Department of Family Medicine, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand.
Med Chem. 2009 Nov;5(6):583-8. doi: 10.2174/157340609790170443.
Previous studies presented evidence that plants contain antioxidants that have free radical-scavenging properties. Overproduction of free radicals leads to oxidative stress, a factor associated with a variety of diseases, such as diabetes. Cytochrome P450 2E1 enzymes (CYP2E1) are involved in drug metabolism in the liver and metabolism of DNA-reaction generating intra-mitochondrial ROS, which leads to micro- and macro-vascular pathology in diabetes. Plant-based chemicals can affect CYP2E1 enzymes and related defense mechanisms, possibly leading to protection against oxidative stress. We investigated the effect of Solanum torvum (ST) extracts on the inhibition of CYP2E1 activity in human liver microsomes. ST extract was analyzed for antioxidant activity by the ABTS method. Polyphenolic compounds were measured by the total phenol content using the Folin-Ciocalteau reagent. Flavonoid and tannin content were analyzed by standard methods. Oxidative stress was evaluated by measuring lipid peroxidation by TBARS and superoxide anion scavenging levels in plasma from diabetic patients. Results showed that 10 mg/ml of ST had CYP2E1 catalytic inhibiting activity (57.16 %). The IC50 value of CYP2E1 catalytic inhibiting activity level was 5.14 mg/ml by concentration in a dependent manner. One gram of concentrated ST extract had an antioxidant activity index of 3.68 mg of trolox and 360.53 mg of ascorbic acid equivalent. Effects on free radical-scavenging, as measured by TBARS and superoxide anion, showed IC50 values of 20.60 and 10.26 microg/ml, respectively. Polyphenolic compounds found included phenol, flavonoid and tannin, measuring 160.30, 104.36 and 65.91 mg/g, respectively. These results imply that ST is a natural source of polyphenolic antioxidants, which have cytochrome P450 2E1 enzyme inhibiting and free radical scavenging properties, as related to lipid peroxidation and superoxide anion activity. ST could potentially be used for reducing oxidative stress in diabetes. Study for usage as a conventional medicine, including dosage and chronic toxicity in humans, should be pursued.
先前的研究表明,植物中含有具有自由基清除特性的抗氧化剂。自由基的过度产生会导致氧化应激,这是与许多疾病(如糖尿病)相关的一个因素。细胞色素 P450 2E1 酶(CYP2E1)参与肝脏中的药物代谢和 DNA 反应生成的线粒体内部 ROS 的代谢,这导致糖尿病中的微血管和大血管病理学。植物化学物质可以影响 CYP2E1 酶和相关的防御机制,可能导致对氧化应激的保护。我们研究了 Solanum torvum(ST)提取物对人肝微粒体中 CYP2E1 活性抑制的影响。通过 ABTS 法分析 ST 提取物的抗氧化活性。使用 Folin-Ciocalteau 试剂通过总酚含量测量多酚化合物。通过标准方法分析类黄酮和单宁的含量。通过测量糖尿病患者血浆中的脂质过氧化产物 TBARS 和超氧阴离子清除水平来评估氧化应激。结果表明,10mg/ml 的 ST 具有 CYP2E1 催化抑制活性(57.16%)。CYP2E1 催化抑制活性水平的 IC50 值为 5.14mg/ml,呈浓度依赖性。一克浓缩的 ST 提取物的抗氧化活性指数为 3.68mg 生育三烯酚和 360.53mg 抗坏血酸当量。通过 TBARS 和超氧阴离子测定的自由基清除作用的影响,IC50 值分别为 20.60 和 10.26μg/ml。发现的多酚化合物包括苯酚、类黄酮和单宁,分别为 160.30、104.36 和 65.91mg/g。这些结果表明,ST 是多酚抗氧化剂的天然来源,具有细胞色素 P450 2E1 酶抑制和自由基清除特性,与脂质过氧化和超氧阴离子活性有关。ST 可能可用于减少糖尿病中的氧化应激。应该研究将其用作常规药物的用途,包括在人体中的剂量和慢性毒性。