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1.
Lasers Med Sci ; 38(1): 74, 2023 Feb 17.
Artículo en Inglés | MEDLINE | ID: mdl-36800063

RESUMEN

We aim to evaluate the clinical efficacy and safety of using laser and light combined with topical minoxidil for alopecia areata. We searched PubMed, Embase, Web of Science, the Cochrane Library, China National Knowledge Infrastructure (CNKI), China Biomedical Literature Database (CBM), VIP database, and Wanfang Data from their inception to September 18, 2022. The risk of bias of the included RCTs was assessed by the Cochrane Collaboration tool. RevMan 5.3 software and Stata 14.0 software were used to perform the statistical analysis. The GRADE system assessed the quality of evidence. Ten studies were enrolled finally. The results of the meta-analysis showed that compared with topical minoxidil alone, the 308-nm excimer laser/light or He-Ne laser combined with topical minoxidil could reduce the SALT (Severity of Alopecia Tool) score (MD= -5.88, 95% CI [-9.79, -1.98], P=0.003). Whether fractional CO2 laser (RR=1.29, 95% CI [1.14, 1.46], P<0.0001), 308-nm excimer laser/light (RR=1.32, 95% CI [1.12, 1.55], P=0.001), He-Ne laser (RR=1.69, 95% CI [1.07, 2.69], P=0.03), or NB-UVB (RR=1.35, 95% CI [1.07,1.70], P=0.01) combined with topical minoxidil may improve the treatment response rate, comparing with topical minoxidil only. The recurrence rate of laser and light combined with topical minoxidil was lower than that of the minoxidil alone group (RR=0.54, 95% CI [0.31, 0.93], P=0.03) when follow-up time was 1 year. In addition, the incidence of adverse events including irritant contact dermatitis, erythema, desquamation, pain, and pruritus was no significant difference between the two groups (RR=1.50, 95% CI [0.95, 2.36], P=0.08). The level of evidence for outcomes was classified as very low to moderate. Based on the available evidence, laser and light combined with topical minoxidil therapy may be effective and safe for alopecia areata. However, more high-quality trials are required for comprehensive analysis and further verification.


Asunto(s)
Alopecia Areata , Minoxidil , Humanos , Minoxidil/uso terapéutico , Alopecia Areata/tratamiento farmacológico , Alopecia Areata/radioterapia , Ensayos Clínicos Controlados Aleatorios como Asunto , Fototerapia , Rayos Láser
2.
Materials (Basel) ; 16(3)2023 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-36770325

RESUMEN

ZK61 magnesium-alloy plate with high tensile strength and elongation is obtained by combined multipass symmetric hot rolling and asymmetric warm rolling. Deformation history considering varying strain rate obtained from the macro-finite element analysis of the selected passes are introduced into the viscoplastic self-consistent model (VPSC) as initial boundary conditions for macro- multiscale and micro-multiscale coupling analysis. VPSC simulation results show that in the initial stage of rolling deformation, the basal slip is the dominated deformation mode, supplemented by prismatic slip and pyramidal slip. With increased rolling strain, the pyramidal slip presents competitive relationship with basal slip, and the activation amount of {101-1} compression twins is limited. During asymmetric rolling, the basal slip is dominant, followed by the pyramidal slip. Experimental results show that the basal texture is gradually strengthened after symmetric rolling, and grain size is refined due to the activation and recrystallization of twins. Asymmetric rolling makes the basal texture deflect 10° to the rolling direction and further refine the grain size. With the ongoing of symmetric rolling, the mechanical anisotropy of the plate weakens, and the yield strength, tensile strength, and plasticity of the material improves. In particular, after asymmetric rolling, the tensile strength in the RD and TD directions of the plate reaches 391.2 MPa and 398.9 MPa, whereas the elongation reaches 19.8% and 25.5%.

