1. Limonoids and tricyclic diterpenoids from Azadirachta indica and their antitumor activities.
- Author
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Zhu WF, Cheng JX, Su SZ, Zhang CF, Akihisa T, Manosroi J, Manosroi A, Feng F, Liu WY, and Zhang J
- Subjects
- Antineoplastic Agents, Phytogenic isolation & purification, Apoptosis drug effects, Cell Line, Tumor, Cell Proliferation drug effects, Crystallography, X-Ray, Diterpenes isolation & purification, Drug Screening Assays, Antitumor, Humans, Limonins isolation & purification, Models, Molecular, Neoplasms drug therapy, Antineoplastic Agents, Phytogenic chemistry, Antineoplastic Agents, Phytogenic pharmacology, Azadirachta chemistry, Diterpenes chemistry, Diterpenes pharmacology, Limonins chemistry, Limonins pharmacology
- Abstract
The chemical constituents of the roots, seeds, and bark of Azadirachta indica var. siamensis were investigated, leading to the isolation of six tricyclic diterpenoids and five limonoids, including two new compounds (2, 5). The structures were elucidated based on NMR spectroscopic techniques, mass spectrometry and single-crystal X-ray diffraction as well as comparison with the literature. Moreover, the cytotoxicity activities of the isolates were evaluated. The results indicated that the compounds 1-3, 5-9 exhibited cytotoxicities against one or more cancer cell lines tested, with IC
50 values in the range of 1.7-88.1 μM. The mechanism of action studies indicated that the most active compound, compound 5, could induce the apoptosis of AZ521 cells. Furthermore, the Western blot analysis showed that compound 5 could reduce the expression levels of procaspases-3, -8, -9 and promote the expression of Bid and AIF., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Inc. All rights reserved.)- Published
- 2020
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