Evaluation of antiaggregatory activity of flavonoid aglycone series

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Abstract

Background

Among natural compounds, present in every day diet, flavonoids have shown beneficial effect in prevention of cardiovascular diseases that can be attributed, at least partially to the described antiaggregatory activity i.e. antiplatelet effects of flavonoids. Due to the ever increasing pharmacological interest in antiplatelet agents a systematic experimental evaluation of large flavonoid series is needed.

Methods

A set of thirty flavonoid aglycones has been selected for the evaluation. All measurements of aggregation were done under standardized and firmly controlled in vitro conditions. The whole blood samples, multiple platelet functional analyzer and adenosine diphosphate (ADP) as a weak agonist of aggregation were selected for this purpose.

Results

The results were expressed as minimal concentration of flavonoid that can significantly lower the platelet aggregation compared to the corresponding untreated sample (minimal antiaggregatory concentration - MINaAC). All analyzed flavonoids exhibited antiaggregatory activity MINaAC ranging from 0.119 μM to 122 μM, while the most potent representatives were 3,6-dihydroxyflavone (0.119 μM) and syringetin (0.119 μM).

Conclusions

Measurable antiplatelet activity established at submicromolar flavonoid concentrations suggests that even a dietary consumption of some flavonoids can make an impact on in vivo aggregation of platelets. These findings also point out a therapeutical potential of some flavonoids.

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Most cited references 25

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Intake of potentially anticarcinogenic flavonoids and their determinants in adults in The Netherlands.

M. G. L. Hertog, P Hollman, M Katan … (1993)

Flavonoids are strong antioxidants that occur naturally in foods and can inhibit carcinogenesis in rodents. Accurate data on population-wide intakes of flavonoids are not available. Here, using data of the Dutch National Food Consumption Survey 1987-1988, we report the intake of the potentially anticarcinogenic flavonoids quercetin, kaempferol, myricetin, apigenin, and luteolin among 4,112 adults. The flavonoid content of vegetables, fruits, and beverages was determined by high-performance liquid chromatography. In all subjects, average intake of all flavonoids combined was 23 mg/day. The most important flavonoid was the flavonol quercetin (mean intake 16 mg/day). The most important sources of flavonoids were tea (48% of total intake), onions (29%), and apples (7%). Flavonoid intake did not vary between seasons; it was not correlated with total energy intake (r = 0.001), and it was only weakly correlated with the intake of vitamin A (retinol equivalents, r = 0.14), dietary fiber (r = 0.21), and vitamin C (r = 0.26). Our use of new analytic technology suggests that in the past flavonoid intake has been overestimated fivefold. However, on a milligram-per-day basis, the intake of the antioxidant flavonoids still exceeded that of the antioxidants beta-carotene and vitamin E. Thus flavonoids represent an important source of antioxidants in the human diet.

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Thromboxane A2: physiology/pathophysiology, cellular signal transduction and pharmacology.

Norimichi Nakahata (2008)

Thromboxane A(2) (TXA(2)), an unstable arachidonic acid metabolite, elicits diverse physiological/pathophysiological actions, including platelet aggregation and smooth muscle contraction. TXA(2) has been shown to be involved in allergies, modulation of acquired immunity, atherogenesis, neovascularization, and metastasis of cancer cells. The TXA(2) receptor (TP) communicates mainly with G(q) and G(13), resulting in phospholipase C activation and RhoGEF activation, respectively. In addition, TP couples with G(11), G(12), G(13), G(14), G(15), G(16), G(i), G(s) and G(h). TP is widely distributed in the body, and is expressed at high levels in thymus and spleen. The second extracellular loop of TP is an important ligand-binding site, and Asp(193) is a key amino acid. There are two alternatively spliced isoforms of TP, TPalpha and TPbeta, which differ only in their C-terminals. TPalpha and TPbeta communicate with different G proteins, and undergo hetero-dimerization, resulting in changes in intracellular traffic and receptor protein conformations. TP cross-talks with receptor tyrosine kinases, such as EGF receptor, to induce cell proliferation and differentiation. TP is glycosylated in the N-terminal region for recruitment to plasma membranes. Furthermore, TP conformation is changed by coupling to G proteins, showing several states of agonist binding. Finally, several drugs modify TP-mediated events; these include cyclooxygenase inhibitors, TXA(2) synthase inhibitors and TP antagonists. Some flavonoids of natural origin also have TP receptor antagonistic activity. Recent advances in TP research have clarified TXA(2)-mediated events in detail, and further study will supply more beneficial information about TXA(2) pathophysiology.

