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1.
Surg Today ; 52(1): 151-164, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34120243

RESUMEN

PURPOSE: The specific genes or pathways in fibroblasts responsible for the pathogenesis of postoperative abdominal adhesion (PAA) remain to be elucidated. We aim to provide a new insight into disease mechanisms at the transcriptome level. METHODS: Male Sprague-Dawley rats were used to establish a PAA model. Primary fibroblasts were separated from normal peritoneal tissue (NF) and postoperative adhesion tissue (PF). RNA sequencing was used to analyze the transcriptome in NF and PF. RESULTS: One thousand two hundred thirty-five upregulated and 625 downregulated DEGs were identified through RNA-Seq. A pathway enrichment analysis identified distinct enriched biological processes, among which the most prominent was related to immune and inflammatory response and fibrosis. HE staining and Masson's trichrome staining histologically validated the RNA-Seq results. Six hub genes, ITGAM, IL-1ß, TNF, IGF1, CSF1R and EGFR were further verified by RT-PCR. CONCLUSIONS: Our study revealed the roles of the immune and inflammatory responses and fibrosis in the process of PAA. We also found six hub genes that may be potential therapeutic targets for PPA.


Asunto(s)
Fibroblastos , Peritoneo/patología , Complicaciones Posoperatorias/genética , Complicaciones Posoperatorias/patología , Análisis de Secuencia de ARN/métodos , Adherencias Tisulares/genética , Adherencias Tisulares/patología , Transcriptoma/genética , Animales , Antígeno CD11b , Modelos Animales de Enfermedad , Receptores ErbB , Fibroblastos/inmunología , Fibroblastos/patología , Humanos , Factor I del Crecimiento Similar a la Insulina , Interleucina-1beta , Masculino , Terapia Molecular Dirigida , Complicaciones Posoperatorias/inmunología , Complicaciones Posoperatorias/terapia , Ratas Sprague-Dawley , Receptores de Factor Estimulante de Colonias de Granulocitos y Macrófagos , Adherencias Tisulares/inmunología , Adherencias Tisulares/terapia , Factor de Necrosis Tumoral alfa
2.
Molecules ; 22(4)2017 Apr 03.
Artículo en Inglés | MEDLINE | ID: mdl-28368360

RESUMEN

A new triflavanoid, kandelin B-5 (1), was isolated from the rhizomes of Smilax china L., together with six known phenylpropanoid substituted flavan-3-ols (2-7), nine flavonoids (8-16), two stilbenoids (17, 18), and two other compounds (19, 20). The structure of compound 1 was determined on the basis of 1D, 2D NMR and HR-ESI-MS data, as well as chemical method. Compounds 2-5, 8-12, 15, 17, and 19 were evaluated for anti-inflammatory activity. Only compounds 10, 15 and 17 showed slightly IL-1ß expression inhibitory activities on LPS induced THP-1 cells, with inhibition rate of 15.8%, 37.3%, and 35.8%, respectively, at concentration of 50 µg/mL.


Asunto(s)
Antiinflamatorios/farmacología , Flavonoides/farmacología , Extractos Vegetales/farmacología , Rizoma/química , Smilax/química , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Línea Celular , Citocinas/biosíntesis , Flavonoides/química , Flavonoides/aislamiento & purificación , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación
3.
Planta Med ; 81(14): 1255-62, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26252831

RESUMEN

Yiru Tiaojing Granule, a traditional Chinese medicine formula, is used to treat hyperprolactinemia. This study was conducted to evaluate the mechanism of action and pharmacological activity of Yiru Tiaojing Granule on prolactin secretion. The animal model of hyperprolactinemia was induced by metoclopramide. The dopamine D2 receptor in hyperprolactinemia rat models was analyzed by immunohistochemistry. The biochemical parameters, including a follicle-stimulating hormone, luteinizing hormone, estradiol, progesterone, testosterone, and prolactin, were measured by an enzyme-linked immunosorbent assay. Furthermore, the expression of prolactin and the dopamine D2 receptor was analyzed by Western blotting. The components in the Yiru Tiaojing Granule-medicated serum were assayed by liquid chromatography-tandem mass spectrometry. The Yiru Tiaojing Granule significantly decreased the prolactin level in the hyperprolactinemia rat model, and increased the estradiol, luteinizing hormone, and progesterone levels. The high and medium doses of Yiru Tiaojing Granule reduced dopamine D2 receptor expression in the brain (p < 0.001) and produced a similar effect on bromocriptine (p < 0.001). Yiru Tiaojing Granule-medicated serum reduced (p < 0.001) prolactin expression in MMQ cells in a concentration-dependent manner, but had no effects on GH3 cells. The level of the dopamine D2 receptor in MMQ cells was also increased dose-dependently (p < 0.05). In addition, the protein kinase A and cyclic adenosine monophosphate in MMQ cells were significantly attenuated dose-dependently by treatment with a high and medium dose of Yiru Tiaojing Granule-medicated serum (p < 0.05) and bromocriptine-medicated serum (p < 0.01). The results suggested that Yiru Tiaojing Granule was effective against hyperprolactinemia, and the activation of the dopamine D2 receptor, which was related to the second messenger cyclic adenosine monophosphate and protein kinase A, might be the potential mechanism.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Hiperprolactinemia/tratamiento farmacológico , Animales , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Bromocriptina/farmacología , Línea Celular/efectos de los fármacos , AMP Cíclico/metabolismo , Proteínas Quinasas Dependientes de AMP Cíclico/metabolismo , Modelos Animales de Enfermedad , Antagonistas de Dopamina/farmacología , Relación Dosis-Respuesta a Droga , Medicamentos Herbarios Chinos/administración & dosificación , Femenino , Haloperidol/farmacología , Hiperprolactinemia/metabolismo , Medicina Tradicional China/métodos , Progesterona/sangre , Prolactina/sangre , Ratas Sprague-Dawley , Receptores de Dopamina D2/metabolismo
4.
Planta Med ; 80(12): 969-73, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25089738

