Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 374
Filtrar
1.
Fitoterapia ; 149: 104812, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-33359423

RESUMEN

Cucumis bisexualis is a favorite wild fruit with high nutritional and medicinal values because of its bioactive constituents. Four previously undescribed coumarin-homoisoflavonoid derivatives (1-4), together with seven known coumarin and homoisoflavonoid derivatives (5-11) were isolated from the fruits of C. bisexualis for the first time. All the compounds were elucidated by their extensive and comprehensive spectroscopic data and references. Compounds (1-11) were evaluated for their hepatoprotective activities in HepG2 cells by the acetaminophen (APAP)-induced damage model at 10.0 µM with bicyclol as the positive control. Among them, compounds 1, 3, 5, and 6 showed moderately hepatoprotective activities to improve the HepG2 cell survival rates from 51.68 ± 2.49% (APAP, 10 mM) to 71.55 ± 4.08%, 65.95 ± 4.39%, 60.77 ± 3.44%, 62.94 ± 2.30%, respectively.


Asunto(s)
Cumarinas/farmacología , Cucumis/química , Flavonoides/farmacología , Frutas/química , Sustancias Protectoras/farmacología , Acetaminofén/toxicidad , China , Flavonoides/aislamiento & purificación , Células Hep G2 , Humanos , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Sustancias Protectoras/aislamiento & purificación
2.
Molecules ; 25(24)2020 Dec 10.
Artículo en Inglés | MEDLINE | ID: mdl-33321994

RESUMEN

Lycii Fructus is a traditional medicine used to prevent liver and kidney diseases, which commonly derives from Lycium chinense and Lycium barbarum. Here, the extracts and ethyl acetate-soluble fractions of L. chinense fruits exhibited better hepatoprotective effects than those of L. barbarum, which was likely due to differences in their composition. Therefore, GC-MS and HPLC analyses were conducted to characterize the metabolite differences between L. chinense and L. barbarum. Based on amino acid (AA) and phenolic acid (PA) profiling, 24 AAs and 9 PAs were identified in the two species. Moreover, each species exhibited unique and readily distinguishable AA and PA star graphic patterns. HPLC analysis elucidated composition differences between the ethyl acetate-soluble layers of the two compounds. Further, NMR analysis identified their chemical structures as 4-(2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl)butanoic acid and p-coumaric acid. The higher content of 4-(2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl)butanoic acid was detected in L. chinense, whereas the content of p-coumaric acid was higher in L. barbarum. Therefore, the differences in the relative contents of these two secondary metabolites in the ethyl acetate-soluble layer of Lycii Fructus could be a good marker to discriminate between L. chinense and L. barbarum.


Asunto(s)
Hepatocitos/efectos de los fármacos , Lycium/química , Lycium/clasificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Sustancias Protectoras/química , Sustancias Protectoras/farmacología , Aminoácidos , Supervivencia Celular/efectos de los fármacos , Fraccionamiento Químico , Relación Dosis-Respuesta a Droga , Cromatografía de Gases y Espectrometría de Masas , Células Hep G2 , Humanos , Hidroxibenzoatos , Estructura Molecular , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/análisis , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/análisis , Sustancias Protectoras/aislamiento & purificación
3.
PLoS One ; 15(8): e0237086, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32764782

RESUMEN

Paramylon is a novel ß-glucan that is stored by Euglena gracilis Z, which is a unicellular photosynthesizing green alga with characteristics of both animals and plants. Recent studies have indicated that paramylon functions as an immunomodulator or a dietary fiber. Currently, chronic kidney disease (CKD) is a global health problem, and there is no effective preventive treatment for CKD progression. However, paramylon may suppress the progression of CKD via the elimination of uremic toxins or modulation of gut microbiota, leading to the alleviation of inflammation. The aim of this study was to evaluate the effect of paramylon in CKD rat model. Eight-week-old male Wistar rats with a 5/6 nephrectomy were given either a normal diet or a diet containing 5% paramylon for 8 weeks. Proteinuria was measured intermittently. Serum and kidney tissues were harvested after sacrifice. We performed a renal molecular and histopathological investigation, serum metabolome analysis, and gut microbiome analysis. The results showed that paramylon attenuated renal function, glomerulosclerosis, tubulointerstitial injury, and podocyte injury in the CKD rat model. Renal fibrosis, tubulointerstitial inflammatory cell infiltration, and proinflammatory cytokine gene expression levels tended to be suppressed with paramylon treatment. Further, paramylon inhibited the accumulation of uremic toxins, including tricarboxylic acid (TCA) cycle-related metabolites and modulated a part of CKD-related gut microbiota in the CKD rat model. In conclusion, we suggest that paramylon mainly inhibited the absorption of non-microbiota-derived uremic solutes, leading to protect renal injury via anti-inflammatory and anti-fibrotic effects. Paramylon may be a novel compound that can act against CKD progression.


