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Evaluation of antioxidant activity and potential toxicity of 1-buthyltelurenyl-2-methylthioheptene

机译:1-甲基丁二烯基-2-甲基硫庚烯的抗氧化活性和潜在毒性的评估

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The aim of the present study was to evaluate pharmacological and toxicological properties of 1-buthyltelurenyl-2-methylthioheptene (compound 1). In vitro, compound 1 at 1 mu M was effective in reducing lipid peroxidation induced by Fe/EDTA. Compound 1 presented neither thiol peroxidase nor thiol oxidase activity and did not change delta-ALA-D (delta-aminolevulinate dehydratase) activity (10-400 mu M). Calculated LD50 of compound 1, administered by oral route, was 65.1 mu mol/kg. Rats treated with compound I did not reveal any motor impairment in the open field. Hepatic, renal and cerebral lipid peroxidation in treated rats did not differ from those in control rats. Conversely, 0.5 mu mol/kg of compound 1 decreased lipid peroxidation in spleen. delta-ALA-D activity in liver and spleen was inhibited in rats treated with the higher dose of compound 1 but no significant differences were detected in renal delta-ALA-D activity. AST (aspartate aminotransferase) and ALT (alanine aminotransferase) activities as well as urea and creatinine levels were increased by high doses of compound 1 (50-75 mu mol/kg). Compound I induced a significant decrease in plasma triglyceride levels but none of the doses tested changed the cholesterol level. This is a promising compound for more detailed pharmacological studies involving organotellurium compounds. (c) 2006 Elsevier Inc. All rights reserved.
机译:本研究的目的是评估1-丁基十四碳二烯基-2-甲基硫庚烯(化合物1)的药理和毒理特性。在体外,1μM的化合物1可有效减少Fe / EDTA诱导的脂质过氧化。化合物1既不显示硫醇过氧化物酶活性,也不显示硫醇氧化酶活性,并且不改变δ-ALA-D(δ-氨基乙酰丙酸酯脱水酶)活性(10-400μM)。口服给药的化合物1的经计算的LD50为65.1μmol/ kg。用化合物I治疗的大鼠在野外没有发现任何运动障碍。治疗大鼠的肝,肾和脑脂质过氧化与对照组大鼠无差异。相反,0.5μmol/ kg的化合物1减少了脾脏中脂质的过氧化。在用较高剂量的化合物1治疗的大鼠中,肝和脾中的delta-ALA-D活性被抑制,但是在肾脏的delta-ALA-D活性中未检测到显着差异。高剂量的化合物1(50-75μmol/ kg)可提高AST(天冬氨酸转氨酶)和ALT(丙氨酸转氨酶)活性以及尿素和肌酐水平。化合物I引起血浆甘油三酸酯水平显着降低,但所测试的剂量均未改变胆固醇水平。对于涉及有机碲化合物的更详细的药理研究,这是一种很有前途的化合物。 (c)2006 Elsevier Inc.保留所有权利。

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