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1.
J Org Chem ; 89(6): 4085-4097, 2024 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-38394366

RESUMEN

A palladium-catalyzed annulative π-extension reaction of bay-iodinated triphenylenes with aryl iodides/o-chloroaromatic carboxylic acids was developed. This approach enabled the synthesis of diverse polycyclic aromatic compounds, including dibenzo[fg,op]tetracenes, azadibenzo[fg,op]tetracenes, and tribenzo[a,g,m]coronenes. Initial studies indicate that the resulting product, 2,3,8,9,14,15-hexakis(decyloxy)tribenzo[a,g,m]coronene, exhibits good liquid-crystalline properties.

2.
Huan Jing Ke Xue ; 44(8): 4698-4705, 2023 Aug 08.
Artículo en Chino | MEDLINE | ID: mdl-37694662

RESUMEN

Carbon (C), nitrogen (N), and phosphorus (P) are important nutrients, and their ecological stoichiometric characteristics can reflect the quality and fertility capacity of soil, which is critical to understanding the stable mechanisms of estuarine wetland ecosystems. Under global changes, the increase in salinity and flooding caused by sea level rise will lead to changes in biogeochemical processes in estuarine wetlands, which is expected to affect the ecological stoichiometric characteristics of soil C, N, and P and ultimately interfere with the stability of wetland ecosystems. However, it remains unclear how the C, N, and P ecological stoichiometric characteristics respond to the water-salt environment in estuarine wetlands. We differentiated changes in the C, N, and P ecological stoichiometric characteristics through an ex-situ culture experiment for 23 months in the Yellow River Estuary Wetland. The five sites with distinct tidal hydrology were selected to manipulate translocation of soil cores from the freshwater marsh to high-, middle-, and low-tidal flats in June 2019. The results showed that soil water content (SWC); electrical conductivity (EC); and C, N, and P ecological stoichiometric characteristics of freshwater marsh soil significantly changed after translocation for 23 months. SWC decreased on the high- and middle-tidal flats (P<0.05) and increased on the low-tidal flat (P<0.05). EC increased to different degrees on all three tidal flats (P<0.05). Soil total organic carbon (TOC) and total nitrogen (TN) were significantly lower on the high-tidal flat (P<0.05), whereas total phosphorus (TP) was significantly lower on the middle- and high-tidal flats (P<0.05). C:N was decreased on the high- and middle-tidal flats (P<0.05); C:P and N:P were lower on the high-tidal flat; and all C, N, and P ecological stoichiometric characteristics showed no change on the low-tidal flat (P>0.05). Pearson's analysis showed that the ecological stoichiometric characteristics of C, N, and P were related to some properties of soil over the culture sites. The PLS-SEM model showed that the water-salt environment had different effects on soil C:N, C:P, and N:P through the main pathways of negative effects on soil TOC and TP. The results suggest that sea level rise may impact the C, N, and P ecological stoichiometric characteristics in freshwater marsh soil, resulting in some possible changes in the nutrient cycles of estuarine wetlands.

3.
Front Psychol ; 14: 1185415, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37564315

RESUMEN

Sailing has gained an increasing attention among children and adolescents in China, which raised a strong need for sail courses through physical education (PE). However, challenges in teaching practice arise with rapid development of the sport. In the current study, we proposed a perspective that virtual reality (VR) technology makes high-quality sail education accessible for students. Critical analysis summarized the prominent features that enhance sail education, including immersive experience, interactive learning, the first-person view, and practice under well-controlled conditions. Further, research on VR sport training indicated successful transfer from virtual environment to real situation. Specifically, significant improvement in skill performance and tactical behaviors were identified, which was attributed to the enhanced perception-action coupling after VR training. Additionally, VR-based coding programs provide students with affordances of designing the virtual environment. The content design education promotes comprehension and application of knowledge and theories when students develop the simulated environment with a high level of presence. Therefore, VR technology is a promising instrument to meet the increasing demand on sail education. While VR enriches educational resources for a large class size, the interdisciplinary feature of VR-based sail course can attract students with different study interests and backgrounds to the class.

