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1.
Sci Rep ; 13(1): 19550, 2023 11 09.
Artículo en Inglés | MEDLINE | ID: mdl-37945746

RESUMEN

China has became the world's second largest pharmaceutical market, and the number of her registered clinical trials exceeded 3000 in 2021. Although thousands of healthy volunteers are participating in a large number of clinical trials in this country, there is no report about the characteristics, recognition, attitude of Chinese healthy volunteers and their concerns of clinical trials. A questionnaire survey was designed and given to 324 healthy volunteers participating in clinical trials in Wuhan, China. Four important findings emerged from our data. First, young, single and less educated men constituted the majority of Chinese healthy volunteers. Second, differences between the male and female healthy volunteers were observed. Female healthy volunteers are supposed to face more challenges and pressure in life, be more cautious about the clinical trials and more concerned about their health and feelings than the male. Third, no sociodemographic characteristic was associated with poorly understanding of the protocol research content, which was subjectively evaluated. Fourth, more support from society/family and more positive media reports about the participation of healthy volunteers in clinical trials are badly needed. These findings would help us to get a better understanding of Chinese healthy volunteers as a group for protecting them and promoting drug development.


Asunto(s)
Actitud , Emociones , Femenino , Humanos , Masculino , China , Voluntarios Sanos , Encuestas y Cuestionarios , Ensayos Clínicos como Asunto
2.
Clin Pharmacol Drug Dev ; 10(12): 1495-1502, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34288578

RESUMEN

This bioequivalence study was conducted to determine the pharmacokinetics and safety profiles of an originator and a generic avanafil formulation in Chinese male subjects under fed and fasting conditions. Each eligible subject was initially randomly given avanafil (200 mg) in a test-reference or reference-test order, before being switched to another study drug sequence after 7 drug-free days. The bioequivalence of test and reference avanafil were determined if the 90%CIs of the geometric mean ratio (GMR) for the area under plasma concentration-time curve (AUC) from time 0 to infinity (AUC0-∞ ), AUC from time 0 to the last detectable concentration (AUC0-t ), and the maximum plasma concentration (Cmax ) fell within the range 80%-125%. Under fasting/fed conditions, the 90%CIs of GMR for AUC0-∞ , AUC0-t , and Cmax were 98.9% to 109.5%/96.0% to 101.2%, 99.6% to 110.3%/96.6% to 102.4%, and 99.3% to 116.8%/94.3% to 106.7%, respectively, which were all within the 80%-125% range. Adverse events (AEs) occurred in 20.8% of subjects under fasting conditions and 20.7% of subjects under fed conditions, with a severity of grade 1. No significant difference was found in the rate of occurrence of AEs and drug-related AEs in the test and reference-avanafil groups (all P > .05). We concluded that the test and reference avanafil were bioequivalent in healthy Chinese male subjects under fasting and fed conditions.


Asunto(s)
Ayuno , Área Bajo la Curva , China , Estudios Cruzados , Voluntarios Sanos , Humanos , Masculino , Pirimidinas , Comprimidos , Equivalencia Terapéutica
3.
Toxicol Appl Pharmacol ; 411: 115384, 2021 01 15.
Artículo en Inglés | MEDLINE | ID: mdl-33359661

RESUMEN

Benign prostatic hyperplasia (BPH) is an age-related disease in men. Mesenchymal /stromal and epithelial cells interactions are essential to prostate functions. In this study, human nonmalignant prostate epithelial RWPE-1 cells were cocultured with testosterone (TE) -exposed prostate stromal fibroblasts WPMY-1 cells (TE-WPMY-1). The survival rate, epithelial-mesenchymal transition (EMT) and collagen deposition of RWPE-1 were observed. The expression profiles of circRNAs, lncRNAs and mRNAs in WPMY-1-derived exosome-like vesicles (WPMY-1-exo) were explored by high-throughput RNA sequencing. Firstly, both TE-WPMY-1 and TE-WPMY-1-exo significantly promoted RWPE-1 cells proliferation. Secondly, 41 circRNAs, 132 lncRNAs and 1057 mRNAs were differentially expressed (DE) between TE-WPMY-1-exo and the control. Functional enrichment analyses, co-expression analyses and quantitative real-time PCR verification showed that the DE RNAs played important roles in cell proliferation, structure, phenotype and fibrosis. Lastly, blocking WPMY-1-exo biogenesis/release by GW4869 can attenuate TE-WPMY-1-stimulated RWPE-1 cells EMT and collagen deposition. Taken together, our results indicated that WPMY-1-exo modulated the phenotypes changes and collagen deposition of prostate epithelial cells. It provided a novel basis for understanding the underlying mechanisms of RWPE-1 cells EMT and fibrosis induced by WPMY-1 in BPH.


