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Phytochemistry investigation on Pteris ensiformis led to the isolation of a new ent-kaurane diterpenoid, ent-kaurane-6ß,16α-diol-3-one (1), along with five known diterpenoids (2-6) and three known sesquiterpenes (7-9). Their structures were established by means of spectroscopic methods. The ethanol extract and the isolated compounds (1-9) were evaluated for their antitumor activity against three cancer cell lines.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/isolamento & purificação , Diterpenos do Tipo Caurano/farmacologia , Pteris/química , Antineoplásicos Fitogênicos/química , Diterpenos/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Diterpenos do Tipo Caurano/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear BiomolecularRESUMO
Two new dihydrochalcone enantiomers (+)-1 and (-)-1, along with eight known compounds 3-10, were obtained from Pteris ensiformis. The planar structures were determined on the basis of extensive 1D and 2DNMR and HRESIMS. The resolution of (+)-1 and (-)-1 was achieved by chiral HPLC analysis. The absolute configurations of (+)-1 and (-)-1 were established by the bulkiness rule using Rh2(O2CCF3)4-induced circular dichroism (ICD) method. Compounds (+)-1, (-)-1, 8, 9 and 10 exhibited the inhibitory assay of NO production in mouse macrophages stimulated by LPS, with IC50 values of 2.0, 2.5, 8.0, 9.5 and 5.6 µM, respectively. Otherwise, compound 10 showed moderate cytotoxic activity against HCT-116, HepG-2 and BGC-823 cell lines with IC50 values of 3.0, 10.5 and 6.3 µM, respectively.
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Antineoplásicos Fitogênicos/isolamento & purificação , Chalconas/isolamento & purificação , Chalconas/farmacologia , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Óxido Nítrico/antagonistas & inibidores , Pteris/química , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Chalconas/química , Cromatografia Líquida de Alta Pressão , Dicroísmo Circular , Diterpenos/química , Humanos , Ativação de Macrófagos/efeitos dos fármacos , Camundongos , Óxido Nítrico/biossíntese , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologiaRESUMO
A new triterpene glycoside ilexdunnoside A (1) and a new sulfated triterpene derivative ilexdunnoside B (2), together with five known analogues 3-7 were isolated from the roots of Ilex dunniana Levl. The structures were established by NMR spectroscopic analysis and acid hydrolysis. Results of an in vivo study of the biological activity showed that 75% ethanol and n-butanol extracts of the plant displayed anti-inflammatory activities against ear edema in mice, with inhibition rates of 23.5% and 37.5%, respectively, at a dose of 50 mg/kg. Furthermore, Compounds 1, 2 and 3 exhibited moderate indirect inhibitory effects on lipopolysaccharide-induced NO production in BV2 microglial cells in vitro, with IC50 values of 11.60, 12.30 and 9.70 µM, respectively.
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Anti-Inflamatórios/farmacologia , Glicosídeos/farmacologia , Ilex/química , Inflamação/tratamento farmacológico , Raízes de Plantas/química , Triterpenos/farmacologia , Animais , Anti-Inflamatórios/química , Linhagem Celular , Edema/tratamento farmacológico , Glicosídeos/química , Camundongos , Triterpenos/químicaRESUMO
Twelve quinolizidine alkaloids were isolated from Sophora tonkinensis by means of silica gel, preparative MPLC, and preparative HPLC. On analysis of NMR spectroscopic data, their structures were established as 3-(4-hydroxyphenyl)-4-(3-methoxy-4-hydroxyphenyl)-3,4-dehydroquinolizidine(1), lanatine A(2), cermizines C(3), senepodines G(4), senepodines H(5), jussiaeiines A(6), jussiaeiines B(7),(+)-5α-hydroxyoxysophocarpine(8),(-)-12ß-hydroxyoxysophocarpine(9),(-)-clathrotropine(10),(-)-cytisine(11), and (-)-N-methylcytisine(12), respectively. Compounds 1-7 were first isolated from Sophora L. plant. In the in vitro assays,the isolated compounds 1, 3, 6-10 exhibited potent activity against CVB3 with IC50 of 6.40, 3.25, 4.66, 3.21, 0.12, 0.23 and 1.60, and with selective index values(SI=TC50/IC50)of 12.0, 5.6, 13.0, 15.1, 50.1, 26.2, and 23.6, respectively. Compounds 1, 3, and 7 exhibited activity against staphylococcus aureus(ATCC 29213)with MICvalues of 8.0, 3.5, 6.0 gâ¢L⻹, respectively. Compounds 1, 3, 7, and 12 exhibited activity against staphylococcus aureus(ATCC 33591)with MIC values of 18.0, 7.5, 8.0, 12.0 gâ¢L⻹, respectively. Compounds 2, 6, 7 exhibited activity against Escherichia coli(ATCC 25922) with MIC values of 1.0, 3.2, 0.8 gâ¢L⻹.
