期刊
MOLECULES
卷 20, 期 9, 页码 17544-17556出版社
MDPI
DOI: 10.3390/molecules200917544
关键词
Isodon excisoides; ent-kaurane diterpene; cytotoxic activity; structure-activity relationship
资金
- National Natural Science Foundation of China [81173486]
- Young Backbone Teachers of Colleges and Universities in Henan Province Fund [2012GGJS-095]
- Medical Science and Technology Project of Henan Province [2013ZY02063]
- Fundamental Scientific Research Funds of Provincial Universities [2014KYYWF-QN02]
- Collaborative Innovation Center of Diagnosis, Treatment and Drug Research for Respiratory Disease, Henan Province, China
Three types of ent-kaurane diterpenoids were isolated from the aerial parts of Isodon excisoides, including three new diterpenoids, 1,7,14-trihydroxy-20-acetoxy-ent-kaur-15-one (1); 1,7,14,18-tetrahydroxy-20-acetoxy-ent-kaur-15-one (2); and 1-acetoxy-14-hydroxy-7,20-epoxy-ent-kaur-16-en-15-one (3); together with six known diterpenes henryin (4); kamebanin (5); reniformin C (6); kamebacetal A (7); kamebacetal B (8); and oridonin (9). The structures of the isolated compounds were elucidated by means of nuclear magnetic resonance spectroscopy and high-resolution mass spectrometry in conjunction with published data for their analogs, as well as their fragmentation patterns. Compounds 5 and 9 were isolated from Isodon excisoides for the first time. To explore the structure-activity relationships of the isolated compounds, they were tested for their cytotoxic effects against five human cancer cell lines: HCT-116, HepG2, A2780, NCI-H1650, and BGC-823. Most of the isolated compounds showed certain cytotoxic activity against the five cancer cell lines with IC50 values ranging from 1.09-8.53 mu M. Among the tested compounds, compound 4 exhibited the strongest cytotoxic activity in the tested cell lines, with IC50 values ranging from 1.31-2.07 mu M. Compounds 1, 6, and 7 exhibited selective cytotoxic activity.
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