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Braz. j. biol ; 83: 1-9, 2023. tab, ilus
Article in English | LILACS, VETINDEX | ID: biblio-1468875


Cisplatin (CP) is a commonly used, powerful antineoplastic drug, having numerous side effects. Casticin (CAS) is considered as a free radical scavenger and a potent antioxidant. The present research was planned to assess the curative potential of CAS on CP persuaded renal injury in male albino rats. Twenty four male albino rats were distributed into four equal groups. Group-1 was considered as a control group. Animals of Group-2 were injected with 5mg/kg of CP intraperitoneally. Group-3 was co-treated with CAS (50mg/kg) orally and injection of CP (5mg/kg). Group-4 was treated with CAS (50mg/kg) orally throughout the experiment. CP administration substantially reduced the activities of catalase (CAT), superoxide dismutase (SOD), peroxidase (POD), glutathione S-transferase (GST), glutathione reductase (GSR), glutathione (GSH) content while increased thiobarbituric acid reactive substances (TBARS), and hydrogen peroxide (H2O2) levels. Urea, urinary creatinine, urobilinogen, urinary proteins, kidney injury molecule-1 (KIM-1), and neutrophil gelatinase-associated lipocalin (NGAL) levels were substantially increased. In contrast, albumin and creatinine clearance was significantly reduced in CP treated group. The results demonstrated that CP significantly increased the inflammation indicators including nuclear factor kappa-B (NF-κB), tumor necrosis factor-α (TNF-α), Interleukin-1β (IL-1β), Interleukin-6 (IL-6) levels and cyclooxygenase-2 (COX-2) activity and histopathological damages. However, the administration of CAS displayed a palliative effect against CP-generated renal toxicity and recovered all parameters by bringing them to a normal level. These results revealed that the CAS is an effective compound having the curative potential to counter the CP-induced renal damage.

A cisplatina (CP) é uma droga antineoplásica poderosa, comumente usada, com vários efeitos colaterais. Casticin (CAS) é considerado um eliminador de radicais livres e um potente antioxidante. A presente pesquisa foi planejada para avaliar o potencial curativo da CAS em lesão renal induzida por PC em ratos albinos machos. Vinte e quatro ratos albinos machos foram distribuídos em quatro grupos iguais. O Grupo 1 foi considerado grupo controle. Os animais do Grupo 2 foram injetados com 5 mg / kg de PB por via intraperitoneal. O Grupo 3 foi cotratado com CAS (50 mg / kg) por via oral e injeção de CP (5 mg / kg). O Grupo 4 foi tratado com CAS (50 mg / kg) por via oral durante todo o experimento. A administração de CP reduziu substancialmente as atividades de catalase (CAT), superóxido dismutase (SOD), peroxidase (POD), glutationa S-transferase (GST), glutationa redutase (GSR), glutationa (GSH), enquanto aumentou as substâncias reativas ao ácido tiobarbitúrico (TBARS) e níveis de peróxido de hidrogênio (H2O2). Os níveis de ureia, creatinina urinária, urobilinogênio, proteínas urinárias, molécula 1 de lesão renal (KIM-1) e lipocalina associada à gelatinase de neutrófilos (NGAL) aumentaram substancialmente. Em contraste, a albumina e a depuração da creatinina foram significativamente reduzidas no grupo tratado com PC. Os resultados demonstraram que a CP aumentou significativamente os indicadores de inflamação, incluindo fator nuclear kappa-B (NF-κB), fator de necrose tumoral-α (TNF-α), interleucina-1β (IL-1β), interleucina-6 (IL-6) níveis e atividade da ciclooxigenase-2 (COX-2) e danos histopatológicos. No entanto, a administração de CAS apresentou um efeito paliativo contra a toxicidade renal gerada por CP e recuperou todos os parâmetros, trazendo-os a um nível normal. Estes resultados revelaram que o CAS é um composto eficaz com potencial curativo para combater o dano renal induzido por CP.

Male , Animals , Rats , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/adverse effects , Antioxidants/administration & dosage , Antioxidants/pharmacology , Kidney/injuries , Free Radical Scavengers/administration & dosage , Free Radical Scavengers/pharmacology , Rats, Inbred Strains
Braz. J. Pharm. Sci. (Online) ; 58: e18747, 2022. tab, graf
Article in English | LILACS | ID: biblio-1374571


Abstract Phenolic compounds are widely distributed in the plant kingdom and in the microorganisms. Cinnamic acid and its hydroxylated derivative-ferulic acid, are phenolic compounds. Ferulic acid possesses antioxidant potential, as well as anti-cancer, anti-inflammatory, and antimicrobial properties. It prevents the harmful effects of radiation both as an ultraviolet absorber and as a free radical scavenger; it is not cytotoxic. Although ferulic acid has beneficial properties, it is hardly used in cosmetic preparations and has been rarely studied in the literature. Herein, we review the literature on ferulic acid, to provide information which can contribute to further research on the compound.

Phenolic Compounds , Literature , Antioxidants/analysis , Acids/administration & dosage , Laboratory and Fieldwork Analytical Methods , Free Radical Scavengers/classification , Neoplasms/diagnosis
Bol. latinoam. Caribe plantas med. aromát ; 20(6): 611-637, nov. 2021. ilus, tab
Article in English | LILACS | ID: biblio-1369862


The objective of the work was to determine the antioxidant potential in vitro of freeze-dried peel extracts of 20 fruits from the northern region of Peru through five tests (Folin-Ciocalteu, DPPH., ABTS+., FRAP and CUPRAC). According to multivariate statistical analyzes, five groups were found: (i.) peel extracts with the highest values of antioxidant capacity (AC) from custard apple, and star fruit; (ii.) rind extracts with high AC values from quince, sweet granadilla, guava, and black grape; (iii.) husk extracts with middle values of AC from passion fruit, and red mombin; (iv.) shell extracts with low AC values from tangerine, mandarine, and bitter orange; and, (v.) coating extracts with the lowest AC values from pawpaw, red pawpaw, muskmelon, dragon fruit, yellow and red indian figs, pear, apple, and green grape. To conclude, the fruit lyophilized-husk extracts of custard apple, star fruit, quince, sweet granadilla, guava, and black grape obtained the best AC.