RESUMEN

Postoperative adhesions develop after nearly every abdominal surgery. The formation of adhesions is associated with the inflammatory response, fibrinolytic system, and extracellular matrix deposition in response to injury. Tanshinone IIA is one of the major extracts obtained from Salvia miltiorrhiza, which has anti-inflammatory effects on many diseases. Postoperative adhesions were induced by injuring the parietal peritoneum and cecum in Wistar rats, followed by the administration of various dosages of tanshinone IIA. The adhesion scores for each group were collected seven days after the initial laparotomy. The activity of the tissue-type plasminogen activator in the peritoneal lavage fluid was measured. The messenger ribonucleic acid expression levels of the tissue-type plasminogen activator, plasminogen activator inhibitor-1, and cyclooxygenase-2 in the ischaemic tissues were measured by quantitative real-time polymerase chain reaction. The intraperitoneal administration of tanshinone IIA is effective for the prevention of the formation of postoperative adhesions in rats. Tanshinone IIA increased fibrinolytic activity in the peritoneal lavage fluid and tissue-type plasminogen activator messenger ribonucleic acid expression in ischaemic peritoneal tissues but decreased the plasminogen activator inhibitor and cyclooxygenase-2 messenger ribonucleic acid expression significantly. These results revealed that tanshinone IIA was a potent postoperative adhesion preventer by enhancing fibrinolytic activity and decreasing cyclooxygenase-2 activity.


Asunto(s)
Abietanos/uso terapéutico , Inhibidores de la Ciclooxigenasa/uso terapéutico , Fibrinolíticos/uso terapéutico , Peritoneo/patología , Fitoterapia , Complicaciones Posoperatorias/prevención & control , Adherencias Tisulares/prevención & control , Abietanos/farmacología , Animales , Ciego/patología , Ciclooxigenasa 2/genética , Ciclooxigenasa 2/metabolismo , Inhibidores de la Ciclooxigenasa/farmacología , Fibrinolíticos/farmacología , Inyecciones Intraperitoneales , Masculino , Peritoneo/cirugía , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Inactivadores Plasminogénicos/genética , Inactivadores Plasminogénicos/metabolismo , Complicaciones Posoperatorias/metabolismo , ARN Mensajero/metabolismo , Ratas Wistar , Salvia miltiorrhiza/química , Adherencias Tisulares/metabolismo , Activador de Tejido Plasminógeno/genética , Activador de Tejido Plasminógeno/metabolismo
5.
Phytomedicine ; 111: 154662, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36681054

RESUMEN

BACKGROUND: Postoperative abdominal adhesion (PAA) is the most common complication after abdominal surgeries, which can lead to intestinal obstruction, chronic abdominal pain or female infertility. Jiawei Xiaochengqi decoction (JWXCQ) is a hospital preparation widely used for PAA treatment in Nanfang Hospital of Southern Medical University for more than twenty years. PURPOSE: This study aimed to investigate the therapeutic effects and potential mechanism of JWXCQ against PAA and provide beneficial information for its clinical application. METHODS: The main active components of JWXCQ were identified using ultra high performance liquid chromatography (UHPLC) combined with standard substance comparison. The efficacy and underlying mechanism of JWXCQ were evaluated through in vivo experiments with a postsurgical-induced peritoneal adhesion rat model, and in vitro studies with LPS-stimulated Raw 264.7 macrophages and primary fibroblasts. H&E and Masson staining were performed to assess histopathological changes. The levels of cytokines/proteins-associated with inflammation and degradation of extracellular matrix as well as CXCL2-CXCR2 pathway-related proteins were determined by ELISA, qRT-PCR, western blot assays or immunohistochemistry, respectively. Furthermore, siCXCR2 transfection was used to validate the mechanism of action of JWXCQ. RESULTS: JWXCQ treatment significantly reduced the formation of PAA, inhibited the inflammation and collagen deposition, and facilitated the secretion of MMP9, decreased the levels of IL-1ß, IL-6, TIMP1, COL-1, and suppressed the CXCL2-CXCR2 pathway in PAA rats. Furthermore, JWXCQ inhibited its downstream pathways, the JAK2-STAT3 and PI3K-AKT signaling, as indicated by the suppression of the phosphorylation levels of STAT3 and AKT. In vitro cell experiments revealed that JWXCQ reduced IL-1ß and IL-6 secretion in Raw 264.7 macrophages and COL-1 in primary fibroblasts. The CXCL2-CXCR2, JAK2-STAT3 and PI3K-AKT pathways were also inhibited after JWXCQ treatment, which were consistent with the in vivo results. More importantly, silence of CXCR2 eliminated the regulatory effects of JWXCQ. CONCLUSION: JWXCQ could effectively prevent the PAA formation by alleviating inflammation and collagen deposition, which was associated with the inhibition of CXCL2-CXCR2 pathway. This study investigated the relevant pharmacological mechanisms of JWXCQ, providing further evidence for the application of JWXCQ in clinical PAA treatment.


