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1.
Biomed Chromatogr ; : e5026, 2020 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-33169423

RESUMO

Bidens bipinnata L. is a folk medicinal plant in China that shows significant antihyperlipidemia effectiveness. However, studies of the underlying mechanism study are lacking. In order to explore the potential action sites and the underlying mechanism of treating hyperlipidemic, this work undertook tissue distribution and molecular docking research on the markers of B. bipinnata L., which were obtained through serum pharmacochemistry and network database retrieval. The results showed that seven compounds (gallic acid, protocatechuic acid, rutin, hyperoside, bipinnate polyacetylenicloside, luteolin and quercetin) were screened out as markers. Owing to the diversity of chemical structures, they exhibited an inconsistent trend in tissue distribution. However, all of them had high levels in the liver and no specific distribution in other tissues. More interestingly, seven proteins-HMGCR (1HWK), NR3C1 (4P6W), CYP1A2 (2HI4), RXRA (4PP3), CES1 (1MX1), HSD11B1 (2RBE) and CYP1A1 (4I8V)-showed significant binding affinity with three or more markers, suggesting that they may be the target proteins of B. bipinnata L. This study preliminarily sheds light on the tissue distribution and targets of B. bipinnata L., providing some useful information on the underlying mechanisms of the antihyperlipidemia effect.

2.
Front Pharmacol ; 11: 579068, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33041823

RESUMO

Integrins are the adhesion molecules and receptors of extracellular matrix (ECM). They mediate the interactions between cells-cells and cells-ECM. The crosstalk between cancer cells and their microenvironment triggers a variety of critical signaling cues and promotes the malignant phenotype of cancer. As a type of transmembrane protein, integrin-mediated cell adhesion is essential in regulating various biological functions of cancer cells. Recent evidence has shown that integrins present on tumor cells or tumor-associated stromal cells are involved in ECM remodeling, and as mechanotransducers sensing changes in the biophysical properties of the ECM, which contribute to cancer metastasis, stemness and drug resistance. In this review, we outline the mechanism of integrin-mediated effects on biological changes of cancers and highlight the current status of clinical treatments by targeting integrins.

3.
Front Microbiol ; 11: 1511, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32765441

RESUMO

Human cytomegalovirus (HCMV), a ubiquitous beta-herpesvirus, is able to establish lifelong latency after initial infection. Periodical reactivation occurs after immunosuppression, remaining a major cause of death in immunocompromised patients. HCMV has to reach a structural and functional balance with the host at its earliest entry. Virion-carried mediators are considered to play pivotal roles in viral adaptation into a new cellular environment upon entry. Additionally, one clear difference between primary infection and reactivation is the idea that virion-packaged factors are already formed such that those molecules can be used swiftly by the virus. In contrast, virion-carried mediators have to be transcribed and translated; thus, they are not readily available during reactivation. Hence, understanding virion-carried molecules helps to elucidate HCMV reactivation. In this article, the impact of virion-packaged molecules on viral structure, biological behavior, and viral life cycle will be reviewed.

4.
J Ethnopharmacol ; 262: 113196, 2020 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-32730873

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hyperlipidemia (HLP) is a prevalence chronic cardiovascular disease, which is treated by traditional Chinese medicine (TCM) in China. More and more attention has been paid to the application of metabolomics in the study of TCM. Bidens bipinnata L. (BBL), a folk medicine in contemporary China, has the efficacy in the treatment of hyperlipidemia (HLP) in China. However, little is known of the underlying mechanism of BBL. This research aimed to investigate ameliorative effects of BBL on hyperlipidemic rats and explore the mechanism by metabolomics method. MATERIALS AND METHODS: Hyperlipidemic rats were established by high fat diet (HFD). Biochemical assay was used to evaluate the efficacy of BBL. A metabolomics approach based on high performance liquid chromatography-linear ion trap/orbitrap high-resolution mass spectrometry (HPLC-LTQ/orbitrap MS) was performed to analyze the serum biomarkers from model group, control group and BBL group. Principle component analysis (PCA) and partial least-squares discriminate analysis (PLS-DA) were utilized to identify differences of metabolic profiles in rats among the three groups. In order to identify possible pathways that were affected by HLP, the identified endogenous metabolites were analyzed by using MetaboAnalyst. In the network pharmacology study, our research group found that PPAR signaling pathway was the most important pathway of BBL in the treatment of HLP. Then, it was found that changes in the major metabolic pathways would affect the PPAR signaling pathway through comprehensive analysis based on KEGG database. Therefore, the expression of key genes in the PPAR signaling pathway was detected by real-time quantitative fluorescence PCR (RT-qPCR). RESULTS: Six metabolites, which showed a significantly restoring trend from HLP to normal condition, were regarded as potential biomarkers of BBL treatment. The levels of phosphorylcholine, mevalonic acid and leukotriene B4 (LTB4) increased significantly (P < 0.01) in hyperlipidemic rats, while the levels of linoleic acid, arachidonic acid (AA) and lysophosphatidylcholine (18:0) (Lyso PC (18:0)) decreased significantly (P < 0.01) in comparison with control rats. Those endogenous metabolites were chiefly involved in linoleic acid metabolism, AA metabolism and terpenoid backbone biosynthesis. According to the results of RT-qPCR analysis, the mRNA expressions of PPAR α, PPAR ß and PPARγ in model group were difference compared with control group. And the expression difference could be regulated closer to normal level after BBL intervention. CONCLUSIONS: The results of biochemical assay, serum metabolic pattern and RT-qPCR analysis showed that BBL could exert a significant improvement on lipid levels, liver function, renal function, as well as the mRNA expression level of PPAR signaling pathway.

5.
Huan Jing Ke Xue ; 41(2): 801-808, 2020 Feb 08.
Artigo em Chinês | MEDLINE | ID: mdl-32608740

RESUMO

From October 2018 to April 2019, the surface sediment and overlying water samples were collected every two months from the upstream and downstream of the effluent outlet of the Caitianpu sewage treatment plant in the Banqiao River, Hefei City. The effects of the sewage treatment plant effluent on both phosphorus forms and the equilibrium phosphate concentration (EPC0) in sediments were analyzed. The response of equilibrium phosphate concentration to external carbon (sodium acetate) and the release risk of phosphorus in sediments were investigated. Result show that the phosphorus pollution in Banqiao River was more severe. The average values of total phosphorus in the sediments at the upper and lower effluent outlet were 789.39 mg·kg-1 and 854.41 mg·kg-1, respectively, and the average bio-available phosphorus amounts were 157.19 mg·kg-1 and 173.37 mg·kg-1, respectively. The EPC0 values of the four sampling points decreased in the order SP1 > SP2 > SP3 > CP, indicating that the sewage treatment plant effluent increased the EPC0 level and phosphorus release risk of the stream sediments. Moreover, the addition of exogenous carbon significantly decreased the EPC0 value of the sediment, especially in SP1, suggesting that the addition of exogenous carbon decreased the risk of phosphorus release from sediments.

6.
Gynecol Minim Invasive Ther ; 9(2): 74-80, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32676284

RESUMO

Objectives: The objective of this study is to evaluate the efficacy of autocross-linked hyaluronic acid (HA) compared with intrauterine device (IUD) for preventing intrauterine adhesions (IUAs) in infertile patients after hysteroscopic adhesiolysis. Materials and Methods: A randomized clinical trial (ChiCTR-IOR-16007746). Upon completion of adhesiolysis, 3 ml of HA gel was placed into the uterine cavity in Group A; 3 ml of HA gel and an IUD were placed in Group B; and only an IUD was placed in Group C. A second hysteroscopic examination was performed in all patients at approximately 1 month postoperatively for the evaluation of IUA. The primary outcome measure was the effective rate of IUA prevention based on the American Fertility Society (AFS) scoring system. Results: Eighty-nine women were randomly distributed into two groups for intention to treat with 30 patients in Group A, 24 patients in Group B, and 35 patients in Group C. Patients were scored and stratified into three degrees and were enrolled using the simple random sampling method. The three groups were well balanced. There were no significant differences in age, endometrial thickness, the previous number of pregnancy, and the distribution of adhesion categories across mild, moderate, and severe between the three groups. The effective rate of IUA prevention, the AFS score after therapy, and the percentage improvements of Chinese score and AFS score before and after surgery were statistically significant difference between Groups A and C. The clinical pregnancy rate in Group A was higher than those in Groups B and C, but the difference was not statistically significant. Conclusion: HA gel has an advantage over an IUD in reducing IUA recurrence and decreasing adhesions.

