Investigations of fungal secondary metabolites with potential anticancer activity.
Fourteen metabolites, isolated from phytopathogenic and toxigenic fungi, were evaluated for their in vitro antigrowth activity for six distinct cancer cell lines, using the MTT colorimetric assay. Bislongiquinolide (1) and dihydrotrichodimerol (5), which belong to the bisorbicillinoid structural class, displayed significant growth inhibitory activity against the six cancer cell lines studied, while the remaining compounds displayed weak or no activity. The data show that 1 and 5 have similar growth inhibitory activities with respect to those cancer cell lines that display certain levels of resistance to pro-apoptotic stimuli or those that are sensitive to apoptosis. Quantitative videomicroscopy analysis revealed that 1 and 5 exert their antiproliferative effect through cytostatic and not cytotoxic activity. The preliminary results from the current study have stimulated further structure-activity investigations with respect to the growth inhibitory activity of compounds belonging to the bisorbicillinoid group.
Balde
ElHadj Saidou
ES
Laboratoire de Toxicologie and Laboratoire de Chimie Analytique, Toxicologie et Chimie Physique Appliquee, Institut de Pharmacie, Universite Libre de Bruxelles (ULB), Brussels, Belgium.
Andolfi
Anna
A
Bruyère
Céline
C
Cimmino
Alessio
A
Lamoral-Theys
Delphine
D
Vurro
Maurizio
M
Damme
Marc Van
MV
Altomare
Claudio
C
Mathieu
Véronique
V
Kiss
Robert
R
Evidente
Antonio
A
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001231:Aspergillus flavus / Q000737:chemistry*; D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005658:Fungi / Q000737:chemistry; D006801:Humans; D051379:Mice; D018715:Microscopy, Video; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014242:Trichoderma / Q000737:chemistry*
D000970:Antineoplastic Agents; D001643:Bridged Bicyclo Compounds; D001952:Bridged-Ring Compounds; C473618:bisorbibutenolide; C508028:tetrahydrotrichodimerol; D015107:4-Butyrolactone