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Licochalcones extracted from Glycyrrhiza inflata inhibit platelet aggregation accompanied by inhibition of COX-1 activity.

ABSTRACT: Licochalcones extracted from Glycyrrhiza inflata are known to have a variety of biological properties such as anti-inflammatory, anti-bacterial, and anti-tumor activities, but their action on platelet aggregation has not yet been reported. Therefore, in this study we investigated the effects of licochalcones on platelet aggregation. Collagen and U46619, a thromboxane A2 receptor agonist, caused rabbit platelet aggregation, which was reversed by pretreatment with licochalcones A, C and D in concentration-dependent manners. Among these compounds, licochalcone A caused the most potent inhibitory effect on collagen-induced platelet aggregation. However, the licochalcones showed marginal inhibitory effects on thrombin or ADP-induced platelet aggregation. In addition to rabbit platelets, licochalcone A attenuated collagen-induced aggregation in human platelets. Because licochalcone A also inhibited arachidonic acid-induced platelet aggregation and production of thromboxane A2 induced by collagen in intact platelets, we further examined the direct interaction of licochalcone A with cyclooxygenase (COX)-1. As expected, licochalcone A caused an inhibitory effect on both COX-1 and COX-2 in vitro. Regarding the effect of licochalcone A on COX-1 enzyme reaction kinetics, although licochalcone A showed a stronger inhibition of prostaglandin E2 synthesis induced by lower concentrations of arachidonic acid, Vmax values in the presence or absence of licochalcone A were comparable, suggesting that it competes with arachidonic acid at the same binding site on COX-1. These results suggest that licochalcones inhibit collagen-induced platelet aggregation accompanied by inhibition of COX-1 activity.

SUBMITTER: Okuda-Tanino A

PROVIDER: S-EPMC5345862 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

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Licochalcones extracted from Glycyrrhiza inflata inhibit platelet aggregation accompanied by inhibition of COX-1 activity.

Okuda-Tanino Asa A Sugawara Daiki D Tashiro Takumi T Iwashita Masaya M Obara Yutaro Y Moriya Takahiro T Tsushima Chisato C Saigusa Daisuke D Tomioka Yoshihisa Y Ishii Kuniaki K Nakahata Norimichi N

PloS one 20170310 3

Licochalcones extracted from Glycyrrhiza inflata are known to have a variety of biological properties such as anti-inflammatory, anti-bacterial, and anti-tumor activities, but their action on platelet aggregation has not yet been reported. Therefore, in this study we investigated the effects of licochalcones on platelet aggregation. Collagen and U46619, a thromboxane A2 receptor agonist, caused rabbit platelet aggregation, which was reversed by pretreatment with licochalcones A, C and D in conce ...[more]

PMID: 28282426

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Project description:AimThe aim of this study was to evaluate the in vitro effect of coumarin and 15 monosubstituted derivatives on the inhibition of human platelet aggregation induced by various proaggregatory agonists, particularly by epinephrine.BackgroundThe emergence of residual platelet reactivity during the use of conventional antiplatelet agents (acetylsalicylic acid and clopidogrel) is one of the main causes of double therapy´s therapeutic failure. Platelet adrenoceptors participate in residual platelet reactivity. Therefore, it is necessary to develop new antiplatelet agents that inhibit epinephrine-induced platelet aggregation as a new therapeutic strategy. Information on the antiplatelet activity of coumarins in inhibiting epinephrine-induced aggregation is limited.ObjectiveThe objective of this study was to establish the structure-activity relationship (SAR) of coumarin derivatives with hydroxy, methoxy, and acetoxy groups in different positions of the coumarin nucleus to identify the most active molecules. Moreover, this study aimed to use in silico studies to suggest potential drug targets to which the molecules bind to produce antiplatelet effects.MethodsThe platelet aggregation was performed using a Lumi-aggregometer; the inhibitory activity of 16 compounds were evaluated by inducing the aggregation of human platelets (250 × 103/μl) with epinephrine (10 μM), collagen (2 μg/ml) or ADP (10 μM). The aggregation of control platelets was considered 100% of the response for each pro-aggregatory agonist.ResultsEleven molecules inhibited epinephrine-induced aggregation, with 3-acetoxycoumarin and 7-methoxycoumarin being the most active. Only coumarin inhibited collagen-induced platelet aggregation, but no molecule showed activity when using ADP as an inducer.ConclusionsIn silico studies suggest that most active molecules might have antagonistic interactions in the α2 and β2 adrenoceptors. The antiplatelet actions of these coumarins have the potential to reduce residual platelet reactivity and thus contribute to the development of future treatments for patients who do not respond adequately to conventional agents.

Project description:Background Soil salinization leads to a significant decline in crop yield and quality, including licorice, an important medicinal cash crop. Studies have proofed that the application of exogenous silicon can significantly improve the ability of licorice to resist salt stress, however, few studies concentrated on the effects of foliar silicon application on the morphology, physiological characteristics, and anatomical structure of licorice leaves under salt stress. In this study, the effects of Si (K2SiO3) on the structural and physiological characteristics of Glycyrrhiza uralensis Fisch. and G. inflata Bat. leaves under different salt concentrations (medium- and high-salt) were studied. Results Compared with the control (without salt), the plant height, total dry weight, leaf area, leaf number, relative water content, xylem area, phloem area, ratio of palisade to spongy tissue, gas exchange parameters, and photosynthetic pigment content of both licorice varieties were significantly reduced under high-salt (12S) conditions. However, the thickness of the leaf, palisade tissue, and spongy tissue increased significantly. Applying Si to the leaf surface increased the area of the vascular bundle, xylem, and parenchyma of the leaf’s main vein, promoted water transportation, enhanced the relative leaf water content, and reduced the decomposition of photosynthetic pigments. These changes extended the area of photosynthesis and promoted the production and transportation of organic matter. G. uralensis had a better response to Si application than did G. inflata. Conclusions In conclusion, foliar application of Si can improve water absorption, enhance photosynthesis, improve photosynthetic capacity and transpiration efficiency, promote growth and yield, and alleviate the adverse effects of salt stress on the leaf structure of the two kinds of licorice investigated. Supplementary Information The online version contains supplementary material available at 10.1186/s12870-022-03783-7.

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Licochalcones extracted from Glycyrrhiza inflata inhibit platelet aggregation accompanied by inhibition of COX-1 activity.

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Licochalcones extracted from Glycyrrhiza inflata inhibit platelet aggregation accompanied by inhibition of COX-1 activity.

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