4.
Org Biomol Chem ; 20(44): 8657-8661, 2022 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-36281731

RESUMEN

A palladium-catalyzed bay-region annulative π-extension reaction of o-halobiphenyls with o-chloropyridinecarboxylic acids was developed. The reaction was carried out with a 1 : 1 ratio of substrates. A variety of azatriphenylene derivatives could be synthesized by this approach. This transformation could be applied to the synthesis of ionic liquid-crystalline molecules.


Asunto(s)
Compuestos Aza , Paladio , Paladio/química , Catálisis , Crisenos
5.
Zhen Ci Yan Jiu ; 47(9): 809-13, 2022 Sep 25.
Artículo en Chino | MEDLINE | ID: mdl-36153456

RESUMEN

OBJECTIVE: To observe the effects of thunder-fire moxibustion on the visual analogue scale (VAS) score, Young's modulus of multifidus and 6 m walking speed in the patients of osteoporosis with low skeletal muscle mass. METHODS: Sixty patients of osteoporosis with low skeletal muscle mass were randomly divided into a medication group (30 cases) and a medication+thunder-fire moxibustion group (30 cases). In the medication group, caltrate was prescribed for oral administration, 2 tablets/day (600 mg/tablet), for 4 weeks. In the medication+thunder-fire moxibustion group, on the base of oral administration with caltrate, thunder-fire moxibustion was exerted at Mingmen (GV4), Yaoyangguan(GV3), and bilateral Shenshu (BL23), Ganshu (BL18) and Dachangshu (BL25), 30 minutes at GV4, GV3 and BL18, and another 30 minutes at BL23 and BL25, once every other day, 3 times a week for 4 weeks. Before and after the treatment, VAS score, Young's modulus of the 4th lumbar multifidus and the average speed of 6 m walking were assessed. RESULTS: After the treatment, the VAS score was decreased (P<0.05, P<0.01) and the speed of 6 m walking was increased (P<0.05, P<0.01) in both groups in comparison with their own pre-treatment. Compared with the medication group, VAS score was decreased remarkably (P<0.05) and the speed of 6 m walking remarkably increased (P<0.01) in the medication+thunder-fire moxibustion group after the treatment. Self-comparison showed that, compared with the same side before the treatment, the value of Young's modulus after the treatment was decreased on both sides in the medication+thunder-fire moxibustion group (P<0.01). After the treatment, compared with the medication group on the same side, the value of Young's modulus was decreased on both sides (P<0.01) in the medication+thunder-fire moxibustion group. CONCLUSION: Thunder-fire moxibustion can relieve pain intensity, decrease the tension of the multifidus, and increase the walking speed.


Asunto(s)
Moxibustión , Osteoporosis , Puntos de Acupuntura , Humanos , Osteoporosis/terapia , Dimensión del Dolor , Músculos Paraespinales
6.
Front Microbiol ; 12: 631445, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34267732

RESUMEN

Marine sponges are known to host a complex microbial consortium that is essential to the health and resilience of these benthic invertebrates. These sponge-associated microbes are also an important source of therapeutic agents. The Neptune's Cup sponge, Cliona patera, once believed to be extinct, was rediscovered off the southern coast of Singapore in 2011. The chance discovery of this sponge presented an opportunity to characterize the prokaryotic community of C. patera. Sponge tissue samples were collected from the inner cup, outer cup and stem of C. patera for 16S rRNA amplicon sequencing. C. patera hosted 5,222 distinct OTUs, spanning 26 bacterial phyla, and 74 bacterial classes. The bacterial phylum Proteobacteria, particularly classes Gammaproteobacteria and Alphaproteobacteria, dominated the sponge microbiome. Interestingly, the prokaryotic community structure differed significantly between the cup and stem of C. patera, suggesting that within C. patera there are distinct microenvironments. Moreover, the cup of C. patera had lower diversity and evenness as compared to the stem. Quorum sensing inhibitory (QSI) activities of selected sponge-associated marine bacteria were evaluated and their organic extracts profiled using the MS-based molecular networking platform. Of the 110 distinct marine bacterial strains isolated from sponge samples using culture-dependent methods, about 30% showed quorum sensing inhibitory activity. Preliminary identification of selected QSI active bacterial strains revealed that they belong mostly to classes Alphaproteobacteria and Bacilli. Annotation of the MS/MS molecular networkings of these QSI active organic extracts revealed diverse classes of natural products, including aromatic polyketides, siderophores, pyrrolidine derivatives, indole alkaloids, diketopiperazines, and pyrone derivatives. Moreover, potential novel compounds were detected in several strains as revealed by unique molecular families present in the molecular networks. Further research is required to determine the temporal stability of the microbiome of the host sponge, as well as mining of associated bacteria for novel QS inhibitors.

