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Diterpenoids from the leaves of Casearia kurzii showing cytotoxic activities
- Source :
- Bioorganic Chemistry. 98:103741
- Publication Year :
- 2020
- Publisher :
- Elsevier BV, 2020.
-
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.
- Subjects :
- Casearia
Apoptosis
01 natural sciences
Biochemistry
HeLa
Structure-Activity Relationship
Cell Line, Tumor
Drug Discovery
medicine
Animals
Humans
Cytotoxic T cell
Cytotoxicity
Molecular Biology
Zebrafish
Cell Proliferation
Dose-Response Relationship, Drug
Molecular Structure
biology
010405 organic chemistry
Chemistry
Cell Cycle
Organic Chemistry
Myeloid leukemia
Cancer
Neoplasms, Experimental
biology.organism_classification
medicine.disease
Antineoplastic Agents, Phytogenic
0104 chemical sciences
Plant Leaves
Disease Models, Animal
010404 medicinal & biomolecular chemistry
Phytochemical
Diterpenes
Drug Screening Assays, Antitumor
Subjects
Details
- ISSN :
- 00452068
- Volume :
- 98
- Database :
- OpenAIRE
- Journal :
- Bioorganic Chemistry
- Accession number :
- edsair.doi.dedup.....2ded09a433308afb5f9acb08bd0e354e