Tang Zhongyan, Lu Lihua, Zhou Xiaoyong, Shen Jie, Song Weiping, Tang Yuedong, Xia Zhengxiang
Department of Emergency and Critical Care Medicine, Jin Shan Hospital, Fudan University, Shanghai, China.
Department of Neonatology, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China.
Nat Prod Res. 2020 Sep;34(17):2448-2455. doi: 10.1080/14786419.2018.1539983. Epub 2019 Jan 9.
A new polycyclic polyprenylated acylphloroglucinol (), nujiangefolin D, together with five known analogues (), were isolated from the fruits of . Compound was screened by the LC-MS and LC-PDA. The structure of was elucidated on the basis of extensive spectroscopic techniques including 1 D and 2 D NMR and MS analyses. The compounds isolated were evaluated for their cytotoxic activities against three cancer cell lines, showed moderate cytotoxic activity against Hela, PANC-1, and MDA-MB-231 cell lines with IC values of 5.6 ± 0.1, 9.1 ± 0.2, and 8.3 ± 0.2 M, respectively. The antitumor mechanism was explained via virtual docking of to the main sites in the human serine/threonine-protein kinase mTOR (mTOR) crystal structure (PDB code: 4DRI). Furthermore, may inhibit Hela cell proliferation through mTOR by the western blotting analysis. Taken together, may be a potential mTOR inhibitor used for the treatment of cervical cancer.
从[植物名称]果实中分离出一种新的多环多异戊烯基酰基间苯三酚（怒江格诺林D）以及五种已知类似物。化合物通过液相色谱 - 质谱联用仪（LC - MS）和液相色谱 - 光电二极管阵列检测器（LC - PDA）进行筛选。基于包括一维和二维核磁共振（NMR）以及质谱（MS）分析在内的广泛光谱技术阐明了化合物的结构。对分离出的化合物针对三种癌细胞系的细胞毒性活性进行了评估，[化合物名称]对Hela、PANC - 1和MDA - MB - 231细胞系表现出中等细胞毒性活性，IC50值分别为5.6±0.1、9.1±0.2和8.3±0.2μM。通过将[化合物名称]与人丝氨酸/苏氨酸蛋白激酶mTOR（mTOR）晶体结构（PDB代码：4DRI）中的主要位点进行虚拟对接来解释其抗肿瘤机制。此外，通过蛋白质印迹分析表明[化合物名称]可能通过mTOR抑制Hela细胞增殖。综上所述，[化合物名称]可能是一种用于治疗宫颈癌的潜在mTOR抑制剂。