Asunto(s)
Glucanos/farmacología , Riñón/efectos de los fármacos , Sustancias Protectoras/farmacología , Proteinuria/tratamiento farmacológico , Insuficiencia Renal Crónica/tratamiento farmacológico , Administración Oral , Animales , Ciclo del Ácido Cítrico/efectos de los fármacos , Citocinas/metabolismo , Modelos Animales de Enfermedad , Euglena gracilis/química , Microbioma Gastrointestinal/efectos de los fármacos , Microbioma Gastrointestinal/inmunología , Glucanos/aislamiento & purificación , Glucanos/uso terapéutico , Humanos , Mediadores de Inflamación/metabolismo , Absorción Intestinal/efectos de los fármacos , Mucosa Intestinal/efectos de los fármacos , Mucosa Intestinal/metabolismo , Mucosa Intestinal/microbiología , Riñón/inmunología , Riñón/patología , Masculino , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/uso terapéutico , Proteinuria/sangre , Proteinuria/patología , Ratas , Ratas Wistar , Insuficiencia Renal Crónica/sangre , Insuficiencia Renal Crónica/patología , Insuficiencia Renal Crónica/orina , Toxinas Biológicas/sangre , Toxinas Biológicas/metabolismo
4.
Food Chem ; 327: 127059, 2020 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-32447138

RESUMEN

The aim of this study was to purify and identify antioxidant peptides from watermelon seed protein hydrolysates (WSPHs-I: Mw < 1 kDa) and further evaluate their cytoprotective effects against H2O2-induced oxidative stress in HepG2 cells. After purification by Sephadex G-15 and semi-preparative reversed-phase high performance liquid chromatography (RP-HPLC), five peptides, RDPEER (P1), KELEEK (P2), DAAGRLQE (P3), LDDDGRL (P4), and GFAGDDAPRA (P5) were sequenced by LC-MS/MS and synthesized with solid-phase synthesis method. These peptides showed desirable 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging capacity (IC50: 0.216 ± 0.01-0.435 ± 0.03), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity (IC50: 0.54 ± 0.02-1.23 ± 0.03), and oxygen radical absorbance capacity (ORAC) (82.36 ± 1.2-130.67 ± 2.2 µM TE/mg). Among them, peptide P1 exhibited the strongest antioxidant capacity. Moreover, the results suggested that peptide P1 may protect HepG2 cells from H2O2-induced oxidative damage by significantly inhibiting reactive oxygen species (ROS), [Ca2+]i, malondialdehyde (MDA) levels and increasing antioxidative enzyme activities.


Asunto(s)
Citrullus/química , Peróxido de Hidrógeno/farmacología , Estrés Oxidativo/efectos de los fármacos , Péptidos/química , Hidrolisados de Proteína/química , Secuencia de Aminoácidos , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Cromatografía Líquida de Alta Presión , Citrullus/metabolismo , Células Hep G2 , Humanos , Oxidación-Reducción , Péptidos/aislamiento & purificación , Péptidos/farmacología , Proteínas de Plantas/metabolismo , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Especies Reactivas de Oxígeno/metabolismo , Semillas/química , Semillas/metabolismo , Relación Estructura-Actividad , Espectrometría de Masas en Tándem
5.
Ecotoxicol Environ Saf ; 200: 110761, 2020 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-32470682

RESUMEN

Benzo()pyrene [B()P], widely originated from environmental pollution or food process such as roasting and frying, is a strong mutagen and potent carcinogen. Utilization of hawthorn has been reported against physical mutagens. Our study found that hawthorn extract (HE) contained abundant phenolic compounds, wherein chlorogenic acid was 2.78 mg/g, procyanidine B2 was 3.58 mg/g, epicatechin was 2.99 mg/g DW, which may contribute to anti-genotoxicity activity. So, the role of HE against B()P-induced genotoxicity in C57BL/6 mice was further assessed. Fifty mice were distributed into five groups: control group, B()P group (30 mg/kg, i.p.), B()P + HE-L group (100 mg/kg, i.g.), B()P + HE-M group (200 mg/kg, i.g.), B()P + HE-H group (400 mg/kg, i.g.). Mice were orally administered with solutions of HE for 10 days and injected intraperitoneally with B()P for 3 days from the 8th day. Results showed that B()P can induce significantly pathological damage in liver, lung and spleen, as well as decrease white blood cells (WBCs). Remarkably elevated levels of reactive oxygen species (ROS), DNA strand breaks (DSBs) and G1 cell cycle arrest were also found in B()P group, with upregulated expressions of p-H2AX, p-p53 and p21 in bone marrow cells. With administration of HE, liver, lung and spleen injury significantly mitigated, while WBCs were evidently increased in B()P-treated mice. Consistently, HE markedly reduced level of ROS, DSBs and G1 cell cycle arrest accompanied by reducing expressions of p-H2AX, p-p53 and p21 in bone marrow cells. Combined, these results indicated a protective role of HE on B()P-induced genotoxicity.


