穿心莲对产超广谱β-内酰胺酶（ESBL）大肠杆菌的疗效。
Efficacy of Andrographis paniculata against extended spectrum β-lactamase (ESBL) producing E. coli.
机构信息
School of Life Sciences, B.S. Abdur Rahman Crescent Institute of Science and Technology, Vandalur, Chennai, 600048, India.
出版信息
BMC Complement Altern Med. 2018 Sep 3;18(1):244. doi: 10.1186/s12906-018-2312-8.
BACKGROUND
A. paniculata is widely known for its medicinal values and is traditionally used to treat a wide range of diseases such as cancer, diabetes, skin infections, influenza, diarrhoea, etc. The phytochemical constituents of this plant possess unique and interesting biological activities. The main focus of this study was to evaluate the antibacterial property of crude ethyl acetate (CEA) extract of A. paniculata against E. coli clinical isolates along with molecular docking of 10 different bioactive components from this plant with CTX-M-15.
METHODS
CEA extract was subjected to phytochemical and FTIR analysis. The E. coli isolates were tested for antibiotic susceptibility through disk-diffusion method to observe their resistance pattern towards different antibiotics. Antibacterial activity and biofilm assay were performed through broth microdilution using a 96-well microplate. CEA extract was further utilized to observe its effect on the expression of a gene encoding CTX-M-15. Finally, in-silico studies were performed where 10 different bioactive compounds from A. paniculata were molecularly docked with CTX-M-15.
RESULTS
Phytochemical and FTIR analysis detected the presence of various secondary metabolites and functional groups in CEA extract respectively. Molecular docking provided the number of residues and bond lengths together with a positive docking score. Antibiotic susceptibility showed the multi-drug resistance of all the clinical strains of E. coli. The antibacterial and antibiofilm efficiency of CEA extract (25, 50 and 100 μg/ml) was tested and 100 μg/ml of the extract was more effective in all the strains of E. coli. All 3 ESBL producing strains of E. coli were subjected to gene expression analysis through PCR. Strains treated with 100 μg/ml of the extract showed a downregulation of the gene encoding CTX-M-15 compared to untreated controls.
CONCLUSIONS
The utilization of CEA extract of A. paniculata proved an economical way of controlling the growth and biofilm formation of ESBL strains of E. coli. CEA extract was also able to downregulate the expression of a gene encoding CTX-M-15. Molecular docking of 10 different bioactive compounds from A. paniculata with CTX-M-15 provided the residues and bond lengths with a positive docking score.
背景
A. paniculata 以其药用价值而广为人知，传统上用于治疗多种疾病，如癌症、糖尿病、皮肤感染、流感、腹泻等。该植物的植物化学成分具有独特而有趣的生物活性。本研究的主要重点是评估 A. paniculata 的粗乙酸乙酯（CEA）提取物对大肠杆菌临床分离株的抗菌特性，同时对该植物的 10 种不同生物活性成分与 CTX-M-15 进行分子对接。
方法
对 CEA 提取物进行植物化学和傅里叶变换红外（FTIR）分析。通过圆盘扩散法测试大肠杆菌分离株对抗生素的敏感性，观察它们对不同抗生素的耐药模式。通过 96 孔微量滴定板进行肉汤微量稀释法进行抗菌活性和生物膜测定。进一步利用 CEA 提取物观察其对 CTX-M-15 编码基因表达的影响。最后，进行了计算机模拟研究，其中对 A. paniculata 的 10 种不同生物活性化合物进行了分子对接与 CTX-M-15。
结果
植物化学和 FTIR 分析分别检测到 CEA 提取物中存在各种次生代谢物和功能基团。分子对接提供了残基数量和键长以及阳性对接评分。抗生素敏感性表明所有大肠杆菌临床分离株均具有多药耐药性。测试了 CEA 提取物（25、50 和 100μg/ml）的抗菌和抗生物膜效率，发现 100μg/ml 的提取物在所有大肠杆菌菌株中更有效。对所有 3 株产 ESBL 的大肠杆菌进行了基因表达分析通过 PCR。与未处理对照相比，用 100μg/ml 提取物处理的菌株显示 CTX-M-15 编码基因的下调。
结论
A. paniculata 的 CEA 提取物的利用为控制 ESBL 株大肠杆菌的生长和生物膜形成提供了一种经济有效的方法。CEA 提取物还能够下调 CTX-M-15 编码基因的表达。A. paniculata 的 10 种不同生物活性化合物与 CTX-M-15 的分子对接提供了残基数量和键长以及阳性对接评分。
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