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从粗榧茎皮中分离得到具有细胞毒性的呋喃喹啉和二氢恶唑烷生物碱。

Furoquinolines and dihydrooxazole alkaloids with cytotoxic activity from the stem bark of Araliopsis soyauxii.

机构信息

Department of Chemistry, University of Dschang, P.O. Box 67, Dschang, Cameroon.

Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55128 Mainz, Germany; Department of Biochemistry, University of Dschang, P.O. Box 67, Dschang, Cameroon.

出版信息

Fitoterapia. 2019 Mar;133:193-199. doi: 10.1016/j.fitote.2019.01.003. Epub 2019 Jan 14.

Abstract

Two new furoquinoline alkaloids, maculine B (1) and kokusaginine B (2) and one new dihydrooxazole alkaloid, veprisazole (3), along with four known compounds namely, N-methyl-3-methoxyrutaecarpine (4), flindersiamine (5), skimmianine (6) and tilianin (7) were isolated from the methanol extract of the stem bark of Araliopsis soyauxii Engl. by various chromatographic methods. Their structures were determined using spectrometry and spectroscopic techniques including NMR and MS. The cytotoxicity of the new compounds compared to that of doxorubicin, the reference anticancer compound, was determined on a panel of nine cancer cell lines including sensitive and drug resistant phenotypes. The three previously undescribed alkaloids displayed selective activities. Maculine B (1), the most active one among the newly described compounds, exhibited IC below 30 μM against CCRF-CEM leukemia and U87MG glioblastoma cells.

摘要

从远志科远志属植物 Araliopsis soyauxii Engl. 的甲醇提取物中,通过各种色谱方法分离得到了两个新的呋喃喹啉生物碱马库林 B(1)和可可萨吉宁 B(2),以及一个新的二氢恶唑生物碱 Veprisazole(3),此外还分离得到了四个已知化合物,即 N-甲基-3-甲氧基紫杉碱(4)、弗林德斯胺(5)、斯凯米宁(6)和替利宁(7)。通过光谱和光谱技术,包括 NMR 和 MS,确定了它们的结构。将新化合物与抗癌药物阿霉素的细胞毒性进行了比较,在包括敏感和耐药表型的 9 种癌细胞系上进行了测定。这三个以前未描述的生物碱表现出选择性的活性。在新描述的化合物中,最活跃的马库林 B(1)对 CCRF-CEM 白血病和 U87MG 神经胶质瘤细胞的 IC 低于 30µM。

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