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Background: Scalp-related symptoms such as dandruff and itching are common with diverse underlying etiologies. We previously proposed a novel classification and scoring system for scalp conditions, called the scalp photographic index (SPI); it grades five scalp features using trichoscopic images with good reliability. However, it requires trained evaluators.Aim: To develop artificial intelligence (AI) algorithms for assessment of scalp conditions and to assess the feasibility of AI-based recommendations on personalized scalp cosmetics.Methods: Using EfficientNet, convolutional neural network (CNN) models (SPI-AI) ofeach scalp feature were established. 101,027 magnified scalp images graded according to the SPI scoring were used for training, validation, and testing the model Adults with scalp discomfort were prescribed shampoos and scalp serums personalized according to their SPI-AI-defined scalp types. Using the SPI, the scalp conditions were evaluated at baseline and at weeks 4, 8, and 12 of treatment.Results: The accuracies of the SPI-AI for dryness, oiliness, erythema, folliculitis, and dandruff were 91.3%, 90.5%, 89.6%, 87.3%, and 95.2%, respectively. Overall, 100 individuals completed the 4-week study; 43 of these participated in an extension study until week 12. The total SPI score decreased from 32.70 ± 7.40 at baseline to 15.97 ± 4.68 at week 4 (p < 0.001). The efficacy was maintained throughout 12 weeks.Conclusions: SPI-AI accurately assessed the scalp condition. AI-based prescription of tailored scalp cosmetics could significantly improve scalp health.
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Cosméticos , Caspa , Adulto , Humanos , Inteligencia Artificial , Cuero Cabelludo , Reproducibilidad de los Resultados , Cosméticos/uso terapéutico , PrescripcionesRESUMEN
The protein extract of Ulva australis hydrolyzed with Alcalase and Flavourzyme was found to have multi-functional properties, including total antioxidant capacity (TAC), collagenase inhibitory, and antibacterial activities. The #5 fraction (SP5) and #7 fraction (SP7) of U. australis hydrolysate from cation-exchange chromatography displayed significantly high TAC, collagenase inhibitory, and antibacterial effects against Propionibacterium acnes, and only the Q3 fraction from anion-exchange chromatography displayed high multi-functional activities. Eight of 42 peptides identified by MALDI-TOF/MS and Q-TOF/MS/MS were selected from the results for screening with molecular docking on target proteins and were then synthesized. Thr-Gly-Thr-Trp (TGTW) displayed ABTS [2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid)] radical scavenging activity. The effect of TAC as Trolox equivalence was dependent on the concentration of TGTW. Asn-Arg-Asp-Tyr (NRDY) and Arg-Asp-Arg-Phe (RDRF) exhibited collagenase inhibitory activity, which increased according to the increase in concentration, and their IC50 values were 0.95 mM and 0.84 mM, respectively. Peptides RDRF and His-Ala-Val-Tyr (HAVY) displayed anti-P. Acnes effects, with IC50 values of 8.57 mM and 13.23 mM, respectively. These results suggest that the U. australis hydrolysate could be a resource for the application of effective nutraceuticals and cosmetics.
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Background and Objectives: Among the cognitively impaired, arts engagement is associated with improved neurocognitive symptoms. Less is known about arts engagement as a potentially modifiable lifestyle factor to prevent or slow cognitive decline. Our aim was to evaluate the association between arts event attendance and cognition. Research Design and Methods: We used data from the 2014 and 2016 waves of the Health and Retirement Study to evaluate the association between arts event attendance and cognition using multivariable linear regressions. Arts event attendance in 2014 was our exposure of interest and included visiting an art museum or art gallery; attending an arts or crafts fair; attending a live performance (concert, play, or reading); and/or going to a movie theater. Cognitive function in 2016 measured on a 27-point scale by the Telephone Interview for Cognitive Status was our main outcome of interest. Results: Of the 1,149 participants included in the final analysis, 70.7% attended an arts event. The mean baseline cognitive score was higher among those who attended art events (16.8 [standard deviation {SD}, ±3.8] vs 13.8 [SD, ±5.0]; p < .001). In our multivariable regressions, those who attended arts events in 2014 exhibited higher cognitive scores in 2016 after controlling for demographic, socioeconomic, health, and baseline cognitive covariates (ß, 1.07 [95% confidence interval {CI}, 0.50-1.64]; p < .001). This association was primarily observed in those with lower baseline cognitive function (ß, 1.19 [95% CI, 0.33-2.06]; p = .008). Discussion and Implications: Arts event attendance may be associated with better cognitive function. Given concerns for residual confounding and reverse causality, this association warrants further study.