Assuntos
Alcaloides/isolamento & purificação , Quinolizidinas/isolamento & purificação , Sophora/química , Antibacterianos/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Quinolizinas , Staphylococcus aureus/efeitos dos fármacosRESUMO
The materials were extracted by 95% ethanol, and the extracting solution was isolated by kinds of chromatographic columns including polyamide, MCI, preparative MPLC, and preparative HPLC. Eight diterpenes and two sesquiterpenes were isolated from the plant. On analysis of ESI-MS and NMR spectroscopic data, the structures were established as ent-3ß-hydroxy-kaur-16-en-19-al (1), 4-epi-kaurenic acid (2), mitrekaurenone (3), 7ß,16α,17-trihydroxy-ent-kauran-19-oic acid (4), crotonkinin E (5), crotonkinin F (6), pterisolic acid A (7), pterisolic acid C (8), (2R)-pterosin P (9), and dehydropterosin B (10). Compounds 1-6 were obtained from Pteris for the first time, and compounds 7-10 were obtained from P. ensiformis for the first time. Compounds 5-8 showed moderate activity against HCT-116, HepG2 and BGC-823 cell lines, separately.
Assuntos
Diterpenos/isolamento & purificação , Pteris/química , Sesquiterpenos/isolamento & purificação , Linhagem Celular Tumoral , Diterpenos/química , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/química , Sesquiterpenos/químicaRESUMO
Vapours of organic matters were determined qualitatively employed with ultraviolet-visible absorption spectroscopy. Vapours of organic matters were detected using ultraviolet-visible spectrophotometer employing polyethylene film as medium, the ultraviolet and visible absorption spectra of vegetable oil vapours of soybean oil, sunflower seed oil, peanut oil, rapeseed oil, sesame oil, cotton seed oil, tung tree seed oil, and organic compound vapours of acetone, ethyl acetate, 95% ethanol, glacial acetic acid were obtained. Experimental results showed that spectra of the vegetable oil vapour and the organic compound vapour could be obtained commendably, since ultra violet and visible spectrum of polyethylene film could be deducted by spectrograph zero setting. Different kinds of vegetable oils could been distinguished commendably in the spectra since the λ(max), λ(min), number of absorption peak, position, inflection point in the ultra violet and visible spectra obtained from the vapours of the vegetable oils were all inconsistent, and the vapours of organic compounds were also determined perfectly. The method had a good reproducibility, the ultraviolet and visible absorption spectra of the vapours of sunflower seed oil in 10 times determination were absolutely the same. The experimental result indicated that polyethylene film as a kind of medium could be used for qualitative analysis of ultraviolet and visible absorption spectroscopy. The method for determination of the vapours of the vegetable oils and organic compounds had the peculiarities of fast speed analysis, well reproducibility, accuracy and reliability and low cost, and so on. Ultraviolet and visible absorption spectrum of organic vapour could provide feature information of material vapour and structural information of organic compound, and provide a novel test method for identifying vapour of compound and organic matter.