3.
BMC Cancer ; 19(1): 1162, 2019 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-31783814

RESUMEN

BACKGROUND: To compare the efficacy and safety between conventional transarterial chemoembolization (cTACE) and drug-eluting beads TACE (DEB-TACE) in patients with infiltrative hepatocellular carcinoma (iHCC). METHODS: A total of 89 iHCC patients who were treated with either cTACE (n = 33) or DEB-TACE (n = 56) between April 2013 and September 2017 were included in this retrospective study. Patients with the situations that might have a poor outcome were defined as advanced disease including Child-Pugh class B, bilobar lesions, tumor size greater than 10 cm, ECOG 1-2, tumor burden of 50-70%, and the presence of ascites, arterioportal shunt (APS), and portal venous tumor thrombus (PVTT). The tumor response was measured 1-month and 3-month after the procedure. Progression-free survival (PFS) was calculated. Toxicity was graded by Common Terminology Criteria for Adverse Events v5.0 (CTCAE v5.0). The differences in tumor response, PFS, and toxicity were compared between the DEB-TACE group and cTACE group. RESULTS: At 1-month and 3-month after the procedure, the objective response rate (ORR) in the overall study population was similar in DEB-TACE group and cTACE group. The disease control rate (DCR), at 1-month after the procedure, was significantly higher in the patients treated with DEB-TACE relative to those treated with cTACE (P = 0.034), while after 3 months, the difference did not differ between two groups. DEB-TACE showed a higher DCR than cTACE in patients with tumor size greater than 10 cm (P = 0.036) or associated with APS (P = 0.030) at 1-month after the procedure, while after 3 months, the difference was only noted in patients with APS (P = 0.036). The median PFS in DEB-TACE group was 96 days, while in cTACE group was 94 days, and there was no difference in PFS between two groups (P = 0.831). In the side effect analysis, abdominal pain (P = 0.034) and fever (P = 0.009) were more frequently present in the cTACE group than DEB-TACE group, but there was no difference in high grade liver toxicity between the two groups. CONCLUSIONS: Compared to cTACE, DEB-TACE offers slightly better DCR and tolerability for iHCC patients, particularly in patients associated with APS and large tumor size. However, DEB-TACE does not provide higher PFS than cTACE.


Asunto(s)
Antibióticos Antineoplásicos/administración & dosificación , Carcinoma Hepatocelular/terapia , Quimioembolización Terapéutica/métodos , Sistemas de Liberación de Medicamentos/métodos , Neoplasias Hepáticas/terapia , Adulto , Anciano , Anciano de 80 o más Años , Antibióticos Antineoplásicos/efectos adversos , Antibióticos Antineoplásicos/química , Carcinoma Hepatocelular/patología , Doxorrubicina/administración & dosificación , Doxorrubicina/efectos adversos , Doxorrubicina/química , Evaluación de Medicamentos , Aceite Etiodizado/administración & dosificación , Aceite Etiodizado/efectos adversos , Aceite Etiodizado/química , Femenino , Humanos , Neoplasias Hepáticas/patología , Masculino , Microesferas , Persona de Mediana Edad , Estudios Retrospectivos , Resultado del Tratamiento
4.
ACS Infect Dis ; 5(4): 521-527, 2019 04 12.
Artículo en Inglés | MEDLINE | ID: mdl-30834747

RESUMEN

Protein-protein interactions (PPIs) underpin essential cellular processes of all organisms and are increasingly considered as drug targets. A number of techniques have been established to study PPIs; however, development of a simple and cost-effective method for in vitro high throughput screening of PPI inhibitors is still in demand or desirable. We report herein a simple method based on protein complementation for the in vitro study of PPIs, as well as screening of inhibitors against the PPI of interest. We have validated this system utilizing bacterial transcription factors NusB and NusE. Three derivatives of an inhibitor targeting the NusB-NusE interaction were synthesized and characterized with the system, which showed specific inhibition and antimicrobial activities. We have further confirmed the system with the RNA polymerase-σ interaction and an inhibitor. This system is expected to be suitable for more extensive high throughput screening of large chemical libraries. Additionally, our vector system can be easily adapted to study other PPI pairs, followed by inhibitor screening for hit identification in the application of early stage drug discovery.


Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Bacterias/metabolismo , Proteínas Bacterianas/metabolismo , Evaluación Preclínica de Medicamentos/métodos , Transcripción Genética/efectos de los fármacos , Antibacterianos/química , Bacterias/química , Bacterias/genética , Infecciones Bacterianas/microbiología , Proteínas Bacterianas/química , Proteínas Bacterianas/genética , Humanos , Unión Proteica/efectos de los fármacos , Factores de Transcripción/química , Factores de Transcripción/genética , Factores de Transcripción/metabolismo
5.
Drug Des Devel Ther ; 13: 601-609, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30809091

