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1.
Pharm Biol ; 61(1): 1343-1363, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37623313

RESUMO

CONTEXT: Tormentic acid (TA), an effective triterpenoid isolated from Chaenomeles speciosa (Sweet) Nakai (Rosaceae) fruits, exerts an effective treatment for gastric damage. OBJECTIVE: To investigate the gastroprotective effect of TA on indomethacin (IND) damaged GES-1 cells and rats, and explore potential mechanisms. MATERIALS AND METHODS: TA concentrations of 1.563-25 µM were used. Cell proliferation, apoptosis and migration were performed using MTT, colony formation, wound healing, migration, Hoechst staining assays. SD rats were divided into control, IND, TA (1, 2 and 4 mg/kg) + IND groups, once a day for 21 continuous days. Twenty-four hours after the last administration, all groups except the control group were given IND (100 mg/kg) by gavage. Gastric juice parameters, gastric ulcer, gastric blood flow (GBF), blood biochemical parameters and cytokine analysis and gastric mucosal histopathology were detected for 2 h and 6 h after IND oral administration. The mRNA and protein expression of miR-139 and the CXCR4/CXCL12/PLC/PKC/Rho A/MLC pathway were analyzed in the IND-damaged GES-1 cells and gastric tissue of rats. RESULTS: TA might ameliorate the gastric mucosal injury by accelerating the IND-damaged GES-1 cell proliferation and migration, ameliorating GBF, ulcer area and pathologic changes, the redox system and cytokine levels, the gastric juice parameters, elevating the gastric pH in IND damaged rats; suppressed miR-139 mRNA expression, elevated CXCR4 and CXCL12 mRNA and protein expression, p-PLC, p-PKC, Rho A, MLCK and p-MLC protein expression. DISCUSSION AND CONCLUSIONS: TA may have potential use as a clinical drug candidate for gastric mucosal lesion treatment.


Assuntos
MicroRNAs , Triterpenos , Animais , Ratos , Ratos Sprague-Dawley , Frutas , Triterpenos/farmacologia , Citocinas , Quimiocina CXCL12
2.
J Pharm Pharmacol ; 74(1): 139-146, 2022 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-34355768

RESUMO

BACKGROUND: Xanthomicrol is one of the methoxylated flavones and a promising cancer chemopreventive agent, but its anti-migration and anti-invasion ability on human hepatocellular carcinoma (HCC) remains unknown. OBJECTIVES: This study aims to explore Xanthomicrol's effects on migration and invasion ability of the human HCC Huh7 cell line. METHODS: Viability of Huh7 cells was measured by cell counting kit-8 (CCK8) assay. Cell apoptosis was assayed with flow cytometry analysis. The ability of migration and invasion of Huh7 cells was then detected through Transwell assays. Epithelial-mesenchymal transition (EMT)-related proteins were also detected through Western blot. KEY FINDINGS: Xanthomicrol inhibits the migration and invasion of Huh7 cells. The overexpression of Μu-opioid receptor (MOR) increases Huh7 cells' proliferation and enhances migration and invasion ability, while xanthomicrol treatment decreases the expression of MOR. Moreover, xanthomicrol can reverse migration, invasion and EMT-related protein expression by overexpressed MOR. CONCLUSIONS: These results suggest that xanthomicrol is a potential MOR antagonist, and it possesses potent anti-migration and anti-invasion ability on Huh7 cells.


Assuntos
Carcinoma Hepatocelular , Movimento Celular/efeitos dos fármacos , Flavonas/farmacologia , Neoplasias Hepáticas , Invasividade Neoplásica/prevenção & controle , Receptores Opioides mu/antagonistas & inibidores , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Transição Epitelial-Mesenquimal/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia
3.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-888085

