Dihydroartemisinin-Bile Acid Hybridization as an Effective Approach to Enhance Dihydroartemisinin Anticancer Activity.
antitumor agents
bile acids
dihydroartemisinin
hepatocellular carcinoma
natural products
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
03 04 2019
03 04 2019
Historique:
received:
28
11
2018
revised:
02
02
2019
pubmed:
7
2
2019
medline:
23
1
2020
entrez:
7
2
2019
Statut:
ppublish
Résumé
A series of hybrid compounds based on natural products-bile acids and dihydroartemisinin-were prepared by different synthetic methodologies and investigated for their in vitro biological activity against HL-60 leukemia and HepG2 hepatocellular carcinoma cell lines. Most of these hybrids presented significantly improved antiproliferative activities with respect to dihydroartemisinin and the parent bile acid. The two most potent hybrids of the series exhibited a 10.5- and 15.4-fold increase in cytotoxic activity respect to dihydroartemisinin alone in HL-60 and HepG2 cells, respectively. Strong evidence that an ursodeoxycholic acid hybrid induced apoptosis was obtained by flow cytometric analysis and western blot analysis.
Identifiants
pubmed: 30724466
doi: 10.1002/cmdc.201800756
doi:
Substances chimiques
Antineoplastic Agents
0
Artemisinins
0
Bile Acids and Salts
0
artenimol
6A9O50735X
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
779-787Informations de copyright
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.