Extract of Glycyrrhiza glabra root attenuates nociception in experimental pain models: the role of BKCa channels / Extracto de raíz de Glycyrrhiza glabra atenúa la nocicepción en modelos experimentales de dolor: el rol de los canales BKCa

Abstract: The aim of this study was to evaluate the functional interaction of Glycyrrhiza glabra root extract (GGRE) on the large conductance Ca 2+ - activated K + (BKCa) channels expressed in the peripheral nervo us system by using nociception and inflammation models in rodents in vivo . Besides toxicity studies and open field tests, nociception and inflammation tests were performed on rodents. Different doses of GGRE were given orally to rats and mice. Naloxone, in domethacin, morphine, NS1619 and iberiotoxin (IbTX) were administered. GGRE had both anti - nociceptive and anti - inflammatory activity in rats and mice. GGRE exhibited an analgesic effect by decreasing the time - course of the pain threshold or reaction time i n some nociceptive tests. Furthermore, GGRE reduced level of pro - inflammatory cytokines, including TNF - α and IL - 1ß. As a conclusion, GGRE can alleviate the pain sensation of the afferent nerves and can reduce inflammation and associated pain by activating B KCa channels and reducing the levels of TNF - α, IL1ß

Resumen: El objetivo de este estudio fue evaluar la interacción funcional del extracto de raíz de Glycyrr hiza glabra (GGRE) en los canales de K + (BKCa) activados por Ca 2+ de gran conductancia expresados en el sistema nervioso periférico mediante el uso de modelos de nocicepción e inflamación en roedores in vivo . Además de los estudios de toxicidad y las prueb as de campo abierto, se realizaron pruebas de nocicepción e inflamación en roedores. Se administraron por vía oral diferentes dosis de GGRE a ratas y ratones. Se administraron naloxona, indometacina, morfina, NS1619 e iberiotoxina (IbTX). GGRE tenía activi dad tanto antinociceptiva como antiinflamatoria en ratas y ratones. GGRE mostró un efecto analgésico al disminuir la evolución temporal del umbral del dolor o el tiempo de reacción en algunas pruebas nociceptivas. Además, GGRE redujo el nivel de citocinas proinflamatorias, incluidas TNF - α e IL - 1ß. Como conclusión, GGRE puede aliviar la sensación de dolor de los nervios aferentes y puede reducir la inflamación y el dolor asociado activando los canales BKCa y reduciendo los niveles de TNF - α, IL1ß.

Preparation and characterization of active oxidized starch films containing licorice residue extracts and its potential against methicillin-resistant S. aureus.

The antibacterial and antioxidant packaging films were fabricated by incorporating licorice residue extracts (LREs) into oxidized starch (OS) films. The bioactive fraction (BF) was firstly obtained from LREs by using bioassay-guided isolation method. The BF showed potent anti-Gram(+) bacteria effects, especially against methicillin-resistant S. aureus (MRSA) with MIC of 32.5 µg/mL. The present results also indicated that the addition of BF could significantly decrease the moisture content, water vapor permeability, light transmittance of OS films. Notably, the antibacterial and antioxidant activities of OS films significantly enhanced with the concentration of BF increasing. Moreover, the films with the highest concentration of BF showed the lowest tensile strength (4.23 MPa) and the highest elongation at break (63.89%). Meanwhile, the bioactive films could release bioactive compounds such as licochalcone A and licochalcone B into the alcoholic and fatty food simulants. Taken together, the active OS films containing LREs have the potential for application in food packaging films, due to its potential against MRSA and antioxidant activity as well as good physicochemical properties.

Lipids Oxidative Stability and Microbial Shelf Life Quality of Licorice (Glycyrrhiza glabra L. ) Extract Supplemented Chicken Patties

