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1.
Environ Pollut ; 313: 120100, 2022 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-36075333

RESUMEN

As the only "tropical base of agricultural production" in China, Hainan lsland is vigorously developing high-value agriculture and is becoming the province with the highest proportion of cash crops. However, this intensive farming with large nutrient inputs has caused cropland degradation, nitrogen (N) and phosphorus (P) overloads and water pollution, which have been reversed to initiate the construction of free trade ports. Here, we systematically review the status, driving factors, and environmental impacts of cropland degradation and nutrient overload with quantified evaluations and compared with other global tropics. Over the last 30 years, the soil pH in Hainan decreased by 0.3 units, and the soil organic carbon (SOC) decreased by 20%. This soil degradation has consequently aggravated nutrient losses, caused low use efficiency, and has required farmers add additional large nutrient to maintain harvests. P overuse is more serious than N overuse in Hainan due to the misuse of high P content compound fertilizers. The current N and P usage densities were 4% and 66% higher than the national average per crop season, i.e., 301 kg N ha-1 and 98 kg P ha-1, respectively, and the application rates were even higher for vegetables, i.e., 43% and 115% higher than the national average for vegetables. Consequently, water quality degradation occurred. The nutrient contents of several estuaries have exceeded the Class III standards. Potential improvement strategies are proposed: (i) Organic materials must be recycled to curb the declines in SOC and pH, and more benefits would be obtained by together use of biochar. (ii) Nutrient quotas must be implemented to balance nutrient budgets and reduce excessive surpluses and losses. (iii) The service functions of ecological protection zones for water and soil conservation must be strengthened. These strategies also apply to other global tropics that face similar challenges of soil and ecological degradation.


Asunto(s)
Fertilizantes , Suelo , Agricultura , Carbono , China , Productos Agrícolas/química , Fertilizantes/análisis , Nitrógeno/análisis , Nutrientes/metabolismo , Fósforo/análisis , Suelo/química
2.
Front Mol Biosci ; 8: 687305, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34805266

RESUMEN

Few studies have reported whether nutrients in the tumor microenvironment can regulate the expression of PD-L1. Since tumor cells are often situated in a low-glutamine environment, we investigated PD-L1 expression under glutamine deprivation in bladder cancer cells. PD-L1 expression and the activation of the EGFR/MEK/ERK/c-Jun signaling pathway under glutamine deprivation were investigated by qPCR, Western blot, and immunofluorescence analyses. C-Jun-mediated transcriptional regulation of the PD-L1 gene was assessed by ChIP. PD-L1 expression and activation of the EGFR/MEK/ERK/c-Jun signaling pathway were assessed in T24 cells, TCCSUP cells and BALB/c mice with or without glutamine supplementation. Additionally, the impact of PD-L1 expression under glutamine deprivation on the function of T cells was investigated by ELISA. The expression of PD-L1 and EGFR/MEK/ERK/c-Jun pathway activation were elevated by glutamine deprivation, and c-Jun was enriched in the enhancer region of PD-L1. The expression of PD-L1 was considerably impaired by inhibiting the EGFR/MEK/ERK/c-Jun pathway and was elevated by activating this signaling pathway. In addition, the elevated PD-L1 expression and MEK/ERK/c-Jun signaling pathway activation were reduced by glutamine supplementation in vitro and in vivo. PD-L1 upregulation by glutamine deprivation in bladder cancer cells could reduce IFN-γ production by T cells. The expression of PD-L1 was upregulated under glutamine deprivation through the EGFR/MEK/ERK/c-Jun pathway to impair T cell function.

3.
Zhongguo Zhong Yao Za Zhi ; 45(10): 2431-2438, 2020 May.
Artículo en Chino | MEDLINE | ID: mdl-32495603

RESUMEN

This research is to predict anti-Alzheimer's disease active constituents on the target of acetylcholinesterase(AChE) from Glycyrrhizae Radix et Rhizoma with the help of pharmacophore and molecular docking. AChE ligand-based pharmacophore model was set up and the molecular library of the constituents from Glycyrrhizae Radix et Rhizoma were established by collecting literature. Then the constituents from Glycyrrhizae Radix et Rhizoma were screen for the potential AChE inhibitory potency in silico through matching with the best pharmacophore model. The flexible docking was used to evaluate the interactions between compounds screened from pharmacophore model and AChE protein(PDB ID:4 EY7). The interactions were expressed including but not limited to CDOCKER interaction energy, hydrogen bonds and non-bonding interactions. The molecular library of Glycyrrhizae Radix et Rhizoma contains 44 chemical constituents. As for the pharmacophore model, six kinds of potential AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma were considered to be the promising compounds according to the results of searching 3 D database of pharmacophore model. The molecular docking was possessed and the interaction patterns were given to show the detail interactions. The compounds screening from the pharmacophore model were consistent with the existing studies to some degree, indicating that the virtual screen protocols of AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma based on pharmacophore and molecular docking was reliable.