Asunto(s)
Fosfatidilinositol 3-Quinasas , Proteínas Proto-Oncogénicas c-akt , Animales , Femenino , Ratas , Quimiocina CXCL2/metabolismo , Citocinas/metabolismo , Inflamación/tratamiento farmacológico , Interleucina-6
6.
Zhong Yao Cai ; 33(4): 610-3, 2010 Apr.
Artículo en Zh | MEDLINE | ID: mdl-20845792

RESUMEN

OBJECTIVE: To prepare long-circulating hydroxycamptothecin nanoparticles and study its in vitro drug release characteristics. METHODS: The HCPT-PEG-PCL-NPs were prepared by solvent-diffusion method using PEG-PCL block copolymer synthesized as a matrix and HCPT as an antitumor agent. Then the obtained NPs were evaluated and its in vitro drug release characteristics were investigated. RESULTS: When using PEG4000-PCL2000, PEG4000-PCL1250, PEG2000-PCL2000, PEG2000-PCL1250 as the carrier material to prepare NPs, the average particle size of NPs in turn were 116.1, 110.0, 119.9, 99.1 nm; the zeta potential were -22.4, - 16. 9, -33.5, - 28.8 mV; the entrapment efficiency were 88.29%, 83.10%, 80.67%, 77.46%; and the drug loading were 2.96%, 2.56%, 2.31%, 2.14%, respectively. HCPT-PEG-PCL-NPs all showed a certain degree of sustained-release characteristics and their release mechanisms were fitted to Weibull modle, which showed that the drug release process included passive diffusion and matrix-eroded procedure. CONCLUSION: The HCPT-PEG-PCL-NPs has high entrapment efficiency, drug loading, uniform particle size, and can retard drug release in vitro, so it provides an extensive prospect for clinical application of HCPT.


Asunto(s)
Camptotecina/análogos & derivados , Camptotecina/farmacocinética , Portadores de Fármacos/química , Lactonas/química , Nanopartículas/química , Polietilenglicoles/química , Tecnología Farmacéutica/métodos , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacocinética , Área Bajo la Curva , Camptotecina/administración & dosificación , Camptotecina/química , Química Farmacéutica , Estabilidad de Medicamentos , Lactonas/síntesis química , Tamaño de la Partícula , Polietilenglicoles/síntesis química , Solubilidad
7.
Zhong Yao Cai ; 33(5): 778-81, 2010 May.
Artículo en Zh | MEDLINE | ID: mdl-20873566

RESUMEN

OBJECTIVE: To investigate the effects of matrine on proliferation, cell cycle, apoptosis rate and beta-catenin-dependent transcriptional activity in cultured hepatoma cell line Hep3B. METHODS: Cell viability was analyzed by cell counting kit-8 (CCK-8) assay. Cell cycle and apoptosis rate wene determined by flow cytometry analysis, beta-catenin-dependent transcriptional activity was assayed with Dual-Luciferase Reporter System. RESULTS: 72 h of matrine (50 - 800 mg/L) exposure significantly suppresses Hep3B cells growth in a concentration-dependent manner (P<0.01), the 50 percent inhibitory concentration (IC50) was 312.53 mg/L. A higher proportion of apoptotic cells in matrine-treated group than in control groups (21.73 +/- 1.66% vs. 4.39 +/- 1.93%) are shown. Cell proportions in G0/G1 phase were respectively 74.48% and 57.39% in matrine-treated group and control group. Cell proportions in S phase wene respectively 12.94% and 27.67%. Beta-catenin reporter activity was also decreased by matrine treatment in a concentration-dependent manner in Hep3B cells (P<0.05 or P<0.01). CONCLUSION: Through inhibition of beta-catenin-dependent transcription, matrine induces cell cycle arrest and apoptosis, and subsequently suppresses proliferation of hepatoma cells.