RESUMEN

BACKGROUND: Ankylosing spondylitis (AS) is a type of rheumatoid disease, which has been reported to be associated with the excessive proliferation of fibroblasts recently. Emodin, a single component from a traditional Chinese medicine Rheum palmatum, exerts anti-inflammation and antirheumatic arthritis activities. However, could emodin be used to treat AS remains unclear? Thus, this study aimed to investigate the effect of emodin on AS. METHODS: Fibroblasts obtained from patients with AS were used in the current study. In addition, multiple cellular and molecular biology techniques such as Cell Counting Kit-8, Western blotting, flow cytometry, monodansylcadaverine staining, and immunofluorescence assay were applied as well. RESULTS: Emodin-induced apoptosis of fibroblasts obtained from patient with AS via increasing active caspase-9, active caspase-3, and Bax levels and downregulating Bcl-2. Meanwhile, emodin enhanced autophagy in fibroblasts via upregulation of the expression of Atg12, Atg5, and Beclin 1, which was further confirmed by monodansylcadaverine staining. As expected, autophagy inhibitor 3-methyladenine (3MA) completely reversed emodin-induced autophagy in fibroblasts. Moreover, 3MA significantly increased emodin-induced apoptosis of fibroblasts obtained from patient with AS by increasing the levels of γH2AX, active caspase-9, active caspase-3, and cleaved poly ADP-ribose polymerase. CONCLUSION: Our results indicated that emodin effectively induced apoptosis and autophagy of fibroblasts obtained from patient with AS. In addition, suppression of autophagy enhanced emodin-induced apoptosis in fibroblasts. Therefore, we proposed that combination of emodin with autophagy inhibitor might be a potent strategy for improving the symptoms of AS in the future.


Asunto(s)
Apoptosis/efectos de los fármacos , Autofagia/efectos de los fármacos , Emodina/farmacología , Fibroblastos/efectos de los fármacos , Espondilitis Anquilosante/tratamiento farmacológico , Adulto , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Emodina/química , Femenino , Fibroblastos/citología , Fibroblastos/metabolismo , Fibroblastos/patología , Humanos , Masculino , Persona de Mediana Edad , Estructura Molecular , Espondilitis Anquilosante/metabolismo , Espondilitis Anquilosante/patología , Relación Estructura-Actividad
6.
Environ Sci Pollut Res Int ; 26(33): 33838-33846, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-29905896

RESUMEN

FeCl3, quick lime, and cationic polyacrylamide (CPAM) were used for excess sludge conditioning from wastewater treatment plant (WWTP) and the dewatering performance by different chemical conditioners was investigated. Experimental results showed that FeCl3 could make small and concentrated sludge particles. Furthermore, new mineral phase structures for building a dewatering framework were obtained by the addition of quick lime, and the coagulation capacity was enhanced by the formation of colloid hydroxyl polymer, which was induced due to the alkaline environment. In addition, the floc particle size significantly increased after the CPAM dosage. The bound water could be released with the stripping of tightly bound extracellular polymeric substance (EPS). Therefore, the dewatering performance and efficiencies were improved and subsequently the hypothetical sludge deep dewatering process was depicted in accordance with the variation of EPS. However, high-strength refractory organics in sludge filtrates caused by quick lime pyrolysis could lead to the unstable operation of the WWTP, because the relatively high concentrations of organic compounds with benzene were dominant in sludge dewatering filtrates.


Asunto(s)
Aguas del Alcantarillado/química , Eliminación de Residuos Líquidos/métodos , Resinas Acrílicas , Compuestos de Calcio , Cationes , Matriz Extracelular de Sustancias Poliméricas , Óxidos , Tamaño de la Partícula , Polímeros/química , Aguas Residuales
7.
Biol Pharm Bull ; 42(1): 50-56, 2019 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-30333377

RESUMEN

The development of ankylosing spondylitis (AS) occurs due to excessive proliferation of fibroblasts. Polydatin, a monomeric compound isolated from a traditional Chinese medicine Polygonum cuspidatum, exhibits anti-inflammatory and anti-arthritic effects. However, the mechanisms underlying the regulatory effects of polydatin on the proliferation, apoptosis and autophagy of fibroblasts obtained from patients with AS remain unclear. The aim of this study was to investigate the therapeutic effects of polydatin on symptoms associated with AS. Multiple cellular and molecular biology experiments were performed in the present study, such as cell viability assay, Western blotting, flow cytometry, monodansylcadaverine (MDC) staining and immunofluorescence assays. In the present study, the results revealed that polydatin induced the apoptosis of fibroblasts isolated from patients with AS by upregulating the expression of active caspase-3 and Bax, and downregulating the expression of Bcl-2. Meanwhile, polydatin was revealed to enhance the autophagy of fibroblasts by increasing the expression levels of LC3II, Beclin 1 and Atg5. The results of MDC and immunofluorescence assays further demonstrated that polydatin significantly induced the formation of autophagosomes in fibroblasts. Furthermore, polydatin-induced apoptosis and autophagy were markedly inhibited following treatment with the autophagy inhibitor, 3-methyladenine (3-MA). In conclusion, the results of the present study indicated that polydatin induces the apoptosis and autophagy of fibroblasts obtained from patients suffering from AS, and that polydatin may represent a therapeutic agent for the future treatment of patients with AS.


