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Investigations into the mechanism of action and antifungal activity of the botanical coumarin surangin B.

机译：植物香豆素素蓝素B的作用机理和抗真菌活性的研究

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摘要

The mechanism of action of surangin B, a coumarin from the roots of Mammea longifolia, was examined in bovine heart mitochondria and mouse brain synaptosomal preparations. The potential antifungal activity of surangin B was also investigated.; Complexes II, III and IV of bovine heart mitochondria were strongly inhibited by surangin B, but complex I was insensitive to this compound. Analysis of surangin B's inhibition of complex II used submitochondrial particles. Surangin B displayed non-competitive kinetics when either succinate or decylubiquinone were used as substrates: indicating that it binds to a site which is distinct from both the succinate binding site and the domain responsible for interacting with ubiquinone. Difference spectra of reduced complex III equilibrated with surangin B closely paralleled those of antimycin A, but were very different to those of the selective Qo site inhibitors myxothiazol and famoxadone. Other experiments used the electron acceptor 2-nitrosofluorene, which intercepts electrons specifically from the Qi site. These experiments confirmed that like antimycin A, surangin B selectively blocks electron diversion to 2-nitrosofluorene through Qi within complex III.; Surangin B causes presynaptic release of both neurotransmitter and non-neurotransmitter amino acids from mouse brain synaptosomes. The stimulatory effect of surangin B and other complex III-specific inhibitors on amino acid release was inhibited by N,N,N',N'-tetramethyl- p-phenylenediamine suggesting that complex III blockade in mitochondria of the nerve ending is an important mechanism causing release.; Surangin B also inhibited in vitro mycelial growth and spore germination in several species of fungi. As an inhibitor of mycelial growth Surangin B showed strongest activity against Rhizoctonia solani (IC50 = 3.8 muM) and Botrytis cinerea (IC50 = 11.2 muM), but inhibitory effects were less pronounced in Alternaria dauci, Fusarium oxysporum and Penicillium sp. (IC50s > 30 muM) and absent in Trichoderma harzianum. Surangin B reduced the level of spore germination in Fusarium oxysporum (IC 50 = 2.3 muM) and Botrytis cinerea (IC50 = 1.4 muM), although Alternaria dauci was considerably more tolerant of this coumarin (IC50 = 500 muM). The activity of surangin B compared favorably with certain commercial fungicides indicating that coumarins of this type may have potential as an antifungal agents.
机译：在牛心脏线粒体和小鼠脑突触体制剂中研究了素菌素surangin B的作用机理。还研究了surangin B的潜在抗真菌活性。 surangin B强烈抑制牛心脏线粒体的复合物II，III和IV，但是复合物I对这种化合物不敏感。分析surangin B对复合物II的抑制作用，使用线粒体颗粒。当将琥珀酸酯或癸基泛醌用作底物时，Surangin B显示出非竞争性动力学：表明它与不同于琥珀酸酯结合位点和负责与泛醌相互作用的结构域的位点结合。与苏兰金B平衡的还原复合物III的差异光谱与抗霉素A的光谱极为相似，但与选择性Qo站点抑制剂myxothiazol和famoxadone的光谱差异很大。其他实验使用电子受体2-亚硝基芴，它专门拦截来自Qi位点的电子。这些实验证实，与抗霉素A一样，苏兰糖素B选择性地阻止电子通过络合物III中的Q 1转移至2-亚硝基芴。 Surangin B引起小鼠脑突触体中神经递质和非神经递质氨基酸的突触前释放。 N，N，N'，N'-四甲基-对苯二胺抑制了surangin B和其他复杂的III型特异性抑制剂对氨基酸释放的刺激作用，表明神经末梢线粒体中的复杂III型阻断是重要的机制导致释放。 Surangin B还抑制了几种真菌的体外菌丝生长和孢子萌发。作为菌丝体生长的抑制剂，苏兰金B表现出最强的抗枯萎病菌（IC50 = 3.8μM）和灰葡萄孢（IC50 = 11.2μM）的活性，但对链格孢菌，尖孢镰刀菌和青霉菌的抑制作用较弱。 （IC50> 30μM），在哈茨木霉中不存在。 Surangin B降低了尖孢镰刀菌（IC 50 = 2.3μM）和灰葡萄孢（IC50 = 1.4μM）中孢子萌发的水平，尽管紫胶链球菌对该香豆素的耐受性要强得多（IC50 = 500μM）。与某些商业杀菌剂相比，surangin B的活性优越，表明该类型的香豆素可能具有作为抗真菌剂的潜力。

著录项

  • 作者

    Deng, Yanshen.;

  • 作者单位

    Simon Fraser University (Canada).;

  • 授予单位 Simon Fraser University (Canada).;
  • 学科 Health Sciences Pharmacology.; Chemistry Biochemistry.
  • 学位 Ph.D.
  • 年度 2005
  • 页码 147 p.
  • 总页数 147
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药理学;生物化学;
  • 关键词

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