Asunto(s)
Medicamentos Herbarios Chinos , Glycyrrhiza , Triterpenos , Simulación del Acoplamiento Molecular , Rizoma
4.
Int J Mol Med ; 44(6): 2189-2200, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31661119

RESUMEN

Changes in metabolism are common phenomena in tumors. Glutamine (Gln) has been documented to play a critical role in tumor growth. In this study, we aimed to to explore the mechanisms through which bladder cancer cells utilize Gln to fulfill their biosynthetic needs during proliferation. In addition, the roles of Gln in the tricarboxylic acid (TCA) cycle, reactive oxygen species (ROS) regulation, and signal transducer and activator of transcription 3 (STAT3) expression were examined in vitro in the T24 bladder cancer cell line. The results revealed that the T24 cell line was markedly Gln­dependent and that Gln supplementation promoted T24 proliferation through the actions of Gln as a ROS moderator and as a metabolic fuel in the TCA cycle. Importantly, extracellular Gln deprivation deregulated the production of the transcription factor, STAT3. Additionally, STAT3 expression was affected by the degree of Gln metabolism, as regulated by Gln intermediates and ROS. Thus, on the whole, the findings of this study demonstrate that Gln promotes the proliferation of the Gln­dependent bladder cancer cell line, T24, by supplementing adenosine triphosphate (ATP) production and neutralizing ROS to activate the STAT3 pathway.


Asunto(s)
Proliferación Celular/genética , Glutamina/metabolismo , Factor de Transcripción STAT3/genética , Neoplasias de la Vejiga Urinaria/genética , Adenosina Trifosfato/metabolismo , Adenosina Trifosfato/farmacología , Apoptosis/genética , Línea Celular Tumoral , Ciclo del Ácido Cítrico/genética , Regulación Neoplásica de la Expresión Génica/genética , Humanos , Especies Reactivas de Oxígeno/metabolismo , Transducción de Señal/genética , Neoplasias de la Vejiga Urinaria/metabolismo , Neoplasias de la Vejiga Urinaria/patología
5.
Cell Physiol Biochem ; 45(5): 2054-2070, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29533936

RESUMEN

BACKGROUND/AIMS: Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a potential anti-cancer agent due to its selective toxicity. However, many human non-small cell lung cancer (NSCLC) cells are partially resistant to TRAIL, thereby limiting its clinical application. Therefore, there is a need for the development of novel adjuvant therapeutic agents to be used in combination with TRAIL. METHODS: In this study, the effect of N-acetyl-glucosamine (GlcNAc), a type of monosaccharide derived from chitosan, combined with TRAIL was evaluated in vitro and in vivo. Thirty NSCLC clinical samples were used to detect the expression of death receptor (DR) 4 and 5. After GlcNAc and TRAIL co-treatment, DR expression was determined by real-time PCR and western blotting. Cycloheximide was used to detect the protein half-life to further understand the correlation between GlcNAc and the metabolic rate of DR. Non-reducing sodium dodecyl sulfate-polyacrylamide gel electrophoresis was used to detect receptor clustering, and the localization of DR was visualized by immunofluorescence under a confocal microscope. Furthermore, a co-immunoprecipitation assay was performed to analyze the formation of death-inducing signaling complex (DISC). O-linked glycan expression levels were evaluated following DR5 overexpression and RNA interference mediated knockdown. RESULTS: We found that the clinical samples expressed higher levels of DR5 than DR4, and GlcNAc co-treatment improved the effect of TRAIL-induced apoptosis by activating DR5 accumulation and clustering, which in turn recruited the apoptosis-initiating protease caspase-8 to form DISC, and initiated apoptosis. Furthermore, GlcNAc promoted DR5 clustering by improving its O-glycosylation. CONCLUSION: These results uncovered the molecular mechanism by which GlcNAc sensitizes cancer cells to TRAIL-induced apoptosis, thereby highlighting a novel effective agent for TRAIL-mediated NSCLC-targeted therapy.