Asunto(s)
Proliferación Celular , Células Epiteliales/metabolismo , Transición Epitelial-Mesenquimal , Exosomas/metabolismo , Comunicación Paracrina , Próstata/metabolismo , Hiperplasia Prostática/metabolismo , Células del Estroma/metabolismo , Línea Celular , Técnicas de Cocultivo , Colágeno/metabolismo , Células Epiteliales/patología , Exosomas/efectos de los fármacos , Exosomas/genética , Exosomas/patología , Fibrosis , Redes Reguladoras de Genes , Humanos , Masculino , Fenotipo , Próstata/efectos de los fármacos , Próstata/patología , Hiperplasia Prostática/genética , Hiperplasia Prostática/patología , ARN Circular/genética , ARN Circular/metabolismo , ARN Largo no Codificante/genética , ARN Largo no Codificante/metabolismo , ARN Mensajero/genética , ARN Mensajero/metabolismo , Células del Estroma/efectos de los fármacos , Células del Estroma/patología , Testosterona/farmacología , Transcriptoma
4.
Int J Antimicrob Agents ; 57(2): 106260, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33309765

RESUMEN

OBJECTIVES: Coronavirus disease 2019 (COVID-19) has become a worldwide pandemic. However, the hazard to newborns in pregnancy remains controversial. The aim of this study was to investigate the vertical transmission of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) from mother to child and developmental toxicity in the fetus. METHODS: All clinical information was recorded on 22 neonates born to mothers with confirmed COVID-19 pneumonia in Tongji Hospital. RESULTS: The average birth weight of the 22 newborns (16 males and 6 females) was 2980 g, and the mean gestational week was 37W+3. The birth weight of three babies was <2500 g, and the gestational week of all three low-birth-weight neonates was less than 36W. Three newborns had minor lesions of infection in the lungs as shown by computed tomography (CT) scans. Furthermore, three newborns had elevated SARS-CoV-2-related immunoglobin M (IgM) antibodies, and 11 newborns (52.4%) had positive immunoglobin G (IgG) antibodies. Notably, both cystatin C and ß2-microglobulin were increased in all newborns. Five of the 21 tested newborns had leukocytosis, and 11 had increased neutrophil levels. In addition, the aspartate aminotransferase of 18 newborns and the γ-glutamyl transpeptidase of 19 newborns were increased. Total bilirubin was elevated in all newborns and serum albumin was reduced in 20 of 22 newborns. CONCLUSIONS: This study was the first to discover that COVID-19 infection in the third trimester of pregnancy could cause fetal kidney developmental injury, as indicated by increased cystatin C and ß2-microglobulin in all neonates. Furthermore, there is the possibility of maternal-fetal transmission of SARS-CoV-2.


Asunto(s)
COVID-19/transmisión , Enfermedades Renales/virología , Complicaciones Infecciosas del Embarazo/virología , Aspartato Aminotransferasas/sangre , Bilirrubina/sangre , COVID-19/etiología , COVID-19/inmunología , Femenino , Humanos , Inmunoglobulina M/sangre , Recién Nacido , Transmisión Vertical de Enfermedad Infecciosa , Enfermedades Renales/embriología , Masculino , Neutrófilos , Embarazo , Complicaciones Infecciosas del Embarazo/etiología , Tercer Trimestre del Embarazo , Estudios Retrospectivos , gamma-Glutamiltransferasa/sangre
5.
Ecotoxicol Environ Saf ; 191: 110202, 2020 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-31945511

RESUMEN

The environmental pollution caused by cigarette smoke (CS) seriously endangers people's health. Epigallocatechin-3-gallate (EGCG) is the most abundant catechin in green tea. In this study, rats were exposed to CS for 90 days. Kidney function was evaluated by detecting the levels of serum creatinine and blood urea nitrogen. Liver function was evaluated by detecting the activities of alanine aminotransferase and aspartate transaminase. The renal and hepatic oxidative stress and inflammation were assessed by detecting the levels of malondialdehyde, reduced glutathione, antioxidant enzymes (superoxide dismutase and glutathione peroxidase) and proinflammatory cytokines. Organ fibrosis was evaluated by observing collagen deposition via masson staining, by examining the hydroxyproline level, by measuring the mRNA levels of fibrosis-associated genes collagen (Col)-1A1 and Col-3A1, as well as by assessing the activity of profibrotic TGF-ß1 pathway. Additionally, renal and hepatic epithelial-mesenchymal transition (EMT) were evaluated. It was observed that EGCG ameliorated the renal and hepatic oxidative stress, inflammation, EMT, as well as inhibited the activation of TGF-ß1 signaling pathway induced by CS. These results showed that EGCG could attenuate CS-induced renal and hepatic fibrosis.


