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1.
Antiviral Res ; 226: 105889, 2024 06.
Artículo en Inglés | MEDLINE | ID: mdl-38631661

RESUMEN

Hepatitis B virus (HBV) infections pose a major threat to human health. HBV can upregulate the expression of the transcription factor Yin Yang 1 (YY1) in in vitro cytological experiments, suggesting an association between YY1 and HBV infection. However, data on YY1 expression in chronic hepatitis B (CHB) patients are lacking. In this study, we aimed to assess the correlation between YY1 expression and HBV infection. We detected serum YY1 levels in 420 patients with chronic HBV infection, 30 patients with chronic hepatitis C virus infection, and 32 healthy controls using an enzyme-linked immunosorbent assay. The correlation between YY1 levels and clinical parameters was analyzed. Meanwhile, the changes of YY1 before and after interferon or entecavir treatment were analyzed. YY1 levels in the liver tissues were detected using immunofluorescence staining. The expression of YY1 in HBV-expressing cells was detected through western blotting. Meanwhile, we explored the effects of YY1 on HBV replication and gene expression. We found that YY1 was highly expressed in the serum and liver tissues of CHB patients. Serum YY1 levels positively correlated with HBV DNA and hepatitis B surface antigen (HBsAg). Additionally, HBV DNA levels increased but HBsAg levels decreased after HBV-expressing cells overexpress YY1. In conclusion, our study demonstrates that YY1 plays an important role in HBV replication and gene expression, providing a potential target for the treatment of CHB.


Asunto(s)
ADN Viral , Antígenos de Superficie de la Hepatitis B , Virus de la Hepatitis B , Hepatitis B Crónica , Hígado , Replicación Viral , Factor de Transcripción YY1 , Humanos , Factor de Transcripción YY1/metabolismo , Factor de Transcripción YY1/genética , Hepatitis B Crónica/virología , Hepatitis B Crónica/tratamiento farmacológico , Hepatitis B Crónica/metabolismo , Virus de la Hepatitis B/genética , Virus de la Hepatitis B/fisiología , Masculino , Femenino , Adulto , Persona de Mediana Edad , ADN Viral/genética , ADN Viral/sangre , Antígenos de Superficie de la Hepatitis B/sangre , Antígenos de Superficie de la Hepatitis B/metabolismo , Hígado/virología , Hígado/metabolismo , Guanina/análogos & derivados , Antivirales/uso terapéutico , Antivirales/farmacología , Interferones/metabolismo , Células Hep G2
2.
Int J Nanomedicine ; 19: 1557-1570, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38406606

RESUMEN

Purpose: The aim of the present study was to fabricate a Fructus Xanthii and Magnolia liliiflora volatile oils liposomes-loaded thermosensitive in situ gel (gel/LIP/volatile oil) for effectively treating allergic rhinitis via intranasal administration. Patients and Methods: Particle size, polymer dispersity index (PDI), entrapment effectiveness, and cumulative drug permeation of the developed liposomes were assessed. Then, a thermoreversible in situ gel was created using the liposomes loaded with volatile oils of Fructus Xanthii and Magnolia liliiflora. The effectiveness of this treatment for allergic rhinitis was confirmed by evaluating nasal symptoms, and hematological results, after injecting the formulation into the ovalbumin (OVA)-sensitized mice, we conducted hematoxylin-eosin staining (HE) and immunohistochemistry to evaluate the outcomes. The effects of the gel/LIP/volatile oil formulation for nasal delivery of volatile oil in the treatment of rhinitis were then assessed. Results: The average particle size was 95.1 ± 3.6 nm, and the encapsulation efficiencies of Fructus Xanthii and Magnolia liliiflora volatile oils were 70.42 ± 5.41% and 67.10 ± 6.08%, respectively. Drug loadings of Fructus Xanthii and Magnolia liliiflora volatile oils were 9.10 ± 0.98% and 16.10 ± 1.03%, respectively. The binary formulation produced a gel rapidly in the nasal cavity with a strong mucosal adherence at a temperature of delivering volatile oil to the nasal mucosa steadily and continuously. After nasal administration, the gel/LIP/volatile oil sustained the volatile oil delivery into the mucosa. In comparison to the monolithic formulations, the gel/LIP/volatile oil binary formulation exhibited superior performance in terms of drug delivery capability and pharmacodynamic effects. Conclusion: This binary preparation displayed the ability to deliver drugs to the nasal mucosa and exhibited positive pharmacodynamic effects in treating OVA-induced rhinitis in mice. As a result, it has the potential to serve as a delivery platform for Traditional Chinese medicine in the treatment of allergic rhinitis.