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Gases/análise , Óleos de Plantas/química , Espectrofotometria Ultravioleta , Óleo de Sementes de Algodão , Ácidos Graxos Monoinsaturados , Óleo de Amendoim , Polietilenos , Óleo de Brassica napus , Reprodutibilidade dos Testes , Sementes , Óleo de Gergelim , Óleo de Soja , Óleo de GirassolRESUMO
BACKGROUND AND PURPOSE: The detection and characterization of functional activities in the gray matter of schizophrenia (SZ) have been widely explored. However, the relationship between resting-state functional signals in the white matter of first-episode SZ and short-term treatment response remains unclear. METHODS: Thirty-six patients with first-episode SZ and 44 matched healthy controls were recruited in this study. Patients were classified as nonresponders and responders based on response to antipsychotic medication during a single hospitalization. The fractional amplitude of low-frequency fluctuation (fALFF), regional homogeneity (ReHo), and functional connectivity (FC) of white matter were calculated. The relationships between functional changes and clinical features were analyzed. In addition, voxel-based morphometry was performed to analyze the white matter volume. RESULTS: One-way analysis of variance showed significant differences of fALFF and ReHo in the left posterior thalamic radiation and left cingulum (hippocampus) in the patient group, and the areas were regarded as seeds. The FC was calculated between seeds and other white matter networks. Compared with responders, nonresponders showed significantly increased FC between the left cingulum (hippocampus) and left posterior thalamic radiation, splenium of corpus callosum, and left tapetum, and were associated with the changes of clinical assessment. However, there was no difference in white matter volume between groups. CONCLUSION: Our work provides a novel insight that psycho-neuroimaging-based white matter function holds promise for influencing the clinical diagnosis and treatment of SZ.
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Esquizofrenia , Substância Branca , Humanos , Esquizofrenia/diagnóstico por imagem , Esquizofrenia/tratamento farmacológico , Substância Branca/diagnóstico por imagem , Substância Cinzenta/diagnóstico por imagem , Córtex Cerebral , Imageamento por Ressonância Magnética/métodos , EncéfaloRESUMO
OBJECTIVE: To study the clinicopathologic features, radiologic findings, treatment options and prognosis of dysembryoplastic neuroepithelial tumor (DNT). METHODS: The clinicopathologic and radiologic features were retrospectively analyzed in 10 cases of DNT. RESULTS: Intractable partial seizure was the main presenting symptom in all patients. The tumor was located in temporal lobe (number = 5), frontal lobe (number = 3) or parietal lobe (number = 2). CT scan displayed a hypodense lesion. MRI scan revealed the tumor was non-enhancing T1WI hypointense and T2WI hyperintense, with internal septation and hyperintense ring around the tumor seen on FLAIR image. There was neither peritumoral edema nor mass effect. Histologically, the tumor showed the presence of glioneuronal element, with oligodendrocyte-like cells, floating neurons, astrocytes and associated microcystic changes. Immunohistochemical study demonstrated positivity for NeuN and synaptophysin in the neurons and some oligodendrocyte-like cells. Olig2 and S-100 protein were also expressed in the oligodendrocyte-like cells. Ki-67 index were lower than 1% in all cases. Nine cases were treated by complete surgical excision and the remaining case was subtotally excised. No post-operative chemotherapy or radiotherapy was given. One of the 10 cases recurred on follow up. CONCLUSIONS: Correct diagnosis of DNT requires correlation with clinicopathologic, radiologic and immunohistochemical findings. Complete resection of the tumor and epileptogenic foci is the mainstay of treatment for DNT, with intraoperative EEG monitoring. Post-operative chemotherapy or radiotherapy is not required.
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Neoplasias Encefálicas/patologia , Neoplasias Neuroepiteliomatosas/patologia , Adolescente , Adulto , Antígenos Nucleares/metabolismo , Fatores de Transcrição Hélice-Alça-Hélice Básicos/metabolismo , Neoplasias Encefálicas/diagnóstico , Neoplasias Encefálicas/metabolismo , Neoplasias Encefálicas/cirurgia , Córtex Cerebral/metabolismo , Córtex Cerebral/patologia , Criança , Feminino , Seguimentos , Humanos , Imageamento por Ressonância Magnética , Masculino , Neoplasias Neuroepiteliomatosas/diagnóstico , Neoplasias Neuroepiteliomatosas/metabolismo , Neoplasias Neuroepiteliomatosas/cirurgia , Proteínas do Tecido Nervoso/metabolismo , Procedimentos Neurocirúrgicos , Fator de Transcrição 2 de Oligodendrócitos , Estudos Retrospectivos , Proteínas S100/metabolismo , Sinaptofisina/metabolismo , Tomografia Computadorizada por Raios X , Adulto JovemRESUMO
Background and Purpose: It is sometimes difficult to effectively distinguish non-neoplastic from neoplastic intracranial enhancement lesions using conventional magnetic resonance imaging (MRI). This study aimed to evaluate the diagnostic performance of three-dimensional pseudo-continuous arterial spin labeling (3D-pCASL) to differentiate non-neoplastic from neoplastic enhancement lesions intracranially. Materials and Methods: This prospective study included thirty-five patients with high-grade gliomas (HGG), twelve patients with brain metastasis, and fifteen non-neoplastic patients who underwent conventional, contrast enhancement and 3D-pCASL imaging at 3.0-T MR; all lesions were significantly enhanced. Quantitative parameters including cerebral blood flow (CBF) and relative cerebral blood flow (rCBF) were compared between neoplastic and non-neoplastic using Student's t-test. In addition, the area under the receiver operating characteristic (ROC) curve (AUC) was measured to assess the differentiation diagnostic performance of each parameter. Results: The non-neoplastic group demonstrated significantly lower rCBF values of lesions and perilesional edema compared with the neoplastic group. For the ROC analysis, both relative cerebral blood flow of lesion (rCBF-L) and relative cerebral blood flow of perilesional edema (rCBF-PE) had good diagnostic performance for discriminating non-neoplastic from neoplastic lesions, with an AUC of 0.994 and 0.846, respectively. Conclusion: 3D-pCASL may contribute to differentiation of non-neoplastic from neoplastic lesions.
