Cyclodextrin enhances spermicidal effects of magainin-2-amide.
Magainins are antimicrobial peptides with known spermicidal activity. Their activity is inhibited by cholesterol present in eukaryotic cell membranes. Pretreatment of spermatozoa with methyl-beta-cyclodextrin, which extracts cholesterol from cell membranes and induces capacitation, sensitizes them to magainin-2-amide as shown by a decrease in human sperm motility determined by computer-assisted sperm analysis and a concomitant decrease in sperm viability, as measured by MitoTracker(R) Red CMXRos labeling. Magainin-2-amide affects mainly the fast progressive spermatozoa inducing them directly into an immotile state, without an increase in motile non-progressive and slow progressive spermatozoa. We conclude that methyl-beta-cyclodextrin highly potentiates the deleterious effect of magainin-2-amide on human spermatozoa. Most probably, this effect can be explained by cholesterol extraction from sperm cell membranes.
Wojcik
C
C
Department of Histology and Embryology, Institute of Biostructure, Warsaw Medical Academy, Warsaw, Poland.
Sawicki
W
W
Marianowski
P
P
Benchaib
M
M
Czyba
J C
JC
Guerin
J F
JF
D000818:Animals; D000890:Anti-Infective Agents; D023181:Antimicrobial Cationic Peptides / Q000008:administration & dosage / Q000494:pharmacology*; D002462:Cell Membrane / Q000378:metabolism; D002478:Cells, Cultured; D002784:Cholesterol / Q000378:metabolism; D003270:Contraceptive Agents; D003505:Cyclodextrins / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D054806:Magainins; D008297:Male; D013075:Sperm Capacitation / Q000187:drug effects; D013094:Spermatozoa / Q000187:drug effects; D029867:Xenopus Proteins; D014982:Xenopus laevis; D047392:beta-Cyclodextrins
D000890:Anti-Infective Agents; D023181:Antimicrobial Cationic Peptides; D003270:Contraceptive Agents; D003505:Cyclodextrins; D054806:Magainins; D029867:Xenopus Proteins; D047392:beta-Cyclodextrins; C108732:methyl-beta-cyclodextrin; C053301:magainin 2 peptide, Xenopus; D002784:Cholesterol