7.
Ann Transl Med ; 8(6): 386, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32355830

RESUMO

Background: This study set out to evaluate the clinical significance and diagnostic effectiveness of serological tests and real-time polymerase chain reactions (RT-PCR) in children of different age groups and disease durations infected with Mycoplasma pneumoniae (MP). Methods: Pediatric patients with lower respiratory tract infection (LRTI) confirmed by polymerase chain reaction (PCR) were enrolled and subjected to bronchoalveolar lavage fluid PCR (BALF-PCR) for MP infection. The diagnostic values of the serum immunoglobulin M (IgM) test, paired sera immunoglobulin G (IgG) test, RT PCR applied to nasopharyngeal aspirates (NPA-PCR), and combined IgM and NPA-PCR test were evaluated. Results: When BALF PCR was used as the gold standard, the MP positivity rate of combined IgM and NPA PCR was 78.85%in children aged 3-5 years. The positivity rates of IgM, NPA PCR, and combined IgM and NPA PCR in children older than 5 years were 71.21%, 72.72%, and 84.85%, respectively. The detection rate of combined IgM and NPA PCR was consistent with BALF PCR (Kappa =0.727). The MP positivity rates of combined IgM and NPA PCR at 1-2 weeks was as high as 91.11%, and was consistent with the BALF PCR (Kappa =0.756). Moreover, the positivity rates of IgM or NPA PCR at 2-3 weeks were 63.16%, and were consistent with each other (Kappa =0.771). Conclusions: Combined IgM and NPA PCR is the optimal test to confirm MP infection among children aged 3-5 years in cases with a disease duration of less than2 weeks, and either NPA PCR or IgM is recommended for children older than 5 years with a disease duration of 2-3 weeks. Keywords: Mycoplasma pneumoniae pneumonia (MPP); diagnosis; children; age; disease duration.

8.
J Integr Neurosci ; 19(1): 21-29, 2020 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-32259883

RESUMO

The neuroprotective role of Fructus Broussonetiae in a model of chronic cerebral hypoperfusion with cognitive decline was focused on neural plasticity and microglia/macrophage polarization. Chronic cerebral hypoperfusion was induced by bilateral common carotid artery ligation. Fructus Broussonetiae shortened escape latency and added the number of platform crossings of rats, up-regulated the expression of synaptophysin in the gray matter and increased myelin basic protein expression in the white matter. Further mechanistic experiments were conducted to examine microglia activation and M1/M2 polarization. It was shown that Fructus Broussonetiae reduced the activation of microglia revealed by decreased expression of ionized calcium-binding adapter molecule-1, inhibited M1 polarization of microglia and improved microglial M2 polarization shown by down-regulated the expression of inducible nitric oxide synthase and Fc fragment of IgG receptor IIIa and up-regulated the expression of arginase-1. In conclusion, the Chinese herb Fructus Broussonetiae can improve cognitive function following chronic cerebral hypoperfusion by down-regulating the activation of microglia, inhibiting microglial M1 polarization, and improving neural plasticity.


Assuntos
Encéfalo/efeitos dos fármacos , Broussonetia , Transtornos Cerebrovasculares/complicações , Disfunção Cognitiva/fisiopatologia , Aprendizagem em Labirinto/efeitos dos fármacos , Microglia/efeitos dos fármacos , Fármacos Neuroprotetores/administração & dosagem , Memória Espacial/efeitos dos fármacos , Animais , Encéfalo/fisiopatologia , Transtornos Cerebrovasculares/fisiopatologia , Disfunção Cognitiva/etiologia , Disfunção Cognitiva/prevenção & controle , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/administração & dosagem , Masculino , Microglia/fisiologia , Ratos Sprague-Dawley
9.
Int J Pharm ; 582: 119331, 2020 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-32289484

RESUMO

The major drawbacks of the cytotoxin like DM1 are the off-target effects. Here, the targeting nanovesicles were developed by synthesizing tocopherol-SS-DM1 and conjugating a pH low insertion peptide (pHLIP) to PEGylated phospholipids, in which tocopherol-SS-DM1 improves the drug loading and is glutathione responsive in the cytoplasm, meanwhile, the pH insertion peptide targets the acidic microenvironment of cancer cells. Besides, these nanovesicles can accumulate at the endoplasmic reticulum and show increased cancer therapeutic effects both in vitro and in vivo. These targeting nanovesicles provide a novel formulation for subcellular organelle targeting, a platform for precisely delivery of cytotoxic DM1 to cancer cells, and an alternative strategy for antibody-drug conjugates (ADCs).