8.
J Nat Prod ; 84(4): 1067-1077, 2021 04 23.
Artículo en Inglés | MEDLINE | ID: mdl-33666437

RESUMEN

Five new aconitine-type C19-diterpenoid alkaloids, apetalrines A-E (1-5), were isolated from Aconitum apetalum. Their structures were determined by analysis of 1D and 2D NMR, IR, and HRESIMS data. Semisynthesis of apetalrine B (2) from its parent compound aconorine was achieved to confirm the structure proposed. Twenty derivatives of 2 (11a-11l, 12a, 12b, 12d, 12e, 12j, 12k, 12m, 12n) were synthesized via a unified approach relying on simple coupling reactions. The evaluation of neuroprotective effects of compounds (1-5, 11b, 11c, 11f-11i, 12a, 12b, 12d, 12e, 12k, 12m, 12n) with low cytotoxicity revealed compound 2 to exhibit good neuroprotective effects in H2O2-treated SH-SY5Y cells at a concentration of 50 µM. A series of studies using flow cytometry, staining, and Western blotting on 2 indicated that its neuroprotective effects may arise from inhibiting cell apoptosis.


Asunto(s)
Aconitum/química , Alcaloides/farmacología , Diterpenos/farmacología , Fármacos Neuroprotectores/farmacología , Alcaloides/química , Apoptosis/efectos de los fármacos , Línea Celular , China , Diterpenos/química , Humanos , Estructura Molecular , Fármacos Neuroprotectores/química , Raíces de Plantas/química
9.
Exp Mol Med ; 53(2): 235-249, 2021 02.
Artículo en Inglés | MEDLINE | ID: mdl-33558591

RESUMEN

Dopamine D1 receptor (D1DR) and D2 receptor (D2DR) are closely associated with pain modulation, but their exact effects on neuropathic pain and the underlying mechanisms remain to be identified. Our research revealed that intrathecal administration of D1DR and D2DR antagonists inhibited D1-D2DR complex formation and ameliorated mechanical and thermal hypersensitivity in chronic constriction injury (CCI) rats. The D1-D2DR complex was formed in the rat spinal cord, and the antinociceptive effects of D1DR and D2DR antagonists could be reversed by D1DR, D2DR, and D1-D2DR agonists. Gαq, PLC, and IP3 inhibitors also alleviated CCI-induced neuropathic pain. D1DR, D2DR, and D1-D2DR complex agonists all increased the intracellular calcium concentration in primary cultured spinal neurons, and this increase could be reversed by D1DR, D2DR antagonists and Gαq, IP3, PLC inhibitors. D1DR and D2DR antagonists significantly reduced the expression of p-PKC γ, p-CaMKII, p-CREB, and p-MAPKs. Levo-corydalmine (l-CDL), a monomeric compound in Corydalis yanhusuo W.T. Wang, was found to obviously suppress the formation of the spinal D1-D2DR complex to alleviate neuropathic pain in CCI rats and to decrease the intracellular calcium concentration in spinal neurons. l-CDL-induced inhibition of p-PKC γ, p-MAPKs, p-CREB, and p-CaMKII was also reversed by D1DR, D2DR, and D1-D2DR complex agonists. In conclusion, these results indicate that D1DR and D2DR form a complex and in turn couple with the Gαq protein to increase neuronal excitability via PKC γ, CaMKII, MAPK, and CREB signaling in the spinal cords of CCI rats; thus, they may serve as potential drug targets for neuropathic pain therapy.