Asunto(s)
Benzo(a)pireno/toxicidad , Crataegus/química , Daño del ADN/efectos de los fármacos , Mutágenos/toxicidad , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Animales , Células de la Médula Ósea/efectos de los fármacos , Células de la Médula Ósea/metabolismo , Expresión Génica/efectos de los fármacos , Histonas/genética , Leucocitos/efectos de los fármacos , Leucocitos/metabolismo , Hígado/efectos de los fármacos , Hígado/patología , Pulmón/efectos de los fármacos , Pulmón/patología , Masculino , Ratones , Ratones Endogámicos C57BL , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Especies Reactivas de Oxígeno/metabolismo , Bazo/efectos de los fármacos , Bazo/patología , Proteína p53 Supresora de Tumor/genética
6.
Andrologia ; 52(3): e13522, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32012329

RESUMEN

Anabolic androgenic steroids (AAS) such as oxymetholone (OM) used for athletic enhancement, but increased free radicals damage and changes in hormonal levels, lead to serious and irreversible organ damage. Vaccinium arctostaphylos(V. arctostaphylos( has been demonstrated to have antioxidant and antiinflammatory effects. The aim of present study was to investigate V. arctostaphylos effect on OM-induced oxidative injury in mouse testis and sperm parameters. In this experimental study, 30 BALB/c mice were divided into five groups, including healthy, positive control(5 mg/kg OM) and three treatment groups (100, 200 and 400 mg/kg of V. arctostaphylos extract + 5 mg/kg OM). At the end of the study, serum luteinizing hormone (LH), follicle-stimulating hormone (FSH) and testosterone levels were measured. Testis stereological and sperm parameters were calculated. Antioxidant status was measured using nitric oxide (NO) and FRAP assay, and malondialdehyde (MDA) levels. Furthermore, the expression of p53, caspase-3, Bax and Bcl-2 was measured. V. arctostaphylos decreased the serum level of testosterone, increased the LH and FSH, and improved the stereological and sperm parameters and down-regulated the p53, caspase-3 and Bax and up-regulated Bcl-2 genes. Furthermore, this dose decreased serum levels of NO and increased testis FRAP and MDA levels in treated groups compared with OM group. V. arctostaphylos extract has protective effects against testicular toxicity caused by OM.


Asunto(s)
Infertilidad Masculina/prevención & control , Oximetolona/toxicidad , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Testículo/efectos de los fármacos , Vaccinium/química , Animales , Apoptosis/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Modelos Animales de Enfermedad , Etanol/química , Frutas/química , Humanos , Infertilidad Masculina/inducido químicamente , Infertilidad Masculina/patología , Masculino , Ratones , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Recuento de Espermatozoides , Motilidad Espermática/efectos de los fármacos , Testículo/citología , Testículo/patología , Agua/química
7.
Int J Biol Macromol ; 148: 591-600, 2020 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-31958563

RESUMEN

The present work aims to investigate the effects and underlying mechanism of a homogeneous Laminaria japonica polysaccharide (LJP61A) on acute kidney injury (AKI) in mice. According to the results of biochemical and pathological analysis, we concluded that LJP61A could protect kidney from the damage of adriamycin in AKI mice. Compared to the model group, the mRNA level of cytokines (TNF-α, IL-1ß and MCP-1) and protein level of mesenchymal markers demsin were decrease by the treatment of LJP61A while the protein levels of podocyte structure markers (Nephrin and WT-1) were increased. Moreover, the adriamycin-induced enhancement of phosphor-p65, phosphor-p38, phosphor-ERK1/2 and phosphor-JNK in the kidney of AKI mice were significantly suppressed by LJP61A. Similar variation was observed in the mRNA and protein levels of TGF-ß1 and Smad3. These results suggested that LJP61A prevented acute kidney injury possibly via regulating TGF-ß1-mediated Smad3, MAPKs and NF-κB signaling pathways.


Asunto(s)
Lesión Renal Aguda/etiología , Lesión Renal Aguda/prevención & control , Antibióticos Antineoplásicos/efectos adversos , Doxorrubicina/efectos adversos , Laminaria/química , Polisacáridos/farmacología , Sustancias Protectoras/farmacología , Lesión Renal Aguda/metabolismo , Lesión Renal Aguda/patología , Animales , Productos Biológicos/química , Productos Biológicos/aislamiento & purificación , Productos Biológicos/farmacología , Biomarcadores , Biopsia , Citocinas/metabolismo , Modelos Animales de Enfermedad , Inmunohistoquímica , Mediadores de Inflamación , Pruebas de Función Renal , Masculino , Ratones , Estructura Molecular , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
8.
Int J Biol Macromol ; 142: 1-10, 2020 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-31805321

RESUMEN

Corbicula fluminea (Asian clam), a freshwater bivalve mollusk, has been consumed in China for centuries as a health food and traditional Chinese medicine for treating liver diseases and alcoholism. This study aimed to evaluate the hepato-protective effects and potential mechanisms of a proteoglycan (PSP) from C. fluminea on alcohol-induced liver injury in mice. Results showed that PSP pretreatment significantly antagonized the increases in serum alanine aminotransferase, aspartate aminotransferase, triacylglycerides, and hepatic malondialdehyde levels; elevated the antioxidant enzyme activities and hepatic glutathione levels; and suppressed the levels of hepatic inflammatory cytokines in alcohol-induced liver injury in mice (P < 0.05). Histopathological observation further revealed the potential hepato-protective effect of PSP against alcohol damage. Particularly, PSP pretreatment resulted in significantly decreased expression of cytochrome P450 2e1 (CYP2E1) while significantly upregulating the expression of hemeoxygenase-1 (HO-1) (P < 0.05). These results suggested that PSP could protect the liver from hepatocyte injury induced by alcohol possibly by alleviating hepatic lipid metabolism, elevating antioxidant-enzyme activity, suppressing the immune inflammatory response, and reversing the expression levels of CYP2E1 and HO-1. Therefore, PSP may be developed as a food supplement that can be used to prevent liver diseases.