Asunto(s)
Apoptosis/efectos de los fármacos , Autofagia/efectos de los fármacos , Fibroblastos/efectos de los fármacos , Fibroblastos/patología , Glucósidos/farmacología , Espondilitis Anquilosante/patología , Estilbenos/farmacología , Adulto , Apoptosis/fisiología , Autofagia/fisiología , Células Cultivadas , Femenino , Glucósidos/uso terapéutico , Humanos , Masculino , Persona de Mediana Edad , Espondilitis Anquilosante/tratamiento farmacológico , Estilbenos/uso terapéutico
8.
Chem Biodivers ; 15(7): e1800137, 2018 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29763975

RESUMEN

There is a growing interest in the exploitation of agricultural byproducts. This study explored the potential beneficial health effects from the main biowaste, tea seed pomace of Camellia oleifera Abel (Theaceae), produced when tea seed is processed. Eighteen compounds were isolated from the 70% EtOH extract of the seed cake of C. oleifera. Their structures were determined by ESI-MS, 1 H- and 13 C-NMR together with literature data. All fractions and compounds were evaluated for the antioxidant and melanogenesis inhibitory activities. As the result, AcOEt fraction has the best in vitro antioxidant and antimelanogenesis activities, compounds 7 - 12 and 15 showed remarkable antioxidant activity, compounds 4, 6, 8, and 15 - 17 exhibited superior inhibitory activities against melanogenesis. Furthermore, tyrosinase inhibitory activity assay suggested that compound 8 could suppress melanogenesis by inhibiting the expression of tyrosinase.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Camellia/química , Inhibidores Enzimáticos/farmacología , Melaninas/antagonistas & inhibidores , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Melaninas/metabolismo , Ratones , Estructura Molecular , Monofenol Monooxigenasa/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Semillas/química , Relación Estructura-Actividad
9.
Breast ; 37: 18-27, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29059538

RESUMEN

Aromatase inhibitor-associated musculoskeletal symptoms (AIMSS) are prevalent among patients on AI therapy, which leads to a lower quality of life and poor adherence to AI treatment. We evaluated whether Yi Shen Jian Gu granules (YSJG) is effective and safe to relieve AIMSS in patients with breast cancer. Eligible participants were randomly assigned to the YSJG group or the placebo group. Both groups had a 12-week treatment period and a 12-week follow-up period. Brief Pain Inventory-Short Form (BPI-SF), Western Ontario and McMaster Universities Osteoarthritis (WOMAC) Index, and the Modified Score for the Assessment and Quantification of Chronic Rheumatoid Affections of the Hands (M-SACRAH) were obtained at baseline and at 4, 8, 12 and 24 weeks. Of 146 participants enrolled, 84 were randomly assigned, and 77 were evaluable at 12 weeks. Baseline characteristics were comparable between two groups. The primary outcome was the differences in mean BPI-SF scores at 12 weeks. The worst pain scores decreased by 3.10 points (50.2%; 95% CI, 2.50 to 3.65) for YSJG group compared with a 1.63-point decrease (26.9%; 95% CI, 3.86 to 4.97) for the placebo group (P = 0.001). Significantly improvements were also observed for the WOMAC and M-SACRAH. Possibly YSJG-related side effects were grade 1 nausea (10%) and grade 2 diarrhea (2%). Serum follicle-stimulating hormone and serum estradiol were kept in the postmenopausal range before and after YSJG treatment. Patients with AIMSS treated with YSJG granules had significant improvements in musculoskeletal symptoms. YSJG is effective, safe and well-tolerated in managing AIMSS. TRIAL REGISTRATION: ISCTN: ISRCTN06129599 (assigned 14 August 2013).


Asunto(s)
Antineoplásicos/efectos adversos , Inhibidores de la Aromatasa/efectos adversos , Neoplasias de la Mama/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Dolor Musculoesquelético/tratamiento farmacológico , Adulto , Anciano , Densidad Ósea , Diarrea/inducido químicamente , Método Doble Ciego , Medicamentos Herbarios Chinos/efectos adversos , Estradiol/sangre , Femenino , Hormona Folículo Estimulante/sangre , Humanos , Cumplimiento de la Medicación , Persona de Mediana Edad , Dolor Musculoesquelético/inducido químicamente , Náusea/inducido químicamente , Dimensión del Dolor , Calidad de Vida , Encuestas y Cuestionarios
10.
Zhongguo Zhong Yao Za Zhi ; 42(4): 644-648, 2017 Feb.
Artículo en Chino | MEDLINE | ID: mdl-28959831

