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1.
Molecules ; 28(3)2023 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-36771107

RESUMEN

We herein report the acid/base-steered two distinct reaction pathways of 2-acylbenzoic acids with isatoic anhydrides. In the presence of Na2CO3, the cascade process consists of the cyclization of 2-acetylbenzoic acid and nucleophilic ring-opening reaction of isatoic anhydride to furnish isobenzofuranone derivatives with high efficiency. However, p-toluenesulfonic acid can promote the product isobenzofuranones to undergo sequential intramolecular rearrangment, nucleophilic addition and cyclization reaction to produce diverse isoindolobenzoxazinones in good yields. The synthetic utility of this method was further demonstrated by the gram-scale preparation of the desired products and the facile transformations of the resulting products.

2.
J Org Chem ; 87(15): 9769-9781, 2022 08 05.
Artículo en Inglés | MEDLINE | ID: mdl-35866754

RESUMEN

Different Lewis acid promotor-steered highly regioselective phosphorylation of tertiary enamides with diverse H-phosphonates or H-phosphine oxides was developed. Under the catalysis of iron salt, the phosphonyl group was introduced into the α-position of tertiary enamides, affording various α-phosphorylated amides in high efficiency. On the other hand, the ß-phosphorylated tertiary enamides were efficiently obtained as the products in the presence of manganese(III) acetylacetonate.


Asunto(s)
Amidas , Ácidos de Lewis , Catálisis , Estructura Molecular , Fosforilación
3.
Org Biomol Chem ; 20(28): 5566-5574, 2022 07 20.
Artículo en Inglés | MEDLINE | ID: mdl-35792054

RESUMEN

A concise manganese(III)-promoted stereoselective ß-phosphorylation of acyclic tertiary enamides and diverse H-phosphine oxides was achieved. This reaction proceeds with absolute E-selectivity in contrast to Z-selectivity obtained in other previous works and affords various E-selective ß-phosphorylated tertiary enamides in high efficiency. To the best of our knowledge, this is the first case of E-selective ß-phosphorylation of tertiary enamides through C-H functionalization. In addition, the method features broad substrate scope, good functional group compatibility and efficient scale-up.


Asunto(s)
Amidas , Manganeso , Humanos , Estructura Molecular , Fosforilación , Estereoisomerismo
4.
J Org Chem ; 87(5): 3014-3024, 2022 03 04.
Artículo en Inglés | MEDLINE | ID: mdl-35073080

RESUMEN

An efficient Au(I)-catalyzed intramolecular cascade reaction of tertiary enamides tethered an alkynyl group has been developed. The process is composed of a propargyl-claisen rearrangement and 5-exo-dig cyclization. This protocol provided a powerful method for the preparation of a variety of pentasubstituted pyrroles derivatives with excellent functional group tolerance in excellent yields. Scale-up experiment and chemical transformations of products exhibited the versatility of tertiary enamides in organic synthesis again.


Asunto(s)
Oro , Pirroles , Catálisis , Ciclización , Oro/química , Estructura Molecular , Pirroles/química
5.
Stem Cells Int ; 2021: 8850820, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33505476

RESUMEN

Rheumatoid arthritis (RA) is a systemic autoimmune disease characterized by articular destruction and functional loss. Methotrexate (MTX) is effective in RA treatment. However, MTX induces several adverse events and 20%-30% of patients do not respond to MTX. Thus, it is urgent to enhance the therapeutic effects and reduce the side effects of MTX. Recent studies showed that mesenchymal stem cells (MSCs) were participants in anti-inflammation, immunoregulation, and tissue regeneration. However, whether the combined application of MSCs and MTX promotes the therapeutic effects and reduces the side effects of MTX has not been studied. In this study, we used bovine type II collagen to induce rheumatoid arthritis in mice (collagen-induced arthritis, CIA). Then, CIA mice were subjected to MTX or MSC treatment, or both. The therapeutic effect and adverse events of different treatments on RA were evaluated with micro-CT, HE staining, and immunohistochemistry in vivo. Apoptosis and proliferation of MODE-K cells were measured after treated with MTX or/and cocultured with UCs. To test M2 polarization, Raw264.7 macrophages were stimulated by MTX with different concentrations or cocultured with UCs. We found that the combined application of MSCs and MTX increased the therapeutic effects on RA, as evidenced by decreased arthritis score, inflammatory responses, and mortality. Moreover, in this combination remedy, MTX prefers to suppress inflammation by facilitating macrophage polarization to M2 type while UCs prefer to eliminate gastrointestinal side effects of MTX via mitigating the apoptosis of intestinal epithelial cells. Thus, a combination of MTX and UCs is a promising strategy for RA treatment.

