/actanaturae.27443

O N Novikova, E S Matyugina, A V Gorshenin, Yu I Velikorodnaya, M D Krengauz, V O Vedernikova, P V Spirin, V S Prassolov, S N Kochetkov, A L Khandazhinskaya

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引用次数: 0

摘要

研究发现，5'-去甲紫霉素对映体的外消旋混合物对白血病细胞具有明显的细胞毒性作用；Jurkat、K562 和 THP-1 细胞系的 IC50 分别为 7.3、1.3 和 3.7 μM。在对白鼠进行的单剂量胃内给药实验中，研究了 5'-noraristeromycin 的一般毒性；确定了毒性计量参数，并研究了急性中毒的临床和病理表现。结果表明，该物质的半数致死剂量为 63.2 (52.7÷75.8) 毫克/千克；半数致死剂量为 44.7 毫克/千克，半数致死剂量为 89.4 毫克/千克。以研究剂量范围内的剂量服用该物质，会对实验动物的内脏和组织造成全身性损害。

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5'-Noraristeromycin Repurposing: Well-known S-Adenosyl-L-homocysteine Hydrolase Inhibitor As a Potential Drug Against Leukemia.

5'-Noraristeromycin as a racemic mixture of enantiomers was found to exhibit a pronounced cytotoxic effect on leukemia cells; IC₅₀ for the Jurkat, K562, and THP-1 cell lines was 7.3, 1.3, and 3.7 μM, respectively. The general toxicity of 5'-noraristeromycin was studied in experiments on white mice upon single-dose intragastric administration; toxicometric parameters were determined, and the clinical and pathomorphological presentation of acute intoxication was studied. LD₅₀ of the substance was shown to be 63.2 (52.7÷75.8) mg/kg; LD16, 44.7 mg/kg, and LD84, 89.4 mg/kg. Administration of the substance at a dose within the studied dose range is accompanied by systemic damage to the internal organs and tissues of the experimental animals.

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来源期刊

Acta Naturae 农林科学-林学

CiteScore

3.50

自引率

5.00%

发文量

审稿时长

>12 weeks

期刊介绍： Acta Naturae is an international journal on life sciences based in Moscow, Russia. Our goal is to present scientific work and discovery in molecular biology, biochemistry, biomedical disciplines and biotechnology. These fields represent the most important priorities for the research and engineering development both in Russia and worldwide. Acta Naturae is also a periodical for those who are curious in various aspects of biotechnological business, innovations in pharmaceutical areas, intellectual property protection and social consequences of scientific progress. The journal publishes analytical industrial surveys focused on the development of different spheres of modern life science and technology. Being a radically new and totally unique journal in Russia, Acta Naturae is useful to both representatives of fundamental research and experts in applied sciences.