Asunto(s)
Catequina/análogos & derivados , Riñón/efectos de los fármacos , Hígado/efectos de los fármacos , Contaminación por Humo de Tabaco/efectos adversos , Animales , Catequina/farmacología , Transición Epitelial-Mesenquimal/efectos de los fármacos , Fibrosis , Inflamación/inducido químicamente , Riñón/metabolismo , Riñón/patología , Hígado/enzimología , Hígado/patología , Cirrosis Hepática/inducido químicamente , Masculino , Estrés Oxidativo/efectos de los fármacos , Ratas , Factor de Crecimiento Transformador beta1/fisiología
6.
Aging (Albany NY) ; 11(22): 10409-10421, 2019 11 17.
Artículo en Inglés | MEDLINE | ID: mdl-31739286

RESUMEN

Chronic cigarette smoke (CS) exposure induces prostate deficits. We previously found that swertiamarin had prostatic protective potential. This study was to investigate the possible protective effect of swertiamarin against CS-induced prostate dysfunction on human prostate epithelial cells, stromal cells and rats. Rat prostate collagen deposition and fibrosis were assessed by sirius red staining and measuring hydroxyproline content, as well as by qPCR and western blot analysis for fibrotic extracellular matrix components. Prostatic levels of oxidative stress and inflammatory-related factors were also analyzed. In order to explore its underling mechanisms, the activities of Hedgehog signaling pathway and epithelial-mesenchymal transition of human prostate cells and rat prostate tissue were estimated. It was found that swertiamarin ameliorated CS-induced prostatic collagen deposition, relieved oxidative stress and local inflammation, inhibited the activation of Hedgehog signaling pathway and attenuated epithelial-mesenchymal transition. It indicated that swertiamarin could ameliorate CS-induced prostatic fibrosis by inhibiting epithelial-mesenchymal transition and Hedgehog pathway.


Asunto(s)
Glucósidos Iridoides/farmacología , Próstata/efectos de los fármacos , Próstata/patología , Pironas/farmacología , Contaminación por Humo de Tabaco/efectos adversos , Animales , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Línea Celular , Transición Epitelial-Mesenquimal/efectos de los fármacos , Fibrosis/inducido químicamente , Proteínas Hedgehog/metabolismo , Humanos , Masculino , Próstata/metabolismo , Ratas , Ratas Wistar , Productos de Tabaco/efectos adversos
7.
Int Immunopharmacol ; 64: 162-169, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30179845

RESUMEN

Green tea is among the most popular beverages in the world and is an important source of phytoestrogens. Epigallocatechin­3­gallate (EGCG) is the major polyphenol in green tea. The aim of this study was to investigate the anti-benign prostatic hyperplasia (BPH) activity and underling mechanisms of EGCG in testosterone-induced BPH rats and in BPH-1 cells. Prostatic levels of oxidative stress and inflammation makers, as well as angiogenesis related growth factors were measured. Additionally, the prostatic levels of sex hormonal mediators (androgen receptor (AR), estrogen receptor (ER)-α and ER-ß), hypoxia-inducible factor (HIF)-1α, transforming growth factor-ß1 (TGF-ß1), type I TGF-ß receptor (TGF-ßRI), Smad3, phosphorylation-Smad3 (p-Smad3), epithelial-mesenchymal transition (EMT) markers (E-cadherin, collagen-I, fibronectin and α-SMA) and microRNA (miR)-133a/b were analyzed by immunohistochemistry assay, western blot and/or quantitative RT-PCR. It was observed that EGCG attenuated the prostatic oxidative stress and inflammatory microenvironment, ameliorated prostatic hyperplasia and collagen deposition, reduced the levels of angiogenesis related growth factors, inhibited the over-expression of AR, ER-α, HIF-1α, TGF-ß1, TGF-ßRI and p-Smad3, enhanced the expression of ER-ß, increased the levels of miR-133a/b, as well as relieved prostatic EMT in rats. Both HIF-1α inhibitor and EGCG decreased the expression of HIF-1α and TGF-ß1, as well as attenuated EMT in BPH-1 cells. It indicated that EGCG could attenuate testosterone-induced BPH and fibrosis.


Asunto(s)
Catequina/análogos & derivados , Próstata/efectos de los fármacos , Hiperplasia Prostática/tratamiento farmacológico , Testosterona/toxicidad , Animales , Catequina/farmacología , Colágeno/metabolismo , Transición Epitelial-Mesenquimal/efectos de los fármacos , Fibrosis , Masculino , MicroARNs/análisis , Estrés Oxidativo , Próstata/metabolismo , Próstata/patología , Hiperplasia Prostática/inducido químicamente , Hiperplasia Prostática/metabolismo , Ratas , Ratas Wistar , Receptores Androgénicos/análisis , Receptores de Estrógenos/análisis , Proteína smad3/análisis , Factor de Crecimiento Transformador beta1/análisis
8.
Cell Physiol Biochem ; 43(4): 1359-1368, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28992620