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OBJECTIVE: To investigate the correlations between traditional Chinese medicine (TCM) syndrome elements and neurologic function and between them and coagulation function in patients with acute cerebral infarction (ACI). METHODS: Two hundred and twenty-three patients with ACI were enrolled. The syndromes of this disease were scored according to Stroke Diagnostic Criteria for Differentiation of Syndromes. Neurologic function deficit score (NDS) was scored according to stroke scale of the National Institutes of Health (NIHSS). The prothrombin time (PT), activated partial thromboplastin time (APTT) and fibrinogen (FIB) contents were detected. The correlations between TCM syndrome elements and NDS and between them and coagulation function were investigated. RESULTS: Two hundred and twenty-three patients with ACI were divided into six syndromes: wind syndrome (n=147, 65.92%), fire syndrome ( n=100, 44.84%), tan syndrome (n=123, 55.16%), blood stasis syndrome (n=78, 34.98%), deficiency of qi syndrome (n=31, 13.90%), and yin deficiency causing hyperactivity of yang syndrome (n=25, 11.21%). The wind, tan and fire syndromes were the main syndrome elements related to ACI. The scores of wind, fire, tan and deficiency of qi syndromes were positively related to NDS (r1=0.207, P1=0.002; r2=0.284, P2=0.000; r3=0.245, P3=0.000; r4=0.152, P4=0.023). The score of deficiency of qi syndrome was negatively correlated with PT (r=-0.170, P=0.011); and the scores of tan, blood stasis, and deficiency of qi syndromes were negatively correlated with APTT (r1=-0.182, P1=0.006; r2=-0.148, P2=0.027; r3=-0.211, P3=0.001).Other syndromes were not correlated to NDS or coagulation factors. CONCLUSION: The neurologic function deficiency due to ACI is more likely influenced by wind, tan, and fire syndromes; deficiency of qi syndrome also has some effects. The syndromes of tan, blood stasis, and deficiency of qi are closely correlated with coagulation function, and their scores may reflect the clotting function in patients with ACI.
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Infarto Cerebral/diagnóstico , Infarto Cerebral/fisiopatologia , Medicina Tradicional Chinesa , Sistema Nervoso/fisiopatologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Coagulação Sanguínea , Infarto Cerebral/sangue , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Deficiência da Energia Yin , Yin-YangRESUMO
In this text the interface of hardware and software for laboratory analyzer is analyzed. Adopting VC++ and multi-thread technique, the real-time communication without errors between LIS and the laboratory analyzer is realized. Practice proves that the system based on the technique is stable in running and all data are received accurately and timely.