Asunto(s)
Acetilglucosamina/farmacología , Apoptosis/efectos de los fármacos , Receptores del Ligando Inductor de Apoptosis Relacionado con TNF/metabolismo , Ligando Inductor de Apoptosis Relacionado con TNF/toxicidad , Células A549 , Acetilglucosamina/uso terapéutico , Animales , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/metabolismo , Carcinoma de Pulmón de Células no Pequeñas/patología , Caspasa 8/metabolismo , Línea Celular Tumoral , Glicosilación/efectos de los fármacos , Humanos , Inmunoprecipitación , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/metabolismo , Neoplasias Pulmonares/patología , Ratones , Ratones Desnudos , Microscopía Confocal , Poli(ADP-Ribosa) Polimerasas/metabolismo , Interferencia de ARN , ARN Interferente Pequeño/metabolismo , Reacción en Cadena en Tiempo Real de la Polimerasa , Receptores del Ligando Inductor de Apoptosis Relacionado con TNF/antagonistas & inhibidores , Receptores del Ligando Inductor de Apoptosis Relacionado con TNF/genética , Ligando Inductor de Apoptosis Relacionado con TNF/uso terapéutico , Trasplante Heterólogo , Regulación hacia Arriba/efectos de los fármacos
6.
Artículo en Chino | WPRIM | ID: wpr-616083

RESUMEN

This article briefly summarized the meaning, category and function of qi, tubes and viscera in human body respectively after combining exploring the theories of traditional Chinese medicine(TCM) and clinical practices. Afterward, we put forward the theory of Qi-Tube-Viscera and elaborated its close relationship with the physiological status of the human, and then we thought the relationships of qi, tube and viscera respectively, at last we draw a conclusion that qi, tube and viscera only came from qi. And the clinical guiding significance of the theory of Qi-Tube-Viscera and itsBalanced steady state, Nature and Man in One, State medicine were narrated to demonstrate that new theory of Qi-Tube-Viscera has high signifance in the theory of TCM and clinical practice.

7.
Artículo en Chino | WPRIM | ID: wpr-335764

RESUMEN

To establish an on-line monitoring method for extraction process of Schisandrae Chinensis Fructus, the formula medicinal material of Yiqi Fumai lyophilized injection by combining near infrared spectroscopy with multi-variable data analysis technology. The multivariate statistical process control (MSPC) model was established based on 5 normal batches in production and 2 test batches were monitored by PC scores, DModX and Hotelling T2 control charts. The results showed that MSPC model had a good monitoring ability for the extraction process. The application of the MSPC model to actual production process could effectively achieve on-line monitoring for extraction process of Schisandrae Chinensis Fructus, and can reflect the change of material properties in the production process in real time. This established process monitoring method could provide reference for the application of process analysis technology in the process quality control of traditional Chinese medicine injections.

8.
J Tradit Chin Med ; 36(6): 784-8, 2016 12.
Artículo en Inglés | MEDLINE | ID: mdl-29949712

RESUMEN

OBJECTIVE: To investigate the effect and underlying mechanisms of combined medicated thread moxibustion therapy plus needle picking therapy of Zhuang nationality medicine on antioxidant levels in a rat model of sciatica. METHODS: One hundred Wistar rats, of specific pathogen free level, were randomly divided into five groups: normal control group, model group, medicated thread moxibustion group, needle picking group, and combination group. Each group contained 20 rats. In the model, medicated thread moxibustion, needle picking, and combination groups, sciatica models were established through chronic constriction injury of the sciatic nerve. After the model was established, the rats in the medicated thread moxibustion, needle picking, and combination groups were given the corresponding therapies for 21 days. The control and model groups received no treatment. Reactive oxygen species, superoxide dismutase, malondialdehyde, and total antioxidant capacity changes were determined. Nicotinamide adenine dinucleotide phosphate (NADPH) oxidase subunit NADPH oxidases 4 (NOX4) mRNA expression and the morphology of cells were observed to detect apoptosis of gamma- aminobutyric acid ergic (GABAergic) neurons. RESULTS: Compared with control group, reactive oxygen species and malondialdehyde levels rose significantly in the model group (P < 0.01), while superoxide dismutase and total antioxidant capacity levels were lowered (P < 0.05). Compared with the model group, reactive oxygen species and malondialdehyde decreased in the needle picking group (P < 0.05), while superoxide dismutase levels were increased (P < 0.05); reactive oxygen species and malondialdehyde significantly decreased in the combination group (P < 0.01). In addition, the model group had higher NOX4 mRNA expression than that of the control group (P < 0.05), and the combination group had lower expression levels than that of the model group (P < 0.05). Apoptosis of GABAergic neurons was observed in the model group, and was attenuated after combined therapy. CONCLUSION: The medicated thread moxibustion therapy plus needle picking therapy of Zhuang nationality medicine can prevent oxidative damage in the rat model of sciatica via down-regulating NOX4 expression, improving antioxidant capacity, and inhibiting the oxidative damage pathway of GABAergic neurons.


