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为了寻找更有效的辐射损伤防护药,改变已知辐射防护剂芥子碱结构,经3,4,5—三甲氧基苯丙烯酸酰氯和二乙胺基代乙硫醇在碱催化下缩合,新合成了辐射防护药芥子酸硫酯衍生物:3.4,5—三甲氧基苯丙烯酸二乙胺基代乙硫醇酯盐酸盐。用ESR波谱研究表明:其保护机理是电子从靶分子脱氧胸腺嘧啶核苷酸(dTMP)及脱氧核糖核酸(DNA)向硫酯保护剂的长程转移。三甲氧基代苯丙烯酸硫醇酯是“潜在硫醇”类新型辐射防护剂,区别于文献熟知的硫代磺酸盐,硫代磷酸酯及硫代乙酸等其他代谢中能释放自由巯基的衍生物,预计芥子酸硫酯类衍生物有较小的毒性,对辐射损伤有防治功能;经小鼠整体抗辐射初步试验:~(60)Coγ射线7.5Gy辐照,用1.5mg/鼠照前预防及照后立即治疗后,预防组及治疗组动物30天中存活率分别比对照组动物提高20％和40％。芥子酸硫酯衍生物不仅对辐射损伤有防护效果,而且还具有增强机体辐射损伤的修复功能。由此推断:芥子酸硫酯类防护药不仅具有抗氧化剂和自由基清除的能力而那样起保护作用,还能通过电子转移保护DNA靶分子并能增强机体的修复能力;本文还报导了新防护药硫酯的质谱、红外及核磁共振光谱。
In order to find a more effective radiation damage protective drug, the structure of the known radioprotectant mustard was changed and synthesized by 3,4,5-trimethoxyphenyl acrylic acid chloride and diethylaminoethanethiol. Radioprotective agents Erucic acid thioester derivatives: Diethylaminoethyl 3,4-dimethoxybenzeneacrylate Diethylaminoethanethiolate hydrochloride. ESR spectroscopy studies show that the mechanism of protection is the long-range transfer of electrons from the target molecules of deoxythymidine (dTMP) and deoxyribonucleic acid (DNA) to thioester protectors. Thiomethoxyphenyl acrylate is a novel “potential thiol” class of radioprotectant that is distinguished from other thiol sulfonate, thiophosphate, and thioacetic acid derivatives known in the literature for the release of free thiols It is estimated that the erucic acid thioester derivatives are less toxic and have a preventive and therapeutic effect on radiation injury. The primary anti-radiation experiment in mice: ~ (60) Co γ-ray irradiation of 7.5 Gy, with 1.5 mg / After prevention and immediate treatment, the survival rates of animals in the prophylaxis group and treatment group increased by 20% and 40% respectively over the 30 days in the control group. Erucic acid thioester derivatives not only have a protective effect on radiation damage, but also have the function of enhancing the radiation damage of the body. From this, we concluded that erucate thioester protectors not only have antioxidant and free radical scavenging capacity, but also protect the DNA repair by electron transfer. This paper also reports new protective measures Mass Spectrometry, Infrared and Nuclear Magnetic Resonance Spectroscopy of Drug Thioesters.