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1.
Front Pharmacol ; 15: 1327647, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38545550

RESUMEN

Introduction: Jinteng Qingbi granules (JTQBG), a traditional Chinese medicine formulation, are widely used for the treatment of rheumatoid arthritis (RA) due to their satisfactory therapeutic efficacy. However, the underlying mechanism of action remains unclear. This study aims to investigate the protective effects of JTQBG against RA and elucidates its potential molecular mechanisms. Methods: A collagen-induced arthritis (CIA) rat model was utilized, and JTQBG (1.25, 2.5, 5 g/kg/day) or methotrexate (MTX, 1 mg/kg/week) was orally administered. The rats' weight, arthritis index (AI), and paw volume were measured weekly. Synovial hyperplasia of the joints was detected using a small animal ultrasound imaging system. Joint destruction was assessed using an X-ray imaging system. Histopathological examinations were performed using hematoxylin-eosin (H&E), Saffron-O and fast green staining. Serum inflammatory cytokines were detected using ELISA. Furthermore, 4D label-free quantitative proteomics of synovial tissues and non-targeted metabolomics of blood serum were conducted to analyze the molecular mechanisms. Results: JTQBG exerted a significant therapeutic effect on CIA rats by reducing inflammatory cell infiltration, synovial hyperplasia, cartilage erosion, and bone destruction. It also decreased the spleen index, inhibited hyperplasia of the white pulp, and decreased the serum levels of IL-1ß and IL-18. Proteomics analysis identified 367 differentially expressed proteins (DEPs) between the Model and Normal groups, and 71 DEPs between the JTQBG and Model groups. These DEPs were significantly enriched in the NF-κB pathway. 11 DEPs were significantly reversed after treatment with JTQBG. Western blot results further validated the expression levels of Nfkb1, Pdk1, and Pecam1, and analyzed the expression levels of p-IKK, p-IκBα, and IκBα. The therapeutic efficacy of JTQBG was partly attributed to the suppression of the NF-κB pathway in synovial tissues. Serum metabolomics identified 17 potential biomarkers for JTQBG treatment of CIA rats, which were closely related to Alanine, aspartate and glutamate metabolism, Tryptophan metabolism, Ascorbate and aldarate metabolism, Arginine metabolism, and Inositol phosphate metabolism. Conclusion: Our findings demonstrated that JTQBG was effective against RA by alleviating synovial inflammation, synovial hyperplasia, and joint destruction. The anti-RA properties of JTQBG were likely attributed to the inhibition of the NF-κB pathway and the regulation of serum metabolite disorders.

3.
Front Pharmacol ; 13: 945565, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36299880

RESUMEN

Introduction: Rheumatoid arthritis (RA) is a chronic autoimmune disease affecting females more than males. Clinical symptoms, disease activity and comorbidities are more severe in females. Moreover, the choice of treatment for females is limited during childbearing age due to the side effects of current drugs. Therefore, developing novel and safer drugs for females is urgently needed. Kunbixiao granules (KBXG), a Chinese medicine formula, has been applied to treat female RA patients in our center as a complementary therapy. However, there is insufficient evidence for its effect. Therefore, we aim to conduct a randomized, controlled, double-blind clinical trial to confirm the efficacy and safety of KBXG for the treatment of female RA. Methods: This study is a single-center, double-blind, randomized, parallel group, placebo-controlled clinical trial. A total of 90 female RA patients with Disease Activity Score for 28 joints (DAS28) > 3.2 will be enrolled. They will be randomly assigned to receive either KBXG or placebo for 12 weeks. The change in DAS28 based on C-reactive protein (DAS28-CRP) and the Clinical Disease Activity Index (CDAI) are the primary outcomes. The secondary outcomes include a rate of achieving 20%, 50% and 70% improvement in the American College Rheumatology criteria (ACR20, ACR50, ACR70), TCM syndrome score, visual analogue scale (VAS), average hands grip strength, the consumption of concomitant medication, Hospital Anxiety and Depression Scale (HADS), lumbar spine bone mineral density (L-BMD) and 7-joint ultrasound score (US7). Any adverse events will also be recorded. Discussion: This trial will provide evidence of KBXG in reducing disease activity, and improving clinical symptoms and quality of life of female RA patients. The long-term effects of KBXG on female RA patients still needs a further follow-up.

4.
J Org Chem ; 77(22): 10035-41, 2012 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-23092430

RESUMEN

Here we report the synthesis and characterization of a series of annelated benzotriazole based polymers with variable bandgap. Benzobistriazole monomers reported by us previously were desymmetrized using partial reduction ring opening followed by ring closure to produce a wide range of annelated benzotriazole based monomers. These monomers were co-polymerized with a fluorene moiety to give polymers with bandgaps ranging from 1.16 to 2.41 eV.

5.
Org Lett ; 14(2): 532-5, 2012 Jan 20.
Artículo en Inglés | MEDLINE | ID: mdl-22191669

RESUMEN

The one-pot synthesis of 4,8-dibromobenzo[1,2-d;4,5-d']bistriazole, followed by alkylation and Stille coupling to yield three different isomeric derivatives with markedly different optoelectronic properties, is reported. These derivatives show potential as new units in organic oligomers and polymers for electronics applications.

6.
J Food Sci ; 74(6): M225-30, 2009 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-19723205

RESUMEN

We investigated the bactericidal activity and exclusion effect of 10 strains of lactic acid bacteria (LAB) isolated from different commercial food products and infant feces against Helicobacter pylori (H. pylori) in human gastric epithelial AGS cells. Antagonistic activity of spent culture supernatants (SCS) from LAB (LAB-SCS) was tested, and the content of organic acids in SCS was analyzed with high-performance liquid chromatography (HPLC). In addition, the bactericidal activities of LAB-SCS were estimated by a time-kill assay and by measuring the exclusion effect of LAB-SCS against H. pylori in AGS cells. The results showed that SCS from certain strains with higher concentrations of organic acids dramatically decreased the viability of H. pylori. We also proved that the organic acids could inhibit H. pylori adhesion and invasion of AGS cells. Furthermore, the concentration and speciation of organic acids in SCS after fermentation of LAB are important factors in the inhibition of H. pylori infection. In addition, the in vitro methods used in this study might provide for the rapid screening of potential probiotics with anti-H. pylori activity in the dairy industry.


Asunto(s)
Antibacterianos/farmacología , Medios de Cultivo Condicionados/farmacología , Células Epiteliales/microbiología , Mucosa Gástrica/microbiología , Helicobacter pylori/crecimiento & desarrollo , Helicobacter pylori/patogenicidad , Ácido Acético/análisis , Ácido Acético/metabolismo , Ácido Acético/farmacología , Adhesión Bacteriana/efectos de los fármacos , Fenómenos Fisiológicos Bacterianos , Línea Celular , Recuento de Colonia Microbiana , Medios de Cultivo Condicionados/química , Enterococcus faecium/aislamiento & purificación , Enterococcus faecium/metabolismo , Heces/microbiología , Microbiología de Alimentos , Mucosa Gástrica/citología , Helicobacter pylori/enzimología , Helicobacter pylori/aislamiento & purificación , Humanos , Concentración de Iones de Hidrógeno , Lactante , Ácido Láctico/análisis , Ácido Láctico/metabolismo , Ácido Láctico/farmacología , Lactobacillus/aislamiento & purificación , Lactobacillus/metabolismo , Viabilidad Microbiana , Pediococcus/aislamiento & purificación , Pediococcus/metabolismo , Factores de Tiempo , Ureasa/metabolismo
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