El objetivo del trabajo fue determinar el potencial antioxidante in vitro de extractos de cáscara liofilizada de 20 frutos de la región norte del Perú mediante cinco pruebas (Folin-Ciocalteu, DPPH., ABTS+., FRAP y CUPRAC). Según análisis estadísticos multivariados, se encontraron cinco grupos: (i.) Extractos de piel con los valores más altos de capacidad antioxidante (CA) de chirimoya y carambola; (ii.) extractos de cáscara con altos valores de CA de membrillo, granadilla dulce, guayaba y uva negra; (iii.) extractos de cáscara con valores medios de CA de maracuyá y mombina roja; (iv.) extractos de cáscara con valores bajos de CA de mandarina, mandarina y naranja amarga; y (v.) recubrir extractos con los valores de CA más bajos de papaya, papaya roja, melón, fruta del dragón, higos indios amarillos y rojos, pera, manzana y uva verde. Para concluir, los extractos de cáscara liofilizada de chirimoya, carambola, membrillo, granadilla dulce, guayaba y uva negra obtuvieron el mejor CA.

Humans , Fruit/chemistry , Antioxidants/chemistry , Peru , Phenols/analysis , In Vitro Techniques , Free Radical Scavengers , Colorimetry , Phenolic Compounds/analysis
Bol. latinoam. Caribe plantas med. aromát ; 20(6): 660-671, nov. 2021. tab, ilus
Article in English | LILACS | ID: biblio-1369981


Search for safe antioxidants and novel nutraceuticals urged to evaluate the antioxidant, anti-acetylcholine esterase and anti-lipoxygenase activity of various leaf extracts of Conocarpus lancifolius. Extraction was optimized from freeze dried plant extracts quenched with liquid nitrogen using water, ethanol, methanol, hexane, ethyl acetate and chloroform. Maximum extract yield, total phenolic contents and total flavonoid contents were obtained in case of ethanolic extraction. The highest 2,2-diphenyl-1-picrylhydrazylradical scavenging in terms of IC50 value of 55.26 µg/mL was observed for ethanolic leaf extract. The acetylcholine esterase and lipoxygenase inhibitory activities (IC50) were also observed for ethanolic extract. These findings for ethanolic extract were statistically significant when compared with other extracts (ρ<0.05). The haemolytic % values indicated that all extracts were associated with very low or negligible toxicity. The epicatechin, isorhamnetin, rutin, scopoleptin, skimmianine, quercetin-3-O-α-rhamnoside, quercetin-3-O-ß-glucoside, cornoside, creatinine, choline, pyruvic acid, α-hydroxybutyric acid, phyllanthin and hypophyllanthin were identified as major functional metabolites in ethanolic leaf extract of C. lancifoliusby 1H-NMR. The identified metabolites were probably responsible for the pharmacological properties of C.lancifolius. The findings may be utilized as pharmacological leads for drug development and food fortification.

Se insta a la búsqueda de antioxidantes seguros y nuevos nutracéuticos para evaluar la actividad antioxidante, anti-acetilcolina esterasa y anti-lipoxigenasa de varios extractos de hojas de Conocarpus lancifolius. La extracción se optimizó a partir de extractos de plantas liofilizados enfriados con nitrógeno líquido usando agua, etanol, metanol, hexano, acetato de etilo y cloroformo. En el caso de extracción etanólica se obtuvo el rendimiento máximo de extracto, el contenido de fenoles totales y el contenido de flavonoides totales. La mayor eliminación de radicales 2,2-difenil-1-picrilhidrazilo en términos de valor de CI50 de 55,26 µg/mL se observó para el extracto de hoja etanólico. También se observaron las actividades inhibidoras de la acetilcolina esterasa y lipoxigenasa (CI50) para el extracto etanólico. Estos hallazgos para el extracto etanólico fueron estadísticamente significativos en comparación con otros extractos (ρ<0.05). Los valores del % hemolítico indicaron que todos los extractos estaban asociados con una toxicidad muy baja o insignificante. Se identificaron la epicatequina, isorhamnetina, rutina, escopoleptina, skimmianina, quercetina-3-O-α-ramnosido, quercetina-3-O-ß-glucósido, cornosido, creatinina, colina, ácido pirúvico, ácido α-hidroxibutírico, filantrina e hipofillantina. como metabolitos funcionales principales en el extracto etanólico de hojas de C. lancifoliuspor 1H-NMR. Los metabolitos identificados probablemente fueron responsables de las propiedades farmacológicas de C. lancifolius. Los hallazgos pueden utilizarse como pistas farmacológicas para el desarrollo de fármacos y la fortificación de alimentos.