Asunto(s)
Medicamentos Herbarios Chinos , Magnolia , Aceites Volátiles , Rinitis Alérgica , Ratones , Animales , Liposomas/uso terapéutico , Aceites Volátiles/uso terapéutico , Rinitis Alérgica/tratamiento farmacológico , Rinitis Alérgica/inducido químicamente , Mucosa Nasal
3.
Food Chem ; 439: 138099, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38039613

RESUMEN

Heating edible oils generates aldehydes, potentially leading to adverse health effects, making their analysis essential for quality control. This study presents a convenient miniaturized kapok fiber-supported liquid-phase extraction/in-situ derivatization method for the simultaneous extraction and derivatization of aldehydes in oils. The method involves placing 150 mg oil into a 1 mL pipette tip packed with 25 mg kapok fiber, adding 150 µL ACN with 1.5 mg mL-1 DNPH, and post 30-minute static extraction, retrieving the extractant with a pipettor for liquid chromatography-tandem mass spectrometry analysis. By optimizing critical parameters through a Box-Behnken design, the method exhibits good linearity (1-500 ng g-1, R2 ≥ 0.991), low detection limits (0.2-1.0 ng g-1), excellent accuracy (95.3-107.1%) and high precisions (relative standard deviation < 7.9%). This method simplifies sample preparation processes, cuts solvent use, and facilitates automation. It effectively identifies ten aldehyde variations in six heated oils, displaying distinct profiles consistent with prior research.


Asunto(s)
Aldehídos , Espectrometría de Masas en Tándem , Espectrometría de Masas en Tándem/métodos , Aldehídos/análisis , Cromatografía Liquida , Extracción Líquido-Líquido/métodos , Aceites de Plantas/química , Cromatografía Líquida de Alta Presión/métodos
4.
Oncol Lett ; 24(3): 304, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35949620

RESUMEN

Cervical cancer is one of the most lethal malignancies of the female reproductive system. Shikonin, a naphthoquinone pigment extracted from the traditional medicinal herb, Lithospermum erythrorhizon, has been demonstrated to exert significant inhibitory effects on a variety of tumours in vitro and in vivo. In the present study, the effects of shikonin on cervical cancer and the underlying mechanisms were investigated. The effects of shikonin on the viability on HeLa and SiHa cervical cancer cells was examined using cell counting kit (CCK-8) and colony formation assays. Immunofluorescence assay was performed to detect the levels of the proliferation-related protein, Ki67. Western blot analysis was utilized to measure the phosphorylated and total expression levels of proteins, including focal adhesion kinase (FAK), AKT, and glycogen synthase kinase 3ß (GSK3ß). Cell migration was determined by using wound healing assay. Metastasis-associated 1 (MTA1), TGFß1 and VEGF mRNA expression levels were determined using reverse transcription-quantitative PCR. It was demonstrated that, shikonin inhibited cervical cancer cell proliferation and migration. The data of the present study revealed that shikonin inhibited the proliferation of HeLa and SiHa cells in a concentration- and time-dependent manner. Mechanistically, shikonin blocked the proliferation of cervical cancer cells by downregulating the phosphorylation of FAK, AKT and GSK3ß induced by EGF. In addition, shikonin significantly suppressed cell migration and reduced the expression of migration-related proteins, including MTA1, TGFß1 and VEGF. On the whole, the present study demonstrates that shikonin may exert an inhibitory effect on the cervical cancer cell proliferation and migration through the FAK/AKT/GSK3ß signaling pathway. These findings suggest that shikonin may function as a potential therapeutic drug for the treatment of cervical cancer.

5.
J Agric Food Chem ; 70(30): 9377-9387, 2022 Aug 03.
Artículo en Inglés | MEDLINE | ID: mdl-35861437

RESUMEN

This study aimed to elucidate the impacts of carrier oil types (long chain triglycerides (LCT), medium chain triglycerides (MCT), and orange oil (indigestible oil)) on the micellization and cellular uptake of ß-carotene (BC) formulated in O/W emulsions, with an emphasis on the role of intestinal transporters. The micellization and cellular uptake of BC in the gastrointestinal tract were evaluated via an in vitro digestion model and a Caco-2 cell monolayer. And the interactions between lipids and intestinal transporters were monitored by nontargeted lipidomics, RT-PCR, and Western blot. The BC micellization rates followed a decreasing trend in emulsions: corn oil (69.47 ± 4.19%) > MCT (22.22 ± 0.89%) > orange oil (11.01 ± 2.86%), whereas the cellular uptake rate of BC was significantly higher in MCT emulsion (56.30 ± 20.13%) than in corn oil emulsion (14.01 ± 1.04%, p < 0.05). The knockdown of SR-B1 led to a 31.63% loss of BC cellular uptake from MCT micelles but had no effect on corn oil micelles. Lipidomics and transporter analysis revealed that TG (10:0/10:0/12:0) and TG (10:0/12:0/12:0) might be the fingerprint lipids that promoted the cellular absorption of BC-MCT micelles via stimulating the mRNA expression of SR-B1.