Asunto(s)
Neuralgia/etiología , Neuralgia/metabolismo , Receptores de Dopamina D1/metabolismo , Receptores de Dopamina D2/metabolismo , Células Receptoras Sensoriales/metabolismo , Traumatismos de la Médula Espinal/etiología , Traumatismos de la Médula Espinal/metabolismo , Animales , Conducta Animal , Biomarcadores , Calcio/metabolismo , Células Cultivadas , Modelos Animales de Enfermedad , Susceptibilidad a Enfermedades , Antagonistas de Dopamina/farmacología , Antagonistas de los Receptores de Dopamina D2/farmacología , Masculino , Complejos Multiproteicos/metabolismo , Neuralgia/diagnóstico , Dimensión del Dolor , Fosforilación , Unión Proteica , Ratas , Receptores de Dopamina D1/antagonistas & inhibidores , Transducción de Señal , Traumatismos de la Médula Espinal/complicaciones , Traumatismos de la Médula Espinal/diagnóstico
10.
J Adv Res ; 28: 139-148, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33364051

RESUMEN

INTRODUCTION: Spinal N-methyl-D-aspartate receptor (NMDAR) is vital in chronic pain, while NMDAR antagonists have severe side effects. NMDAR has been reported to be controlled by G protein coupled receptors (GPCRs), which might present new therapeutic targets to attenuate chronic pain. Dopamine receptors which belong to GPCRs have been reported could modulate the NMDA-mediated currents, while their exact effects on NMDAR in chronic bone cancer pain have not been elucidated. OBJECTIVES: This study was aim to explore the effects and mechanisms of dopamine D1 receptor (D1DR) and D2 receptor (D2DR) on NMDAR in chronic bone cancer pain. METHODS: A model for bone cancer pain was established using intra-tibia bone cavity tumor cell implantation (TCI) of Walker 256 in rats. The nociception was assessed by Von Frey assay. A range of techniques including the fluorescent imaging plate reader, western blotting, and immunofluorescence were used to detect cell signaling pathways. Primary cultures of spinal neurons were used for in vitro evaluation. RESULTS: Both D1DR and D2DR antagonists decreased NMDA-induced upregulation of Ca2+ oscillations in primary culture spinal neurons. Additionally, D1DR/D2DR antagonists inhibited spinal Calcitonin Gene-Related Peptide (CGRP) and c-Fos expression and alleviated bone cancer pain induced by TCI which could both be reversed by NMDA. And D1DR/D2DR antagonists decreased p-NR1, p-NR2B, and Gαq protein, p-Src expression. Both Gαq protein and Src inhibitors attenuated TCI-induced bone cancer pain, which also be reversed by NMDA. The Gαq protein inhibitor decreased p-Src expression. In addition, D1DR/D2DR antagonists, Src, and Gαq inhibitors inhibited spinal mitogen-activated protein kinase (MAPK) expression in TCI rats, which could be reversed by NMDA. CONCLUSIONS: Spinal D1DR/D2DR inhibition eliminated NMDAR-mediated spinal neuron activation through Src kinase in a Gαq-protein-dependent manner to attenuate TCI-induced bone cancer pain, which might present a new therapeutic strategy for bone cancer pain.

