期刊
ORGANIC LETTERS
卷 18, 期 14, 页码 3398-3401出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b01560
关键词
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资金
- National Natural Science Foundation of China [81172958]
- China Scholarships Council
- Basic Research Subject of Key Laboratory Supported by Educational Commission of Liaoning Province of China [LZ2014044]
In this study, we screened 17 medicinal plants for binding activity to G-quadruplex d(TTGGGTT)(4) by H-1 NMR spectroscopy and found that the crude extract of Peganum harmala L. seeds showed the most potential binding activity. Subsequently, H-1 NMR- and bioassay -guided isolation of the extract of P. harmala L. was performed to obtain four pairs of partially racemized beta-carboline alkaloids, pegaharmines A-D (1-4). Their structures and absolute configurations were determined by extensive NMR analyses, X-ray crystallography, ECD calculations, and CD exciton chirality approaches. Interestingly, pegaharmine D (4), which showed the strongest G-quadruplex interaction, exhibited significant cytotoxic activity against three cancer cell lines. This work contributed a practical strategy for the discovery of novel G-quadruplex ligands from natural products and provided potential insights for using beta-carboline alkaloids as anticancer lead compounds specifically targeting G-quadruplexes.
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