RESUMEN

BACKGROUND/AIMS: Cadmium (Cd) is an environmental pollutant with reproductive toxicity. Swertia mileensis is used in Chinese medicine for the treatment of prostatic deficits and named as Qing Ye Dan (QYD). This study was undertaken to investigate the potential protective effects of QYD against Cd-induced prostatic deficits. METHOD: Rat model of prostatic deficits was induced by 0.2 mg/kg/d CdCl2 subcutaneous injection for 15 days. The prostatic oxidative stress was evaluated by detecting the levels of malondialdehyde, nitric oxide, reduced/ oxidized glutathione, total sulfhydryl groups and enzymatic antioxidant status. The prostatic inflammation was estimated by testing the levels of pro-inflammatory cytokines. The levels of epithelial-mesenchymal transition (EMT) markers E-cadherin, fibronectin, vimentin and α-smooth muscle actin were measured by qPCR analysis. Additionally, the prostatic expressions of transforming growth factor-ß1 (TGF-ß1), type I TGF-ß receptor (TGF-ßRI), Smad2, phosphorylation-Smad2 (p-Smad2), Smad3, p-Smad3, Smad7, nuclear related factor-2 (Nrf-2), heme oxygenase-1 (HO-1), B-cell CLL/lymphoma (Bcl)-2 and Bcl-2-associated X protein (Bax) were measured by western blot assay. RESULTS: It was found that QYD ameliorated the Cd-induced prostatic oxidative stress and inflammation, attenuated prostatic EMT, inhibited the TGF-ß1/Smad pathway, increased Bcl-2/Bax ratio and enhanced the activity of Nrf-2/HO-1 pathway. CONCLUSION: These results showed that QYD could ameliorate Cd-induced prostatic deficits via modulating Nrf-2/HO-1 and TGF-ß1/Smad pathways.


Asunto(s)
Cadmio/efectos adversos , Medicamentos Herbarios Chinos/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Próstata/efectos de los fármacos , Enfermedades de la Próstata/inducido químicamente , Enfermedades de la Próstata/tratamiento farmacológico , Transducción de Señal/efectos de los fármacos , Animales , Transición Epitelial-Mesenquimal/efectos de los fármacos , Hemo-Oxigenasa 1/metabolismo , Masculino , Factor 2 Relacionado con NF-E2/metabolismo , Próstata/metabolismo , Próstata/patología , Enfermedades de la Próstata/metabolismo , Enfermedades de la Próstata/patología , Ratas , Ratas Wistar , Proteínas Smad/metabolismo , Factor de Crecimiento Transformador beta1/metabolismo
9.
Biomed Pharmacother ; 91: 707-713, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28499242

RESUMEN

Grape (Vitis vinifera) is consumed as fruit and wine for people. In this study, rat model of prostatic deficits was induced by orally receiving 60mg/L cadmium chlorine (CdCl2) through drinking water for 20 weeks. Grape seed-derived polyphenols extract (GSP) was orally given for 20 weeks. Finally, the prostatic levels of E-cadherin, fibronectin, and α-smooth muscle actin were measured by immunohistochemical and qPCR analysis. The oxidative stress was measured by detecting the levels of malondialdehyde, nitric oxide, reduced glutathione/oxidized glutathione and enzymatic antioxidant status. Additionally, the prostatic expressions of transforming growth factor-ß1 (TGF-ß1), type I TGF-ß receptor (TGF-ßRI), Smad3, phosphorylation-Smad3 (p-Smad3), Smad7, nuclear related factor-2 (Nrf-2), heme oxygenase-1 (HO-1) and γ-glutamate cysteine ligase catalytic subunit (γ-GCLC) were measured by western blot. The levels of microRNA (miR)-133a/b were measured by qPCR. It was observed that GSP ameliorated the prostatic oxidative stress and fibrosis induced by CdCl2. GSP also inhibited the over-generation of TGF-ß1 and p-Smad3, as well as enhanced the levels of Smad7, Nrf-2, HO-1, γ-GCLC and miR-133a/b. These results showed that GSP could attenuate Cd-induced prostatic deficits.


Asunto(s)
Cadmio/toxicidad , Polifenoles/farmacología , Próstata/patología , Semillas/química , Vitis/química , Actinas/metabolismo , Animales , Peso Corporal/efectos de los fármacos , Cadherinas/metabolismo , Colágeno/metabolismo , Transición Epitelial-Mesenquimal/efectos de los fármacos , Fibronectinas/metabolismo , Glutamato-Cisteína Ligasa/metabolismo , Hemo-Oxigenasa 1/metabolismo , Masculino , MicroARNs/metabolismo , Factor 2 Relacionado con NF-E2/metabolismo , Estrés Oxidativo/efectos de los fármacos , Próstata/efectos de los fármacos , Próstata/metabolismo , Proteínas Serina-Treonina Quinasas/metabolismo , Ratas Wistar , Receptor Tipo I de Factor de Crecimiento Transformador beta , Receptores de Factores de Crecimiento Transformadores beta/metabolismo , Proteínas Smad/metabolismo
10.
Behav Brain Res ; 328: 81-86, 2017 06 15.
Artículo en Inglés | MEDLINE | ID: mdl-28411149

RESUMEN

This study was conducted to elucidate the neuroprotective effect of caffeic acid phenethyl ester (CAPE), (R)-2-Hydroxy-3-(3,4-dihydroxyphenyl) propionic acid (Danshensu) and Curcumin, three caffeic acid derivatives which are contained in fruits, grains and certain dietary supplements. Our results showed that these compounds significantly attenuated H2O2-induced toxicity in PC12 cells in a dose-dependent manner. Furthermore, these compounds significantly improved the behavioral performance of d-gal-treated mice in both step-down avoidance test and Morris water maze test. Biochemical examination and western blot analysis showed that these compounds could ameliorate oxidative stress and facilitate activation of the protein kinase A (PKA)-cyclic AMP response element-binding protein (CREB) pathway. Its beneficial effects may partly relate to enhancing the activity of endogenous antioxidant enzymes and modulating the PKA/CREB signaling pathway. Furthermore, our results also indicated that the presence of 3, 4-dihydroxyphenyl groups in A ring may enhance their neuroprotective activity.