Plant Extracts/pharmacology , Combretaceae/chemistry , Antioxidants/pharmacology , Phenols/analysis , Flavonoids/analysis , In Vitro Techniques , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/chemistry , Free Radical Scavengers , Lipoxygenase Inhibitors/pharmacology , Lipoxygenase Inhibitors/chemistry , Ethanol , Antioxidants/chemistry
Bol. latinoam. Caribe plantas med. aromát ; 20(5): 524-535, sept. 2021. tab, ilus
Article in English | LILACS | ID: biblio-1369071


Microsechium helleri (Cucurbitaceae) has been used in ethnopharmacological as a lotion to prevent hair loss, diuretic and cathartic, in the region of central Veracruz, Mexico is used as antidiabetic. The antioxidant properties of the hexanic (EHex), chloroformic (ECHCl3) and ethanolic (EEtOH) extracts, were evaluated by 2,2diphenyl-1-pychrylhydrazyl (DPPH) test, the Ferric Reducing/Antioxidant Power (FRAP) and the total phenolic content test. The anti-inflammatory effect was evaluated in the acute ear edema induced with phorbol 12-myristate 13-acetate (TPA) in mouse and the hypoglycemic and cardioprotective effects of the EEtOH were determined in rats. The EEtOH was the most active in the antioxidant potential DPPH test and the ECHCl3 was the best in the FRAP assay and the total polyphenols content. In the anti-inflammatory assay, the ECHCl3 showed the most activity. The EEtOH had the decreased the glucose levels and reduced myocardial damage. The results support the use of this plant in folk medicine in Mexico as antioxidant, anti-inflammatory, hypoglycemic and cardioprotective.

Microsechium helleri (Cucurbitaceae) se utiliza en etnofarmacología como una loción para prevenir la caída del cabello, como diurético y catártico, en la región del centro de Veracruz, México es usado como antidiabético. Las propiedades antioxidantes de los extractos hexánico (EHex), clorofórmico (ECHCl3) y etanólico (EEtOH), se evaluaron mediante la prueba de 2,2difenil-1-psililhidrazilo (DPPH), el poder reductor férrico/poder antioxidante (FRAP) y el contenido fenólico total. El efecto anti-inflamatorio se evaluó en el edema agudo de la oreja inducido con forbol 12-miristato 13-acetato (TPA) en ratones y se determinaron los efectos hipoglucémicos y cardioprotectores del EEtOH en ratas. El EEtOH fue el más activo en la prueba DPPH de potencial antioxidante y el ECHCl3 fue el mejor en el ensayo FRAP y el contenido total de polifenoles. En el ensayo antiinflamatorio, el ECHCl3 mostró la mayor actividad. El EEtOH disminuyó los niveles de glucosa y redujo el daño miocárdico. Los efectos hipoglucémicos y cardioprotector del extracto de EEtOH se determinaron en ratas, donde el extracto disminuyó los niveles de glucosa y redujo el daño miocárdico. Los resultados apoyan el uso de esta planta en la medicina popular en México como antioxidante, anti-inflamatorio, hipoglucemiante y cardioprotector.

Plant Extracts/pharmacology , Cardiotonic Agents/pharmacology , Cucurbitaceae/chemistry , Hypoglycemic Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Plant Extracts/chemistry , Cardiotonic Agents/chemistry , Free Radical Scavengers , Phenolic Compounds/analysis , Hypoglycemic Agents/chemistry , Medicine, Traditional , Mexico , Anti-Inflammatory Agents/chemistry
Electron. j. biotechnol ; 52: 13-20, July. 2021. tab, graf, ilus
Article in English | LILACS | ID: biblio-1283173


BACKGROUND: In fish farming, the plant extracts containing antioxidant compounds have been added to the diet for enhancing pathogen resistance. In vitro studies evaluating the antioxidant effect of herbal extracts on fish cell models have focused on ROS production and the respiratory burst mechanism. However, the effects on enzymatic antioxidant defense on salmon leukocytes have not been evaluated. This study aims to evaluate the enzymatic antioxidant defense and ROS-induced cell damage in Salmon Head Kidney-1 (SHK-1) cell line exposed to polyphenol-enriched extract from Sambucus nigra flowers. RESULTS: Firstly, the Total Reactive Antioxidant Power (TRAP) assay of elderflower polyphenol (EP) was evaluated, showing 459 and 489 times more active than gallic acid and butyl hydroxy toluene (BHT), respectively. The toxic effect of EP on salmon cells was not significant at concentrations below 120 mg/ mL and no hemolysis activity was observed between 20 and 400 mg/mL. The treatment of SHK-1 cell line with EP decreased both the lipid peroxidation and protein oxidation induced by H2O2, which could be associated with decreasing oxidative stress in the SHK-1 cells since the GSH/GSSG ratio increased when only EP was added. CONCLUSIONS: These results suggest that plant extracts enriched with polyphenols could improve the enzymatic antioxidant defense of salmon leukocytes and protect the cells against ROS-induced cell damage

Salmon , Plant Extracts/pharmacology , Sambucus nigra/chemistry , Polyphenols/pharmacology , Lipid Peroxidation , Free Radical Scavengers , Reactive Oxygen Species , Aquaculture , Oxidative Stress , Salmo salar , Disease Resistance , Leukocytes , Antioxidants
Bol. latinoam. Caribe plantas med. aromát ; 20(3): 226-243, may. 2021. ilus, tab
Article in English | LILACS | ID: biblio-1342815


Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 µg/mL) and FFA (IC50: 1.14 µg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 µg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 µg/mL for EBF and 532.68 µg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.

Varias especies del género Myrcia se han utilizado en la medicina popular para tratar la diabetes. Por lo tanto, el objetivo de este trabajo fue investigar la actividad inhibitoria de la α-glucosidasa y la lipasa pancreática en el extracto crudo (EBF) y en la fracción de acetato de etilo (FFA) de Myrcia hatschbachii, así como identificar compuestos fenólicos aislados y evaluar la propiedad antioxidante y toxicidad in vitro preliminar contra Artemia salina. EBF (IC50: 3.21 µg/mL) y FFA (IC50: 1.14 µg/mL) mostraron una actividad inhibitoria superior a la acarbosa (IC50: 193.65 µg/mL). Además, mostraron efectos inhibitorios de la lipasa pancreática (IC50: 556.58 µg/mL para EBF y 532.68 µg/mL para FFA), potencial antioxidante, ausencia de toxicidad preliminar y presencia de ácidos gálico y elágico en FFA. Los resultados relevantes en la inhibición de la α-glucosidasa y la lipasa pancreática motivan nuevos estudios para el desarrollo de medicamentos a base de hierbas que ayudan en el tratamiento de pacientes diabéticos.

Plant Extracts/pharmacology , Myrtaceae/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Lipase/drug effects , Antioxidants/pharmacology , Pancreas/enzymology , Phenols/analysis , X-Ray Diffraction , In Vitro Techniques , Plant Extracts/toxicity , Plant Extracts/chemistry , Free Radical Scavengers , Complex Mixtures , Ellagic Acid , Gallic Acid , Antioxidants/chemistry
Int. arch. otorhinolaryngol. (Impr.) ; 24(1): 47-52, Jan.-Mar. 2020. graf
Article in English | LILACS | ID: biblio-1090559


Abstract Introduction Cisplatin damages the auditory system and is related to the generation of free radicals. Glutathione peroxidase is an endogenous free radicals remover. Objective To investigate the mechanisms involved in otoprotection by N-acetylcys- teine through the expression of glutathione peroxidase in outer hair cells from rats treated with cisplatin. Methods Male Wistar rats were intraperitoneally injected with cisplatin (8 mg/Kg) and/or received oral administration by gavage of N-acetylcysteine (300 mg/Kg) for 3 consecutive days. On the 4th day, the animals were euthanized and beheaded. The tympanic bullae were removed and prepared for scanning electron microscopy and Results Among the groups exposed to ototoxic doses of cisplatin, there was an increase in glutathione peroxidase immunostaining in two groups, the one exposed to cisplatin alone, and the group exposed to both cisplatin and N-acetylcysteine. Conclusion The expression of glutathione peroxidase in the outer hair cells of rats exposed to cisplatin showed the synthesis of this enzyme under cellular toxicity conditions.

Animals , Male , Acetylcysteine/therapeutic use , Free Radical Scavengers/therapeutic use , Cisplatin/toxicity , Oxidative Stress/drug effects , Antineoplastic Agents/toxicity , Acetylcysteine/metabolism , Acetylcysteine/pharmacology , Microscopy, Electron, Scanning , Evoked Potentials, Auditory, Brain Stem , Free Radical Scavengers/metabolism , Free Radical Scavengers/pharmacology , Fluorescent Antibody Technique , Cisplatin/therapeutic use , Rats, Wistar , Cochlea/anatomy & histology , Cochlea/drug effects , Free Radicals , Glutathione Peroxidase/metabolism , Hearing Loss, Sensorineural/prevention & control
Einstein (Säo Paulo) ; 18: eAO5022, 2020. graf
Article in English | LILACS | ID: biblio-1090060


ABSTRACT Objective To evaluate the effects of oxidative stress on insulin signaling in cardiac tissue of obese mice. Methods Thirty Swiss mice were equally divided (n=10) into three groups: Control Group, Obese Group, and Obese Group Treated with N-acetylcysteine. After obesity and insulin resistance were established, the obese mice were treated with N-acetylcysteine at a dose of 50mg/kg daily for 15 days via oral gavage. Results Higher blood glucose levels and nitrite and carbonyl contents, and lower protein levels of glutathione peroxidase and phosphorylated protein kinase B were observed in the obese group when compared with their respective control. On the other hand, treatment with N-acetylcysteine was effective in reducing blood glucose levels and nitrite and carbonyl contents, and significantly increased protein levels of glutathione peroxidase and phosphorylated protein kinase B compared to the Obese Group. Conclusion Obesity and/or a high-lipid diet may result in oxidative stress and insulin resistance in the heart tissue of obese mice, and the use of N-acetylcysteine as a methodological and therapeutic strategy suggested there is a relation between them.

RESUMO Objetivo Avaliar os efeitos do estresse oxidativo sobre a sinalização da insulina em tecido cardíaco de camundongos obesos. Métodos Utilizaram-se 30 camundongos Swiss subdivididos igualmente (n=10) em três grupos: Grupo Controle, Grupo Obeso e Grupo Obeso Tratado com N-acetilcisteína. Após estabelecidas a obesidade e a resistência à insulina, os camundongos obesos foram tratados diariamente, durante 15 dias, via gavagem oral, com N-acetilcisteína na dose de 50mg/kg. Resultados Observaram-se maiores níveis de glicose sanguínea, conteúdos de nitrito e carbonil, e menores níveis proteicos de glutationa peroxidase e proteína quinase B fosforilada no Grupo Obeso quando comparado a seu respectivo controle. Por outro lado, o tratamento com N-acetilcisteína se mostrou eficiente em diminuir os níveis glicêmicos, os conteúdos de nitrito e carbonil, e aumentar significativamente os níveis proteicos de glutationa peroxidase e proteína quinase B fosforilada, quando comparados ao Grupo Obeso. Conclusão Obesidade e/ou dieta hiperlipídica levam a estresse oxidativo e à resistência à insulina no tecido cardíaco de camundongos obesos, e o uso da N-acetilcisteína como estratégia metodológica e terapêutica sugeriu haver relação entre ambos.

Humans , Animals , Male , Mice , Acetylcysteine/pharmacology , Insulin Resistance/physiology , Free Radical Scavengers/pharmacology , Oxidative Stress/physiology , Diet, High-Fat , Myocardium/metabolism , Reference Values , Spectrophotometry , Blood Glucose/analysis , Body Weight , Blotting, Western , Reactive Oxygen Species/analysis , Oxidative Stress/drug effects , Protein Carbonylation , Fluoresceins/analysis
Article in English | LILACS | ID: biblio-1283651


This study presents analyses on the chemistry, biology, pharmacology and chromatography of essential oils extracted from three species of the Ocotea genus: O. minor, O. ceanothifolia and O. leucoxylon. Leaves and stems, as well as the bark of O. minor, were processed using a modified Clevenger apparatus. Seven essential oils were obtained and analyzed using GC-FID and GC-MS, and their chemical compositions were determined. Assays of cytotoxicity, antioxidant and free radical scavenging activity, as well as tyrosinase and elastase inhibition were performed. In total, 25 constituents were identified, the principal being sesquiterpenes, such as spathulenol caryophyllene and its oxide. The oils did not present cytotoxicity using a hemolytic model, but also did not show antioxidant activity in the DPPH assay. Essential oil from stems of O. ceanothifolia, rich in spathulenol and caryophyllene oxide, demonstrated the capacity to inhibit 49.08% of tyrosinase activity at a concentration of 100 µg/mL. This research contributes to the chemical profile analysis of the three species of Ocoteathrough chemical investigations and biological activity, which are reported for the first time here in this study.

Este trabajo realiza un estudio químico, biológico, farmacológico y cromatográfico de aceites esenciales extraídos de tres especies del género Ocotea: O. minor, O. ceanothifoliay O. leucoxylon. Las hojas y tallos, así como la corteza de O. minor, se procesaron utilizando un aparato Clevenger modificado. Se obtuvieron siete aceites esenciales y se analizaron usando GC-FID y GC-MS, y se determinaron sus composiciones químicas. Se realizaron ensayos de citotoxicidad, actividad antioxidante y de atrapamiento de radicales libres, así como inhibición de tirosinasa y elastasa. En total, se identificaron 25 componentes, siendo los principales sesquiterpenos, como el spathulenol cariofileno y su óxido. Los aceites no presentaron citotoxicidad en un modelo hemolítico y tampoco mostraron actividad antioxidante en el ensayo con DPPH. El aceite esencial de tallos de O. ceanothifolia, rico en espatulenol y óxido de cariofileno, mostró capacidad para inhibir el 49.08% de la actividad de tirosinasa a una concentración de 100 µg/mL. Esta investigación contribuye al análisis del perfil químico de las tres especies de Ocotea a través de investigaciones químicas y actividad biológica la cual se informan por primera vez.

Oils, Volatile/pharmacology , Monophenol Monooxygenase/antagonists & inhibitors , Ocotea/chemistry , Oxides/analysis , Sesquiterpenes/analysis , Oils, Volatile/chemistry , Free Radical Scavengers , Lauraceae/chemistry , Cosmetic Industry , Flame Ionization , Gas Chromatography-Mass Spectrometry
Acta cir. bras ; 35(2): e202000203, 2020. graf
Article in English | LILACS | ID: biblio-1100882


Abstract Purpose To evaluate the effect of remote ischemic conditioning associated to N-acetylcysteine (NAC) on testicular ischemia∕reperfusion (I∕R) injury in rats. Methods Twenty-five adult male Wistar rats were randomly distributed into five experimental groups (n=5), as follows: Sham, I∕R, Perconditioning (PER), NAC and PER+NAC. Two-hour ischemia was induced by rotating the left testis 720° to clockwise direction, followed by 4 hours of reperfusion. Perconditioning was performed by three I/R cycles of 10 min each on the left limb, 30 min before reperfusion. N-acetylcysteine (150 mg∕kg) was administered 30 min before reperfusion. Results Statistical differences were observed in MDA levels between I/R group with all groups (p<0.01), in addition there was statistical difference between PER and Sham, and PER+ NAC groups (p<0.05) in plasma. Conclusions The protective effect of perconditioning isolated in the reduction of lipid peroxidation related to oxidative stress was demonstrated. However, when Perconditioning was associated with NAC, there was no protective effect against testicular injury of ischemia and reperfusion.

Animals , Male , Rats , Acetylcysteine/pharmacology , Testis/blood supply , Reperfusion Injury , Free Radical Scavengers/pharmacology , Oxidative Stress/drug effects , Ischemic Preconditioning/methods , Testis/drug effects , Random Allocation , Rats, Wistar , Drug Evaluation, Preclinical , Oxygen Radical Absorbance Capacity
Biol. Res ; 53: 28, 2020. graf
Article in English | LILACS | ID: biblio-1124213


BACKGROUND: Kidney ischemia-reperfusion injury is a common pathophysiological phenomenon in the clinic. A large number of studies have found that the tyrosine protein kinase/signal transducer and activator of transcription (JAK/STAT) pathway is involved in the development of a variety of kidney diseases and renal protection associated with multiple drugs. Edaravone (EDA) is an effective free radical scavenger that has been used clinically for the treatment of postischemic neuronal injury. This study aimed to identify whether EDA improved kidney function in rats with ischemia-reperfusion injury by regulating the JAK/STAT pathway and clarify the underlying mechanism. METHODS: Histomorphological analysis was used to assess pathological kidney injury, and mitochondrial damage was observed by transmission electron microscopy. Terminal deoxynucleotidyl transferase-mediated dUTP nick endlabeling (TUNEL) staining was performed to detect tubular epithelial cell apoptosis. The expression of JAK2, P-JAK2, STAT3, P-STAT3, STAT1, P-STAT1, BAX and Bcl-2 was assessed by western blotting. Mitochondrial function in the kidney was assessed by mitochondrial membrane potential (ΔψM) measurement. RESULTS: The results showed that EDA inhibited the expression of p-JAK2, p-STAT3 and p-STAT1, accompanied by downregulation of the expression of Bax and caspase-3, and significantly ameliorated kidney damage caused by ischemia-reperfusion injury (IRI). Furthermore, the JC-1 dye assay showed that edaravone attenuated ischemia-reperfusion-induced loss of kidney (ΔψM). CONCLUSION: Our findings indicate that EDA protects against kidney damage caused by ischemia-reperfusion through JAK/STAT signaling, inhibiting apoptosis and improving mitochondrial injury.

Animals , Male , Rats , Reperfusion Injury/drug therapy , Free Radical Scavengers/pharmacology , Edaravone/pharmacology , Signal Transduction/drug effects , Rats, Sprague-Dawley , Apoptosis , STAT Transcription Factors/drug effects , Janus Kinases/drug effects , Mitochondria
Rev. Inst. Nac. Hig ; 50(1-2): 14-21, Diciembre 2019. tab
Article in Spanish | LILACS, LIVECS | ID: biblio-1118362


El Paraquat (PQ) es un herbicida de contacto bipiridilico ampliamente utilizado en agricultura. La intoxicación en humanos por este agente ocasiona fibrosis pulmonar. Evaluamos los cambios histológicos pulmonares de ratas intoxicadas con PQ y tratadas con N-aceticisteina (NAC) administrada vía inhalatoria. Realizamos un estudio experimental descriptivo con 25 ratas adultas, machos cepa Wistar, divididas en cinco grupos. Al grupo I no se les administro ni PQ ni NAC. Grupo II, recibió NAC inhalada a 15mg/kg diaria c/12 horas. Grupo III, PQ vía oral (VO) 15mg/kg. Grupo IV, PQ a 15mg/kg, por VO y a la hora NAC 150mg/kg. Grupo V, PQ a 15mg/kg, por VO y a las seis horas NAC dosis de 150mg/kg. Los pulmones fueron extraídos y se evaluaron mediante cortes histológicos. Resultados: Los grupos I y II (supervivencia del 100%, n=10) no desarrollaron sintomatología de intoxicación. Grupos III, IV y V predominaron síntomas respiratorios, diversos grados de edema pulmonar, enfisema, congestión vascular y hemorragia intra-alveolar focal. La eficacia de la NAC sobre la intoxicación por PQ en términos de sobrevivencia al primer día, fue del 100% y al segundo día, fue del 80% (p= 0,005; prueba Chi-cuadrado). El PQ indujo un proceso inflamatorio (agudo-crónico) por infiltrado de segmentados neutrófilos y linfocitos, lo cual fue revertido parcialmente por la administración inhalada de NAC. Conclusión: Los cambios histopatológicos observados a nivel pulmonar fueron aminorados por el tratamiento con NAC, lo que sugiere un posible efecto protector de este fármaco sobre el daño oxidativo inducido por el herbicida

Paraquat (PQ) is a bipyridyl contact herbicide widely used in agriculture. Intoxication in humans by this agent causes pulmonary fibrosis. We evaluated pulmonary histological changes of rats intoxicated with PQ and treated with N-acetycysteine (NAC) administered via inhalation. We conducted a descriptive experimental study with 25 adult rats, male Wistar strain, divided into five groups. Group I was not administered PQ or NAC. Group II, received NAC inhaled at 15mg/kg daily c/12 hours. Group III, PQ orally (VO) 15mg/ kg. Group IV, PQ at 15mg/kg, by VO and at hour NAC 150mg/ kg. Group V, PQ at 15mg/kg, by VO and at six hours NAC dose of 150mg/kg. The lungs were extracted and evaluated by histological sections. Results: Groups I and II (100% survival, n=10) did not develop intoxication symptoms. Groups III, IV and V predominantly respiratory symptoms, various degrees of pulmonary edema, emphysema, vascular congestion and focal intra-alveolar hemorrhage. The efficacy of NAC on PQ poisoning in terms of survival on the first day was 100% and on the second day it was 80% (p = 0.005, Chi-square test). The PQ induced an inflammatory process (acute-chronic) by infiltration of segmented neutrophils and lymphocytes, which was partially reversed by the inhaled administration of NAC. Conclusion: The histopathological changes observed at the pulmonary level were reduced by the treatment with NAC, which suggests a possible protective effect of this drug on the oxidative damage induced by the herbicide.

Animals , Male , Rats , Paraquat/poisoning , Pulmonary Fibrosis/chemically induced , Pulmonary Fibrosis/drug therapy , Acetylcysteine/therapeutic use , Free Radical Scavengers/therapeutic use , Herbicides/poisoning , Paraquat/administration & dosage , Acetylcysteine/administration & dosage , Time Factors , Administration, Inhalation , Survival Analysis , Free Radical Scavengers/administration & dosage , Treatment Outcome , Rats, Wistar , Models, Animal , Herbicides/administration & dosage
Bol. latinoam. Caribe plantas med. aromát ; 18(3): 277-288, mayo 2019. ilus
Article in English | LILACS | ID: biblio-1007989


Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)Is a popular folk remedy for in Central America. The plant is of commercial value in Guatemala but so far there is not any monograph to guide regional laboratories on ensuring identity and chemical tests for this species. As identity test we here run macro and micro morphoanatomical studies of the characters of the vegetative organs. We also developed standard chemical tests for quality by both TLC and HPLC for infusions and tinctures of varying alcoholic strength. Their radical scavenging activities in DPPH and NO were also measured. Macro and micro morphoanatomical characters of the vegetative organs present a set of characteristics to facilitate the identification of dry powdered samples of this species. We developed optimal conditions for the TLC and HPLC phytochemical fingerprints of the 4 most common pharmacopoeial liquid herbal preparations from this herbal drug, namely infusion, 70%, 45% and 20% hydroalcoholic tinctures. Our work provides the Latin-American industry with a set of analyses to establish the identity and chemistry of N. lobata samples for quality control purposes.

