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Updated: Oct 11, 2026
Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Previously undescribed antileukemic coumarins from Zanthoxylum dimorphophyllum var. spinifolium: isolation, structure
Hui-Min Fang1, Wei-Wu Xia2, Fei-Bi Xiong3
1College of Pharmacy, Guizhou University, Guiyang 550025, China; State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Natural Products Research Center of Guizhou Province, Guizhou Medical University, Guiyang 550014, China.
Abstract:
Six previously undescribed coumarins (1-6), including one pair of enantiomers, along with 23 known coumarin derivatives (7-29), were isolated from the branches and leaves of Zanthoxylum dimorphophyllum var. spinifolium. Their structures were elucidated through comprehensive spectroscopic analysis, including HR-ESIMS, NMR, and ECD. These compounds were subsequently evaluated for their antileukemic activity. Among them, the previously undescribed compound 5 exhibited significant antiproliferative activity against three cancer cell lines: erythroleukemia (HEL), promyelocytic (HL-60), and chronic myelogenous leukemia (K562), with IC50 values of 30.5 ± 1.2, 10.2 ± 0.7, and 19.8 ± 1.2 μM, respectively. HL-60 cells were the most sensitive to compound 5, exhibiting the lowest IC50 value of 10.2 ± 0.7 μM. Flow cytometric analysis revealed that compound 5 induced apoptosis in HL-60 cells in a dose-dependent manner and induced significant cell cycle arrest at the S phase. Furthermore, in a zebrafish xenograft model, compound 5 significantly inhibited the proliferation of HL-60 cells in vivo.
