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Evidence for the mechanism of action of the antifungal phytolaccoside B isolated from Phytolacca tetramera Hauman.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2008 Oct , DOI: 10.1021/np070660i
Andrea Escalante 1 , Martha Gattuso 1 , Pilar Pérez 1 , Susana Zacchino 1
Affiliation  

Phytolaccoside B (1), an antifungal monodesmoside triterpenoid glycoside isolated from berries of Phytolacca tetramera Hauman (Phytolaccaceae), alters the morphology of yeasts and molds. The malformations were similar to those produced by enfumafungin, a known inhibitor of (1-->3)-beta-D-glucan synthase, an enzyme that catalyzes the synthesis of (1-->3)-beta-D-glucan, one of the major polymers of the fungal cell wall. However, enzymatic assays revealed that 1 did not inhibit (1-->3)-beta-D-glucan synthase, but it did produce a notable enhancement of the chitin synthase 1 activity and, concomitantly, a rise in chitin, another important polymer of the fungal cell walls. This finding was corroborated by fluorescence microscopy and also by quantification of the chitin. In addition, a 2-fold increase in the thickness of the fungal cell wall was observed with transmission electronic microscopy. On the other hand, 1 neither bound to ergosterol nor caused hemolysis of red blood cells, although some fungal membrane damage was observed at the MIC of 1.

中文翻译:

从四倍体植物Phytolacca tetramera Hauman分离出的抗真菌植物性糖苷B的作用机理的证据。

phytolaccoside B(1)是一种抗真菌的单去糖苷三萜糖苷,它是从Phytolacca tetramera Hauman(Phytolaccaceae)的浆果中分离出来的,可改变酵母和霉菌的形态。畸形类似于恩富玛芬净(已知的(1-> 3)-β-D-葡聚糖合酶抑制剂,一种催化(1-> 3)-β-D-葡聚糖合成的酶)产生的畸形。真菌细胞壁的主要聚合物之一。但是,酶法测定显示1不会抑制(1-> 3)-β-D-葡聚糖合酶,但确实会显着提高几丁质合酶1的活性,并随之增加另一种重要的聚合物几丁质。真菌细胞壁。荧光显微镜和几丁质的定量证实了这一发现。此外,用透射电子显微镜观察到真菌细胞壁厚度增加了2倍。另一方面,尽管在MIC为1时观察到一些真菌膜损伤,但1既不结合麦角固醇也不引起红细胞溶血。
更新日期:2017-01-31
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