Lim Jeong-Hyeon, Kim Hyung-Wook, Jeon Ju-Hyun, Lee Hoi-Seon
Department of Agricultural Chemistry and Institute of Agricultural Science & Technology, College of Agriculture & Life Science, Chonbuk National University, Chonju 561-756, South Korea.
J Agric Food Chem. 2008 Nov 12;56(21):9962-6. doi: 10.1021/jf8022244. Epub 2008 Oct 10.
Allyl isothiocyanate (AITC) and phenethyl isothiocyanate (PEITC) were isolated from Sinapis alba L. seeds and their effects against Dermatophagoides farinae and D. pteronyssinus were evaluated using the impregnated fabric disk method. The LD 50 values of their compounds and derivatives were then compared with those of a commercial acaricide, benzyl benzoate. On the basis of the LD 50 values against D. farinae, PEITC (0.21 microg/cm(2)) was the most toxic, followed by benzyl isothiocyanate (0.55 microg/cm(2)), phenyl isothiocyanate (1.09 microg/cm(2)), butyl isothiocyanate (1.24 microg/cm(2)), and AITC (1.36 microg/cm(2)); acetyl isothiocyanate (195.01 microg/cm(2)) was the least toxic. In addition, the acaricidal effects of AITC and PEITC against D. farinae were 7.4- and 47.8-fold greater than those of benzyl benzoate, respectively. Against D. pteronyssinus, PEITC was the most toxic (0.19 microg/cm(2)), followed by benzyl isothiocyanate (0.77 microg/cm(2)), phenyl isothiocyanate (1.37 microg/cm(2)), butyl isothiocyanate (1.50 microg/cm(2)), and AITC (2.88 microg/cm(2)); acetyl isothiocyanate (168.82 microg/cm(2)) was the least toxic. AITC and PEITC were 3.3- and 50.4-fold more active than benzyl benzoate against D. pteronyssinus, respectively. Taken together, these findings indicate that AITC, PEITC, and partial derivatives may be useful as preventive agents against dust mites. In addition, these results indicate that structure-activity is related to the aromatic structure, the number of carbon atoms, and the compounds hydrophobicity.
从白芥子种子中分离出异硫氰酸烯丙酯（AITC）和异硫氰酸苯乙酯（PEITC），并采用浸渍织物圆盘法评估它们对粉尘螨和屋尘螨的作用。然后将其化合物和衍生物的半数致死剂量（LD50）值与市售杀螨剂苯甲酸苄酯的LD50值进行比较。基于对粉尘螨的LD50值，PEITC（0.21微克/平方厘米）毒性最大，其次是异硫氰酸苄酯（0.55微克/平方厘米）、异硫氰酸苯酯（1.09微克/平方厘米）、异硫氰酸丁酯（1.24微克/平方厘米）和AITC（1.36微克/平方厘米）；异硫氰酸乙酰酯（195.01微克/平方厘米）毒性最小。此外，AITC和PEITC对粉尘螨的杀螨效果分别比苯甲酸苄酯高7.4倍和47.8倍。对于屋尘螨，PEITC毒性最大（0.19微克/平方厘米），其次是异硫氰酸苄酯（0.77微克/平方厘米）、异硫氰酸苯酯（1.37微克/平方厘米）、异硫氰酸丁酯（1.50微克/平方厘米）和AITC（2.88微克/平方厘米）；异硫氰酸乙酰酯（168.82微克/平方厘米）毒性最小。AITC和PEITC对屋尘螨的活性分别比苯甲酸苄酯高3.3倍和50.4倍。综上所述，这些发现表明AITC、PEITC和部分衍生物可能作为预防尘螨的药剂。此外，这些结果表明结构活性与芳香结构、碳原子数和化合物疏水性有关。
