RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Walnut kernel, a well-known TCM, is often used after being defatted in tradition. And defatted walnut powder extract (DWPE) has the actions of tonifying the liver and kidney, dissipating stagnation and removing blood stasis, which has the effect on non-alcoholic fatty liver disease (NAFLD). However, the effective components of DWPE in vivo were unclear and the multiple mechanisms of DWPE against NAFLD have not been explored. AIM OF THE STUDY: The studies were performed to screen the effective substances in vivo by identification of the metabolites of DWPE in rats and to seek the potential mechanisms of DWPE on NAFLD by construction of the network pharmacology based on metabolites and verification of the highly correlated pathway. MATERIALS AND METHODS: To explore the effective substances in vivo, the metabolites of DWPE were identified in SD rats' bio-samples through UPLC-Q-Exactive Orbitrap MS. To analyze the mechanisms of DWPE on NAFLD, a Metabolite-Target-Disease network was established and the potential mechanisms were predicted. Then, highly correlated pathway was verified in animal and cells studies. RESULTS: A total of 52 metabolites of DWPE were identified in vivo, which were derived from gallic acid, ellagic acid (EA) and glansreginin A (Gla A). The possible metabolic pathways were phase â (hydroxylation, hydrolyzation, etc) and phase â ¡ metabolic reactions (methylation, sulfation and glucuronidation). Furthermore, in the network pharmacology, 54 core targets were enriched into pathways in cancer, nitrogen metabolism and other 9 pathways, which were essential pathways of DWPE against NAFLD. And the mechanism of nitrogen metabolism was verified in both of animal and cells studies. The results showed that DWPE could decline the concentration of ammonia and increase the expressions of carbonic anhydrase 2 (CA2) and carbamoylphosphate synthetase (CPS1) in nitrogen metabolism. CONCLUSION: Taken together, the study revealed the absorption components and their metabolic pathways and demonstrated the mechanism of nitrogen metabolism of DWPE on anti-NAFLD.
Assuntos
Cromatografia Líquida/métodos , Juglans/química , Espectrometria de Massas/métodos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Nozes/química , Extratos Vegetais/metabolismo , Animais , Camundongos , Estrutura Molecular , Farmacologia em Rede/métodos , Compostos Fitoquímicos , Fitoterapia , Extratos Vegetais/química , Pós/química , Pós/metabolismo , Ratos , Ratos Sprague-DawleyRESUMO
Frankincense (FRA), the oily resin consisting of essential oils, boswellic acids (BAs) and polysaccharides, has been used to improve the blood circulation and relieve pain against carbuncles. According to the theory of traditional Chinese medicine, vinegar processed frankincense (VPF) can increase the effects of promoting blood circulation and relieving pain. Existing studies have carried out much on BAs and essential oils. However, the comparative analysis of polysaccharides from FRA and VPF has not been reported. In this paper, two polysaccharides were isolated and purified from FRA and the other two were from VPF, and their structures and physicochemical properties were analyzed. The immunological and anticoagulatant activities of the four polysaccharides were tested in RAW 264.7 cell and Sprague-Dawley rats, respectively. The polysaccharides purified from VPF showed better immunological and anticoagulatant activities than those in FRA. Therefore, polysaccharides may be one of the active substances for the synergistic effect of VPF.
Assuntos
Boswellia , Franquincenso , Óleos Voláteis , Ácido Acético , Animais , Boswellia/química , Franquincenso/química , Franquincenso/farmacologia , Óleos Voláteis/farmacologia , Dor , Polissacarídeos/farmacologia , Ratos , Ratos Sprague-DawleyRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Capsella bursa-pastoris (L.) Medic. (CBP) is a cruciferous plant valuable in reducing fever, improving eyesight and calming the liver. This herb was recorded in the Compendium of Materia Medica for cataract treatment. AIM OF THE STUDY: To determine the effects and mechanism of CBP on cataract prevention and treatment using a selenite cataract model. MATERIALS AND METHODS: The main compounds in CBP extract were analyzed by UPLC, 1H-NMR and 13C-NMR spectroscopic techniques. Flavonoids formed a significant proportion of its compounds, thus necessitating an evaluation of their inhibitory effects on the development of cataract using a selenite cataract model. The protective effects of CBP flavonoids (CBPF) against oxidative damage and the modulation of mitochondrial apoptotic pathway were subsequently verified on H2O2-treated SRA01/04 lens epithelial cells. RESULTS: CBPF significantly alleviated the development of cataract by decreasing the MDA level and increasing the GSH-Px and SOD levels in the lens. It also inhibited H2O2-induced apoptosis in SRA01/04 cells, increased the expression of Bcl-2 protein and decreased the expressions of Caspase-3 and Bax proteins. CONCLUSION: CBPF exerts a significant preventive effect on cataract development by regulating the mitochondrial apoptotic pathway of the lens epithelial cells. It is thus a potent traditional Chinese medicine (TCM) whose application should be further developed for the clinical treatment of cataract.