Assuntos
Sistemas de Informação em Laboratório Clínico , Design de Software , Sistemas Computacionais , Interface Usuário-ComputadorRESUMO
BACKGROUND: Scutellarin is a natural flavone compound that possesses anti-tumor and chemosensitization effects in several cancers. However, the effects of scutellarin on metastasis and chemoresistance in glioma have not been illustrated. METHODS: Glioma cells were treated with scutellarin in the presence or absence of LY294002. Cell proliferation was measured using a Cell Proliferation BrdU ELISA kit. Cell migration and invasion were analyzed using transwell assay. The expressions of E-cadherin, N-cadherin, vimentin, p-PI3K, PI3K, p-AKT, AKT, p-mTOR and mTOR were measured using Western blot. Furthermore, cells were incubated in the presence of cisplatin with or without the pretreatment of scutellarin. Cell viability was detected by the MTT assay. Cell apoptosis was measured using a histone/DNA ELISA detection kit. The expressions of ABCB1 and ABCG2 were detected using Western blot. RESULTS: In the present study, we found that scutellarin inhibited the proliferation, migration, and invasion of glioma cells. Scutellarin induced E-cadherin expression and reduced the expressions of N-cadherin, and vimentin in glioma cells. Our results also revealed that scutellarin enhanced chemosensitivity to cisplatin, as evidenced by the decreased cell viability to cisplatin and induced cell apoptosis. Moreover, scutellarin inhibited the expressions of ATP-binding cassette subfamily B member 1 and ATP-binding cassette sub-family G member 2 in cisplatin-resistant glioma cells. Scutellarin also prevented the activation of phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin pathway. CONCLUSION: The data suggested that scutellarin suppressed metastasis and chemoresistance in glioma cells. Scutellarin might be a new therapeutic approach for the glioma therapy.
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In this study, attention has been focused on the ecology of yeasts during the spontaneous and inoculated fermentation processes of Vidal blanc icewine in northeast China, which is very important for screening autochthonous yeast strains, understanding the roles of these strains, and managing fermentation. The strategies were to conduct spontaneous and inoculated laboratory-scale fermentation processes simultaneously and to analyze the samples taken at different fermentation stages by culture-dependent and -independent methods. Three hundred and thirty-eight yeast strains were isolated and twelve genera were identified by sequencing. During the spontaneous fermentation process, non-Saccharomyces yeasts were predominant in the initial and middle stages, whereas Saccharomyces dominated in the later stages; Candida was preponderant in the whole process, and its abundance in the final stages was only lower than Saccharomyces. The inoculated fermentation was characterized by a predominance of Saccharomyces throughout the fermentation process; non-Saccharomyces yeasts were observed in the early stage. The internal transcribed spacer (ITS) 2 region gene was firstly used to analyze the yeast diversity in the samples during the icewine fermentation processes by high-throughput sequencing (HTS), and a more complex mycobiota was revealed. Moreover, the dynamics of other major fungi (mainly Davidiella and Alternaria) during icewine fermentation processes were also revealed, which have never been reported in icewine before.
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UGTs play crucial roles in the metabolism and detoxification of both endogenous and xenobiotic compounds. The key roles of UGTs in human health have garnered great interest in the design and development of specific probes for human UGTs. However, in contrast to other human enzymes, the probe substrates for human UGTs are rarely reported, owing to the highly overlapping substrate specificities of UGTs and the lack of the integrated crystal structures of UGTs. Over the past decades, many efforts are made to develop specific probe substrates for UGTs and use them in both basic research and drug discovery. This review focuses on recent progress in the development of probe substrates for UGTs and their biomedical applications. A long list of chemical probes for UGTs, including non-fluorescent and fluorescent probes along with their structural information and kinetic parameters, are prepared and analyzed. Additionally, challenges and future directions in this field are highlighted in the final section. All information and knowledge presented in this review provide practical tools/methods for measuring UGT activities in complex biological samples, which will be very helpful for rapid screening and characterization of UGT modulators, and for exploring the relevance of UGT enzymes to human diseases.