The current study envisaged to evaluate the role of licorice (Glycyrrhiza glabra L.) extract on lipid oxidation, quality attributes, sensorial as well as microbial stability of chicken meat patties at refrigerated (4 ­C) storage. Accordingly, 4 levels of licorice extract were added @0.25, 0.5, 1.0 and 1.25% in chicken patties development process along with positive (0.25% butylatedhydroxyanisole) and negative control (without antioxidant). The developed patties were cooked and subjected to thiobarbituric acid reactive substances (TBARS), total phenolics (TPC), ferric reducing antioxidant power (FRAP), color, pH, sensory evaluation, total plate count (TPC) and Escherichia coli analysis at 0, 3rd and 7th day of storage. The findings indicated that the addition of licorice extract decreased malonaldehyde (MDA) generation along with higher pH and redness of patties (p0.05). The lowest MDA reported in T5 (1.25g LE/kg meat) was 0.63±0.04 whereas, the highest in T0 (control) was 0.90±0.02 that increased to 1.59±0.06 and 2.28±0.06 at the completion of the study. Also, the microbial load of chicken patties declined with treatments as indicated by the total plate count compared to the control. Conclusively, licorice extract incorporation in chicken patties is a pragmatic approach to improve oxidative stability, quality attributes and extended shelf life with preservation effect.

Lipids Oxidative Stability and Microbial Shelf Life Quality of Licorice (Glycyrrhiza glabra L. ) Extract Supplemented Chicken Patties

The current study envisaged to evaluate the role of licorice (Glycyrrhiza glabra L.) extract on lipid oxidation, quality attributes, sensorial as well as microbial stability of chicken meat patties at refrigerated (4 ­C) storage. Accordingly, 4 levels of licorice extract were added @0.25, 0.5, 1.0 and 1.25% in chicken patties development process along with positive (0.25% butylatedhydroxyanisole) and negative control (without antioxidant). The developed patties were cooked and subjected to thiobarbituric acid reactive substances (TBARS), total phenolics (TPC), ferric reducing antioxidant power (FRAP), color, pH, sensory evaluation, total plate count (TPC) and Escherichia coli analysis at 0, 3rd and 7th day of storage. The findings indicated that the addition of licorice extract decreased malonaldehyde (MDA) generation along with higher pH and redness of patties (p0.05). The lowest MDA reported in T5 (1.25g LE/kg meat) was 0.63±0.04 whereas, the highest in T0 (control) was 0.90±0.02 that increased to 1.59±0.06 and 2.28±0.06 at the completion of the study. Also, the microbial load of chicken patties declined with treatments as indicated by the total plate count compared to the control. Conclusively, licorice extract incorporation in chicken patties is a pragmatic approach to improve oxidative stability, quality attributes and extended shelf life with preservation effect.(AU)

Antibacterial Activity of Glycyrrhiza Glabra Roots against food-borne bacterial pathogens / Actividad Antibacteriana de la Raíz de Glycyrrhiza glabra Contra las Bacterias Patógenas Transmitidas por los Alimentos

ABSTRACT Objective: The antibacterial activity of Glycyrrhiza glabra (Liquorice) roots was evaluated against several food-borne bacterial pathogens. Methods: The in vitro anti-bacterial activity was evaluated by determining the zone diameter of inhibition (ZDI), minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) using the aqueous. Ethanolic and methanolic extracts of the roots of Glycyrrhiza glabra. Results: Therefore, significant increase in inhibitory feature was observed because of increase in extracts concentration. In addition, the aqueous extract was more effective than the others; while, among the tested bacteria, Staphylococcus aureus and Pseudomonas aeruginosa were the most sensitive and the most resistant, respectively. Conclusion: Extracts of Glycyrrhiza glabra roots can potentially be used in the pharmaceutical and food industries as preservatives or antimicrobial agents.

RESUMEN Objetivo: La actividad antibacteriana del extracto de raíces de Glycyrrhiza glabra (regaliz) fue evaluada frente a varias bacterias patógenas trasmitidas por los alimentos. Métodos: La actividad antimicrobiana se evalúa determinando el diámetro de la zona de inhibición (DZI), y la concentración bactericida mínima (CBM). Extractos acuosos, etanólicos y metanólicos de la raíz de Glycyrrhiza glabra fueron analizados en su actividad antibacteriana in vitro. Resultados: Por lo tanto, se observó un aumento significativo en la característica inhibitoria debido al aumento en la concentración de extractos. Además, el extracto acuoso fue más eficaz que los otros, en tanto que, entre las bacterias probadas, Staphylococcus aureus y Pseudomonas aeruginosa fueron las más sensibles y las más resistentes, respectivamente. Conclusión: Los resultados sugieren que los extractos de raíz de Glycyrrhiza glabra tienen un uso potencial en la industria farmacéutica y alimentaria, y pueden ser útiles como conservantes o agentes antimicrobianos.

