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1.
Planta Med ; 89(6): 663-673, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-36202093

RESUMEN

Five new diarylbutyrolactones and sesquilignans (1A/1B:  - 4: ), including one pair of enantiomers (1A/1B: ), together with 10 known analogues (5:  - 14: ), were isolated from the whole plants of Saussurea medusa. Compound 1: was found to possess an unusual 7,8'-diarylbutyrolactone lignan structure. Separation by chiral HPLC analysis led to the isolation of one pair of enantiomers, (+)-1A: and (-)-1B: . The structures of the new compounds were elucidated by extensive spectroscopic data. All compounds, except compounds 5, 7: and 9: , were isolated from S. medusa for the first time. Moreover, compounds 1:  -  4, 8: and 10:  - 14: had never been obtained from the genus Saussurea previously. Compounds (+)- 1A, 2, 5, 7: , and 9:  - 11: were found to inhibit the lipopolysaccharide (LPS)-induced release of NO by RAW264.7 cells with IC50 values ranging from 10.1 ± 1.8 to 41.7 ± 2.1 µM. Molecular docking and iNOS expression experiments were performed to examine the interactions between the active compounds and the iNOS enzyme.


Asunto(s)
Lignanos , Saussurea , Ratones , Animales , Lipopolisacáridos , Saussurea/química , Simulación del Acoplamiento Molecular , Lignanos/farmacología , Células RAW 264.7
2.
Int J Mol Sci ; 23(22)2022 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-36430559

RESUMEN

Three pairs of novel enantiomeric 8-O-4' type neolignans (1a/1b−3a/3b), together with seven known analogues (4−10), were isolated from the whole plants of Saussurea medusa. Their structures were elucidated by extensive spectroscopic data analysis and electric circular dichroism (ECD) calculations after chiral separations. All compounds were obtained from S. medusa for the first time, and compounds 1−3 and 5−10 had never been obtained from the genus Saussurea previously. The anti-inflammatory activities of the compounds were evaluated by determining their inhibitory activities on the production of NO and inducible nitric oxide synthase (iNOS) expression in LPS-stimulated RAW 264.7 cells. Compounds (+)-1a, (−)-1b and 5−7 inhibited NO production and had IC50 values ranging from 14.3 ± 1.6 to 41.4 ± 3.1 µM. Compound 7 induced a dose-dependent reduction in the expression of iNOS in LPS-treated RAW 264.7 cells. Molecular docking experiments showed that all active compounds exhibited excellent docking scores (<−7.0 kcal/mol) with iNOS. Therefore, compounds (+)-1a, (−)-1b and 5−7 isolated from the whole plants of S. medusa may have therapeutic potential in inflammatory diseases.


Asunto(s)
Lignanos , Saussurea , Simulación del Acoplamiento Molecular , Lipopolisacáridos/toxicidad , Lignanos/química , Antiinflamatorios/farmacología , Antiinflamatorios/química
3.
Angew Chem Int Ed Engl ; 60(2): 800-805, 2021 01 11.
Artículo en Inglés | MEDLINE | ID: mdl-32918358

RESUMEN

Organic dye based NIR-II fluorescent probes, owing to their high signal-to-background ratio and deeper penetration, are highly useful for deep-tissue high-contrast imaging in vivo. However, it is still a challenge to design activatable NIR-II fluorescent probes. Here, a novel class of polymethine dyes (NIRII-RTs), with bright (quantum yield up to 2.03 %), stable, and anti-solvent quenching NIR-II emission, together with large Stokes shifts, was designed. Significantly, the novel NIR-II dyes NIRII-RT3 and NIRII-RT4, equipped with a carboxylic acid group, can serve as effective NIR-II platforms for the design of activatable bioimaging probes with high contrast. As a proof of concept, a series of target-activatable NIRII-RT probes (NIRII-RT-pH, NIRII-RT-ATP and NIRII-RT-Hg) for pH, adenosine triphosphate (ATP), and metal-ion detection, were synthesized. By applying the NIRII-RT probe, the real-time monitoring of drug-induced hepatotoxicity was realized.


