Division of Bioorganic Chemistry, School of Pharmacy, University of Saarland, Campus B2 1, D-66123 Saarbruecken, Germany; CNRS, UMR 7565, SRSMC, F-54506 Vandoeuvre-lès-Nancy, France; Université de Lorraine, UMR 7565, SRSMC, F-54506 Vandoeuvre-lès-Nancy, France; Laboratoire de Botanique et Ecologie Végétale, Université de Lomé, BP 1515 Lomé, Togo.
CNRS, UMR 7565, SRSMC, F-54506 Vandoeuvre-lès-Nancy, France; Université de Lorraine, UMR 7565, SRSMC, F-54506 Vandoeuvre-lès-Nancy, France.
J Ethnopharmacol. 2018 Feb 15;212:200-207. doi: 10.1016/j.jep.2017.10.020. Epub 2017 Nov 6.
Pterocarpus erinaceus has been chosen based on ethnobotanical surveys carried out in the Tchamba district of the Republic of Togo.
Investigation of the antibacterial as well as cytotoxic activities of whole extracts, fractions and compounds isolated from the leaves, trunk bark and roots of Pterocarpus erinaceus.
Bio-guided fractionation of the raw extracts of plant parts and subsequent isolation of compounds from active fractions using normal phase open column chromatography. The broth microdilution method was used to evaluate the antibacterial activity, based on the determination of Minimal Inhibitory Concentrations (MICs) against several bacterial species representative of the most commonly encountered infectious diseases worldwide. The cytotoxicity of the raw extract and the most active fractions on a human non-cancerous cell (namely MRC-5) was estimated with a MTT assay. The chemical structure of the compounds isolated was elucidated using a combination of advanced Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS).
All extracts and fractions tested have shown good activities against Gram-positive bacteria (including Methicillin-Resistant Staphylococcus aureus, MRSA) and against Pseudomonas aeruginosa with MIC values ranging from 32µg/mL to 256µg/mL. In contrast, extracts were not toxic to MRC-5 cells. Four compounds have been isolated: Compound 1 (friedeline); Compound 2 (2,3 dihydroxypropyloctacosanoate); Compound 3 (a mixture of β-sitosterol, stigmasterol and campesterol); Compound 4 (β-sitosteryl-β-D-glucopyranoside) and shown to be active against some of the bacteria tested. They were active with MIC equal to 4µg/mL against strains of S. aureus (including MRSA). To the best of our knowledge, all of them except friedeline have never been reported in this plant species.
P. erinaceus is confirmed as a plant harboring promising antibacterial activity with activities against serious human pathogens at very low concentrations. Some of the compounds isolated are also active at concentrations as low as 4µg/mL and therefore, may provide new leads for the development of antibacterial agents.
多蕊苏木是根据在多哥共和国塔姆巴地区进行的民族植物学调查选择的。
研究多蕊苏木叶、干皮和根的全提取物、馏分和化合物的抗菌和细胞毒性活性。
对植物部分的粗提取物进行生物导向分离，然后使用正相开放柱色谱法从活性馏分中分离化合物。采用肉汤微量稀释法，根据对代表世界范围内最常见传染病的几种细菌的最小抑菌浓度（MIC）的测定，评价抗菌活性。MTT 测定法评估粗提取物和最活跃馏分对非癌细胞（即 MRC-5）的细胞毒性。通过先进的核磁共振（NMR）和质谱（MS）的组合，阐明了分离化合物的化学结构。
所有测试的提取物和馏分对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌，MRSA）和铜绿假单胞菌均表现出良好的活性，MIC 值范围为 32µg/mL 至 256µg/mL。相比之下，提取物对 MRC-5 细胞没有毒性。分离出四种化合物：化合物 1（friedeline）；化合物 2（2,3 二羟基丙基二十八烷酸酯）；化合物 3（β-谷甾醇、豆甾醇和菜油甾醇的混合物）；化合物 4（β-谷甾醇-β-D-吡喃葡萄糖苷），并证明对一些测试的细菌有效。它们对金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌）的 MIC 值等于 4µg/mL。据我们所知，除了 friedeline 之外，它们在该植物物种中从未有过报道。
多蕊苏木被证实为一种具有 promising antibacterial activity 的植物，对严重的人类病原体具有非常低的浓度活性。分离出的一些化合物在低至 4µg/mL 的浓度下也具有活性，因此可能为开发抗菌剂提供新的线索。