6.
Gen Comp Endocrinol ; 242: 92-100, 2017 02 01.
Artículo en Inglés | MEDLINE | ID: mdl-26497252

RESUMEN

Glucotoxicity and lipotoxicity are major hallmarks of metabolic disorder. High consumption of fat or carbohydrate rich food is a major risk of metabolic disorder. However, the evolution of high fat or high carbohydrate diet-induced metabolic disorder is not clear. In the study, we tried to find distinguished and common ways involved in the pathogenesis of insulin resistance induced by high fat (HF) and high sucrose (HS) diet. We found that HS diet induced mild glucose intolerance (2month), followed by a "temporary non-symptom phase" (3month), and then induced significant metabolic abnormality (4month). HF diet induced an early "responsive enhancement phase" (2month), and then gradually caused severe metabolic dysfunction (3-4month). After a mild induction of mitochondrial ROS generation (2month), HS diet resulted in a "temporary non-symptom phase" (3month), and then induced a more significant mitochondrial ROS production (4month). The impairment of mitochondrial function induced by HS diet was progressive (2-4month). HF diet induced gradual mitochondrial ROS generation and hyperpolarization. HF diet induced an early "responsive enhancement" of mitochondrial function (2month), and then gradually resulted in severe decrease of mitochondrial function (3-4month). Despite the patterns of HS and HF diet-induced insulin resistance were differential, final mitochondrial ROS generation combined with mitochondrial dysfunction may be the common pathway. These findings demonstrate a novel understanding of the mechanism of insulin resistance and highlight the pivotal role of mitochondrial ROS generation and mitochondrial dysfunction in the pathogenesis of metabolic disorder.


Asunto(s)
Dieta Alta en Grasa/efectos adversos , Sacarosa en la Dieta/efectos adversos , Mitocondrias/efectos de los fármacos , Animales , Sacarosa en la Dieta/administración & dosificación , Metabolismo Energético , Glucosa/metabolismo , Intolerancia a la Glucosa/metabolismo , Insulina/metabolismo , Resistencia a la Insulina , Masculino , Enfermedades Metabólicas , Mitocondrias/fisiología , Oxidación-Reducción , Estrés Oxidativo , Ratas
7.
Psychiatry Res ; 244: 130-8, 2016 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-27479103

RESUMEN

Personalities are determined by convergent factors, including physical environment, culture, special experience, and heredity. It has been shown that abuse of substance and alcohol among individuals with personality disorders predict criminality (Glenn and Raine, 2014; Hernandez-Avila et al., 2000). Thus, it is important to clarify the relationship between psychological characteristics and valence of criminal practice, even in the population without substance abuse. Here, we focused on a population with military experience in Shaanxi province of China to screen the psychological characteristics and correlate these characteristics to criminal behaviors. The study population included incarcerated veterans, incarcerated civilians, and three groups of military troops with different lengths of active duty history (<1 month, 1 year, and 2 years). We used the MAST (Michigan Alcoholism Screening Test), EMBU (Egna Minnen av Barndoms Uppfostran), and 16PF (Sixteen Personality Factor Questionnaire) for the screening purpose. Eight hundred seventy-five valid packets of questionnaires were collected during November 2014-January 2015. Comparison of the mean scores was used to evaluate the difference among the five groups. Incarcerated veterans and incarcerated civilians shared the alcohol abuse-relevant characteristics, including negative parental attitudes during their childhood and decreased emotional stability. Compared to the incarcerated civilians, incarcerated veterans scored higher in emotional stability, self-reliance, and perfectionism, but a lower score in apprehension. Personality characteristics associated with criminal behavior of incarcerated veterans seem to be unrelated to their military service per se as evidenced by the control groups. Conversely, military service may benefit the personnel characteristics even in the incarcerated veteran population.