RESUMEN

To provide guidance for quality control and variety breeding of Gastrodia elata f. glauca cultivated form in Zhaotong, nine agronomic traits of G. elata f. glauca cultivation form were measured and the traits were analyzed using multiple comparison,correlation analysis, multiple stepwise regression analysis and path analysis. The results of multiple comparison and analysis showed that the number of dot ring and the length-width ratio of tuber were no different in G. elata f. glauca cultivation form. The coefficient of variation about the single tuber fresh weigh, ring spacing and belly button diameter was about 20%. The coefficient of variation about the length of the tuber, the width of the tuber, the thickness of the tuber, the length-width ratio of tuber and the number of dot ring was near 10%. The correlation analysis results showed that the single tuber fresh weigh and the length,the width and the thickness of the tuber were extremely significant positive correlated. The results of multiple stepwise regression analysis and path analysis showed that the length, the width and the thickness of the tuber were the main factors affecting the fresh weight of single tuber,which were the best agronomic traits on high yield of G. elata f. glauca. The length of the tuber,the width of the tuber and the thickness of the tuber, which would be used as indicators of the characteristics of high yield varieties in Zhaotong. The number of dot ring and the length-width ratio of tuber, which would be selected as quality control indicators of the genuine Chinese medicinal materials in Zhaotong.


Asunto(s)
Gastrodia/crecimiento & desarrollo , Tubérculos de la Planta/crecimiento & desarrollo , Plantas Medicinales/crecimiento & desarrollo , China , Fenotipo , Fitomejoramiento , Control de Calidad
11.
Biochemistry ; 56(38): 5049-5052, 2017 09 26.
Artículo en Inglés | MEDLINE | ID: mdl-28782938

RESUMEN

We report the discovery of the first bacterial ribosomal RNA (rRNA) synthesis inhibitor that has specific antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA). A pharmacophore model was constructed on the basis of the protein-protein interaction between essential bacterial rRNA transcription factors NusB and NusE and employed for an in silico screen to identify potential leads. One compound, (E)-2-{[(3-ethynylphenyl)imino]methyl}-4-nitrophenol (MC4), demonstrated antimicrobial activity against a panel of S. aureus strains, including MRSA, without significant toxicity to mammalian cells. MC4 resulted in a decrease in the rRNA level in bacteria, and the target specificity of MC4 was confirmed at the molecular level. Results obtained from this work validated the bacterial rRNA transcription machinery as a novel antimicrobial target. This approach may be extended to other factors in rRNA transcription, and MC4 could be applied as a chemical probe to dissect the relationship among MRSA infection, MRSA growth rate, and rRNA synthesis, in addition to its therapeutic potential.


Asunto(s)
Antibacterianos/farmacología , Hidrazonas/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Nitrofenoles/farmacología , ARN Ribosómico/antagonistas & inhibidores , Antibacterianos/efectos adversos , Proteínas Bacterianas/química , Proteínas Bacterianas/metabolismo , Simulación por Computador , Evaluación Preclínica de Medicamentos/métodos , Proteínas de Escherichia coli/química , Proteínas de Escherichia coli/metabolismo , Hidrazonas/química , Staphylococcus aureus Resistente a Meticilina/genética , Staphylococcus aureus Resistente a Meticilina/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana , Nitrofenoles/química , Conformación Proteica , ARN Ribosómico/biosíntesis , ARN Ribosómico/genética , Proteínas Ribosómicas/química , Proteínas Ribosómicas/metabolismo , Factores de Transcripción/química , Factores de Transcripción/metabolismo
12.
Molecules ; 22(5)2017 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-28505136

RESUMEN

Gubenyiliu II (GYII), a Traditional Chinese Medicine (TCM) formula used in our hospital, has shown beneficial effects in cancer patients. In this study, we investigated the molecular mechanisms underlying the beneficial effects of GYII on murine breast cancer models. GYII showed significant inhibitory effects on tumor growth and metastasis in the murine breast cancer model. Additionally, GYII suppressed the proliferation of 4T1 and MCF-7 cells in a dose-dependent manner. A better inhibitory effect on 4T1 cell proliferation and migration was found in the decomposed recipes (DR) of GYII. Moreover, heparanase expression and the degree of angiogenesis were reduced in tumor tissues. Western blot analysis showed decreased expression of heparanase and growth factors in the cells treated with GYII and its decomposed recipes (DR2 and DR3), and thereby a reduction in the phosphorylation of extracellular signal-regulated kinase (ERK) and serine-threonine kinase (AKT). These results suggest that GYII exerts anti-tumor growth and anti-metastatic effects in the murine breast cancer model. The anti-tumor activity of GYII and its decomposed recipes is, at least partly, associated with decreased heparanase and growth factor expression, which subsequently suppressed the activation of the ERK and AKT pathways.