Assuntos
Glucuronosiltransferase/metabolismo , Glucuronosiltransferase/genética , Humanos , Cinética , Especificidade por SubstratoRESUMO
The tripartite motif-containing (TRIM) family is a group of proteins that are implicated in a plethora of pathological conditions. TRIM22 has been found to be involved in various cancers; however, the role of TRIM22 in gliomas has not been reported. The present study aimed to evaluate the expression pattern of TRIM22 and its function in gliomas. TRIM22 expressions in glioma tissues and cell lines were measured by RT-PCR and western blot analysis. To knockdown TRIM22 by small hairpin RNAs (shTRIM22), the U118 cells were transfected with pLKO.1-shTRIM22 plasmid or pLKO.1 plasmid. Cell proliferation was measured using CCK-8 assay. Transwell assays were performed to evaluate the migration and invasion. The epithelial-mesenchymal transition (EMT) was assessed by detecting the expressions of E-cadherin, N-cadherin and vimentin with western blot analysis. A xenograft mouse model was established to evaluate the effect of TRIM22 silencing on tumor growth in vivo. The expressions of ß-catenin, cyclin D1, and c-Myc were analyzed by western blot analysis. TRIM22 was significantly overexpressed in glioma tissues and cell lines. In vitro studies demonstrated that TRIM22 knockdown inhibited cell proliferation, migration, and invasion. Additionally, TRIM22 silencing increased the expressions of E-cadherin, and decreased the expressions of N-cadherin and vimentin. Nude mouse xenograft assay showed that TRIM22 silencing inhibited tumor growth in vivo. Furthermore, silencing of TRIM22 inhibited the activation of the Wnt/ß-catenin pathway. Treatment with LiCl, an activator of the Wnt/ß-catenin pathway, attenuated the effects of shTRIM22 on U118 cells. Silencing of TRIM22 inhibited proliferation, migration and invasion, as well as repressing the EMT process in glioma cells. The Wnt/ß-catenin pathway was involved in the effect of TRIM22.
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Amentoflavone (AMF), an abundant natural biflavonoid found in many medicinal plants, displays various beneficial effects including anti-inflammatory, anti-oxidative and anti-cancer. Despite the extensive studies on pharmacological activities, the toxicity or undesirable effects of AMF are rarely reported. In this study, the inhibitory effects of AMF on human UDP-glucuronosyltransferases (UGTs) were carefully investigated. AMF displayed strong inhibition towards most of human UGTs including UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A8, 1A9, 1A10, 2B4 and 2B17, with the IC50 values ranging from 0.12⯵M to 16.81⯵M. Inhibition constants (Ki) of AMF against various human UGTs varied from 0.29⯵M to 11.51⯵M. Further investigation demonstrated that AMF was a noncompetitive inhibitor of UGT1A1 mediated NCHN-O-glucuronidation but functioned as a competitive inhibitor of UGT1A1 mediated 4-MU-O-glucuronidation. In addition, AMF was a competitive inhibitor of UGT1A4 mediated TFP-N-glucuronidation in both UGT1A4 and human liver microsomes, while functioned as a competitive inhibitor of UGT1A9 mediated propofol or 4-MU-O-glucuronidation. These findings demonstrated that AMF was a strong and broad-spectrum natural inhibitor of most human UGTs, which might bring potential risks of herb-drug interactions (HDIs) via UGT inhibition. Additionally, this study provided novel insights into the underlying mechanism of AMF-associated toxicity from the perspective of UGT inhibition.
Assuntos
Biflavonoides/metabolismo , Glucuronosiltransferase/metabolismo , Biflavonoides/química , Cromatografia Líquida de Alta Pressão , Glucuronosiltransferase/antagonistas & inibidores , Glucuronosiltransferase/genética , Humanos , Himecromona/química , Himecromona/metabolismo , Concentração Inibidora 50 , Cinética , Microssomos Hepáticos/metabolismo , Propofol/química , Propofol/metabolismo , Proteínas Recombinantes/biossíntese , Proteínas Recombinantes/química , Proteínas Recombinantes/genéticaRESUMO
Excess fructose consumption can lead to metabolic syndrome, including insulin resistance, dyslipidemia, and hepatic injury, which are associated with oxidative stress and inflammation. The present study was to investigate whether fisetin improved multiple disturbances induced by fructose consumption. First, fisetin was found to be nontoxic to mice after an 8 week treatment. Second, the mice fed with a high-fructose (HFru)-diet for 8 weeks exhibited insulin resistance, dyslipidemia, hepatic injury, oxidative stress, and inflammation. Fisetin supplementation effectively improved the undesirable results mentioned above when compared to the HFru group. Meanwhile, fisetin significantly suppressed the nuclear factor κ-light-chain-enhancer of activated B cells (NF-κB) pathway and activated the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway in mice fed with HFru. Our findings demonstrated that fisetin exerted the beneficial effects in HFru-feeding mice, which might be associated with suppression of NF-κB and activation of the Nrf2 pathway.