Asunto(s)
Medios de Contraste/química , Colorantes Fluorescentes/química , Imagen Óptica/métodos , Animales , Vasos Sanguíneos/diagnóstico por imagen , Enfermedad Hepática Inducida por Sustancias y Drogas/diagnóstico por imagen , Verde de Indocianina/química , Ganglios Linfáticos/diagnóstico por imagen , Ratones , Polímeros/química , Espectroscopía Infrarroja Corta
4.
J Asian Nat Prod Res ; 21(11): 1043-1051, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30773910

RESUMEN

Two new sesquiterpene pyridine alkaloids, Chinese bittersweet alkaloid A (1) and Chinese bittersweet alkaloid B (2), together with five known compounds 3ß- hydroxyolean-9(11),12-diene, ß-sitosterol, 1ß,2ß,6α,15ß-tetraacetoxy-8ß,9α- dibenzoyloxy-ß-dihydroagarofuran, angulatin A and angulatin J, were isolated from the root barks of Celastrus angulatus. The structures of 1 and 2 were elucidated as 1ß,6α,8ß,9ß-tetraacetoxy-2ß,4α-dihydroxy-15ß-isobutanoyloxy-(3,12)-evoninoyloxy-ß-dihydroagarofuran and 1ß,2ß,6α,8ß,9ß-pentaacetoxy-4α-hydroxy-15ß- isobutanoyloxy- (3,12)- evoninoyloxy-ß-dihydroagarofuran mainly by NMR spectroscopic means.


Asunto(s)
Alcaloides , Celastrus , Sesquiterpenos , Estructura Molecular , Piridinas
5.
J Am Chem Soc ; 140(24): 7716-7722, 2018 06 20.
Artículo en Inglés | MEDLINE | ID: mdl-29792690

RESUMEN

Fluorescent dyes have enabled much progress in the broad range of biomedical fields. However, many commercially available dyes suffer from small Stokes shifts, resulting in poor signal-to-noise ratio and self-quenching on current microscope configurations. In this work, we have developed a general method to significantly increase the Stokes shifts of common fluorophores. By simply appending a 1,4-diethyl-decahydro-quinoxaline (DQ) moiety onto the conjugated structure, we introduced a vibronic backbone that could facilely expand the Stokes shifts, emission wavelength, and photostability of 11 different fluorophores by more than 3-fold. This generalizable method could significantly improve the imaging efficiency of commercial fluorophores. As a demonstration, we showed that the DQ derivative of hemicyanine generated 5-fold signal in mouse models over indocyanine green. Furthermore, the DQ-modified fluorophores could pair with their parent molecules to conduct one-excitation, multiple emission imaging, allowing us to study the cell behavior more robustly. This approach shows promise in generating dyes suitable for super-resolution microscopy and second window near-infrared imaging.

6.
Yao Xue Xue Bao ; 50(4): 475-9, 2015 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-26223131

RESUMEN

A new benzene derivative microintegerrin C (1) and a new norsesquiterpenoid microintegerrin D (2), along with six known compounds (3-8), were isolated and identified from stems and leaves of Micromelum integerrimum by various chromatographies such as silica gel, Sephadex LH-20, RP-18 column chromatography and HPLC. Their structures were mainly identified based on the spectral data analysis such as 1D-, 2D-NMR and HR-EI-MS. All known compounds were isolated from this plant for the first time.


Asunto(s)
Hojas de la Planta/química , Tallos de la Planta/química , Rutaceae/química , Cromatografía Líquida de Alta Presión , Sesquiterpenos/aislamiento & purificación
7.
Yi Chuan ; 35(5): 655-65, 2013 May.
Artículo en Zh | MEDLINE | ID: mdl-23732673