Asunto(s)
Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/tratamiento farmacológico , Corbicula/química , Hígado/efectos de los fármacos , Proteoglicanos/aislamiento & purificación , Proteoglicanos/farmacología , Alanina Transaminasa/sangre , Animales , Antioxidantes , Aspartato Aminotransferasas/sangre , Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/patología , Citocromo P-450 CYP2E1/metabolismo , Citocinas/metabolismo , Modelos Animales de Enfermedad , Etanol/efectos adversos , Glutatión/metabolismo , Hemo-Oxigenasa 1/metabolismo , Hígado/patología , Masculino , Malondialdehído/metabolismo , Medicina China Tradicional , Ratones , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología
9.
J Immunoassay Immunochem ; 41(1): 84-96, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31739724

RESUMEN

Acetaminophen is a common analgesic-antipyretic agent, which is safe in therapeutic doses but in higher doses can produce hepatic necrosis. The aim of this study is to investigate the hepatoprotective effects of artichoke, silymarin, and both agents in acetaminophen-induced liver damage in mice. Forty male mice were divided into five main groups, (1) control (2) Acetaminophen (APAP) (3) Artichoke leaf extracts (ALE) and APAP (4) silymarin and APAP group (5) ALE, silymarin and APAP groups. Blood samples were collected for the measurement of liver enzymes (ALT, AST, and ALP). The liver was excised, weighed and dissected into two parts, one used for measurement of malondialdehyde (MDA) and glutathione reductase, and the other part used for histopathological examination and assessment of proliferative cell nuclear antigen (PCNA) immunohistochemical expression. APAP group showed a significant increase in liver weight, ALT, AST, ALP, MDA, and PCNA expression with a significant decrease in glutathione reductase in comparison to control group. All these parameters were significantly improved in the three treated groups when compared to APAP group. APAP group showed marked portal inflammation and parenchyma necrosis. Co-administration of ALE and/or silymarin to acetaminophen treated mice showed a significant reduction in PCNA expression compared to APAP group. Both ALE and silymarin co-treatment showed a significant decrease in PCNA percentage to a level near to control group. Artichoke and/or silymarin are suggested to protect against acetaminophen-induced hepatotoxicity in mice by ameliorating liver enzymes, antioxidant effect, decreasing liver damage and proliferation.Abbreviation: ALT, alanine transaminase. AST, aspartate transaminase. ALP, alkaline phosphatase.MDA, malondialdehyde. PCNA, proliferative cell nuclear antigen.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Cynara scolymus/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Sustancias Protectoras/farmacología , Silimarina/farmacología , Acetaminofén , Animales , Proliferación Celular/efectos de los fármacos , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Inmunohistoquímica , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Masculino , Ratones , Ratones Endogámicos C57BL , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Silimarina/química
10.
Carbohydr Polym ; 229: 115475, 2020 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-31826430

RESUMEN

The integrity of the intestinal mucosal barrier is important for the health of the host. In this study, longan pulp polysaccharides (LP) prevented the intestinal mucosal injury by increasing the expression of mucin 2, tight junction proteins zonulae occludens-1 (ZO-1), claudin-1, claudin-4, and adherens junction E-cadherin in cyclophosphamide-treated mice. To further identify the principle bioactive component of LP, four acidic polysaccharides (LPIa, LPIIa, LPIIIa, and LPIVa) were purified, and their intestinal protection activity in vitro was compared. LPIa, LPIIa, and LPIIIa displayed an ability to increase mRNA expression of ZO-1, claudin-1, occludin, and E-cadherin in differentiated Caco-2 cells, especially LPIa. LPIa has specific structure characteristics: porous surface structure, a high molecular weight (1.47 × 105 Da), and two specific glycosidic linkages of α-Araf-(1→ and →5)-α-Araf-(1→. These structure characteristics might primarily contribute to greater intestinal barrier protective effect of LPIa.


Asunto(s)
Enfermedades Intestinales/tratamiento farmacológico , Mucosa Intestinal/efectos de los fármacos , Polisacáridos/uso terapéutico , Sustancias Protectoras/uso terapéutico , Sapindaceae/química , Uniones Estrechas/efectos de los fármacos , Uniones Adherentes/efectos de los fármacos , Animales , Células CACO-2 , Ciclofosfamida , Frutas/química , Humanos , Íleon/patología , Enfermedades Intestinales/inducido químicamente , Masculino , Ratones , Ratones Endogámicos BALB C , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Células RAW 264.7 , ARN Mensajero/metabolismo
11.
Biol Pharm Bull ; 43(1): 145-152, 2020 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-31666439

