The protective effect and mechanism of tea polyphenols on oral cancer in mice / 中国医师杂志

Objective:To explore the protective mechanism of tea polyphenols (TP) on mouse oral cancer.Methods:A total of 50 mice were divided into control group, model group, TP group, Selisistat group, TP+ Selisistat group, with 10 mice in each group. The control group was gavaged with physiological saline, while the model group, TP group, Selisistat group, and TP+ Selisistat group were gavaged with 300 mg/L 4-NQO to establish a mouse oral cancer model. Physiological saline, 200 mg/kg TP, 0.01 mg/kg Selisistat, and 200 mg/kg TP+ 0.01 mg/kg Selisistat were gavaged respectively. The weight changes of each group of mice were compared; HE staining was used to observe the morphology of mouse oral tumor tissue; Enzyme linked immunosorbent assay was used to detect the levels of malondialdehyde (MDA) and superoxide dismutase (SOD) in serum; Immunoblotting and immunohistochemistry were used to detect the expression of silencing information regulatory factor (Sirt1) and nuclear factor E2 related factor 2 (Nrf2) proteins in mouse oral tissues.Results:Compared with the control group, the model group mice had a decrease in body weight [(23.19±1.36)g], a decrease in serum SOD level [(91.64±8.75)U/ml], an increase in MDA level [(5.18±0.46)nmol/ml], a decrease in Sirt1 (0.38±0.05) and Nrf2 (0.36±0.05) protein expression in oral tissue, and an increase in Nrf2 acetylation level (0.84±0.11) (all P<0.05). Compared with the model group, the TP group mice had an increase in body weight [(25.28±1.25)g], elevated serum SOD levels [(121.24±10.68)U/ml], decreased MDA levels [(3.89±0.42)nmol/ml], increased expression of Sirt1 (0.61±0.09) and Nrf2 (0.58±0.06) proteins in oral tissue, and decreased Nrf2 protein acetylation levels (0.39±0.05); The Selisistat group mice showed a decrease in body weight [(21.41±1.07)g], a decrease in serum SOD levels [(72.16±7.43)U/ml], an increase in MDA levels [(5.87±0.41)nmol/ml], a decrease in Sirt1 (0.23±0.04) and Nrf2 protein (0.24±0.03) expression in oral tissue, and an increase in Nrf2 acetylation levels (1.12±0.14) ( P<0.05). The body weight [(23.32±1.27)g], serum SOD levels [(92.58±8.13)U/ml], and oral Sirt1 (0.41±0.06) and Nrf2 (0.38±0.05) protein expression in the TP+ Selisistat group mice were higher than those in the Selisistat group, while MDA [(5.11±0.38)nmol/ml] and Nrf2 acetylation levels (0.82±0.09) were lower than those in the Selisistat group (all P<0.05). Conclusions:Tea polyphenols can alleviate oral tissue damage and alleviate oxidative stress in mice with oral cancer, and their mechanism may be related to the upregulation of the Sirt1/Nrf2 pathway.

Polyphenol analysis in human milk by a rapid, cost-effective, and accurate micromethod: translational development / Análise de polifenóis no leite humano por meio de um micrométodo rápido, econômico e preciso: desenvolvimento translacional

ABSTRACT Objective: To develop a rapid method for analysing polyphenols, which are potentially active antioxidants against neonatal oxidative stress, from small human milk (HM) volumes. Methods: Acid and alkaline extractions were compared using two dyes: Folin-Ciocalteu and Fast Blue BB. Linearity, sensitivity, recovery percentage, polyphenol content, precision, and stability were assessed in 14 HM samples and compared using the Kruskal-Wallis H test (p<0.05). The best technique was applied to 284 HM samples to determine their polyphenolic content and its association with maternal diet by multifactorial linear regression. Results: Acidic extraction successfully recovered the gallic acid reference standard, whereas alkaline extraction overestimated it. Calibration curves for all methods were linear (R2>0.96) up to 500 mg/L. All bicarbonate-based Folin-Ciocalteu methods assayed were stable and repeatable, whereas Fast Blue BB-based variants were not. HM polyphenols (mean=94.68 mg/L) positively correlated to the dietary intake of hydroxycinnamic acids, the most consumed polyphenolic family in this population. Conclusions: A bicarbonate-based Folin-Ciocalteu micromethod allowed the accurate determination of polyphenols in HM, which might be useful for translational research settings and HM banks.

RESUMO Objetivo: Desenvolver um método rápido para analisar polifenóis, que são antioxidantes potencialmente ativos contra o estresse oxidativo neonatal, em pequenos volumes de leite humano (LH). Métodos: Foram comparadas extrações ácidas e alcalinas usando dois corantes: Folin-Ciocalteu e Fast Blue BB. Foram avaliadas variáveis como linearidade, sensibilidade, percentagem de recuperação, teor de polifenóis, precisão e estabilidade em 14 amostras de LH, comparadas usando o teste de Kruskal-Wallis H (p<0,05). A melhor técnica foi aplicada a 284 amostras de LH para determinar seu teor polifenólico e sua associação com a dieta materna por regressão linear multifatorial. Resultados: A extração ácida recuperou com sucesso o padrão de referência do ácido gálico, enquanto a extração alcalina o superestimou. As curvas de calibração para todos os métodos foram lineares (R2>0,96) até os 500 mg/L. Todos os métodos testados baseados em Folin-Ciocalteu com bicarbonato foram estáveis e repetíveis, enquanto as variantes baseadas em Fast Blue BB não. Os polifenóis do HM (média=94,68 mg/L) correlacionaram-se positivamente com a ingestão dietética de ácidos hidroxicinâmicos, a família de polifenóis mais consumida nesta população. Conclusões: Um micrométodo baseado em bicarbonato de Folin-Ciocalteu permitiu a determinação precisa de polifenóis no HM, o que pode ser útil para configurações de pesquisa translacional e bancos de HM.

Can the combination of proanthocyanidin and vitamin E or palm oil effectively protect enamel against in vitro erosive and abrasive challenges?

