PUBLICATION
Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities
- Authors
- Liang, Y., Zhang, Q., Yang, X., Li, Y., Zhang, X., Li, Y., Du, Q., Jin, D.Q., Cui, J., Lall, N., Tuerhong, M., Lee, D., Abudukeremu, M., Xu, J., Shuai, L., Guo, Y.
- ID
- ZDB-PUB-200403-187
- Date
- 2020
- Source
- Bioorganic chemistry 98: 103741 (Journal)
- Registered Authors
- Cui, Jianlin, Li, Yuhao
- Keywords
- Apoptosis, Casearia kurzii, Cell cycle, Clerodane diterpenoids, Cytotoxic activities, Zebrafish xenograft model
- MeSH Terms
-
- Animals
- Antineoplastic Agents, Phytogenic/chemistry
- Antineoplastic Agents, Phytogenic/isolation & purification
- Antineoplastic Agents, Phytogenic/pharmacology*
- Apoptosis/drug effects
- Casearia/chemistry*
- Cell Cycle/drug effects
- Cell Line, Tumor
- Cell Proliferation/drug effects
- Disease Models, Animal
- Diterpenes/chemistry
- Diterpenes/isolation & purification
- Diterpenes/pharmacology*
- Dose-Response Relationship, Drug
- Drug Screening Assays, Antitumor
- Humans
- Molecular Structure
- Neoplasms, Experimental/drug therapy
- Neoplasms, Experimental/pathology
- Plant Leaves/chemistry
- Structure-Activity Relationship
- Zebrafish
- PubMed
- 32213364 Full text @ Bioorg. Chem.
Citation
Liang, Y., Zhang, Q., Yang, X., Li, Y., Zhang, X., Li, Y., Du, Q., Jin, D.Q., Cui, J., Lall, N., Tuerhong, M., Lee, D., Abudukeremu, M., Xu, J., Shuai, L., Guo, Y. (2020) Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities. Bioorganic chemistry. 98:103741.
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.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping