Vig P J, Desaiah D, Mehrotra B D
Department of Neurology, University of Mississippi School of Medicine, Jackson 39216.
J Appl Toxicol. 1990 Feb;10(1):55-7. doi: 10.1002/jat.2550100110.
The effects of organochlorine (O.C.) compounds, such as aldrin, dieldrin, endrin, isodrin, chlordecone and mirex, on calmodulin (CaM) activity were investigated. Changes induced by O.C. compounds on biological and physical properties of CaM were monitored in terms of phosphodiesterase stimulation and tyrosine fluorescence, respectively. None of the O.C. compounds altered tyrosine fluorescence of CaM in the presence of Ca2+. Except for chlordecone, none of the O.C. compounds inhibited CaM-activated phosphodiesterase (PDE). Chlordecone significantly decreased (P less than 0.05) CaM-activated PDE in a concentration-dependent manner without affecting the basal enzyme. Combination of chlordecone with W-7 (CaM antagonist) increased the inhibitory effect of W-7 on CaM activity. These results suggest that O.C. compounds may not be changing the tyrosine fluorescence of CaM. Among the O.C. compounds tested, chlordecone is a specific inhibitor of CaM-activated PDE.
研究了有机氯（O.C.）化合物，如艾氏剂、狄氏剂、异狄氏剂、氯丹、十氯酮和灭蚁灵，对钙调蛋白（CaM）活性的影响。分别根据磷酸二酯酶刺激和酪氨酸荧光监测了O.C.化合物对CaM生物学和物理性质的诱导变化。在Ca2+存在的情况下，没有一种O.C.化合物改变CaM的酪氨酸荧光。除十氯酮外，没有一种O.C.化合物抑制CaM激活的磷酸二酯酶（PDE）。十氯酮以浓度依赖性方式显著降低（P小于0.05）CaM激活的PDE，而不影响基础酶。十氯酮与W-7（CaM拮抗剂）联合使用增加了W-7对CaM活性的抑制作用。这些结果表明，O.C.化合物可能不会改变CaM的酪氨酸荧光。在所测试的O.C.化合物中，十氯酮是CaM激活的PDE的特异性抑制剂。