Abstract Objectives This study aimed to assess the effect of proanthocyanidin, palm oil and vitamin E against erosive and erosive+abrasive challenges in vitro after enamel pellicle formation in situ. Methodology Bovine enamel blocks (n=84) were obtained and divided into the following treatment groups: negative control (NC) - deionized water; positive control (PC) - SnCl2/NaF/AmF-containing solution; palm oil (PO); 2% proanthocyanidin (P2); vitamin E (VitE); 2% proanthocyanidin+palm oil (P2PO); and 2% proanthocyanidin+vitamin E (P2VitE). For 5 days, one half of the sample from each group was subjected to erosion and the other half was subjected to erosion+abrasion. The acquired enamel pellicle (AEP) was pre-formed in situ for 30 minutes. The specimens were then treated in vitro with solutions (500 µl, 30s for each group). Subsequently, the blocks were left in the oral cavity for another hour to obtain the modified AEP. The blocks were immersed in 0.5% citric acid (pH=2.5) for 90s, 4×/day. AEP formation and treatment were carried out before the first and third erosive challenges, and after these challenges, abrasive cycles (15s) were performed on half of the samples. Enamel wear was quantified by profilometry and data were analyzed by two-way ANOVA and Tukey's test (p<0.05). Results All groups showed higher wear when exposed to erosion+abrasion than when exposed to erosion alone (p=0.0001). PO, P2VitE, P2, and P2PO showed enamel wear similar to the PC group, but only PC, PO and P2VitE differed from the NC group. The other groups behaved similarly to NC. Conclusion It was concluded that the combination of proanthocyanidin and vitamin E was effective in reducing wear in the face of in vitro erosive and erosive+abrasive challenges.

Modeling Mediated Crossover Acute and Subacute Damage to the Pulmonary System During Systemic (Subcutaneous) Administration of Bleomycin in Mice to Test the Potential Therapeutic Effect of Polyphenols / Modelado del Daño Agudo y Subagudo Cruzado Mediado al Sistema Pulmonar Durante la Infección Sistémica (Subcutánea) de Administración de Bleomicina a Ratones para Probar el Posible Efecto Terapéutico de los Polifenoles

SUMMARY: The potential anti-inflammatory and antifibrotic activity of polyphenolic extracts of blueberry and grape was evaluated in a mouse model of lung damage induced by subcutaneous administration of bleomycin. The results of testing the polyphenolic extracts on two different systemic administration variants of bleomycin (intraperitoneal and subcutaneous) were compared. It was found that regardless of the method of bleomycin administration, indirect cross-acute and subacute damage to the pulmonary system was observed. Both patterns exhibited the same prevalence and severity. The administration of polyphenolic extracts of blueberry and grape to mice resulted in a significant decrease in theseverity of acute and subacute patterns of lung damage, suggesting their protective properties for the microcirculatory bed and a pronounced anti-inflammatory effect.

La potencial actividad antiinflamatoria y antifibrótica de los extractos polifenólicos de arándano y uva se evaluó en un modelo de daño pulmonar en ratón inducido por la administración subcutánea de bleomicina. Se compararon los resultados de las pruebas de los extractos polifenólicos en dos variantes diferentes de administración sistémica de bleomicina (intraperitoneal y subcutánea). Se encontró que, independientemente del método de administración de bleomicina, se observaba daño indirecto cruzado, agudo y subagudo al sistema pulmonar. Ambos patrones exhibieron la misma prevalencia y gravedad. La administración de extractos polifenólicos de arándano y uva a ratones dio como resultado una disminución significativa en la gravedad de los patrones agudos y subagudos de daño pulmonar, lo que sugiere sus propiedades protectoras del lecho micro- circulatorio y un efecto antiinflamatorio pronunciado.

Chemical composition and antioxidant capacity of purified extracts of Prosopis pallida (Humb. & Bonpl. ex Willd.) Kunth (Fabaceae) fruits from Northern Peru / Composición química y capacidad antioxidante de extractos purificados de frutos de Prosopis pallida (Humb. & Bonpl. Ex Willd.) Kunth (Fabaceae) del norte de Perú

The purpose of this work was to evaluate the antioxidant capacity of Prosopis pallida (Fabaceae) fruits "algarrobo", in addition to determine their main chemical components. Fruit purified extracts from the regions of Tumbes, Piura, Lambayeque, and La Libertad (Peru) were evaluated using infusion, decoction, and alcoholic extraction at concentrations of 45, 70 and 96%. To measure the antioxidant capacity of the extracts, the determination of total phenolics content was performed, followed by the antioxidant evaluation using DPPH, FRAP and ABTS. The chemical identification was carried out through UHPLC-UV-MS/MS. The results showed that the decoction of the sample from the region of La Libertad, as well as the ethanol extracts at 45% of the samples from Tumbes and Lambayeque presented greater antioxidant capacity. Moreover, ten major substances of these extracts were identified: nine phenolic derivatives (vicenin II as the main constituent of the extracts) and one diterpene (7-oxodehydroabietic acid).

El propósito de este trabajo fue evaluar la capacidad antioxidante de frutos de Prosopis pallida (Fabaceae) "algarrobo", además de determinar sus principales componentes químicos. Se estudiaron extractos purificados de frutos de las regiones de Tumbes, Piura, Lambayeque y La Libertad (Perú), mediante infusión, decocción y extracción alcohólica en concentraciones de 45, 70 y 96%. Para medir la capacidad antioxidante de los extractos, se realizó la determinación del contenido de fenoles totales, seguida de la evaluación antioxidante mediante DPPH, FRAP y ABTS. La identificación química se realizó mediante UHPLC-UV-MS/MS. Los resultados mostraron que la decocción de la muestra de la región de La Libertad, así como los extractos de etanol al 45% de las muestras de Tumbes y Lambayeque presentaron mayor capacidad antioxidante. Además, se identificaron diez sustancias principales de estos extractos: nueve derivados fenólicos (vicenin II como componente principal de los extractos) y un diterpeno (ácido 7-oxodehidroabiético).