Neurolaena lobata (L.) R.Br. ex cass. (Asteraceae) es un remedio popular popular en América Central. La planta tiene un valor comercial en Guatemala, pero hasta el momento no existe una monografía que guíe a los laboratorios regionales para garantizar la identidad y las pruebas químicas para esta especie. Como prueba de identidad proponemos estudios macro y micro morfoanatómicos de los caracteres de los órganos vegetativos. También desarrollamos pruebas químicas de calidad mediante CCF y CLAR para infusiones y tinturas de grado alcohólico variable. También se midieron sus actividades de captación de radicales en DPPH y NO. Los caracteres macro y micro morfoanatómicos de los órganos vegetativos presentan un conjunto de características para facilitar la identificación de muestras de polvo seco de esta especie. Desarrollamos condiciones óptimas para las huellas dactilares fitoquímicas de CCF y CLAR de las 4 preparaciones herbales líquidas farmacopéicas más comunes de esta droga herbal, a saber, infusión, 70%, 45% y 20% tinturas hidroalcohólicas. Nuestro trabajo proporciona a la industria latinoamericana un conjunto de análisis base para establecer la identidad y la química de las muestras de N. lobata con fines de control de calidad.

Asteraceae/anatomy & histology , Asteraceae/chemistry , Phytochemicals/analysis , Quality Control , Spectrophotometry, Ultraviolet , Free Radical Scavengers , Chromatography, High Pressure Liquid , Chromatography, Thin Layer , Asteraceae/ultrastructure , Guatemala , Microscopy
Article in Chinese | WPRIM | ID: wpr-773192


To establish the spectrum-effect relationship between HPLC fingerprint and free radicals activity scavenging in Guizhi Shaoyao Zhimu Decoction( GSZD),and provide a basis for the quality evaluation and modernization of classical prescriptions. Shimadsu GL-science C18 column( 4. 6 mm×250 mm,5 μm) was used with acetonitrile-0. 1% formic acid solution as the mobile phase for gradient elution. The detective wave length was 254 nm; the column temperature was set at 32 ℃; the injection volume was 20 μL; and the flow rate was 1. 0 m L·min-1.10 batches of primary standard samples of GSZD were detected,and their HPLC fingerprint was established by using the similarity evaluation system for chromatographic fingerprint of traditional Chinese medicine( TCM). The activity of scavenging free radicals was studied by 1,1-diphenyl-2-trinitrophenylhydrazine( DPPH) method,and the spectrum-effect relationship was studied by Pearson bivariate correlation analysis. The common mode of GSZD fingerprints was established,and 26 common peaks were marked,with similarities ranging from 0. 929 to 0. 998. Eight of the chromatographic peaks were identified by using the control comparison method: gallic acid,mangiferin,paeoniflorin,glycyrrhizin,asparagus,5-O-methylvisamicin,cinnamic acid,and ammonium glycyrrhetate. Among them,the content changes of No. 14( paeoniside),20,12( mangiferin),13 and 23( cinnamic acid) common peaks were negatively correlated with free radical scavenging activity. The fingerprint showed high precision,repeatability and stability,and the common peaks were well separated,so it can be used for the quality evaluation of GSZD,and could provide reference for further studies on the material basis of GSZD.

Chromatography, High Pressure Liquid , Cinnamomum aromaticum , Chemistry , Drugs, Chinese Herbal , Chemistry , Free Radical Scavengers , Chemistry , Medicine, Chinese Traditional
Article in Chinese | WPRIM | ID: wpr-773123


To isolate and identify secondary metabolites of marine-derived Streptomyces sp.MDW-06,the isolations and purifications of compounds were performed by means of column chromatography over silica gel. And their structures were elucidated through the spectroscopic analysis of MS,NMR and specific rotations. The bioactivities were assayed by paper diffusion and DPPH method. From the fermentation broth of marine-derived Streptomyces sp.MDW-06,five compounds( 1-5) were isolated and identified as streptopentanoic acid( 1),germicidin A( 2),germicidin B( 3),isogermicidin A( 4),isogermicidin B( 5) and oxohygrolidin( 6),respectively. Compound 1 is a new compound. Compound 1 shows DPPH radical scavenging activity with 36. 4% at 100 mg·L~(-1).

Chromatography , Fermentation , Free Radical Scavengers , Chemistry , Magnetic Resonance Spectroscopy , Polyketides , Chemistry , Streptomyces , Chemistry
Article in Chinese | WPRIM | ID: wpr-777474


Chemical constituents were isolated from the fruiting bodies of Ganoderma australe by various column chromatographic techniques and HPLC method, and their chemical structures were identified through the combined analysis of physicochemical properties and spectral data. Meanwhile, their α-glucosidase inhibitory activity and anti-oxidative ability were evaluated. Seven compounds were isolated from G. australe and were identified as 6-methoxyl-cyclo-(Phe-Ile)(1), applanoxidic acid A methyl ester(2), ergosta-7,22 E-dien-3β-ol(3), cinnamic acid(4), 5α,8α-epidioxy-(20S,22E,24R)-ergosta-6,22-diene-3β-ol(5), 1-(3, 4-dihydroxyphenyl) ethanone(6), salicylic acid(7) and benzoic acid(8). Among the compounds, compound 1 was a new cyclic dipeptide. Compound 2 was a new lanosta natural product, and compounds 4, 6, 7 and 8 were obtained from G. australe for the first time. Moreover, compounds 4 and 8 exhibited α-glucosidase inhibitory activity with inhibition rates of 36.8% and 34.7%, and compounds 4, 7 and 8 had a certain activity in DPPH free radical scavenging activity with IC_(50) values of 0.168, 0.458 and 0.170 g·L~(-1), respectively. The DPPH radical scavenging rate of compound 1 was 41.1%.

