摘要
目的:对半边旗中二萜类有效成分及抗肿瘤活性作进一步研究。方法:半边旗乙醇提取物上活性炭柱,乙醇氯仿(10∶1)洗,减压浓缩后上硅胶柱,甲醇氯仿(90∶2)洗脱,得纯化合物,经二维核磁共振(NMR)确定了化合物的空间结构。以噻唑蓝(MTT)法测定肿瘤细胞存活率,。IC50按改良Karber公式计算。结果:共分得5个化合物B,4F,5F,6F及A,其中A是新化合物,6F是首次从该植物中分离得到。5F,A,6F明显抑制人白血病粒细胞HL60,人低分化胃腺癌上皮细胞MGC803、人低分化鼻咽癌上皮细胞CNE2Z和人肝癌上皮细胞BEL7402的增殖,活性依次增强。6F对HL60细胞的活性最强[IC50为(0.09±0.01)μmol·L-1],阳性对照5Fu的IC50为:(52.5±2.8)μmol·L-1。结论:从半边旗分离得到的一类二萜化合物具有显著抑制多种癌细胞增殖的活性,其中6F活性最强。
OBJECTIVE: To investigate the
diterpenoid constituents and anticancer action of the pteris semipinnata L.(PSL).
METHOD:TBZThe ethanol extract was fractionated over an active charcoal column,eluted with
ethanolchloroform(101).After concentrating,the remainder was chromatographed on sillica gel
column,eluted with chloroformmethanol (902).The pure compounds were obtained.Their
structures were confirmed by spectra,espectially by twodimensional nuclear magnetic
resonance (2DNMR) for their stereo structures.Cell viability was determined using the
3(4,5Dimethyl2thiazolyl)2,5diphenyl2Htetrazolium bromide(MTT) test,and the IC50 value were
calculated by the modified Karber formula. RESULTS: Five compounds,B,4F,5F,6F and A ,were
obtained.A is a new compuound,6F was isolated from the plant for the first time.A and 6F
exhibited obvious activity to inhibit the growth of human promyelocytic leukemia cells
(HL60),gastric adenocarcinom cell line (MGC803),human nasopharyngeal carcinoma cells in
low differentiation ( CNE2Z) and human liver adenocarcinoma cell line (BEL7402),6F is more
active than the positive control by 5Fu,their IC50 for LC60 were 0.09molL-1 and
52.5molL-1,respectively. CONCLUSION: The diterpenoids obtained from the PSL possess
obvious antitumour activity.The preliminary study on the structuralactivity relationship
suggested that the cytotoxic activity is related to the methylene cyclopentanone moity.The 6F is
the most active one.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1999年第8期512-514,共3页
Chinese Pharmaceutical Journal
基金
广东省科委重点科技攻关资助
广东省科委重点科技攻关资助