Analysis of drying kinetic of brewer ́s spent grains: effect of the temperature on the physical properties and the content of bioactive compounds / Análisis de la cinética de secado del bagazo residual de malta: efecto de la temperatura sobre las propiedades físicas y el contenido de compuestos bioactivos

Background: Brewer ́s spent grain (BSG) is a biomass by-product generated in large volumes during industrial beer production. BSG has become a growing environmental problem, as most breweries discard it inappropriately, negatively impacting the environment. Alternatives for the exploitation of this by-product have consisted of elaborating food supplements for farm animals, obtaining biofuels, developing adsorbents, and obtaining substances for the food industry. However, the high moisture content in BSG (approximately 70%), poses a significant challenge in exploring various reuse alternatives. Therefore, the implementation of a pre-drying process becomes essential. Objective: This study aimed to analyze the BSG drying kinetics at different temperatures and the effect of the drying temperature on the physical properties and the content of bioactive compounds. Methods: BSG samples were dried at different temperatures (50, 60, 70, 80, 90, and 105°C) and analyzed for their moisture ratio, water activity, total polyphenol content (TPC), and DPPH (1,1-diphenyl-2-picrylhydrazil) radical scavenging activity. Also, four kinetics models were fitted to the drying data. Results:It was determined that the effective diffusivity was between 5.23x10

Antecedentes: El Bagazo residual de malta (BSG por sus siglas en inglés) es un subproducto biomásico generado en grandes volúmenes durante la producción industrial de cerveza. El BSG se ha convertido en un creciente problema para el medio ambiente, debido a que la mayoría de las cervecerías descartan inapropiadamente este residuo generando un impacto negativo al ambiente. Las alternativas para el aprovechamiento de este subproducto han consistido especialmente en la elaboración de suplementos alimenticios para animales de granja, obtención de biocombustibles, desarrollo de adsorbentes y obtención de productos para la industria alimentaria. Sin embargo, el alto contenido de humedad (~70%) del BSG representa un reto para el desarrollo de diferentes alternativas de reutilización, por lo que se hace necesario un proceso de secado previo. Objetivos: En este estudio se analizó la cinética de secado del BSG a diferentes temperaturas y el efecto de la temperatura de secado sobre sus propiedades físicas y contenido de compuestos bioactivos. Métodos: Las muestras de BSG fueron secadas a diferentes temperaturas (50, 60, 70, 80, 90 y 105°C) y analizadas en términos de razón de humedad, actividad acuosa, contenido de polifenoles totales (TPC) y actividad secuestradora del radical DPPH. Además, se ajustaron 4 modelos cinéticos a los datos de secado. Resultados: Se determinó que la difusividad efectiva del BSG varió entre 5.23x10

Phytochemical Investigation and in Vitro Antioxidant Activity of Panchavalkala Bark Extracts

Natural antioxidants have an important role in the prevention of many age-related diseases and promotion of health. Among natural antioxidants from plants, flavonoids and other phenolic compounds are potent antioxidants and chelating agents. Panchavalkala the barks of five trees i.e. Nyagrodha (Ficus benghalensis L.), Udumbara (Ficus racemosa L.), Ashwatha (Ficus religiosa L.), Plaksha (Ficus virens Aiton) and Parisha (Thespesia populnea (L.)Sol.ex Correa) are also known as Pancha Ksheeri Vrikshas in use since Vedic period. Barks of these trees are dried in shade and are used for different formulations (Pancha Kashaya Kalpanas), in different pathological conditions, especially as wound healing, gynecological disorders and etc. The plant samples were extracted using ethanol and water, and subjected for the phytochemical analysis. It was confirmed that samples contain many biologically active compounds like flavonoids, polyphenols, tannins, alkaloids, glycosides and terpinoids etc. The marker compound of each trial drug and the quantitative analysis has been carried out by high performance liquid chromatography. The antioxidant study was done by using in vitro method 1, 1­-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay. The marker compounds caffeic acid and gallic acid were quantified in each extract for their quality and efficacy. PVK barks showed high free radical scavenging activity as evidenced by the low IC50 values in DPPH (EE PVK- 20.46µg/ml, AE PVK-37.79µg/ml, EE T.poulenea-22µg/ml, AE T. poulenia- 23.31µg/ml AE F. benghalensis- 25.53µg/ml, EE F. benghalensis- 26.23µg/ml, EE F. religiosa - 34µg/ml). Quercetin- IC50 value 4.026µg/ml is used as standard. The results of the study demonstrated that PVK barks possess phyto-constituent’s viz. tannins, flavonoids, polyphenols etc. and has potential antioxidant activity. Thus these barks have good therapeutic potential as natural antioxidant and might be used in life style related conditions like hyperlipidemia, diabetes, obesity, cardiovascular disorders and etc.

Potential antifibrotic effect of blueberry and grape polyphenol extracts in acute and subacute bleomycin-induced lung tissue injury models in mice / Potencial efecto antifibrótico de los extractos de polifenoles de arándano y uva en modelos de lesión tisular pulmonar aguda y subaguda inducida por bleomicina en ratones

SUMMARY: An experimental morphological and morphometric study of the antifibrotic function of blueberry and grape extracts was carried out on a model of lung injury in mice induced by intraperitoneal administration of bleomycin. During intraperitoneal administration of bleomycin to mice, acute and subacute damage to the pulmonary system was noted. Both patterns had the same prevalence and severity. The administration of polyphenolic extracts of blueberry and grape to mice showed a significant reduction in the severity of the acute and subacute pattern of lung injury. Blueberry and grape extracts reduce the acute phase of damage to the microvasculature, enhance phagocytic function, have an anti-inflammatory effect, reducing the degree of lymphohistiocytic infiltration and locoregional foci of residual inflammatory effects.

Se realizó un estudio experimental morfológico y morfométrico de la función antifibrótica de extractos de arándano y uva en un modelo de lesión pulmonar en ratones inducida por la administración intraperitoneal de bleomicina. Durante la administración intraperitoneal de bleomicina a ratones, se observaron daños agudos y subagudos en el sistema pulmonar. Ambos patrones tuvieron la misma prevalencia y severidad. La administración de extractos polifenólicos de arándano y uva a ratones mostró una reducción significativa en la severidad del patrón agudo y subagudo de lesión pulmonar. Los extractos de arándano y uva reducen la fase aguda del daño a la microvasculatura, mejoran la función fagocítica, tienen un efecto antiinflamatorio, reducen el grado de infiltración linfohistiocítica y los focos locorregionales de efectos inflamatorios residuales.

