Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, Yaoundé P.O. Box 812, Cameroon.
Department of Chemistry, Faculty of Science, University of Buea, Buea P.O. Box 63, Cameroon.
Molecules. 2022 Dec 12;27(24):8820. doi: 10.3390/molecules27248820.
Medicinal plants are known as sources of potential antimicrobial compounds belonging to different classes. The aim of the present work was to evaluate the antimicrobial potential of the crude extract, fractions, and some isolated secondary metabolites from the leaves of , a Cameroonian medicinal plant traditionally used for the treatment of microbial infections. Repeated column chromatography of the ethyl acetate and n-butanol fractions led to the isolation of seventeen previously known compounds (), among which three steroids (), one triterpene (), four flavonoids (), two stilbenoids ( and ) four ellagic acid derivatives (), one geraniinic acid derivative (), one coumarine (), and one glyceride (). Their structures were elucidated mainly by means of extensive spectroscopic and spectrometric (1D and 2D NMR and, MS) analysis and comparison with the published data. The crude extract, fractions, and isolated compounds were all screened for their antimicrobial activity. None of the natural compounds was active against strains. However, the crude extract, fractions, and compounds showed varying levels of antibacterial properties against at least one of the tested bacterial strains, with minimal inhibitory concentrations (MICs) ranging from 250 to 1000 μg/mL. The -butanol (-BuOH) fraction was the most active against ATCC 25922, with an MIC value of 250 μg/mL. Among the isolated compounds, schweinfurthin B () exhibited the best activity against NR 46003 with a MIC value of 62.5 μg/mL. In addition, schweinfurthin O () and isomacarangin () also exhibited moderate activity against the same strain with a MIC value of 125 μg/mL. Therefore, pharmacomodulation was performed on compound and three new semisynthetic derivatives () were prepared by allylation and acetylation reactions and screened for their in vitro antimicrobial activity. None of the semisynthetic derivatives showed antimicrobial activity against the same tested strains. The chemophenetic significance of the isolated compounds is also discussed in this paper.
药用植物被认为是具有不同类别潜在抗菌化合物的来源。本研究的目的是评估来自 Cameroonian 药用植物 的叶的粗提取物、馏分和一些分离的次生代谢产物的抗菌潜力,该植物传统上用于治疗微生物感染。乙酸乙酯和正丁醇馏分的反复柱层析导致分离出十七种先前已知的化合物(),其中三种甾体()、一种三萜()、四种类黄酮()、两种二苯乙烯(和)、四种鞣花酸衍生物()、一种 geraniinic 酸衍生物()、一种香豆素()和一种甘油酯()。它们的结构主要通过广泛的光谱和光谱(1D 和 2D NMR 和 MS)分析以及与已发表数据的比较来阐明。粗提取物、馏分和分离化合物均进行了抗菌活性筛选。没有一种天然化合物对 菌株具有活性。然而,粗提取物、馏分和化合物均表现出不同程度的抗至少一种测试细菌菌株的抗菌特性,最小抑菌浓度(MIC)范围为 250 至 1000μg/mL。正丁醇(-BuOH)馏分对 ATCC 25922 的活性最高,MIC 值为 250μg/mL。在分离的化合物中,schweinfurthin B()对 NR 46003 的活性最好,MIC 值为 62.5μg/mL。此外,schweinfurthin O()和异马卡林()对同一菌株也表现出中等活性,MIC 值为 125μg/mL。因此,对化合物 进行了药物修饰,并通过烯丙基化和乙酰化反应制备了三个新的半合成衍生物(),并对其体外抗菌活性进行了筛选。这些半合成衍生物对相同测试菌株均无抗菌活性。本文还讨论了分离化合物的化学生物学意义。