RESUMEN

Schisandra chinensis is widely used and effective in protecting liver. There are many mechanisms of drug-induced hepatocyte injury, among which endoplasmic reticulum (ER) stress-induced cell injury plays an important role. However, little is known about whether schisandra chinensis can inhibit rifampicin (RFP)-induced hepatocyte injury by affecting ER stress. In our study, firstly, L02 cells were treated with different concentrations of RFP for different time intervals, and the apoptosis, survival rate and endoplasmic reticulum stress gene and protein expressions of glucose-regulated protein 78 (GRP 78), PKR-like ER kinase (PERK), activating transcription factor (ATF)4, C/EBP-homologus protein (CHOP), ATF6, arginine-rich, mutated in early stage tumors (ARMET), p-inositol-requiring enzyme 1 (IRE1) and X-box binding protein 1 (XBP-1) were measured. We found that RFP increased apoptosis of L02 cells, decreased cell survival, and increased the gene and protein expression levels of GRP78, PERK, ATF4, CHOP, ATF6, ARMET, p-IRE1 and XBP-1, suggesting that RFP could induce hepatocyte injury, and the degree of injury was positively correlated with the dose and time of RFP. Next, we treated RFP-damaged hepatocytes with schizandrin B. We found that schizandrin B increased cell survival rate in dose-dependent and time-dependent manner, decreased cell apoptosis rate, and reduced protein and gene expression levels of GRP78, PERK, ATF4, CHOP, ATF6, ARMET and XBP-1. These results indicate that schizandrin B alleviates RFP-induced injury in L02 cells by inhibiting ER stress.


Asunto(s)
Apoptosis/efectos de los fármacos , Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/prevención & control , Estrés del Retículo Endoplásmico/efectos de los fármacos , Hepatocitos/efectos de los fármacos , Lignanos/farmacología , Compuestos Policíclicos/farmacología , Sustancias Protectoras/farmacología , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/metabolismo , Ciclooctanos/aislamiento & purificación , Ciclooctanos/farmacología , Relación Dosis-Respuesta a Droga , Estrés del Retículo Endoplásmico/genética , Hepatocitos/metabolismo , Humanos , Lignanos/aislamiento & purificación , Compuestos Policíclicos/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Schisandra/química
12.
J Pharm Pharmacol ; 72(1): 101-110, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31667861

RESUMEN

OBJECTIVES: Combined chemotherapy and radiotherapy usually associated with various comorbidities especially on rapidly proliferating cells as testis. This study aimed to characterize main constituents of Ocimum basilicum L. (OB) aqueous extract and examine its protective effect on doxorubicin/irradiation (DOXO/IR)-induced testicular injury in rats. METHODS: Spectrophotometric analysis showed considerable amount of polyphenolic (146.31 µg/mg) and flavonoid contents (28.63 µg/mg); UPLC-ESI-MS/MS analysis revealed that the major flavonoid was apigenin-O-glucoside (7.53%) followed by luteolin (5.94%), while rosmarinic acid was the major polyphenolic (15.76%) followed by caftaric acid (9.39%); rutin and querctin were also present and were quantified using high-performance liquid chromatography. Administration of OB extract (200 mg/kg per day; p.o.) to DOXO/IR rats resulted in marked improvement of associated testicular damage. KEY FINDINGS: Ocimum basilicum L. significantly decreased testicular levels of nuclear factor-kappa B and B-cell lymphoma-2 (Bcl2)-associated protein X, along with caspase-3 immunohistochemical staining. In addition, OB elevated testicular total antioxidant capacity, nuclear erythroid-related factor-2, Bcl2 and testosterone contents and Ki-67 immunohistochemical staining. Such changes were also accompanied by restoration of testicular architecture. CONCLUSIONS: The study highlights the protective role of OB aqueous extract in hampering most of the harmful chemotherapy/radiotherapy-induced outcomes via its antioxidant, antiapoptotic and cell regeneration abilities. Such findings may offer an incentive in expanding its use during chemotherapy and radiotherapy.


Asunto(s)
Antibióticos Antineoplásicos/toxicidad , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Doxorrubicina/toxicidad , Ocimum basilicum , Estrés Oxidativo/efectos de los fármacos , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Testículo/efectos de los fármacos , Animales , Apoptosis/efectos de la radiación , Proteínas Reguladoras de la Apoptosis/metabolismo , Proliferación Celular/efectos de la radiación , Masculino , FN-kappa B/metabolismo , Ocimum basilicum/química , Estrés Oxidativo/efectos de la radiación , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Ratas Wistar , Transducción de Señal , Testículo/metabolismo , Testículo/patología , Testículo/efectos de la radiación
13.
Drug Chem Toxicol ; 43(3): 240-254, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-30033764

RESUMEN

Biological and chemical agents cause dangerous effects on human health via different exposing ways. Recently, herbal medicine is considered as a biological and safe treatment for toxicities. Silybum marianum (milk thistle), belongs to the Asteraceae family, possesses different effects such as hepatoprotective, cardioprotective, neuroprotective, anti-inflammatory and anti-carcinogenic activities. Several studies have demonstrated that this plant has protective properties against toxic agents. Herein, the protective effects of S. marianum and its main component, silymarin, which is the mixture of flavonolignans including silibinin, silydianin and silychristin acts against different biological (mycotoxins, snake venoms, and bacterial toxins) and chemical (metals, fluoride, pesticides, cardiotoxic, neurotoxic, hepatotoxic, and nephrotoxic agents) poisons have been summarized. This review reveals that main protective effects of milk thistle and its components are attributed to radical scavenging, anti-oxidative, chelating, anti-apoptotic properties, and regulating the inflammatory responses.


