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黄芪皂苷酸：一种使用极为简单的TEMPO介导氧化法制备的黄芪甲苷IV新型水溶性衍生物。

Astragalosidic Acid: A New Water-Soluble Derivative of Astragaloside IV Prepared Using Remarkably Simple TEMPO-Mediated Oxidation.

作者信息

Qing Lin-Sen, Peng Shu-Lin, Liang Jian, Ding Li-Sheng

机构信息

Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.

出版信息

Molecules. 2017 Jul 31;22(8):1275. doi: 10.3390/molecules22081275.

DOI:10.3390/molecules22081275
PMID:28758976
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6152088/
Abstract

There is an urgent need for a water-soluble derivative of astragaloside IV for drug R&D. In the present study, a remarkably simple method for the preparation of such a water-soluble derivative of astragaloside IV has been developed. This protocol involves oxidative 2,2,6,6-tetramethylpiperidine-1-oxyl free radical (TEMPO)-mediated transformation of astragaloside IV to its carboxylic acid derivative, which is a new compound named astragalosidic acid. The structure of astragalosidic acid was elucidated by means of spectroscopic analysis. Its cardioprotective activity was investigated using an in vitro model of cardiomyocyte damage induced by hypoxia/reoxygenation in H9c2 cells. The oxidative TEMPO-mediated transformation proposed in the present study could be applied to other natural saponins, offering an effective and convenient way to develop a new compound with greatly improved structure-based druggability.

摘要

迫切需要一种用于药物研发的黄芪甲苷IV水溶性衍生物。在本研究中，已开发出一种制备黄芪甲苷IV水溶性衍生物的极为简单的方法。该方案涉及通过氧化2,2,6,6-四甲基哌啶-1-氧基自由基（TEMPO）介导将黄芪甲苷IV转化为其羧酸衍生物，这是一种名为黄芪苷酸的新化合物。通过光谱分析阐明了黄芪苷酸的结构。使用H9c2细胞中缺氧/复氧诱导的心肌细胞损伤体外模型研究了其心脏保护活性。本研究中提出的氧化TEMPO介导的转化可应用于其他天然皂苷，为开发具有基于结构的药物可及性大大提高的新化合物提供了一种有效且便捷的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/9678e0106969/molecules-22-01275-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/13395af16262/molecules-22-01275-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/b189a2c2e710/molecules-22-01275-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/635e928c12fe/molecules-22-01275-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/9678e0106969/molecules-22-01275-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/13395af16262/molecules-22-01275-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/b189a2c2e710/molecules-22-01275-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/635e928c12fe/molecules-22-01275-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/298a/6152088/9678e0106969/molecules-22-01275-g004.jpg

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本文引用的文献

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2
Research review on the pharmacological effects of astragaloside IV.黄芪甲苷IV药理作用的研究综述
Fundam Clin Pharmacol. 2017 Feb;31(1):17-36. doi: 10.1111/fcp.12232. Epub 2016 Sep 23.
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Rg1 prevents myocardial hypoxia/reoxygenation injury by regulating mitochondrial dynamics imbalance via modulation of glutamate dehydrogenase and mitofusin 2.
黄芪甲苷衍生物与人血清白蛋白的结合机制及其对斑马鱼胚胎心脏毒性的阐明。
Front Pharmacol. 2022 Sep 23;13:987882. doi: 10.3389/fphar.2022.987882. eCollection 2022.
4
The Astragaloside IV Derivative LS-102 Ameliorates Obesity-Related Nephropathy.黄芪甲苷衍生物 LS-102 可改善肥胖相关性肾病。
Drug Des Devel Ther. 2022 Mar 14;16:647-664. doi: 10.2147/DDDT.S346546. eCollection 2022.
5
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Eur J Drug Metab Pharmacokinet. 2019 Apr;44(2):251-259. doi: 10.1007/s13318-018-0515-5.
人参皂苷Rg1通过调节谷氨酸脱氢酶和线粒体融合蛋白2来调控线粒体动力学失衡，从而预防心肌缺氧/复氧损伤。
Mitochondrion. 2016 Jan;26:7-18. doi: 10.1016/j.mito.2015.11.003. Epub 2015 Nov 24.
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Pharmacological effects of Astragaloside IV: a literature review.黄芪甲苷的药理作用：文献综述。
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