Gao Ying, He Chunnian
Tennessee Center for Botanical Medicine Research and the Department of Biology, Middle Tennessee State University, Murfreesboro, TN 37132, USA.
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Beijing 100193, P.R. China.
Oncol Lett. 2017 Jun;13(6):4371-4377. doi: 10.3892/ol.2017.5982. Epub 2017 Apr 4.
from the section of the genus is an important Chinese medicinal herb. In our previous study, 10 oligostilbenes from the seeds of , including -resveratrol and its dimers and trimers, were isolated and identified. In the present study, the anti-proliferative effects of these 10 oligostilbenes were systemically evaluated in a panel of human lung, breast and bone cancer cell lines, and their apoptotic effects were analyzed using a high-content multiplex apoptosis assay and a fluorescent caspase-3/7 assay. Furthermore, their anti-metastasis effects were examined in an invasive breast cancer cell line. Among the ten compounds, two resveratrol dimers, - and -gnetin H, showed the most potent anti-proliferative and anti-metastasis effects. All -oligostilbenes were more effective than their -forms, and trimers of resveratrol were more effective than dimers and the resveratrol isomer. The structure-activity relationships revealed that the polymerization degree, the double bond in the stilbene skeleton, and the steric arrangement and conformation of oligostilbenes obviously affected their antitumor potential. The results from this study provide valuable information for future semi-synthesis of resveratrol derivatives to develop novel cancer chemopreventive agents.
属的该部分是一种重要的中药材。在我们之前的研究中,从该植物种子中分离并鉴定出了10种低聚芪类化合物,包括白藜芦醇及其二聚体和三聚体。在本研究中,对这10种低聚芪类化合物在一组人肺癌、乳腺癌和骨癌细胞系中的抗增殖作用进行了系统评估,并使用高内涵多重凋亡检测法和荧光半胱天冬酶-3/7检测法分析了它们的凋亡作用。此外,在侵袭性乳腺癌细胞系中检测了它们的抗转移作用。在这10种化合物中,两种白藜芦醇二聚体,即 - 和 - 葛藟素H,表现出最有效的抗增殖和抗转移作用。所有 - 低聚芪类化合物都比它们的 - 形式更有效,白藜芦醇的三聚体比二聚体和白藜芦醇异构体更有效。构效关系表明,低聚芪类化合物的聚合度、芪骨架中的双键以及空间排列和构象明显影响它们的抗肿瘤潜力。本研究结果为未来白藜芦醇衍生物的半合成以开发新型癌症化学预防剂提供了有价值的信息。