以类黄酮为原料开发抗癌药物的潜在示踪剂99mtc -芦丁的优化合成方法

E. M. Widyasari, Esty Kusumawardhany, R. J. Sugiharti, M. E. Sriyani, Muharam Marzuki
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引用次数: 3

摘要

根据2013年印度尼西亚卫生部的基本卫生研究数据,印度尼西亚恶性肿瘤和肿瘤恶性肿瘤的死亡率仍然很高,癌症患病率约为1.4%。化疗仍然是癌症治疗方式的主要选择,使用化疗药物来根除和抑制癌细胞的生长;然而,这种治疗的成本非常高。因此,患者倾向于寻求替代治疗,如服用传统草药治疗癌症。芦丁因其具有抗氧化活性,是一类极具吸引力的植物化学物质黄酮类化合物。然而,作为传统的中草药,由于缺乏科学资料,其有效性尚未完全确定。放射性示踪剂可被定义为一种特定的放射性标记分子,可监测功能分子的体内行为,并可用于提供生命系统中的生物信息。因此,为了提供芦丁治疗癌症的药理信息,我们合成了放射性标记的类黄酮99mtc -芦丁作为放射性示踪剂。本研究的目的是在不同的芦丁用量、不同的药剂浓度和不同的孵育时间条件下,制备99mtc -芦丁。逐一改变所选参数进行标记研究,确定最佳标记条件。观察标记效率最高的条件后,在不孵育的条件下,以700 μg的芦丁,加入20 μg SnCl2.2H2O作为还原剂,1-3 mCi 99mTcO4-制备99mtc -芦丁。用放射性薄层色谱法测定99mtc -芦丁的放射化学收率,收率为99.28±0.14%,稳定达4小时。从本研究结果来看,成功标记的99mtc -芦丁可作为后续临床前研究的参考。此外,放射性标记99mt -芦丁有望作为芦丁抗癌药物研究和开发的工具,从天然产物中获得其疗效的详细信息。关键词:放射性示踪剂,99mtc -芦丁,癌症,标记化合物
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The Optimization Method for Synthesis of 99mTc-Rutin as Potential Radiotracer in The Development of Cancer Drugs From Flavonoid
Based on the Basic Health Research Data of Ministry of Health's of Indonesia in 2013, mortality rates from malignant and tumor malignancies in Indonesia are still high with prevalence of cancer is about 1.4%. Chemotherapy is still the primary choice in cancer modality that uses chemotherapeutic drugs to eradicate and inhibit the growth of cancer cells; however the cost this treatment is extremely high. Therefore, patient tends to seek alternative treatment such as consuming traditional herbal medicine for cancer treatment. Rutin is one of the attractive phytochemicals flavonoids because of its antioxidant activities. However, as traditional herbal medicine, its effectiveness is not yet been fully established due to the lack of scientific information. A radiotracer can be defined as a specific radiolabeled molecule that monitors the in vivo behaviour of a functional molecule, and can be used to provide biological information in a living system. Hence, to provide pharmacological information of rutin for cancer treatment, we synthesized radiolabeled flavonoid 99mTc-rutin as radiotracer. The aim of the present study is to develop 99mTc-rutin under varying conditions of rutin quantity, reducing agent concentration and incubation time. Labeling studies were performed by changing the selected parameters one by one and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency, 99mTc-rutin was obtained with preparation of 700 μg of rutin with addition of 20 μg of SnCl2.2H2O as reductor and 1-3 mCi 99mTcO4- without any incubation. Radiochemical yield of 99mTc-rutin was determined with radio thin layer chromatography which was found 99.28 ± 0.14% and stable up to 4 hour. From the result of this study, the successfully labeled 99mTc-rutin can be used as a reference for following preclinical study. Furthermore radiolabeled 99mTc-rutin is expected as tools in research and development of rutin as cancer drugs from natural product to obtain detailed information its efficacy.Keywords: radiotracer, 99mTc-rutin, cancer, labeled compounds
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