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海洋海绵 sp. 的 dysidenin 影响幼虫的体外运动和形态。

Dysidenin from the Marine Sponge sp. Affects the Motility and Morphology of Larvae In Vitro.

机构信息

Griffith Institute for Drug Discovery, School of Environment and Science, Griffith University, Brisbane, QLD 4111, Australia.

Department of Veterinary Biosciences, Faculty of Veterinary and Agricultural Sciences, Melbourne Veterinary School, The University of Melbourne, Parkville, VIC 3010, Australia.

出版信息

Mar Drugs. 2021 Dec 9;19(12):698. doi: 10.3390/md19120698.

DOI:10.3390/md19120698
PMID:34940697
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8708643/
Abstract

High-throughput screening of the NatureBank marine extract library ( = 7616) using a phenotypic assay for the parasitic nematode identified an active extract derived from the Australian marine sponge sp. Bioassay-guided fractionation of the CHCl/MeOH extract from sp. resulted in the purification of two known hexachlorinated peptides, dysidenin () and dysideathiazole (). Compound inhibited the growth/development of larvae and induced multiple phenotypic changes, including a lethal evisceration () phenotype and/or somatic cell and tissue destruction. This is the first report of anthelmintic activity for these rare and unique polychlorinated peptides.

摘要

高通量筛选 NatureBank 海洋提取物文库(=7616),使用寄生线虫的表型测定法,鉴定出一种来源于澳大利亚海洋海绵 sp. 的活性提取物。从 sp. 的 CHCl/MeOH 提取物进行生物活性导向分离,导致两种已知的六氯肽的纯化,即 dysidenin () 和 dysideathiazole ()。化合物 抑制 幼虫的生长/发育,并诱导多种表型变化,包括致命的内脏暴露 ()表型和/或体细胞和组织破坏。这是这些罕见且独特的多氯化肽具有驱虫活性的首次报道。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/464e42c48475/marinedrugs-19-00698-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/4258972061c2/marinedrugs-19-00698-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/bb8401a8289f/marinedrugs-19-00698-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/464e42c48475/marinedrugs-19-00698-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/4258972061c2/marinedrugs-19-00698-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/bb8401a8289f/marinedrugs-19-00698-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f499/8708643/464e42c48475/marinedrugs-19-00698-g003.jpg

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本文引用的文献

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2
High-Throughput Phenotypic Assay to Screen for Anthelmintic Activity on .高通量表型分析用于筛选对……的驱虫活性
Pharmaceuticals (Basel). 2021 Jun 26;14(7):616. doi: 10.3390/ph14070616.
3
Advances in the discovery and development of anthelmintics by harnessing natural product scaffolds.
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Adv Parasitol. 2021;111:203-251. doi: 10.1016/bs.apar.2020.10.002. Epub 2021 Jan 8.
4
Screening for Small Molecule Inhibitors of BMP-Induced Osteoblastic Differentiation from Indonesian Marine Invertebrates.从印度尼西亚海洋无脊椎动物中筛选 BMP 诱导成骨分化的小分子抑制剂。
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Pathogens. 2020 Jul 9;9(7):550. doi: 10.3390/pathogens9070550.
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