Elephantopinolide A-P, germacrane-type sesquiterpene lactones from Elephantopus scaber induce apoptosis, autophagy and G2/M phase arrest in hepatocellular carcinoma cells.
Antineoplastic Agents
/ chemical synthesis
Apoptosis
/ drug effects
Autophagy
/ drug effects
Carcinoma, Hepatocellular
/ drug therapy
Cell Cycle Checkpoints
/ drug effects
Cell Division
/ drug effects
Cell Line, Tumor
Drug Screening Assays, Antitumor
G2 Phase
Humans
Lactones
/ chemistry
Liver Neoplasms
/ drug therapy
MAP Kinase Signaling System
Magnoliopsida
/ chemistry
Membrane Potential, Mitochondrial
/ drug effects
Models, Molecular
Plant Extracts
/ chemical synthesis
Proto-Oncogene Proteins c-akt
/ metabolism
Reactive Oxygen Species
/ metabolism
Sesquiterpenes
/ chemistry
Sesquiterpenes, Germacrane
/ chemistry
Structure-Activity Relationship
Anti-hepatocarcinoma effect
Apoptosis
Elephantopus scaber
Germacrane-type sesquiterpene lactones
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Jul 2020
15 Jul 2020
Historique:
received:
05
03
2020
revised:
17
04
2020
accepted:
17
04
2020
pubmed:
7
5
2020
medline:
27
1
2021
entrez:
7
5
2020
Statut:
ppublish
Résumé
Chromatographic purification of Elephantopus scaber led to 16 new germacrane-type sesquiterpene lactones (1-16), named elephantopinolide A-P, along with a known analogue (17). Their structures were confirmed by comprehensive spectroscopic analyses, single-crystal X-ray diffraction, and comparison between the experimental and calculated ECD spectra. Their hepatocellular inhibition activities against Hep3B and HepG2 cells were screened by MTT assay, and the structure-activity relationships were examined. The results revealed that 10 (IC
Identifiants
pubmed: 32371334
pii: S0223-5234(20)30332-9
doi: 10.1016/j.ejmech.2020.112362
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Lactones
0
Plant Extracts
0
Reactive Oxygen Species
0
Sesquiterpenes
0
Sesquiterpenes, Germacrane
0
Proto-Oncogene Proteins c-akt
EC 2.7.11.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112362Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
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.