来自维腊木 Xylopia vielana 的罕见二聚大牻牛儿酮及其多药耐药逆转活性。
Rare dimeric guaianes from Xylopia vielana and their multidrug resistance reversal activity.
机构信息
Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
出版信息
Phytochemistry. 2019 Feb;158:26-34. doi: 10.1016/j.phytochem.2018.11.004. Epub 2018 Nov 15.
Thirteen undescribed dimeric guaianes were isolated from the leaves of Xylopia vielana Pierre. Their structures were elucidated by NMR spectroscopy and mass spectrometry, and the absolute configurations of vielanins G-Q were determined by a combination of the circular dichroism (CD) exciton chirality method, chemical conversion, and electronic CD (ECD) spectroscopy analysis. Vielaninors A and B are the first examples of trinor-guaiane-dimers. Multidrug resistance reversal activity assay of the isolates was evaluated in doxorubicin-resistant human breast cancer cells. Vielanins H, K-M, P, and Q were noncytotoxic and enhanced the cytotoxicity of doxorubicin by 2.1-41.6-fold at 10 μM.
从 Xylopia vielana Pierre 的叶子中分离得到 13 种未描述的二聚愈创木烷。通过 NMR 光谱和质谱阐明了它们的结构，并通过圆二色性（CD）外消旋手性方法、化学转化和电子 CD（ECD）光谱分析相结合，确定了 vielanins G-Q 的绝对构型。Vielaninors A 和 B 是三降-愈创木烷-二聚体的第一个例子。对分离物的多药耐药逆转活性进行了评价，在 10 μM 时，vielanins H、K-M、P 和 Q 无细胞毒性，并将阿霉素的细胞毒性增强了 2.1-41.6 倍。
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