Wang Cong, Zaman K H Ahammad Uz, Sarotti Ariel M, Wu Xiaohua, Zheng Shao-Liang, Cao Shugeng
Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, HI 96720 USA.
Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi University for Nationalities, Nanning, 530006 People's Republic of China.
3 Biotech. 2021 Aug;11(8):391. doi: 10.1007/s13205-021-02877-7. Epub 2021 Jul 30.
Bioassay-guided experimental design and chromatographic analysis led to the isolation and identification of ten compounds (1-10) including two unusual sulfur-containing curvularin macrolides (1 and 2) from a Hawaiian fungal strain FS910. Compounds 1 and 2 are rare curvularin macrolides each with a five-membered cyclic sulfur-containing moiety. The structures of the compounds were identified by HRESIMS, NMR spectroscopy, X-ray crystallography, ECD and DFT energy calculation, as well as comparing with previous literatures. Compounds 4, 6 and 8 were active against TNF-α-induced NF-κB inhibitory activity with IC values of 26.45, 5.41 and 15.8 µM, respectively. Compounds 3 and 5-8 exhibited anti-proliferative activity against HT1080, T46D, and A2780S cell lines, with IC values ranging from 2.48 to 29.17 μM. Additionally, Compound 3 showed promising antimicrobial activity against methicillin-resistant (MRSA), , and . Moreover, when tested in combination with antibiotic adjuvant disulfiram [4 µg/mL], compounds 4, 5 and 10 also displayed significant antibacterial activity against .
The online version contains supplementary material available at 10.1007/s13205-021-02877-7.
通过生物测定指导的实验设计和色谱分析，从夏威夷真菌菌株FS910中分离并鉴定出10种化合物（1 - 10），其中包括两种不寻常的含硫弯孢菌素大环内酯（1和2）。化合物1和2是罕见的弯孢菌素大环内酯，每种都含有一个五元环状含硫部分。通过高分辨电喷雾电离质谱（HRESIMS）、核磁共振光谱、X射线晶体学、电子圆二色光谱（ECD）和密度泛函理论（DFT）能量计算，以及与先前文献比较，确定了这些化合物的结构。化合物4、6和8对肿瘤坏死因子-α（TNF-α）诱导的核因子κB（NF-κB）抑制活性具有活性，IC值分别为26.45、5.41和15.8 μM。化合物3和5 - 8对HT1080、T46D和A2780S细胞系表现出抗增殖活性，IC值范围为2.48至29.17 μM。此外，化合物3对耐甲氧西林金黄色葡萄球菌（MRSA）表现出有前景的抗菌活性。此外，当与抗生素佐剂双硫仑[4 μg/mL]联合测试时，化合物4、5和10对[具体细菌名称缺失]也表现出显著的抗菌活性。
在线版本包含可在10.1007/s13205-021-02877-7获取的补充材料。
