Spiculisporic acid analogues of the marine-derived fungus, Aspergillus candidus strain HDf2, and their antibacterial activity
Spiculisporic acid analogues of the marine-derived fungus, Aspergillus candidus strain HDf2, and their antibacterial activity
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海洋源性真菌白曲霉 HDf2 菌株的穗孢酸类似物及其抗菌活性
DOI：
10.1007/s10482-015-0462-y
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发表时间：
2015-07-01
影响因子：
2.6
通讯作者：
Shen, Ming Hui
中科院分区：
文献类型：
--
作者：
Wang, Rong;Guo, Zhi Kai;Shen, Ming Hui
从海胆来源的白曲霉菌株HDf 2的发酵液中通过生物活性导向分级分离分离得到两个新的抗生素刺孢青霉酸类似物，命名为刺孢青霉酸F（1）和G（2），以及两个已知化合物，（-）-刺孢青霉酸（3）和裂刺孢青霉酸B（4）。通过1D和2D NMR的综合分析和高分辨率MS光谱以及与已知化合物的比较，明确地确定了它们的结构。生物活性实验表明，化合物1和2对革兰氏阴性青枯假单胞菌和革兰氏阳性金黄色葡萄球菌具有抗菌活性，对人胃腺癌细胞株SGC-7901和人肺腺癌细胞株SPC-A-1无细胞毒性。这是确定刺孢青霉酸衍生物作为土传病原体青枯菌（E. solanacearum）潜在生物防治剂的第一个关键证据。F.史密斯（Smith）这些发现为这类化合物的化学和生物活性多样性提供了进一步的见解。
Two novel antibiotic spiculisporic acid analogues, named as spiculisporic acid F (1) and G (2), and two known compounds, (-)-spiculisporic acid (3) and secospiculisporic acid B (4), were isolated by bioactivity-guided fractionation from the fermentation broth of the sea urchin-derived Aspergillus candidus strain HDf2. Their structures were unambiguously established by comprehensive analysis of 1D and 2D NMR, and high-resolution MS spectra, and by comparison with known compounds. Biological experiments demonstrated that compounds 1 and 2 displayed antibacterial activity against Gram-negative Pseudomonas solanacearum and Gram-positive Staphylococcus aureus, but showed no cytotoxicity against SGC-7901 human gastric adenocarcinoma and SPC-A-1 human lung adenocarcinoma tumor cell lines. This is the first critical evidence identifying spiculisporic acid derivatives as a potential bio-control agent for the soil borne pathogen P. solanacearum (E. F. Smith) Smith. These findings provide further insight into the chemical and biological activity diversity of this class of compounds.