M. E. Uspenskaya, T. A. Fedotcheva, A. N. Usenko, N. L. Shimanovsky
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引用次数: 0
摘要
类固醇激素 5-雄烯二醇(5-AED)被认为是一种可能的电离辐射防护对策。它在电离辐射照射前后都非常有效,而且安全、耐受性良好。5-AED 可提高骨髓细胞祖细胞的存活率以及循环中性粒细胞和血小板的数量,从而防止辐射引起的造血功能抑制。5-AED 的辐射防护功效基于通过激活 NF-кB 通路刺激 G-CSF 合成、抑制热凋亡和细胞凋亡、修复辐射诱导的 DNA 损伤以及增加诱导性 NO 合成酶基因的表达。开发新的合成 5-AED 衍生物有助于提高其生物利用度,并使 5-AED 成为开发新型安全有效的辐射防护药物的前瞻性分子。
The Prospects of 5-Androstenediol and its Synthetic Derivatives as Novel Radioprotective Drugs
The steroid hormone 5-androstenediol (5-AED) has been advanced as a possible countermeasure for protection from ionizing radiation. It is highly effective both before and after exposure to ionizing radiation and is safe and well-tolerated. 5-AED prevents radiation-induced suppression of hematopoiesis by increasing the survival of bone-marrow cell progenitors and the numbers of circulating neutrophils and platelets. The radioprotective effectiveness of 5-AED is based on stimulation of G-CSF synthesis through NF-кB pathway activation, inhibition of pyroptosis and apoptosis, repair of radiation-induced DNAdamage, and increased expression of inducible NO-synthase genes. Development of new synthetic 5-AED derivatives helps to enhance its bioavailability and makes 5-AED a prospective molecule for creating novel safe and effective radioprotective drugs.
期刊介绍:
Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including:
methods of synthesis;
results of pharmacological, toxicological, and biochemical studies;
investigation of structure - activity relationships in prediction of new compounds;
methods and technical facilities used; and
problems associated with the development of ecologically safe and economically feasible methods of industrial production.
In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world.
Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April.
All articles are peer-reviewed.