Asunto(s)
Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Medicamentos Herbarios Chinos/uso terapéutico , Glucuronidasa/metabolismo , Animales , Neoplasias de la Mama/enzimología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Femenino , Humanos , Células MCF-7 , Ratones , Fosforilación/efectos de los fármacos , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal/efectos de los fármacos
13.
Eur J Med Chem ; 136: 382-392, 2017 Aug 18.
Artículo en Inglés | MEDLINE | ID: mdl-28525839

RESUMEN

Reduction of hippocampal neurogenesis caused by aging and neurological disorders would impair neural circuits and result in memory loss. A new lead compound (N-trans-3',4'-methylenedioxystilben-4-yl acetamide 27) has been discovered to efficiently stimulate adult rats' neurogenesis. In-depth structure-activity relationship studies proved the necessity of a stilbene scaffold that is absent in highly cytotoxic analogs such as chalcones and heteroaryl rings and inactive analogs such as diphenyl acetylene and diphenyl ethane, and validated the importance of an NH in the carboxamide and a methylenedioxy substituent on the benzene ring. Immunohistochemical staining and biochemical analysis indicate, in contrast to previously reported neuroprotective chemicals, N-stilbenyl carboxamides have extra capacity for neuroproliferation-type neurogenesis, thereby providing a foundation for improving the plasticity of the adult mammalian brain.


Asunto(s)
Acetanilidas/farmacología , Descubrimiento de Drogas , Hipocampo/efectos de los fármacos , Neurogénesis/efectos de los fármacos , Extractos Vegetales/química , Estilbenos/farmacología , Acetanilidas/química , Acetanilidas/aislamiento & purificación , Animales , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Masculino , Estructura Molecular , Ratas , Ratas Sprague-Dawley , Estilbenos/química , Estilbenos/aislamiento & purificación , Relación Estructura-Actividad
14.
BMC Complement Altern Med ; 16(1): 504, 2016 Dec 05.
Artículo en Inglés | MEDLINE | ID: mdl-27919258

RESUMEN

BACKGROUND: Senkyunolide I (SEI) is one of the most important bioactive phthalides of Ligusticum chuanxiong Hort. (Umbelliferae), a Traditional Chinese Medicine. Our previous studies suggested that it might be developed as a potential treatment for migraine. METHODS: In this paper, we aimed to isolate and characterize the main metabolites of SEI after gavage feeding in rats. Their structures were identified precisely on the basis of nuclear magnetic resonance (NMR) spectroscopy and UPLC/Q-TOF-MS spectrometry. We also established the main metabolic pathways of SEI in rats. RESULTS: Four metabolites (M1-M4) were isolated, for the first time, from bile samples of rats by preparative high-performance liquid chromatography. Their structures were determined as SEI-6S-O-ß-D-glucuronide (M1), SEI-7S-O-ß-D-glucuronide (M2), SEI-7S-S-glutathione (M3) and SEI-7R-S-glutathione (M4) on the basis of the molecular mass of the analytes, using ultra performance liquid chromatography/quadrupole-time-of-flight mass spectrometry and 1D and 2D NMR. CONCLUSIONS: The results demonstrated that glucuronide and glutathione conjugation were the major pathways of SEI metabolism in vivo, and the configuration at the 7th-position could be inverted during glutathione conjugation.


Asunto(s)
Benzofuranos/química , Medicamentos Herbarios Chinos/química , Ligusticum/química , Animales , Benzofuranos/metabolismo , Cromatografía Líquida de Alta Presión , Imagen por Resonancia Magnética , Masculino , Estructura Molecular , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem
15.
Zhongguo Zhong Yao Za Zhi ; 41(11): 2044-2048, 2016 Jun.
Artículo en Chino | MEDLINE | ID: mdl-28901099

RESUMEN

In order to provide a basis for establishing seed testing rules and seed quality standard of Bletilla striata, the seed quality of B.striata from different producing area was measured referring to the Rules for Agricultural Seed Testing(GB/T 3543-1995).The results showed that the seeds of B.striata passed through 20-mesh sieve for purity analysis.The weight of seeds was measured by 1000-seed method and the water content was measured at the higher temperature (133±2) ℃ for 3 hours.The seeds were cultured on the wet filter paper at 30 ℃ for 4-20 days in light for germination testing.The method of testing seed viability was that seeds were dipped into 1% TTC solution for 7 hours at temperature of 40 ℃.