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Enterovirus A71 (EV71), coxsackievirus A16 (CVA16), and coxsackievirus B3 (CVB3) are pathogenic members of the Picornaviridae family that cause a range of diseases, including severe central nervous system complications, myocarditis, and pancreatitis. Despite the considerable public health impact of these viruses, no approved antiviral treatments are currently available. In the present study, we confirmed the potential of saucerneol, a compound derived from Saururus chinensis, as an antiviral agent against EV71, CVA16, and CVB3. In the in vivo model, saucerneol effectively suppressed CVB3 replication in the pancreas and alleviated virus-induced pancreatitis. The antiviral activity of saucerneol is associated with increased mitochondrial ROS (mROS) production. In vitro inhibition of mROS generation diminishes the antiviral efficacy of saucerneol. Moreover, saucerneol treatment enhanced the phosphorylation of STING, TBK-1, and IRF3 in EV71- and CVA16-infected cells, indicating that its antiviral effects were mediated through the STING/TBK-1/IRF3 antiviral pathway, which was activated by increased mROS production. Saucerneol is a promising natural antiviral agent against EV71, CVA16, and CVB3 and has potential against virus-induced pancreatitis and myocarditis. Further studies are required to assess its safety and efficacy, which is essential for the development of effective antiviral strategies against these viruses.
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Enterovirus Humano A , Infecciones por Enterovirus , Enterovirus , Miocarditis , Pancreatitis , Saururaceae , Humanos , Especies Reactivas de Oxígeno/metabolismo , Miocarditis/tratamiento farmacológico , Infecciones por Enterovirus/tratamiento farmacológico , Antígenos Virales/metabolismo , Antivirales/farmacología , Pancreatitis/tratamiento farmacológico , Saururaceae/metabolismo , Factor 3 Regulador del Interferón/metabolismoRESUMEN
Five-aminolevulinic acid (5-ALA)-photodynamic therapy combined with infrared radiation is an effective and safe therapy for facial acne. Although there are various available agents for treating acne, therapies for resistant or severe strains have been limited. The aim of this study was to investigate the inhibitory efficacy of ALACELL synthesized by combining 5-ALA with Y-G-G-F-L peptide against Staphylococcus aureus, Bacillus cereus, Escherichia coli, and Yersinia enterocolitica, as well as Cutibacterium acnes. Furthermore, other effects of ALACELL on human skin cells, melanin formation, intracellular tyrosinase activity, and Ultra Violet B (UVB)-irradiated cell death were measured by treatment of ALACELL in vitro. ALACELL particularly showed a growth inhibitory effect on C. acnes and no inhibitory effect on the four bacteria strains. ALACELL reduced melanin formation and intracellular tyrosinase activity by α-melanin cell-stimulating hormone (α-MSH) in B16F10 cells, with no cytotoxicity. ALACELL also improved cell viability in UVB-irradiated HaCaT cells. The results of the experiment show that ALACELL exhibits more efficacy than 5-ALA against antimicrobial activity, melanin formation, intracellular tyrosinase activity, and UVB-irradiated cell death. Therefore, ALACELL is recommended as a candidate for clinical application in the treatment of acne and skin aging and will be further investigated to study the mode of action and in actual situations.