Asunto(s)
Terapia por Acupuntura , Moxibustión , Ciática/terapia , Puntos de Acupuntura , Animales , Antioxidantes/metabolismo , Terapia Combinada , Modelos Animales de Enfermedad , Femenino , Humanos , Masculino , Malondialdehído/metabolismo , NADPH Oxidasa 4/genética , NADPH Oxidasa 4/metabolismo , Estrés Oxidativo , Ratas , Ratas Wistar , Ciática/genética , Ciática/metabolismo , Superóxido Dismutasa/genética , Superóxido Dismutasa/metabolismo
9.
Artículo en Chino | WPRIM | ID: wpr-307119

RESUMEN

Currently, near infrared spectroscopy (NIRS) has been considered as an efficient tool for achieving process analytical technology(PAT) in the manufacture of traditional Chinese medicine (TCM) products. In this article, the NIRS based process analytical system for the production of salvianolic acid for injection was introduced. The design of the process analytical system was described in detail, including the selection of monitored processes and testing mode, and potential risks that should be avoided. Moreover, the development of relative technologies was also presented, which contained the establishment of the monitoring methods for the elution of polyamide resin and macroporous resin chromatography processes, as well as the rapid analysis method for finished products. Based on author's experience of research and work, several issues in the application of NIRS to the process monitoring and control in TCM production were then raised, and some potential solutions were also discussed. The issues include building the technical team for process analytical system, the design of the process analytical system in the manufacture of TCM products, standardization of the NIRS-based analytical methods, and improving the management of process analytical system. Finally, the prospect for the application of NIRS in the TCM industry was put forward.

10.
Nutrients ; 7(10): 8657-69, 2015 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-26506375

RESUMEN

Millettiae speciosae Champ. Leguminosae (MSC), is a well-known Chinese herb traditionally used as food material and medicine for enhancing physical strength. Our preliminary study found that the aqueous extract of this herb (MSE) had an anti-fatigue effect. In this paper, we further separated MSE into total polysaccharides (MSP) and supernatant (MSS) by alcohol precipitation, and explored which fraction was active for its anti-fatigue effect. Mice were orally administered with MSP or MSS at the doses of 200, 400, and 800 mg/kg for 20 days and the anti-fatigue effect was assessed by exhaustive swimming exercise (ESE). The biochemical parameters related to fatigue after ESE and the in vitro antioxidant activity of active fraction were determined. Our results showed that MSP, instead of MSS, significantly extended the swimming time to exhaustion (p < 0.05), indicating that MSP is responsible for the anti-fatigue effect of MSE. In addition, MSP treatment increased the levels of glucose (Glu) and muscle glycogen, whereas it decreased the accumulations of blood urea nitrogen (BUN) and lactic acid (Lac). Moreover, ESE increased the levels of creatine phosphokinase (CK), lactic dehydrogenase (LDH), and malondialdehyde (MDA) but reduced superoxide dismutase (SOD) and glutathione (GSH) in plasma. In contrast, MSP inhibited all the above changes relating to fatigue. Furthermore, an in vitro antioxidant test revealed that MSP dose-dependently scavenged ·OH and DPPH free radicals. Taken together, these findings strongly suggested that MSP was able to alleviate physical fatigue by increasing energy resources and decreasing accumulation of detrimental metabolites. The antioxidant activity may crucially contribute to the observed anti-fatigue effect of MSP.


Asunto(s)
Antioxidantes/uso terapéutico , Fabaceae/química , Fatiga/tratamiento farmacológico , Resistencia Física/efectos de los fármacos , Fitoterapia , Polisacáridos/uso terapéutico , Animales , Antioxidantes/metabolismo , Antioxidantes/farmacología , Fatiga/metabolismo , Masculino , Ratones , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Polisacáridos/aislamiento & purificación , Polisacáridos/farmacología , Natación
11.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 35(7): 778-82, 2015 Jul.
Artículo en Chino | MEDLINE | ID: mdl-26380437