Asunto(s)
Aceite de Maíz , beta Caroteno , Disponibilidad Biológica , Células CACO-2 , Emulsiones/metabolismo , Humanos , Micelas , Triglicéridos , beta Caroteno/metabolismo
6.
Plant Cell ; 33(8): 2685-2700, 2021 08 31.
Artículo en Inglés | MEDLINE | ID: mdl-34003932

RESUMEN

MEIOSIS ARRESTED AT LEPTOTENE1 (MEL1), a rice (Oryza sativa) Argonaute (AGO) protein, has been reported to function specifically at premeiotic and meiotic stages of germ cell development and is associated with a novel class of germ cell-specific small noncoding RNAs called phased small RNAs (phasiRNAs). MEL1 accumulation is temporally and spatially regulated and is eliminated after meiosis. However, the metabolism and turnover (i.e. the homeostasis) of MEL1 during germ cell development remains unknown. Here, we show that MEL1 is ubiquitinated and subsequently degraded via the proteasome pathway in vivo during late sporogenesis. Abnormal accumulation of MEL1 after meiosis leads to a semi-sterile phenotype. We identified a monocot-specific E3 ligase, XBOS36, a CULLIN RING-box protein, that is responsible for the degradation of MEL1. Ubiquitination at four K residues at the N terminus of MEL1 by XBOS36 induces its degradation. Importantly, inhibition of MEL1 degradation either by XBOS36 knockdown or by MEL1 overexpression prevents the formation of pollen at the microspore stage. Further mechanistic analysis showed that disrupting MEL1 homeostasis in germ cells leads to off-target cleavage of phasiRNA target genes. Our findings thus provide insight into the communication between a monocot-specific E3 ligase and an AGO protein during plant reproductive development.


Asunto(s)
Oryza/fisiología , Proteínas de Plantas/metabolismo , Esporas/crecimiento & desarrollo , Ubiquitina/metabolismo , Proteínas Argonautas/genética , Proteínas Argonautas/metabolismo , Regulación de la Expresión Génica de las Plantas , Lisina/metabolismo , Meiosis , Oryza/genética , Proteínas de Plantas/genética , Plantas Modificadas Genéticamente , Polen/genética , Polen/crecimiento & desarrollo , Complejo de la Endopetidasa Proteasomal/metabolismo , Proteolisis , ARN de Planta/genética , ARN de Planta/metabolismo , ARN Pequeño no Traducido/genética , ARN Pequeño no Traducido/metabolismo , Esporas/genética , Ubiquitina-Proteína Ligasas/genética , Ubiquitina-Proteína Ligasas/metabolismo , Ubiquitinación
7.
Pharmacol Res ; 164: 105406, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-33359913

RESUMEN

It is well known that free fatty acids (FFAs) have beneficial effects on the skeletal system, however, which fatty acid sensing GPCR(s) and how the GPCR(s) regulating cartilage development and osteoarthritis (OA) pathogenesis is largely unknown. In this study, we found Gpr84, a receptor for medium-chain FFAs (MCFA), was the only FFA-sensing GPCR in human and mouse chondrocytes that exhibited elevated expression when stimulated by interleukin (IL)-1ß. Gpr84-deficiency upregulated cartilage catabolic regulator expression and downregulated anabolic factor expression in the IL-1ß-induced cell model and the destabilization of the medial meniscus (DMM)-induced OA mouse model. Gpr84-/- mice exhibited an aggravated OA phenotype characterized by severe cartilage degradation, osteophyte formation and subchondral bone sclerosis. Moreover, activating Gpr84 directly enhanced cartilage extracellular matrix (ECM) generation while knockout of Gpr84 suppressed ECM-related gene expression. Especially, the agonists of GPR84 protected human OA cartilage explants against degeneration by inducing cartilage anabolic factor expression. At the molecular level, GPR84 activation inhibited IL-1ß-induced NF-κB signaling pathway. Furthermore, deletion of Gpr84 had little effect on articular and spine cartilaginous tissues during skeletal growth. Together, all of our results demonstrated that fatty acid sensing GPCR (Gpr84) signaling played a critical role in OA pathogenesis, and activation of GPR84 or MCFA supplementation has potential in preventing the pathogenesis and progression of OA without severe cartilaginous side effect.


Asunto(s)
Osteoartritis/genética , Receptores Acoplados a Proteínas G/genética , Animales , Artralgia/genética , Artralgia/metabolismo , Artralgia/patología , Cartílago/metabolismo , Cartílago/patología , Células Cultivadas , Condrocitos/efectos de los fármacos , Condrocitos/metabolismo , Ácidos Grasos/metabolismo , Homeostasis , Humanos , Interleucina-1beta/farmacología , Articulación de la Rodilla/patología , Masculino , Ratones Endogámicos C57BL , Ratones Noqueados , FN-kappa B/metabolismo , Osteoartritis/metabolismo , Osteoartritis/patología , Receptores Acoplados a Proteínas G/metabolismo , Transducción de Señal , Columna Vertebral/patología , Tibia/patología
8.
J Invest Surg ; 33(10): 950-959, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30885012

RESUMEN

Backgrounds: Enteral immunonutrition (EIN) has received increasing attention, however, evidence on its immunomodulatory and anti-inflammatory function in gastric cancer patients undergoing gastrectomy is poorly investigated. Objectives of this study were to evaluate the effect of EIN on immune function, inflammation response and nutrition status when compared to standard enteral nutrition (SEN). Methods: Totally 124 gastric cancer patients after gastrectomy were randomized to receive early 5-days postoperative EIN (formula enriched with arginine, glutamine, omega-3 fatty acids and nucleotide), or SEN. The primary end-points were CD4+ T-cells, CD3+ T-cells as well as counts of CD4+/CD8+, IgG, IgM, and IgA levels. Second-points included white blood cell (WBC), C-reactive protein (CRP), procalcitonin (PCT), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) levels and nutritional index such as serum albumin, prealbumin, and transferrin concentration. Results: There existed significant difference in primary end-points between EIN group and SEN group. The proportion of CD4+ T-cells, CD3+ T-cells and the counts of CD4+/CD8+, IgG, IgM, and IgA were higher in EIN group eventually. Meanwhile, the level of WBC, CRP and TNF-α were significantly lower in EIN group finally. But there were no other significant differences in nutritional markers between two groups. Conclusion: Early postoperative EIN significantly improves immune function and inflammatory response in gastric cancer patients undergoing gastrectomy.


Asunto(s)
Estado Nutricional , Neoplasias Gástricas , Nutrición Enteral , Gastrectomía , Humanos , Periodo Posoperatorio , Neoplasias Gástricas/cirugía
9.
J Med Chem ; 62(13): 6047-6062, 2019 07 11.
Artículo en Inglés | MEDLINE | ID: mdl-31181158

RESUMEN

We report that compound 13, a novel phosphatidylserine-targeting zinc(II) dipicolylamine drug conjugate, readily triggers a positive feedback therapeutic loop through the in situ generation of phosphatidylserine in the tumor microenvironment. Linker modifications, pharmacokinetics profiling, in vivo antitumor studies, and micro-Western array of treated-tumor tissues were employed to show that this class of conjugates induced regeneration of apoptotic signals, which facilitated subsequent recruitment of the circulating conjugates through the zinc(II) dipicolylamine-phosphatidylserine association and resulted in compounding antitumor efficacy. Compared to the marketed compound 17, compound 13 not only induced regressions in colorectal and pancreatic tumor models, it also exhibited at least 5-fold enhancement in antitumor efficacy with only 40% of the drug employed during treatment, culminating in a >12.5-fold increase in therapeutic potential. Our study discloses a chemically distinct apoptosis-targeting theranostic, with built-in complementary functional moieties between the targeting module and the drug mechanism to expand the arsenal of antitumor therapy.


Asunto(s)
Antineoplásicos/uso terapéutico , Complejos de Coordinación/uso terapéutico , Indolizinas/uso terapéutico , Neoplasias/tratamiento farmacológico , Fosfatidilserinas/metabolismo , Picolinas/uso terapéutico , Animales , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Diseño de Fármacos , Humanos , Indolizinas/síntesis química , Indolizinas/química , Masculino , Ratones Endogámicos ICR , Ratones Desnudos , Estructura Molecular , Picolinas/síntesis química , Picolinas/química , Relación Estructura-Actividad , Inhibidores de Topoisomerasa I/síntesis química , Inhibidores de Topoisomerasa I/química , Inhibidores de Topoisomerasa I/uso terapéutico , Ensayos Antitumor por Modelo de Xenoinjerto , Zinc/química
10.
J Agric Food Chem ; 66(11): 2765-2774, 2018 Mar 21.
Artículo en Inglés | MEDLINE | ID: mdl-29502409

RESUMEN

Rice bran oil (RBO) possesses a plasma cholesterol-lowering activity, while effect of wheat bran oil (WBO) on plasma cholesterol remains unknown. The present study compared the cholesterol-lowering activity of WBO with that of RBO in hamsters. Fifty-four male hamsters were divided into seven groups fed either a noncholesterol diet (NCD) or one of six high-cholesterol diets, namely HCD diet (0.2% cholesterol +9.5% lard), HCD+C diet (0.2% cholesterol +9.5% lard +0.5% cholestyramine), WL diet (0.2% cholesterol +4.8% Lard +4.8% WBO), WH diet (0.2% cholesterol +9.5% WBO), RL diet (0.2% cholesterol +4.8% Lard +4.8% RBO), and RH diet (0.2% cholesterol +9.5% RBO). Plasma total cholesterol (TC) in HCD group was 327.4 ± 31.8 mg/dL, while plasma TC in two WBO and two RBO groups was 242.2 ± 20.8, 243.1 ± 31.7, 257.1 ± 16.3, and 243.4 ± 46.0 mg/dL, respectively, leading to a decrease in plasma TC by 22-26% ( P < 0.01). No significant difference in cholesterol-lowering potency was seen between WBO and RBO. Plasma cholesterol-lowering activity of WBO and RBO was accompanied by down-regulation of hepatic 3-hydroxy-3-methylglutaryl-CoA reductase and fatty acid synthase, while up-regulation of cholesterol-7α-hydroxylase. WL, WH, RL, and RH diets increased the fecal excretion of total neutral sterols by 72.8%, 106.9%, 5.4%, and 36.8% ( P < 0.01) respectively. Results indicated WBO and RBO could inhibit cholesterol absorption via down-regulation of intestinal Niemann-Pick C1 like 1 protein, acyl CoA:cholesterol acyltransferase 2, and ATP binding cassette transporter 5. In summary, WBO was equally effective as RBO in decreasing plasma cholesterol in hypercholesterolemia hamsters.


Asunto(s)
Anticolesterolemiantes/administración & dosificación , Colesterol/sangre , Hipercolesterolemia/dietoterapia , Aceites de Plantas/metabolismo , Aceite de Salvado de Arroz/metabolismo , Animales , Colesterol 7-alfa-Hidroxilasa/metabolismo , Cricetinae , Grasas Insaturadas en la Dieta/metabolismo , Fibras de la Dieta/análisis , Humanos , Hipercolesterolemia/sangre , Hipercolesterolemia/enzimología , Masculino , Esterol O-Aciltransferasa/metabolismo
11.
Exp Gerontol ; 82: 95-103, 2016 09.
Artículo en Inglés | MEDLINE | ID: mdl-27329928

RESUMEN

A high fat diet induces the accumulation of lipid hydroperoxides (LPO), accelerates the ageing process and causes a greater mortality in Drosophila melanogaster. Purple sweet potato is rich in antioxidant anthocyanin. The purpose of the present study was to examine if supplementation of purple sweet potato anthocyanin (PSPA) could reduce the mortality of fruit flies fed a high-fat diet. Results showed that the mean lifespan of fruit flies was shortened from 56 to 35days in a dose-dependent manner when lard in the diet increased from 0% to 20%. PSPA supplementation partially attenuated the lard-induced mortality. The maximum lifespan and 50% survival time were 49 and 27days, respectively, for the 10% lard control flies, in contrast, these parameters increased to 57 and 30days in the PSPA-supplemented fruit flies. Similarly, addition of lard into diet increased the total body LPO, while addition of PSPA partially attenuated its increase. Real-time PCR analysis indicated that PSPA-supplemented diet significantly up-regulated the mRNA of superoxide dismutase (SOD), catalase (CAT) and Rpn11, compared with the control lard diet. The western blot analysis also demonstrated that PSPA supplementation was associated with up-regulation protein mass of SOD1, SOD2, and CAT. In addition, PSPA supplementation could restore the climbing ability of fruit flies fed a 10% lard diet. We could conclude that the lifespan-prolonging activity of PSPA was potentially mediated by modulating the genes of SOD, CAT and Rpn11.


Asunto(s)
Antocianinas/farmacología , Antioxidantes/farmacología , Dieta Alta en Grasa/efectos adversos , Drosophila melanogaster/fisiología , Ipomoea batatas/química , Longevidad/efectos de los fármacos , Animales , Catalasa/genética , Catalasa/metabolismo , Suplementos Dietéticos , Proteínas de Drosophila/genética , Proteínas de Drosophila/metabolismo , Endopeptidasas/genética , Endopeptidasas/metabolismo , Peróxidos Lipídicos/metabolismo , Masculino , Estrés Oxidativo , Paraquat/farmacología , Superóxido Dismutasa-1/genética , Superóxido Dismutasa-1/metabolismo , Regulación hacia Arriba
12.
Atherosclerosis ; 242(1): 77-86, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26184696

RESUMEN

OBJECTIVE: Cholesterol analogs have been used to treat hypercholesterolemia. The present study was to examine the effect of dihydrocholesterol (DC) on plasma total cholesterol (TC) compared with that of ß-sitosterol (SI) in hamsters fed a high cholesterol diet. METHODS AND RESULTS: Forty-five male hamsters were randomly divided into 6 groups, fed either a non-cholesterol diet (NCD) or one of five high-cholesterol diets without addition of DC and SI (HCD) or with addition of 0.2% DC (DA), 0.3% DC (DB), 0.2% SI (SA), and 0.3% SI (SB), respectively, for 6 weeks. Results showed that DC added into diet at a dose of 0.2% could reduce plasma TC by 21%, comparable to that of SI (19%). At a higher dose of 0.3%, DC reduced plasma TC by 15%, less effective than SI (32%). Both DC and SI could increase the excretion of fecal sterols, however, DC was more effective in increasing the excretion of neutral sterols but it was less effective in increasing the excretion of acidic sterols compared with SI. Results on the incorporation of sterols in micellar solutions clearly demonstrated both DC and SI could displace the cholesterol from micelles with the former being more effective than the latter. CONCLUSION: DC was equally effective in reducing plasma cholesterol as SI at a low dose. Plasma TC-lowering activity of DC was mediated by inhibiting the cholesterol absorption and increasing the fecal sterol excretion.


Asunto(s)
Anticolesterolemiantes/uso terapéutico , Colestanol/uso terapéutico , Colesterol/sangre , Hiperlipoproteinemia Tipo II/dietoterapia , Absorción Intestinal/efectos de los fármacos , Tejido Adiposo/efectos de los fármacos , Tejido Adiposo/patología , Alimentación Animal/análisis , Animales , Anticolesterolemiantes/administración & dosificación , Enfermedades de la Aorta/etiología , Enfermedades de la Aorta/patología , Enfermedades de la Aorta/prevención & control , Aterosclerosis/etiología , Aterosclerosis/patología , Aterosclerosis/prevención & control , Ácidos y Sales Biliares/análisis , Colestanol/administración & dosificación , Colesterol en la Dieta/administración & dosificación , Colesterol en la Dieta/farmacocinética , Cricetinae , Evaluación Preclínica de Medicamentos , Heces/química , Perfilación de la Expresión Génica , Hiperlipoproteinemia Tipo II/sangre , Hiperlipoproteinemia Tipo II/complicaciones , Lípidos/sangre , Lipoproteínas/sangre , Hígado/química , Hígado/patología , Masculino , Mesocricetus , Redes y Vías Metabólicas/genética , Micelas , Estructura Molecular , Tamaño de los Órganos/efectos de los fármacos , Placa Aterosclerótica/patología , ARN Mensajero/biosíntesis , Distribución Aleatoria , Sitoesteroles/administración & dosificación , Sitoesteroles/uso terapéutico , Esteroles/análisis , Vísceras/efectos de los fármacos , Vísceras/patología
13.
Exp Gerontol ; 69: 189-95, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26159161

