RESUMO
Acetyl-CoA carboxylase (ACC) plays a regulatory role in both fatty acid synthesis and oxidation, controlling the process of lipid deposition in the liver. Given that existing studies have shown a close relationship between low phosphorus (P) and hepatic lipid deposition, this study was conducted to investigate whether ACC plays a crucial role in this relationship. Zebrafish liver cell line (ZFL) was incubated under low P medium (LP, P concentration: 0.77 mg/L) or adequate P medium (AP, P concentration: 35 mg/L) for 240 h. The results showed that, compared with AP-treated cells, LP-treated cells displayed elevated lipid accumulation, and reduced fatty acid ß-oxidation, ATP content, and mitochondrial mass. Furthermore, transcriptomics analysis revealed that LP-treated cells significantly increased lipid synthesis (Acetyl-CoA carboxylases (acc), Stearyl coenzyme A dehydrogenase (scd)) but decreased fatty acid ß-oxidation (Carnitine palmitoyltransferase I (cptI)) and (AMP-activated protein kinase (ampk)) mRNA levels compared to AP-treated cells. The phosphorylation of AMPK and ACC, and the protein expression of CPTI were significantly decreased in LP-treated cells compared with those in AP-treated cells. After 240 h of LP treatment, PF-05175157 (an ACC inhibitor) was supplemented in the LP treatment for an additional 12 h. PF-05175157-treated cells showed higher phosphorylation of ACC, higher protein expression of CPTI, and lower protein expression of FASN, lower TG content, enhanced fatty acid ß-oxidation, increased ATP content, and mitochondrial mass compared with LP-treated cells. PF-05175157 also relieved the LP-induced oxidative stress and inflammatory response. Overall, these findings suggest that ACC is a promising target for treating LP-induced elevation of lipid deposition in ZFL, and can alleviate oxidative stress and inflammatory response.
Assuntos
Acetil-CoA Carboxilase , Peixe-Zebra , Animais , Peixe-Zebra/metabolismo , Acetil-CoA Carboxilase/genética , Acetil-CoA Carboxilase/metabolismo , Proteínas Quinases Ativadas por AMP/genética , Fígado/metabolismo , Estresse Oxidativo , Ácidos Graxos/metabolismo , Fósforo , Lipídeos , Trifosfato de Adenosina/metabolismoRESUMO
The treatment ideas with acupuncture for knee osteoarthritis (KOA) are explored on the base of Dongyuan needling technology. Regarding the rules of acupoint selection, Zusanli (ST 36) is predominant, the back-shu points are used for the disorders related to the invasion of exogenous factors, and the front-mu points are for the cases caused by internal injury. Besides, the xing-spring points and shu-stream points are preferred. In treatment of KOA, besides the local points, the front-mu points, i.e. Zhongwan (CV 12), Tianshu (ST 25) and Guanyuan (CV 4), are selected specially to tonifying the spleen and stomach. The earth points and acupoints on the earth meridians (i.e. Yinlingquan [SP 9], Xuehai [SP 10], Liangqiu [ST 34], Dubi [ST 35], Zusanli [ST 36] and Yanglingquan [GB 34]) are optional to coordinate yin and yang, essence and qi , and regulate the qi movement of spleen and stomach. The shu-stream points of liver, spleen and kidney meridians (Taichong [LR 3], Taibai [SP 3] and Taixi [KI 3]) are chosen to promote meridian circulation and regulate zangfu functions.