RESUMEN

OBJECTIVE: To observe the protection of Qingyuan Shenghua Decoction (QSD) on multiple organs of sepsis patients after bone trauma, and to preliminarily explore its mechanism. METHODS: Totally 60 sepsis patients after bone trauma were randomly assigned to the treatment group and the control group according to random digit table, 30 in each group. All patients received routine Western medical treatment. Patients in the treatment group additionally took QSD or were nasally fed with QSD, one dose per day for 1 week. Changes of WBC, oxygenation index (PaO2/FiO2), serum creatinine (SCr), total bilirubin (TBIL), aspartate aminotransferase (AST), fibrinogen (FIB), D-dimer (DD), activated partial thromboplastin time (APTT), pro-calcitonin (PCT), C-reactive protein (CRP), heart rate (HR), mean arterial pressure (MAP), intra-abdominal pressure, scores for Acute Physiology and Chronic Health Evaluation II (APACHE II), sequential organ failure assessment (SOFA) scores were observed before treatment and on day 1, 3 and 7 after treatment. RESULTS: Compared with the control group at the same time point, MAP increased at post-treatment day 1 and 3; CRP, APTT, HR, SCr, TBIL, AST, intra-abdominal pressure at post-treatment day 3 obviously decreased in the treatment group (P < 0.05, P < 0.01). WBC, SOFA scores, PCT, CRP, APACHE II, APTT, D-D, HR, SCr, TBIL, AST and intra-abdominal pressure significantly decreased; FIB, MAP and PaO2/FiO2 obviously increased at post-treatment day 7 (P < 0.05, P < 0.01). CONCLUSION: QSD had good protective effect on multiple organ function in sepsis patients after bone trauma, and its mechanism might be related with effectively clearing endotoxin, alleviating inflammatory reactions, and fighting against coagulation dysfunction.


Asunto(s)
Enfermedades Óseas/complicaciones , Medicamentos Herbarios Chinos/farmacología , Sepsis/tratamiento farmacológico , APACHE , Coagulación Sanguínea , Proteína C-Reactiva/metabolismo , Calcitonina/metabolismo , Medicamentos Herbarios Chinos/uso terapéutico , Productos de Degradación de Fibrina-Fibrinógeno/metabolismo , Humanos , Inflamación , Tiempo de Tromboplastina Parcial , Precursores de Proteínas/metabolismo , Sepsis/etiología
12.
Oncol Rep ; 33(5): 2477-83, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-25812575

RESUMEN

Triple-negative breast cancer (TNBC), characterized by distinct biological and clinicopathological features, has a poor prognosis due to lack of effective therapeutic targets. Our previous data revealed that high levels of USP39 were selectively present in TNBC samples compared with their normal breast tissue samples and USP39 was also expressed at different levels in cultured TNBC cells and normal breast cells. Yet, the underlying cellular and molecular mechanisms of USP39 remain unclear. In the present study, we describe a doxycycline (DOX)-regulated lentiviral vector system expressing shRNA or cDNA of the USP39 gene in the TNBC cell line MDA-MB-231. USP39 expression was knocked down by the miR-30-based inducible lentiviral short hairpin RNA (shRNA) delivery system or overexpressed by the inducible cDNA system. The inducible shRNA-mediated downregulation of USP39 expression markedly reduced the proliferation and colony-forming ability of MDA-MB-231 cells, while overexpression of USP39 by the inducible system did not promote cancer cell proliferation. The lentiviral vector-mediated Tet-on system demonstrated efficient and inducible knockdown of USP39 or overexpression of USP39 in TNBC cells, facilitating a wide variety of applications for gene knockdown and overexpression experiments in gene functional studies in vitro and in vivo.


Asunto(s)
ADN Complementario/genética , Doxiciclina/farmacología , Vectores Genéticos/genética , Lentivirus/genética , ARN Interferente Pequeño/genética , Neoplasias de la Mama Triple Negativas/genética , Proteasas Ubiquitina-Específicas/genética , Mama/efectos de los fármacos , Mama/metabolismo , Línea Celular , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Proliferación Celular/genética , Regulación hacia Abajo/efectos de los fármacos , Regulación hacia Abajo/genética , Femenino , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Regulación Neoplásica de la Expresión Génica/genética , Técnicas de Silenciamiento del Gen/métodos , Células HEK293 , Humanos , MicroARNs/genética
13.
J Ethnopharmacol ; 162: 69-78, 2015 Mar 13.
Artículo en Inglés | MEDLINE | ID: mdl-25557028

