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从黄酮类化合物开发抗癌药物过程中锝-99m-木犀草素作为放射性示踪剂合成的优化方法。

The optimization method for synthesis of technetium-99m-luteolin as radiotracer in the development of cancer drugs from flavonoid.

作者信息

Ramdhani Danni, Sriyani Maula Eka, Nabila S Fairuz

机构信息

Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Padjadjaran University, Sumedang, West Java, Indonesia.

Applied Nuclear Science and Technology Center (PSTNT), National Atomic Energy Agency (BATAN), Bandung, West Java, Indonesia.

出版信息

J Adv Pharm Technol Res. 2020 Apr-Jun;11(2):59-63. doi: 10.4103/japtr.JAPTR_161_19. Epub 2020 Apr 22.

Abstract

The aim of this study is to find the optimum conditions of labeling luteolin flavonoid compounds with technetium-99m (Tc) to meet the purity requirements stated in the United States Pharmacopeia. This compound is expected to be a potential radiotracer compound for diagnosing cancer. The optimization method in labeling luteolin with technetium determines the parameters such as pH, SnCl.2HO, genistein concentration, and incubation time. Optimization results of Technetium-99m-luteolin labeling obtained optimum pH conditions 8, the amount of SnCl.2HO as a reducing agent 60 μL, the optimum amount of luteolin 6 mg/ml, and the optimum incubation time is 30 min. This optimum condition obtained a Tc-Luteolin radiochemical purity yield of 94.15%. The radiochemical purity percentage of the Tc-Luteolin compound has fulfilled the requirements listed at United States Pharmacopeia, which is ≥90%.

摘要

本研究的目的是找到用99m锝(Tc)标记木犀草素类黄酮化合物的最佳条件,以满足美国药典规定的纯度要求。该化合物有望成为一种潜在的用于诊断癌症的放射性示踪剂化合物。用锝标记木犀草素的优化方法确定了诸如pH值、SnCl·2H₂O、染料木黄酮浓度和孵育时间等参数。99m锝-木犀草素标记的优化结果得到最佳pH条件为8,作为还原剂的SnCl·2H₂O用量为60μL,木犀草素的最佳用量为6mg/ml,最佳孵育时间为30分钟。此最佳条件下获得的Tc-木犀草素放射化学纯度产率为94.15%。Tc-木犀草素化合物的放射化学纯度百分比已满足美国药典列出的要求,即≥90%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c291/7305782/1ca1a99845d3/JAPTR-11-59-g001.jpg

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