In vitro inhibition of 1,3-beta-glucan synthase by glycolipids from convolvulaceous species.
Sixteen convolvulaceous glycolipids selected from the tricolorin (1 - 7) and orizabin (8 - 16) series, proved to be strong in vitro inhibitors of the enzyme that catalyzes the synthesis of 1,3-beta-D-glucan, a major polymer of fungal cell-walls. Results provide an insight into function of the specific structures of these complex macrocyclic lactones as inhibitors of the 1,3-beta-D-glucan synthase and open the possibility of using these compounds as starting points for the development of antifungal agents that act by inhibiting fungal cell-wall synthesis.
Castelli
María V
MV
Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Rosario, Argentina.
Cortés
Juan C G
JC
Escalante
Andrea M
AM
Bah
Moustapha
M
Pereda-Miranda
Rogelio
R
Ribas
Juan C
JC
Zacchino
Susana A
SA
D000935:Antifungal Agents / Q000494:pharmacology*; D027722:Convolvulaceae / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D005964:Glucosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006017:Glycolipids / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008565:Membrane Proteins; D015394:Molecular Structure; D029702:Schizosaccharomyces pombe Proteins
D000935:Antifungal Agents; D006017:Glycolipids; D008565:Membrane Proteins; D029702:Schizosaccharomyces pombe Proteins; D005964:Glucosyltransferases; C020570:1,3-beta-glucan synthase