Assuntos
Terapia por Acupuntura , Meridianos , Osteoartrite do Joelho , Humanos , Pontos de Acupuntura , BaçoRESUMO
BACKGROUND: The majority of global population suffer from various functional gastrointestinal disorders. Pugionium cornutum (L.) Gaertn. (PCG) is used to relieve indigestive symptoms in traditional Chinese medicine. However, little is known about the effects of bioactive components from PCG extracts on gastrointestinal motility. METHODS: Crude ethanol extract of PCG (EEP) was prepared from Pugionium cornutum (L.) Gaertn. Different solvents were used to prepare fine extracts from EEP, including water extract of PCG (WEP), petroleum ether extract of PCG (PEEP), dichloromethane extract of PCG (DEP) and ethyl acetate extract of PCG (EAEP). Smooth muscle cell model and colonic smooth muscle stripe model were used to test the bioactive effects and mechanisms of different PCG extracts on contraction and relaxation. Diverse chromatographic methods were used to identify bioactive substances from PCG extracts. RESULTS: EEP was found to promote the relaxation of gastric smooth muscle cell and inhibit the contraction of colonic smooth muscle strip. Among the fractions of EEP, EAEP mainly mediated the relaxation effect by stimulating intracellular calcium influx. Further evidences revealed that EAEP was antagonistic to acetylcholine. In addition, COX and NO-GC-PKC pathways may be also involved in EAEP-mediated relaxation effect. Quercetin was identified as a bioactive compound from PCG extract for the relaxation effect. CONCLUSION: Our research supports the notion that PCG extracts promote relaxation and inhibits contraction of gastrointestinal smooth muscle at least partially through the effect from quercetin.
Assuntos
Gastroenteropatias/tratamento farmacológico , Motilidade Gastrointestinal/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Extratos Vegetais/farmacologia , Humanos , Quercetina/farmacologiaRESUMO
BACKGROUND: Omacetaxine mepesuccinate (OME) has antileukemic effects against acute myeloid leukemia (AML) carrying an internal tandem duplication of Fms-like tyrosine kinase 3 (FLT3-ITD). A phase 2 clinical trial was conducted to evaluate a combination treatment of sorafenib and omacetaxine mepesuccinate (SOME). METHODS: Relapsed or refractory (R/R) or newly diagnosed patients were treated with sorafenib (200-400 mg twice daily) and OME (2 mg daily) for 7 (first course) or 5 days (second course onward) every 21 days until disease progression or allogeneic hematopoietic stem cell transplantation (HSCT). The primary endpoint was composite complete remission, which was defined as complete remission (CR) plus complete remission with incomplete hematologic recovery (CRi). Secondary endpoints were leukemia-free survival (LFS) and overall survival (OS). RESULTS: Thirty-nine R/R patients and 5 newly diagnosed patients were recruited. Among the R/R patients, 28 achieved CR or CRi. Two patients showed partial remission, and 9 patients did not respond. Among the 5 newly diagnosed patients, 4 achieved CR, and 1 achieved CRi. The median LFS and OS were 5.6 and 10.9 months, respectively. Prior Fms-like tyrosine kinase 3 (FLT3) inhibitor exposure (P = .007), 2 or more inductions (P = .001), and coexisting IDH2 (P = .008) and RUNX1 mutations (P = .003) were associated with lower CR/CRi rates. HSCT consolidation and deep molecular responses (defined as an FLT3-ITD variant allelic frequency [VAF] ≤ 0.1% or a nucleophosmin 1 [NPM1] mutant VAF ≤ 0.01%) were associated with better OS and LFS. Prior FLT3 inhibitor exposure and 2 or more inductions were associated with inferior LFS. CONCLUSIONS: SOME was safe and effective for R/R and newly diagnosed FLT3-ITD AML.
Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/administração & dosagem , Mepesuccinato de Omacetaxina/administração & dosagem , Leucemia Mieloide Aguda/terapia , Recidiva Local de Neoplasia/terapia , Sorafenibe/administração & dosagem , Tirosina Quinase 3 Semelhante a fms/genética , Adulto , Idoso , Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos , Protocolos de Quimioterapia Combinada Antineoplásica/farmacocinética , Progressão da Doença , Intervalo Livre de Doença , Esquema de Medicação , Resistencia a Medicamentos Antineoplásicos , Sinergismo Farmacológico , Éxons/genética , Feminino , Duplicação Gênica , Transplante de Células-Tronco Hematopoéticas , Mepesuccinato de Omacetaxina/efeitos adversos , Mepesuccinato de Omacetaxina/farmacocinética , Humanos , Leucemia Mieloide Aguda/genética , Leucemia Mieloide Aguda/mortalidade , Leucemia Mieloide Aguda/patologia , Masculino , Pessoa de Meia-Idade , Recidiva Local de Neoplasia/genética , Recidiva Local de Neoplasia/mortalidade , Recidiva Local de Neoplasia/patologia , Nucleofosmina , Indução de Remissão/métodos , Sorafenibe/efeitos adversos , Sorafenibe/farmacocinética , Transplante Homólogo , Adulto Jovem , Tirosina Quinase 3 Semelhante a fms/antagonistas & inibidores , Tirosina Quinase 3 Semelhante a fms/farmacocinéticaRESUMO
OBJECTIVE: examine the efficacy and safety of Shenmai to the cardiac rehabilitation in patients received coronary artery bypass grafting. DESIGN: a single-center randomized, single blind clinical trial. SETTING: Department of Cardiovascular Surgery, Beijing Anzhen Hospital, Capital Medical University, Beijing, China. SUBJECTS: Patients with coronary artery disease who received coronary artery bypass grafting in our center were studied. They must be competent to complete the 6-minute walking test without any assistance and without any severe comorbidity. INTERVENTIONS: in Shemmai group, the participants were treated with Shenmai injection (100â¯ml/day) right after the surgery to discharge for 9.28⯱â¯3.75 days and then capsule (3.6â¯g/day) sequentially for 30 days in addition to the cardiac rehabilitation. In control group, only cardiac rehabilitation was conducted. MAIN MEASURES: the 6-Minute Walking Test was measured at three time points: one day before operation, on the day of discharge and 30 days follow up. RESULTS: The sample (nâ¯=â¯166) was predominately male (84%), with mean age was 61.12⯱â¯9.13 years. There was no significant difference between groups in baseline characteristics and the procedural characteristics. There was one death in control group and one stroke in Shenmai group right after the surgery. Overall, there was group (pâ¯=â¯.005) and time effect (pâ¯<â¯.001) on the 6-minute walking distance. Participants in the Shenmai group walked longer distance in meters compared with control group on the day of discharge (314.54⯱â¯64.14 vs. 271.29⯱â¯76.82, Pâ¯<â¯.001), while no significant differences before operation (399.72⯱â¯93.19 vs. 403.67⯱â¯91.99, pâ¯=â¯.78) and on 30-day follow up (436.54⯱â¯67.64 vs. 421.64⯱â¯83.53, pâ¯=â¯.21). CONCLUSION: Shenmai improves the exercise tolerance in the early stage of the cardiac rehabilitation for patients received coronary artery bypass grafting.
Assuntos
Reabilitação Cardíaca/métodos , Ponte de Artéria Coronária , Doença da Artéria Coronariana/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Idoso , Terapia Combinada , Doença da Artéria Coronariana/cirurgia , Combinação de Medicamentos , Teste de Esforço , Tolerância ao Exercício , Feminino , Humanos , Masculino , Medicina Tradicional Chinesa , Pessoa de Meia-Idade , Método Simples-CegoRESUMO
Aquaculture jeopardizes the aquatic environment by discharge of the most dietary phosphorus (P) into the water. Reducing the dietary P level is a common approach for decreasing the P discharge but it may result in increased risk of P deficiency leading to vertebral deformities. However, the molecular mechanism of vertebral deformities is poorly understood. We assessed vertebral transcriptome and compared the genes associated with bone metabolism in Japanese seabass (Lateolabrax japonicus) fed three diets containing different P and Ca levels including: diet I (0.4% P, 0.3% Ca), diet II (0.8% P, 0.3% Ca) and diet III (0.8% P, 3% Ca). The results showed that P deficiency reduces the ossification of vertebrae and induces visible vertebral deformities. Moreover, 256 gens were up-regulated and 125 genes were down-regulated in fish fed P deficient diets. Furthermore, administration of the diet with adequate P and Ca excess (diet III) resulted in the significant enhancement in expression of 19 genes and reduced expression of 93 genes. Comparing group II with group III, expression of 109 genes was up-regulated and expression of 1369 genes was down-regulated. Gene ontology enrichment analysis revealed significant alterations in biological functions by P deficiency. In summary, these findings indicated that both dietary P shortage and Ca excess lead to reduced differentiation and proliferation of osteoblast and induce a higher activity of osteoclastogenesis, which could subsequently impair vertebral mineralization and cause skeletal deformities.
