期刊
BIOORGANIC CHEMISTRY
卷 38, 期 1-3, 页码 108-114出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2009.12.001
关键词
Antioxidant activity; Platelet aggregation; Store-operated calcium entry; Hydroxytyrosyl gallate; Hydroxytyrosyl protocatechuate; Hydroxytyrosyl caffeate; Rosmarinic acid analogs
资金
- Spanish Ministerio de Ciencia e Innovacion [BFU2007-60104, CTQ2005-07005]
- Junta de Extremadura-Fundesalud [PR108A003]
- Junta de Andalucia (FS/FN/ARM)
Polyphenols, such as rosmarinic acid, are widely distributed natural products with relevant antioxidant activity. Oxidative stress plays an important role in the pathogenesis of a number of disorders. Here, we report on the synthesis and biological effects of the polyphenolic esters hydroxytyrosyl gallate (1), hydroxytyrosyl protocatechuate (2) and hydroxytyrosyl caffeate (3), structurally related to rosmarinic acid. The three compounds showed a greater free radical scavenging activity than their precursors and also than rosmarinic acid. Esters 1 and 3 significantly reduced thrombin-evoked platelet aggregation, which is likely mediated to the attenuation of thrombin-stimulated Ca2+ release and entry. The three compounds reduced the ability of platelets to accumulate Ca2+ in the intracellular stores, probably by enhancing the Ca2+ leakage rate and reduced store-operated Ca2+ entry in these cells. These observations suggest that the structurally-simplified analogs to rosmarinic acid, compounds 1 and 3, might be the base of therapeutic strategies to prevent thrombotic complications associated to platelet hyperaggregability due to oxidative stress. (C) 2009 Elsevier Inc. All rights reserved.
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