RESUMEN

Cranberry is an excellent source of dietary antioxidants. The present study investigated the effect of cranberry anthocyanin (CrA) extract on the lifespan of fruit flies with focus on its interaction with aging-related genes including superoxide dismutase (SOD), catalase (CAT), methuselah (MTH), insulin receptor (InR), target of rapamycin (TOR), hemipterus (Hep), and phosphoenolpyruvate carboxykinase (PEPCK). Results showed that diet containing 20mg/mL CrA could significantly prolong the mean lifespan of fruit flies by 10% compared with the control diet. This was accompanied by up-regulation of SOD1 and down-regulation of MTH, InR, TOR and PEPCK. The stress resistance test demonstrated that CrA could reduce the mortality rate induced by H2O2 but not by paraquat. It was therefore concluded that the lifespan-prolonging activity of CrA was most likely mediated by modulating the genes of SOD1, MTH, InR, TOR and PEPCK.


Asunto(s)
Antocianinas/farmacología , Proteínas de Drosophila/genética , Expresión Génica/efectos de los fármacos , Longevidad , Estrés Oxidativo/efectos de los fármacos , Vaccinium macrocarpon , Animales , Antioxidantes/farmacología , Regulación hacia Abajo/efectos de los fármacos , Drosophila , Longevidad/efectos de los fármacos , Longevidad/fisiología , Extractos Vegetales/farmacología , Resultado del Tratamiento , Regulación hacia Arriba/efectos de los fármacos
14.
J Agric Food Chem ; 62(43): 10515-21, 2014 Oct 29.
Artículo en Inglés | MEDLINE | ID: mdl-25290252

RESUMEN

The present study investigated the cholesterol-lowering activity of gingerol- and shogaol-enriched ginger extract (GSE). Thirty hamsters were divided into three groups and fed the control diet or one of the two experimental diets containing 0.5 and 1.0% GSE. Plasma total cholesterol, liver cholesterol, and aorta atherosclerotic plaque were dose-dependently decreased with increasing amounts of GSE added into diets. The fecal sterol analysis showed dietary GSE increased the excretion of both neutral and acidic sterols in a dose-dependent manner. GSE down-regulated the mRNA levels of intestinal Niemann-Pick C1-like 1 protein (NPC1L1), acyl CoA:cholesterol acyltransferase 2 (ACAT2), microsomal triacylglycerol transport protein (MTP), and ATP binding cassette transporter 5 (ABCG5), whereas it up-regulated hepatic cholesterol-7α-hydroxylase (CYP7A1). It was concluded that beneficial modification of the lipoprotein profile by dietary GSE was mediated by enhancing excretion of fecal cholesterol and bile acids via up-regulation of hepatic CYP7A1 and down-regulation of mRNA of intestinal NPC1L1, ACAT2, and MTP.


Asunto(s)
Aterosclerosis/tratamiento farmacológico , Catecoles/administración & dosificación , Colesterol/sangre , Antagonistas Colinérgicos/administración & dosificación , Alcoholes Grasos/administración & dosificación , Extractos Vegetales/administración & dosificación , Esteroles/metabolismo , Zingiber officinale/química , Transportadoras de Casetes de Unión a ATP/genética , Transportadoras de Casetes de Unión a ATP/metabolismo , Animales , Aterosclerosis/enzimología , Aterosclerosis/genética , Aterosclerosis/metabolismo , Transporte Biológico , Colesterol 7-alfa-Hidroxilasa/genética , Colesterol 7-alfa-Hidroxilasa/metabolismo , Cricetinae , Humanos , Mucosa Intestinal/metabolismo , Intestinos/enzimología , Hígado/enzimología , Hígado/metabolismo , Masculino , Mesocricetus , Esterol O-Aciltransferasa/genética , Esterol O-Aciltransferasa/metabolismo , Esterol O-Aciltransferasa 2
15.
J Agric Food Chem ; 62(33): 8415-20, 2014 Aug 20.
Artículo en Inglés | MEDLINE | ID: mdl-25078570

RESUMEN

Capsaicinoids exist in chili peppers, whereas capsinoids are present in some sweet peppers. The present study investigated the effects of capsaicinoids and capsinoids on plasma lipids, relaxation of the aorta, atherosclerotic plaque development, and fecal sterol excretion in hamsters fed a high-cholesterol diet. Five groups of male hamsters were given the control diet or one of the four experimental diets containing 1.3 mmol of capsaicinoids (NL), 2.6 mmol of capsaicinoids (NH), 1.3 mmol of capsinoids (OL), or 2.6 mmol of capsinoids (OH), respectively. Results showed capsaicinoids but not capsinoids could decrease plasma total cholesterol (TC), reduce the formation of atherosclerotic plaque, and relax the aortic artery. This was accompanied by a 28-175% increase in fecal excretion of acidic sterols in hamsters fed the diets containing capsaicinoids. Similarly, capsaicinoids but not capsinoids could decrease the pad weights of epididymal and prerenal adipose tissues. It was concluded that capsaicinoids but not capsinoids could favorably modulate plasma lipids and possess beneficial vascular activity.


