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从红树林植物中靶向分离抗锥虫萘醌化合物

Targeted Isolation of Anti-Trypanosomal Naphthofuran-Quinone Compounds from the Mangrove Plant .

机构信息

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, The John Arbuthnott Building, 161 Cathedral Street, Glasgow G4 0RE, UK.

Faculty of Science and Marine Environment, Universiti Malaysia Terengganu, Kuala Nerus 21030, Terengganu, Malaysia.

出版信息

Mar Drugs. 2020 Dec 21;18(12):661. doi: 10.3390/md18120661.

DOI:10.3390/md18120661
PMID:33371387
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7767399/
Abstract

The discovery of new secondary metabolites from natural origins has become more challenging in natural products research. Different approaches have been applied to target the isolation of new bioactive metabolites from plant extracts. In this study, bioactive natural products were isolated from the crude organic extract of the mangrove plant collected from the east coast of Peninsular Malaysia in the Setiu Wetlands, Terengganu, using HRESI-LCMS-based metabolomics-guided isolation and fractionation. Isolation work on the crude extract used high-throughput chromatographic techniques to give two new naphthofuranquinone derivatives, hydroxyavicenol C () and glycosemiquinone (), along with the known compounds avicenol C (), avicequinone C (), glycoquinone (), taraxerone (), taraxerol (), β-sitosterol () and stigmasterol (). The elucidation and identification of the targeted bioactive compounds used 1D and 2D-NMR and mass spectrometry. Except for , all isolated naphthoquinone compounds () from the mangrove plant showed significant anti-trypanosomal activity on with MIC values of 3.12-12.5 μM. Preliminary cytotoxicity screening against normal prostate cells (PNT2A) was also performed. All compounds exhibited low cytotoxicity, with compounds and showing moderate cytotoxicity of 78.3% and 68.6% of the control values at 100 μg/mL, respectively.

摘要

从天然产物中发现新的次生代谢产物在天然产物研究中变得越来越具有挑战性。已经应用了不同的方法来从植物提取物中靶向分离新的生物活性代谢物。在这项研究中,从马来西亚半岛东海岸的赛丁湿地采集的红树林植物的粗有机提取物中,使用基于 HRESI-LCMS 的代谢组学指导的分离和分级,分离出生物活性天然产物。对粗提取物的分离工作使用了高通量色谱技术,得到了两种新的萘并呋喃醌衍生物,羟基阿维醇 C()和半醌(),以及已知化合物阿维醇 C()、阿维醌 C()、糖苷醌()、蒲公英酮()、蒲公英醇()、β-谷甾醇()和豆甾醇()。目标生物活性化合物的阐明和鉴定使用了 1D 和 2D-NMR 和质谱。除了 ,从红树林植物中分离出的所有萘醌化合物()均表现出对 显著的抗锥虫活性,MIC 值为 3.12-12.5 μM。还对正常前列腺细胞(PNT2A)进行了初步的细胞毒性筛选。所有化合物的细胞毒性均较低,化合物 和 对 100 μg/mL 时的细胞毒性分别为对照值的 78.3%和 68.6%。

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Antibacterial and antioxidant activity of naphthofuranquinones from the twigs of tropical mangrove .萘并呋喃醌类化合物的抑菌和抗氧化活性来自热带红树林的小枝。
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