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首页> 外文期刊>The Internet Journal of Pharmacology >The effect of pretreatment with plant extract, nicotine and caffeine on sleeping time induced by pentobarbitone in mice
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The effect of pretreatment with plant extract, nicotine and caffeine on sleeping time induced by pentobarbitone in mice

机译：植物提取物，尼古丁和咖啡因预处理对戊巴比妥诱导的小鼠睡眠时间的影响

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Objective: To determine the effects of plant extract, nicotine and caffeine on the activities of the liver metabolizing-enzyme induced by pentobarbitone. Materials and Method: Seven groups of mice were pretreated with high doses of sample extracts (0.4 mg/g body weight sample extract, but nicotine at 0.1 mg/g body weight) and one control group was pretreated with saline. On day 5, pentobarbitone (0.005 ml of 8 mg/ml) was administered and the sleeping time was determined. The test was repeated but at low doses (0.1 mg/g body weight sample extract, but nicotine at 0.05mg/g body weight). Results: At high doses, bitter gourd, 'tempeh', nicotine, caffeine, nicotine+bitter gourd, nicotine+'tempeh' and nicotine+caffeine induced the activities of liver metabolizing enzyme significantly compared to control. At low doses, bitter gourd, nicotine, caffeine, nicotine+bitter gourd, nicotine+'tempeh' and nicotine+caffeine induced the enzyme but 'tempeh' did not. Conclusion: The findings suggest that bitter gourd, nicotine and caffeine act as enzyme inducers, but 'tempeh' only demonstrate this ability at high dose. Source of support: University of Malaya SuXCeS laboratory Introduction Cytochrome P450 is the collective name for a distinct group of protoheme containing proteins that show a Soret absorption band at around 450 nm (448 to 452 nm) in the CO-difference spectrum of dithionite-reduced sample. 450 represent a large group of hemethiolate enzymes that exhibit remarkably diverse activities for the metabolism of numerous endogenous and exogenous chemicals [1]. Some plant extracts such as leaves of Helietta apiculata [2] and grape fruit juices [3] have been documented to have certain effects on the activity of cytochrome P450. Cytochrome P450 is responsible for the metabolism of a large proportion of drugs [1]. Whenever two or more drugs are administered concurrently, the possibility of drug interaction exist [4]. Drug-drug interactions can be explained by alterations in the metabolic enzymes that are present in the liver and other extrahepatic tissues. Many of the major pharmacokinetic interactions between drugs are due to hepatic cytochrome P450 (P450 or CYP) enzymes being affected by previous administration of other drugs. After coadministration, some drugs act as potent enzyme inducers, whereas others as inhibitors [5].In this study, the effect of bitter gourd (Momordica charantia), ‘tempeh', nicotine and caffeine on liver metabolizing enzymes were assessed. Bitter gourd is a well known tropical vegetable in South East Asia. ‘Tempeh' also known as soy cake is made from fermented soy beans and is widely consumed in daily diet in Malaysia and Indonesia. Nicotine is a major substance found in tobacco while caffeine is found in coffee, soft drinks and other beverages. The effects of these chosen sample extracts on the activity of liver metabolizing enzyme cytochrome P450, were determined by measuring the sleeping time induced by pentobarbitone. Pentobarbitone is known to be metabolized by cytochrome P450 [6]. This study also investigated the effects of different doses of these sample extracts in affecting activity of the liver metabolizing enzymes. This was done as the literature has reported that metabolic drug interaction may depend on the magnitude of the change in the concentration of active species (parent drug and/or active metabolites) at the site of pharmacological action and the therapeutic index of the drug. The smaller the difference between toxic and effective concentration, the greater the likelihood that the drug interaction will have serious clinical consequences [7]. Materials and methods MaterialsThe study was carried out on mice (2 batches of 7 groups (10 mice per group)). The mice were maintained under standard laboratory conditions of food and water before the start of the experiment. The handling of mice was conducted in accordance with the Guiding Principles in the Use of Animals in Toxicology, which was adopted by the
机译：目的：确定植物提取物，尼古丁和咖啡因对戊巴比妥诱导的肝脏代谢酶活性的影响。材料和方法：七组小鼠用高剂量样品提取物（0.4 mg / g体重样品提取物，但尼古丁含量为0.1 mg / g体重）预处理，而一组对照组用盐水预处理。在第5天，施用戊巴比妥（0.005ml，8mg / ml）并确定睡眠时间。重复测试，但剂量低（0.1 mg / g体重的样品提取物，但尼古丁浓度为0.05mg / g的体重）。结果：与对照相比，高剂量的苦瓜，'tempeh'，尼古丁，咖啡因，尼古丁+苦瓜，尼古丁+'tempeh'和尼古丁+咖啡因显着诱导了肝脏代谢酶的活性。在低剂量下，苦瓜，尼古丁，咖啡因，尼古丁+苦瓜，尼古丁+'tempeh'和尼古丁+咖啡因诱导了该酶，但'tempeh'却没有。结论：研究结果表明，苦瓜，尼古丁和咖啡因可作为酶的诱导剂，但'tempeh'仅在高剂量时显示出这种能力。支持来源：马来亚大学SuXCeS实验室简介细胞色素P450是一组独特的含有原血红素的蛋白质的总称，该蛋白质在连二亚硫酸盐还原的CO差异光谱中显示约450 nm（448至452 nm）的Soret吸收带。样品。 450代表一大批异丁酸酶，它们对许多内源性和外源性化学物质的代谢表现出明显不同的活性[1]。一些植物提取物，例如Helietta apiculata的叶子[2]和葡萄汁[3]已被证明对细胞色素P450的活性有一定的影响。细胞色素P450负责大部分药物的代谢[1]。每当同时使用两种或多种药物时，就存在药物相互作用的可能性[4]。药物相互作用可以通过肝脏和其他肝外组织中存在的代谢酶的改变来解释。药物之间的许多主要药代动力学相互作用是由于肝细胞色素P450（P450或CYP）酶受到其他药物先前给药的影响。共同给药后，某些药物可作为有效的酶诱导剂，而另一些则可作为抑制剂[5]。在本研究中，评估了苦瓜（Momordica charantia），'tempeh'，尼古丁和咖啡因对肝脏代谢酶的作用。苦瓜是东南亚著名的热带蔬菜。 “ Tempeh”也称为大豆蛋糕，是由发酵大豆制成的，在马来西亚和印度尼西亚的日常饮食中广泛食用。尼古丁是烟草中发现的主要物质，而咖啡因则存在于咖啡，软饮料和其他饮料中。通过测量戊巴比妥诱导的睡眠时间来确定这些选定的样品提取物对肝脏代谢酶细胞色素P450活性的影响。已知戊巴比妥被细胞色素P450代谢[6]。这项研究还研究了不同剂量的这些样品提取物对肝脏代谢酶活性的影响。这样做是因为文献报道了代谢药物的相互作用可能取决于药理作用部位的活性物质（母体药物和/或活性代谢物）浓度变化的幅度和药物的治疗指数。毒性和有效浓度之间的差异越小，药物相互作用产生严重临床后果的可能性就越大[7]。材料和方法材料研究是在小鼠（2批，每组7组，每组10只）上进行的。在实验开始之前，将小鼠维持在食物和水的标准实验室条件下。小鼠的处理是根据《动物学在毒理学中使用的指导原则》进行的。

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