Asunto(s)
Aterosclerosis/sangre , Capsaicina/farmacología , Capsicum/química , Colesterol/sangre , Extractos Vegetales/farmacología , Animales , Aorta/efectos de los fármacos , Aterosclerosis/tratamiento farmacológico , Capsaicina/análogos & derivados , Capsaicina/química , Sistema Cardiovascular/efectos de los fármacos , Cricetinae , Humanos , Mesocricetus , Extractos Vegetales/química
16.
Biomaterials ; 35(22): 5805-13, 2014 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-24767788

RESUMEN

The synergistic therapy, the combination of photothermal therapy and chemotherapy, has become a potential treatment in the battles with cancer. Here, we developed a synergistic therapy tool that based on CuS nanoparticles-decorated graphene oxide functionalized with polyethylene glycol (PEG-GO/CuS) for cervical cancer treatment. The as-synthesized PEG-GO/CuS nanocomposites with excellent biocompatibility was revealed to have high storage capacity for anticancer drug of doxorubicin (Dox) and high photothermal conversion efficiency, and were effectively employed for the ablation of tumor. In addition, the therapeutic efficacy of Dox-loaded PEG-GO/CuS (PEG-GO/CuS/Dox) nanocomposites was evaluated in vitro and in vivo for cervical cancer therapy. In vitro cell cytotoxicity tests of PEG-GO/CuS/Dox demonstrate about 1.3 and 2.7-fold toxicity than PEG-GO/CuS and free Dox under 5 min irradiation with NIR laser at 1.0 W/cm(2), owing to both PEG-GO/CuS-mediated photothermal ablation and cytotoxicity of light-triggered Dox release. In mouse models, mouse cervical tumor growth was found to be significantly inhibited by the chemo-photothermal effect of PEG-GO/CuS/Dox nanocomposites, resulting in effective tumor reduction. Overall, compared with chemotherapy or photothermal therapy alone, the combined treatment demonstrates better therapeutic efficacy of cancer in vitro and in vivo. These findings highlight the promise of the highly versatile multifunctional nanoparticles in biomedical application.


Asunto(s)
Antibióticos Antineoplásicos/uso terapéutico , Cobre/uso terapéutico , Doxorrubicina/uso terapéutico , Grafito/uso terapéutico , Nanocompuestos/uso terapéutico , Polietilenglicoles/uso terapéutico , Neoplasias del Cuello Uterino/terapia , Animales , Antibióticos Antineoplásicos/administración & dosificación , Cuello del Útero/efectos de los fármacos , Cuello del Útero/patología , Terapia Combinada , Cobre/química , Doxorrubicina/administración & dosificación , Femenino , Grafito/química , Células HeLa , Humanos , Hipertermia Inducida , Ratones , Nanocompuestos/química , Óxidos/química , Óxidos/uso terapéutico , Fototerapia , Polietilenglicoles/química , Neoplasias del Cuello Uterino/patología
17.
Pharm Biol ; 52(5): 539-43, 2014 May.
Artículo en Inglés | MEDLINE | ID: mdl-24236532

RESUMEN

CONTEXT: To this day, there are no reports that marine compounds isolated from microorganisms of the Lianyungang area of China have been used for the treatment of Alzheimer's disease. OBJECTIVE: The present study was to isolate fungi from the sea sediment of the Lianyungang area and screen for acetylcholineseterase inhibition activities of ethyl acetate extracts. MATERIALS AND METHODS: Fungi were isolated from the sea sediment and fermented. After centrifugation, the supernate was extracted with ethyl acetate. The ethyl acetate extract was then fractionated into five fractions. Acetylcholinesterase inhibition activities of the ethyl acetate extracts and five sub-fractions were tested at a concentration of 500 µg/mL with the Ellman's method. RESULTS: Forty-three marine fungi were isolated; 15 extracts inhibited acetylcholinestrease >50% and 3 extracts inhibited the acetylcholinesterase >80% at the concentration of 500 µg/mL. The 3 extracts (L1705, S1101, SH0701) inhibited AChE dose-dependently with IC50 values of 11.3 ± 1.2, 72.1 ± 2.3, and 7.8 ± 2.8 µg/mL, respectively. After the extract of SH0701 was fractionated into five fractions, the ethyl acetate fraction possessed the highest acetylcholinesterase inhibitory activity with an inhibition rate of 71.55% at the concentration of 10 µg/mL. The fungus SH0701 was identified as Aspergillus ochraceus SH0701 according to morphology and molecular identification. DISCUSSION AND CONCLUSION: The present results indicates that some ethyl acetate extracts of marine fungi isolated from Lianyungang area of China could inhibit AChE potently. Therefore, some novel AChE inhibitors might exist in those extracts.