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Rayos Ultravioleta , Ácido Aminolevulínico , Humanos , Melaninas , Monofenol MonooxigenasaRESUMEN
Coxsackievirus B3 (CVB3) is an important human pathogen associated with the development of acute pancreatitis, myocarditis, and type 1 diabetes. Currently, no vaccines or antiviral therapeutics are approved for the prevention and treatment of CVB3 infection. We found that Saururus chinensis Baill extract showed critical antiviral activity against CVB3 infection in vitro. Further, manassantin B inhibited replication of CVB3 and suppressed CVB3 VP1 protein expression in vitro. Additionally, oral administration of manassantin B in mice attenuated CVB3 infection-associated symptoms by reducing systemic production of inflammatory cytokines and chemokines including TNF-α, IL-6, IFN-γ, CCL2, and CXCL-1. We found that the antiviral activity of manassantin B is associated with increased levels of mitochondrial ROS (mROS). Inhibition of mROS generation attenuated the antiviral activity of manassantin B in vitro. Interestingly, we found that manassantin B also induced cytosolic release of mitochondrial DNA based on cytochrome C oxidase DNA levels. We further confirmed that STING and IRF-3 expression and STING and TBK-1 phosphorylation were increased by manassantin B treatment in CVB3-infected cells. Collectively, these results suggest that manassantin B exerts antiviral activity against CVB3 through activation of the STING/TKB-1/IRF3 antiviral pathway and increased production of mROS.
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Antivirales/farmacología , Infecciones por Coxsackievirus/metabolismo , Infecciones por Coxsackievirus/virología , Enterovirus Humano B/efectos de los fármacos , Furanos/farmacología , Factor 3 Regulador del Interferón/metabolismo , Proteínas de la Membrana/metabolismo , Proteínas Serina-Treonina Quinasas/metabolismo , Animales , Chlorocebus aethiops , Infecciones por Coxsackievirus/tratamiento farmacológico , Citocinas/metabolismo , Proteínas del Complejo de Cadena de Transporte de Electrón/antagonistas & inhibidores , Femenino , Humanos , Mediadores de Inflamación/metabolismo , Ratones , Mitocondrias/metabolismo , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Células Vero , Replicación Viral/efectos de los fármacosRESUMEN
In this study, skin cream containing ziyuglycoside I isolated from Sanguisorba officinalis was manufactured and examined the protective effects of the skin cream against UVB-induced hairless mice. UVB-induced hairless mice were topically treated with the skin cream once a day for 5 weeks. Application of the skin cream did not exhibit side effect on body growth showing normal body weight and food efficiency in the mice. The skin cream treatment also was inhibited mRNA expression of interleukin (IL)-1ß, matrix metalloproteinase (MMP)-2, MMP-9, and MMP-2 protein expression in the mice. Furthermore, the skin cream treatment inhibits epidermal wrinkle formation, wrinkle depth, wrinkle thickness, and collagen degradation in UVB-induced hairless mice. Therefore, the skin cream was able to play a role in the attenuation of photoaging caused by UVB irradiation via downregulation of mRNA expression of inflammatory cytokine IL-1ß, MMP-2, MMP-9, and suppression of MMP-2 proteins expression.