Optimization of microwave-assisted extraction of green tea polyphenols by response surface methodology / 药学实践与服务

Objective To optimize the microwave-assisted extraction process of green tea polyphenols. Methods The extraction yield of tea polyphenols was figured up by building the standard curve of gallic acid and examining the concentration of tea polyphenols in green tea extract with the introduction of a correction factor. The effects of four single factor levels of microwave extraction time, microwave output power, liquid-to-material yield, and ethanol volume fraction on the extraction yield of tea polyphenols were primarily studied in this experiment. The response surface was applied to further optimize the extraction process of green tea polyphenols after exploring the appropriate range of four single factor levels. Results The optimal extraction process was as follows: extraction time 37 s, microwave output power 350 w, material - liquid yield 1∶45 (g/ml), ethanol volume fraction 55%, and the actual extraction yield of tea polyphenols was 25.65%, which was not much different from the theoretical value. Conclusion The microwave-assisted green tea polyphenol extraction process optimized by response surface methodology is time-saving and practicable, and the extraction yield is high.

The protective effect of betelnut polyphenols on exercise-induced fatigue at high altitude and its network pharmacology in rats / 中国药理学通报

Aim: To explore the protective effect of betelnut polyphenols on high altitude exercise-induced fatigue in rats, and to select the main targets to carry out network pharmacology research to preliminarily explore its protective mechanism. Methods: We compared the protective effects of areca catechu polyphenols on high altitude exercise fatigue in rats in low, medium and high dose groups (400, 800, and 1600 mg·kg

Oxidative stress, the blood-brain barrier and neurodegenerative diseases: The critical beneficial role of dietary antioxidants

In recent years, growing awareness of the role of oxidative stress in brain health has prompted antioxidants, especially dietary antioxidants, to receive growing attention as possible treatments strategies for patients with neurodegenerative diseases (NDs). The most widely studied dietary antioxidants include active substances such as vitamins, carotenoids, flavonoids and polyphenols. Dietary antioxidants are found in usually consumed foods such as fresh fruits, vegetables, nuts and oils and are gaining popularity due to recently growing awareness of their potential for preventive and protective agents against NDs, as well as their abundant natural sources, generally non-toxic nature, and ease of long-term consumption. This review article examines the role of oxidative stress in the development of NDs, explores the 'two-sidedness' of the blood-brain barrier (BBB) as a protective barrier to the nervous system and an impeding barrier to the use of antioxidants as drug medicinal products and/or dietary antioxidants supplements for prevention and therapy and reviews the BBB permeability of common dietary antioxidant suplements and their potential efficacy in the prevention and treatment of NDs. Finally, current challenges and future directions for the prevention and treatment of NDs using dietary antioxidants are discussed, and useful information on the prevention and treatment of NDs is provided.

Production of hispidin polyphenols from medicinal mushroom Sanghuangporus vaninii in submerged cultures / 中草药·英文版

OBJECTIVE@#The medicinal mushroom Sanghuangporus vaninii produces pharmaceutically valuable hispidin polyphenols in natural habitats. However, due to the slow growth in nature, S. vaninii grown in the field (sclerotia) is not reliable for pharmaceutical purposes. Although higher biomass of fungal mycelia can be obtained in submerged cultures, the accumulation of hispidin polyphenols is rare.@*METHODS@#In this study, the polyunsaturated fatty acids (PUFAs), linoleic acid (LA), linolenic acid (ALA), and methyl jasmonate (MeJa) were employed as the stimulant agents to coordinate the accumulation of biomass and hispidin polyphenols in its submerged cultures.@*RESULTS@#The addition of LA and ALA promoted the mycelial accumulation, while the addition of MeJa inhibited the growth of S. vaninii concomitant with reduced total polyphenols. UPLC-Triple-TOF-MS analysis revealed an increased production of hispidin, phellinstatin, pinnilidine, and its derivatives upon the addition of LA and ALA, and hypholomine B and its isomer, 3,14'-bihispidinyl, and phelligridin E upon the addition of MeJa on day 13. Intriguingly, total polyphenols from the MeJa-supplementing cultures harbored a high capacity in scavenging free radicals. Chemical structural analysis showed that hispidin polyphenols had higher antioxidant activity due to more hispidin moieties induced by MeJa.@*CONCLUSION@#The supplement of PUFAs affects the synthesis and composition of hispidin polyphenols in S. vaninii. Our results provide a possibility to coordinate the production of hispidin polyphenols via submerged cultures of S. vaninii.

Phytochemical screening of Cordia glabrata (MART.) A.DC. extracts and its potential antioxidant, photoprotective, antimicrobial and antiviral activities / Triagem fitoquímica de extratos de Cordia glabrata (MART.) A.DC. e sua potencial atividade antioxidante, fotoprotetora, antimicrobiana e antiviral

