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首页> 外文期刊>Scientific reports. >Decreasing undesirable absorbed radiation to the intestine after administration of radium-223 dichloride for treatment of bone metastases
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Decreasing undesirable absorbed radiation to the intestine after administration of radium-223 dichloride for treatment of bone metastases

机译：施用亚氯化钠-223-二氯化物以治疗骨转移后，将不希望的吸收辐射降低

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[223Ra]RaCl2 is the first alpha-particle emitting radiopharmaceutical to be used for castration-resistant prostate cancer patients with bone metastases because of its excellent therapeutic effects. [223Ra]RaCl2 is excreted via the intestine into feces, and some is absorbed from the intestine into the blood, which may be undesirable in terms of the exposure to radiation. Recently, we showed that a complex of myo-inositol-hexakisphosphate (InsP6) with zinc is a useful decorporation agent against radiostrontium. In this study, we hypothesized that Zn-InsP6 could bind to not only strontium but also to radium, and could inhibit the absorption of radium from the intestine. In in vitro binding experiments, Zn-InsP6 showed a high binding affinity for radium. In in vivo biodistribution experiments by intravenous injection of [223Ra]RaCl2 after treatment of Zn-InsP6, mice treated with Zn-InsP6 showed significantly lower bone accumulation of radioactivity (34.82?±?1.83%Dose/g) than the mice in the non-treatment control group (40.30?±?2.78%Dose/g) at 48?h postinjection. These results indicate that Zn-InsP6 bound radium in the intestine and inhibited the absorption of radium into the blood. Therefore, the insoluble Zn-InsP6 complex has high potential to decrease the side effects of [223Ra]RaCl2.
机译：[223RA] RACL2是第一个用于用于抗阉割前列腺癌患者的α-粒子发射放射性药物，因为其具有优异的治疗效果，其具有骨转移患者。 [223RA] RACL2通过肠道排出粪便，一些从肠道吸收到血液中，这在暴露于辐射方面可能是不希望的。最近，我们表明，用锌的肌醇 - 六种磷酸盐（Insp6）复合物是一种避免辐射器的有用的装饰剂。在这项研究中，我们假设Zn-Insp6不仅可以与锶结合而且还可以抑制山克的吸收。在体外结合实验中，Zn-Insh6显示了对镭的高结合亲和力。在体内生物分布试验中通过静脉注射[223RA] Racl2在治疗Zn-Insp6之后，用Zn-Insp6处理的小鼠显示出低于非活动中的小鼠的放射性骨积累显着降低骨积累（34.82〜±1.83％的剂量/ g）。 -Treatment对照组（40.30？±2.78％剂量/ g）在48次出汗。这些结果表明肠道中的Zn-Insp6结合镭，抑制镭的吸收到血液中。因此，不溶性Zn-Insh6复合物具有高潜力，以降低[223RA] RACL2的副作用。

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