Asunto(s)
Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Proliferación Celular/efectos de los fármacos , Quinolizinas/farmacología , Sophora/química , beta Catenina/metabolismo , Alcaloides/administración & dosificación , Apoptosis/efectos de los fármacos , Carcinoma Hepatocelular/patología , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Relación Dosis-Respuesta a Droga , Citometría de Flujo , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , Neoplasias Hepáticas/patología , Quinolizinas/administración & dosificación , Transducción de Señal , Factores de Transcripción TCF/metabolismo , Matrinas
8.
Zhong Yao Cai ; 33(5): 775-8, 2010 May.
Artículo en Zh | MEDLINE | ID: mdl-20873565

RESUMEN

OBJECTIVE: To study the pharmacological effects of compound Centella asiatica enema on chronic renal failure (CRF) rats. METHODS: Rats were divided into control group, CRF model group, Niaoduqing positive control group, compound Centella asiatica enema high, middle and low three groups kidney coefficient, electrolyte levels, hematocrit (HCT), red blood cell counts (RBC), hemoglobin (HGB) content were observed after 30 days's treatment. RESULTS: Compared with the model group, the level of the electrolyte, HCT, RBC, HGB of rats in compound Centella asiatica enema high-doses group and the Niaoduqing group were significantly improved. CONCLUSION: High-doses of compound Centella asiatica enema has significant therapeutic effect on CRF rats.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Electrólitos/sangre , Fallo Renal Crónico/tratamiento farmacológico , Riñón/efectos de los fármacos , Adenina/administración & dosificación , Animales , Modelos Animales de Enfermedad , Combinación de Medicamentos , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/farmacología , Recuento de Eritrocitos , Femenino , Hematócrito , Hemoglobinas/análisis , Riñón/patología , Fallo Renal Crónico/inducido químicamente , Fallo Renal Crónico/patología , Masculino , Tamaño de los Órganos , Plantas Medicinales/química , Ratas , Ratas Sprague-Dawley
9.
J Ethnopharmacol ; 257: 112862, 2020 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-32294507

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Paeoniflorin, a prominent component in some Chinese formulas for hyperprolactinemia-associated disorders, has been found to inhibit prolactin secretion in prolactinoma cells. AIM: To examine the efficacy of paeoniflorin on hyperprolactinemia and the underlying mechanisms of action. MATERIALS AND METHODS: Hyperprolactinemia in female rats was generated by administration of olanzapine (5 mg/kg, by a gavage method, once daily, × 13 weeks). The rats were co-treated with paeoniflorin (10 and 50 mg/kg). Prolactin and TGF-ß1 concentrations were detected by ELISA. Protein expression was determined by Western blot. The effect in MMQ cells was also examined. RESULTS: Paeoniflorin inhibited olanzapine-induced increases in plasma prolactin concentration and prolactin protein overexpression in the pituitary and hypothalamus of rats. Further, paeoniflorin restored olanzapine-induced downregulation of pituitary and hypothalamic dopamine D2 receptor (D2R) protein expression. More importantly, paeoniflorin attenuated olanzapine-suppressed protein expression of transforming growth factor (TGF)-ß1 and its downstream genes, type II TGF-ß receptor, type I TGF-ß receptor and phosphorylated SMAD3 in the tissues. However, paeoniflorin did not affect plasma TGF-ß1 concentration and hepatic TGF-ß1 protein expression. In accord, olanzapine-induced increase in prolactin concentration, upregulation of prolactin protein expression, and downregulation of protein expression of the D2R and TGF-ß1 signals in MMQ cells were attenuated. CONCLUSIONS: This study demonstrates that paeoniflorin ameliorates olanzapine-induced hyperprolactinemia in rats by attenuating impairment of the D2R and TGF-ß1 signaling pathways in the hypothalamus and pituitary. Our findings may provide evidence to support the use of paeoniflorin-contained Chinese herbs and formulas for hyperprolactinemia and its associated disorders.


Asunto(s)
Glucósidos/farmacología , Hiperprolactinemia/prevención & control , Hipotálamo/efectos de los fármacos , Monoterpenos/farmacología , Hipófisis/efectos de los fármacos , Prolactina/sangre , Receptores de Dopamina D2/metabolismo , Factor de Crecimiento Transformador beta1/metabolismo , Animales , Antipsicóticos , Biomarcadores/sangre , Línea Celular Tumoral , Modelos Animales de Enfermedad , Femenino , Hiperprolactinemia/inducido químicamente , Hiperprolactinemia/metabolismo , Hipotálamo/metabolismo , Olanzapina , Hipófisis/metabolismo , Ratas Sprague-Dawley , Transducción de Señal
10.
Am J Transl Res ; 12(11): 7420-7429, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33312378

