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甘草次酸在 C-30 位的转化及其对抗肿瘤活性的影响。

Conversions at C-30 of glycyrrhetinic acid and their impact on antitumor activity.

机构信息

Martin-Luther-Universität Halle-Wittenberg, Bereich Organische Chemie, Halle (Saale), Germany.

出版信息

Arch Pharm (Weinheim). 2012 Mar;345(3):223-30. doi: 10.1002/ardp.201100046. Epub 2011 Oct 14.

DOI:10.1002/ardp.201100046
PMID:21997717
Abstract

The extracts of the roots of licorice have been used in traditional and folk medicine to treat a broad variety of maladies. The main ingredient of these extracts is glycyrrhicinic acid. Its aglycon, glycyrrhetinic acid, has many biological activities, among them a pronounced cytotoxicity against tumor cells. In this study we varied glycyrrhetinic acid at position C-30 to get "simple" derivatives, for example esters, amides and a nitrile. The influence of these changes on the cytotoxic activity is noteworthy and was determined by a colorimetric sulphorhodamine B test using 7 human tumor cell lines and mouse embryonic fibroblasts (NIH3T3) for comparison. A Trypan blue test as well as an acridine orange/ethidium bromide test was used to discover the ability of the compounds to induce apoptosis.

摘要

甘草根提取物在传统和民间医学中被用于治疗多种疾病。这些提取物的主要成分是甘草酸。其苷元甘草次酸具有许多生物活性,其中对肿瘤细胞具有明显的细胞毒性。在这项研究中,我们在 C-30 位改变了甘草次酸,得到了“简单”的衍生物,例如酯、酰胺和腈。这些变化对细胞毒性的影响值得注意,并通过使用 7 个人类肿瘤细胞系和小鼠胚胎成纤维细胞(NIH3T3)进行比较的比色磺基罗丹明 B 试验来确定。使用台盼蓝试验和吖啶橙/溴化乙锭试验来发现化合物诱导细胞凋亡的能力。

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