RESUMEN

Bioactive gibberellins (GAs) are a type of important plant growth regulators, which play the key roles in multiple processes, such as seed germination, leaf expansion, flowering, fruit bearing, and stem development. Its biosynthesis is regulated by a variety of enzymes including gibberellin 3-oxidase that is a key rate-limiting enzyme. In Arabidopsis, gibberellin 3-oxidase consists of four members, of which AtGA3OX1 and AtGA3OX2 are highly expressed in stems, suggesting the potential roles in the stem development played by the two genes. To date, there are few studies on AtGA3OX1 and AtGA3OX2 regulating secondary wall thickening in stems. In this study, we used the atga3ox1atga3ox2 double mutant as the materials to study the effects of AtGA3OX1 and AtGA3OX2 genes on secondary wall thickening in stems. The results indicated that simulations repression of AtGA3OX1 and AtGA3OX2 genes resulted in significantly reduction of secondary wall thickening of fiber cells, but not that of vessel cells. Three main components (cellulose, hemicelluloses, and lignin) were also dramatically suppressed in the double mutants. qRT-PCR analysis demonstrated that the expressions of secondary wall biosynthetic genes and the associated transcription factors were obviously affected in AtGA3OX1 and AtGA3OX2 double mutant. Therefore, we presume that Arabidopsis AtGA3OX1 and AtGA3OX2 genes might activate the expression of these transcription factors, thus regulate secondary wall thickening in stems. Together, our results provide a theoretical basis for enhancing the lodging resistance of food crops and improving the biomass of energy plants by genetically engineering Arabidopsis AtGA3OX homologs.


Asunto(s)
Arabidopsis/enzimología , Pared Celular/metabolismo , Oxigenasas de Función Mixta/metabolismo , Tallos de la Planta/metabolismo , Arabidopsis/química , Arabidopsis/genética , Arabidopsis/metabolismo , Pared Celular/genética , Celulosa/metabolismo , Regulación de la Expresión Génica de las Plantas , Oxigenasas de Función Mixta/química , Oxigenasas de Función Mixta/genética , Datos de Secuencia Molecular , Filogenia , Tallos de la Planta/genética , Plantas/clasificación , Plantas/enzimología , Homología de Secuencia de Aminoácido
8.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 33(8): 1054-8, 2013 Aug.
Artículo en Zh | MEDLINE | ID: mdl-24325053

RESUMEN

OBJECTIVE: To observe the efficacy and features of treating early-to-middle stage nontraumatic osteonecrosis of femoral head (NONFH) patients by Jianpi Huogu Recipe (JHR). METHODS: Using retrospective paired control method, early-to-middle stage NONFH patients treated by JHR and followed-up for 2 years were recruited as the test group (47 cases). Those accepted surgery of core decompression, focus debridement and bone graft were recruited as the control group (48 cases). Radiographic images and clinical data of patients were collected before and after treatment. The stable rate and excellent rate of Harris score were taken as efficacy evaluation indicators. RESULTS: (1) There was no statistical difference in excellent rate of Harris score between the two groups (95.74% vs. 79.17%, P > 0.05). But better effects were obtained in the test group in relieving pain, improving joint deformation, joint mobility, and total Harris score (P < 0. 05, P < 0. 01). There was no statistical difference in the stable rate of radiography between the two groups (74.47% vs. 75.00%, P > 0.05). (2) There was no statistical difference in the stable rate of radiography at phase II and Ill [staging by Association Research Circulation Osseous (ARCO)] between the two groups (82.05% vs. 80.00%, 37.50% vs. 50.00%, P > 0.05). (3) The stable rate of radiography and excellent rate of Harris score were obviously higher in ARCO phase II patients than in ARCO phase Il patients (82.05% vs. 37.50%,97.44% vs. 87.50%, P < 0.01). CONCLUSIONS: Equivalent stable rate of radiography to that of surgery could be obtained in treating early-to-middle stage NONFH patients by JHR. But it was better than surgery in relieving pain, improving joint deformation and joint mobility.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Necrosis de la Cabeza Femoral/tratamiento farmacológico , Fitoterapia , Adulto , Estudios de Casos y Controles , Femenino , Necrosis de la Cabeza Femoral/etiología , Humanos , Masculino , Persona de Mediana Edad , Estudios Retrospectivos , Resultado del Tratamiento , Adulto Joven
9.
J Mol Model ; 29(10): 326, 2023 Sep 28.
Artículo en Inglés | MEDLINE | ID: mdl-37770669

