Kurnia Dikdik, Apriyanti Eti, Soraya Cut, Satari Mieke H
Department of Chemistry, Faculty of Mathematic and Natural Sciences, Universitas Padjadjaran-Bandung, Sumedang, Indonesia.
Department of Concervative Dentistry, Faculty of Dentistry, Syiah Kuala Universty, Banda Aceh, Indonesia.
Curr Drug Discov Technol. 2019;16(3):290-296. doi: 10.2174/1570163815666180828113920.
A significant number of antibiotics are known to inhibit peptidoglycan synthesis in the cross-linking stage, while the drug fosfomycin is the only one known to inhibit MurA. Escalated antibiotic resistance has had an impact on the efficacy of fosfomycin, thus demanding the discovery of suitable substitutes with improved potential for MurA inhibition. The aim of this work is to isolate antibacterial compounds from Sarang Semut (Myrmecodia pendans) and to evaluate their antibacterial activity against pathogenic oral bacteria of Enterococcus faecalis ATCC 29212 and inhibitory activity against MurA enzyme.
The antibacterial compounds from Sarang Semut were isolated by a bioactivity-guided separation method with various solvents and combination of column chromatography on normal and reverse phases. The compounds with concentrations of 1000 and 5000 ppm were assessed against E. faecalis ATCC 29212 by agar well diffusion method, with chlorhexidine and fosfomycin being used as positive controls.
Two antibacterial compounds isolated from Sarang Semut were identified as two new flavonoids derivates of 1 (10 mg) and 2 (4 mg). Both compounds were tested for antibacterial activities against E. faecalis. MIC values of compounds 1 and 2 were 8.15 and 8.05 mm at 1000 ppm and 8.62 and 8.55 mm at 5000 ppm, respectively. MBC values were 156 and 625 ppm for 1 and 625 and 2500 ppm for 2, respectively. In an inhibitory murA enzyme activity assay, compounds 1 and 2 were shown to inhibit the enzyme activity by IC50 values of 21.7 and 151.3 ppm.
The study demonstrated that ethyl acetate fraction of Sarang Semut contained antibacterial flavonoids as active constituents that showed activity against E. faecalis. These results showed the plant's potential in herbal medicine and the development of new antibacterial agent for pathogenic dental caries.
已知大量抗生素在交联阶段抑制肽聚糖合成，而药物磷霉素是已知唯一抑制MurA的药物。抗生素耐药性的加剧对磷霉素的疗效产生了影响，因此需要发现具有更好MurA抑制潜力的合适替代物。本研究的目的是从蚂蚁窝（Myrmecodia pendans）中分离抗菌化合物，并评估它们对粪肠球菌ATCC 29212等致病性口腔细菌的抗菌活性以及对MurA酶的抑制活性。
采用生物活性导向分离法，使用各种溶剂以及正相和反相柱色谱组合，从蚂蚁窝中分离抗菌化合物。通过琼脂孔扩散法，以洗必泰和磷霉素作为阳性对照，评估浓度为1000和5000 ppm的化合物对粪肠球菌ATCC 29212的抗菌活性。
从蚂蚁窝中分离出的两种抗菌化合物被鉴定为两种新的黄酮类衍生物1（10 mg）和2（4 mg）。对这两种化合物进行了针对粪肠球菌的抗菌活性测试。化合物1和2在1000 ppm时的最低抑菌浓度（MIC）值分别为8.15和8.05 mm，在5000 ppm时分别为8.62和8.55 mm。化合物1和2的最低杀菌浓度（MBC）值分别为156和625 ppm以及625和2500 ppm。在MurA酶抑制活性测定中，化合物1和2对该酶活性的半数抑制浓度（IC50）值分别为21.7和151.3 ppm。
该研究表明，蚂蚁窝的乙酸乙酯馏分含有抗菌黄酮类化合物作为活性成分，对粪肠球菌具有活性。这些结果显示了该植物在草药医学以及开发新型龋齿病原菌抗菌剂方面的潜力。