Species of the genus Cordia have shown biological activities, such as anti-inflammatory, analgesic, antioxidant, antiviral, and antifungal activities. The species Cordia glabrata (MART) A.DC. Has no information concerning its phytochemical profile and possible biological activities. Thus, this study aimed to evaluate this profile in ethanolic extracts of young, adult and senescent leaves, as well as their antioxidant, photoprotective, antimicrobial, and virucidal potentials. Phytochemical analysis was performed by TLC (thin-layer chromatography) and showed the presence of flavonoids, tannins, and terpenes. The evaluation by UPLC-MS/MS (Ultra performance liquid chromatography - tandem mass spectrometer) evidenced the presence of caffeic (3.89 mgL-¹), p-cumaric (6.13 mgL-¹), and ferulic (0.58 mgL-¹) acids, whilst, in GC/MS (Gas chromatography–mass spectrometry) analysis there was a greater amount of palmitic (51.17%), stearic (20.34%), linoleic (9.62%), and miristic (8.16%) fatty acids. The DPPH (2,2-Diphenyl-1-picrylhydrazyl) and ABTS+ (2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radicals were used to verify the potential antioxidant activity, observing a better activity for the leaf extract in the adult phenological stage: 54.63 ± 1.06 µgmL-¹ (DPPH) and 44.21 ± 1.69 mM (ABTS). The potential photoprotective activity of the extracts was determined by spectrophotometry and the in vitro values of SPF (Sun Protection Factor) in young and adult leaves (5.47 and 5.41, respectively) showed values close to the minimum SPF of 6.0 required by ANVISA (Brazilian Health Regulatory Agency). It was not observed an antimicrobial activity for Staphylococcus aureus with a minimum inhibitory concentration of 2000 µgmL-¹, however the anti-herpetic assay against the Herpes simplex virus type 2 (HSV-2) showed a potent virucidal activity at the tested concentrations with CV50 value <0.195 µgmL-¹ and a Selectivity Index (SI = CC50 / CV50) greater than 448. The results [...].

Espécies do gênero Cordia apresentam atividades biológicas, como anti-inflamatória, analgésica, antioxidante, antiviral e antifúngica. Para a espécie Cordia glabrata (MART) A.DC., ainda não existem informações sobre seu perfil fitoquímico e possíveis atividades biológicas, deste modo, o presente estudo teve como objetivo avaliar este perfil em extratos etanólicos de folhas jovens, adultas e senescentes, bem como o potencial antioxidante, fotoprotetor, antimicrobiano e virucida. A análise fitoquímica foi realizada por CCD (Cromatografia em Camada Delgada), mostrando a presença de flavonóides, taninos e terpenos. Na avaliação por CLAE EM/EM (Cromatografia Líquida de Ultra Eficiência acoplada a Espectrometria de Massas) foi evidenciado a presença dos ácidos caféico (3,89 mgL-¹), p-cumárico (6,13 mgL-¹) e ferúlico (0,58 mgL-¹), paralelamente, na CG/EM (Cromatografia Gasosa acoplada a Espectrometria de Massas) verificou-se maior quantidade dos ácidos graxos palmítico (51,17%), esteárico (20,34%), linoléico (9,62%) e mirístico (8,16%). Os radicais DPPH (2,2-Difenil-1-picrilhidrazil) e ABTS+ (2′-Azino-bis (ácido 3-etilbenzotiazolina-6-sulfônico)) foram utilizados para verificar o potencial antioxidante, observando se uma atividade superior para o extrato da folha em sua fase fenológica adulta: 54,63 ± 1,06 µgmL-¹ (DPPH) e 44,21 ± 1,69 mM (ABTS+). A potencial atividade fotoprotetora dos extratos foi determinada espectrofotometricamente e os valores in vitro de FPS (Fator de Proteção Solar) em folhas jovens e adultas (5,47 e 5,41 respectivamente) apresentaram valores próximos ao FPS mínimo de 6,0 exigido pela ANVISA (Agência Nacional de Vigilância Sanitária). Não foi observada atividade antimicrobiana para Staphylococcus aureus sendo a concentração inibitória mínima de 2000 µgmL-¹, no entanto o ensaio anti-herpético contra o vírus Herpes simplex tipo 2 (HSV-2) mostrou uma potente atividade virucida nas concentrações testadas [...].

Phytochemical screening of Cordia glabrata (MART.) A.DC. extracts and its potential antioxidant, photoprotective, antimicrobial and antiviral activities

Abstract Species of the genus Cordia have shown biological activities, such as anti-inflammatory, analgesic, antioxidant, antiviral, and antifungal activities. The species Cordia glabrata (MART) A.DC. Has no information concerning its phytochemical profile and possible biological activities. Thus, this study aimed to evaluate this profile in ethanolic extracts of young, adult and senescent leaves, as well as their antioxidant, photoprotective, antimicrobial, and virucidal potentials. Phytochemical analysis was performed by TLC (thin-layer chromatography) and showed the presence of flavonoids, tannins, and terpenes. The evaluation by UPLC-MS/MS (Ultra performance liquid chromatography - tandem mass spectrometer) evidenced the presence of caffeic (3.89 mgL-1), p-cumaric (6.13 mgL-1), and ferulic (0.58 mgL-1) acids, whilst, in GC/MS (Gas chromatographymass spectrometry) analysis there was a greater amount of palmitic (51.17%), stearic (20.34%), linoleic (9.62%), and miristic (8.16%) fatty acids. The DPPH (2,2-Diphenyl-1-picrylhydrazyl) and ABTS+ (2-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radicals were used to verify the potential antioxidant activity, observing a better activity for the leaf extract in the adult phenological stage: 54.63 ± 1.06 µgmL-1 (DPPH) and 44.21 ± 1.69 mM (ABTS). The potential photoprotective activity of the extracts was determined by spectrophotometry and the in vitro values of SPF (Sun Protection Factor) in young and adult leaves (5.47 and 5.41, respectively) showed values close to the minimum SPF of 6.0 required by ANVISA (Brazilian Health Regulatory Agency). It was not observed an antimicrobial activity for Staphylococcus aureus with a minimum inhibitory concentration of 2000 gmL-1, however the anti-herpetic assay against the Herpes simplex virus type 2 (HSV-2) showed a potent virucidal activity at the tested concentrations with CV50 value 0.195 gmL-1 and a Selectivity Index (SI = CC50 / CV50) greater than 448. The results obtained in this study suggest that extracts of leaves of C. glabrata in their adult phenological stage have potential antioxidant, photoprotective and virucidal activity, considering in vitro test results.

