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Synthesis, quality control, and bio‐evaluation of 99mTc‐cyclophosphamide
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-10-09 , DOI: 10.1111/cbdd.13107 Tanveer Hussain Bokhari 1 , Samina Roohi 2 , Saira Hina 3 , Muhammad Usman Akbar 1 , Muhammad Sohaib 4 , Munawar Iqbal 5
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-10-09 , DOI: 10.1111/cbdd.13107 Tanveer Hussain Bokhari 1 , Samina Roohi 2 , Saira Hina 3 , Muhammad Usman Akbar 1 , Muhammad Sohaib 4 , Munawar Iqbal 5
Affiliation
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Cancer is found to be the leading cause of death worldwide characterized by uncontrolled cell division. Nuclear medicines imaging using radiopharmaceuticals have pronounced potential for the diagnosis and treatment of cancers. Cyclophosphamide (CPH) is an antineoplastic drug which targets selectively cancer cells. In the present work, labeling of CPH with Tc‐99m is performed for diagnostic purpose, which gave labeling yield as high as 99% using 20 μg SnCl2·2H2O, 200 μg of ligand at pH 7 for 10 min reaction time at room temperature. The characterization of the prepared complex was performed using ITLC, electrophoresis, and HPLC. In vitro stability was analyzed in the presence of human serum at 37°C which has maximum value of 94 ± 0.5. The biodistribution studies of 99mTc‐CPH were performed in normal and tumor bearing Swiss Webster mice. The high accumulation of 99mTc‐CPH was observed in liver and tumours respectively at 4 hr after injection. Biodistribution results revealed that 99mTc‐CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.
中文翻译：
99mTc-环磷酰胺的合成，质量控制和生物评价
发现癌症是全球范围内以细胞分裂不受控制为特征的主要死亡原因。使用放射性药物的核医学成像在癌症的诊断和治疗方面具有显着的潜力。环磷酰胺（CPH）是一种抗肿瘤药，可选择性靶向癌细胞。在目前的工作中，出于诊断目的，用Tc-99m标记了CPH，使用20μgSnCl 2 ·2H 2 O，200μg配体在pH 7下于10min的反应时间可达到99％的标记产率。室内温度。使用ITLC，电泳和HPLC对所制备的复合物进行表征。在人血清存在下于37°C（最大值为94±0.5）进行体外稳定性分析。99m的生物分布研究Tc-CPH在正常和荷瘤的Swiss Webster小鼠中进行。注射后4小时，分别在肝脏和肿瘤中观察到99m Tc-CPH的高积累。生物分布结果表明，与化疗同时进行，99m Tc-CPH可能是潜在的肿瘤诊断剂。
更新日期：2017-10-09
中文翻译：
99mTc-环磷酰胺的合成，质量控制和生物评价
发现癌症是全球范围内以细胞分裂不受控制为特征的主要死亡原因。使用放射性药物的核医学成像在癌症的诊断和治疗方面具有显着的潜力。环磷酰胺（CPH）是一种抗肿瘤药，可选择性靶向癌细胞。在目前的工作中，出于诊断目的，用Tc-99m标记了CPH，使用20μgSnCl 2 ·2H 2 O，200μg配体在pH 7下于10min的反应时间可达到99％的标记产率。室内温度。使用ITLC，电泳和HPLC对所制备的复合物进行表征。在人血清存在下于37°C（最大值为94±0.5）进行体外稳定性分析。99m的生物分布研究Tc-CPH在正常和荷瘤的Swiss Webster小鼠中进行。注射后4小时，分别在肝脏和肿瘤中观察到99m Tc-CPH的高积累。生物分布结果表明，与化疗同时进行，99m Tc-CPH可能是潜在的肿瘤诊断剂。
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