秃杉中taiwanins E和H的分离鉴定及除草、细胞毒性研究

Isolation and identification of taiwanins E and H from Taiwania flousiana Gaussen and their herbicidal activity and cytotoxicity

秃杉提取物除草活性筛选结果表明,100μg/mL的乙酸乙酯层萃取物对胜红蓟的根长和鲜重抑制率均达到100%。通过活性追踪,利用各种色谱和波谱学方法分离鉴定了2种化合物:taiwanin E(1)和taiwanin H(2)。进一步活性测定结果表明,化合物1对龙葵和胜红蓟具有优异的根长抑制活性,处理7天后的IC_(50)值分别为6.84和8.76μg/mL,化合物2对龙葵、马齿苋、薇甘菊、荷莲荳草的根长IC_(50)值均在10μg/mL以下;二者对胜红蓟的鲜重抑制活性最高,处理7天后的IC_(50)值分别为24.12和21.31μg/mL。细胞毒力研究发现taiwanin H能破坏烟草细胞核,并表现出良好的细胞毒性。化合物1、2的除草活性为首次报道。

The herbicidal activity of the extract of Taiwania flousiana Gaussen was evaluated by the cup method.Results showed that the fraction of ethyl acetate at 100 μg/mL completely inhibited the growth of Ageratum conyzoides L.The inhibition rates of root length and fresh weight were 100%.Two active ingredients were isolated and identified by the bioassay-guided isolation.Further,the inhibition rates of root length and fresh weight of the two active ingredients were investigated on 19 weed species.Results showed that taiwanin E showed significant activities on the root length of Solanum nigrum L.and A.conyzoides and the IC_(50) values of 7 d after the treatment were 6.84 and 8.76 μg/mL,respectively.The IC_(50) values of 7 d after the treatment of taiwanin H on S.nigrum,Portulaca oleracea L.,Mikania micrantha Kunth and Drymaria diandra Blume were less than 10 μg/mL.As far as the fresh weight was concerned,the two active ingredients showed the best activity on A.conyzoides and the IC_(50) values of 7 d after the treatment were 24.12 and 21.31 μg/mL,respectively.Generally,the two active ingredients were more active on the broadleaves than the grass weeds and taiwanin H showed a better activity than taiwanin E.Cytotoxicity studies revealed that taiwanin H could destroy the nucleus of the tobacco BY-2 cells and showed cytotoxicity.The herbicidal activities of taiwanins H and E,belonging to lignans,were firstly reported.