Asunto(s)
Alcoholismo/psicología , Conducta Criminal , Criminales/psicología , Personal Militar/psicología , Personalidad , Veteranos/psicología , Adolescente , Adulto , Pueblo Asiatico , Actitud , Estudios de Casos y Controles , China , Emociones , Femenino , Humanos , Masculino , Padres , Perfeccionismo , Trastornos de la Personalidad , Trastornos Relacionados con Sustancias/psicología , Encuestas y Cuestionarios , Adulto Joven
8.
Mol Neurobiol ; 53(5): 3258-3266, 2016 07.
Artículo en Inglés | MEDLINE | ID: mdl-26059811

RESUMEN

Aspirin, one of the most commonly used anti-inflammatory drugs, has been recently reported to display multiple effects in the central nervous system (CNS), including neuroprotection and upregulation of ciliary neurotrophic factor (CNTF) expression in astrocytes. Although it was most recently reported that aspirin could promote the proliferation and differentiation of oligodendrocyte precursor cells (OPCs) after white matter lesion, the underlying mechanisms remain unclear. To dissect the effects of aspirin on oligodendroglial development and explore possible mechanisms, we here demonstrated the following: (i) in vitro treatment of aspirin on OPC cultures significantly increased the number of differentiated oligodendrocytes (OLs) but had no effect on the number of proliferative OPCs, indicating that aspirin can promote OPC differentiation but not proliferation; (ii) in vivo treatment of aspirin on neonatal (P3) rats for 4 days led to a nearly twofold increase in the expression of myelin basic protein (MBP), devoid of change in OPC proliferaion, in the corpus callosum (CC); (iii) finally, aspirin treatment increased the phosphorylation level of ß-catenin and counteracted Wnt signaling pathway synergist QS11-induced suppression on OPC differentiation. Together, our data show that aspirin can directly target oligodendroglial lineage cells and promote their differentiation through inhibition of Wnt/ß-catenin signaling pathway. These findings suggest that aspirin may be a novel candidate for the treatment of demyelinating diseases.


Asunto(s)
Aspirina/farmacología , Diferenciación Celular/efectos de los fármacos , Oligodendroglía/citología , Oligodendroglía/metabolismo , Vía de Señalización Wnt/efectos de los fármacos , Animales , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Factor Neurotrófico Ciliar/metabolismo , Cuerpo Calloso/citología , Oligodendroglía/efectos de los fármacos , Fosforilación/efectos de los fármacos , Ratas Sprague-Dawley , beta Catenina/metabolismo
9.
Mol Pharmacol ; 83(5): 1099-108, 2013 May.
Artículo en Inglés | MEDLINE | ID: mdl-23470287