Assuntos
Ração Animal , Cálcio/análise , Peixes/genética , Fósforo/análise , Coluna Vertebral/metabolismo , Transcriptoma , Ração Animal/análise , Animais , Cálcio/administração & dosagem , Osteoblastos/citologia , Osteoclastos/citologia , Fósforo/administração & dosagem , Fósforo/deficiência , Coluna Vertebral/anormalidades , Coluna Vertebral/citologiaRESUMO
This study evaluated the effects of supplementing chitooligosaccharide (COS) in low fish meal (FM) diets on growth, immune response, intestine and hepatopancrease histology, and expression of inflammatory and immune-related genes in Pacific white shrimp (Litopenaeus vannamei). A basal diet was formulated using FM and soybean meal (SM) as primary protein sources and considered as a high FM (HFM) diet, then a low FM (LFM) diet was prepared by substituting 50% of FM with SM and supplemented with 0, 0.3, 0.6, 0.9, 1.2 or 1.5â¯g COS kg-1 diet (LFM, COS3, COS6, COS9, COS12 and COS15 diets). Each diet was fed to quadruplicate groups of shrimp (0.9â¯g) to apparent satiation three times daily for eight weeks. At the end of the experiment no significant changes in growth and survival rate were observed among treatments (Pâ¯>â¯0.05). FM replacement led to significant (Pâ¯<â¯0.05) reduction of serum lysozyme activity and significant improvements were obtained by adding 0.3 or 0.6â¯gâ¯kg-1 COS to the LFM diet. A significant decrease in nitric oxide synthase activity was found in LFM group and no beneficial effects could be achieved by COS application. LFM group showed higher hepatopancrease superoxide dismutase and glutathione peroxidase activities than HFM group and further enhancements were obtained by COS application. Hepatopancrease total antioxidant capacity and alkaline phosphatase activity decreased in LFM group and COS supplementation improved their values. Expression of lysozyme, crustin, Pen3 and proPo genes were significantly up-regulated in hepatopancrease of groups received 0.3-0.9â¯g COS kg-1 diet. FM substitution enhanced the expression of HSP70 and inflammatory genes such as AIF and TNF in hepatopancrease and intestine, and COS administration at a moderate level down-regulated their expression level. Remarkable enhancement in intestinal fold height was obtained by inclusion of 0.3 or 0.6â¯g COS kg-1 diet compared to the group received LFM diet. Shrimps fed HFM and COS containing diets exhibited higher number of E-cells within their hepatopancrease tubules than the LFM group. The findings in this study clearly demonstrated that COS could enhance non-specific immune response and antioxidant activity, and ameliorate the negative impacts of high SM diets on gut and hepatopancrease health in pacific white shrimp. The optimum inclusion level of COS seems to be 0.3-0.6â¯gâ¯kg-1 of diet.