Free Radical Scavengers , Fruiting Bodies, Fungal , Chemistry , Ganoderma , Chemistry , Glycoside Hydrolase Inhibitors , Molecular Structure
Article in Chinese | WPRIM | ID: wpr-777527


The hydrogen peroxide generation system was used to analyze the scavenging activity of hydrogen peroxide by Liropes Radix from different origins by HPLC-UV-CL. The UV-CL fingerprints of Liropes Radix from different origins were evaluated,and the HPLC-UV and LC-CL fingerprints were systematically analyzed and evaluated. The results showed that the ether fractions of Liriope spicata var. prolifera and L. muscari had good scavenging activity of hydrogen peroxide,and the total activity of different origins varied greatly,while the similar samples had similar activities. The total antioxidant activity of L. muscari is higher than that of L. spicata var.prolifera. The similarity analysis of the two fingerprints was carried out by two different analytical methods. The chemical fingerprints and the active fingerprints have different characteristics. The contribution of each fingerprint to the total peak area and total activity is also different. There are significant differences between the two different fingerprint clustering results.

Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Free Radical Scavengers , Chemistry , Hydrogen Peroxide , Liriope Plant , Chemistry , Phytochemicals , Chemistry , Plant Extracts , Chemistry , Plant Roots , Chemistry
Braz. arch. biol. technol ; 62: e19170757, 2019. tab, graf
Article in English | LILACS | ID: biblio-1011528


Abstract Lasia spinosa (L.) Thwaites is a widely used ethnomedicinal plant in Bangladesh. In this study, we investigated phenolic contents, volatile compounds and fatty acids, and essential oil components of extracts prepared from aerial parts of the plant. The main volatile compounds were methyl ester of oleic acid, palmitic acid and stearic acid as determined by GC/MS. Phenolic contents of the extracts were determined qualitatively and quantitatively by HPLC/TOF-MS. Six phenolic compounds (syringic acid, morin, gentistic acid, 4-hydroxybenzoic acid, cinnamic acid, and apigenin) were found in the extracts. GC/MS analysis of steam distilled essential oil showed camphor, α-pinene and δ-3-carene as the main constituents. In DPPH radical scavenging assay, the highest free radical scavenging activity was observed for the methanol extract with an IC50 value of 0.48 ± 0.04 mg/mL, whereas, in metal chelating activity on ferrous ions (Fe2+) assay, the highest chelating activity was observed for hexane extract (IC50 = 0.55 ± 0.08 mg/mL). The extracts and essential oil were tested against five severe human pathogenic bacteria using disc diffusion assay and subsequent MIC values were also determined. All the extracts (except methanol extract) and the essential oil were found to possess potential antimicrobial activity with corresponding inhibition zone and minimum inhibitory concentration (MIC) ranging from 9-23 mm and 62.5-500 µg/mL. This study has been explored the plant Lasia spinosa can be seen as a potential source of biologically active compounds.

Chelating Agents/analysis , Free Radical Scavengers , Phenolic Compounds/analysis , Volatile Organic Compounds/analysis , Fatty Acids/analysis
Bol. latinoam. Caribe plantas med. aromát ; 17(6): 566-574, nov. 2018. tab, ilus
Article in English | LILACS | ID: biblio-1007336


The composition of the essential oil obtained by hydrodistillation from Minthostachys mollis Griseb (Lamiaceae) aerial parts was determined by GC and GC/MS. Menthone (13.2%), pulegone (12.4%), cis-dihydrocarvone (9.8%) and carvacrol acetate (8.8%) were the main essential oil components. The cytotoxic activity of the essential oil was in vitro measured using the MTT colorimetric assay. IC50 values were calculated on healthy non-tumor cells (HEK-293) and three human cancer cell lines (T24, DU-145 and MCF-7). In such latter cells, the estimated values were around 0.2 mg/mL. In addition, the antioxidant activity was determined by interaction with the stable free radical 2,2"-diphenyl-1-picrylhydrazyl. The essential oil was almost devoid of antioxidant activity indicating that its anti-proliferative action relies on other unknown mechanism.

La composición del aceite esencial obtenido por hidrodestilación a partir de partes aéreas de Minthostachys mollis Griseb (Lamiaceae) se determinó mediante GC y GC/MS. Mentona (13.2%), pulegona (12.4%), junto con cis-dihidrocarvona (9.8%) y acetato de carvacrol (8.8%) fueron los principales componentes del aceite esencial. La actividad citotóxica del aceite esencial se midió in vitro utilizando el ensayo colorimétrico MTT tanto en células sanas no tumorales (HEK-293) como en tres líneas celulares de cáncer humano (T24, DU-145 y MCF-7). Los valores de IC50 calculados fueron de alrededor de 0.2 mg/mL. Además, se determinó la actividad antioxidante por su interacción con el radical libre 2,2"-difenil-1-picrilhidrazilo. El aceite esencial tiene baja actividad antioxidante, lo que indica que su acción antiproliferativa depende de otro mecanismo desconocido.

Oils, Volatile/pharmacology , Lamiaceae , Cell Line, Tumor/drug effects , Antioxidants/pharmacology , Peru , Picrates , Terpenes/analysis , Biological Assay , Biphenyl Compounds , Calorimetry , Oils, Volatile/chemistry , Cell Survival/drug effects , Free Radical Scavengers , Gas Chromatography-Mass Spectrometry , Antioxidants/chemistry