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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Bulbispermine: A Crinine-Type Amaryllidaceae Alkaloid Exhibiting Cytostatic Activity toward Apoptosis-Resistant Glioma Cells
ChemMedChem, Volume 7, No. 5, Year 2012
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Description
The Amaryllidaceae alkaloid bulbispermine was derivatized to produce a small group of synthetic analogues. These, together with bulbispermine's natural crinine-type congeners, were evaluated invitro against a panel of cancer cell lines with various levels of resistance to pro-apoptotic stimuli. Bulbispermine, haemanthamine, and haemanthidine showed the most potent antiproliferative activities as determined by the MTT colorimetric assay. Among the synthetic bulbispermine analogues, only the C1,C2-dicarbamate derivative exhibited notable growth inhibitory properties. All active compounds were found not to discriminate between the cancer cell lines based on the apoptosis sensitivity criterion; they displayed similar potencies in both cell types, indicating that the induction of apoptosis is not the primary mechanism responsible for antiproliferative activity in this series of compounds. It was also found that bulbispermine inhibits the proliferation of glioblastoma cells through cytostatic effects, possibly arising from rigidification of the actin cytoskeleton. These findings lead us to argue that crinine-type alkaloids are potentially useful drug leads for the treatment of apoptosis-resistant cancers and glioblastoma in particular. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Authors & Co-Authors
Luchetti, Giovanni
United States, Socorro
New Mexico Institute of Mining and Technology
Johnston, Robert
United States, Socorro
New Mexico Institute of Mining and Technology
Mathieu, Véronique
Belgium, Brussels
Université Libre de Bruxelles
Lefranc, Florence
Belgium, Brussels
Université Libre de Bruxelles
Belgium, Brussels
Hôpital Erasme
Hayden, Kathryn
United States, Socorro
New Mexico Institute of Mining and Technology
Andolfi, Anna
Italy, Naples
Università Degli Studi Di Napoli Federico Ii
Lamoral-Theys, Delphine
Belgium, Brussels
Université Libre de Bruxelles
Reisenauer, Mary Rose
United States, Socorro
New Mexico Institute of Mining and Technology
Champion, Cody J.
United States, Socorro
New Mexico Institute of Mining and Technology
Pelly, Stephen C.
South Africa, Stellenbosch
Stellenbosch University
van Otterlo, Willem A. L.
South Africa, Stellenbosch
Stellenbosch University
Magedov, Igor V.
United States, Socorro
New Mexico Institute of Mining and Technology
Kiss, Robert
Belgium, Brussels
Université Libre de Bruxelles
Evidente, Antonio
Italy, Naples
Università Degli Studi Di Napoli Federico Ii
Rogelj, Snežna
United States, Socorro
New Mexico Institute of Mining and Technology
Kornienko, Alexander V.
United States, Socorro
New Mexico Institute of Mining and Technology
Statistics
Citations: 35
Authors: 16
Affiliations: 5
Identifiers
Doi:
10.1002/cmdc.201100608
ISSN:
18607179
e-ISSN:
18607187
Research Areas
Cancer