Zhang Dewu, Tao Xiaoyu, Gu Guowei, Wang Yujia, Zhao Wenxia, Zhao Wuli, Ren Yan, Dai Shengjun, Yu Liyan
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
School of Pharmacy, Binzhou Medical University, Yantai, China.
Front Microbiol. 2021 Apr 14;12:662321. doi: 10.3389/fmicb.2021.662321. eCollection 2021.
Biotransformation of the -clerodane diterpene, scutebarbatine F (), by sp. CPCC 205437 was investigated for the first time, which led to the isolation of nine new metabolites, scutebarbatine F-F (-). Their structures were determined by extensive high-resolution electrospray ionization mass spectrometry (HRESIMS) and NMR data analyses. The reactions that occurred included hydroxylation, acetylation, and deacetylation. Compounds - and - possess 18-OAc fragment, which were the first examples of 13-spiro -clerodanes with 18-OAc group. Compounds - were the first report of 13-spiro -clerodanes with 2-OH. Compounds - were biologically evaluated for the cytotoxic, antiviral, and antibacterial activities. Compounds , , and exhibited cytotoxic activities against H460 cancer cell line with inhibitory ratios of 46.0, 42.2, and 51.1%, respectively, at 0.3 μM. Compound displayed a significant anti-influenza A virus activity with inhibitory ratio of 54.8% at 20 μM, close to the positive control, ribavirin.
首次研究了菌株CPCC 205437对克罗烷二萜类化合物野黄芩素F（ ）的生物转化，由此分离得到9种新的代谢产物，即野黄芩素F - F（ ）。通过广泛的高分辨率电喷雾电离质谱（HRESIMS）和核磁共振（NMR）数据分析确定了它们的结构。发生的反应包括羟基化、乙酰化和脱乙酰化。化合物 和 具有18 - OAc片段，这是具有18 - OAc基团的13 - 螺克罗烷的首例。化合物 - 是具有2 - OH的13 - 螺克罗烷的首次报道。对化合物 - 进行了细胞毒性、抗病毒和抗菌活性的生物学评价。化合物 、 和 对H460癌细胞系表现出细胞毒性活性，在0.3 μM时抑制率分别为46.0%、42.2%和51.1%。化合物 在20 μM时表现出显著的抗甲型流感病毒活性，抑制率为54.8%，接近阳性对照利巴韦林。