Asunto(s)
Antídotos/farmacología , Cardo Lechoso/química , Extractos Vegetales/farmacología , Animales , Antídotos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Quelantes/aislamiento & purificación , Quelantes/farmacología , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Humanos , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología
14.
Nat Prod Res ; 34(10): 1373-1379, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-30445878

RESUMEN

The fresh leaves of Metapanax delavayi (Araliaceae) have been used as a common wild vegetable for salad and soup, and also herbal tea by the local people living in its growing areas of Yunnan province, China. Detailed chemical investigation led to the identification of a new triterpenoid saponin, 3-O-α-L-arabinopyranosyl-28-O-ß-D-glucopyranosyl-(1→6)-O-ß-D-glucopyranosyl-3ß-hydroxyolean-12-ene-28,29-dioic acid (1) from the fresh leaves, together with 11 known compounds, including six triterpenoid saponins (2-7), two caffeoylquinic acid derivatives (8-9), and three flavonoid glycosides (10-12). Their structures were determined on the basis of spectroscopic analysis and acidic hydrolysis. Compounds 3-5 and 8-12 were isolated from M. delavayi for the first time. Moreover, the known saponins 3-O-ß-D-xylopyranosyl-3ß-hydroxyolean-12-ene-28,29-dioic acid (3) and yiyeliangwanoside IV (5) exhibited protective effects on HepG2 cells damaged by the alcohol intakes, at a concentration of 1.0 µg/mL. The results indicated M. delavayi is an ideal dietary vegetable and herbal tea with potential hepatoprotective activity.[Formula: see text].


Asunto(s)
Araliaceae/química , Hojas de la Planta/química , Sustancias Protectoras/aislamiento & purificación , Saponinas/aislamiento & purificación , Triterpenos/aislamiento & purificación , China , Glicósidos/análisis , Células Hep G2/efectos de los fármacos , Humanos , Estructura Molecular , Extractos Vegetales/química , Sustancias Protectoras/química , Sustancias Protectoras/farmacología , Saponinas/química , Saponinas/farmacología , Triterpenos/análisis , Triterpenos/química , Triterpenos/farmacología
15.
Nat Prod Res ; 34(17): 2528-2532, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-30623721

RESUMEN

Copaifera langsdorffii L. is one of the most known medicinal species in Brazil. Its leaves are rich in phenolic compounds with potential biological activities as an antioxidant and chelating agent. This paper reports the isolation of four compounds from the hydroalcoholic extract of the leaves of C. langsdorffii and the investigation of their possible cytoprotective effects against heavy metal poisoning. Quercitrin (1), afzelin (2), 3,5-di-O-(3-O-methyl galloyl) quinic acid (3) and 4,5-di-O-(3-O-methyl galloyl) quinic acid (4), were associated with toxic doses of methylmercury and lead and evaluated by Alamar blue cell viability assays in HepG2 and PC12. The compounds displayed significant cytoprotective effect for the HepG2 cell line against both metals. Compounds 1-4 did not protect PC12 cells against methylmercury induced-cytotoxicity, but at lower concentrations, they protected against lead induced-cytotoxicity. The evaluated compounds showed a promising cytoprotection effect against exposure to heavy metals and should be further investigated as protective agents.


Asunto(s)
Fabaceae/química , Intoxicación por Metales Pesados/tratamiento farmacológico , Compuestos de Metilmercurio/antagonistas & inhibidores , Extractos Vegetales/farmacología , Sustancias Protectoras/aislamiento & purificación , Animales , Antioxidantes , Brasil , Línea Celular , Intoxicación por Metales Pesados/prevención & control , Humanos , Plomo/toxicidad , Intoxicación por Plomo/tratamiento farmacológico , Intoxicación por Plomo/prevención & control , Manósidos , Intoxicación por Mercurio/tratamiento farmacológico , Intoxicación por Mercurio/prevención & control , Compuestos de Metilmercurio/toxicidad , Fenoles , Hojas de la Planta/química , Proantocianidinas , Sustancias Protectoras/farmacología , Quercetina/análogos & derivados , Ácido Quínico , Ratas
16.
Planta Med ; 86(1): 32-44, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31689719

RESUMEN

Gastric ulcer is a major health problem. Current treatment options of gastric ulcer, including antagonists of histamine H2 receptor and inhibitors of the proton pump, do not cure gastric ulcers, but only provide temporary relief of symptoms and can be associated with severe side effects. The lack of effective and safe medications for this global health problem urges for the discovery of novel classes of compounds with potent activity and an acceptable safety profile. Ethanol-induced ulceration in rats was used to evaluate the gastroprotective activity of casuarinin, an ellagitannin isolated from Melaleuca leucadendra. Casuarinin (25, 50, and 100 mg/kg) reduced the ulcer area by 45, 78, and 99%, respectively, compared with the ulcer group. Casuarinin (100 mg/kg) increased mucin content by 1.8-fold and reduced acidity by 42%. At the same dose, it also increased the levels of reduced glutathione by 194%, catalase by 586%, and prostaglandin E2 to its normal level. In contrast, it attenuated the ethanol-increased levels of malondialdehyde by 56%, TNF-α by 58%, and caspase-3 by 87%. Histological findings demonstrated that casuarinin exhibited a protective effect against tissue alterations in response to the ethanol-induced ulcer. Casuarinin suppressed the immunoexpression of nuclear factor-kappa B, cyclooxygenase-2, and inducible nitric oxide synthase to their normal values. It also induced the expression of heat shock protein-70, reaching up to 4.9-fold in comparison with the ulcer group. The potent gastroprotective effect of casuarinin was thus attributed to its anti-inflammatory, antioxidant, and antiapoptotic effects. Our results suggest the potential application of casuarinin as an antiulcer agent from natural sources.