RESUMEN

Fibroblasts migrating to peritoneum injuries play an important role in the development of postoperative peritoneal adhesions due to the excessive synthesis and deposition of extracellular matrix (ECM). This effect is mainly induced by the transforming growth factor-ß (TGF-ß). Studies indicate that elevated TGF-ß1 levels and TGF-ß1/Smad signaling are both implicated in the formation of peritoneal adhesions. To confirm the effect of TGF-ß1/Smad signaling interference in regulating excessive ECM synthesis, a total of four different R-Smad-targeting small interference RNA (siRNA) duplexes (Smad2-500, Smad2-956, Smad3-378, Smad3-1385) were tested in this study using a TGF-ß1-stimulated adhesion tissue fibroblasts (ATFs) cell model. The in vitro assessments show that all proposed siRNAs are capable of significantly downregulating the mRNA and protein levels of Smad2 and Smad3 in ATFs. They also inhibit the phosphorylation of both Smads, which confirms their effect in blocking the TGF-ß1/Smad signaling pathway. Moreover, the siRNA duplexes can appreciably lower the elevated levels of fibronectin and collagen 3 alpha 1 (COL3A1) in TGF-ß1-stimulated ATFs, and the Smad3-378 siRNA can actually restore both molecules (fibronectin and COL3A1) to normal levels. Therefore, the Smad3-378 siRNA is suitable for both adhesion prevention and wound healing. Overall, our results indicate that postoperative adhesion prophylaxis may be achieved by temporarily blocking TGF-ß1/Smad signaling transduction.

11.
Artículo en Inglés | MEDLINE | ID: mdl-32419827

RESUMEN

Adhesion is a frequent complication after abdominal surgery. Although various methods have been applied to prevent and treat postoperative abdominal adhesion (PAA), few modern drugs designed for clinical applications have reached the expected preventive or therapeutic effect so far. There is an imperative to develop some new strategies for the treatment of PAA. Traditional Chinese medicine (TCM) has been widely practiced for thousands of years and played an indispensable role in the prevention and treatment of diseases. Modern medicine researchers have accepted the therapeutic effects of many active components derived from Chinese medicinal herbs. The review stresses the most commonly used TCM treatment, including Chinese medicinal herbals and monomers, TCM formulas, and acupuncture treatment.

12.
Phytomedicine ; 69: 153193, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32120245

RESUMEN

BACKGROUND: Although mechanical barriers and modern surgical techniques have been developed to prevent postoperative adhesion formation, high incidence of adhesions still represents an important challenge in abdominal surgery. So far, there has been no available therapeutic drug in clinical practice. PURPOSE: In this study, we explored the efficacy of sodium aescinate (AESS) treatment against postoperative peritoneal adhesions, the potential molecular mechanism was also investigated. STUDY DESIGN AND METHODS: Sixty male Sprague-Dawley rats were randomly divided into 6 groups for the study: the blank, vehicle, positive control and three AESS administration groups (0.5, 1 and 2 mg/kg/d, intravenous administration for 7 days). Adhesions were induced by discretely ligating peritoneal sidewall. An IL-1ß-induced HMrSV5 cell model was also performed to explore possible functional mechanism. RESULTS: The results indicated that the incidence and severity of peritoneal adhesions were significantly lower in the AESS-treated groups than that in the vehicle and positive control group. AESS-treated groups showed that the secretion, activity, and expression of tPA in rat peritoneum were notably increased. The FIB levels in rat plasma were decreased. The immunohistochemical staining analysis demonstrated that collagen I and α-SMA deposition were significantly attenuated in AESS-treated peritoneal tissues. Besides, we found that AESS treatment reduced the protein levels of p-MYPT1. To further explore the mechanisms of AESS, both activator and inhibitors of RhoA/ROCK pathway were employed in this study. It was found that AESS-induced up-regulation of tPA was reversed by activator of ROCK, but the effects of ROCK inhibitors were consistent with AESS. CONCLUSION: Taken together, the findings of in vivo and in vitro experiments proved that AESS could significantly suppress postoperative peritoneal adhesion formation through inhibiting the RhoA/ROCK signaling pathway. Our researches provide important pharmacological basis for AESS development as a potential therapeutic agent on peritoneal adhesions.


Asunto(s)
Enfermedades Peritoneales/tratamiento farmacológico , Complicaciones Posoperatorias/tratamiento farmacológico , Saponinas/farmacología , Triterpenos/farmacología , Proteínas de Unión al GTP rho/metabolismo , Quinasas Asociadas a rho/metabolismo , Animales , Línea Celular , Colágeno Tipo I/metabolismo , Fibrinógeno/metabolismo , Humanos , Interleucina-1beta/metabolismo , Interleucina-1beta/farmacología , Masculino , Enfermedades Peritoneales/patología , Enfermedades Peritoneales/prevención & control , Peritoneo/citología , Peritoneo/cirugía , Complicaciones Posoperatorias/patología , Complicaciones Posoperatorias/prevención & control , Ratas Sprague-Dawley , Transducción de Señal/efectos de los fármacos , Adherencias Tisulares
13.
J Agric Food Chem ; 68(42): 11747-11757, 2020 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-33047600