Assuntos
Dieta , Flavonoides/administração & dosagem , Frutose/administração & dosagem , Síndrome Metabólica/prevenção & controle , Animais , Antioxidantes/administração & dosagem , Flavonóis , Inflamação/prevenção & controle , Resistência à Insulina , Masculino , Síndrome Metabólica/etiologia , Camundongos , Camundongos Endogâmicos C57BL , Fator 2 Relacionado a NF-E2/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Estresse Oxidativo/efeitos dos fármacosRESUMO
OBJECTIVE: To observe the clinical effect of TCM treatment for dissolving phlegm and dispelling stasis (DP-DS) on acute cerebral infarction (ACI) and its influences on plasma protein C and S and soluble thrombomodulin (TM). METHODS: One hundred and twenty-two patients were randomly assigned to two groups, the treated group (62 cases) and the control group (60 cases). They were all treated with the conventional treatment, and DP-DS treatment was given to the treated group additionally. The treatment course was 14 days. The changes in scores of TCM syndrome and neurofunction impairment (NIHSS), levels of plasma protein C (PC), protein S (PS) and TM before and after treatment in the two groups were observed. RESULTS: The total effective rate of TCM syndrome in the treated group was higher than that in the control group (P= 0.00). After treatment, NIHSS in the two groups was significantly different (P=0.00), and the score in the treated group was superior to that in the control group (P = 0.00). NIHSS score and levels of PC and PS were improved in both groups (P = 0.024, 0.028), and the improvement of PC in the treated group was superior to that in the control group respectively (P = 0.049). But no significant change of TM was shown after treatment. CONCLUSION: TCM DP-DS treatment shows significant effect in improving TCM syndrome and neurofunction impairment of the patients with acute cerebral infarction, and raise the levels of PC and PS.
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Infarto Cerebral/terapia , Medicina Tradicional Chinesa/métodos , Proteína C/metabolismo , Trombomodulina/sangue , Idoso , Infarto Cerebral/sangue , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , FitoterapiaRESUMO
Hepatocellular carcinoma-related protein 1 (HCRP1), also known as the homologue of vacuolar protein sorting 37A (hVps37A), serves as a membrane trafficking complex to mediate internalization and degradation of ubiquitinated membrane receptors. Recently, more and more researchers have showed that HCRP1 plays a critical role in tumorigenesis. However, the biological roles of HCRP1 in glioma remain to be elucidated. In the present study, we detected the expression pattern of HCRP1 in glioma. The results showed that HCRP1 was significantly down-regulated in glioma tissues and cell lines. On the basis of further analysis, we demonstrated that up-regulation of HCRP1 efficiently inhibited glioma cell proliferation and invasion in vitro, and as well as suppressed glioma cell growth in vivo. In addition, we found that HCRP1 up-regulation decreased the levels of p-ERK and p-AKT in glioma cells. We also emphasized that the ERK and AKT signaling pathways were the mechanisms underlying the inhibitory effect of HCRP1 on glioma cells. Taken together, we provided evidence in support of the prognostic value of HCRP1 in glioma and suggested it as a promising target for glioma treatment.
Assuntos
Complexos Endossomais de Distribuição Requeridos para Transporte/metabolismo , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Glioma/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Regulação para Cima , Animais , Astrócitos/efeitos dos fármacos , Astrócitos/metabolismo , Linhagem Celular Tumoral , Regulação para Baixo , MAP Quinases Reguladas por Sinal Extracelular/genética , Feminino , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , Invasividade Neoplásica , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/metabolismo , Proteínas Proto-Oncogênicas c-akt/genética , Transdução de Sinais/fisiologiaRESUMO
Progestin and AdipoQ Receptor 3 (PAQR3), a member of the PAQR family, is down-regulated in several types of cancers and has been closely associated with tumor progression and development. However, little is known about the functions of PAQR3 in the tumorigenesis of human glioma. Therefore, in this report, we investigated the role of PAQR3 in human glioma. Our results showed that the expression of PAQR3 was significantly reduced in human glioma tissues and cell lines. PAQR3 overexpression inhibited the proliferation of glioma cells in vitro and attenuated tumor xenograft growth in vivo. In addition, PAQR3 overexpression suppressed the migration and invasion of glioma cells, as well as prevented the EMT process. Mechanistic studies demonstrated that PAQR3 overexpression significantly down-regulated the levels of phosphorylated PI3K and Akt in U251 cells. In conclusion, these results demonstrated that PAQR3 inhibited the proliferation, migration and invasion in glioma cells, at least in part, through the inactivation of PI3K/Akt signaling pathway. Therefore, PAQR3 may be a therapeutic target for the treatment of glioma.