Resumo Espécies do gênero Cordia apresentam atividades biológicas, como anti-inflamatória, analgésica, antioxidante, antiviral e antifúngica. Para a espécie Cordia glabrata (MART) A.DC., ainda não existem informações sobre seu perfil fitoquímico e possíveis atividades biológicas, deste modo, o presente estudo teve como objetivo avaliar este perfil em extratos etanólicos de folhas jovens, adultas e senescentes, bem como o potencial antioxidante, fotoprotetor, antimicrobiano e virucida. A análise fitoquímica foi realizada por CCD (Cromatografia em Camada Delgada), mostrando a presença de flavonóides, taninos e terpenos. Na avaliação por CLAE EM/EM (Cromatografia Líquida de Ultra Eficiência acoplada a Espectrometria de Massas) foi evidenciado a presença dos ácidos caféico (3,89 mgL-1), p-cumárico (6,13 mgL-1) e ferúlico (0,58 mgL-1), paralelamente, na CG/EM (Cromatografia Gasosa acoplada a Espectrometria de Massas) verificou-se maior quantidade dos ácidos graxos palmítico (51,17%), esteárico (20,34%), linoléico (9,62%) e mirístico (8,16%). Os radicais DPPH (2,2-Difenil-1-picrilhidrazil) e ABTS+ (2-Azino-bis (ácido 3-etilbenzotiazolina-6-sulfônico)) foram utilizados para verificar o potencial antioxidante, observando-se uma atividade superior para o extrato da folha em sua fase fenológica adulta: 54,63 ± 1,06 µgmL-1 (DPPH) e 44,21 ± 1,69 mM (ABTS+). A potencial atividade fotoprotetora dos extratos foi determinada espectrofotometricamente e os valores in vitro de FPS (Fator de Proteção Solar) em folhas jovens e adultas (5,47 e 5,41 respectivamente) apresentaram valores próximos ao FPS mínimo de 6,0 exigido pela ANVISA (Agência Nacional de Vigilância Sanitária). Não foi observada atividade antimicrobiana para Staphylococcus aureus sendo a concentração inibitória mínima de 2000 gmL-1, no entanto o ensaio anti-herpético contra o vírus Herpes simplex tipo 2 (HSV-2) mostrou uma potente atividade virucida nas concentrações testadas com um valor de CV50 0,195 gmL-1 e um Índice de Seletividade (IS = CC50 / CV50) maior que 448. Os resultados obtidos neste estudo sugerem que extratos de folhas de C. glabrata em seu estágio fenológico adulto apresentam potencial antioxidante, fotoprotetora e virucida, considerando os resultados de testes in vitro.

Antineoplastic properties of polyphenols in TPC-1 human papillary thyroid carcinoma cell line: a systematic review

ABSTRACT Thyroid cancer usually responds to surgical and ablative therapy, but when it's refractory the alternative lies in tyrosine kinase inhibitors that, in addition to harmful side effects, acts only in a palliative way. The concern for other therapeutic possibilities brought evidence on flavonoids, hypothesizing a possible strategy. This review aimed to organize a compilation of in vitro studies using polyphenol substances in TPC-1 (human papillary thyroid carcinoma cell line) summarizing it's results and describing the metabolic pathways involved. Articles were selected on PubMed, Google Scholar, LILACS, BVS and SciELO, using keywords "thyroid cancer", "flavonoids" and "TPC-1", until June 2022. 185 studies were selected. After identification and exclusion of duplicates and exclusion criteria applied, 11 original articles were evaluated. Of these, the findings of flavonoids added to TPC-1 were: inhibition of cell growth and viability, promotion of cell cycle arrest and induction of apoptosis. Polyphenolic compounds have antineoplastic properties by different mechanisms as shown in vitro, but the concentrations needed are above usual dietary consumption and the findings are limited to experimental cellular studies. Despite that, these results should be useful to guide further analysis aiming to reveal the real safety and efficacy of polyphenols in this scenario.

Rinsing solutions containing natural extracts and fluoride prevent enamel erosion in vitro

Abstract Polyphenols interact with salivary proteins and thus can improve the pellicle's erosion protective properties. This effect could be exploited to create rinsing solutions with polyphenols as active ingredients for erosion prevention. Different from the current gold standard for erosion protective rinsing solutions, these rinses would not rely on stannous ions. This would offer alternatives for patients with concerns regarding the composition of rinsing solutions and preferring bio-products. Objective To develop an erosion-preventive rinsing solution containing natural polyphenol-rich extracts. Methodology Solutions were prepared with polyphenols from either grapeseed extract or cranberry extract, 500 ppm fluoride added, and additionally flavors and sweeteners. Controls were deionized water, 500 ppm fluoride solution, and the gold standard rinse in the field (Sn2+/F-). In total, 135 enamel specimens (n=15/group) were subjected to five cycles of salivary pellicle formation (30 min, 37°C), modification with the solutions (2 min, 25°C), further salivary pellicle formation (60 min, 37°C), and erosive challenge (1 min, 1% citric acid, pH 3.6). Relative surface microhardness (rSMH), surface reflection intensity (rSRI), and amount of calcium release (CaR) were investigated. Data were analyzed with Kruskal-Wallis and Wilcoxon rank sum tests (α=0.05). Results The polyphenol solutions containing fluoride, as well as additional flavors, protected enamel better than fluoride alone, and similar to the Sn2+/F- solution, when investigating both rSMH and CaR. When measuring rSRI, Sn2+/F- showed the best protection, while the polyphenol solutions were similar to fluoride. Conclusion For two of the three assessed parameters (rSMH and CaR), both developed polyphenol-rich rinsing solutions were able to protect enamel from erosion, improving/potentializing the effect of fluoride and matching the protection offered by the current gold standard rinsing solution.