RESUMEN

Pelvic inflammatory disease (PID) is a common inflammation in the upper reproductive tract in women and may cause serious and costly consequences without effective treatment. Engeletin is a flavanonol glycoside and a naturally derived aldose reductase (AR) inhibitor that is widely distributed in vegetables, fruits, and plant-based foods. The present study investigated the anti-PID activity of engeletin in a mucilage-induced rat model of PID and LPS-stimulated RAW 264.7 macrophages. Engeletin significantly reduced inflammation and ameliorated the typical uterine pathological changes in PID rats. Engeletin also inhibited AR-dependent PLC/PKC/NF-κB and MAPK inflammatory pathways, as indicated by the suppression of the phosphorylation levels of PLC, PKC, p38, ERK, and JNK and the nuclear translocation of NF-κB p65. In vitro studies demonstrated that engeletin significantly inhibited inflammatory mediator expression and enhanced the phagocytic ability of LPS-induced RAW 264.7 macrophages. RNA interference of AR prevented the engeletin-induced inhibition of inflammatory mediators. Engeletin also inhibited AR-dependent PLC/PKC/NF-κB and MAPK inflammatory pathways, which was consistent with the in vivo results. These findings support engeletin as a potential agent for prevention or treatment of PID.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Antiinflamatorios/administración & dosificación , Inhibidores Enzimáticos/administración & dosificación , Flavonoles/administración & dosificación , Glicósidos/administración & dosificación , Enfermedad Inflamatoria Pélvica/dietoterapia , Proteína Quinasa C/inmunología , Factor de Transcripción ReIA/inmunología , Fosfolipasas de Tipo C/inmunología , Aldehído Reductasa/genética , Aldehído Reductasa/inmunología , Animales , Femenino , Humanos , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Macrófagos/efectos de los fármacos , Macrófagos/inmunología , Ratones , Enfermedad Inflamatoria Pélvica/genética , Enfermedad Inflamatoria Pélvica/inmunología , Proteína Quinasa C/genética , Células RAW 264.7 , Ratas , Ratas Sprague-Dawley , Factor de Transcripción ReIA/genética , Fosfolipasas de Tipo C/genética
14.
J Ethnopharmacol ; 256: 112785, 2020 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-32222576

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Smilax china L. has been used clinically to treat various inflammatory disorders with a long history. AIM OF THE STUDY: To investigate the mechanisms underlying anti-inflammatory action of the extract from the herb. MATERIALS AND METHODS: The extract was identified and quantified using the Ultra Performance Liquid Chromatography-Photo Diode Array-Mass Spectrometer method. The anti-inflammatory activities were examined in xylene-induced mouse ear edema and cotton ball-induced rat granuloma. The inflammatory mediators, pro-inflammatory cytokines and TLR-4-mediated signals in LPS-stimulated RAW264.7 macrophages were determined using ELISA, real-time PCR, Western blot and/or immunofluorescence, respectively. RESULTS: The extract was found to enrich flavonoids (44.3%, mainly astilbin, engeletin, isoastilbin, cinchonain Ia, quercetin-3-O-a-L-rhamnopyranoside and chlorogenic acid). The flavonoid-enriched extract (FEE) inhibited xylene-induced mouse ear edema and cotton ball-induced rat granuloma, and suppressed LPS-induced over-release and/or overexpression of tumor necrosis factor-α, cyclooxygenase-2, inducible nitric oxide synthase, interleukin-1ß and interleukin-6 in RAW264.7 macrophages. Mechanistically, FEE suppressed protein overexpression of TLR-4 and its downstream signals, MyD88 protein, phosphorylated inhibitory κB-α, NF-κB-P65 and MAPK p38, as well as phosphorylation of phosphoinositide 3-kinase (PI3K) p85α at Tyr607 and Akt at Ser473 in LPS-stimulated macrophages. The mode of the anti-inflammatory action of FEE was similar to that of TAK-242 (a selective TLR-4 inhibitor). CONCLUSIONS: The present results demonstrate that FEE inhibit inflammatory responses via the TLR-4-mediated signaling pathway. Our findings go a new insight into the mechanisms underlying anti-inflammatory action of the herb, and provide a better understanding of its use for inflammatory diseases.


Asunto(s)
Antiinflamatorios/farmacología , Flavonoides/farmacología , Mediadores de Inflamación/metabolismo , Inflamación/tratamiento farmacológico , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Receptor Toll-Like 4/metabolismo , Animales , Catalasa/metabolismo , Citocinas/metabolismo , Glutatión/metabolismo , Inflamación/metabolismo , Interleucina-1beta/metabolismo , Masculino , FN-kappa B/metabolismo , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo
15.
J Ethnopharmacol ; 252: 112602, 2020 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-32004632

