Gad S C, Dunn B J, Gavigan F A, Reilly C, Peckham J C
Department of Toxicology, Allied Corporation, Morristown, NJ 07960.
J Appl Toxicol. 1988 Feb;8(1):35-42. doi: 10.1002/jat.2550080107.
Two structurally related acetylenic compounds, 5,7,11-Dodecatriyn-1-ol, (Compound A), and 5,7,11,13-Octadecatetrayne-1,18-Diol (Compound B), were evaluated in a tier I toxicology testing program as part of an ongoing research and development program. This battery of acute tests included acute oral, guinea pig maximization, photosensitization, dermal irritation, Ames and multiple genetic endpoint and a 2 week oral fetotoxicity study. Compound A was found to have an oral LD50 of 0.25 ml/kg, be an extreme dermal sensitizer, a mild dermal irritant (PDII of 1.7), and not mutagenic or fetotoxic in the tests employed. Compound B had an oral LD50 greater than 4 g/kg, was a moderate dermal sensitizer and mild dermal irritant (PDII of 1.4), was not mutagenic in the Ames test but weakly increased the incidence of SCEs and gene mutations in Chinese Hamster Ovary cells, and was not fetotoxic. Neither compound was found to be a photosensitizer, but during the course of the photosensitization study Compound A was found to cause neuromuscular signs (including hind limb paralysis) and a bilateral necrosis of the medulla oblongata in female guinea pigs. A similar lesion was found in female rats receiving a single oral dose of 0.25 ml/kg and in nonpregnant females dosed daily for two weeks at 0.03 ml/kg. Compound B was not found to produce any of these neurologic effects.
作为一项正在进行的研发项目的一部分,两种结构相关的炔类化合物,5,7,11-十二碳三炔-1-醇(化合物A)和5,7,11,13-十八碳四炔-1,18-二醇(化合物B),在一级毒理学测试项目中进行了评估。这一系列急性测试包括急性经口毒性、豚鼠最大化试验、光敏性、皮肤刺激性、艾姆斯试验和多个遗传终点试验,以及一项为期2周的经口胚胎毒性研究。结果发现,化合物A的经口半数致死量为0.25毫升/千克,是一种极强的皮肤致敏剂、轻度皮肤刺激物(光毒性指数为1.7),在所采用的测试中无致突变性或胚胎毒性。化合物B的经口半数致死量大于4克/千克,是一种中度皮肤致敏剂和轻度皮肤刺激物(光毒性指数为1.4),在艾姆斯试验中无致突变性,但在中国仓鼠卵巢细胞中轻微增加了姐妹染色单体交换和基因突变的发生率,且无胚胎毒性。两种化合物均未被发现具有光敏性,但在光敏性研究过程中,发现化合物A可导致雌性豚鼠出现神经肌肉症状(包括后肢麻痹)和延髓双侧坏死。在单次经口给予0.25毫升/千克的雌性大鼠以及以0.03毫升/千克的剂量每日给药两周的未孕雌性大鼠中也发现了类似病变。未发现化合物B会产生任何这些神经学效应。