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Baicalin and scutellarin are the principal bioactive components of Scutellaria baicalensis Georgi which has extensively been incorporated into heat-clearing and detoxification formulas for the treatment of Helicobacter pylori-related gastrointestinal disorders in traditional Chinese medicine. However, the mechanism of action remained to be defined. AIM OF THE STUDY: To explore the inhibitory effect, kinetics and mechanism of Helicobacter pylori urease (the vital pathogenetic factor for Helicobacter pylori infection) inhibition by baicalin and scutellarin, for their therapeutic potential. MATERIALS AND METHODS: The ammonia formations, indicator of urease activity, were examined using modified spectrophotometric Berthelot (phenol-hypochlorite) method. The inhibitory effect of baicalin and scutellarin was characterized with IC50 values, compared to acetohydroxamic acid (AHA), a well known Helicobacter pylori urease inhibitor. Lineweaver-Burk and Dixon plots for the Helicobacter pylori urease inhibition of baicalin and scutellarin was constructed from the kinetic data. SH-blocking reagents and competitive active site Ni(2+) binding inhibitors were employed for mechanism study. Molecular docking technique was used to provide some information on binding conformations as well as confirm the inhibition mode. Moreover, cytotoxicity experiment using Gastric Epithelial Cells (GES-1) was evaluated. RESULTS: Baicalin and scutellarin effectively suppressed Helicobacter pylori urease in dose-dependent and time-independent manner with IC50 of 0.82±0.07 mM and 0.47±0.04 mM, respectively, compared to AHA (IC50=0.14±0.05 mM). Structure-activity relationship disclosed 4'-hydroxyl gave flavones an advantage to binding with Helicobacter pylori urease. Kinetic analysis revealed that the types of inhibition were non-competitive and reversible with inhibition constant Ki of 0.14±0.01 mM and 0.18±0.02 mM for baicalin and scutellarin, respectively. The mechanism of urease inhibition was considered to be blockage of the SH groups of Helicobacter pylori urease, since thiol reagents (L,D-dithiothreitol, L-cysteine and glutathione) abolished the inhibitory action and competitive active site Ni(2+) binding inhibitors (boric acid and sodium fluoride) carried invalid effect. Molecular docking study further supported the structure-activity analysis and indicated that baicalin and scutellarin interacted with the key residues Cys321 located on the mobile flap through S-H·π interaction, but did not interact with active site Ni(2+). Moreover, Baicalin (at 0.59-1.05 mM concentrations) and scutellarin (at 0.23-0.71 mM concentrations) did not exhibit significant cytotoxicity to GES-1. CONCLUSIONS: Baicalin and scutellarin were non-competitive inhibitors targeting sulfhydryl groups especially Cys321 around the active site of Helicobacter pylori urease, representing potential to be good candidate for future research as urease inhibitor for treatment of Helicobacter pylori infection. Furthermore, our work gave additional scientific support to the use of Scutellaria baicalensis in traditional Chinese medicine (TCM) to treat gastrointestinal disorders.


Asunto(s)
Apigenina/farmacología , Flavonoides/farmacología , Glucuronatos/farmacología , Helicobacter pylori/enzimología , Ureasa/antagonistas & inhibidores , Apigenina/química , Línea Celular , Supervivencia Celular/efectos de los fármacos , Flavonoides/química , Glucuronatos/química , Humanos , Simulación del Acoplamiento Molecular , Ureasa/química , Ureasa/metabolismo
14.
Phytother Res ; 29(1): 67-72, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25243578

RESUMEN

The aim of this study is to evaluate the antibacterial activity and urease inhibitory effects of patchouli alcohol (PA), the bioactive ingredient isolated from Pogostemonis Herba, which has been widely used for the treatment of gastrointestinal disorders. The activities of PA against selected bacteria and fungi were determined by agar dilution method. It was demonstrated that PA exhibited selective antibacterial activity against Helicobacter pylori, without influencing the major normal gastrointestinal bacteria. Noticeably, the antibacterial activity of PA was superior to that of amoxicillin, with minimal inhibition concentration value of 78 µg/mL. On the other hand, PA inhibited ureases from H.pylori and jack bean in concentration-dependent fashion with IC50 values of 2.67 ± 0.79 mM and 2.99 ± 0.41 mM, respectively. Lineweaver-Burk plots indicated that the type of inhibition was non-competitive against H.pylori urease whereas uncompetitive against jack bean urease. Reactivation of PA-inactivated urease assay showed DL-dithiothreitol, the thiol reagent, synergistically inactivated urease with PA instead of enzymatic activity recovery. In conclusion, the selective H.pylori antibacterial activity along with urease inhibitory potential of PA could make it a possible drug candidate for the treatment of H.pylori infection.