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Sanguisorba/química , Saponinas/farmacología , Envejecimiento de la Piel/efectos de los fármacos , Envejecimiento de la Piel/efectos de la radiación , Crema para la Piel/farmacología , Rayos Ultravioleta , Animales , Peso Corporal/efectos de los fármacos , Ensayo de Inmunoadsorción Enzimática , Femenino , Interleucina-1beta/genética , Metaloproteinasa 2 de la Matriz/genética , Metaloproteinasa 9 de la Matriz/genética , Ratones , Ratones Pelados , ARN Mensajero/antagonistas & inhibidores , ARN Mensajero/metabolismo , Reacción en Cadena en Tiempo Real de la Polimerasa , Reacción en Cadena de la Polimerasa de Transcriptasa InversaRESUMEN
OBJECTIVES: This study was conducted to determine whether essential oils had anti-influenza A/WS/33 virus activity and whether there were specific compounds associated with this activity. METHODS: There were 63 essential oils evaluated for anti-influenza (A/WS/33 virus) activity using a cytopathic effect reduction method. The chemical composition of the anti-influenza essential oils was phytochemically analyzed by gas chromatography-mass spectrometry. RESULTS: The antiviral assays demonstrated that 11 of the 62 essential oils (100 µg/mL) possessed anti-influenza activity, reducing visible cytopathic effects of influenza A/WS/33 virus activity by > 30%. Furthermore, marjoram, clary sage and anise oils exhibited anti-influenza A/WS/33 virus activity of > 52.8%. However, oseltamivir (the anti-influenza A and B drug), showed cytotoxicity at the same concentration (100 µg/mL) as the essential oils. The chemical composition detected by GC-MS analysis, differed amongst the 3 most potent anti-viral essential oils (marjoram, clary sage and anise oils) except for linalool, which was detected in all 3 essential oils. CONCLUSION: This study demonstrated anti-influenza activity in 11 essential oils tested, with marjoram, clary sage and anise essential oils being the most effective at reducing visible cytopathic effects of the A/WS/33 virus. All 3 oils contained linalool, suggesting that this may have anti-influenza activity. Further investigation is needed to characterize the antiviral activity of linalool against influenza A/WS/33 virus.
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This study aimed to investigate in vitro the anti-influenza B/Lee/40 virus effect of sakuranetin and mode of its action. The sakuranetin exhibited potent antiviral activity against influenza B/Lee/40 virus, reducing the formation of a visible cytopathic effect, with a 50% inhibitory concentration (IC50 ) of 7.21 µg/ml and no cytotoxicity at a concentration of 100 µg/ml, and the derived therapeutic index (TI) was >13.87. Oseltamivir showed weak anti-influenza B/Lee/40 virus activity with IC50 of 80.74 µg/ml, 50% cytotoxicity concentration of >100 µg/ml, and TI of >1.24. Sakuranetin also showed effective inhibitory effects when added at the viral attachment, entry, and postentry steps. Moreover, sakuranetin effectively inactivated influenza B/Lee/40 virus infection in dose- and temperature-dependent manners. Sakuranetin indicated an inhibitory effect in viral RNA synthesis in the presence of 100 µg/ml of sakuranetin. Overall, this research revealed that sakuranetin could inhibit influenza B/Lee/40 virus replication and that sakuranetin may be involved in the virus attachment, entry, and postentry. Therefore, sakuranetin is a good candidate for a chemopreventive agent for influenza virus-related diseases.
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Flavonoides/farmacología , Virus de la Influenza B/efectos de los fármacos , Replicación Viral/efectos de los fármacos , Animales , Antivirales/farmacología , Perros , Virus de la Influenza B/fisiología , Concentración 50 Inhibidora , Células de Riñón Canino Madin Darby , Infecciones por Orthomyxoviridae/tratamiento farmacológico , Infecciones por Orthomyxoviridae/virología , Transducción de Señal/efectos de los fármacosRESUMEN
Herbal dietary supplements have attracted more and more attention owing to their relative effectiveness in obesity -related metabolic disorders and diseases. This study investigated the therapeutic effects and underlying mechanisms of Capsosiphon fulvescens (CF) extracts on obesity, their associated metabolic disorders and hepatic steatosis in high-fat diet (HFD)-induced obese mice. Male C57BL/6 mice were fed with normal, HFD/Vehicle and HFD/CF (orally 300 mg/kg/day for CF). After 12 weeks, CF blocked HFD-induced body weight, food intake, liver weight, hepatic triglyceride (TG), fat mass (weight of abdominal subcutaneous fat and epididymal adipose tissue) and biochemical parameters (total cohlesterol, glucose, TG, creatinine, high-density lipoproteins cholesterol and low-density lipoprotein cholesterol) of serum. CF also had improved serum levels of adiponectin, leptin and insulin-like growth factor-1 in HFD/CF mice. Moreover, CF ameliorated the hepatic steatosis-reducing size of white adipose tissue. These results indicate that CF have anti-obesity effects and are effective for reducing metabolic risk and hepatic steatosis.
