Antithrombotic effect of Glycyrrhizin, a plant-derived thrombin inhibitor

Mendes‐Silva, Wallace; Assafim, Mariane; Ruta, Bruno; Monteiro, Robson Q.; Guimarães, Jorge A.; Zingali, Russolina B.

doi:10.1016/j.thromres.2003.10.014

Cited by 86 publications

(52 citation statements)

References 30 publications

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“…This and consecutive studies indicate potential applications of proteinase inhibitors in plant protection, agriculture and biotechnology. Plant proteinase inhibitors possess specificities for animal and microbial enzymes (Sanchez-Serrano et al 1986), therefore interactions of proteinase inhibitors with relevant enzymes can lead to the exploitation of natural plant inhibitors or extracts in synthetic drug development and therapeutic applications in medicine (Birk 1993;Banerji & Fernandes 1994;Mendes-Silva et al 2003;Neuhof et al 2003;Park & Ohba 2004). From this point of view, mainly Trifolium pratense accessions exhibiting the highest relative TrIA in our study could be interesting for additional and relevant testing.…”

Section: Resultsmentioning

confidence: 84%

Proteinase inhibition and antioxidant activity of selected forage crops

et al. 2010

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The hypothesis of the possible therapeutic potential of selected species of forage crops is discussed. Extracts from genotypes of Anthyllis sp., Astragalus sp., Coronilla sp., Lotus sp., Medicago sp., Melilotus sp., Onobrychis sp. and Trifolium sp. were prepared and tested for proteinase inhibition and antioxidant activities. We found that Trifolium pratense accession POLKIE99-3 expressed the highest relative trypsin inhibition activity (80.0%) compared to standards. The highest thrombin inhibition activity (81.4%) was detected in the Medicago sativa old cultivar Hodonínka, whereas the highest relative urokinase inhibition activity (62.5%) was expressed by the local population Nitranka. Relatively high antioxidant properties of Trifolium sp. accessions, Trifolium pratense genetic resources SVKZAH98-40, were of interest. Results of this study confirmed that there are significant differences in proteinase inhibition and antioxidant activity among important selected agricultural crops. The present paper may also be the starting point of the research aimed for development of new functional food and nutraceuticals, and/or of the research focused on new secondary metabolites with potential as bioactive compounds.Key words: trypsin; thrombin; urokinase; inhibition; antioxidant; activity; forage crops.Abbreviations: AOX, antioxidant activity; BBI, Bowman-Birk inhibitor; DMSO, dimethyl sulphoxide; Rel%BT, relative percentage value of activity to standardized black tea extract; Rel%Q, relative percentage value of activity to standard quercetin; SHE, sunflower oil hydrolysate ethanol; SITh, selectivity index of thrombin; SIU, selectivity index of urokinase; ThIA, thrombin inhibition activity; TrIA, trypsin inhibition activities; UIA, urokinase inhibition activity.

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Section: Resultsmentioning

confidence: 84%

Proteinase inhibition and antioxidant activity of selected forage crops

et al. 2010

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“…The drugs were administered one hour before thrombosis induction. Thrombus formation by a combination of stasis and hypercoagulability was induced after administration of each compound, as described by Mendes-Silva and coworkers 17) with slight modifications. The animals had been previously anesthetized with xylazine (16 mg/kg, intramuscularly) followed by ketamine (100 mg/kg, intramuscularly).…”

Section: Stasis-induced Thrombus Formationmentioning

confidence: 99%

Oral Antithrombotic Effects of Acylhydrazone Derivatives

Frattani

Coriolano

Lima

et al. 2013

JAT

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Aim:In the search for new antithrombotic drug candidates, the synthesis and anti-platelet activity of a new series of N-acylhydrazones that were designed as thrombin inhibitors has been previously described. The aim of this work was to further characterize the effects of these compounds on thrombin-induced platelet aggregation and induced thrombosis in vivo. Methods: In this work, four compounds were tested, LASSBio-693, 694, 743 and 752, on platelet aggregation induced by thrombin, ADP and TRAP-4A. These compounds were further tested using a mouse pulmonary thromboembolism model induced by collagen (500 μg/kg) and norepinephrine (80 μg/kg) or thrombin (2,000 UI), and a deep venous thrombosis model.

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“…In the period covered by this review, some new pharmacological activities were reported for GL (1), such as: antiviral (against flavivirus3 6 , HIV 37 and SARScoronavirus 38 ) antiallergic, 39 antithrombotic in experimental models in rats, 40,41 capable of lowering hepatocellular carcinogenesis rates in patients with interferon-resistant active chronic hepatitis C, 42 presenting a protective in vitro effect in gastric epithelial cells against H 2 O 2 -induced cell death 43 and as an inhibitor of influenza A virus uptake into human lung cells. 44 GL and GLA (2) were also reported as possessing a protective effect on acute cholestasis induced by α-naphtyl isocyanate in rats 45 and GLA was reported as an apoptosis inductor in human hepatoma, promyelotic leukemia and stomach cancer cells, 46 as an antihyperglycemic agent in rats with streptozocin-induced diabetes, 47 and as presenting antiviral activity against herpes simpex virus 1 (HSV-1).…”

Section: New Pharmacological Activities Reported For Gl and Glamentioning

confidence: 99%

“…49 GL is also described as an inhibitor of thrombin, a protease involved in the blood clotting cascade. 40 As mentioned before, the antiinflammatory activity of GL and GLA is accounted for the inhibition of the β-hydroxysteroid dehydrogenase enzyme 2 (β-HSD-2), an enzyme responsible for the conversion of the glucocorticoid hormone cortisol in its active form cortisone.…”

Section: New Pharmacological Activities Reported For Gl and Glamentioning

confidence: 99%

Glycyrrhizin and glycyrrhetic acid: scaffolds to promising new pharmacologically active compounds

Graebin¹,

Verli²,

Guimarães³

2010

J. Braz. Chem. Soc.

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O ácido glicirrizínico (GL), também conhecido como glicirrizina, é uma saponina triterpênica, um produto natural encontrado na raiz de Glycyrrhyza glabra L. ("licquorice" ou "alcaçuz"), utilizada mundialmente como edulcorante e também na medicina tradicional do Oriente. Este artigo de revisão enfoca os novos compostos sintetizados usando GL ou sua aglicona, o ácido glicirretínico (GLA), como materiais de partida e as atividades farmacológicas descritas para os mesmos e seus derivados.Glycyrrhizinic acid (GL), also known as glycyrrhizin, is a triterpene saponin, a natural product found on the root of Glycyrrhyza glabra L. ("licquorice"), used worldwide as sweetener and in the traditional eastern medicines. This review is focused on a series of new derivatives synthesized using GL and its aglycon, glycyrrhetinic acid (GLA), as starting materials, the pharmacological activities described for those compounds, as well as new activities reported for GL and GLA themselves.

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Antithrombotic effect of Glycyrrhizin, a plant-derived thrombin inhibitor

Cited by 86 publications

References 30 publications

Proteinase inhibition and antioxidant activity of selected forage crops

Proteinase inhibition and antioxidant activity of selected forage crops

Oral Antithrombotic Effects of Acylhydrazone Derivatives

Glycyrrhizin and glycyrrhetic acid: scaffolds to promising new pharmacologically active compounds

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