RESUMEN

CONTEXT: To comprehend the microscopic property alterations within the ConMoS cluster (n=1-5), this study investigates its internal interactions, electronic characteristics, and orbital correlations employing density functional theory. Structural optimization and theoretical analysis of the cluster are conducted using the Gaussian09 software package, considering various spin multiplicities and employing the B3LYP/def2tzvp quantum chemical method as the computational standard. The outcomes reveal the optimization of the cluster, resulting in 21 stable configurations while continually acquiring energy from the external environment. Analysis of the interaction region indicator functions, the independent gradient model based on Hirshfeld partition, the localized orbital indicator functions, and the electron localization function reveals a trend toward chemical bonding interactions within the interatomic interaction regions. Moreover, the interatomic forces exhibit a high likelihood of engaging in covalent bonding interactions. Both Co and Mo atoms display greater electron delocalization, facilitating the exchange of electrons with the external environment. The paper discuss electron space range, hardness and softness, polarizability, dipole moment, Mulliken population analysis, density of states, HOMO-LUMO diagram, and UV-Vis spectra. Configuration 5a exhibits the broadest electron delocalization and the highest reactivity. It maintains structural stability in external conditions and displays the most polarized molecules. Metal atoms in this cluster exhibit superior mobility compared to non-metal atoms. We elucidate the electron density aggregation region within the cluster. Configuration 1a demonstrates the highest correlation with molar absorption coefficient for its peak. Analyzing the HOMO and LUMO orbital delocalization index and center-of-mass distances revealed that the front orbits of configuration 5a exhibited a broad distribution in space and the minimum center-of-mass distance. METHODS: This study presents a theoretical investigation of Co-Mo-S clusters employing density functional theory (DFT). DFT is a prevalent method for exploring the electronic structure and characteristics of atoms, molecules, and solids. The paper examines cluster attributes encompassing interatomic interactions, electronic properties, and frontier orbitals. Gaussian09 software is employed for optimizing cluster structures, while the analysis is augmented using Multiwfn wave function analysis software. By harnessing these theoretical and computational tools, it aims to delve deeper into cluster properties, yielding valuable insights.

10.
Nat Prod Res ; 37(18): 3074-3082, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36373778

RESUMEN

Objectives: An ethanol extract of the whole plants of Saussurea medusa had been investigated to find novel anti-inflammatory sesquiterpenoids. Methods: Extensive spectroscopic data and chemical methods were applied to elucidate the structures of the compounds. Results: One new megastigmane sesquiterpenoid (1), along with 11 known analogues (2-12), were obtained from S. medusa. All isolates, except compounds 3 and 6, were mentioned from the studied plant for the first time. Compounds 1, 2, 4, 5, 7, 8 and 12 were firstly isolated from the genus Saussurea. Compounds 2, 9 and 10 were found to inhibit the lipopolysaccharide (LPS)-induced release of NO by RAW264.7 cells with IC50 values ranging from 21.1 ± 1.7 to 46.7 ± 1.9 µM. Furthermore, iNOS expression experiment was performed to examine the interactions between the active compounds and the iNOS enzyme.

