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Folate-appended cyclodextrin improves the intratumoral accumulation of existing boron compounds.
Applied Radiation and Isotopes ( IF 1.6 ) Pub Date : 2020-04-27 , DOI: 10.1016/j.apradiso.2020.109201
Yoshitaka Matsumoto 1 , Kenjiro Hattori 2 , Hidetoshi Arima 3 , Keiichi Motoyama 4 , Taishi Higashi 5 , Hitoshi Ishikawa 1 , Nobuyoshi Fukumitsu 6 , Teruhito Aihara 7 , Kei Nakai 1 , Hiroaki Kumada 8 , Hideyuki Sakurai 1
Affiliation  

In this study, the tumor accumulation and antitumor effect of folate-modified cyclodextrin (ND201) purified with folate receptor (FR) connotated with BSH were examined. ND201 and BSH were stably bound in blood, and the mixing ratio 1:1 was most efficient. ND-BSH showed higher boron concentration (38.5 ppm) than BSH alone (11.25 ppm). The maximum ND-BSH tumor/blood ratio was also markedly higher (6.58) than that of BSH alone (1.04). ND-BSH showed a significant antitumor effect compared with BSH after neutron irradiation.



中文翻译:

添加叶酸的环糊精改善了现有硼化合物的肿瘤内积累。

在这项研究中,研究了用 BSH 内涵的叶酸受体 (FR) 纯化的叶酸修饰环糊精 (ND201) 的肿瘤积累和抗肿瘤作用。ND201和BSH在血液中稳定结合,1:1的混合比例最有效。ND-BSH 显示出比单独的 BSH (11.25 ppm) 更高的硼浓度 (38.5 ppm)。最大 ND-BSH 肿瘤/血液比率也显着高于单独的 BSH (1.04) (6.58)。与中子照射后的 BSH 相比,ND-BSH 显示出显着的抗肿瘤作用。

更新日期:2020-04-27
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