Bioassay-Guided Isolation and HPLC Determination of Bioactive Compound That Relate to the Antiplatelet Activity (Adhesion, Secretion, and Aggregation) fromSolanum lycopersicum

Abstract

In seeking the functionality of foodstuff applicable to medicine, ripe tomato fruits were found to show an antiplatelet activity. Therefore, the bioactive compound was isolated, structurally identified, and studied for an inhibitory effects on platelet adhesion, secretion, and aggregation. The concentration of adenosine in ripe tomato fruits (pulp and skin extracts) and its processing by-products (paste and pomace) was determined by reversed-phase high-performance liquid chromatography (HPLC). According to platelet aggregation inhibition induced by ADP, the total extract residual was fractionated by liquid-liquid separation, obtaining aqueous, ethyl acetate and petroleum ether extracts. The aqueous extract was subjected to repeated permeation over sephadex LH-20 and semipreparative TLC. The isolate finally obtained was identified as adenosine on the basis of ESI-MS, 1H NMR, HPLC, and UV spectra. Adenosine concentration dependently (2.3–457 μM) platelet aggregation inhibited induced by ADP. Also, adenosine present inhibition of platelet secretion and thrombus formation under flow conditions. The quantitative HPLC analysis revealed significant amounts of adenosine in ripe tomato fruits and its processing by-products. From these results, extracts/fractions of ripe tomato fruits and their processing by-products may be referred to as functional food and functional ingredients containing a compound that inhibits platelet function with a potent preventive effect on thrombus formation, as those that occur in stroke.

Fruitflow®: the first European Food Safety Authority-approved natural cardio-protective functional ingredient

“…In summary, these results demonstrating the actions of tAF on different platelet functions were all consistent with potential effects mediated partly through polyphenols and PDI and partly through nucleosides elevating cAMP and cGMP levels in platelets [13, 67]. Effects on TF binding suggested that tAF components could have a larger effect on some aspects of the coagulatory response, such as thrombin generation, than previously imagined.…”

Inhibitory effects ofCyperus digitatusextract on human platelet functionin vitro

“…In addition, our group recently isolated and identified adenosine and guanosine from S. lycopersicum. Adenosine and guanosine at a low concentration showed potent antiplatelet activity through the inhibition of platelet secretion, adhesion, and aggregation [15,41]. In the present study, we extended these observations by exploring the antiplatelet effects of extracts and fractions from C. digitatus.…”

Protective Mechanisms ofS. lycopersicumAqueous Fraction (Nucleosides and Flavonoids) on Platelet Activation and Thrombus Formation:In Vitro,Ex VivoandIn VivoStudies

“…Because we have recently demonstrated that the aqueous fraction from S. lycopersicum contains significant amounts of adenosine [20], we hypothesized that the antiplatelet effect could be exerted by rising cAMP levels. At 1 mg/mL the aqueous fraction significantly increased the intraplatelet levels of cAMP from 3.5 ± 1 to 20 ± 2 pmol/10 8 platelets ( P < 0.05).…”

“…Total extract and aqueous fraction from Solanum lycopersicum were obtained according to Fuentes et al [20]. Briefly, the total extract was fractionated by liquid-liquid separation, obtaining an aqueous, ethyl acetate, and petroleum ether fractions.…”