11.
Huan Jing Ke Xue ; 44(11): 6007-6014, 2023 Nov 08.
Artículo en Zh | MEDLINE | ID: mdl-37973085

RESUMEN

To study the characteristics of atmospheric dust fall pollution in Mentougou District of Beijing, the monthly average monitoring results of 57 atmospheric dust fall samples from two state-controlled ambient air stations in Mentougou District from 2018 to 2022 were collected, and the atmospheric dust fall pollution status and its time variation characteristics in Mentougou District were analyzed. In order to explore the characteristics of chemical components of atmospheric dust fall and the results of quality mass reconstruction and their sources, 57 dust fall samples were collected using the active suction method at the Sanjiadian State-controlled Ambient Air Station. The mass concentration of dust fall and its chemical components were measured, the characteristics of chemical components in atmospheric dust fall were studied, and the mass reconstruction of the main components of atmospheric dust fall was performed using particle mass reconstruction technology. The reliability of the mass reconstruction results and the reasons for its undetermined components were also discussed. The results showed that from 2018 to 2022, the monthly dust fall in Mentougou District of Beijing changed periodically, being the maximum in April or May in spring and the minimum in October or November in autumn, and the maximum monthly dust fall was 3.2 to 8.4 times the minimum monthly dust fall. The order of the quarterly average monthly dust fall was as follows:spring>summer>autumn>winter, and the dust fall mainly came from spring and summer, accounting for 40.1%-43.0% and 23.8%-37.5% of the total annual dust fall, respectively. The annual average monthly dust fall in Mentougou District of Beijing showed a significant downward trend. The dust fall in 2022 had decreased by 52.8% compared with that in 2018, with an average annual decline of 13.2%, which was related to the improvement in the fine management level of urban environmental protection in Beijing in recent years. In 2021, soil dust had a significant impact on dust fall in Mentougou District, with an actual contribution of 44.2%. The chemical components in the atmospheric dust fall in Mentougou District were mainly water-soluble ions, crustal elements, organic carbon(OC), and elemental carbon(EC). The total mass of the measured chemical components accounted for 65.0% of the mass fraction of the dust fall. The secondary organic carbon(SOC) was also an important component of the atmospheric dust fall, and its mass concentration was 13.5 µg·m-3, accounting for 96.4% of the mass fraction of OC. The main components of atmospheric dust fall mass reconstruction were crust element fugitive dust, organic matter(OM), SO42-, NO3-, NH4+, trace elements, EC, and Cl-, with mass concentrations of 34.8, 28.0, 20.6, 15.0, 5.6, 4.3, 3.2, and 2.2 µg·m-3, accounting for 25.5%, 20.6%, 15.1%, 11.1%, 4.1%, 3.2%, 2.3%, and 1.6% of the dust fall quality, respectively. The atmospheric dust fall mainly came from the soil dust, construction cement dust, biomass combustion, waste incineration, and secondary transformation process. The measured mass concentration of atmospheric dust fall had a good correlation with the reconstructed mass concentration of chemical components, and the determination coefficient R2 was 0.8173. The undetermined components in the mass reconstruction results accounted for 16.5% of the dust fall mass, of which the particle bound water(PBW) in the dust fall accounted for 6.2% of the dust fall mass, and the remaining undetermined components might have been related to the unmeasured components, the selected estimation coefficient of OM and crustal elemental dust, the particle size composition, the selected chemical component analysis method, and its measurement error.

12.
Kaohsiung J Med Sci ; 38(9): 858-868, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35866347

RESUMEN

This study aimed to determine whether regular recruitment maneuvers (RMs) are essential for obese patients (OPs) undergoing elective laparoscopic bariatric surgery (LBS) during intraoperative ventilation with individualized positive end-expiratory pressure (PEEP). Patients were randomly assigned to two arms: the RM + PEEP-EIT arm consisted of individualized PEEP titrated by electrical impedance tomography (EIT) with two regular RMs and the PEEP-EIT arm consisted of individualized PEEP titrated by EIT without additional RMs. For these two arms together, EIT-guided PEEP varied among individuals. The partial pressure of oxygen in arterial blood to fractional inspired oxygen (PaO2 /FiO2 ) ratio in the RM + PEEP-EIT arm was higher than that in the PEEP-EIT arm at 1 h after pneumoperitoneum (p = 0.024) and at the end of surgery (p = 0.035). There was no great difference in the PaO2 /FiO2 ratio between these two arms when measured 5 min prior to postanesthesia care unit (PACU) departure and on postoperative day 1. Compared with the PEEP-EIT arm, patients in the RM + PEEP-EIT arm had significantly higher intraoperative dynamic respiratory system compliance (p < 0.001) but consumed more vasopressors (p = 0.036). Postoperative pulmonary complications occurred in 1 of 29 patients in the RM + PEEP-EIT arm compared with 2 of 31 patients in the PEEP-EIT arm. Regular lung RMs can improve intraoperative oxygenation and respiratory system compliance among OPs undergoing LBS with EIT-guided individual PEEP. However, the improvement might disappear before leaving the PACU, and regular RMs resulted in more vasopressor consumption.


Asunto(s)
Cirugía Bariátrica , Respiración con Presión Positiva , Impedancia Eléctrica , Humanos , Obesidad/complicaciones , Obesidad/cirugía , Oxígeno , Respiración con Presión Positiva/métodos , Complicaciones Posoperatorias
13.
Chem Commun (Camb) ; 55(76): 11462-11465, 2019 Sep 28.
Artículo en Inglés | MEDLINE | ID: mdl-31490473

RESUMEN

We report here a single-benzene based fluorescent framework, amino-terephthalonitrile, denoted SB-Fluor. This scaffold displays versatile emission wavelength tunability via structure modification, covering the full visible light spectrum, both in the solution and solid state. Moreover, one molecule, SBF3, exhibits polymorphism-dependent reversible mechanochromic luminescence.