To evaluate of the effect of adding licorice to the standard treatment regimen of Helicobacter pylori

ABSTRACT Objective: The aim of this study was to evaluate the effect of licorice in H. pylori eradication in patients suffering from dyspepsia either with peptic ulcer disease (PUD) or non-ulcer dyspepsia (NUD) in comparison to the clarithromycin-based standard triple regimen. Methods: In this randomized controlled clinical trial, 120 patients who had positive rapid urease test were included and assigned to two treatment groups: control group that received a clarithromycin-based triple regimen, and study group that received licorice in addition to the clarithromycin-based regimen for two weeks. H. pylori eradication was assessed six weeks after therapy. Data was analyzed by chi-square and t-test with SPSS 16 software. Results: Mean ages and SD were 38.8 ± 10.9 and 40.1 ± 10.4 for the study and control groups, respectively, statistically similar. Peptic ulcer was found in 30% of both groups. Response to treatment was 83.3% and 62.5% in the study and control groups, respectively. This difference was statistically significant. Conclusion: Addition of licorice to the triple clarithromycin-based regimen increases H. pylori eradication, especially in the presence of peptic ulcer disease.

To evaluate of the effect of adding licorice to the standard treatment regimen of Helicobacter pylori.

OBJECTIVE: The aim of this study was to evaluate the effect of licorice in H. pylori eradication in patients suffering from dyspepsia either with peptic ulcer disease (PUD) or non-ulcer dyspepsia (NUD) in comparison to the clarithromycin-based standard triple regimen. METHODS: In this randomized controlled clinical trial, 120 patients who had positive rapid urease test were included and assigned to two treatment groups: control group that received a clarithromycin-based triple regimen, and study group that received licorice in addition to the clarithromycin-based regimen for two weeks. H. pylori eradication was assessed six weeks after therapy. Data was analyzed by chi-square and t-test with SPSS 16 software. RESULTS: Mean ages and SD were 38.8±10.9 and 40.1±10.4 for the study and control groups, respectively, statistically similar. Peptic ulcer was found in 30% of both groups. Response to treatment was 83.3% and 62.5% in the study and control groups, respectively. This difference was statistically significant. CONCLUSION: Addition of licorice to the triple clarithromycin-based regimen increases H. pylori eradication, especially in the presence of peptic ulcer disease.

Schistosomicidal activity and docking of Schistosoma mansoni ATPDase 1 with licoflavone B isolated from Glycyrrhiza inflata (Fabaceae).

Schistosomiasis is one of the world's major public health problems, and its treatment is widely dependent on praziquantel (PZQ), the only available drug. Schistosoma mansoni ATP diphosphohydrolases are ecto-enzymes localized on the external tegumental surface of S. mansoni and considered an important target for action of new drugs. In this work, the in vitro schistosomicidal activity of the crude extract of Glycyrrhiza inflata roots (GI) and its isolated compounds echinatin, licoflavone A and licoflavone B were evaluated against S. mansoni adult worms. Results showed that GI (200 µg/mL) was active against adult schistosomes, causing 100% mortality after 24 h of incubation. Chromatographic fractionation of GI led to isolation of echinatin, licoflavone A and licoflavone B. Licoflavone B (25-100 µM) caused 100% mortality, tegumental alterations, and reduction of oviposition and motor activity of all adult worms, without affecting mammalian Vero cells. Confocal laser scanning microscopy showed tegumental morphological alterations and changes on the numbers of tubercles of S. mansoni worms in a dose-dependent manner after incubation with licoflavone B. Licoflavone B also showed high S. mansoni ATPase (IC50 of 23.78 µM) and ADPase (IC50 of 31.50 µM) inhibitory activities. Docking studies predicted different interactions between licoflavone B and S. mansoni ATPDase 1, corroborating with the in vitro inhibitory activity. This report demonstrated the first evidence for the schistosomicidal activity of licoflavone B and suggests that its mechanism of action involve the inhibition of S. mansoni ATP diphosphohydrolases.

