正交体烷 A-E，β-咔啉生物碱，来自澳大利亚采集的苔藓动物。

Orthoscuticellines A-E, β-Carboline Alkaloids from the Bryozoan Collected in Australia.

机构信息

Environmental Futures Research Institute , Griffith University , Gold Coast , QLD 4222 , Australia.

Griffith Institute for Drug Discovery , Griffith University , Brisbane , QLD 4111 , Australia.

出版信息

J Nat Prod. 2020 Feb 28;83(2):422-428. doi: 10.1021/acs.jnatprod.9b00933. Epub 2020 Jan 21.

DOI:10.1021/acs.jnatprod.9b00933

PMID:31961680

Abstract

Antiplasmodial high-throughput screening of extracts derived from marine invertebrates collected from northern NSW, Australia, resulted in the methanol extract of the bryozoan being identified as inhibitory toward the 3D7 strain of . Purification of this extract resulted in two new bis-β-carbolines that possess a cyclobutane moiety, orthoscuticellines A and B ( and ), three new β-carboline alkaloids, orthoscuticellines C-E (-), and six known compounds, 1-ethyl-4-methylsulfone-β-carboline (), 1-ethyl-β-carboline (), 1-acetyl-β-carboline () 1-(1'-hydroxyethyl)-β-carboline (), 1-methoxycarbonyl-β-carboline (), and 1-vinyl-β-carboline (). The structures of all compounds were determined from analysis of MS and 1D and 2D NMR data. The compounds showed modest antiplasmodial activity against in the range of 12-21 μM.

摘要

从澳大利亚新南威尔士州北部采集的海洋无脊椎动物提取物进行抗疟原虫高通量筛选，结果表明苔藓动物甲醇提取物对 3D7 株具有抑制作用。该提取物的纯化得到了两个具有环丁烷部分的新双-β-咔啉，即正交斯卡汀 A 和 B（和），三个新的β-咔啉生物碱，正交斯卡汀 C-E（-），以及六个已知化合物，1-乙基-4-甲砜基-β-咔啉（），1-乙基-β-咔啉（），1-乙酰基-β-咔啉（）1-（1'-羟基乙基）-β-咔啉（），1-甲氧基羰基-β-咔啉（）和 1-乙烯基-β-咔啉（）。所有化合物的结构均通过分析 MS 和 1D 和 2D NMR 数据确定。这些化合物对显示出中等的抗疟原虫活性，范围为 12-21 μM。