Son Sangkeun, Ko Sung-Kyun, Jang Mina, Kim Jong Won, Kim Gil Soo, Lee Jae Kyoung, Jeon Eun Soo, Futamura Yushi, Ryoo In-Ja, Lee Jung-Sook, Oh Hyuncheol, Hong Young-Soo, Kim Bo Yeon, Takahashi Shunji, Osada Hiroyuki, Jang Jae-Hyuk, Ahn Jong Seog
Anticancer Agent Research Center, Korea Research Institute of Bioscience and Biotechnology, Cheongju 363-883, Korea.
University of Science and Technology (UST), Daejeon 305-333, Korea.
Mar Drugs. 2016 Apr 2;14(4):72. doi: 10.3390/md14040072.
Salterns, one of the most extreme natural hypersaline environments, are a rich source of halophilic and halotolerant microorganisms, but they remain largely underexplored ecological niches in the discovery of bioactive secondary metabolites. In continued efforts to investigate the metabolic potential of microbial populations from chemically underexplored sites, three new lipopeptides named iturin F₁, iturin F₂ and iturin A₉ (1-3), along with iturin A₈ (4), were isolated from Bacillus sp. KCB14S006 derived from a saltern. The structures of the isolated compounds were established by 1D-, 2D-NMR and HR-ESIMS, and their absolute configurations were determined by applying advanced Marfey's method and CD spectroscopy. All isolates exhibited significant antifungal activities against various pathogenic fungi and moderate cytotoxic activities toward HeLa and src(ts)-NRK cell lines. Moreover, in an in vitro enzymatic assay, compound 4 showed a significant inhibitory activity against indoleamine 2,3-dioxygenase.
盐田是最极端的天然高盐环境之一,是嗜盐和耐盐微生物的丰富来源,但在生物活性次生代谢产物的发现方面,它们仍是很大程度上未被充分探索的生态位。为持续努力研究来自化学探索不足地点的微生物种群的代谢潜力,从盐田分离出的芽孢杆菌属KCB14S006中分离出了三种新的脂肽,命名为iturin F₁、iturin F₂和iturin A₉(1-3),以及iturin A₈(4)。通过一维、二维核磁共振和高分辨电喷雾电离质谱确定了分离化合物的结构,并应用先进的马尔费方法和圆二色光谱确定了它们的绝对构型。所有分离物对各种致病真菌均表现出显著的抗真菌活性,对HeLa和src(ts)-NRK细胞系表现出中等的细胞毒性活性。此外,在体外酶分析中,化合物4对吲哚胺2,3-双加氧酶表现出显著的抑制活性。