Assuntos
Ração Animal , Quitina/análogos & derivados , Penaeidae/efeitos dos fármacos , Fosfatase Alcalina/metabolismo , Animais , Quitina/farmacologia , Quitosana , Dieta/veterinária , Peixes , Expressão Gênica/imunologia , Glutationa Peroxidase/metabolismo , Hepatopâncreas/efeitos dos fármacos , Hepatopâncreas/metabolismo , Imunidade Inata/efeitos dos fármacos , Intestinos/anatomia & histologia , Intestinos/efeitos dos fármacos , Muramidase/sangue , Oligossacarídeos , Penaeidae/genética , Penaeidae/crescimento & desenvolvimento , Penaeidae/imunologia , Glycine max , Superóxido Dismutase/metabolismoRESUMO
An 8-week feeding trial was undertaken to evaluate supplemental effects of AviPlus® (AP), a blend of organic acids [citric acid, 25%; sorbic acid, 16.7%] and essential oils [thymol, 1.7%; vanillin, 1.0%], on growth, gut microbiota, innate immunity and disease resistance of Pacific white shrimp (Litopenaeus vannamei) against Vibrio parahaemolyticus. A basal experimental diet was formulated and supplemented with 0, 0.3, 0.6, 0.9 and 1.2 g kg-1 AP to produce five test diets (Con, AP0.3, AP0.6, AP0.9 and AP1.2). Each diet was fed to triplicate groups of shrimp (0.2 ± 0.01 g, mean ± SE) to apparent satiation three times daily. Growth performance and survival rate were not significantly influenced by AP supplementation (P > 0.05). Significantly (P < 0.05) higher serum total protein was found in groups fed ≥ 0.6 g kg-1 AP compared to control. Serum alkaline phosphatase and phenoloxidase activities were significantly increased in AP0.9 and AP1.2 groups. Also, the group received AP0.6 diet showed significantly higher glutathione peroxidase activity than control. Expression of gut pro-inflammatory genes including TNF-α, LITAF and RAB6A were down-regulated by AP administration. Gut microbiota analysis showed the significant enhancement of the operational taxonomic unit (OTU) diversity and richness indices by AP application. AP supplementation led to increased abundance of Firmicutes and a reduction in abundance of Proteobacteria. Also, dietary inclusion of 1.2 g kg-1 AP led to a significant increase in the abundance of Lactobacillus in shrimp gut. The group offered AP0.3 diet showed significantly higher disease resistance than control group. Furthermore, AP application significantly enhanced relative expression of immune related genes including lysozyme, penaeidin and catalase at 48 h post challenge. In conclusion, these findings show that the tested organic acids and essential oils mixture beneficially affects intestinal microflora and improves immune response and disease resistance of L. vannamei.
Assuntos
Ácido Cítrico/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacos , Imunidade Inata/efeitos dos fármacos , Óleos Voláteis/metabolismo , Penaeidae/imunologia , Ácido Sórbico/metabolismo , Vibrio parahaemolyticus/fisiologia , Ração Animal/análise , Animais , Benzaldeídos/administração & dosagem , Benzaldeídos/metabolismo , Ácido Cítrico/administração & dosagem , Dieta , Suplementos Nutricionais/análise , Óleos Voláteis/administração & dosagem , Penaeidae/crescimento & desenvolvimento , Ácido Sórbico/administração & dosagem , Timol/administração & dosagem , Timol/metabolismoRESUMO
Fish farming seriously influences the aquatic environment because most dietary phosphorus (P) is excreted in the effluent. To increase the P utilization in fish, molecular techniques should be explored given the remarkable development of these techniques. Thus, to identify the candidate genes related to P utilization and molecular alterations following administration of a P-deficient diet in seabass Lateolabrax japonicus, we assessed the de novo pituitary, gill, intestine, liver, kidney, scales and vertebra transcriptomes, and we compared the expression of hepatic genes with three diets varying in P and Ca levels: diet I (0.4% P, 0.3% Ca), diet II (0.8% P, 0.3% Ca), and diet III (0.8% P, 3% Ca). In total, we identified 99,392 unigenes, and 37,086 (37.31%) unigenes were annotated. The results showed that 48 unigenes were significantly (P<0.05) up-regulated, while 55 genes were significantly down-regulated in the liver of group I compared with group II. Offering the P-sufficient and high Ca diet, diet III significantly up-regulated 24 unigenes and down-regulated 46 genes in the liver. There were significant differences in the regulation of 8 unigenes (3 up-regulated and 5 down-regulated) between groups II and III. Gene ontology (GO) functional enrichment and KEGG pathway analysis of differently expressed genes were performed for each pair of groups. The GO analysis showed that a large number of biological processes were significantly altered between P-deficient and P-sufficient treatments (I vs II and I vs III). Comparing group I and group II, seven KEGG terms were enriched significantly: glycine, serine and threonine metabolism, one carbon pool by folate, arginine and proline metabolism, the biosynthesis of unsaturated fatty acids, fatty acid elongation, drug metabolism-cytochrome P450, and fatty acid metabolism. There was no significantly enriched KEGG pathway between groups II and III. In conclusion, our study revealed that a P-deficient diet could increase catabolism and decrease anabolism of protein, as highlighted by low protein efficiency in fish fed the P-deficient diet. Furthermore, P-deficiency could motivate the biosynthesis of fatty acids. However, the dietary Ca level had no significant effect on the growth and expression of hepatic genes in L. japonicus.
