Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis
- Publication type:
- Journal article
- Metadata:
-
- Autoren
- Alba G Blazquez
- Manuel Fernandez-Dolon
- Laura Sanchez-Vicente
- Alba D Maestre
- Ana B Gomez-San Miguel
- Marcelino Alvarez
- Maria A Serrano
- Herwig Jansen
- Thomas Efferth
- Jose JG Marin
- Marta R Romero
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000320838200053&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1016/j.bmc.2013.04.059
- eISSN
- 1464-3391
- Externe Identifier
- Clarivate Analytics Document Solution ID: 170GK
- PubMed Identifier: 23685181
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 14
- Zeitschrift
- BIOORGANIC & MEDICINAL CHEMISTRY
- Schlüsselwörter
- Chemotherapy
- HBV
- HCV
- Hepatoblastoma
- Hepatocarcinoma
- Paginierung
- 4432 - 4441
- Datum der Veröffentlichung
- 2013
- Status
- Published
- Titel
- Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis
- Sub types
- Article
- Ausgabe der Zeitschrift
- 21
Data source: Web of Science (Lite)
- Other metadata sources:
-
- Autoren
- Alba G Blazquez
- Manuel Fernandez-Dolon
- Laura Sanchez-Vicente
- Alba D Maestre
- Ana B Gomez-San Miguel
- Marcelino Alvarez
- Maria A Serrano
- Herwig Jansen
- Thomas Efferth
- Jose JG Marin
- Marta R Romero
- DOI
- 10.1016/j.bmc.2013.04.059
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 14
- Zeitschrift
- Bioorganic & Medicinal Chemistry
- Sprache
- en
- Paginierung
- 4432 - 4441
- Datum der Veröffentlichung
- 2013
- Status
- Published
- Herausgeber
- Elsevier BV
- Herausgeber URL
- http://dx.doi.org/10.1016/j.bmc.2013.04.059
- Datum der Datenerfassung
- 2023
- Titel
- Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis
- Ausgabe der Zeitschrift
- 21
Data source: Crossref
- Abstract
- Antitumor and antiviral properties of the antimalaria drug artemisinin from Artemisia annua have been reported. Novel artemisinin derivatives (AD1-AD8) have been synthesized and evaluated using in vitro models of liver/colon cancer and viral hepatitis B and C. Cell viability assays after treating human cell lines from hepatoblastoma (HepG2), hepatocarcinoma (SK-HEP-1), and colon adenocarcinoma (LS174T) with AD1-AD8 for a short (6h) and long (72h) period revealed that AD5 combined low acute toxicity together with high antiproliferative effect (IC50=1-5μM). Since iron-mediated activation of peroxide bond is involved in artemisinin antimalarial activity, the effect of iron(II)-glycine sulfate (ferrosanol) and iron(III)-containing protoporphyrin IX (hemin) was investigated. Ferrosanol, but not hemin, enhanced antiproliferative activity of AD5 if the cells were preloaded with AD5, but not if both compouds were added together. Five derivatives (AD1>AD2>AD7>AD3>AD8) were able to inhibit the cytopathic effect of bovine viral diarrhoea virus (BVDV), a surrogate in vitro model of hepatitis C virus (HCV), used here to evaluate the anti-Flaviviridae activity. Moreover, AD1 and AD2 inhibited the release of BVDV-RNA to the culture medium. Co-treatment with hemin or ferrosanol resulted in enhanced anti-Flaviviridae activity of AD1. In HepG2 cells permanently infected with hepatitis B virus (HBV), AD1 and AD4, at non-toxic concentrations for the host cells were able to reduce the release of HBV-DNA to the medium. In conclusion, high pharmacological interest deserving further evaluation in animal models has been identified for novel artemisinin-related drugs potentially useful for the treatment of liver cancer and viral hepatitis B and C.
- Addresses
- Laboratory of Experimental Hepatology and Drug Targeting (HEVERFARM), IBSAL, University of Salamanca, Spain.
