Department of Chemistry, Tshwane University of Technology, Pretoria, 0001, South Africa.
Department of Chemistry, Rhodes University, Makhanda (Grahamstown), 6140, South Africa.
BMC Complement Med Ther. 2022 Mar 25;22(1):90. doi: 10.1186/s12906-022-03571-8.
Euphorbia grandicornis is widely utilized in traditional medicine for the treatment of microbial infections including sexually transmitted diseases such as syphilis, gonorrhoea and for healing of wounds.
The aim of this work was to isolate and evaluate the antibacterial and anticancer activities of Euphorbia grandicornis chemical constituents.
Chemical constituents were isolated and identified using various spectroscopic techniques such as IR, MS, and NMR. The single point growth inhibitory potential of the compounds was determined using a 96-well plate based assay.
The CHCl crude extracts exhibited potent antibacterial activity against Escherichia coli ATCC 8739 and Staphylococcus aureus ATCC 6538 with percentage growth of 94.90 ± 4.24 and 29.47 ± 4.89 respectively. Hence, the CHCl crude extract was further subjected to column chromatography which resulted in the isolation of methyl 2,5-dihydroxybenzoate (1), n-octyl benzoate (2), friedelanol (3), and germanicol (4) and identification of compounds 12-24 for the first time in the species based on the LC-MS/MS spectroscopic data. The purified compounds (1-4), and previously reported compounds (5-11) were evaluated for antibacterial activities against S. aureus and E. coli, as well as the cytotoxicity effects against HeLa cells. Of the purified compounds, methyl 2,5-dihydroxybenzoate (1), was the most active against E.coli and S. aureus with a percentage growth of 19.12 ± 0.65 and 23.32 ± 0.23 respectively. β-amyrin (6), and β-sitosterol (8), were active against S. aureus with percentage growth of 27.17 ± 0.07, and 47.79 ± 2.99 respectively.
The results obtained from this study indicate that E. grandicornis, is a rich source of chemical constituents that may provide new lead compounds for the development of antibacterial agents.
大飞扬草在传统医学中被广泛用于治疗微生物感染，包括梅毒、淋病等性传播疾病以及伤口愈合。
本工作旨在分离和评估大飞扬草的化学成分的抗菌和抗癌活性。
采用各种光谱技术，如 IR、MS 和 NMR，分离和鉴定化学成分。使用基于 96 孔板的测定法测定化合物的单点生长抑制潜力。
CHCl 粗提取物对大肠杆菌 ATCC 8739 和金黄色葡萄球菌 ATCC 6538 表现出很强的抗菌活性，其生长百分比分别为 94.90±4.24%和 29.47±4.89%。因此，进一步对 CHCl 粗提取物进行柱层析，分离得到了 2,5-二羟基苯甲酸甲酯（1）、正辛基苯甲酸酯（2）、friedelanol（3）和 germanicol（4），并根据 LC-MS/MS 光谱数据首次鉴定了化合物 12-24。对纯化化合物（1-4）和以前报道的化合物（5-11）进行了抗菌活性评价，包括对金黄色葡萄球菌和大肠杆菌的活性，以及对 HeLa 细胞的细胞毒性作用。在纯化的化合物中，2,5-二羟基苯甲酸甲酯（1）对大肠杆菌和金黄色葡萄球菌的生长抑制作用最为显著，其生长百分比分别为 19.12±0.65%和 23.32±0.23%。β-香树脂醇（6）和β-谷甾醇（8）对金黄色葡萄球菌具有活性，其生长百分比分别为 27.17±0.07%和 47.79±2.99%。
本研究结果表明，大飞扬草是化学成分的丰富来源，可能为开发抗菌剂提供新的先导化合物。