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Chlorophyta/química , Dieta Alta en Grasa/efectos adversos , Hígado Graso/tratamiento farmacológico , Enfermedades Metabólicas/tratamiento farmacológico , Enfermedades Metabólicas/etiología , Obesidad/etiología , Fitoterapia , Extractos Vegetales/administración & dosificación , Adiponectina/sangre , Animales , Glucemia/metabolismo , Hígado Graso/sangre , Hígado Graso/etiología , Factor I del Crecimiento Similar a la Insulina/metabolismo , Leptina/sangre , Metabolismo de los Lípidos , Masculino , Enfermedades Metabólicas/metabolismo , Ratones Endogámicos C57BL , Obesidad/metabolismo , Extractos Vegetales/farmacologíaRESUMEN
OBJECTIVES: Echovirus 30 is a major cause of meningitis in children and adults. The aim of this study was to investigate whether the antifungal drug itraconazole could exhibit antiviral activity against echovirus 30. METHODS: The cytopathic effect and viral RNA levels were assessed in RD cells as indicators of viral replication. The effects of itraconazole were compared to those of two known antiviral drugs, rupintrivir and pleconaril. The time course and time-of-addition assays were used to approximate the time at which itraconazole exerts its activity in the viral cycle. RESULTS: Itraconazole and rupintrivir demonstrated the greatest potency against echovirus 30, demonstrating concentration-dependent activity, whereas pleconaril showed no antiviral activity. Itraconazole did not directly inactivate echovirus 30 particles or impede viral uptake into RD cells, but did affect the initial stages of echovirus 30 infection through interference with viral replication. CONCLUSION: Itraconazole can be considered a lead candidate for the development of antiviral drugs against echovirus 30 that may be used during the early stages of echovirus 30 replication.
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OBJECTIVES: Rhinoviruses (RVs) cause common cold and are associated with exacerbation of chronic inflammatory respiratory diseases. Until now, no clinically effective antiviral chemotherapeutic agents to treat diseases caused by human rhinoviruses (HRVs) have been reported. We assessed the anti-HRV3 activity of sakuranetin isolated from Sorbus commixta Hedl. in human epithelioid carcinoma cervix (HeLa) cells, to evaluate its anti-rhinoviral potential in the clinical setting. METHODS: Antiviral activity and cytotoxicity as well as the effect of sakuranetin on HRV3-induced cytopathic effects (CPEs) were evaluated using the sulforhodamine B (SRB) method using CPE reduction. The morphology of HRV3-infected cells was studied using a light microscope. RESULTS: Sakuranetin actively inhibited HRV3 replication and exhibited antiviral activity of more than 67% without cytotoxicity in HeLa cells, at 100 µg/mL. Ribavirin showed anti-HRV3 activity similar to that of sakuranetin. Treatment of HRV-infected HeLa cells with sakuranetin visibly reduced CPEs. CONCLUSION: The inhibition of HRV production by sakuranetin is mainly due to its general antioxidant activity through inhibition of viral adsorption. Therefore, the antiviral activity of sakuranetin should be further investigated to elucidate its mode of action and prevent HRV3-mediated diseases in pathological conditions.