RESUMO

This study aimed to explore the mechanism of Xiaoyao San(XYS) in the treatment of three diseases of liver depression and spleen deficiency, ie, depression, breast hyperplasia, and functional dyspepsia, and to provide a theoretical basis for the interpretation of the scientific connotation of "treating different diseases with the same method" of traditional Chinese medicines. Traditional Chinese medicine systems pharmacology database and analysis platform(TCMSP) was used to screen the active components of XYS which underwent principal component analysis(PCA) with the available drugs for these three diseases to determine the corresponding biological activities. The targets of XYS on depression, breast hyperplasia, and functional dyspepsia were obtained from GeneCards, TTD, CTD, and DrugBank databases. Cytoscape was used to plot the "individual herbal medicine-active components-potential targets" network. The resulting key targets were subjected to Kyoto encyclopedia of genes and genomes(KEGG) pathway analysis and gene ontology(GO) enrichment analysis. A total of 121 active components of XYS and 38 common targets in the treatment of depression, breast hyperplasia, and functional dyspepsia were collected. The key biological pathways were identified, including advanced glycation and products(AGEs)-receptor for advanced glycation and products(RAGE) signaling pathway in diabetic complications, HIF-1 signaling pathway, and cancer-related pathways. The key targets of XYS in the treatment of depression, breast hyperplasia, and functional dyspepsia included IL6, IL4, and TNF, and the key components were kaempferol, quercetin, aloe-emodin, etc. As revealed by the molecular docking, a strong affinity was observed between the key components and the key targets, which confirmed the results. The therapeutic efficacy of XYS in the treatment of diseases of liver depression and spleen deficiency was presumedly achieved by reducing the inflammatory reactions. The current findings are expected to provide novel research ideas and approaches to classify the scientific connotation of "treating different diseases with the same method" of Chinese medicines, as well as a theoretical basis for understanding the mechanism of XYS and exploring its clinical applications.


Assuntos
Humanos , Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Dispepsia/tratamento farmacológico , Hiperplasia/tratamento farmacológico , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular
4.
Journal of Forensic Medicine ; (6): 501-505, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-663139

RESUMO

Objective To explore the applied value of electroencephalogram (EEG) in assessment of psychiatric impairment among patients with mental disorders due to traumatic brain injury.Methods According to the ICD-10,a total of 271 subjects were enrolled and assessed with the criterion of mental disorders due to traumatic brain injury.Activity of Daily Living Scale (ADL),Functional Activities Questionnaire (FAQ) and Social Disability Screening Schedule (SDSS) were used to evaluate the severity of patients.All the participants were tested by Wechsler Adult Intelligence Scale (WAIS) and examined by EEG.Results Totally 215 patients accomplished the study.The results of Glasgow Coma Scale (GCS),the severity of craniocerebral injury and the scores of FAQ,SDSS and ADL showed significant difference among the patients with different severity of EEG (P<0.05).The grades of psychiatric impairment showed significant difference among the patients with different abnormal EEG (P<0.05).Conclusion EEG can reflect the severity of craniocerebral injury,assist evaluate the social function and activity of daily living of patients with mental disorders due to traumatic brain injury,and distinguish the mild psychiatric impairment grades,which suggest that EEG has a certain reference value in the assessment of psychiatric impairment.

5.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-640912

RESUMO

Objective To explore the optimal cut-off points of body mass index(BMI),percentage of body fat(PBF) and body fat mass index(BFMI) for identification of cardiovascular risk factors clustering among elderly males. MethodsThe data of physical examinations from 1 052 Shanghai elderly males in 2007 were collected.The relationship between cardiovascular risk factors clustering and different strata of BMI,PBF and BFMI was analyzed.Receiver Operator Characteristic(ROC) curve analysis was employed to determine the optimal cut-points for identification of cardiovascular risk factors clustering,and area under curve(AUC) was worked out.The population attributable risk proportion(PARP) of risk factors clustering was calculated. Results Odds ratios of risk factors clustering tended to increase with BMI,PBF and BFMI.BMI≥24 kg/m2,PBF≥21% and BFMI≥5 kg/m2 were the cut-off points that had approximate sensitivity and specificity,and/or had the shortest distance in ROC curve.AUC of all the three indexes was larger than 0.5.Analysis of PARP indicated that BMI under 24 kg/m2,PBF under 21% and BFMI under 5 kg/m2 could prevent 27.1%,37.44% and 36.63% risk factors clustering,respectively. Conclusion BMI≥24 kg/m2,PBF≥21% and BFMI≥5 kg/m2 can well reflect the cardiovascular risk factors clustering among elderly males.

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