14.
Water Res ; 88: 758-765, 2016 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-26595097

RESUMEN

The self-alkalization of denitrifying automatic circulation (DAC) reactor resulted in a large increase of pH up to 9.20 and caused a tremendous accumulation of nitrite up to 451.1 ± 49.0 mgN L(-1) at nitrate loading rate (NLR) from 35 kgN m(-3) d(-1) to 55 kgN m(-3) d(-1). The nitrite accumulation was greatly relieved even at the same NLR once the pH was maintained at 7.6 ± 0.2 in the system. Enzymatic assays indicated that the long-term bacterial exposure to high pH significantly inhibited the activity of copper type nitrite reductase (NirK) rather than the cytochrome cd1 type nitrite reductase (NirS). The terminal restriction fragment length polymorphism (T-RFLP) analysis revealed that the dominant denitrifying bacteria shifted from the NirS-containing Thauear sp. 27 to the NirK-containing Hyphomicrobium nitrativorans strain NL23 during the self-alkalization. The significant nitrite accumulation in the high-rate denitrification system could be therefore, due to the inhibition of Cu-containing NirK by high pH from the self-alkalization. The results suggest that the NirK-containing H. nitrativorans strain NL23 could be an ideal functional bacterium for the conversion of nitrate to nitrite, i.e. denitritation, which could be combined with anaerobic ammonium oxidation (Anammox) to develop a new process for nitrogen removal from wastewater.


Asunto(s)
Bacterias/metabolismo , Desnitrificación , Nitrato-Reductasa/metabolismo , Nitrito Reductasas/metabolismo , Eliminación de Residuos Líquidos/métodos , Bacterias/enzimología , Bacterias/genética , Bacterias/aislamiento & purificación , ADN Bacteriano/genética , Concentración de Iones de Hidrógeno , Datos de Secuencia Molecular , Nitritos/metabolismo , Óxido Nitroso/metabolismo , Filogenia , Reacción en Cadena de la Polimerasa , Polimorfismo de Longitud del Fragmento de Restricción , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN
15.
Brain Res ; 1583: 79-88, 2014 Oct 02.
Artículo en Inglés | MEDLINE | ID: mdl-25084036

RESUMEN

Activation of signal transducer and activator of transcription-3 (STAT3) is suggested to be critically involved in the development of chronic pain, but the complex regulation of STAT3-dependent pathway and the functional significance of inhibiting this pathway during the development of neuropathic pain remain elusive. To evaluate the contribution of the JAK2/STAT3 pathway to neuropathic pain and the potentiality of this pathway as a novel therapeutic target, we examined the effects of the STAT3 inhibitor WP1066 by intrathecal administration in a rat model of bilateral chronic constriction injury (bCCI). The pain behavior tests were performed before the surgery and on postoperative day 3, 7, 14 and 21. L4-L6 dorsal spinal cord were harvested at each time point. Both RT-PCR and Western blot were performed to evaluate the activation of JAK2/STAT3 pathway. To observe the influence of WP1066 on neuropathic pain and its molecular mechanism, WP1066 (10 µl, 10 mmol/L in DMSO) or the same capacity of DMSO as the control were applied through the intrathecal tube on the day before bCCI surgery, and on the postoperative day 3 and 5. Behavioral tests were performed to observe the therapeutic effect on mechanical, thermal and cold hyperalgesia. L4-L6 dorsal spinal cord was harvested on postoperative day fourteen, followed by RT-PCR and Western blot evaluation of the JAK2/STAT3 pathway activation. The mechanical, thermal and cold hyperalgesia of the bCCI rats were significantly decreased when compared with the Sham or the Naïve group at each postoperative time point (P<0.05). JAK2 mRNA and STAT3 mRNA were significantly increased in the bCCI rats, accompanied by SOCS3 mRNA with a similar tendency. Western blot analysis showed that JAK2 and phosphorylated STAT3 increased significantly since 3 days after bCCI. JAK2 peaked on postoperative day 14 while phosphorylated STAT3 peaked on postoperative day 7 and gradually decreased thereafter and SOCS3׳s peak level on postoperative day 3. When WP1066 were administered intrathecally, the pain behaviors of the bCCI rats were significantly improved (P<0.05). WP1066 also inhibited the mRNA level of JAK2, STAT3 and SOCS3 in bCCI rats significantly, together with the protein level of JAK2, phosphorylated STAT3 and SOCS3 on postoperative day 14 as well. Our results found that the JAK2/STAT3 pathway in the spinal cord dorsal horn was significantly activated in the bCCI neuropathic pain rats. WP1066, which inhibited the STAT3 pathway specifically, could partially alleviate the pain behavior of the bCCI rats. So it may serve as a novel therapeutic strategy against neuropathic pain.