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Severe complications associated with EV71 infections are a common cause of neonatal death. Lack of effective therapeutic agents for these infections underlines the importance of research for the development of new antiviral compounds. In the present study, the anti-EV71 activity of norwogonin, oroxylin A, and mosloflavone from Scutellaria baicalensis Georgi was evaluated using a cytopathic effect (CPE) reduction method, which demonstrated that all three compounds possessed strong anti-EV71 activity and decreased the formation of visible CPEs. Norwogonin, oroxylin A, and mosloflavone also inhibited virus replication during the initial stage of virus infection, and they inhibited viral VP2 protein expression, thereby inhibiting viral capsid protein synthesis. However, ribavirin has a relatively weaker efficacy compared to the other drugs. Therefore, these findings provide important information that will aid in the utilization of norwogonin, oroxylin A, and mosloflavone for EV71 treatment.
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The active constituents of Korean Papaver rhoeas bee pollen conferring neuraminidase inhibitory activities (H1N1, H3N2, and H5N1) were investigated. Six flavonoids and one alkaloid were isolated and characterized by nuclear magnetic resonance and mass spectrometry data. These included kaempferol-3-sophoroside (1), kaempferol-3-neohesperidoside (2), kaempferol-3-sambubioside (3), kaempferol-3-glucoside (4), quercetin-3-sophoroside (5), luteolin (6), and chelianthifoline (7). All compounds showed neuraminidase inhibitory activities with IC50 values ranging from 10.7 to 151.1 µM. The most potent neuraminidase inhibitor was luteolin, which was the dominant content in the ethyl acetate fraction. All tested compounds displayed noncompetitive inhibition of H3N2 neuraminidase. Furthermore, compounds 1-7 all reduced the severity of virally induced cytopathic effects as determined by the Madin-Darby canine kidney cell-based assay showing antiviral activity with IC50 values ranging from 10.7 to 33.4 µM (zanamivir: 58.3 µM). The active compounds were quantified by high-performance liquid chromatography, and the total amount of compounds 1-7 made up about 0.592 g/100 g bee pollen, contributing a rich resource of a natural antiviral product.
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Antivirales/química , Antivirales/farmacología , Inhibidores Enzimáticos/farmacología , Neuraminidasa/antagonistas & inhibidores , Papaver/química , Polen/química , Animales , Abejas , Perros , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Inhibidores Enzimáticos/química , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Subtipo H1N1 del Virus de la Influenza A/efectos de los fármacos , Subtipo H3N2 del Virus de la Influenza A/efectos de los fármacos , Subtipo H5N1 del Virus de la Influenza A/efectos de los fármacos , Células de Riñón Canino Madin Darby/efectos de los fármacos , Células de Riñón Canino Madin Darby/virología , Espectroscopía de Resonancia Magnética , Estructura MolecularRESUMEN
Human rhinoviruses and enteroviruses (family Picornaviridae) infect millions of people worldwide each year, but little is known about effective therapeutical treatment for the infection caused by these viruses. We sought to determine whether or not Zanthoxylum (Rutaceae) species can exhibit antiviral activity against picornaviruses. The leaf parts of four Zanthoxylum species were extracted with methanol, and the extracts were investigated for their antiviral activity against picornaviruses using cytopathic effects by cytopathic effect reduction. Leaf extracts of Zanthoxylum piperitum among four Zanthoxylum species were found to possess only broad-spectrum antipicornavirus activity against human rhninovirus 2 with a 50% inhibitory concentration (IC50) value of 59.48 µg/mL, human rhinovirus 3 with an IC50 value of 39.94 µg/mL, coxsackie A16 virus with an IC50 value of 45.80 µg/mL, coxsackie B3 virus with an IC50 value of 68.53 µg/mL, coxsackie B4 virus with an IC50 value of 93.58 µg/mL, and enterovirus 71 virus with an IC50 value of 4.48 µg/mL. However, ribavirin did not possess antiviral activity against human rhinovirus 3 and four enteroviruses. Therefore, leaves of Z. piperitum showed broad-spectrum antipicornavirus activity, and may be useful as a candidate for studying picornavirus agents and development of pharmaceuticals.
