Luo Na, Yang Ya-Bin, Yang Xue-Qiong, Miao Cui-Ping, Li Yi-Qing, Xu Li-Hua, Ding Zhong-Tao, Zhao Li-Xing
Yunnan Institute of Microbiology, College of Life Science, Yunnan University 2 Cuihu North Road Kunming People's Republic of China 650091
Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, School of Chemical Science and Technology, Yunnan University 2 Cuihu North Road Kunming People's Republic of China 650091
RSC Adv. 2018 Oct 12;8(61):35042-35049. doi: 10.1039/c8ra06690f. eCollection 2018 Oct 10.
Eleven new compounds with streptazolin- and obscurolide-type skeletons were isolated from soil-derived obtained from Tibet, China. Two types of unprecedented skeletons of obscurolide dimer and an obscurolide-type compound with an aromatic polyketide of pentanone substituted at the benzene ring were determined by spectral data analysis. Compound 11 was the first evidence of two nitrogens in streptazolin-type structures. Compound 1 indicated an inhibitory effect on nitric oxide production in LPS-activated macrophages with an inhibition ratio of 51.7% at 50 μM, and on anticoagulant activity on platelet activating factor (PAF)-induced platelet aggregation with an inhibition ratio of 26.0 ± 9.1% at 200 μg mL. 11 had anti-acetylcholinesterase activity with an inhibition ratio of 27.2% at a concentration of 50 μM. Mechanistic aspects of the non-enzymatic reaction as well as a more detailed picture of the biosynthetic relationships of the streptazolin- and obscurolide-type metabolites are described. Acidic and basic conditions can inhibit the growth of , and γ-butyrolactones were found to be hormones controlling antibiotic production in . In the pH fermentation tests, acylation of γ-butyrolactones was successfully used to explain the mechanism of influence on the growth of .
从中国西藏土壤中分离出11种具有链唑啉和暗霉素型骨架的新化合物。通过光谱数据分析确定了两种前所未有的暗霉素二聚体骨架类型以及一种苯环上有戊酮芳香聚酮取代的暗霉素型化合物。化合物11是链唑啉型结构中存在两个氮原子的首个证据。化合物1对脂多糖激活的巨噬细胞中一氧化氮的产生具有抑制作用，在50 μM时抑制率为51.7%，对血小板活化因子（PAF）诱导的血小板聚集的抗凝活性在200 μg/mL时抑制率为26.0±9.1%。化合物11在50 μM浓度下具有抗乙酰胆碱酯酶活性，抑制率为27.2%。描述了非酶反应的机制方面以及链唑啉和暗霉素型代谢物生物合成关系的更详细情况。酸性和碱性条件可抑制[具体微生物名称未给出]的生长，并且发现γ-丁内酯是控制[具体微生物名称未给出]中抗生素产生的激素。在pH发酵试验中，γ-丁内酯的酰化作用成功用于解释对[具体微生物名称未给出]生长的影响机制。