Asunto(s)
Analgésicos/farmacología , Neuralgia/tratamiento farmacológico , Piridinas/farmacología , Factor de Transcripción STAT3/antagonistas & inhibidores , Tirfostinos/farmacología , Animales , Enfermedad Crónica , Frío , Constricción Patológica , Modelos Animales de Enfermedad , Femenino , Calor , Hiperalgesia/tratamiento farmacológico , Hiperalgesia/fisiopatología , Janus Quinasa 2/metabolismo , Vértebras Lumbares , Neuralgia/fisiopatología , ARN Mensajero/metabolismo , Distribución Aleatoria , Ratas Sprague-Dawley , Factor de Transcripción STAT3/metabolismo , Transducción de Señal , Médula Espinal/efectos de los fármacos , Médula Espinal/fisiopatología , Proteína 3 Supresora de la Señalización de Citocinas , Proteínas Supresoras de la Señalización de Citocinas/metabolismo , Tacto
16.
Chin J Nat Med ; 12(8): 619-22, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25156288

RESUMEN

AIM: To investigate the chemical and bioactive constituents from the stems and leaves of Micromelum integerrimum. METHOD: The chemical constituents were isolated and purified by silica gel, Sephadex LH-20, and HPLC. Their structures were mainly elucidated on the basis of extensive 1D- and 2D-NMR spectroscopy and mass spectrometry. Their cytotoxicity and antimicrobial activities were tested by the SRB and turbidimetric methods, respectively. RESULTS: Two new phenylpropanoids and two known coumarins were obtained, and their structures were identified as microintegerrin A (1), microintegerrin B (2), scopoletin (3), and scopolin (4). All of the compounds were tested for their cytotoxicity against three cancer cell lines (HeLa, A549, and BGC-823) and for antimicrobial activity against the fungus Candida albicans and the bacterium Staphylococcus aureus. CONCLUSION: Two new phenylpropanoids 1 and 2 were isolated and identified from the stems and leaves of M. intgerrimum. None of the compounds showed cytotoxic or antimicrobial activity at the tested concentration of 20 µg·mL(-1).


Asunto(s)
Fenilpropionatos/aislamiento & purificación , Extractos Vegetales/química , Rutaceae/química , Candida albicans/efectos de los fármacos , Cumarinas/aislamiento & purificación , Cumarinas/farmacología , Glucósidos/aislamiento & purificación , Glucósidos/farmacología , Células HeLa , Humanos , Estructura Molecular , Fenilpropionatos/química , Fenilpropionatos/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta , Tallos de la Planta , Escopoletina/aislamiento & purificación , Escopoletina/farmacología , Staphylococcus aureus/efectos de los fármacos
17.
Chin J Integr Med ; 18(5): 378-84, 2012 May.
Artículo en Inglés | MEDLINE | ID: mdl-22549392

RESUMEN

OBJECTIVE: To study the mechanism of Huogu I formula (I) in treating osteonecrosis of femoral head. METHODS: Forty-eight healthy female Leghorn chickens were randomly divided into control group, model group and Huogu I group, and each group consisted of 16 chickens. At the meantime of model establishment, chickens of the Huogu I group were administrated with decoction, while the model and control group with distilled water by gavage. At the 8th and 16th week after medication, blood samples were obtained for blood lipid detection while both sides of femoral head were harvested for the rest of examinations. Specifically, expressions of bone morphogenetic protein-2 (BMP2), transforming growth factor beta1 (TGFß(1)), Smad4 and Smad7 were evaluated by immunohistochemistry, while expression of osteoprotegerin/receptor activator of nuclear factor kappaB ligand (OPG/RANKL) mRNA was detected by in situ hybridization. RESULTS: Compared with the control group, serum levels of total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) in the model group rose significantly. Positive cell counting of BMP2, TGFß(1), Smad4 and OPG in femoral head of the model group dropped prominently. Positive cell counting of Smad7 and RANKL increased dramatically. In contrast with the model group, levels of TC, TG and LDL-C in Huogu I group reduced significantly. Positive cell counting of BMP2, TGFß(1), Smad4 and OPG in femoral head of the Huogu I group increased prominently. Indices of Smad7 and RANKL both decreased significantly. Especially at the 8th week, these variations were more significant. CONCLUSION: Huogu I formula is effective in promoting repair of necrotic femoral head by regulating the expressions of BMP2, TGFß(1), Smads and OPG/RANKL of osteoclast in femoral head.