Asunto(s)
Antiulcerosos/aislamiento & purificación , Taninos Hidrolizables/uso terapéutico , Melaleuca/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Animales , Antiulcerosos/farmacología , Ciclooxigenasa 2/metabolismo , Etanol , Proteínas HSP70 de Choque Térmico/metabolismo , Taninos Hidrolizables/química , Taninos Hidrolizables/aislamiento & purificación , Masculino , Estructura Molecular , Mucinas/metabolismo , FN-kappa B/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Ratas , Ratas Sprague-Dawley , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/patología
17.
Recent Pat Drug Deliv Formul ; 13(4): 310-322, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31849292

RESUMEN

BACKGROUND: Excessive blue light light-emitting diode (LED) exposure and consequent oxidative stress causes corneal damage and corneal injuries are the major problem arising these days due to excessive use of mobile phone, TV, environment pollution, etc. Objective: In the present investigation, the protectiveness of carboxymethyl Terminalia catappa (CTC) from blue light LED-induced corneal damage was explored. METHODS: For this purpose, Terminalia catappa (TC) was functionalized by carboxymethylation and its structural modification was confirmed by spectral attributes. Further, the CTC protective eye drop formulations (0.025-1%, w/v) were prepared and evaluated for their capability of protection from blue light LEDinduced corneal damage as compared to CTC protective eye gel (1.25-7%, w/v). The findings pointed towards excellent protection of CTC gel formulations as compared to CTC eye drop formulations. In addition, the prepared optimized CTC gel had thixotropic behavior as evident from percentage structural recovery which was 1.75 fold higher than marketed formulation (I-Comfort, HPMC 2%, w/v). The safety and non-toxicity of CTC protective eye drop and gel were confirmed by HET-CAM test. Further, a rat eye model was implemented that mimic blue light light-emitting diode induced corneal damage in day to day life to assess the protective effect of CTC protective eye drop and gel. RESULTS: The order of protectiveness of CTC formulations was found to be CTC protective eye gel (4%, w/v) (no corneal damage)>marketed eye gel (12.34% corneal damage)=CTC protective eye drop (0.75%, w/v) (17.48% corneal damage)> marketed eye drop (51% corneal damage). The mechanism behind the protective effect of CTC eye drop and gel was associated with good free radical scavenging activity and corneal adhesive property of CTC. It is established from the present work that, carboxymethyl Terminalia catappa has protective action against blue light light-emitting diode induced corneal damage.


Asunto(s)
Lesiones de la Cornea/prevención & control , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Terminalia/química , Administración Oftálmica , Animales , Lesiones de la Cornea/etiología , Relación Dosis-Respuesta a Droga , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Luz/efectos adversos , Soluciones Oftálmicas , Estrés Oxidativo/efectos de los fármacos , Polisacáridos/química , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/farmacología , Ratas
18.
Int J Mol Sci ; 20(23)2019 Nov 30.
Artículo en Inglés | MEDLINE | ID: mdl-31801293

RESUMEN

The gastric secretory trefoil factor family (TFF) peptides xP1 and xP4 are the Xenopus laevis orthologs of mammalian TFF1 and TFF2, respectively. The aim of this study was to analyze the molecular forms of xP1 and xP4 in the X. laevis gastric mucosa by FPLC. xP1 mainly occurred in a monomeric low-molecular-mass form and only a minor subset is associated with the mucus fraction. The occurrence of monomeric xP1 is unexpected because of its odd number of cysteine residues. Probably a conserved acidic residue flanking Cys55 allows monomeric secretion. Furthermore, Cys55 is probably post-translationally modified. For the first time, we hypothesize that the free thiol of monomeric xP1-and probably also its mammalian ortholog TFF1-could have a protective scavenger function, e.g., for reactive oxygen/nitrogen species. In contrast, xP4 mainly occurs in a high-molecular-mass form and is non-covalently bound to a mucin similarly as TFF2. In vitro binding studies with radioactively labeled porcine TFF2 even showed binding to X. laevis gastric mucin. Thus, xP4 is expected to bind as a lectin to an evolutionary conserved sugar epitope of the X. laevis ortholog of mucin MUC6 creating a tight mucus barrier. Taken together, xP1 and xP4 appear to have different gastric protective functions.