11.
Artículo en Chino | WPRIM (Pacífico Occidental) | ID: wpr-906275

RESUMEN

Objective:To explore the regulatory effect of modified Liu Junzitang on the immune function, nutritional status and intestinal microecology in advanced gastric cancer patients with syndrome of deficiency of Qi and blood. Method:The 86 advanced gastric cancer patients with syndrome of deficiency of Qi and blood were randomly divided into control group and observation group according to their admission numbers, with 43 cases in each group. The control group was given Yiqi Yangxue oral liquid on the basis of basic treatment while the observation group was given modified Liu Junzitang. After 4 weeks, compare the clinical efficacy of two groups of patients, traditional Chinese medicine (TCM) syndrome score, gastrointestinal function recovery, adverse reaction and quality of life, immune function, T cell subsets CD3<sup>+</sup>, CD4<sup>+</sup>, CD8<sup>+</sup>, C<sub>3</sub> and C<sub>4</sub> levels, immunoglobulin A (IgA), immunoglobulin G (IgG), immunoglobulin M (IgM), nutritional status: albumin (propagated), prealbumin (PA), serum total protein (TP) and hemoglobin (Hb) content changes, the intestinal micro ecology: <italic>Bifidobacterium</italic>, <italic>Lactobacillus</italic>, <italic>Enterococcus aureus</italic>, <italic>Escherichia coli</italic> content changes. Result:The total effective rate of the observation group was 95.35% (41/43), which was significantly higher than 79.07% (34/43) of the control group (<italic>χ<sup>2</sup></italic>=5.108,<italic>P</italic><0.05), after treatment, the TCM syndromes such as dizziness, pale complexion, palpitation, shortness of breath and fatigue in the observation group were significantly lower than those in the control group (<italic>P</italic><0.05), the bowel sound recovery, exhaust and defecation time of the observation group were significantly lower than those of the control group (<italic>P</italic><0.05), the quality of life scores in the observation group, such as the nature-to-human correspondence, form and spirit integration, specific modules, functional areas, and overall health score, were significantly higher than those in control group (<italic>P</italic><0.05), the CD3<sup>+</sup>, CD4<sup>+</sup>, CD4<sup>+</sup>/CD8<sup>+</sup>, C<sub>3</sub>, C<sub>4</sub>, IgA, immune function indexes such as IgG and IgM were significantly higher than those of the control group, and the CD8<sup>+</sup> level was lower than which of control group (<italic>P</italic><0.05), the nutritional status levels such as Alb, PA, TP and Hb in the observation group were significantly higher than those of the control group (<italic>P</italic><0.05), <italic>Bifidobacterium</italic>, <italic>Lactobacillus</italic>, and <italic>E. faecalis </italic>in the observation group were higher than those in the control group, and <italic>E. coli</italic> was lower than the control group (<italic>P</italic><0.05), the adverse reaction rate of the observation group was 11.63% (5/43) and the control group was 16.28% (7/43) , and there was no statistical difference between two groups. Conclusion:Modified Liu Junzitang has a good clinical effect on advanced gastric cancer patients with syndrome of deficiency of Qi and blood. It can improve TCM syndromes and gastrointestinal function, improve quality of life, and its mechanism is related to improving immune function, enhancing nutritional status, and improving intestinal microecology, and it has good safety.

12.
Phytochemistry ; 178: 112459, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32888673

RESUMEN

Nine unprecedented diterpenoid alkaloid, including a diterpenoid alkaloid featuring a diterpenoid moiety, anthoroidine A; one bisditerpenoid alkaloid joined with a carbon-carbon single bond, anthoroidine B; three racemulosine-type C20-diterpenoid alkaloids, anthoroidines C-E; one hetidine-type C20-diterpenoid alkaloid, anthoroidine F; and three hetisine-type C20-diterpenoid alkaloids, anthoroidines G-I, together with ten known diterpenoid alkaloids were isolated from Aconitum anthoroideum DC. Their structures were established via detailed spectroscopic analyses. Most of the isolated compounds along with five known diterpenoid alkaloids obtained in a previous study were screened for neuroprotective activities and acetylcholinesterase inhibitory effects. Nominine showed potent protective activity against MPP+-induced apoptosis in SH-SY5Y cells, with a rescue rate of 34.4% (50 µM). Rotundifosine F showed a significant inhibitory activity against AChE (IC50 = 0.3 µM). The structure-activity relationship of these alkaloids is also briefly discussed.


Asunto(s)
Aconitum , Alcaloides , Diterpenos , Acetilcolinesterasa , Aconitum/química , Alcaloides/farmacología , Apoptosis , Línea Celular Tumoral , Diterpenos/farmacología , Humanos , Estructura Molecular , Raíces de Plantas
13.
Cell Commun Signal ; 18(1): 66, 2020 04 20.
Artículo en Inglés | MEDLINE | ID: mdl-32312253