Asunto(s)
Acetilcolinesterasa/metabolismo , Organismos Acuáticos , Inhibidores de la Colinesterasa/farmacología , Hongos , Sedimentos Geológicos/microbiología , Animales , Organismos Acuáticos/química , Organismos Acuáticos/aislamiento & purificación , Encéfalo/enzimología , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Hongos/química , Hongos/aislamiento & purificación , Concentración 50 Inhibidora , Medicina Tradicional China , Conejos
18.
Pharm Biol ; 49(7): 752-5, 2011 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-21639688

RESUMEN

CONTEXT: Helicobacter pylori is a major causative factor in gastritis-like disorders, and urease plays a key role in Helicobacter pylori colonizing and persisting in the mucous layer of the human stomach. In China, a variety of Chinese medicinal herbs have been prescribed to attenuate or eradicate gastritis-like disorders. However, little is known about the urease inhibition of Chinese medicinal herbs. OBJECTIVE: The present study was conducted to investigate the urease inhibition activities of the ethanol and water extracts of 15 Chinese medicinal herbs. MATERIALS AND METHODS: The ethanol and water extracts derived from 15 medicinal herbs, traditionally used for the treatment of gastritis-like disorders in China, were tested for urease-inhibition activity using the phenol red method. RESULTS: Screened at 10 µg/mL, 14 ethanol extracts and 10 water extracts showed urease inhibition. The ethanol extracts of Magnolia officinalis Rehd. et Wils. (Magnoliaceae) and Cassia obtusifolia L. (Leguminosae) possessed inhibition rates higher than 50% with IC50 values of 6.5 and 12.3 µg/mL, respectively. After fractionating successively, the petroleum ether fraction of the ethanol extracts of Magnolia officinalis showed the best activity with 90.8% urease inhibition at a concentration of 10 µg/mL. The bioautography of the petroleum ether fraction indicated the existence of the urease inhibitors in the herb. DISCUSSION AND CONCLUSION: The present results indicated that some Chinese medicinal herbs might treat gastritis-like disorders via the inhibition of Helicobacter pylori urease and the further possibility for discovering useful novel urease inhibitors from the Chinese medicinal herbs.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Inhibidores Enzimáticos/farmacología , Ureasa/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Medicamentos Herbarios Chinos/administración & dosificación , Inhibidores Enzimáticos/administración & dosificación , Etanol/química , Helicobacter pylori/enzimología , Concentración 50 Inhibidora , Solventes/química , Agua/química
19.
J Agric Food Chem ; 58(15): 8604-11, 2010 Aug 11.
Artículo en Inglés | MEDLINE | ID: mdl-20681649

RESUMEN

In this study, the possibility of producing stable O/W emulsions incorporating beta-carotene in oil droplets surrounded by multiple-layer interfacial membranes has been demonstrated. Emulsions were prepared using a two-stage process by homogenization, which relied on the adsorption of chitosan to anionic droplets coated with soybean soluble polysaccharides (SSPS). Results showed that the zeta-potential, particle size, and rheological properties of emulsions were greatly dependent on the chitosan concentration. The electrical charge on the droplets increased from -34 to 58.2 mV as the chitosan concentration was increased from 0 to 2 wt %, which indicated that chitosan adsorbed to the droplet surfaces. The mean particle diameter of the emulsions increased dramatically with the rise of chitosan concentration from 0 to 0.33 wt %, indicating the formation of large aggregated structures. At chitosan concentrations above 0.33 wt %, the mean particle diameter of emulsions decreased and reached a minimum value of 0.79 mum at a chitosan concentration of 0.5 wt %. Dynamic oscillatory shear tests indicated that the viscoelastic behavior could be enhanced by the adsorption of chitosan onto the SSPS-coated droplet surfaces. Chitosan concentration had a significant (p < 0.05) impact on the stability of beta-carotene. The least degradation occurred in the emulsion with chitosan concentration of 0.5%. These results implied that the physicochemical stability of beta-carotene emulsions has been improved by the adsorption of chitosan.


Asunto(s)
Química Farmacéutica , Quitosano/química , Glycine max/química , Extractos Vegetales/química , Polisacáridos/química , beta Caroteno/química , Fenómenos Químicos , Estabilidad de Medicamentos , Emulsiones , Excipientes/química , Reología
20.
Zhonghua Yi Shi Za Zhi ; 36(3): 148-51, 2006 Jul.
Artículo en Chino | MEDLINE | ID: mdl-17278437

RESUMEN

Wenrebing Zhinan Ji (Collection of Guide for Warm Heat Disease) was not a lengthy work, but it had quite a few influences among the medical works of warm heat disease. Regarding the evolvement of the edition and contents of the book, relative records in some authoritative bibliographic tool references had mistakes, errors and defects. The records of the author were complicated and confusing. There were five versions of the book recorded in the Quanguo Zhongyi Tushu Lianhe Mulu (Nationwide Union Catalog of Books of Traditional Chinese Medicine). The study found that there are other versions to be added here, including Wenre Zuiyan (Verbosity of Warm Heat Disease) supplemented to Sanjia Yian Heke (United Collection of Medical Cases of Three Physicians) and Wenre Jingwei (Longitude and Latitude of Warm Heat Diseases) by Wang Mengying, with the xylographic version of Guangxu of the Qing Dynasty excluded. Each version possesses its own special features and values.


Asunto(s)
Libros , Calor , China , Medicina Tradicional China , Médicos
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