Improving the thrombin inhibitory activity of glycyrrhizin, a triterpenic saponin, through a molecular simplification of the carbohydrate moiety.

Glycyrrhizin, a saponin, and its aglycone glycyrrhetinic acid are natural products found in the Liquorice (Glycyrrhiza glabra L.) root extract. This saponin is known for its in vitro and in vivo thrombin inhibitory activity. The design and synthesis of five glycyrrhizin derivatives were carried out to improve the natural product activity. Compound 3b, a phthalic ester derivative of glycyrrhizin, presented a more pronounced thrombin inhibition (IC50  = 114.4 ± 1.3 µm) than the saponin (IC50  = 235.7 ± 1.4 µm). Molecular docking simulations performed to investigate the molecular interaction between compound 3b and the enzyme indicate that this product is, as previously determined for glycyrrhizin, an allosteric thrombin inhibitor.

Association of emblica, licorice and belides as an alternative to hydroquinone in the clinical treatment of melasma.

BACKGROUND: Melasma is a common skin pigment disorder with a difficult clinical response to treatment. OBJECTIVES: To evaluate the clinical efficacy and safety of the association of Belides, Emblica and Licorice 7%, compared to Hydroquinone 2%, in the treatment of melasma. METHODS: After 60 days of exclusive use of an SPF35 sunscreen, 56 women, 18 to 60 years of age, phototypes I to IV, with epidermal or mixed melasma, were divided into two different groups in a mono-blind clinical study: A) cream with Belides, Emblica and Licorice, applied twice a day; B) cream with Hydroquinone 2%, used at night. They were observed in a 60-day study; every 15 days, they were submitted to medical evaluation, self-evaluation, and photographic registration (Visia(®)). RESULTS: 50 volunteers (89%), 23 in Group A and 27 in Group B, concluded the study. Two volunteers in Group A and 7 in Group B had mild skin adverse events. Depigmentation was observed through medical evaluation (Group A: 78.3%; Group B: 88.9%) and volunteers' self-evaluation (Group A: 91.3%; Group B: 92.6%); these results were statistically significant (p<0.001), with no differences between groups (p>0.05). This pattern of results was observed by Visia® in the number (p = 0.001) and size and tone (p<0.001) of the uv stains, for both groups, with no differences between them (p>0.05). CONCLUSION: There were no statistic differences between groups in the improvement of melasma. Group A showed less skin adverse events. Therefore, the association of Emblica, Licorice and Belides is a safe and efficient alternative for the treatment of melasma.

Associação de emblica, licorice e belides como alternativa à hidroquinona no tratamento clínico do melasma / Association of emblica, licorice and belides as an alternative to hydroquinone in the clinical treatment of melasma

FUNDAMENTOS: Melasma é uma melanodermia comum, cuja terapêutica representa um desafio clínico. OBJETIVOS: Avaliar a eficácia e segurança clínicas do complexo despigmentante emblica, licorice e belides, em comparação à hidroquinona 2 por cento, na abordagem do melasma. MÉTODOS: Após 60 dias de uso exclusivo de fotoprotetor FPS35, 56 mulheres com idades entre 18 e 60 anos, fotótipos I a IV, com melasma epidérmico ou misto, foram divididas em dois grupos de um estudo clínico monocego: A) creme contendo complexo despigmentante emblica, licorice e belides 7 por cento, usado duas vezes ao dia; B)creme de hidroquinona 2 por cento, usado à noite. O estudo durou 60 dias consecutivos e avaliações médica, das voluntárias (auto-avaliação) e fotográfica (Visia®) foram realizadas quinzenalmente. RESULTADOS: 89 por cento das voluntárias (50/56), 23 do Grupo A e 27 do Grupo B, concluíram o estudo. Duas voluntárias do Grupo A contra sete do Grupo B apresentaram eventos adversos leves transitórios. Houve despigmentação do melasma pelas avaliações médica (Grupo A: 78,3 por cento; Grupo B: 88,9 por cento) e auto-avaliação (Grupo A: 91,3 por cento; Grupo B: 92,6 por cento), todos estatisticamente significantes (p<0,001), sem diferenças entre os grupos (p>0,05). O mesmo padrão foi observado pelo Visia®, tanto no número (p = 0,001) quanto no tamanho e no tom (p<0,001), para ambos os grupos, e sem diferenças entre eles (p>0,05) nas manchas UV. CONCLUSÕES: Não houve diferença estatística na melhora do melasma nos dois grupos; o Grupo A apresentou menor incidência de eventos adversos. Logo, o complexo despigmentante emblica, licorice e belides é uma alternativa segura e eficaz na abordagem do melasma.

