- 作者： 陳漢恒; D. R. Buhler
- 作者服務機構： 中國文化大學應用化學研究所; 奧勤岡州立大學農業化學系及環境衛生科學中心
- 中文摘要：
本文乃研究Nitrosocarbaryl及Carbaryl在in vitro情況下，對老鼠肝中的化學藥物代謝?的影響。由實驗結果得知
， Nitrosocarbaryl與Carbaryl兩者之間對化學藥物代謝?的影響有極大之差異(P 0.05)。Nitrosocarbaryl對肝中之
Microsomal aryl hydrocarbon hydroxylase,aminopyrine N-demethylase,epoxide hydrolase及Cytosolic glutathione-S-
transferase有極大之抑制作用，其抑制作用與 Nitrosocarbaryl 量成正比。Nitrosocarbaryl在 1x10 M時顯著地(P
0.001)抑制 aryl hydrocarbon hydroxylase 及 aminopyrine N-demethylase 的活性，其I 值各為 1.8x10 及 3.5x10
M。Nitrosocarbaryl在1.3xl0 至 1.2x10 M時，抑制 epoxide hydrolase 18%，且在 1.2x10 M時其抑制性與對照
組有顯著性差異(P 0.01)。Nitrosocarbaryl在1.6x10 M以上時，便顯著地(P 0.001)抑制 Cytosolic glutathione-
S-transferase的活性，其I 為3.8x10 M。相反地Carbaryl在3x10 4 M時，並不抑制 aryl hydrocarbon hydroxylase
活性，增加至6x 10 M時，纔抑制20%。Carbaryl約在1x10 M時，顯著地(P 0.05)增加epoxide hydrolase活性
23%。Carbaryl在1.4x10 M時只稍抑制 Cytosolic glutathione-S-transferase 活性15%，但卻顯著地(P 0.001)抑制
aminopyrine N-demethylase，其I 為5.4x10 M；但與 Nitrosocarbaryl 比較，則Carbaryl對demethylase的抑制
性較弱。
總言之，Nitrosocarbaryl與Carbaryl比較下，Nitrosocarbaryl對上述之藥物代謝wil更具很大之抑制作用。
- - 英文摘要： The Comparative effects of nitrosocarbaryl and carbaryl on rat hepatic microsomal aryl hydrocarbonhydroxylase, aminopyrine-N-demethylase, epoxide hydrolase and cytosolic glutathione-S-transferase invitro was investigated. The effects of nitrosocarbaryl on these hepatic drug metabolizing enzyme systemsdiffer markedly (P<0.05) from carbaryl. Nitrosocarbaryl was more potent and had much higher inhib-itory effect than carbaryl on microsomal aryl hydrocarbon hydroxylase, aminopyrine N-demethylase,epoxide hydrolase and cytosolic glutathione-S-transferase. Inhibition of these enzyme sysetems by nitroso-carbaryl was dose-dependent. In microsomes, nitrosocarbaryl showed a significant (P<0.001) inhibitionof aryl hydrocarbon hydroxylase and aminopyrine N-demethylase as compared with the control when theconcentration of nitrosocarbaryl added was above 1x10 M. The I values were 1.8x10 M and 3.5x10 M, respectively. Nitrosocarbaryl inhibited epoxide hvdrolase activity gradually up to 18% at the range ofconcentration studied (1.3x10 M - 1.2x10 M) and showed a significant (P<0.001) inhibition at theconcentration of 1.2x10 M. Nitrosocarbarvl at concentrations above 1.6x10 M showed a significant(P<0.001) inhibition of cytosolic glutathione-S-transferase activity with an I value of 3.8x10 M. By Contrast, carbaryl failed to inhibit aryl hydrocarbon hydroxylase at concentrations below 3x10 M. The pesticide inhibited the enzyme activity only by 20% at the maximum concentration studied (6x10 M). Carbaryl stimulated the activity of epoxide hydrolase significantly (P<0.05), reaching a maxi-mum of 123% of control activity at a concentration of approximately 10 M. Carbarylhad little inhibitoryeffect (15%) on cytosolic glutathione-S-transferase at concentrations up to 1.4x10 M. Carbaryl was apotent (P<0.001）inhibitor of aminopyrine-N-demethylase as compared with control, exhibiting an I concentration of 5.4x10 M. However the pestrcrae nao a slightly less rnrirbrtory eltect on amrnopyrrne-N-demethylase than did its nitroso analog.
- 中文關鍵字： carbaryl; nitrosocarbaryl; drug metabolizing enzymes; microsomal; hepatic
- 英文關鍵字： --