RESUMEN

Inhibition of oxidative stress and inflammation in vascular endothelial cells (ECs) may represent a new therapeutic strategy against endothelial activation. Sinapic acid (SA), a phenylpropanoid compound, is found in natural herbs and high-bran cereals and has moderate antioxidant activity. We aimed to develop new SA agents with the properties of antioxidation and blocking EC activation for possible therapy of cardiovascular disease. We designed and synthesized 10 SA derivatives according to their chemical structures. Preliminary screening of the compounds involved scavenging hydroxyl radicals and 2,2-diphenyl-1-picrylhydrazyl (DPPH(⋅)), croton oil-induced ear edema in mice, and analysis of the mRNA expression of adhesion molecules in ECs. 1-Acetyl-sinapic acyl-4-(3'-chlorine-)benzylpiperazine (SA9) had the strongest antioxidant and anti-inflammatory activities both in vitro and in vivo. Thus, the effect of SA9 was further studied. SA9 inhibited tumor necrosis factor α-induced upregulation of adhesion molecules in ECs at both mRNA and protein levels, as well as the consequent monocyte adhesion to ECs. In vivo, result of face-to-face immunostaining showed that SA9 reduced lipopolysaccharide-induced expression of intercellular adhesion molecule-1 in mouse aortic intima. To study the molecular mechanism, results from luciferase assay, nuclear translocation of NF-κB, and Western blot indicated that the mechanism of the anti-inflammatory effects of SA9 might be suppression of intracellular generation of ROS and inhibition of NF-κB activation in ECs. SA9 is a prototype of a novel class of antioxidant with anti-inflammatory effects in ECs. It may represent a new therapeutic approach for preventing endothelial activation in cardiovascular disorders.


Asunto(s)
Ácidos Cumáricos/farmacología , Células Endoteliales/efectos de los fármacos , Endotelio Vascular/efectos de los fármacos , Animales , Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Antioxidantes/síntesis química , Antioxidantes/farmacología , Aorta/efectos de los fármacos , Aorta/metabolismo , Compuestos de Bifenilo/farmacología , Adhesión Celular/efectos de los fármacos , Ácidos Cumáricos/síntesis química , Aceite de Crotón/farmacología , Oído , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/metabolismo , Células Endoteliales/metabolismo , Endotelio Vascular/metabolismo , Depuradores de Radicales Libres/síntesis química , Depuradores de Radicales Libres/farmacología , Células Endoteliales de la Vena Umbilical Humana , Humanos , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Molécula 1 de Adhesión Intercelular/metabolismo , Lipopolisacáridos/farmacología , Ratones , Ratones Endogámicos BALB C , Ratones Endogámicos C57BL , Monocitos/efectos de los fármacos , Monocitos/metabolismo , FN-kappa B/metabolismo , Estrés Oxidativo/efectos de los fármacos , Picratos/farmacología , Factor de Necrosis Tumoral alfa/metabolismo
10.
Neurochem Int ; 59(6): 847-52, 2011 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-21835217

RESUMEN

Maternal deprivation (MD) is a well-established protocol used to investigate neurobiological changes that are associated with the etiology of and vulnerability to stress-related diseases in animal models. The resulting psychophysiological effects, the timing and duration of these adverse stimuli, and the method by which they exert their effects on the animals remain unclear. This study characterized differences in the hippocampal expression of glucocorticoid receptors (GRs) and the calcium-binding proteins calretinin (CALR) and calbindin-D28k (CALB) in male and female rats that underwent different MD paradigms during the stress hyporesponsive period (SHRP). Both GRs and the two calcium-binding proteins were much more abundant in females than in males. MD paradigms had a significant effect on CALR and CALB expression in both males and females but affected GR levels only in males. Additionally, expression of the two calcium-binding proteins in the hippocampus responded differently to MD-induced stress, especially in females. Taken together, these results indicate that females are able to modulate their response to stress better than males.


Asunto(s)
Hipocampo/metabolismo , Privación Materna , Receptores de Glucocorticoides/biosíntesis , Proteína G de Unión al Calcio S100/biosíntesis , Caracteres Sexuales , Estrés Psicológico/metabolismo , Envejecimiento/fisiología , Envejecimiento/psicología , Animales , Calbindina 1 , Calbindina 2 , Calbindinas , Modelos Animales de Enfermedad , Femenino , Hipocampo/crecimiento & desarrollo , Hipocampo/fisiopatología , Masculino , Embarazo , Ratas , Ratas Sprague-Dawley , Receptores de Glucocorticoides/metabolismo , Estrés Psicológico/fisiopatología
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