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Select flavonoids and whole juice from purple grapes inhibit platelet function and enhance nitric oxide release.

Mark Iafrati, B Frei, Kristen L. Deak … (2001)

Moderate red wine consumption is inversely associated with coronary ischemia, and both red wine and purple grape juice (PGJ) contain flavonoids with antioxidant and antiplatelet properties believed to be protective against cardiovascular events. Acute cardiac events are also associated with decreased platelet-derived nitric oxide (NO) release. In this study, the effects of PGJ and PGJ-derived flavonoids on platelet function and platelet NO production were determined. Incubation of platelets with dilute PGJ led to inhibition of aggregation, enhanced release of platelet-derived NO, and decreased superoxide production. To confirm the in vivo relevance of these findings, 20 healthy subjects consumed 7 mL. kg(-1). d(-1) of PGJ for 14 days. Platelet aggregation was inhibited after PGJ supplementation, platelet-derived NO production increased from 3.5+/-1.2 to 6.0+/-1.5 pmol/10(8) platelets, and superoxide release decreased from 29.5+/-5.0 to 19.2+/-3.1 arbitrary units (P<0.007 and P<0.05, respectively). alpha-Tocopherol levels increased significantly after PGJ consumption (from 15.6+/-0.7 to 17.6+/-0.9 micromol/L; P<0.009), and the plasma protein-independent antioxidant activity increased by 50.0% (P<0.05). Last, incubation of platelets with select flavonoid fractions isolated from PGJ consistently attenuated superoxide levels but had variable effects on whole-blood aggregation, platelet aggregation, and NO release. Both in vitro incubation and oral supplementation with PGJ decrease platelet aggregation, increase platelet-derived NO release, and decrease superoxide production. These findings may be a result of antioxidant-sparing and/or direct effects of select flavonoids found in PGJ. The suppression of platelet-mediated thrombosis represents a potential mechanism for the beneficial effects of purple grape products, independent of alcohol consumption, in cardiovascular disease.

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Author and article information

Journal

Journal ID (nlm-ta): Nutr J

Title: Nutrition Journal

Publisher: BioMed Central

ISSN (Electronic): 1475-2891

Publication date Collection: 2011

Publication date (Electronic): 11 July 2011

Volume: 10

Page: 73

Affiliations

[1 ]University of Zagreb, Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, A. Kovačića 1, 10000 Zagreb, Croatia

[2 ]Department of Clinical Laboratory Diagnostics, CHC Osijek, J. Huttlera 4, 31000 Osijek, Croatia

[3 ]Croatian Institute of Transfusion Medicine, Department of Platelet and Leukocyte Immunology, Petrova 3, 10000 Zagreb, Croatia

[4 ]Agency for Medicinal Products and Medical Devices of Croatia, Ksaverska cesta 4, Zagreb, Croatia

Article

Publisher ID: 1475-2891-10-73

DOI: 10.1186/1475-2891-10-73

PMC ID: 3166895

PubMed ID: 21745360

SO-VID: 1caa780d-5d16-4132-9ac7-33bcc6e5184d

License:

This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Evaluation of antiaggregatory activity of flavonoid aglycone series

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Abstract

Background

Methods

Results

Conclusions

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Karger: Nutrition and Dietetics

Most cited references 25

Intake of potentially anticarcinogenic flavonoids and their determinants in adults in The Netherlands.

Thromboxane A2: physiology/pathophysiology, cellular signal transduction and pharmacology.

Select flavonoids and whole juice from purple grapes inhibit platelet function and enhance nitric oxide release.

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