Assuntos
Capsella/química , Catarata/prevenção & controle , Células Epiteliais/efeitos dos fármacos , Cristalino/citologia , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Apoptose/efeitos dos fármacos , Apoptose/fisiologia , Caspase 3/genética , Caspase 3/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Glutationa Peroxidase/genética , Glutationa Peroxidase/metabolismo , Peróxido de Hidrogênio , Malondialdeído/metabolismo , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ratos , Ratos Wistar , Superóxido Dismutase/genética , Superóxido Dismutase/metabolismo , Proteína X Associada a bcl-2/genética , Proteína X Associada a bcl-2/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Walnut kernel has the actions of removing meteorism, dissipating stagnation and removing blood stasis and is used after being defatted in TCM. Defatted walnut powder extract (DWPE) has the abilities of anti-oxidation and lowering lipid levels in vivo. However, the effects and the potential mechanisms of DWPE on NAFLD have not been explored. AIM OF THE STUDY: The study were to investigate the anti-NAFLD effect of DWPE in high fat diet-induced C57BL/6 mice and demonstrate that whether DWPE developed the effect on anti-NAFLD by remodeling the compositions and abundances of gut microbiota. MATERIALS AND METHODS: The inhibitory effect of DWPE on the development of NAFLD was conducted on C57BL/6 mice with a high fat diet and the regulation effect of DWPE on gut microbiota was verified on pseudo-sterile mice with treatment of broad spectrum antibiotics. RESULTS: The results showed that the oral administration of DWPE remarkably alleviated hepatic lipid accumulation by decreasing the levels of TG, TC, LDL, MDA and increasing HDL. Meanwhile, the expressions of NF-κB and MAPKs family proteins were reduced by DWPE compared with HFD group. Otherwise, the efficacy of anti-NAFLD of DWPE was significantly decreased after treatment of antibiotics, which indicated the key role of gut microbiota in the therapeutic process. Furthermore, sequencing of 16S rRNA gene revealed that DWPE could revert the decreased relative abundance of gut microbiota caused by the long term of a high fat diet. And the disordered microflora was remodeled by DWPE including the reduction of Erysipelotrichia, Firmicutes and Actinobacteria as well as the increment of Bacteroidetes, Clostridiales, Bacteroidales S24-7, Prevotellaceae and Bacteroides. CONCLUSION: Taken together, DWPE had a preventing effect on NAFLD, which might be associated with the regulation of gut microbiota.
Assuntos
Microbioma Gastrointestinal/efeitos dos fármacos , Juglans/química , Hepatopatia Gordurosa não Alcoólica/prevenção & controle , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Glicemia/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/patologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Inflamação/metabolismo , Inflamação/prevenção & controle , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Camundongos Endogâmicos C57BL , Hepatopatia Gordurosa não Alcoólica/induzido quimicamente , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Pós/uso terapêutico , RNA Ribossômico 16S/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Morning glory seed (MGS), has been widely used in treating constipation especially towards children. Clinically, people usually take fried MGS (MGSF) in formulas to reduce its side effect. However, the safety of MGSF other than MGS has yet to be explored. OBJECTIVE: The study aimed to reveal the potential mechanisms of using MGSF instead of MGS basing on chemistry, pharmacodynamics and toxicology. METHODS: The chemical compositions of the extracts of MGS and MGSF were compared using UPLC-Q-TOF/MS method. Simultaneously, to prove the availability and safety of MGSF, we investigated the laxative effect and subchronic toxicity of MGS and MGSF and addressed the mechanism of laxative effect of them. RESULTS: In this study, less phenolic acids and more fatty acids were detected in MGSF compared with the compounds in MGS. Moreover, we found that MGS group had stronger laxative effect than MGSF group via downregulating the expression of AQP3 protein. As for subchronic toxicity test, the body weights of MGS group were lower than MGSF group. In serum biochemistry and histopathological examinations, MGS group could cause more serious toxicity in liver, kidney and colon than MGSF group with higher values of BUN, Cr, AST and ALP. CONCLUSION: Based on the findings in this study, MGSF with varied compounds contents could still keep the laxative effect while retain less subchronic toxicity, which emphasized the necessity of processing and provided an insight into the rational use of MGSF in clinical practice.
Assuntos
Ipomoea , Laxantes/farmacologia , Animais , Aquaporina 3/metabolismo , Colo/efeitos dos fármacos , Colo/metabolismo , Colo/patologia , Culinária , Defecação/efeitos dos fármacos , Diarreia/induzido quimicamente , Diarreia/metabolismo , Temperatura Alta , Rim/efeitos dos fármacos , Rim/patologia , Laxantes/química , Laxantes/toxicidade , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Camundongos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Ratos Sprague-Dawley , Sementes , Testes de Toxicidade SubcrônicaRESUMO
A simple sample preparation method was developed by using a centrifugal ultrafiltration (CF-UF) device with hollow fiber (HF) for the determination of cefaclor in plasma by HPLC. Samples were placed into a homemade device, which was consisted of a glass tube and a U-shaped hollow fiber. The filtrate was withdrawn from the hollow fiber into a syringe after centrifugation and 20 µL was directly injected into the HPLC for analysis. The HPLC method had a linear calibration curve in the concentration range of 6.00×10(-2)-30.7 µg mL(-1)(r=0.9996). The limit of detection (LOD) and limit of quantitation (LOQ) were 0.02 and 0.06 µg mL(-1), respectively. The intra and inter-day precisions (RSD) were 1.7%, 1.2%, 1.0% and 3.6%, 2.5%, 1.9%, respectively, for three concentrations. Assay accuracy was higher than 99.2% and the absolute recovery was 86.8-92.5%. It is feasible to use this novel and low cost device for sample pretreatment for the analysis of cefaclor in plasma.