放射性同位素在制药科学中的应用研究

H. Sakurai
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引用次数: 0

摘要

放射性同位素和辐射的使用在生命科学的研究中是不可或缺的,特别是在制药科学中。制药科学的研究课题主要分为以下三个研究领域。(1)生命系统和环境中的微量元素,使用多种示踪剂和中子活化分析。(2)新药物开发中的放射性同位素,其中放射免疫测定、放射受体测定、药代动力学、放射自显影、放射探针、药物输送系统和基因技术需要各种各样的放射性同位素。(3)核医学领域的放射性药物,不仅在体外和体内诊断性放射性药物,而且在体内治疗性放射性药物都得到了广泛的发展。自1971年以来,我们使用了多种示踪剂,并采用中子活化分析(NAA)方法(表1)来了解放射性防护剂的化学作用机制,微量元素和葡萄糖进入细胞和器官的摄取,动物器官中必需微量元素的状态,以及实验动物亚细胞颗粒和器官中金属的掺入,金属配合物作为未来金属药物的候选物。本文综述了我国在药学研究方面的研究进展,重点介绍了以下三个方面。(i)铜催化的混合二硫化物形成(II)与放射性保护剂半胱胺(2-巯基乙胺)的辐射防护能力有关。(ii)口服锌(ii)及其配合物对活体动物皮肤活性氧(ROS)的抑制作用与紫外线(UV)光下皮肤损伤的关系。(iii)胰岛素模拟钒基(IV) (VO(II))复合物改善糖尿病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Studies on the Usefulness of Radioisotopes in Pharmaceutical Sciences
The use of radioisotopes and radiation is indispensable in the research of life science, especially in pharmaceutical sciences. Research topics in pharmaceutical sciences are mainly classified into three research fields as follows. (1) Trace elements in living systems and environment, where many kinds of tracers and neutron activation analysis are used. (2) Radioisotopes in the development of new pharmaceutics, where a wide variety of radioisotopes are needed for radioimmunoassay, radioreceptor assay, pharmacokinetics, imaging by autoradiography, radioprobes, drug delivery systems, and gene technology. (3) Radiopharmaceutics in nuclear medicine, where not only in vitro and in vivo diagnostic radiopharmaceutics but also in vivo therapeutic radiopharmaceutics have extensively been developed. Since 1971, we have used many tracers, and performed neutron activation analysis (NAA) method (Table 1) to know the chemical action mechanism of radioprotective agents, uptake of trace elements and glucose into the cells and organs, state of essential trace elements in organs of animals, and metal incorporations in subcellular particles and organs in experimental animals that were treated with metallo-pharmaceutics as well as metal complexes as candidates for future metallo-pharmaceutics. This review article describes progress in our investigation on the research of pharmaceutical sciences, focusing on the following three topics. (i) Mixed disulfide formation catalyzed by Cu(II) in relation to the radioprotective ability of a radioprotector, cysteamine (2-mercaptoethylamine). (ii) Suppression of reactive oxygen species (ROS) in the skin of live animals given oral administrations of Zn(II) and its complexes in relation to the skin damage under ultra-violet (UV) light. (iii) Improvement of diabetes mellitus by insulin-mimetic vanadyl(IV) (VO(II)) complexes.
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