Synthetic analogues of flavonoids with improved activity against platelet activation and aggregation as novel prototypes of food supplements. (15th May 2015)

• Record Type: Journal Article
• Authors: Del Turco, Serena; Sartini, Stefania; Cigni, Giulia; Sentieri, Cassandra; Sbrana, Silverio; Battaglia, Debora; Papa, Angela; Da Settimo, Federico; La Motta, Concettina; Basta, Giuseppina
• Is Part Of: Food chemistry. Volume 175(2015)
• Page Start: 494
• Page End: 499
• Publication Date: 2015-05-15
• Subjects: Quercetin, 2-(3, 4-dihydroxyphenyl)-3, 5, 7-trihydroxychromen-4-one (PubChem CID: 5280343) -- Apigenin, 5, 7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one (PubChem CID: 5280443) -- 2-Phenyl-4H-pyrido[1, 2-a]pyrimidin-4-one derivatives, 1–4 (Chart 1) -- 2, 3-Diphenyl-4H-pyrido[1, 2-a]pyrimidin-4-one derivatives, 5–7 (Chart 1); Quercetin -- Apigenin -- Platelet aggregation -- P-selectin expression -- 2-Phenyl-4H-pyrido[1, 2-a]pyrimidin-4-ones -- 2, 3-Diphenyl-4H-pyrido[1, 2-a]pyrimidin-4-ones; Food -- Analysis -- Periodicals; Food -- Composition -- Periodicals; 664
• DOI: 10.1016/j.foodchem.2014.12.005
• Languages: English
• ISSNs: 0308-8146

Abstract

Highlights: New synthetic analogues of flavonoids modulate platelet aggregation and activation. They are more effective than two well known flavonoids, quercetin and apigenin. They represent novel prototypes of food supplements. Abstract: We investigated the ability of quercetin and apigenin to modulate platelet activation and aggregation, and compared the observed efficacy with that displayed by their synthetic analogues 2-phenyl-4 H -pyrido[1, 2- a ]pyrimidin-4-ones, 1 –4, and 2, 3-diphenyl-4 H -pyrido[1, 2- a ]pyrimidin-4-ones, 5 –7 . Platelet aggregation was explored through a spectrophotometric assay on platelet-rich plasma (PRP) treated with the thromboxane A2 mimetic U46619, collagen and thrombin in presence/absence of various bioisosteres of flavonoids (12.5–25–50–100 μM). The platelet density, (mean platelet component, MPC), was measured by the Advia 120 Hematology System as a marker surrogate of platelet activation. The induced P-selectin expression, which reflects platelet degranulation/activation, was quantified by flow cytometry on PRP. Our synthetic compounds modulated significantly both platelet activation and aggregation, thus turning out to be more effective than the analogues quercetin and apigenin when tested at a concentration fully consistent with their use in vivo . Accordingly, they might be used as food supplements to increase the efficacy of natural flavonoids.