Pine M J, Mirand E A, Ambrus J L, Bock F G
J Med. 1983;14(5-6):433-49.
2--amino-2-thiazoline (AT) and 1-thiazolidine-4-carboxylate (TC, thioproline), which have been previously proposed as agents of reverse transformation, have been examined as antitumor agents in several rodent tumor systems. AT administration reduced tumor incidence in sym-dimethylhydrazine treated outbred ICR Swiss female mice and doubled the survival of DBA/2Ha female mice infected with polycythemic Friend leukemia virus. Indomethacin, pentoxyphylline, RA233 and diethyldithiocarbamate (DTC), with potential for altering host or tumor prostaglandin levels, platelet aggregation and host immunity, respectively, ranged from marginally effective to ineffective against Friend virus infection. AT was, however, ineffective against 4 other induced and transplanted mouse tumors and did not notably increase differentiation or decrease transformation in any of several tumor cell systems. No in vitro or in vivo tumor system was found to be more than marginally affected by TC. Thus, AT alone was of significant antitumor activity in inhibiting late stages of viral- or carcinogen induced tumor progression, but could not be demonstrated as an agent of reverse transformation.
2-氨基-2-噻唑啉（AT）和1-噻唑烷-4-羧酸盐（TC，硫代脯氨酸），先前已被提议作为逆转转化剂，在几种啮齿动物肿瘤系统中作为抗肿瘤剂进行了研究。给予AT可降低经对称二甲基肼处理的远交系ICR瑞士雌性小鼠的肿瘤发生率，并使感染红细胞增多性Friend白血病病毒的DBA/2Ha雌性小鼠的存活率提高一倍。吲哚美辛、己酮可可碱、RA233和二乙基二硫代氨基甲酸盐（DTC）分别具有改变宿主或肿瘤前列腺素水平、血小板聚集和宿主免疫力的潜力，但对Friend病毒感染的效果从微效到无效不等。然而，AT对其他4种诱导和移植的小鼠肿瘤无效，并且在任何几种肿瘤细胞系统中均未显著增加分化或减少转化。未发现体外或体内肿瘤系统受TC的影响超过微效。因此，单独使用AT在抑制病毒或致癌物诱导的肿瘤进展后期具有显著的抗肿瘤活性，但不能证明其为逆转转化剂。