Asunto(s)
Germinación , Orchidaceae , Control de Calidad , Semillas , Temperatura
16.
Zhongguo Zhong Yao Za Zhi ; 41(17): 3155-3163, 2016 Sep.
Artículo en Chino | MEDLINE | ID: mdl-28920364

RESUMEN

In this paper, the potential distribution information and ecological suitability regionalization for Gastrodia elata in Zhaotong were studied based on the climate, terrain, soil and vegetation factors analysis by Maxent and ArcGIS. The results showed that the highly potential distribution (suitability index>0.6) mainly located in Zhaotong, Yunnan province(Zhenxiong,Yiliang and Daguan county, with an area of 2 872 km²ï¼‰, and Bijie, Guizhou province (Hezhang,Bijie,Weining county, 1 251 km²ï¼‰. The AUC of ROC curve was above 0.99, indicating that the predictive results with the Maxent model were highly precise. The main ecological factors determining the potential distribution were the altitude, average rainfall in November, average rainfall in October, vegetation types, average rainfall in March, average rainfall in April,soil types,isothermal characteristic and average rainfall in June. The environmental variables in the highly potential areas were determined as altitude around 1 450-2 200 m,annual average temperature around 18.0-20.4 ℃,annual average precipitation around 900 mm,yellow soil or yellow brown soil,and acid sandy loam or slightly acidic sandy loam.The results will provide valuable references for plantation regionalization and the siting for imitation wild planting of G. elata in Zhaotong.


Asunto(s)
Gastrodia/crecimiento & desarrollo , China , Clima , Ecología , Sistemas de Información Geográfica , Suelo
17.
Zhong Yao Cai ; 38(2): 381-5, 2015 Feb.
Artículo en Chino | MEDLINE | ID: mdl-26415417

RESUMEN

OBJECTIVE: To optimize conditions for extracting total flavonoids from Schizonepeta tenuifolia by the method of analytical hierarchy process with the correlation method of dose-effect. METHODS: Take the amount and concentration of ethanol,the extraction time and times as examine factors, with the inhibition rate of Caco-2 human cloning colonic cancer cell as index to optimize the optimum conditions of total flavonoids from Schizonepeta tenuifolia by orthogonal experiment design, and analyze the Pearson correlation coefficient between the total flavonoids content, hesperidin content, extraction rate and pharmacodynamics indexes through SPSS 19.0 software to determine the dose-effect comparative indicators, and then analytic hierarchy process is adopted to define the weight coefficients range of the content of total flavonoids and hesperidin. RESULTS: The best extraction process conditions were as follows:15 times the amount of 75% ethanol, water circumfluence extracting for 3 times,each time for 2 hours; The weight coefficient ranges of the content of total flavonoids and hesperidin were 0.7500-0.9000 and 0.1000-0.2500 respectively. CONCLUSION: Using the comprehensive scores of the content of total flavonoids and hesperidin, which is calculated by weight coefficient ranges that based on the analytical hierarchy process,to replace the inhibition rate as the indicator to optimize the optimum extraction process is scientific and reasonable. This optimization process is simple and practical,which provides a new method for selecting the best extraction indicators to get effective ingredients from traditional Chinese medicine.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Flavonoides/aislamiento & purificación , Lamiaceae/química , Células CACO-2 , Relación Dosis-Respuesta a Droga , Etanol , Flavonoides/química , Hesperidina/química , Humanos , Tecnología Farmacéutica , Agua
18.
Zhong Nan Da Xue Xue Bao Yi Xue Ban ; 40(1): 46-52, 2015 Jan.
Artículo en Chino | MEDLINE | ID: mdl-25652374

RESUMEN

OBJECTIVE: To explore the eff ect of grape seed proanthocyanidins extract (GSPE) on the growth of pancreatic cancer cells and the underlying mechanisms. METHODS: The pancreatic cancer AsPC-1 cells were cultured in vitro. The effects of GSPE on cell proliferation, apoptosis and migration were analyzed by MTT, Annexin V-FITC/PI and Transwell migration assay, respectively. The expression of miR-27a and FOXO1 in AsPC-1 cells was determined by real-time RT-PCR and Western blot, respectively. The miR-27a inhibitors were applied to verify the role of miR-27a in mediation of GSPE effects. RESULTS: GSPE inhibited cell growth in a dose-dependent manner. This inhibitory effect was significant when the dosage of GSPE was more than 50 µg/mL (P<0.05 vs control). GSPE also could induce apoptosis and inhibit cell migration. MiR-27a expression was notably down-regulated when the dosage of GSPE was 75 µg/mL (P<0.01 vs control). Compared with the control group, cell proliferation inhibition was significantly increased in the miR-27a inhibitor group, the GSPE group and the miR-27a inhibitor plus GSPE group (P<0.01), while cell migration was significantly decreased (P<0.01). Compared with the GSPE or the miR-27a inhibitor group, the growth and migration inhibitory effects in the miR-27a inhibitor plus GSPE group were more obviously (P<0.01). Both GSPE and miR-27a inhibitor alone could up-regulate FOXO1 expression. But these effects were more apparent when they are applied in combination. CONCLUSION: GSPE inhibites AsPC-1 cells' growth and migration partly through down-regulation of miR-27a expression.