- Autoren
- Alba G Blazquez
- Manuel Fernandez-Dolon
- Laura Sanchez-Vicente
- Alba D Maestre
- Ana B Gomez-San Miguel
- Marcelino Alvarez
- Maria A Serrano
- Herwig Jansen
- Thomas Efferth
- Thomas Efferth
- Jose JG Marin
- Marta R Romero
- DOI
- 10.1016/j.bmc.2013.04.059
- eISSN
- 1464-3391
- Externe Identifier
- PubMed Identifier: 23685181
- Open access
- false
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 14
- Zeitschrift
- Bioorganic & medicinal chemistry
- Schlüsselwörter
- Cell Line, Tumor
- Animals
- Humans
- Hepatitis, Viral, Human
- Colonic Neoplasms
- Liver Neoplasms
- Artemisinins
- Virus Replication
- Cell Proliferation
- Cell Survival
- Molecular Structure
- Sprache
- eng
- Medium
- Print-Electronic
- Online publication date
- 2013
- Paginierung
- 4432 - 4441
- Datum der Veröffentlichung
- 2013
- Status
- Published
- Datum der Datenerfassung
- 2013
- Titel
- Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
- Sub types
- Research Support, Non-U.S. Gov't
- Journal Article
- Ausgabe der Zeitschrift
- 21
Data source: Europe PubMed Central
- Abstract
- Antitumor and antiviral properties of the antimalaria drug artemisinin from Artemisia annua have been reported. Novel artemisinin derivatives (AD1-AD8) have been synthesized and evaluated using in vitro models of liver/colon cancer and viral hepatitis B and C. Cell viability assays after treating human cell lines from hepatoblastoma (HepG2), hepatocarcinoma (SK-HEP-1), and colon adenocarcinoma (LS174T) with AD1-AD8 for a short (6h) and long (72h) period revealed that AD5 combined low acute toxicity together with high antiproliferative effect (IC50=1-5μM). Since iron-mediated activation of peroxide bond is involved in artemisinin antimalarial activity, the effect of iron(II)-glycine sulfate (ferrosanol) and iron(III)-containing protoporphyrin IX (hemin) was investigated. Ferrosanol, but not hemin, enhanced antiproliferative activity of AD5 if the cells were preloaded with AD5, but not if both compouds were added together. Five derivatives (AD1>AD2>AD7>AD3>AD8) were able to inhibit the cytopathic effect of bovine viral diarrhoea virus (BVDV), a surrogate in vitro model of hepatitis C virus (HCV), used here to evaluate the anti-Flaviviridae activity. Moreover, AD1 and AD2 inhibited the release of BVDV-RNA to the culture medium. Co-treatment with hemin or ferrosanol resulted in enhanced anti-Flaviviridae activity of AD1. In HepG2 cells permanently infected with hepatitis B virus (HBV), AD1 and AD4, at non-toxic concentrations for the host cells were able to reduce the release of HBV-DNA to the medium. In conclusion, high pharmacological interest deserving further evaluation in animal models has been identified for novel artemisinin-related drugs potentially useful for the treatment of liver cancer and viral hepatitis B and C.
- Date of acceptance
- 2013
- Autoren
- Alba G Blazquez
- Manuel Fernandez-Dolon
- Laura Sanchez-Vicente
- Alba D Maestre
- Ana B Gomez-San Miguel
- Marcelino Alvarez
- Maria A Serrano
- Herwig Jansen
- Thomas Efferth
- Jose JG Marin
- Marta R Romero
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/23685181
- DOI
- 10.1016/j.bmc.2013.04.059
- eISSN
- 1464-3391
- Ausgabe der Veröffentlichung
- 14
- Zeitschrift
- Bioorg Med Chem
- Schlüsselwörter
- Animals
- Artemisinins
- Cell Line, Tumor
- Cell Proliferation
- Cell Survival
- Colonic Neoplasms
- Hepatitis, Viral, Human
- Humans
- Liver Neoplasms
- Molecular Structure
- Virus Replication
- Sprache
- eng
- Country
- England
- Paginierung
- 4432 - 4441
- PII
- S0968-0896(13)00385-4
- Datum der Veröffentlichung
- 2013
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2014
- Titel
- Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
- Sub types
- Journal Article
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 21
Data source: PubMed
- Beziehungen:
- Property of