Asunto(s)
Ácidos Cafeicos/farmacología , Curcumina/farmacología , Proteína de Unión a Elemento de Respuesta al AMP Cíclico/metabolismo , Proteínas Quinasas Dependientes de AMP Cíclico/metabolismo , Lactatos/farmacología , Fármacos Neuroprotectores/farmacología , Estrés Oxidativo/efectos de los fármacos , Alcohol Feniletílico/análogos & derivados , Animales , Reacción de Prevención/efectos de los fármacos , Reacción de Prevención/fisiología , Ácidos Cafeicos/química , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Curcumina/química , Relación Dosis-Respuesta a Droga , Galactosa , Peróxido de Hidrógeno , Lactatos/química , Aprendizaje por Laberinto/efectos de los fármacos , Aprendizaje por Laberinto/fisiología , Ratones , Fármacos Neuroprotectores/química , Estrés Oxidativo/fisiología , Células PC12 , Alcohol Feniletílico/química , Alcohol Feniletílico/farmacología , Distribución Aleatoria , Ratas , Transducción de Señal/efectos de los fármacos , Memoria Espacial/efectos de los fármacos , Memoria Espacial/fisiología
11.
Pharm Biol ; 2013 Nov 21.
Artículo en Inglés | MEDLINE | ID: mdl-24256126

RESUMEN

Abstract Context: Cyclosorus acuminatus (Houtt.) Nakai (Thelypteridaceae) is used in Chinese traditional medicine for inflammation and pyretic stranguria. Objective: This study investigates the prostatic protective potential of the flavonoid-rich [(2S)-5,7,5'-trihydroxyflavanone glycosides] fraction from C. acuminatus (FCA). Materials and methods: Chronic non-bacterial prostatitis (CNBP) was induced by injecting 20 µl of 1% carrageenan into the rat prostate. Subsequently, FCA (150 or 300 mg/kg/d) was orally given once a day for 4 weeks. Finally, the levels of proinflammatory cytokines and the prostatic expression of peroxisome proliferator activated receptor-γ (PPAR-γ) were evaluated. Results: Treatment with 300 mg/kg/d FCA ameliorated the carrageenan-induced higher prostatic index (PI) state and proinflammatory cytokines levels (NFκB from 2602 ± 588 to 1348 ± 300 pg/ml, TNF-α from 151.6 ± 10.4 to 126.0 ± 3.52 pg/ml, IL-1ß from 153.7 ± 14.8 to 63.9 ± 6.7 pg/ml, COX-2 from 313.3 ± 16.5 to 263.1 ± 15.1 pg/ml, PGE from 1532 ± 130 to 864 ± 126 pg/ml, NOS from 33.7 ± 3.0 to 23.6 ± 1.6 U/mg protein, and NO from 40.3 ± 2.9 to 27.1 ± 2.9 µmol/g protein) as well as regulated the prostatic expression of PPAR-γ (increased about 3.50-fold) when compared to the rat model of prostatitis. Discussion and conclusion: FCA could exert a prostatic protective response via modulating the prostatic expression of PPAR-γ and eventually alleviating the NFκB dependent inflammatory response.

12.
Neurochem Res ; 38(8): 1686-94, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-23670091

RESUMEN

The aim of this study was to investigate the neuroprotective effects of (2S)-5, 2', 5'-trihydroxy-7-methoxyflavanone (TMF), a natural product from Abacopteris penangiana (Hook.) Ching, in oxidative stress-induced neurodegeneration models in vitro and in vivo. In PC12 cells, preincubation of TMF (3-20 µM) for 24 h decreased the dopamine-induced toxicity and attenuated the redox imbalance in PC12 cells through regulating the ratio of reduced glutathione/oxidized glutathione (GSH/GSSG), which is a sensitive marker of oxidative stress. Additionally, long-term intraperitoneal (i.p.) injection of TMF (4 or 8 mg/kg/day) for 2 weeks significantly improved the behavioral performance of D-galactose (D-gal) treated mice in a Morris water maze test. Biochemical analysis revealed that TMF inhibited the activation of AP-1 (activator protein-1) and upregulated the level of BDNF (brain derived neurophic factor) as well as the ratio of GSH/GSSG in the hippocampus of D-gal treated mice. Furthermore, western blotting analysis indicated that TMF increased phosphorylation of cAMP-response element-binding protein (CREB). Therefore, the natural product TMF possessed a potential for the treatment of neurodegenerative diseases.