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Hyperthyroidism is closely associated with liver injury. The preliminary clinical observation suggests that Yinning Tablet, a hospitalized preparation of traditional Chinese formula for hyperthyroidism, improves not only hyperthyroidism, but also hyperthyroidism-associated liver injury. AIM: To evaluate the effect and underlying mechanisms of Yinning Tablet on thyroid hormone-induced liver injury. MATERIALS AND METHODS: Female rats were orally administered L-thyroxine (1 mg/kg) once daily for 60 days, and co-treated with the carefully identified Yinning Tablet extract (0.6-2.4 g/kg) during the last 30 days. Blood and liver variables were determined enzymatically, histologically, by ELISA, radioimmunoassay, Real-Time PCR or Western blot, respectively. RESULTS: Co-treatment with the extract attenuated L-thyroxine-induced increases in serum alanine transaminase and aspartate transaminase activities, the ratio of liver weight to body weight, cytoplasmic vacuolization in hepatocytes, infiltrated inflammatory cells and confused structures in liver tissue, accompanied by attenuation of increased serum triiodo-l-thyronine concentration and hepatic deiodinase type I overexpression in rats. Importantly, Yinning Tablet suppressed L-thyroxine-triggered hepatic Bax, cleaved caspases-3, -8 and -9 protein overexpression, and Bcl-2 protein downregulation. Furthermore, the increases in cytochrome c protein expression, Ca2+-ATPase activity and malondialdehyde content, and decreases in activities of Na+/K+-ATPase, catalase, superoxide dismutase and glutathione peroxidase, and total antioxidant capacity in liver tissue were attenuated. CONCLUSION: The present results suggest that Yinning Tablet ameliorates thyroid hormone-induced liver injury in rats by regulating mitochondria-mediated apoptotic signals. Our findings go insight into the pharmacological basis of the hospitalized preparation for treatment of hyperthyroidism-associated liver injury.


Asunto(s)
Hipertiroidismo/tratamiento farmacológico , Hepatopatías/tratamiento farmacológico , Mitocondrias/efectos de los fármacos , Sustancias Protectoras/uso terapéutico , Tiroxina , Alanina Transaminasa/sangre , Animales , Apoptosis/efectos de los fármacos , Aspartato Aminotransferasas/sangre , Medicamentos Herbarios Chinos , Femenino , Formularios de Hospitales como Asunto , Hipertiroidismo/complicaciones , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Hepatopatías/etiología , Hepatopatías/genética , Hepatopatías/patología , Estrés Oxidativo/efectos de los fármacos , Sustancias Protectoras/farmacología , Ratas Sprague-Dawley , Tiroxina/sangre , Transcriptoma/efectos de los fármacos , Triyodotironina/sangre
16.
Zhong Yao Cai ; 32(4): 604-7, 2009 Apr.
Artículo en Zh | MEDLINE | ID: mdl-19645250

RESUMEN

OBJECTIVE: To prepare hydroxycamptothecin nanoparticles of amphiphilic block copolymer and study its characterization initially. METHODS: Polyethyleneglycol-polycaprolactone (PEG-PCL) was synthesized and its structure was characterized by 1H-NMR. The HCPT-PEG-PCL-NPs were prepared by solvent-diffusion method using PEG-PCL block copolymer as a matrix and HCPT as an antitumor agent. Then the obtained NPs were evaluated and the physical stabilities of both suspl and freeze drying powder were investigated. RESULTS: The mean particle size of the prepared NPs was 164.5 nm, polydispersity index (PI) was 0.14, drug loading (DL) was 5.49%, entrapment efficiency (EE) was 83.2%, zeta potential was -26.1 mV. The physical stability of freeze drying powder was better and hot environment seemed to be bad for the stability. CONCLUSION: The HCPT-PEG-PCL-NPs increase the solubility of HCPT in water and are valuable for the development of the novel dosage form of HCPT.


Asunto(s)
Antineoplásicos Fitogénicos/administración & dosificación , Camptotecina/análogos & derivados , Portadores de Fármacos/química , Nanopartículas/química , Polímeros/química , Antineoplásicos Fitogénicos/química , Camptotecina/administración & dosificación , Estabilidad de Medicamentos , Lactonas/química , Microscopía Electrónica de Transmisión , Tamaño de la Partícula , Polietilenglicoles/química , Solubilidad , Tecnología Farmacéutica
17.
Zhong Yao Cai ; 32(3): 375-7, 2009 Mar.
Artículo en Zh | MEDLINE | ID: mdl-19565715

RESUMEN

OBJECTIVE: To develop a high-performance liquid chromatographic-tandem mass/mass spectrometric method to determine the concentration of 1-deoxynojirimycin (1-DNJ) in mulberry leaves. METHODS: 1-deoxynojirimycin was separated on an SHIMADZU HRC-NH2 column with the mobile phase consisting of acetonitrile and 0.1% formic acid. The mass spectrometric system equipped with a atmospheric pressure chemical ionization (APCI) interface was operated in Multiple Reaction Monitoring (MRM) mode. RESULTS: The retention time of 1-deoxynojirimycin was 2.87 min, and the calibration curve was linear over a concentration range from 482 microg/L to 2410 microg/L, the average recovery was 95.8%. The detection limit was 53.6 microg/L. CONCLUSION: The method is selective and sensitive for determining 1-deoxynojirimycin in mulberry leaves.


