New Insights into the Metabolic Profile and Cytotoxic Activity of Kigelia africana Stem Bark.

IF 4.2 2区 化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Dimitrina Zheleva-Dimitrova, Rositsa Mihaylova, Maria Nikolova, Nisha Singh, Spiro Konstantinov
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Abstract

Ultra-high-performance liquid chromatography coupled to Orbitrap high-resolution mass spectrometry (UHPLC-HRMS) was recently employed in many fields to obtain a rapid characterization of plant extracts. Kigelia africana (family Bignoniaceae) is a quintessential African herbal medicinal plant with immense indigenous medicinal and non-medicinal applications. The aim of the present research was to obtain an in-depth metabolite profiling of the K. africana stem bark extract using UHPLC-HRMS and to conduct a preliminary screening of its anticancer activity against a panel of malignant human cell lines of different origin. The UHPLC-HRMS analysis revealed 63 secondary metabolites including phenolic acids, gallo- and ellagitannins, iridoids, naphthoquinones, and anthraquinones. A total of 34 of all annotated compounds are reported for the first time in K. africana stem bark. The studied profile was dominated by trimethylellagic acid, dimethylellagic acid isomers, and ellagic acid. In all tumor models, we established a pronounced inhibition of cell growth in a mostly dose-dependent manner, with IC50 values ranging near and well below (4-30 µg/mL) the lowest treatment concentration of 25 µg/mL. The established cytotoxicity profile of the K. africana extract, highly biased toward malignantly transformed but not normal cells, suggests specific modulation of defined molecular tumor targets. This study revealed K. africana stem bark as a new source of gallo- and ellagitannins, and highlighted the studied herbal drug as an antiproliferative agent with potential pharmaceutical application.

非洲桂树茎皮代谢特征和细胞毒活性的新认识。
近年来,超高效液相色谱-高分辨率质谱联用技术(UHPLC-HRMS)被广泛应用于植物提取物的快速表征。非洲大戟属(大戟科)是一种典型的非洲草本药用植物,具有巨大的本土药用和非药用应用。本研究的目的是利用UHPLC-HRMS对非洲栎树皮提取物进行深入的代谢物分析,并对其对不同来源的恶性人类细胞系的抗癌活性进行初步筛选。UHPLC-HRMS分析发现了63种次生代谢物,包括酚酸、五gallo和鞣花单宁、环烯醚萜类、萘醌类和蒽醌类。其中34种化合物为首次在非洲栎茎皮中发现。研究的图谱以三甲基鞣花酸、二甲基鞣花酸异构体和鞣花酸为主。在所有肿瘤模型中,我们以剂量依赖的方式建立了对细胞生长的明显抑制,IC50值接近或远低于最低处理浓度25µg/mL(4-30µg/mL)。已建立的非洲蓟提取物的细胞毒性谱,高度偏向于恶性转化而不是正常细胞,表明特定的分子肿瘤靶标调节。本研究揭示了非洲栎树皮是一种新的甘露单宁和鞣花单宁的来源,并强调了所研究的草药作为一种具有潜在药用价值的抗增殖剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Molecules
Molecules 化学-有机化学
CiteScore
7.40
自引率
8.70%
发文量
7524
审稿时长
1.4 months
期刊介绍: Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.
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