title: Evaluation of the effects of several zoanthamine-type alkaloids on the aggregation of human platelets.
abstract: 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.
authors.affiliation: Departamento de Farmacoloxía, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
authors.forename: Rosa M
authors.initials: RM
authors.lastname: Villar
authors.forename: José
authors.initials: J
authors.lastname: Gil-Longo
authors.forename: Antonio H
authors.initials: AH
authors.lastname: Daranas
authors.forename: María L
authors.initials: ML
authors.lastname: Souto
authors.forename: José J
authors.initials: JJ
authors.lastname: Fernández
authors.forename: Solange
authors.initials: S
authors.lastname: Peixinho
authors.forename: Miguel A
authors.initials: MA
authors.lastname: Barral
authors.forename: Gilmar
authors.initials: G
authors.lastname: Santafé
authors.forename: Jaime
authors.initials: J
authors.lastname: Rodríguez
authors.forename: Carlos
authors.initials: C
authors.lastname: Jiménez
mesh_terms: 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
chemical_list: D000470:Alkaloids; D000925:Anticoagulants; D006571:Heterocyclic Compounds; D010975:Platelet Aggregation Inhibitors; D016718:Arachidonic Acid; D003094:Collagen; D013917:Thrombin