Alshaibani Muhanna, Zin Noraziah Mohamad, Jalil Juriyati, Sidik Nik, Ahmad Siti Junaidah, Kamal Nurkhalida, Edrada-Ebel Ruangelie
Programme of Biomedical Science, School of Diagnostic and Applied Health Sciences, Faculty of Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.
Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.
J Microbiol Biotechnol. 2017 Jul 28;27(7):1249-1256. doi: 10.4014/jmb.1608.08032.
In our search for new sources of bioactive secondary metabolites from sp., the ethyl acetate extracts from endophytic SUK 25 afforded five active diketopiperazine (DKP) compounds. The aim of this study was to characterize the bioactive compounds isolated from endophytic SUK 25 and evaluate their bioactivity against multiple drug resistance (MDR) bacteria such as and spp., and their cytotoxic activities against the human hepatoma (HepaRG) cell line. The production of secondary metabolites by this strain was optimized through Thornton's medium. Isolation, purification, and identification of the bioactive compounds were carried out using high-performance liquid chromatography, high-resolution mass liquid chromatography-mass spectrometry, Fourier transform infrared spectroscopy, and nuclear magnetic resonance, and cryopreserved HepaRG cells were selected to test the cytotoxicity. The results showed that endophytic SUK 25 produces four active DKP compounds and an acetamide derivative, which were elucidated as -(-Val--Pro), -(-Leu--Pro), -(-Phe--Pro), -(-Val--Phe), and -(7-hydroxy-6-methyl-octyl)-acetamide. These active compounds exhibited activity against methicillin-resistant S. aureus ATCC 43300 and , with low toxicity against human hepatoma HepaRG cells. Endophytic SUK 25 has the ability to produce DKP derivatives biologically active against some MDR bacteria with relatively low toxicity against HepaRG cells line.
在我们从[具体物种]中寻找生物活性次生代谢物新来源的过程中，内生菌SUK 25的乙酸乙酯提取物产生了五种活性二酮哌嗪（DKP）化合物。本研究的目的是对从内生菌SUK 25中分离出的生物活性化合物进行表征，并评估它们对耐多药（MDR）细菌如[具体细菌名称1]和[具体细菌名称2]等的生物活性，以及它们对人肝癌（HepaRG）细胞系的细胞毒性活性。通过桑顿培养基优化了该菌株次生代谢物的产生。使用高效液相色谱、高分辨率质谱液相色谱 - 质谱联用、傅里叶变换红外光谱和核磁共振进行生物活性化合物的分离、纯化和鉴定，并选择冷冻保存的HepaRG细胞来测试细胞毒性。结果表明，内生菌SUK 25产生了四种活性DKP化合物和一种乙酰胺衍生物，分别鉴定为 -(-缬氨酸 - -脯氨酸)、 -(-亮氨酸 - -脯氨酸)、 -(-苯丙氨酸 - -脯氨酸)、 -(-缬氨酸 - -苯丙氨酸)和 -(7 - 羟基 - 6 - 甲基 - 辛基)-乙酰胺。这些活性化合物对耐甲氧西林金黄色葡萄球菌ATCC 43300和[具体细菌名称2]表现出活性，对人肝癌HepaRG细胞毒性较低。内生菌SUK 25具有产生对某些MDR细菌具有生物活性且对HepaRG细胞系毒性相对较低的DKP衍生物的能力。
