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丹酰脂素 A 衍生物的合成及生物活性。

Syntheses and Biological Activities of Danicalipin A Derivatives.

机构信息

Graduate School of Environmental Science, Hokkaido University, N10W5, Sapporo, 060-0810, Japan.

Chemistry Department, Universitas Islam Indonesia, Sleman, Yogyakarta, Indonesia.

出版信息

Chem Biodivers. 2023 Jun;20(6):e202300400. doi: 10.1002/cbdv.202300400. Epub 2023 May 9.

Abstract

Synthesis of three derivatives of danicalipin A, tetrachloride, trisulfate and a fluorescent probe was achieved through Wittig reaction strategy. Toxicity of the derivatives against brine shrimp (Artemia salina) as also investigated to provide useful information for the biological activity; i) less chloride derivative showed similar toxicity to danicalipin A, ii) the amphiphilic property, a characteristic feature of danicalipin A, was crucial because trisulfate considerably decreased the toxicity and iii) fluorescent derivative kept brine shrimp toxicity of danicalipin A.

摘要

通过威蒂希反应策略,成功合成了三种达卡脂素 A 的衍生物,包括四氯化物、三硫酸盐和荧光探针。还研究了衍生物对卤虫(盐水丰年虾)的毒性,为生物活性提供了有用的信息;i)含氯较少的衍生物表现出与达卡脂素 A 相似的毒性,ii)两亲性是达卡脂素 A 的特征,因此三硫酸盐显著降低了毒性,iii)荧光衍生物保持了达卡脂素 A 对卤虫的毒性。

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