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来自 sp. IRD-009 的普拉地米星-IRD 及其抗微生物和细胞毒性活性。

Pradimicin-IRD from sp. IRD-009 and its antimicrobial and cytotoxic activities.

机构信息

a Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto , Universidade de São Paulo , Ribeirão Preto , Brazil.

b Departamento de Química Orgânica e Inorgânica , Universidade Federal do Ceará , Fortaleza , Brazil.

出版信息

Nat Prod Res. 2019 Jun;33(12):1713-1720. doi: 10.1080/14786419.2018.1434639. Epub 2018 Feb 16.

Abstract

A new polycyclic antibiotic, pradimicin-IRD, was isolated from actinobacteria sp. IRD-009 recovered from soil of Brazilian rainforest undergoing restoration area. This molecule is the major compound produced in solid culture media. The new compound was detected by a focused method of precursor ion (high-performance liquid chromatography coupled to tandem mass spectrometer) developed previously to identify unusual aminoglycosyl sugar moieties. The compound was isolated and its structure was, therefore, elucidated by high-resolution mass spectrometry, and 1D and 2D nuclear magnetic resonance experiments. Pradimicin-IRD displayed potential antimicrobial activity against (MIC 3.1 μg/mL), (MIC 3.1 μg/mL) and (MIC 3.1 μg/mL), and also cytotoxicity against tumour and non-tumour cell lines with IC values ranging from 0.8 μM in HCT-116 colon carcinoma cells to 2.7 μM in MM 200 melanoma cells. Particularly, these biological properties are described for the first time for this chemical class.

摘要

一种新型多环抗生素——普拉地霉素-IRD,从巴西雨林恢复区土壤中分离出的放线菌 sp.IRD-009 中分离得到。该分子是固体培养基中主要产生的化合物。该新化合物通过以前开发的前体离子(高效液相色谱与串联质谱联用)的聚焦方法检测到,用于鉴定不寻常的氨基糖苷糖部分。通过高分辨率质谱、一维和二维核磁共振实验对该化合物进行了分离和结构阐明。普拉地霉素-IRD 对 (MIC3.1μg/mL)、 (MIC3.1μg/mL)和 (MIC3.1μg/mL)表现出潜在的抗菌活性,并且对肿瘤和非肿瘤细胞系也具有细胞毒性,IC 值范围从结肠癌细胞 HCT-116 的 0.8μM 到黑色素瘤细胞 MM 200 的 2.7μM。特别是,这些生物学特性是首次在该化学类中描述的。

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