title: Molecular mechanism of tanshinone IIA and cryptotanshinone in platelet anti-aggregating effects: an integrated study of pharmacology and computational analysis.
abstract: Tanshinone IIA and cryptotanshinone are two pharmacologically active diterpenoids extracted from the roots of Salvia milthiorriza Bunge, a plant used in Chinese traditional medicine for the treatment of some cardiovascular and cerebrovascular disease. Until now, the molecular mechanisms of action of these two diterpenoids on platelets are partially known. To clarify this aspect, here we utilized an integrated study of pharmacology and computational analysis. Our results demonstrate that cryptotanshinone is able to inhibit in a concentration dependent manner the rat platelet aggregation and also is endowed of Gi-coupled P2Y12 receptor antagonist as demonstrated by docking studies. This computational method was also performed for tanshinone IIA demonstrating even for this diterpenoid an interaction with the same receptor. The findings from our study enable a better understanding of tanshinone IIA and cryptotanshinone biological properties, which could ultimately lead to the development of novel pharmaceutical strategies for the treatment and/or prevention of some cardiovascular disease.
authors.affiliation: Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Maione
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
authors.forename: Vincenza
authors.initials: V
authors.lastname: Cantone
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
authors.forename: Maria Giovanna
authors.initials: MG
authors.lastname: Chini
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
authors.forename: Vincenzo
authors.initials: V
authors.lastname: De Feo
authors.affiliation: Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy. Electronic address: nmascolo@unina.it.
authors.forename: Nicola
authors.initials: N
authors.lastname: Mascolo
authors.affiliation: Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy. Electronic address: bifulco@unisa.it.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Bifulco
mesh_terms: D045784:Abietanes / Q000494:pharmacology*; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects*; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D008297:Male; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D010616:Phenanthrenes / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D058921:Purinergic P2Y Receptor Antagonists / Q000494:pharmacology; D017208:Rats, Wistar
chemical_list: D045784:Abietanes; D004365:Drugs, Chinese Herbal; D010616:Phenanthrenes; D058921:Purinergic P2Y Receptor Antagonists; C021751:tanshinone; C037886:cryptotanshinone
keywords: Docking study; P2Y receptors; Platelet aggregation; Salvia miltiorrhiza Bunge; Tanshinones