Teores de polifenóis totais e de umidade em amostras de rizomas de Limonium brasiliense / Total polyphenols and moisture contents in samples of Limonium brasiliense rhizomes / Polifenoles totales y contenido de humedad en muestras de rizomas de Limonium brasiliense

O Limonium brasiliense (Boiss.) Kuntze (Plumbaginaceae), chamado popularmente de baicuru ou guaicuru é uma erva perene presente em todo litoral sul do Brasil, sendo indicada tradicionalmente para síndrome pré-menstrual e distúrbios menstruais. Essas atividades são atribuídas à presença dos polifenóis concentrados em seus rizomas, que também apresentam atividades bacteriostáticas, antioxidantes, antivirais e anti-inflamatórias. No desenvolvimento de formulações feitas a partir da droga vegetal são necessários testes de controle de qualidade durante todo o processo a fim de garantir a segurança, eficácia e qualidade da matéria-prima até sua formulação final. As metodologias utilizadas no desenvolvimento deste trabalho foram de análises físico-químicas para o controle de qualidade, análises quantitativas para determinação do teor de polifenóis totais e, por fim, uma análise comparativa entre os resultados obtidos no ano da coleta do material vegetal (2010) e das mesmas características após 13 anos da coleta, utilizando amostras do L. brasiliense com a presença de fungos ou sem nos rizomas. Sendo assim, este trabalho teve como objetivo realizar o controle de qualidade comparativo dos rizomas de Limonium brasiliense coletados em 2010 em relação ao teor de polifenóis totais e de umidade em 2023. Os resultados obtidos evidenciaram a produção de polifenóis pelos fungos na amostra contaminada, além de mostrarem a qualidade de armazenagem da droga vegetal. Com isso, foi possível concluir que o teor de polifenóis totais da amostra com fungo aumentou após 13 anos da coleta, e que neste interim não houve mudanças no teor de umidade da amostra sem fungo, garantindo sua qualidade no desenvolvimento de formulações ou pesquisas futuras.

Limonium brasiliense (Boiss.) Kuntze (Plumbaginaceae), popularly called baicuru or guaicuru, is a perennial herb present throughout the southern coast of Brazil, traditionally indicated for premenstrual syndrome and menstrual disorders. These activities are attributed to the presence of polyphenols concentrated in its rhizomes, which also have bacteriostatic, antioxidant, antiviral and anti-inflammatory activities. When developing formulations made from plant-based drugs, quality control tests are necessary throughout the process to ensure the safety, efficacy and quality of the raw material until its final formulation. The methodologies used in the development of this work were physical-chemical analyzes for quality control, quantitative analyzes to determine the total polyphenol content and, finally, a comparative analysis between the results obtained in the year the plant material was collected (2010) and the same characteristics after 13 years of collection, using samples of L. brasiliense with or without the presence of fungi in the rhizomes. Therefore, this work aimed to carry out comparative quality control of Limonium brasiliense rhizomes collected in 2010 in relation to the content of total polyphenols and moisture in 2023. The results obtained showed the production of polyphenols by fungi in the contaminated sample, in addition to show the storage quality of the plant drug. With this, it was possible to conclude that the total polyphenol content of the sample with fungus increased after 13 years of collection, and that in the meantime there were no changes in the moisture content of the sample without fungus, guaranteeing its quality in the development of formulations or future research.

Limonium brasiliense (Boiss.) Kuntze (Plumbaginaceae), popularmente llamada baicuru o guaicuru, es una hierba perenne presente en toda la costa sur de Brasil, tradicionalmente indicada para el síndrome premenstrual y trastornos menstruales. Estas actividades se atribuyen a la presencia de polifenoles concentrados en sus rizomas, que también tienen actividades bacteriostáticas, antioxidantes, antivirales y antiinflamatorias. Cuando se desarrollan formulaciones elaboradas a partir de medicamentos de origen vegetal, son necesarios ensayos de control de calidad durante todo el proceso para garantizar la seguridad, eficacia y calidad de la materia prima hasta su formulación final. Las metodologías utilizadas en el desarrollo de este trabajo fueron análisis físico- químicos para control de calidad, análisis cuantitativos para determinar el contenido de polifenoles totales y, finalmente, un análisis comparativo entre los resultados obtenidos en el año de recolección del material vegetal (2010) y el mismas características después de 13 años de colecta, utilizando muestras de L. brasiliense con o sin presencia de hongos en los rizomas. Por lo tanto, este trabajo tuvo como objetivo realizar un control de calidad comparativo de los rizomas de Limonium brasiliense recolectados en 2010 en relación al contenido de polifenoles totales y humedad en 2023. Los resultados obtenidos mostraron la producción de polifenoles por hongos en la muestra contaminada, además de mostrar la calidad de almacenamiento de la droga vegetal. Con esto se pudo concluir que el contenido total de polifenoles de la muestra con hongos aumentó después de 13 años de colecta, y que mientras tanto no hubo cambios en el contenido de humedad de la muestra sin hongos, garantizando su calidad en el desarrollo. de formulaciones o investigaciones futuras.

Phytochemical screening of Cordia glabrata (MART.) A.DC. extracts and its potential antioxidant, photoprotective, antimicrobial and antiviral activities / Triagem fitoquímica de extratos de Cordia glabrata (MART.) A.DC. e sua potencial atividade antioxidante, fotoprotetora, antimicrobiana e antiviral

Abstract Species of the genus Cordia have shown biological activities, such as anti-inflammatory, analgesic, antioxidant, antiviral, and antifungal activities. The species Cordia glabrata (MART) A.DC. Has no information concerning its phytochemical profile and possible biological activities. Thus, this study aimed to evaluate this profile in ethanolic extracts of young, adult and senescent leaves, as well as their antioxidant, photoprotective, antimicrobial, and virucidal potentials. Phytochemical analysis was performed by TLC (thin-layer chromatography) and showed the presence of flavonoids, tannins, and terpenes. The evaluation by UPLC-MS/MS (Ultra performance liquid chromatography - tandem mass spectrometer) evidenced the presence of caffeic (3.89 mgL-1), p-cumaric (6.13 mgL-1), and ferulic (0.58 mgL-1) acids, whilst, in GC/MS (Gas chromatography-mass spectrometry) analysis there was a greater amount of palmitic (51.17%), stearic (20.34%), linoleic (9.62%), and miristic (8.16%) fatty acids. The DPPH (2,2-Diphenyl-1-picrylhydrazyl) and ABTS+ (2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radicals were used to verify the potential antioxidant activity, observing a better activity for the leaf extract in the adult phenological stage: 54.63 ± 1.06 µgmL-1 (DPPH) and 44.21 ± 1.69 mM (ABTS). The potential photoprotective activity of the extracts was determined by spectrophotometry and the in vitro values of SPF (Sun Protection Factor) in young and adult leaves (5.47 and 5.41, respectively) showed values close to the minimum SPF of 6.0 required by ANVISA (Brazilian Health Regulatory Agency). It was not observed an antimicrobial activity for Staphylococcus aureus with a minimum inhibitory concentration of 2000 μgmL-1, however the anti-herpetic assay against the Herpes simplex virus type 2 (HSV-2) showed a potent virucidal activity at the tested concentrations with CV50 value <0.195 μgmL-1 and a Selectivity Index (SI = CC50 / CV50) greater than 448. The results obtained in this study suggest that extracts of leaves of C. glabrata in their adult phenological stage have potential antioxidant, photoprotective and virucidal activity, considering in vitro test results.