Asunto(s)
Flavonas/farmacología , Fármacos Neuroprotectores/farmacología , Pteridaceae/química , Animales , Conducta Animal/efectos de los fármacos , Dopamina/metabolismo , Ensayo de Inmunoadsorción Enzimática , Flavonas/aislamiento & purificación , Glutatión/metabolismo , Disulfuro de Glutatión/metabolismo , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Técnicas In Vitro , Aprendizaje por Laberinto/efectos de los fármacos , Ratones , Proteínas del Tejido Nervioso/metabolismo , Fármacos Neuroprotectores/aislamiento & purificación , Células PC12 , Ratas
13.
Food Chem ; 135(4): 2702-7, 2012 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-22980861

RESUMEN

The potential of three natural flavonols (galangin, kaempferol and myricetin) to protect against D-galactose-induced cognitive impairment in mice was investigated. After 8 weeks treatment, the mice were assessed by behavioural tests. The levels of oxidative stress, the amount of Na(+),K(+)-ATPase and extracellular signal-regulated kinases (ERK)-cyclic AMP response element binding protein (CREB) signaling pathway in hippocampus were also analysed. It was found that all the three dietary flavonols could ameliorate the oxidative stress, enhance the activity of Na(+),K(+)-ATPase and regulate the expression of ERK-CREB pathway in mice. However, only kaempferol and myricetin could significantly improve the learning and memory capability when compared with D-galactose model. Our results suggest that the presence of hydroxyl groups in the B ring of flavonols may have contribution to the neuroprotective activity.


Asunto(s)
Trastornos del Conocimiento/tratamiento farmacológico , Trastornos del Conocimiento/metabolismo , Flavonoides/administración & dosificación , Quempferoles/administración & dosificación , Fármacos Neuroprotectores/administración & dosificación , Estrés Oxidativo/efectos de los fármacos , Animales , Conducta Animal/efectos de los fármacos , Trastornos del Conocimiento/inducido químicamente , Trastornos del Conocimiento/psicología , Proteína de Unión a Elemento de Respuesta al AMP Cíclico/genética , Proteína de Unión a Elemento de Respuesta al AMP Cíclico/metabolismo , Quinasas MAP Reguladas por Señal Extracelular/genética , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Galactosa/efectos adversos , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Humanos , Masculino , Ratones , Transducción de Señal/efectos de los fármacos
14.
J Ethnopharmacol ; 139(1): 207-13, 2012 Jan 06.
Artículo en Inglés | MEDLINE | ID: mdl-22101083

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Macrothelypteris torresiana is traditionally used in Chinese folk medicine for the treatment of edema for patients suffering from kidney/bladder problems due to its satisfactory therapeutic effectiveness. AIM OF THE STUDY: The aim of this study was to investigate the renoprotective nature of the total polyphenols fraction from Macrothelypteris torresiana (PMT). MATERIALS AND METHODS: The biochemical criterions of plasma and kidney tissues were evaluated to study the effects of PMT on puromycin aminonucleoside-induced chronic nephrotic syndrome (NS) in hyperlipidemic mice. RESULTS: In this study, the NS and hyperlipidemia were ameliorated after 9 weeks administration of PMT. Besides, PMT was able to modulate the level of renal oxidative stress and vascular endothelial growth factor-nitric oxide (VEGF-NO) pathway. CONCLUSIONS: It represented a potential resource of PMT for the treatment of NS involved in metabolic syndrome.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Helechos , Hiperlipidemias/tratamiento farmacológico , Síndrome Nefrótico/tratamiento farmacológico , Polifenoles/uso terapéutico , Sustancias Protectoras/uso terapéutico , Animales , Glucemia/análisis , Nitrógeno de la Urea Sanguínea , Creatinina/sangre , Dieta Alta en Grasa , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos/farmacología , Hiperlipidemias/etiología , Hiperlipidemias/metabolismo , Riñón/efectos de los fármacos , Riñón/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Lípidos/sangre , Masculino , Ratones , Síndrome Nefrótico/inducido químicamente , Síndrome Nefrótico/metabolismo , Óxido Nítrico/sangre , Óxido Nítrico Sintasa de Tipo II/sangre , Estrés Oxidativo/efectos de los fármacos , Fitoterapia , Polifenoles/farmacología , Dicromato de Potasio , Sustancias Protectoras/farmacología , Puromicina Aminonucleósido , Factor A de Crecimiento Endotelial Vascular/sangre , Factor A de Crecimiento Endotelial Vascular/metabolismo
15.
Food Chem ; 134(4): 1959-66, 2012 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-23442644

RESUMEN

This study was conducted to characterise the flavonoid components of total flavan glycoside from Abacopteris penangiana rhizomes (TFA) and its acid hydrolysate (AHT) through HPLC-DAD-ESI-MS/MS analysis, and to investigate the hypothesis that TFA and AHT exhibit anti-benign prostatic hyperplasia (BPH) potential in castrated rats with testosterone-induced BPH. HPLC-MS/MS analysis indicated that TFA is rich in flavan-4-ol glycosides and AHT mainly contains 3-deoxygenated anthocyanidin. After 4 weeks of administration, TFA and AHT successfully decreased the prostate index and prostate specific antigen plasma concentrations in the rats. Histoarchitectural improvement in the prostate gland was also observed. Reduced dihydrotestosterone, VEGF, bFGF, EGF, and KGF levels were observed both in TFA- and AHT-treated rats. Furthermore, the prostatic expression of Blc-2 was inhibited, whereas that of Bax and p53 was activated by TFA and AHT. In conclusion, TFA and AHT have anti-BPH properties. Hence, plants with flavan glycosides have potential use in the treatment of BPH.


