バジフンギン

バジフンギン 化学特性,用途語,生産方法

• 効能

  抗真菌薬

• 使用

  Basifungin, also known as aureuobacidin A, is an orally available cyclic depsipeptide antibiotic produced by Aureobasidium pullulans that is a fungicide at low concentrations. Aureobasidin A inhibits inositol phosphorylceramide synthase, an enzyme that catalyzes a key step in fungal sphingolipid biosynthesis. This may inhibit fungal cell growth.

• 定義

  ChEBI: Basifungin is a cyclodepsipeptide antibiotic, which is isolated from the filamentous fungus Aureobasidium pullulans R106 and is toxic to yeast at low concentrations (0.1-0.5 ug/ml).

• 臨床応用

  Aureobasidin A (Basifungin) is a cyclic depsipeptide that is produced byfermentation in cultures of Aureobasidium pullulan.Aureobasidin A acts as a tight-binding noncompetitive inhibitorof the enzyme inositol phosphorylceramide synthase(IPC synthase), which is an essential enzyme for fungalsphingolipid biosynthesis. A unique structural feature of theaureobasidins is the N-methylation of four of seven amide nitrogenatoms. The lack of tautomerism dictated by N-methylationmay contribute to forming a stable solution conformerthat is shaped somewhat like an arrowhead, the presumed biologicallyactive conformation of aureobasidin-A.The pradimycins and benanomycins are naphthacenequinonesthat bind mannan in the presence of Ca²⁺ to disrupt the cell membrane in pathogenic fungi. Both demonstrate good in vitro and in vivo activity againstCandida spp. and C. neoformans clinical isolates.

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