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Five polyphenols were isolated from the ethanolic extract of the fruiting bodies of Phellinus baumii. These compounds were identified by various spectroscopic methods as hispidin, hypholomine B, inoscavin A, davallialactone, and phelligridin D. All compounds inhibited noncompetitively H1N1, H5N1, and H3N2 neuraminidase activity and reduced the amount of virally-induced cytopathic effect (CPE) according to an MDCK cell-based assay.
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Agaricales/química , Antivirales/farmacología , Basidiomycota/química , Orthomyxoviridae/efectos de los fármacos , Polifenoles/farmacología , Animales , Antivirales/aislamiento & purificación , Efecto Citopatogénico Viral/efectos de los fármacos , Perros , Relación Dosis-Respuesta a Droga , Cuerpos Fructíferos de los Hongos/química , Subtipo H1N1 del Virus de la Influenza A/efectos de los fármacos , Subtipo H1N1 del Virus de la Influenza A/enzimología , Subtipo H3N2 del Virus de la Influenza A/efectos de los fármacos , Subtipo H3N2 del Virus de la Influenza A/enzimología , Subtipo H5N1 del Virus de la Influenza A/efectos de los fármacos , Subtipo H5N1 del Virus de la Influenza A/enzimología , Cinética , Células de Riñón Canino Madin Darby , Medicina Tradicional de Asia Oriental , Neuraminidasa/antagonistas & inhibidores , Orthomyxoviridae/enzimología , Polifenoles/química , Polifenoles/aislamiento & purificaciónRESUMEN
Porcine epidemic diarrhea virus (PEDV) is the predominant cause of severe entero-pathogenic diarrhea in swine. Until now there is no recorded clinically effective antiviral chemotherapeutic agent for treatment of diseases caused by PEDV. This study aimed to investigate in vitro anti-PEDV effect of polysaccharide from Ginkgo biloba exocarp and mode of its action. The polysaccharide exhibited potent antiviral activity against PEDV reducing the formation of a visible CPE [a 50% inhibitory concentration (IC50)=1.7±1.3µg/mL], compared to positive control, ribavirin and it did not show cytotoxicity at 100µg/mL [a 50% cytotoxicity concentration (CC50)=100µg/mL]. Polysaccharide also showed effective inhibitory effects when added at the viral attachment and entry steps. Moreover, polysaccharide effectively inactivated PEDV infection in time-, dose- and temperature-dependent manners. Overall, this research revealed that polysaccharide could inhibit PEDV infection, and that polysaccharide may be involved in PEDV-Vero cell interactions, as the virus attachment and entry to the Vero cells was hindered by the polysaccharide. Therefore, polysaccharide possessing effective inhibitory effect on viral attachment and entry steps of PEDV life cycle is a good candidate for development of antivirals.
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Antivirales/farmacología , Ginkgo biloba/química , Polisacáridos/farmacología , Virus de la Diarrea Epidémica Porcina/efectos de los fármacos , Animales , Antivirales/aislamiento & purificación , Chlorocebus aethiops , Efecto Citopatogénico Viral/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Concentración 50 Inhibidora , Polisacáridos/aislamiento & purificación , Porcinos , Temperatura , Células VeroRESUMEN
Coccidiosis affects many vertebrates worldwide, but treatment with known anti-coccidial drugs causes several adverse side effects. There is a critical need for the development and evaluation of new drugs. The anti-coccidial effect of 1-[4-(4-nitrophenoxy)phenyl]propane-1-one (NPPP), a synthetic compound, was studied in vitro and in vivo. Treatment with NPPP showed anti-Toxoplasma activity in vitro with a lower EC50 value than pyrimethamine. In ICR mice infected with Toxoplasma gondii, oral administration of NPPP for 4 days showed statistically significant anti-Toxoplasma activity with lower numbers of tachyzoite than those of the negative control (p < 0.01). NPPP also exhibited strong anti-Eimeria activity in Eimeria tenella-infected chickens when treated for 4 days with orally administered NPPP at a dose of 100 mg/kg. Potential target proteins of NPPP were analyzed by proteomic profiles of T. gondii tachyzoites. Two hypothetical proteins were identified as possible targets of NPPP, a putative ortholog of vacuolar ATP synthase subunit C and a class I S-adenosylmethionine-dependent methyltransferase. Our data show that the NPPP might be an anti-coccidial drug candidate for clinical application against coccidial infections. Future investigations will focus on identifying the function of proteins regulated by NPPP.
