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首页> 外文期刊>Human and Experimental Toxicology >In vivo protection by amifostine and DRDE-07 against sulphur mustard toxicity.
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In vivo protection by amifostine and DRDE-07 against sulphur mustard toxicity.

机译：氨磷汀和DRDE-07在体内对硫芥子碱毒性的保护作用。

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The study was aimed at investigating the prophylactic efficacy of orally administered amifostine and a newly synthesized compound, S-2(2-amino-ethylamino)ethyl phenyl sulphide (DRDE-07), against dermally applied sulphur mustard (SM) in mice and rats. The LD50 values of amifostine and DRDE-07 were determined following oral and intraperitoneal routes and the LD50 of SM diluted in PEG-300 was determined following dermal route. Amifostine or DRDE-07 (equivalent to their 0.05 LD50, 0.10 LD50 and 0.20 LD50) dissolved in water was fed to mice and rats and, after 30 min, various doses of SM were applied to the hair-clipped area of the skin and were observed for 14 days for mortality. The protection index (PI) was calculated as a ratio of LD50 with treatment to LD50 without treatment. The estimated percutaneous LD50 of SM was found to be 8.1 and 2.4 mg/kg for female mice and male rats, respectively. A dose-related protection was observed with all the three doses of both compounds. Thirty minutes prior, the administration of amifostine in female mice offered a PI of 3.0 at the lowest pretreatment dose (52.5 mg/ kg) followed by PI of 6.7 and 9.5 at 105 and 210 mg/kg pretreatment doses, respectively. DRDE-07 offered better protection against SM in female mice, i.e., a PI of 4.8 at pretreatment dose of 62.5 mg/kg, a PI of 12.0 at the dose of 124.7 mg/kg and a PI of 27.0 at the dose of 249.4 mg/kg. In male rats, DRDE-07 gave a PI of about 3.0 at all the three pretreatment doses (80, 160 and 320 mg/kg), whilst amifostine offered a PI of 3.1 at the highest pretreatment dose (452 mg/kg). The present study showed that oral administration of both amifostine and DRDE-07 was effective as a prophylactic agent for protecting against SM toxicity, and that DRDE-07 offered better protection.
机译：这项研究旨在研究口服给予氨磷汀和一种新合成的化合物S-2（2-氨基-乙基氨基）乙基苯硫醚（DRDE-07）对小鼠和大鼠皮肤施用的硫芥菜（SM）的预防作用。按照口服和腹膜内途径确定氨磷汀和DRDE-07的LD50值，按照皮肤途径确定在PEG-300中稀释的SM的LD50。将溶解在水中的氨磷汀或DRDE-07（相当于其0.05 LD50、0.10 LD50和0.20 LD50）喂给小鼠和大鼠，并在30分钟后将各种剂量的SM应用于皮肤毛发闭合的部位，观察14天的死亡率。保护指数（PI）计算为经治疗的LD50与未经治疗的LD50的比率。发现雌性小鼠和雄性大鼠的经皮经皮LD50估计分别为8.1和2.4mg / kg。两种化合物的全部三个剂量均观察到剂量相关的保护作用。三十分钟前，在雌性小鼠中服用氨磷汀在最低预处理剂量（52.5 mg / kg）下提供的PI为3.0，然后在105和210 mg / kg预处理​​剂量下分别提供6.7和9.5的PI。 DRDE-07为雌性小鼠提供了更好的抗SM的保护，即62.5 mg / kg的预处理剂量时PI为4.8，124.7 mg / kg的剂量时PI为12.0，249.4 mg的剂量时PI为27.0。 /公斤。在雄性大鼠中，在三种预处理剂量（80、160和320 mg / kg）下，DRDE-07的PI均约为3.0，而氨磷汀在最高预处理剂量（452 mg / kg）下的PI值为3.1。目前的研究表明，口服氨磷汀和DRDE-07可以有效预防SM毒性，DRDE-07可以提供更好的保护作用。

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