代谢
当将50毫克的球茎螨（Rhizoglyphus echinopus，Fumouze and Robin）样本置于涂有0.53微克放射性碳标记的炔丙醇的玻璃小瓶中1小时后，大约12%（1.27微克/克）的杀螨剂转移到了螨虫体内。用炔丙醇处理的螨虫被保存在保存小瓶中，并在6、12、24和48小时后评估代谢的程度。放射性碳的内部水平占剂量的14.8%至17.4%，并且在大约相等的比例下分配给螨虫提取物和螨虫残留物部分。当以内提取物中总回收放射性碳的百分比表示时，炔丙醇的内部提取水平在6小时时从5.9%降至48小时时的2.5%，当以内提取物中放射性碳的相对百分比表示时，从6小时时的61.5%降至48小时时的29.8%。因此，炔丙醇被螨虫缓慢降解。代谢物4-叔丁基酚和2-(4-叔丁基苯氧基)环己醇（甘醇醚）以低水平存在（<0.5%）。炔丙醇通过球茎螨匀浆体外降解，12000离心上清液的活性大约是相应沉淀的四倍。外源性NADPH和谷胱甘肽显著增强了上清液部分对炔丙醇的降解。然而，在谷胱甘肽存在下的降解并非全部是酶促的；当炔丙醇在没有螨虫上清液的情况下与辅因子在缓冲液中孵化时，大约15%的炔丙醇转化为4-叔丁基酚。体外炔丙醇降解产物主要由未识别的极性代谢物组成，但4-叔丁基酚和甘醇醚也以低水平存在。
When 50-mg samples of bulb mites, Rhizoglyphus echinopus (Fumouze and Robin), were placed for 1 hr in glass vials coated with 0.53 mug of radiocarbon-labeled propargite, about 12% (1.27 ug/g) of the acaricide was transferred to the mites. Mites treated with propargite were kept in holding vials and the extent of metabolism was evaluated after 6, 12, 24, and 48 hr. Internal levels of radiocarbon ranged from 14.8 to 17.4% of the dose and were divided about equally between the mite extrat and mite residue fractions. Levels of propargite in the internal extract decreased from 5.9 at 6 hr to 2.5 at 48 hr when expressed as percentage of total recovered radiocarbon and from 61.5 at 6 hr to 29.8 at 48 hr when expressed as relative percentage of radiocarbon in the internal extract. Thus, propargite was degraded slowly by the mites. The metabolites 4-tert-butylphenol and 2-(4-tert-butylphenoxy) cyclohexanol (glycol ether) were present at low levels (< 0.5%). Propargite was degraded in vitro by bulb mite homogenates with the 12,000 pernatant being about four times more active than the corresponding pellet. Exogenous NADPH and glutathione greatly enhanced propargite degradation by the supernatant fraction. However, not all of the degradation in the presence of glutathione was enzymatic; about 15% of the propargite was converted to 4-tert-butylphenol when the acaricide was incubated with cofactor in buffer in the absence of the mite supernatant. In vitro propargite degradation products consisted mainly of unindentified polar metabolites, but low levels of 4-tert-butylphenol and glyol ether also were present.
来源:Hazardous Substances Data Bank (HSDB)