Assuntos
Bass/metabolismo , Cálcio da Dieta/metabolismo , Fígado/metabolismo , Fósforo na Dieta/metabolismo , Transcriptoma/fisiologia , Animais , Bass/genética , Bass/fisiologia , Cálcio da Dieta/análise , Proteínas Alimentares/química , Proteínas Alimentares/metabolismo , Ácidos Graxos/metabolismo , Perfilação da Expressão Gênica , Fígado/química , Fósforo/deficiência , Fósforo na Dieta/análise , Reação em Cadeia da Polimerase em Tempo Real , Reprodutibilidade dos Testes , Transcriptoma/genéticaRESUMO
Based on the crystal structures of the previously proposed low energy η-P and θ-P, five new phosphorene allotropes were predicted through gene segments recombination method. These five new phosphorene allotropes are confirmed dynamically stable and energetically more favorable than their parents (η-P and θ-P). Especially, the XX-XX type G1-P is confirmed energetically more favorable than most of all the previously proposed phosphorene allotropes, including black phosphorene and blue phosphorene, which is highly expected to be synthesized in future experiment through vapor deposition or epitaxial growth method like blue ß-P. The calculated results also show that such a new promising phosphorene allotrope G1-P is a potential candidate for application in nano-electronics according to its middle band gap of about 1.491 eV from DFT-HSE06 calculation.
Assuntos
Fósforo/química , Análise Espectral RamanRESUMO
BACKGROUND: Panax ginseng root is used in traditional oriental medicine for human health. Its main active components such as saponins and polysaccharides have been widely evaluated for treating diseases, but secondary active components such as oligosaccharides have been rarely studied. This study aimed to assess the impact of water-soluble ginseng oligosaccharides (WGOS), which were isolated from the warm-water extract of Panax ginseng root, on scopolamine-induced cognitive impairment in mice and its antineuroinflammatory mechanisms. METHODS: We investigated the impact of WGOS on scopolamine-induced cognitive impairment in mice by using Morris water maze and novel object recognition task. We also analyzed the impact of WGOS on scopolamine-induced inflammatory response (e.g., the hyperexpression of proinflammatory cytokines IL-1ß and IL-6 and astrocyte activation) by quantitative real-time polymerase chain reaction and glial fibrillary acid protein (GFAP) immunohistochemical staining. RESULTS: WGOS pretreatment protected against scopolamine-induced learning and memory deficits in the Morris water maze and in the novel object recognition task. Furthermore, WGOS pretreatment downregulated scopolamine-induced hyperexpression of proinflammatory cytokines interleukin (IL)-1ß and IL-6 mRNA and astrocyte activation in the hippocampus. These results indicate that WGOS can protect against scopolamine-induced alterations in learning and memory and inflammatory response. CONCLUSION: Our data suggest that WGOS may be beneficial as a medicine or functional food supplement to treat disorders with cognitive deficits and increased inflammation.
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A high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC/Q-TOF MS) was developed for the analysis of chemical composition change in the production process of Re Du Ning injection, a Chinese medicine preparation with a combination of Lonicera japonica Thunb., Gardenia jasminoides Ellis and Artemisia annua L. A total of 90 compounds from raw materials-intermediates-Re Du Ning injection were detected; among them, 55 compounds were identified or tentatively characterized, and the characteristic ions of different types of compounds were described. Based on these studies, the different types of compounds in the various process routes were analyzed. A total of 28 compounds, including seven iridoid glycosides and six monoterpenes from G. jasminoides Ellis, five iridoid glycosides, nine phenolic acids and one unknown compound from L. japonica Thunb., were transferred to Re Du Ning injection, and two unknown compounds were generated in the production process of Re Du Ning injection. The results indicated that the Chinese Medicine Pharmaceutical process control is very important. This method could provide some reference for other Chinese medicine preparations.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Glicosídeos Iridoides/análise , Glicosídeos Iridoides/química , Fenóis/análise , Fenóis/química , Terpenos/análise , Terpenos/químicaRESUMO
Secosesquside (1), a new secoiridoid glucoside-sesquiterpene conjugate, together with three known secoiridoid derivatives, were isolated from flower buds of Lonicerajaponica. The isolated compounds were elucidated by extensive spectroscopic analyses, especially 2D NMR experiments. The anti-inflammatory activities of the new compound were also evaluated by enzyme-linked immunosorbent assay.
