Evaluation of the effects of several zoanthamine-type alkaloids on the aggregation of human platelets.
Ten zoanthamine-type alkaloids from two marine zoanthids belonging to the Zoanthus genus (Zoanthus nymphaeus and Zoanthus sp.) along with one semisynthetic derivative were evaluated for their antiplatelet activities on human platelet aggregation induced by several stimulating agents. 11-Hydroxyzoanthamine (11) and a synthetic derivative of norzoanthamine (16) showed strong inhibition against thrombin-, collagen- and arachidonic acid-induced aggregation, zoanthenol (15) displayed a selective inhibitory activity induced by collagen, while zoanthaminone (10) behaved as a potent aggregant agent. These evaluations allowed us to deduce several structure-activity relationships and suggest some mechanisms of action for this type of compounds.
Villar
Rosa M
RM
Departamento de Farmacoloxía, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Gil-Longo
José
J
Daranas
Antonio H
AH
Souto
María L
ML
Fernández
José J
JJ
Peixinho
Solange
S
Barral
Miguel A
MA
Santafé
Gilmar
G
Rodríguez
Jaime
J
Jiménez
Carlos
C
D000470:Alkaloids / Q000145:classification / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D037421:Anthozoa / Q000737:chemistry*; D000925:Anticoagulants / Q000494:pharmacology*; D016718:Arachidonic Acid; D001792:Blood Platelets / Q000187:drug effects*; D003094:Collagen; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013917:Thrombin
D000470:Alkaloids; D000925:Anticoagulants; D006571:Heterocyclic Compounds; D010975:Platelet Aggregation Inhibitors; D016718:Arachidonic Acid; D003094:Collagen; D013917:Thrombin