Asunto(s)
Helechos/química , Flavonoides/administración & dosificación , Glicósidos/administración & dosificación , Extractos Vegetales/administración & dosificación , Hiperplasia Prostática/tratamiento farmacológico , Rizoma/química , Animales , Cromatografía Líquida de Alta Presión , Factor de Crecimiento Epidérmico/genética , Factor de Crecimiento Epidérmico/metabolismo , Flavonoides/química , Glicósidos/química , Humanos , Masculino , Espectrometría de Masas , Extractos Vegetales/química , Hiperplasia Prostática/genética , Hiperplasia Prostática/metabolismo , Ratas , Ratas Sprague-Dawley , Factor A de Crecimiento Endotelial Vascular/genética , Factor A de Crecimiento Endotelial Vascular/metabolismo
16.
Food Chem Toxicol ; 49(12): 3206-10, 2011 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-21963953

RESUMEN

This study was to investigate the hypolipidemic and anti-inflammatory properties of Abacopterin A (APA), a flavonoid compound isolated from Abacopteris penangiana (Hook.) Ching. Male C57BL/6J mice were divided randomly and equally into five groups: the normal control group (N), the model group (M), the positive control group (P), the high and low doses of APA treated groups (H and L). All the animals except that in N group were fed with high-fat diet for 8 weeks. In the last 4 weeks, the mice in P, H and L groups were orally administered with simvastatin (at the dose of 20mg/kg/day) and APA (at the dose of 40 or 20mg/kg/day), respectively. Then the lipid profiles and related biochemical criterions of the studied mice were determined. The effects of high-fat diet on activating nuclear transcription factor-κB (NFκB) expression, elevating inflammatory factors tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) levels, and increasing triacylglycerol (TG) and total cholesterol (TC) levels were abolished on daily supplementation with APA. APA also enhanced lipoprotein lipase (LPL) and hepatic lipase (HL) activities. These results suggested that APA had hypolipidemic and anti-inflammatory properties through inhibiting NFκB expression, and reducing inflammatory response.


Asunto(s)
Antocianinas/farmacología , Antiinflamatorios/farmacología , Dieta Alta en Grasa , Glicósidos/farmacología , Hiperlipidemias/tratamiento farmacológico , Hipolipemiantes/farmacología , Extractos Vegetales/farmacología , Animales , Colesterol/sangre , Grasas de la Dieta/administración & dosificación , Helechos/química , Regulación de la Expresión Génica , Hiperlipidemias/inducido químicamente , Interleucina-6/sangre , Lipoproteína Lipasa/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , FN-kappa B/genética , FN-kappa B/metabolismo , Fitoterapia , Triglicéridos/sangre , Factor de Necrosis Tumoral alfa/sangre
17.
J Asian Nat Prod Res ; 13(8): 707-13, 2011 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-21751838

RESUMEN

Two neuropective compounds were isolated from the rhizomes of Abacopteris penangiana, one was a new flavone and the other was a flavanone. Both compounds were firstly separated from natural plant. The isolation work was guided by the antioxidant activity. Both the compounds showed a significant antioxidant activity in vitro and a protective effect on dopamine-induced neurotoxicity in PC12 cells.


Asunto(s)
Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Helechos/química , Flavanonas/aislamiento & purificación , Flavanonas/farmacología , Flavonas/aislamiento & purificación , Flavonas/farmacología , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/farmacología , Animales , Antioxidantes/química , Dopamina/farmacología , Flavanonas/química , Flavonas/química , Estructura Molecular , Fármacos Neuroprotectores/química , Células PC12 , Ratas , Rizoma/química
18.
J Ethnopharmacol ; 136(1): 217-23, 2011 Jun 14.
Artículo en Inglés | MEDLINE | ID: mdl-21549824