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Coccidiostáticos/administración & dosificación , Coccidiostáticos/química , Sistemas de Liberación de Medicamentos/métodos , Toxoplasma/efectos de los fármacos , Toxoplasmosis/tratamiento farmacológico , Animales , Pollos , Evaluación Preclínica de Medicamentos/métodos , Femenino , Células HeLa , Humanos , Ratones , Ratones Endogámicos ICR , Toxoplasmosis/patologíaRESUMEN
Three saikosaponins were isolated from the MeOH extract of the roots of Bupleurum falcatum L.: saikosaponins B3 (1); B4 (2); and D (3). Of the three, compound 3 inhibited the interaction of selectins (E, L, and P) and THP-1 cells with IC50 values of 1.8, 3.0 and 4.3 µM, respectively. Also, the aglycone structure 4 of compound 3 showed moderate inhibitory activity on L-selectin-mediated cell adhesion. From these results, we suspect that compound 3 isolated from Bupleurum falcatum roots would be a good candidate for therapeutic strategies to treat inflammation.
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Bupleurum/química , Adhesión Celular/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Saponinas/farmacología , Selectinas/farmacología , Moléculas de Adhesión Celular/genética , Moléculas de Adhesión Celular/metabolismo , Línea Celular , Supervivencia Celular/efectos de los fármacos , Células Endoteliales/efectos de los fármacos , Células Endoteliales/metabolismo , Expresión Génica , Humanos , Inmunofenotipificación , Estructura Molecular , Monocitos/efectos de los fármacos , Monocitos/metabolismo , Ácido Oleanólico/química , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Raíces de Plantas/química , Saponinas/química , Saponinas/aislamiento & purificación , Factor de Necrosis Tumoral alfaRESUMEN
BACKGROUND: Ginsenosides are the major components responsible for the biochemical and pharmacological actions of ginseng, and have been shown to have various biological activities. In this study, we investigated the antiviral activities of seven ginsenosides [protopanaxatriol (PT) type: Re, Rf, and Rg2; protopanaxadiol (PD) type: Rb1, Rb2, Rc, and Rd)] against coxsackievirus B3 (CVB3), enterovirus 71 (EV71), and human rhinovirus 3 (HRV3). METHODS: Assays of antiviral activity and cytotoxicity were evaluated by the sulforhodamine B method using the cytopathic effect (CPE) reduction assay. RESULTS: The antiviral assays demonstrated that, of the seven ginsenosides, the PT-type ginsenosides (Re, Rf, and Rg2) possess significant antiviral activities against CVB3 and HRV3 at a concentration of 100 µg/mL. Among the PT-type ginsenosides, only ginsenoside Rg2 showed significant anti-EV71 activity with no cytotoxicity to cells at 100 µg/mL. The PD-type ginsenosides (Rb1, Rb2, Rc, and Rd), by contrast, did not show any significant antiviral activity against CVB3, EV71, and HRV3, and exhibited cytotoxic effects to virus-infected cells. Notably, the antiviral efficacies of PT-type ginsenosides were comparable to those of ribavirin, a commonly used antiviral drug. CONCLUSION: Collectively, our findings suggest that the ginsenosides Re, Rf, and Rg2 have the potential to be effective in the treatment of CVB3, EV71, and HRV3 infection.