RESUMEN

BACKGROUND: Anti-nerve growth factor (NGF) monoclonal antibodies (anti-NGF mAbs) have been reported to significantly attenuate pain, but the mechanism involved has not been fully elucidated, and the serious adverse events associated with mAbs seriously limit their clinical use. This study further investigated the mechanism by which peripheral NGF is involved in neuropathic pain and found safe, natural compounds that target NGF to attenuate neuropathic pain. METHODS: Nociception was assessed by the Von Frey hair and Hargreaves' methods. Western-blotting, qPCR and immunofluorescence were used to detect the cell signaling pathway. RAW264.7 macrophages and RSC96 Schwann cells were cultured for in vitro evaluation. RESULTS: Intraplantar administration of anti-NGF mAbs suppressed the expression of phosphorylated transforming growth factor-ß-activated kinase 1 (TAK1) in the dorsal root ganglion (DRG) and sciatic nerve. Intraplantar administration of a TAK1 inhibitor attenuated CCI-induced neuropathic pain and suppressed the expression of phosphorylated mitogen-activated protein kinases (MAPKs) in the DRG and sciatic nerve. Perisciatic nerve administration of levo-corydalmine (l-CDL) on the operated side obviously attenuated CCI-induced neuropathic pain and suppressed the expression of mNGF and proNGF. In addition, l-CDL-induced antinociception was reversed by intraplantar administration of NGF. Further results indicated that l-CDL-induced suppression of phosphorylated TAK1, MAPKs, and p65 and expression of the proinflammatory cytokines TNF-α and IL-1ß in the DRG and sciatic nerve were all abolished by NGF. In addition, in vitro experiments indicated that l-CDL suppressed the secretion of NGF and proNGF in RAW264.7 macrophages and RSC96 Schwann cells, which was abolished by AP-1 and CREB agonists, respectively. CONCLUSIONS: This study showed NGF inhibition suppressed TAK1 in the periphery to attenuate CCI-induced neuropathic pain through inhibition of downstream MAPK and p65 signaling. The natural compound l-CDL inhibited NGF secretion by macrophages and Schwann cells and downstream TAK1-MAPK/NF-κB signaling in the periphery to attenuate CCI-induced neuropathic pain. Video abstract Proposed mechanisms underlying the effect of l-CDL in periphery of CCI rats. In CCI rats, macropahages and Schwann cells could secret NGF to act on the receptors in the periphery to activate TAK1-MAPK/NF-κB axis and promote the release of proinflammatory cytokines, including TNF-α and IL-1ß to promote neuropathic pain. l-CDL decreased the secretion of NGF through inhibiting AP-1 and CREB respectively in RAW264.7 and RSC96 Schwann cells to attenuate CCI-induced neuropathic pain by inhibiting the TAK1-p38 MAPK/NF-κB signaling pathway.


Asunto(s)
Anticuerpos Monoclonales , Quinasas Quinasa Quinasa PAM , Factor de Crecimiento Nervioso , Neuralgia/tratamiento farmacológico , Extractos Vegetales , Animales , Anticuerpos Monoclonales/farmacología , Anticuerpos Monoclonales/uso terapéutico , Corydalis/química , Quinasas Quinasa Quinasa PAM/antagonistas & inhibidores , Quinasas Quinasa Quinasa PAM/metabolismo , Ratones , Factor de Crecimiento Nervioso/antagonistas & inhibidores , Factor de Crecimiento Nervioso/inmunología , Factor de Crecimiento Nervioso/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Células RAW 264.7 , Ratas , Ratas Sprague-Dawley , Transducción de Señal
14.
Reg Anesth Pain Med ; 45(3): 219-229, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-31898581

RESUMEN

BACKGROUND AND OBJECTIVES: Neuropathic pain is partially refractory to currently available treatments. Although some studies have reported that apoptosis signal-regulating kinase 1 (ASK1) may inhibit chronic pain, the mechanisms underlying this process have not been fully elucidated. METHODS: Chronic constriction injury (CCI) of the rat sciatic nerve was used to establish a neuropathic pain model. Nociception was assessed using von Frey hair and Hargreaves' methods. Western blot and immunofluorescence were used to detect the cell signaling pathway. BV2 cell line was cultured for in vitro evaluation. RESULTS: Our results indicated that spinal ASK1 was co-expressed with the microglia marker ionized calcium binding adaptor 1. Additionally, intrathecal administration of ASK1 inhibitor suppressed the activation of spinal microglia and attenuated CCI-induced neuropathic pain. The ASK1 inhibitor also decreased the levels of phosphorylated ASK1 (p-ASK1), p65, p38 mitogen-activated protein kinase (MAPK) and tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) messenger RNA in lipopolysaccharide-stimulated BV2 microglia cells. Intragastric administration of levo-corydalmine (l-CDL) significantly attenuated CCI-induced neuropathic pain and inhibited the expression of p-ASK1 in the spinal cord. l-CDL conspicuously suppressed the activation of spinal microglia in vitro and in vivo. Translocation of nuclearfactor-kappa B (NF-κB) and upregulation of p-p65, TNF-α, IL-1ß were inhibited by l-CDL. Further, the analgesic effects of l-CDL were associated with reduced levels of phosphorylated protein kinase C (PKC γ), c-JunNH2-terminal kinase, and extracellular signal-regulated kinase. CONCLUSIONS: This study showed that the expression of ASK1 in spinal microglia and ASK1 inhibitor suppressed microglia activation via suppression of p38 MAPK/NF-κB, which ultimately attenuated CCI-induced neuropathic pain. l-CDL also inhibited the ASK1-P38 MAPK/NF-κB axis to attenuate CCI-induced neuropathic pain.


