Uncoupling and Antioxidant Effects of Ursolic Acid in Isolated Rat Heart Mitochondria
Uncoupling and Antioxidant Effects of Ursolic Acid in Isolated Rat Heart Mitochondria
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DOI：
10.1021/np200060p
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发表时间：
2011-07-01
影响因子：
5.1
通讯作者：
Bernatoniene, Jurga
中科院分区：
文献类型：
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作者：
Liobikas, Julius;Majiene, Daiva;Bernatoniene, Jurga
熊果酸(1)是一种五环三萜酸，是一些传统药用植物的主要成分之一，具有抗炎、抗氧化、细胞毒活性等广泛的生物学活性。此外，在用于心脏病患者的商业草药制剂中，当1的浓度为1.6-5 ng/ml时，也可能发挥促心脏活性。有几种间接的暗示，熊果酸的心脏保护机制可能涉及线粒体；然而，其作用机制仍不清楚。因此，我们研究了0.4-200 ng/mL熊果酸(1)对大鼠心脏线粒体氧化丙酮酸、苹果酸、琥珀酸或棕榈酸-肉碱+苹果酸功能的影响。结果发现，1诱导了氧化磷酸化的解偶联作用。与5 ng/mL1孵育后，线粒体中H202的产生显著减少。这一作用与经典解偶联剂3-氯苯肼的效果相当。由于轻度线粒体解偶联被认为是心脏保护的机制之一，目前的结果表明熊果酸(1)具有潜在的心脏保护化合物的用途。
Ursolic acid (1), a pentacyclic triterpene acid, is one of the major components of certain traditional medicinal plants and possesses a wide range of biological effects, such as anti-inflammatorr, antioxidative, and cytotoxic activities. Furthermore, 1, when present at 1.6-5 ng/mL concentrations in commercial herbal preparations used for patients with cardiac disorders, may also exert pro-cardiac activities. There are several indirect suggestions that the cardioprotective mechanism of ursolic acid could involve the mitochondria; however the of action is still not known. Therefore, the effects of 0.4-200 ng/mL ursolic acid (1) on the functions of isolated rat heart mitocho.ndria oxidizing either pyruvate and malate, succinate, or palmitoyk-carnitine plus malate were investigated. It was found that 1 induced a statistically significant uncoupling of oxidative phosphorylation. A statistically significant decrease in H202 production in the mitochondria was observed after incubation with 5 ng/mL 1. This effect was comparable to the effectiveness of the classical uncoupler carbonyl cyanide 3-chlorophenylhydrazone. Since mild mitochondria] uncoupling has been proposed as one of the mechanisms of cardioprotection, the present results indicate that ursolic acid (1) has potential use as a cardioprotective compound.