Asunto(s)
Regeneración Ósea/efectos de los fármacos , Medicamentos Herbarios Chinos/farmacología , Necrosis de la Cabeza Femoral/inducido químicamente , Necrosis de la Cabeza Femoral/tratamiento farmacológico , Esteroides/farmacología , Animales , Proteína Morfogenética Ósea 2/metabolismo , Regeneración Ósea/fisiología , Pollos , Condrocitos/metabolismo , Modelos Animales de Enfermedad , Femenino , Necrosis de la Cabeza Femoral/metabolismo , Metabolismo de los Lípidos/fisiología , Osteocitos/metabolismo , Osteoprotegerina/genética , Osteoprotegerina/metabolismo , Receptor Activador del Factor Nuclear kappa-B/genética , Receptor Activador del Factor Nuclear kappa-B/metabolismo , Proteína Smad4/metabolismo , Proteína smad7/metabolismo , Factor de Crecimiento Transformador beta1/metabolismo
18.
Int J Syst Evol Microbiol ; 57(Pt 5): 911-915, 2007 May.
Artículo en Inglés | MEDLINE | ID: mdl-17473232

RESUMEN

Two moderately halophilic strains, SL014B-69(T) and SL014B-62A2, were isolated from a saline soil contaminated with crude oil in Gudao in the coastal Shengli oilfield in China; the isolates were Gram-negative, rod-shaped and carried lateral flagella. Growth occurred at NaCl concentrations of 1-20 % (w/v), at temperatures of 10-42 degrees C and at pH 8.0-9.0. Strain SL014B-69(T) had C(18 : 1)omega7c (28.61 %), C(19 : 1) cyclo omega7c (27.97 %), C(16 : 0) (19.66 %) and C(12 : 0) 3-OH (8.87 %) as the predominant fatty acids and Q9 as the major ubiquinone, with the G+C content of genomic DNA being 64.0 mol%. Phylogenetic analyses based on 16S rRNA gene sequences indicated that the two strains belonged to genus of Halomonas in the Gammaproteobacteria, with the highest 16S rRNA gene sequence similarities of 96.4 % with Halomonas campisalis ATCC 700597(T) and 96.0 % with Halomonas desiderata FB2(T). DNA-DNA relatedness of strain SL014B-69(T) with strain SL014B-62A2, H. campisalis ATCC 700597(T) and H. desiderata DSM 9502(T) was 97.4, 42.9 and 36.8 %, respectively. On the basis of these data, a novel species of the genus Halomonas, Halomonas gudaonensis sp. nov., is proposed for strain SL014B-69(T) and SL014B-62A2. The type strain is SL014B-69(T) (=LMG 23610(T)=CGMCC 1.6133(T)).


Asunto(s)
Halomonas/clasificación , Halomonas/aislamiento & purificación , Microbiología del Suelo , Técnicas de Tipificación Bacteriana , Composición de Base , China , ADN Bacteriano/química , ADN Bacteriano/genética , ADN Ribosómico/química , ADN Ribosómico/genética , Ácidos Grasos/análisis , Flagelos/ultraestructura , Genes de ARNr , Violeta de Genciana , Halomonas/química , Halomonas/fisiología , Concentración de Iones de Hidrógeno , Microscopía Electrónica de Rastreo , Microscopía Electrónica de Transmisión , Datos de Secuencia Molecular , Hibridación de Ácido Nucleico , Petróleo/microbiología , Fenazinas , Filogenia , Quinonas/análisis , ARN Bacteriano/genética , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN , Homología de Secuencia de Ácido Nucleico , Cloruro de Sodio/metabolismo , Temperatura
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