Asunto(s)
Berberina/análogos & derivados , MAP Quinasa Quinasa Quinasa 5/metabolismo , Microglía/metabolismo , FN-kappa B/metabolismo , Neuralgia/metabolismo , Médula Espinal/metabolismo , Proteínas Quinasas p38 Activadas por Mitógenos/metabolismo , Animales , Berberina/farmacología , Interleucina-1beta/metabolismo , Masculino , Neuralgia/tratamiento farmacológico , Ratas , Ratas Sprague-Dawley , Nervio Ciático , Transducción de Señal/efectos de los fármacos , Factor de Necrosis Tumoral alfa/metabolismo
15.
Spectrochim Acta A Mol Biomol Spectrosc ; 228: 117775, 2020 Mar 05.
Artículo en Inglés | MEDLINE | ID: mdl-31718968

RESUMEN

Two salamo-like copper(II) complex probes, L1-Cu2+ and L2-Cu2+, were designed and synthesized for sensitive and efficient identification of CN-. UV spectroscopy, high resolution mass spectrometry, RGB analysis and naked eye recognition were performed to explore their recognition mechanisms. High resolution mass spectra indicated that the probes L1-Cu2+ and L2-Cu2+ formed complexes with CN-. The two probes could recognize CN- by the naked eye and the color of the solution changed from light yellow to red. In terms of application, the contents of CN- in the environmental water samples were tested. In addition, the optimal pH ranges for probe detection of CN- were investigated by pH value measurement.

16.
J Nat Prod ; 82(12): 3482-3488, 2019 12 27.
Artículo en Inglés | MEDLINE | ID: mdl-31763840

RESUMEN

A new cyclic decapeptide, trikoramide A (1), has been isolated from samples of the marine cyanobacterium Symploca hydnoides, collected from Bintan Island, Indonesia. Trikoramide A (1) is a C-prenylated cyclotryptophan-containing cyanobactin. Its planar structure was deduced by 1D and 2D NMR spectroscopy as well as HR-MS/MS data. In addition, its absolute configuration was determined by Marfey's method and 2D NOESY NMR spectroscopic analysis. Compound 1 possessed cytotoxicity against the MOLT-4 and AML2 cancer cell lines with IC50 values of 4.8 and 8.2 µM, respectively.


Asunto(s)
Antineoplásicos/aislamiento & purificación , Cianobacterias/metabolismo , Agua de Mar/microbiología , Antineoplásicos/química , Antineoplásicos/farmacología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Concentración 50 Inhibidora , Prenilación , Análisis Espectral/métodos
17.
Microbiol Resour Announc ; 8(42)2019 Oct 17.
Artículo en Inglés | MEDLINE | ID: mdl-31624171

RESUMEN

Here, we report the draft genome sequence of a marine bacterium, Mycolicibacterium sp. strain 018/SC-01/001, isolated from the marine sponge Iotrochota sp. collected from the Singapore Strait. The analysis of the bacterial genome using the bioinformatics tool antiSMASH 4.0.2 revealed the presence of a number of unique natural product biosynthetic pathways.

18.
Microbiol Resour Announc ; 8(35)2019 Aug 29.
Artículo en Inglés | MEDLINE | ID: mdl-31467090

RESUMEN

We report the draft genome sequence of a marine bacterium, Bacillus sp. strain 007/AIA-02/001, isolated from the marine sponge Coelocarteria singaporensis, obtained from water off the coast of Singapore. The analysis of the bacterial genome using the bioinformatics tool antiSMASH 4.0.2 showed the presence of a number of unique natural product biosynthetic pathways.

