Srinivas P N, Reddy G R, Chetty C S
Department of Zoology, Sri Venkateswara University, Tirupati, India.
Biochem Int. 1989 Jul;19(1):209-14.
Effect in vitro of benthiocarb, an organocarbamate herbicide on neonate rat (3 day old) brain was studied to understand the interaction of benthiocarb with Na+K+-ATPase. Na+K+-ATPase of the developing rat brain was selected as an index enzyme since alterations in the Na+K+-ATPase activity leads to neuronal dysfunction. The assay of Na+K+-ATPase in the presence of 1-8 mu moles of benthiocarb showed decreased activity and a concentration dependent inhibition of Na+K+-ATPase was noticed upto 7 mu moles of benthiocarb. Based on IC50 values (median concentration), 50% inhibition of the enzyme was observed with 5 mu moles of benthiocarb. Norepinephrine (NE) was selected to study the modulation of benthiocarb inhibited enzyme. Maximum increase (76.7%) of Na+K+-ATPase was noticed with 35 mu moles of NE and effective concentration (EC50) of NE which produced 50% activation of the enzyme was found to be 20 mu moles. This study suggests that NE acts as a protective agent in reversing the benthiocarb in vitro inhibited neonate rat brain Na+K+-ATPase.
为了解杀草丹与钠钾 -ATP 酶的相互作用,研究了有机氨基甲酸酯类除草剂杀草丹对新生大鼠(3 日龄)脑的体外作用。发育中大鼠脑的钠钾 -ATP 酶被选为指标酶,因为钠钾 -ATP 酶活性的改变会导致神经元功能障碍。在存在 1 - 8 微摩尔杀草丹的情况下对钠钾 -ATP 酶进行测定,结果显示其活性降低,并且在高达 7 微摩尔杀草丹时观察到钠钾 -ATP 酶存在浓度依赖性抑制。根据半数抑制浓度(IC50)值,5 微摩尔杀草丹可使该酶产生 50%的抑制。选择去甲肾上腺素(NE)来研究其对杀草丹抑制的酶的调节作用。在 35 微摩尔 NE 时观察到钠钾 -ATP 酶的最大增加量(76.7%),发现产生该酶 50%激活的 NE 有效浓度(EC50)为 20 微摩尔。这项研究表明,在体外,NE 可作为一种保护剂来逆转杀草丹对新生大鼠脑钠钾 -ATP 酶的抑制作用。