BACKGROUND: Melasma is a common skin pigment disorder with a difficult clinical response to treatment. OBJECTIVES: To evaluate the clinical efficacy and safety of the association of Belides, Emblica and Licorice 7 percent, compared to Hydroquinone 2 percent, in the treatment of melasma. METHODS: After 60 days of exclusive use of an SPF35 sunscreen, 56 women, 18 to 60 years of age, phototypes I to IV, with epidermal or mixed melasma, were divided into two different groups in a mono-blind clinical study: A) cream with Belides, Emblica and Licorice, applied twice a day; B) cream with Hydroquinone 2 percent, used at night. They were observed in a 60-day study; every 15 days, they were submitted to medical evaluation, self-evaluation, and photographic registration (Visia®). RESULTS: 50 volunteers (89 percent), 23 in Group A and 27 in Group B, concluded the study. Two volunteers in Group A and 7 in Group B had mild skin adverse events. Depigmentation was observed through medical evaluation (Group A: 78.3 percent; Group B: 88.9 percent) and volunteers' self-evaluation (Group A: 91.3 percent; Group B: 92.6 percent); these results were statistically significant (p<0.001), with no differences between groups (p>0.05). This pattern of results was observed by Visia® in the number (p = 0.001) and size and tone (p<0.001) of the uv stains, for both groups, with no differences between them (p>0.05). CONCLUSION: There were no statistic differences between groups in the improvement of melasma. Group A showed less skin adverse events. Therefore, the association of Emblica, Licorice and Belides is a safe and efficient alternative for the treatment of melasma.

Assays of physical stability and antioxidant activity of a topical formulation added with different plant extracts.

In the present investigation the changes on physical stability (pH, viscosity, flow index and tixotropy) of topical formulations were evaluated following inclusion of different plant extracts containing flavonoids. Also, the antioxidant effect of these plant extracts alone and after addition in the formulation was evaluated using chemiluminescence and the stable free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH(.-)) assays, as well as the inhibition of lipid peroxidation. Formulation added with dl-alpha-tocopherol was used to compare the physical stability and antioxidant activity. Formulations with plant extracts showed pseudoplastic behavior with decreasing on viscosity and tixotropy. The Glycyrrhiza glabra (GG) and Ginkgo biloba (GB) extracts alone and the formulations containing these extracts showed great antioxidant and free radical scavenging activities while the other extracts studied (mixture of Glycyrrhiza glabra, Symphytum officinale L and Arctium majus root, Nelumbium speciosum and soybean) showed lower activity. The results suggest that GG and GB extracts may be used in topical formulations in order to protect skin against damage caused by free radical and reactive oxygen species.

Identification of glycyrrhizin as a thrombin inhibitor.

Glycyrrhizin (GL), an anti-inflammatory compound isolated from Glycyrrhiza glabra, was identified as a new thrombin inhibitor: (a) It prolonged plasma recalcification and thrombin and fibrinogen clotting times, and (b) it inhibited thrombin-induced, but not collagen-, PAF- or convulxin-induced platelet aggregation. On the other hand, GL did not block thrombin's amidolytic activity upon S-2238. Furthermore, the fluorescence emission intensity of dansyl-thrombin was increased upon GL binding. Moreover, GL displaced hirudin as an inhibitor of thrombin-catalyzed hydrolysis of S-2238. Our data provide evidence that GL is a selective inhibitor of thrombin (the first one isolated from plants) that is able to exert its anti-thrombin action by interacting with the enzyme's anion binding exosite 1. A pharmacophoric search identified GL as a sialyl Lewis X (SLe[X]) mimetic compound able to inhibit selectin binding to SLe(X). However, SLe(X) did not affect thrombin clotting activities, which indicates a lack of its interaction with thrombin and distinguishes both molecules. It is suggested that the anti-inflammatory effect of GL may be due to its effective anti-thrombin action.