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1-异丁酰基-2-异丙基异硫脲磷酸盐，T1082：一种安全有效的肿瘤放射治疗并发症预防剂。

1-Isobutanoil-2-isopropylisothiourea Phosphate, T1082: A Safe and Effective Prevention of Radiotherapy Complications in Oncology.

机构信息

A. Tsyb Medical Radiological Research Center-Branch of the National Medical Research Radiological Center of the Ministry of Health of the Russian Federation, 249036 Obninsk, Russia.

National Medical Research Radiological Center of the Ministry of Health of the Russian Federation, 249036 Obninsk, Russia.

出版信息

Int J Mol Sci. 2022 Feb 28;23(5):2697. doi: 10.3390/ijms23052697.

DOI:10.3390/ijms23052697
PMID:35269835
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8911053/
Abstract

The radioprotective effects of a new 1-isobutanoil-2-isopropylisothiourea derivative named T1082 are presented. Research methods included toxic characteristics, radioprotective activity (Till-McCulloch's test and 30-day survival test) in γ-ray total-body-irradiated mice, and a clinical and histological study of the effect of T1082 on acute radiation skin reactions (RSR) in rats after a single or fractionated β-ray local irradiation. T1082 is more effective than its analogue, the NOS inhibitor T1023, at low concentrations and doses (1/12-1/8 LD), both parenterally and intragastrically. In this case, its therapeutic index (LD/ED) reaches 30, and the optimal radioprotective doses (ED-141-224 mg/kg) are an order less than the maximum tolerated doses-1/16-1/10 LD. These properties allowed T1082, at a low intragastrical dose (160 mg/kg; 1/14 LD10), to significantly limit the severity of acute RSR after single (40 Gy) and fractionated (78 Gy) β-ray irradiation. The results confirm T1082 as one of the safest emergency radioprotectors and indicate the prospects for its further development as a pharmacological agent for the prevention of RT complications.

摘要

本文介绍了一种新型的 1-异丁酰基-2-异丙基异硫脲衍生物 T1082 的放射防护作用。研究方法包括毒性特征、γ 射线全身照射小鼠的放射保护活性（Till-McCulloch 试验和 30 天存活试验），以及 T1082 对单次或分次β射线局部照射后大鼠急性放射性皮肤反应（RSR）影响的临床和组织学研究。T1082 在低浓度和剂量（1/12-1/8 LD）下，无论是通过肠外途径还是口服途径，都比其类似物、NOS 抑制剂 T1023 更有效。在这种情况下，其治疗指数（LD/ED）达到 30，最佳的放射保护剂量（ED141-224mg/kg）比最大耐受剂量（1/16-1/10 LD）低一个数量级。这些特性使得 T1082 能够在低口服剂量（160mg/kg；1/14 LD10）下，显著限制单次（40Gy）和分次（78Gy）β射线照射后急性 RSR 的严重程度。这些结果证实了 T1082 是一种最安全的紧急放射防护剂之一，并表明了其作为预防 RT 并发症的药理学药物进一步开发的前景。

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