Asunto(s)
Proteínas Anfibias/química , Depuradores de Radicales Libres/química , Mucosa Gástrica/metabolismo , Sustancias Protectoras/química , Procesamiento Proteico-Postraduccional , Factor Trefoil-1/química , Proteínas Anfibias/aislamiento & purificación , Proteínas Anfibias/metabolismo , Proteínas Anfibias/farmacología , Animales , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/metabolismo , Depuradores de Radicales Libres/farmacología , Peso Molecular , Mucinas/química , Mucinas/metabolismo , Sustancias Protectoras/aislamiento & purificación , Sustancias Protectoras/metabolismo , Sustancias Protectoras/farmacología , Unión Proteica , Isoformas de Proteínas/química , Isoformas de Proteínas/aislamiento & purificación , Isoformas de Proteínas/metabolismo , Isoformas de Proteínas/farmacología , Especies de Nitrógeno Reactivo/antagonistas & inhibidores , Especies de Nitrógeno Reactivo/metabolismo , Especies Reactivas de Oxígeno/antagonistas & inhibidores , Especies Reactivas de Oxígeno/metabolismo , Porcinos , Factor Trefoil-1/aislamiento & purificación , Factor Trefoil-1/metabolismo , Factor Trefoil-1/farmacología , Xenopus laevis/fisiología
19.
Molecules ; 24(24)2019 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-31861213

RESUMEN

Cisplatin is a platinum-based anticancer agent used for treating a wide range of solid cancers. One of the side effects of this drug is its severe nephrotoxicity, limiting the safe dose of cisplatin. Therefore, many natural products have been studied and applied to attenuate the toxicity of this compound. In this study, we found that steamed Vietnamese ginseng (Panax vietnamensis) could significantly reduce the kidney damage of cisplatin in an in vitro model using porcine proximal tubular LLC-PK1 kidney cells. From processed ginseng under optimized conditions (120 °C, 12 h), we isolated seven compounds (20(R,S)-ginsenoside Rh2, 20(R,S)-ginsenoside Rg3, ginsenoside Rk1, ginsenoside-Rg5, and ocotillol genin) that showed kidney-protective potential against cisplatin toxicity. By comparing the 50% recovery concentration (RC50), the R form of ginsenoside, Rh2 and Rg3, had RC50 values of 6.67 ± 0.42 µM and 8.39 ± 0.3 µM, respectively, while the S forms of ginsenoside, Rh2 and Rg3, and Rk1, had weaker protective effects, with RC50 ranging from 46.15 to 88.4 µM. G-Rg5 and ocotillol, the typical saponin of Vietnamese ginseng, had the highest RC50 (180.83 ± 33.27; 226.19 ± 66.16, respectively). Our results suggest that processed Vietnamese gingseng (PVG), as well as those compounds, has the potential to improve kidney damage due to cisplatin toxicity.


Asunto(s)
Antineoplásicos/farmacología , Cisplatino/farmacología , Riñón/efectos de los fármacos , Panax/química , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Fraccionamiento Químico/métodos , Relación Dosis-Respuesta a Droga , Concentración 50 Inhibidora , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación
20.
Biomolecules ; 9(12)2019 12 17.
Artículo en Inglés | MEDLINE | ID: mdl-31861234

RESUMEN

Polyacetylenic compounds isolated from Panax species are comprised of non-polar C17 compounds, exhibiting anti-inflammatory, antitumor, and antifungal activities. Panaxynol represents the major component of the essential oils of ginseng. We investigated whether panaxynol isolated from Panax vietnamensis (Vietnamese ginseng, VG) could prevent cisplatin-induced renal damage induced in vitro and in vivo. Cisplatin-induced apoptotic cell death was observed by staining with annexin V conjugated with Alexa Fluor 488, and western blotting evaluated the molecular mechanism. Panaxynol at concentrations above 0.25 µM prevented cisplatin-induced LLC-PK1 porcine renal proximal tubular cell death. LLC-PK1 cells treated with cisplatin demonstrated an increase in apoptotic cell death, whereas pretreatment with 2 and 4 µM panaxynol decreased this effect. Cisplatin demonstrated a marked increase in the phosphorylation of c-Jun N-terminal kinase (JNK), P38, and cleaved caspase-3. However, pretreatment with 2 and 4 µM panaxynol reversed the upregulated phosphorylation of JNK, P38, and the expression of cleaved caspase-3. We confirmed that the protective effect of panaxynol isolated from P. vietnamensis in LLC-PK1 cells was at least partially mediated by reducing the cisplatin-induced apoptotic damage. In the animal study, panaxynol treatment ameliorated body weight loss and blood renal function markers and downregulated the mRNA expression of inflammatory mediators.


Asunto(s)
Lesión Renal Aguda/tratamiento farmacológico , Cisplatino/farmacología , Diinos/farmacología , Alcoholes Grasos/farmacología , Túbulos Renales Proximales/efectos de los fármacos , Panax/química , Sustancias Protectoras/farmacología , Lesión Renal Aguda/inducido químicamente , Animales , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Nitrógeno de la Urea Sanguínea , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Creatinina/sangre , Diinos/química , Diinos/aislamiento & purificación , Alcoholes Grasos/química , Alcoholes Grasos/aislamiento & purificación , Túbulos Renales Proximales/patología , Masculino , Ratones , Ratones Endogámicos C57BL , Sustancias Protectoras/química , Sustancias Protectoras/aislamiento & purificación , Porcinos
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...