Resumo Espécies do gênero Cordia apresentam atividades biológicas, como anti-inflamatória, analgésica, antioxidante, antiviral e antifúngica. Para a espécie Cordia glabrata (MART) A.DC., ainda não existem informações sobre seu perfil fitoquímico e possíveis atividades biológicas, deste modo, o presente estudo teve como objetivo avaliar este perfil em extratos etanólicos de folhas jovens, adultas e senescentes, bem como o potencial antioxidante, fotoprotetor, antimicrobiano e virucida. A análise fitoquímica foi realizada por CCD (Cromatografia em Camada Delgada), mostrando a presença de flavonóides, taninos e terpenos. Na avaliação por CLAE EM/EM (Cromatografia Líquida de Ultra Eficiência acoplada a Espectrometria de Massas) foi evidenciado a presença dos ácidos caféico (3,89 mgL-1), p-cumárico (6,13 mgL-1) e ferúlico (0,58 mgL-1), paralelamente, na CG/EM (Cromatografia Gasosa acoplada a Espectrometria de Massas) verificou-se maior quantidade dos ácidos graxos palmítico (51,17%), esteárico (20,34%), linoléico (9,62%) e mirístico (8,16%). Os radicais DPPH (2,2-Difenil-1-picrilhidrazil) e ABTS+ (2′-Azino-bis (ácido 3-etilbenzotiazolina-6-sulfônico)) foram utilizados para verificar o potencial antioxidante, observando-se uma atividade superior para o extrato da folha em sua fase fenológica adulta: 54,63 ± 1,06 µgmL-1 (DPPH) e 44,21 ± 1,69 mM (ABTS+). A potencial atividade fotoprotetora dos extratos foi determinada espectrofotometricamente e os valores in vitro de FPS (Fator de Proteção Solar) em folhas jovens e adultas (5,47 e 5,41 respectivamente) apresentaram valores próximos ao FPS mínimo de 6,0 exigido pela ANVISA (Agência Nacional de Vigilância Sanitária). Não foi observada atividade antimicrobiana para Staphylococcus aureus sendo a concentração inibitória mínima de 2000 μgmL-1, no entanto o ensaio anti-herpético contra o vírus Herpes simplex tipo 2 (HSV-2) mostrou uma potente atividade virucida nas concentrações testadas com um valor de CV50 <0,195 μgmL-1 e um Índice de Seletividade (IS = CC50 / CV50) maior que 448. Os resultados obtidos neste estudo sugerem que extratos de folhas de C. glabrata em seu estágio fenológico adulto apresentam potencial antioxidante, fotoprotetora e virucida, considerando os resultados de testes in vitro.

Therapeutic Potential of Pomegranate in SARS-CoV-2 and Acute Respiratory Distress Syndrome (ARDS)

COVID-19 is a viral disease caused by Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2), which has rapidly spread across the world causing a global health crisis. Due to the paucity of therapeutics against SARS-CoV-2, there is an urgent need for the identification of safe and effective treatments for this global pandemic. Thus, existing anti-viral and immunosuppressive drugs, are being evaluated as potential candidates and also an extensive amount of research is being conducted to develop novel therapeutic agents against COVID-19. Since ancient times natural products have been used as a treatment for a variety of diseases and to aid in the synthetic drug development process. The phytochemical constituents of Pomegranate have been extensively investigated in the past decade for their anti-tumor activity. The purpose of this review is to elaborate on how the major phytochemicals of pomegranate such as delphinidin, cyanidin, ellagitannin, and punicalagin could be utilized as pharmacological agents to suppress SARS-CoV-2 cell entry, replication, and immunological sequences that give rise to ARDS, based on current knowledge of interactome between host cells and SARS-CoV-2. The SARS-CoV-2 uses various biological mechanisms to modulate immune reactions, uncontrolled gene expression, and cell invasion to improve their survival inside the human host cells similar to those observed in certain tumors. Existing evidence suggests that certain tumors and SARS-CoV-2 use similar biological pathways for human cell invasion. Therefore, this review utilizes the findings of existing tumor-related research which describe how pomegranate extract interacts with various biological pathways associated with tumor suppression as indirect evidence for its ability to act as a potential therapeutic agent against SARS-CoV-2.

Role of Condensed Tannins in the Antioxidant Activity of Seeds of Cola nitida (Vent.) Schott & Endl. (Malvaceae)

Background: Native to West Africa, Cola nitida is a tropical tree of about 8-12 in height that grows in lowland rainforest. This plant is best known in Africa for its seeds, used in phytotherapy but for their socio-cultural importance. Aims/Objective: This study investigated the antioxidant activity of condensed tannins of Cola nitida seeds by carrying out two antioxidant tests (DPPH and FRAP). Methods: From a hydro-ethanolic extract of Cola nitida seeds, two samples were made. One treated with casein (EC) and another one without treatment (EWC). The researsh of condensed tannins were carried out by precipitation with Stiasny reagent. The total polyphenol and tannin contents were evaluated by the Folin-Denis method and the antioxidant power by DPPH and FRAP tests. Results: Extract without treatment (EWC) showed more antioxidant activity than the extract treated with casein (EC). Thus, the IC50 of EWC which contains condensed tannins was 5.54±0.005 µg/ml, while that of EC (without condensed tannins) reached 61.92±0.165 µg/ml. Conclusion: Cola nitida seeds are rich in condensed tannins that play an important role in the antioxidant activity.