Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities
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Date
Authors
Liang, Yue
Zhang, Qi
Yang, Xueyuan
Li, Ying
Zhang, Xuke
Li, Yuhao
Du, Qing
Jin, Da-Qing
Cui, Jianlin
Lall, Namrita
Journal Title
Journal ISSN
Volume Title
Publisher
Elsevier
Abstract
A phytochemical investigation to obtain bioactive substances as lead compounds or agents for cancer led to the obtainment of six new and two known clerodane diterpenoids from the leaves of Casearia kurzii. Their structures were elucidated using NMR techniques and electronic circular dichroism (ECD) calculations. The subsequent biological cytotoxicity evaluation of these isolates toward human lung cancer A549, human cervical cancer HeLa, human chronic myeloid leukemia K562, and human hepatocellular carcinoma HepG2 was carried out. The most active compound 4 with an IC50 value of 9.7 μM against HepG2 cells was selected to examine the cytotoxic mechanism, which induced the apoptosis and arrested the HepG2 cell cycle at S stage. The in vivo zebrafish experiments revealed that compound 4 had the property of inhibiting tumor proliferation and migration.
Description
Keywords
Zebrafish xenograft model, Cytotoxic activities, Apoptosis, Cell cycle, Clerodane diterpenoids, Casearia kurzii, Electronic circular dichroism (ECD)
Sustainable Development Goals
Citation
Liang, Y., Zhang, Q., Yang, X. et al. 2020, 'Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities', Bioorganic Chemistry, vol. 98, art. 103741, pp. 1-10.