19.
World J Clin Cases ; 7(9): 1087-1092, 2019 May 06.
Artículo en Inglés | MEDLINE | ID: mdl-31123683

RESUMEN

BACKGROUND: The Janus kinase 2 (JAK2) V617F mutation is common in patients with breakpoint cluster region-Abelson1 (BCR-ABL1)-negative myeloproliferative neoplasms, including polycythemia vera, essential thrombocythemia and primary myelofibrosis, but is rarely detected in BCR-ABL1-positive chronic myeloid leukemia (CML) patients. Here, we report a CML patient with both a BCR-ABL1 rearrangement and JAK2 V617F mutation. CASE SUMMARY: A 45-year-old Chinese woman was admitted to our department with a history of significant thrombocytosis for 20 d. Color Doppler ultrasound examination showed mild splenomegaly. Bone marrow aspiration revealed a karyotype of 46, XX, t(9;22)(q34;q11.2) in 20/20 metaphases by cytogenetic analysis, rearrangement of BCR-ABL1 (32.31%) by fluorescent polymerase chain reaction (PCR) and mutation of JAK2 V617F (10%) by PCR and Sanger DNA sequencing. The patient was diagnosed with CML and JAK2 V617F mutation. Following treatment with imatinib for 3 mo, the patient had an optimal response and BCR-ABL1 (IS) was 0.143%, while the mutation rate of JAK2 V617F rose to 15%. CONCLUSION: Emphasis should be placed on the detection of JAK2 mutation when CML is diagnosed to distinguish JAK2 mutation-positive CML and formulate treatment strategies.

20.
J Anim Physiol Anim Nutr (Berl) ; 103(4): 1081-1089, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31008545

RESUMEN

This study was conducted to investigate the effects of dietary supplementation with montmorillonite (MMT) on performance, intestinal endotoxin concentration, gut mucosal oxidation status, intestinal morphology and permeability, and immunological barrier function of laying hens during late production. Four hundred and eighty 75-week-old laying hens (Lohmann Brown) were randomly assigned to five treatments with eight replicates per treatment and 12 hens in each replicate. The hens were fed the basal diet supplemented with 0 (control), 0.3, 0.6, 0.9, or 1.2 g MMT/kg for 70 days. Compared with the control, supplemented with 0.9 g MMT/kg increased egg mass significantly (p < 0.05) during weeks 1-5 of the experiment. Supplemented with 0.6 and 0.9 g MMT/kg also increased the endotoxin concentration in the ileal digesta (p < 0.05), but decreased the MDA concentration in the ileum significantly (p < 0.05). The T-AOC in the jejunum of the group fed 0.3 g MMT/kg was significantly increased (p < 0.05). Compared with the control, the villus height:crypt depth of ileum from the groups fed 0.6, 0.9, and 1.2 g MMT/kg increased significantly (p < 0.05). The sIgA concentration of jejunum in the groups fed 0.6 and 0.9 g MMT/kg was higher (p < 0.05) than the control. The MMT supplementation linearly increased (p < 0.05) the mRNA expression of claudin-1 and claudin-5 in the jejunum. Dietary MMT supplementation down-regulated the mRNA expression of NF-κB P65 and TNF-α in the jejunum in a linear and quadratic manner (p < 0.05). The IL-1ß mRNA expression of jejunum in the group fed 0.6 g MMT/kg was lower (p < 0.05) than the control. In conclusion, dietary supplementation with MMT may improve the gut barrier functions and suggests that 0.9 g/kg of MMT in diets may be the optimal supplemental level for laying hens in late production.


Asunto(s)
Bentonita/farmacología , Pollos/fisiología , Mucosa Intestinal/efectos de los fármacos , Alimentación Animal , Fenómenos Fisiológicos Nutricionales de los Animales , Animales , Dieta/veterinaria , Suplementos Dietéticos , Endotoxinas/química , Femenino , Contenido Digestivo/química , Íleon/efectos de los fármacos , Íleon/fisiología , Mucosa Intestinal/fisiología , Yeyuno/efectos de los fármacos , Yeyuno/fisiología
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