当前位置: X-MOL 学术Phytochemistry › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Bioactive norditerpenoids from Cephalotaxus fortunei var. alpina and C. lanceolata
Phytochemistry ( IF 3.8 ) Pub Date : 2018-04-14
Ling Ni, Xiu-Hong Zhong, Xiao-Jiao Chen, Bing-Jie Zhang, Mei-Fen Bao, Xiang-Hai Cai

Twenty-eight naturally occurring Cephalotaxus tropone analogues, including 19 previously undescribed ones, were identified from Cephalotaxus fortunei Hook. var. alpina H. L. Li and C. lanceolata K. M. Feng. The presence of the C20 cephinoids A−E revealed that these tropones were assigned to the norditerpenoids and were perhaps derived from labdane-type diterpenoids. These norditerpenoids showed excellent cytotoxicity against human cancer cells (IC50, 20–0.1 μM) in vitro. The SAR (structure-activity relationship) analysis disclosed that the tropone moiety and the lactone ring were crucial structural features for the observed activities. Further SAR analyses led to a new candidate, cephinoid H, which demonstrated an inhibition of 49.0% by administration to zebrafish at a dose of 60.0 ng/mL, compared to cisplatin (DDP, 22.4%) at 15.0 μg/mL. These compounds might affect the NF-κB signaling pathway rather than binding to microtubules. Additionally, the isolated norditerpenoids showed almost equal anti-inflammatory activities compared to the positive control, MG132.



中文翻译:

从生物活性norditerpenoids尖杉变种。阿尔皮娜C. lanceolata

二十八个自然发生的三尖杉庚三烯酮类似物,包括19个以前未描述的,从确定的三尖杉挂钩。变种 Allpina HL Li和C. lanceolata KM Feng。C20炔属化合物A–E的存在表明,这些托普酮被分配给降冰片萜烯类化合物,并且可能源自拉丹烷型二萜烯类化合物。这些norditerpenoids显示针对人类癌细胞的细胞毒性优异(IC 50,μM20-0.1)体外。SAR(结构-活性关系)分析显示,托普酮部分和内酯环是观察到的活性的关键结构特征。进一步的SAR分析导致了一种新的候选化合物,类胡萝卜素H,与以15.0μg/ mL的顺铂(DDP,22.4%)相比,以60.0 ng / mL的剂量向斑马鱼给药可显示49.0%的抑制作用。这些化合物可能会影响NF-κB信号传导途径,而不是与微管结合。此外,与阳性对照MG132相比,分离的去甲类萜类化合物显示出几乎相等的抗炎活性。

更新日期:2018-04-25
down
wechat
bug