Asunto(s)
Antibacterianos/farmacología , Helicobacter pylori/efectos de los fármacos , Lamiaceae/química , Sesquiterpenos/farmacología , Ureasa/antagonistas & inhibidores , Amoxicilina/farmacología , Helicobacter pylori/enzimología , Pruebas de Sensibilidad Microbiana
15.
The Journal of Practical Medicine ; (24): 1176-1179, 2015.
Artículo en Chino | WPRIM | ID: wpr-464356

RESUMEN

Objective To explore whether 5 to -7-day of folic acid supplementation prior to pemetrexed therapy is needed. Methods We retrospectively evaluate the outcomes of non-small cell lung cancer patients received less than the advised folic acid premedication. Seventy patients with Ⅲ-Ⅳ NSCLC were randomly divided into two groups: patients who initiated vitamin supplementation on 7 days before the first dose of pemetrexed (group A) and patients who initiated vitamin supplementation on the day of the first dose of pemetrexed (group B). Results In group A and group B, CR 0 and 0, PR 10 and 8, the response rates of 28.6% and 22.9% were observed, respectively. There was no statistically significant differences between these two groups. No significant differences were observed in the incidence of hematologic and non-hematologic toxicities. Conclusions The initiation of pemetrexed-based chemotherapy does not need to accommodate a vitamin supplementation schedule.

16.
Artículo en Chino | WPRIM | ID: wpr-237940

RESUMEN

<p><b>OBJECTIVE</b>To observe the protection of Qingyuan Shenghua Decoction (QSD) on multiple organs of sepsis patients after bone trauma, and to preliminarily explore its mechanism.</p><p><b>METHODS</b>Totally 60 sepsis patients after bone trauma were randomly assigned to the treatment group and the control group according to random digit table, 30 in each group. All patients received routine Western medical treatment. Patients in the treatment group additionally took QSD or were nasally fed with QSD, one dose per day for 1 week. Changes of WBC, oxygenation index (PaO2/FiO2), serum creatinine (SCr), total bilirubin (TBIL), aspartate aminotransferase (AST), fibrinogen (FIB), D-dimer (DD), activated partial thromboplastin time (APTT), pro-calcitonin (PCT), C-reactive protein (CRP), heart rate (HR), mean arterial pressure (MAP), intra-abdominal pressure, scores for Acute Physiology and Chronic Health Evaluation II (APACHE II), sequential organ failure assessment (SOFA) scores were observed before treatment and on day 1, 3 and 7 after treatment.</p><p><b>RESULTS</b>Compared with the control group at the same time point, MAP increased at post-treatment day 1 and 3; CRP, APTT, HR, SCr, TBIL, AST, intra-abdominal pressure at post-treatment day 3 obviously decreased in the treatment group (P < 0.05, P < 0.01). WBC, SOFA scores, PCT, CRP, APACHE II, APTT, D-D, HR, SCr, TBIL, AST and intra-abdominal pressure significantly decreased; FIB, MAP and PaO2/FiO2 obviously increased at post-treatment day 7 (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>QSD had good protective effect on multiple organ function in sepsis patients after bone trauma, and its mechanism might be related with effectively clearing endotoxin, alleviating inflammatory reactions, and fighting against coagulation dysfunction.</p>


Asunto(s)
Humanos , APACHE , Coagulación Sanguínea , Enfermedades Óseas , Proteína C-Reactiva , Metabolismo , Calcitonina , Metabolismo , Medicamentos Herbarios Chinos , Farmacología , Usos Terapéuticos , Productos de Degradación de Fibrina-Fibrinógeno , Metabolismo , Inflamación , Tiempo de Tromboplastina Parcial , Precursores de Proteínas , Metabolismo , Sepsis , Quimioterapia
17.
Artículo en Chino | WPRIM | ID: wpr-351281

RESUMEN

Based on variation of Pinus massoniana families, heritablility and correlation analysis, the contents of shikimic acid and procyanidine (heritability 0.90, 0.70), dry weight of single branch (heritability 0.60) and and leaf length (heritability 0.46) were screened out as quality, yield and harvest cost traits of Folium Pini, respectively. For the different medicinal application of Folium Pini, varied methods were chosen to estimate weight and construct index equation. Weight adjustment based.on equal emphasis were used as economic weight determining method to select the best families, and the index (accuracy 0. 936 4 and heritability 0. 881 6) obtained was a little better than that obtained by equal emphasis, and much better than that by restricted index. The superior families selected with adjustment weight and equal emphasis were No. 46, 43 and 28. Partial regression were used as economic weight determining method to select the best families,and the index obtained had the highest accuracy (0.941 5) , index heritability (0. 889 9) and the genetic gain of shikimic acid content. The superior families selected with this method were No. 46, 27 and 47. No. 46 was the best families with maximal economic benefit. Our study indicated that suitable method for estimate weight and construct index equation can be applied for better accuracy of superior families selection of P. massoniana.


