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首页> 外文期刊>Parasitology >Role of mitochondria in the leishmanicidal effects and toxicity of acyl phloroglucinol derivatives: nemorosone and guttiferone A
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Role of mitochondria in the leishmanicidal effects and toxicity of acyl phloroglucinol derivatives: nemorosone and guttiferone A

机译：线粒体在酰基间苯三酚衍生物：nemorosone和guttiferone A的杀菌作用和毒性中的作用

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摘要

Nemorosone (Nem) and guttiferone A (GutA) are acyl phloroglucinol derivatives (APD) that are present in different natural products. For both compounds anti-cancer and anti-microbial properties have been reported. In particular, an anti-leishmanial activity of both compounds was demonstrated. The aim of this study was to explore the possible role of mitochondria in the anti-leishmanial activity of Nem and GutA in comparison with their action on mammalian mitochondria. Both APD inhibited the growth of promastigotes of Leishmania tarentolae (LtP) with half maximal inhibitory concentration (IC50) values of 0.67 +/- 0.17 and 6.2 +/- 2.6 mu M; while IC50 values for cytotoxicity against peritoneal macrophages from BALB/c mice were of 29.5 +/- 3.7 and 9.2 +/- 0.9 mu M, respectively. Nemorosone strongly inhibited LtP oxygen consumption, caused species-specific inhibition (P < 0.05) of succinate: ubiquinone oxidoreductase (complex II) from LtP-mitochondria and significantly increased (P < 0.05) the mitochondrial superoxide production. In contrast, GutA caused only a moderate reduction of respiration in LtP and triggered less superoxide radical production in LtP compared with Nem. In addition, GutA inhibited mitochondrial complex III in bovine heart submitochondrial particles, which is possibly involved in its mammalian toxicity. Both compounds demonstrated at low micromolar concentrations an effect on the mitochondrial membrane potential in LtP. The present study suggests that Nem caused its anti-leishmanial action due to specific inhibition of complexes II/III of mitochondrial respiratory chain of Leishmania parasites that could be responsible for increased production of reactive oxygen species that triggers parasite death.
机译：Nemorosone（Nem）和guttiferone A（GutA）是存在于不同天然产物中的酰基间苯三酚衍生物（APD）。对于这两种化合物，已经报道了抗癌和抗微生物特性。特别地，证明了两种化合物的抗利什曼活性。这项研究的目的是探讨线粒体与其在哺乳动物线粒体中的作用相比，在Nem和GutA的抗利什曼活性中的可能作用。两种APD均能抑制塔氏疟原虫（LtP）前鞭毛体的生长，最大抑制浓度（IC50）值的一半为0.67 +/- 0.17和6.2 +/- 2.6μM。而针对BALB / c小鼠腹膜巨噬细胞的细胞毒性IC50值分别为29.5 +/- 3.7和9.2 +/- 0.9μM。 Nemorosone强烈抑制LtP的耗氧量，引起LtP线粒体的琥珀酸盐：泛醌氧化还原酶（复合体II）对琥珀酸的物种特异性抑制（P <0.05），并显着增加（P <0.05）线粒体超氧化物的产生。相比之下，与Nem相比，GutA仅引起LtP呼吸的中度减少，并触发LtP中较少的超氧自由基产生。此外，GutA抑制牛心脏线粒体颗粒中的线粒体复合物III，这可能与其哺乳动物毒性有关。两种化合物均以低微摩尔浓度显示出对LtP中线粒体膜电位的影响。本研究表明，Nem引起其抗利什曼肽作用的原因是对利什曼原虫寄生虫线粒体呼吸链复合物II / III的特异性抑制，这可能导致触发寄生虫死亡的活性氧的产生增加。

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