Assuntos
Flores/química , Glucosídeos Iridoides/química , Lonicera/química , Sesquiterpenos/química , Modelos Moleculares , Estrutura MolecularRESUMO
The aim of this study was to explore the effect of a traditional Chinese medicine (Xiaochaihu Tang, XCHT) on the expression of matrix metalloproteinase-2 (MMP-2) and MMP-9 in rats with endometriosis (EMs). A total of 48 specific-pathogen-free (SPF) female Sprague-Dawley (SD) rats were randomly divided into control (n=8) and EMs (n=40) groups. The EMs model was established using a surgical procedure. At 21 days, the rats with EMs were screened and divided into four subgroups (n=8): the model control, low-dose (7.5 g/kg) XCHT-treated, high-dose (15 g/kg) XCHT-treated and gestrinone-treated (0.5 mg/kg) groups. Following 21 days of treatment, the rats were sacrificed. Reverse transcription-polymerase chain reaction (RT-PCR) and western blotting were used to examine the mRNA and protein levels of MMP-2 and MMP-9 in the endometrium. The expression levels of MMP-2 and MMP-9 were significantly increased in the rats with EMs compared with those in normal rats. Moreover, XCHT was able to significantly inhibit the expression of MMP-2 and MMP-9 compared with that in the model control group. In conclusion, XCHT was able to decrease the expression of MMP-2 and MMP-9 in the ectopic endometrium. The present results may provide a potential theoretical basis for the therapy of EMs.
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BACKGROUND: Wheat bran is a traditional Chinese medicine; however, it is mostly used as feedstuff in China. Wheat bran is widely accepted as an important ingredient in many low-glycemic index foods in modern western societies; however, its glycemic control mechanism is unknown. OBJECTIVE: To determine potent α-glucosidase inhibitory compounds from wheat bran and to identify the inhibition on α-glucosidase. MATERIALS AND METHODS: Ethanolic extract of wheat bran was prepared to evaluate the inhibitory activity on α-glucosidase, then fractionation of the extract was guided by in vitro enzyme-inhibition assay, and the potent α-glucosidase inhibitory compounds were identified by high performance liquid chromatography and atmospheric pressure chemical ionization-mass spectrometry; finally the enzyme inhibition process was studied using the Michaelis-Menton and the Lineweaver-Burk equations. RESULTS: Both baker's yeast and rat intestinal enzymes were mostly inhibited (87.9% and 66.8% inhibition, respectively) at concentration 0.6 mg/mL of the ethanolic extract of wheat bran. The petroleum ether fraction in the ethanolic extract of wheat bran showed significant activity against rat intestinal α-glucosidase, and revealed a dose-dependent effect. The inhibition was 76.57% at 0.3 mg/mL and 100% at 0.6 mg/mL. The active fraction 13 of petroleum ether fraction was identified as alkylresorcinols (ARs). ARs showed strong inhibition towards α-glucosidase and its IC50 value was found to be 37.58 µg/mL. The enzyme kinetic studies showed that, in the presence of ARs, the Michaelis-Menton constant (K m) remains constant whereas the maximal velocity (V max) decreases, revealing a non-competitive type of inhibition. CONCLUSION: The therapeutic potentiality of ARs in the management of the postprandial hyperglycemia will proliferate the utilization of wheat bran in controlling type 2 diabetes.