Asunto(s)
Cruzamiento , Medicamentos Herbarios Chinos , Pinus , Química , Clasificación , Genética , Hojas de la Planta , Química , Plantas Medicinales , Química , Clasificación , Genética
18.
Artículo en Chino | WPRIM | ID: wpr-351232

RESUMEN

After studying the discipline of chemical components distribution in peony root, it was found that the content distribution of albiflorin, paeoniflorin, benzoylpaeoniflorin and paeonol was inhomogeneous in different parts of peony root, as same as in different roots belonging to a same plant. Therefore, in order to minimize the effects of different qualities of materials on experimental result, the content changing percentages of four chemical components was chosen as indicators to study processing method of Paeoniae Radix Alba. The processing technique of Paeoniae Radix Alba was put peony roots in the boiled water for at most ten minutes, and cut them into 2-3 mm slices after peeling the root bark, finally dry them in a oven under 55 degrees C, which was similar to the traditional processing method used in Bozhou. And the peeling, boiling and drying methods would affect the contents of albiflorin, paeoniflorin, benzoylpaeoniflorin and paeonol on several levels.


Asunto(s)
Química Farmacéutica , Métodos , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos , Química , Paeonia , Química , Raíces de Plantas , Química
19.
Artículo en Chino | WPRIM | ID: wpr-330250

RESUMEN

<p><b>OBJECTIVE</b>An UPLC method was developed to evaluate the quality of Paeoniae Radix by simultaneously determining four components, paeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol in Paeoniae Radix Alba decoction pieces.</p><p><b>METHOD</b>The UPLC chromatographic column was ACQUITY UPLC® HSS T3. The mobile phase was acetonitrile-0.05% phosphoric acid water with gradient elution. The column temperature was 30 °C and detection wavelength was 230 nm with a flow rate of 0.4 mL · min(-1). A linear model was obtained through principal component analysis (PCA), and PCA scores were used to evaluate the quality of Radix Paeoniae Alba decoction pieces comprehensively.</p><p><b>RESULT</b>Paeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol could be well separated from other components, and the results of specificity, precision, repeatability, linearity, recovery rate and stability reached the standards, respectively. The content of paeoniflorin in 9 batches of Paeoniae Radix Alba decoction pieces was below the standard given by Chinese Pharmacopoeia (2010 edition). Using the comprehensive scoring method with principal component analysis, the results showed that the samples from Zhejiang province have better quality than those from Anhui and Shandong provinces.</p><p><b>CONCLUSION</b>The method established in this study can effectively determine the content of paeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol, which could be used for quality control of Paeoniae Radix Alba.</p>


Asunto(s)
Medicamentos Herbarios Chinos , Paeonia , Química , Análisis de Componente Principal
20.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 34(12): 1453-6, 2014 Dec.
Artículo en Chino | MEDLINE | ID: mdl-25632745

RESUMEN

OBJECTIVE: To explore the effect of Tongfu Jinghua Decoction (TJD) on hemodynamics and tissue oxygen metabolism in patients with post-traumatic sepsis shock. METHODS: Totally 60 patients were randomly assigned to the treatment group and the control group, 30 in each group. Patients in the treatment group took TJD or were administered with TJD by nasal feeding in combined with conventional Western medical treatment, while patients in the control group only received conventional Western medical treatment. Changes of each index in hemodynamics and tissue oxygen metabolism were observed before treatment, and at 6, 12, 24, and 48 h after treatment. RESULTS: Compared with before treatment in the same group, hemodynamic changes were significantly improved at each time point in the two groups. All indices of tissue oxygen metabolism at each time point of the two groups were significantly improved, except changes of O2 extraction ratio (ER) after treatment in the control group (P < 0.05, P < 0.01). Compared with the control group in the same period, heart rate (HR), systemic vascular resist- ance (SVR), and cardiac output (CO) were significantly improved with statistical difference (P < 0.05, P < 0.01). Mean arterial pressure (MAP), central venous pressure (CVP), and cardiac index (CI) were significantly improved at 6, 12, and 24 h after treatment with statistical difference (P < 0.05, P < 0.01). Each index of tissue oxygen metabolism in the treatment group were all improved at each time point with statistical difference (P < 0.05, P < 0.01). CONCLUSION: TJD combined with conventional Western medical treatment could quickly improve hemodynamics and tissue oxygen metabolism disorder in patients with septic shock, and its curative effect was superior to that of conventional Western medical treatment alone.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Hemodinámica/efectos de los fármacos , Oxígeno/metabolismo , Choque Séptico/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Frecuencia Cardíaca , Humanos , Sepsis , Choque Séptico/metabolismo
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