Asunto(s)
1-Desoxinojirimicina/análisis , Morus/química , Plantas Medicinales/química , 1-Desoxinojirimicina/aislamiento & purificación , Medicamentos Herbarios Chinos/química , Hojas de la Planta/química , Control de Calidad , Reproducibilidad de los Resultados , Sensibilidad y Especificidad , Soluciones , Espectrometría de Masas en Tándem
18.
Zhong Yao Cai ; 31(8): 1190-3, 2008 Aug.
Artículo en Zh | MEDLINE | ID: mdl-19112899

RESUMEN

OBJECTIVE: To observe the effect of Shenshuaining dispersible tablets on the levels of NO, NOS, SOD and MDA in kidney of chronic renal failure (CRF) rats induced by adenine. METHODS: Seventy-two Sprague-Dawley rats were randomly divided into 6 groups: normal control group, model control group, Niaoduqing group, Shenshuaining dispersible tablets group(high, middle and low dose). From the second to the sixth group, the rats were prepared for model of CRF by being fed 0.5% adenine. After giving corresponding drugs for 7 weeks, we detected the levels of nitric oxide (NO), total nitric oxide synthase (T-NOS), inducing nitric oxide synthase (iNOS), configuration nitric oxide synthase (cNOS), total superoxide dismutase (SOD), Cu/Zn-SOD and malonaldehyde (MDA) in every rat's kidney tissue. RESULTS: Compared with normal rats, CRF rats' renal tissue's levels of NO, T-NOS, cNOS, T-SOD and Cu/Zn-SOD markedly decreased. Both the iNOS and MDA contents significantly increased. Shenshuaining dispersible tablets could markedly ameliorate above indexes. CONCLUSION: Shenshuaining dispersible tablets can effectively improve CRF rats' antioxidation effect and reduce damnification of free radical and protect the kidney.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Fallo Renal Crónico/tratamiento farmacológico , Riñón/efectos de los fármacos , Óxido Nítrico Sintasa/metabolismo , Óxido Nítrico/metabolismo , Superóxido Dismutasa/metabolismo , Adenina , Animales , Modelos Animales de Enfermedad , Combinación de Medicamentos , Medicamentos Herbarios Chinos/uso terapéutico , Femenino , Riñón/metabolismo , Riñón/patología , Fallo Renal Crónico/inducido químicamente , Fallo Renal Crónico/metabolismo , Masculino , Malondialdehído/metabolismo , Plantas Medicinales/química , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Comprimidos
19.
Zhong Yao Cai ; 31(9): 1402-4, 2008 Sep.
Artículo en Zh | MEDLINE | ID: mdl-19180970

RESUMEN

OBJECTIVE: To establish a rat model of hyperthyroidism Yin-deficiency. METHODS: SD rats separate male and female were randomly divided into four groups, a total of eight groups, each with six. The first group for the control group, 2 to 4 for the experimental drug-treated group, including thyroid-low, medium and high-dose group. In addition to the first group lavage volume of saline, the other groups were given the concentration of 2. 5, 5, 10 mg/kg-saline suspension of the thyroid. Once a day, 30 days for delivery. RESULTS: Compared with the control group, with the exception of Group 4 female rats serum T3, T4, FT3, FT4 values were significantly higher (P < 0.01), serum TSH was significantly lower (P < 0.05), the other treatment groups had different values no significant difference (P > 0.05). Group 4 that female rats modeling was success. CONCLUSION: Administration of thyroid-Suspension 10 mg/ kg for 30 d, female rats hyperthyroidism Yin-deficiency rat model is success.


Asunto(s)
Modelos Animales de Enfermedad , Hipertiroidismo , Hormonas Tiroideas/sangre , Tiroxina/administración & dosificación , Deficiencia Yin , Animales , Femenino , Hipertiroidismo/sangre , Hipertiroidismo/inducido químicamente , Masculino , Radioinmunoensayo , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Glándula Tiroides/efectos de los fármacos , Glándula Tiroides/patología , Tirotropina/sangre , Triyodotironina/sangre , Deficiencia Yin/sangre , Deficiencia Yin/inducido químicamente
20.
Nat Prod Res ; 31(13): 1495-1500, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28081652

RESUMEN

A new dimeric stilbene, gnetifolin P (1), was isolated from the lianas of Gnetum parvifolium, together with seven known compounds 2-8. The structure of compound 1 was determined by extensive NMR and HRESIMS data analyses, and quantum chemical calculations. All the compounds were evaluated for their anti-inflammatory activity. Compounds 1 and 6 inhibited the expression of IL-1ß on LPS induced THP-1 cells with the inhibition rate of 35.78 and 64.67%, respectively, at concentration of 25 µg/mL.


Asunto(s)
Antiinflamatorios/aislamiento & purificación , Gnetum/química , Estilbenos/aislamiento & purificación , Antiinflamatorios/química , Antiinflamatorios/farmacología , Línea Celular , Humanos , Interleucina-1beta/antagonistas & inhibidores , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura Molecular , Estilbenos/química , Estilbenos/farmacología
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