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OBJECTIVE: To study the molluscicidal activity, the influence on glycogen content of Oncomelania hupensis and the acute toxicity to zebra fish of the extract from Phytolacca americana Linn leaf. METHODS: The different polar factions of the extract of Phytolacca americana Linn leaf were separated by using the systemic solvent segregation method, and then the molluscicidal activity of the fractions was detected according to the Laboratory Final Milluscicides Screening Method issued by WHO. The glycogen content of soft tissues of Oncomelania hupensis treated by the ethyl acetate polar fraction was determined by the anthrone method. Finally, the acute toxicity of the ethyl acetate polar fraction to non-targets was studied with zebra fish. RESULTS: The ethyl acetate polar fraction was the best active components against the snails. Its 48 h LC50 and LC90 were 6.0 mg/100 ml and 26.1 mg/ 100 ml, respectively. The glycogen content of soft tissues of the snails decreased by 20% after treated with the fraction. The fish treated by the concentration of LC50 (48 h) of the ethyl acetate polar fraction survived for 12 h. CONCLUSION: The Phytolacca americana Linn leaf possesses an adequate molluscicidal activity and a significant acute toxicity to the zebra fish.
Assuntos
Glicogênio/toxicidade , Moluscocidas/toxicidade , Phytolacca americana/química , Extratos Vegetais/toxicidade , Folhas de Planta/química , Caramujos/efeitos dos fármacos , Animais , Relação Dose-Resposta a Droga , Dose Letal Mediana , Controle de Pragas , Caramujos/crescimento & desenvolvimento , Peixe-ZebraRESUMO
A feeding experiment was conducted to investigate the effects of exogenous enzymes (phytase, non-starch polysaccharide enzymes: WX and VP, supplied by DSM) on growth performance and excretion of Japanese seabass (Lateolabrax japonicus) (initial mass 6.26+/-0.10 g). A basal diet was used as a control that contained a mixed protein source, and lysine, methionine and valine were supplemented to simulate the essential amino acid pattern of fish meal. Four other diets were supplemented with 200 mg phytase (500 IU), 400 mg VP, 800 mg WX, or a combination of 800 mg WX and 400 mg VP per kg diet, respectively. Each diet was assigned to triplicate groups of fish in floating sea cages, and each cage was stocked with 60 fish. The results showed specific growth rate (SGR) and feed efficiency ratio (FER) were not significantly improved by the phytase supplementation. However, supplementations with WX and VP significantly enhanced the SGR and FER (P<0.05). Phosphorus retention was significantly increased by the supplementation with phytase, whereas nitrogen retention was also enhanced by supplementations of non-starch polysaccharide enzymes (P<0.05). The excretion experiment showed that the soluble phosphorus and ammonia nitrogen in starved fish were constant, irrespective of dietary treatments. The total phosphorus effluent in fish fed the diet with phytase supplementation was significantly lower compared with the control group after feeding to satiation (P<0.05), but soluble phosphorus excretion was still independent of dietary treatments. The ammonia excretion in satiated fish significantly decreased with supplementations of non-starch polysaccharide enzymes.
Assuntos
6-Fitase/farmacologia , Ração Animal , Bass/crescimento & desenvolvimento , Bass/metabolismo , Nitrogênio/metabolismo , Fósforo/metabolismo , Animais , Composição Corporal/efeitos dos fármacos , Privação de Alimentos/fisiologia , Análise de Sobrevida , Oligoelementos/análiseRESUMO
AIM: To investigate whether if the Habenula is the main relay involved in the vasopressor effect induced by the stimulus of insular cortex, central-, lateral amygdaloid nucleus respectively. METHODS: Electrostimulation of the nuclei mention above respectively, and microinjection of lidocaine into Habenula unilaterally and bilaterally. RESULTS: When INS or CeA was stimulated, inducing an obvious increase of blood pressure. To stimulate INS or CeA after microinjecting lidocaine into Hb 5 minutes, the amplitudes of the vasopressor responses were decreased significantly, and the decrease of the bilaterally was larger (decreased value: 41.7% in INS, 46.1% in CeA) than that of unilaterally (decreased value: 36.9% in INS, 39.6% in CeA). CONCLUSION: Habenula is one of the main relays involved in the vasopressor effects induced by the stimulus of insular cortex, central-, lateral amygdaloid nucleus.