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: "Sanxuelian", the rhizome of Abacopteris penangiana (AP), is traditionally used in Chinese medicine for the treatment of blood circulation stasis, hemorheology barriers, edema and inflammation for patients of metabolic syndrome. This study was to investigate the protective effect of the total flavanol glycosides from AP (FAP) on diabetic vascular impairments by measuring the extents of oxidative stress and inflammatory response in mice. MATERIALS AND METHODS: The experimental aortic pathology in diabetic mice was induced by fed on high-fat diet and injected with streptozotocin. The activities of FAP on attenuating aortas injuries, hypoglycemic, hypolipidemic, inhibiting oxidative stress and anti-inflammation were investigated. Additionally, the aortic expressions of nuclear transcription factor-κB (NFκB) were determined by western blot and immunohistochemistry analysis. Furthermore, the effects of FAP on human umbilical vein endothelia cells (HUVECs) were studied. RESULTS: In animal study, the results showed that FAP enhanced the activities of antioxidant enzymes and attenuated the levels of proinflammatory cytokines. The plasma lipid profiles and glucose level in FAP treated groups were significantly decreased along with the vascular impairments were alleviated. Moreover, the aortic expression of NFκB was decreased. In cellular experiment, FAP could inhibit the apoptosis of HUVECs induced by H(2)O(2). CONCLUSIONS: The results indicated that FAP had hypolipidemic, hypoglycemic and vascular protective activities and represented a potential herb for the treatment of aortic pathology involved with metabolic syndrome.


Asunto(s)
Complicaciones de la Diabetes/prevención & control , Helechos/química , Flavonoles/uso terapéutico , FN-kappa B/metabolismo , Estrés Oxidativo/efectos de los fármacos , Fitoterapia , Enfermedades Vasculares/prevención & control , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Aorta/metabolismo , Aorta/patología , Apoptosis/efectos de los fármacos , Glucemia/metabolismo , Citocinas/metabolismo , Complicaciones de la Diabetes/metabolismo , Diabetes Mellitus Experimental/complicaciones , Diabetes Mellitus Experimental/metabolismo , Grasas de la Dieta/efectos adversos , Células Endoteliales/efectos de los fármacos , Células Endoteliales/metabolismo , Flavonoles/farmacología , Glicósidos/farmacología , Glicósidos/uso terapéutico , Humanos , Lípidos/sangre , Masculino , Ratones , Ratones Endogámicos , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Rizoma , Transducción de Señal/efectos de los fármacos , Factores de Transcripción/metabolismo , Venas Umbilicales/citología , Enfermedades Vasculares/etiología , Enfermedades Vasculares/metabolismo
20.
J Ethnopharmacol ; 134(2): 275-80, 2011 Mar 24.
Artículo en Inglés | MEDLINE | ID: mdl-21167928

RESUMEN

AIM OF THE STUDY: Abacopterin E (AE) was isolated from Abacopteris penangiana (Hook.) Ching. This study was to elucidate its neuroprotective effects against hydrogen peroxide (H(2)O(2)) induced oxidative damage in PC12 cells and d-galactose (d-Gal) induced neurotoxicity in mice brain. MATERIALS AND METHODS: In vitro, the protective effect of AE against H(2)O(2)-induced oxidative damage in the PC12 was investigated by the method of MTT (3,(4,5-dimethylthiazole-2-yl)2,5-diphenyl-tetrazolium bromide). In vivo, the protective effect of AE against d-Gal-induced neurotoxicity in mice was studied. The mice in the model group and the AE treatment groups were injected with the d-Gal 150 mg/(kg d) for 7 weeks while the mice in the control group were injected with the same volume of saline (0.9%). From the sixth week, the treatment groups were subcutaneously injected 4 or 8 mg/(kg d) of AE. In order to explore the potential mechanism of AE's action, the mice were assessed by behavioral and electrophysiological tests at the end of the administration. Then the mice brain tissues were measured for the levels of superoxide dismutases (SOD), glutathione peroxidase (GSH-Px), and malondialdehyde (MDA). RESULTS: This study showed that AE lowered the H(2)O(2)-induced cytotoxicity, and AE significantly improved the learning and memory ability in behavioral performance. The biochemical examination revealed that AE restored the activities of SOD and GSH-Px, and attenuated the increase of MDA. Moreover, the electrophysiological analysis evidently showed that AE ameliorated the long-term potentiation (LTP). CONCLUSIONS: These results suggested that AE had neuroprotective effects, and its beneficial effects may be linked with inhibiting the generation of free radical and enhancing the activities of endogenous antioxidant enzymes.


Asunto(s)
Antocianinas/uso terapéutico , Antioxidantes/uso terapéutico , Helechos/química , Glicósidos/uso terapéutico , Memoria/efectos de los fármacos , Síndromes de Neurotoxicidad/tratamiento farmacológico , Estrés Oxidativo/efectos de los fármacos , Fitoterapia , Animales , Antocianinas/aislamiento & purificación , Antocianinas/farmacología , Antioxidantes/metabolismo , Antioxidantes/farmacología , Conducta Animal/efectos de los fármacos , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Modelos Animales de Enfermedad , Galactosa , Glutatión Peroxidasa/metabolismo , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Peróxido de Hidrógeno , Potenciación a Largo Plazo/efectos de los fármacos , Malondialdehído/metabolismo , Ratones , Ratones Endogámicos , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Síndromes de Neurotoxicidad/metabolismo , Células PC12 , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Superóxido Dismutasa/metabolismo
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