Asunto(s)
Apoptosis , Extracto de Semillas de Uva/farmacología , MicroARNs/metabolismo , Neoplasias Pancreáticas/patología , Proantocianidinas/farmacología , Línea Celular Tumoral/efectos de los fármacos , Movimiento Celular , Proliferación Celular , Regulación hacia Abajo , Humanos , MicroARNs/genética , Regulación hacia Arriba
19.
Chin J Integr Med ; 2014 Dec 23.
Artículo en Inglés | MEDLINE | ID: mdl-25537148

RESUMEN

OBJECTIVE: To investigate the inhibitory effects of Guben Yiliu Formula II(II, GFII) and its blood activation prescription (BAP) on the growth of MCF-7 human breast cancer xenografts in nude mice, and explore their mechanisms of action. METHODS: After the establishment of the MCF-7 human breast cancer xenograft model in nude mice, the mice in the GFII and BAP groups were administered with GFII (6.56 g/mL) and BAP (1.65 g/mL) by gavage for 28 days, respectively. The tumor volume and weight were measured twice a week throughout the treatment period. Apoptotic cells were identified by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling. The expression of microtubule associated protein 1 light chain 3 (LC3) was examined by immunohistochemistry, and Western blotting analysis was performed to detect the expression of anti-apoptotic protein Bcl-2 and LC3, as well as the effects on phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway. RESULTS: Compared with the control group, the GFII and BAP groups could significantly inhibit the growth of MCF-7 human breast cancer xenografts in nude mice. The expression of Bcl-2 protein was lower in the GFII and BAP than in the control group, whereas both the percentage of apoptotic cells and LC3-II/LC3-I ratio were higher than in the control group. In addition, significantly reduced expression of phospho-Akt, phosphor-mTOR and mTOR were observed in the blood activation group (P<0.05). CONCLUSIONS: To some extent, the GFII and its BAP can exert their inhibitory effect on the growth of MCF-7 human breast cancer xenografts by inducing the cell apoptosis and autophagy. In addition to the induction of cell apoptosis, we also found that the BAP of GFII could induce cell autophagy by inhibiting of PI3K/Akt/mTOR signaling pathway, and then suppress the breast cancer cell growth.

20.
Trials ; 15: 171, 2014 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-24885324

RESUMEN

BACKGROUND: Aromatase inhibitors (AIs) are widely used as an adjuvant endocrine treatment in postmenopausal women with early-stage breast cancer. One of the main adverse effects of AIs is musculoskeletal symptoms, which leads to a lower quality of life and poor adherence to AI treatment. To date, no effective management of aromatase inhibitor-associated musculoskeletal symptoms (AIMSS) has been developed. METHODS/DESIGN: To determine whether the traditional Chinese medicine Yi Shen Jian Gu granules could effectively manage AIMSS we will conduct a multicenter, randomized, double-blind, placebo-controlled clinical trial. Patients experiencing musculoskeletal symptoms after taking AIs will be enrolled and treated with traditional Chinese medicine or placebo for 12 weeks. The primary outcome measures include Brief Pain Inventory-Short Form, Western Ontario and McMaster Universities Osteoarthritis Index, and Modified Score for the Assessment and Quantification of Chronic Rheumatoid Affections of the Hands, which will be obtained at baseline and at 4, 8, 12 and 24 weeks. DISCUSSION: The results of this study will provide a new strategy to help relieve AIMSS. TRIAL REGISTRATION ISCTN: ISRCTN06129599 (assigned 14 August 2013).


Asunto(s)
Antineoplásicos Hormonales/efectos adversos , Inhibidores de la Aromatasa/efectos adversos , Neoplasias de la Mama/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Enfermedades Musculoesqueléticas/tratamiento farmacológico , Proyectos de Investigación , Neoplasias de la Mama/patología , China , Protocolos Clínicos , Método Doble Ciego , Medicamentos Herbarios Chinos/efectos adversos , Femenino , Humanos , Enfermedades Musculoesqueléticas/inducido químicamente , Enfermedades Musculoesqueléticas/diagnóstico , Dimensión del Dolor , Encuestas y Cuestionarios , Factores de Tiempo , Resultado del Tratamiento
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