10.
World J Clin Cases ; 7(15): 2110-2119, 2019 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-31423445

RESUMO

BACKGROUND: Cystic fibrosis (CF) is rare in Asian populations relative to the Caucasian population. In this paper, we report the cystic fibrosis transmembrane conductance regulator (CFTR) variation in a family of Chinese CF patients, and systematically review the previous literature. CASE SUMMARY: Here we report a 30-month-old Chinese girl who was diagnosed with CF based on her history and symptoms such as recurrent productive cough, wheezing with repeated infection of Pseudomonas aeruginosa, and parasinusitis. Chest computed tomography (CT) scanning revealed obvious exudative lesions and bilateral bronchiectasis. Liver CT scanning revealed a low-density lesion in the left lobe of the liver. A diagnosis of CF was made based upon CFTR gene tests. The CFTR gene was sequenced using the blood samples of her and her parents and showed a heterozygous novel missense mutation of c.753_754delAG in exon 7. In addition, a heterozygous c.1240 C>T mutation was found in exon 10 of the CFTR. The mutation c.753_754delAG was verified to have been inherited from her mother, and the c.1240 C>T mutation was from her father who was diagnosed with congenital absence of vas deferens. CONCLUSION: A novel mutation of CFTR, c.753_754delAG, was found in a Chinese CF child. c.2909G>A is the most common mutation among Chinese CF patients.

11.
Artigo em Inglês | MEDLINE | ID: mdl-31320916

RESUMO

Objective. To ascertain the efficacy and safety of Ganji Formulation (GF) for patients with Hepatocellular carcinoma (HCC) who had undergone surgery. Materials and Methods. A total of 262 HCC patients who had undergone liver resection, local ablation, or transcatheter arterial chemoembolization (TACE) were divided randomly into the treatment group and control group. The former was treated with GF and the later with placebo, both for 6 months. The primary endpoint was overall survival (OS). Second endpoints were disease-free survival (DFS) or time to disease progression (TTP). Results. OS of the treatment group was significantly longer than that of the control group (P < 0.05). Subgroup analysis showed that, for patients who received TACE, the TTP was significantly longer in the treatment group than in the control group (P < 0.05). However, for patients who underwent liver resection or local ablation, there was no significant difference in DFS between the two groups (P > 0.05). Conclusion. GF could improve postoperative cumulative survival and prolong the TTP. This clinical trial number is registered with ChiCTR-IOR-15007349.

12.
Zhongguo Dang Dai Er Ke Za Zhi ; 21(6): 505-510, 2019 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-31208500

RESUMO

OBJECTIVE: To investigate the viral etiology and allergen distribution in infants and young children at high risk of asthma during a wheezing episode. METHODS: A total of 135 infants and young children at high risk of asthma were enrolled who were admitted due to asthmatic bronchitis or asthmatic bronchopneumonia between April 2016 and August 2017. Fluorescent probe PCR was used to measure influenza A (Flu A), respiratory syncytium virus (RSV), adenovirus (ADV), parainfluenza virus (PinF), human rhinovirus (HRV), human partial lung virus (hMPV) and human bocavirus (HBoV) in nasopharyngeal aspirates. ImmunoCAP was used to measure inhaled allergens, food allergens, and total IgE concentration. RESULTS: Among the 135 patients, the overall virus detection rate of nasopharyngeal aspirates was 49.6%, and HRV had the highest detection rate of 25.2%, followed by HBoV (9.6%), RSV (8.1%), PinF (5.9%), Flu-A (3.7%), ADV (1.5%) and hMPV (0.7%). The 1-3 years group had a significantly higher detection rate of HRV than the <1 year group (P<0.05). The positive rate of allergen screening was 59.3%, with 44% for inhaled allergens and 89% for food allergens. Among the inhaled allergens, dust mites had the highest positive rate of 77%, followed by mould (37%), pollen (26%) and animal dander (9%). Among the food allergens, egg white had a positive rate of 73% and milk had a positive rate of 68%. The <1 year group had a significantly higher positive rate of inhaled allergens than the 1-3 years group (P<0.05). The 1-3 years age group had a significantly higher level of T-IgE than the <1 year group (P<0.05). The positive virus group had a significantly higher positive rate of inhaled allergens than the non-virus group (P<0.05). The children with the second wheezing episode had significantly higher positive rates of inhaled allergens and food allergens and level of T-IgE than those with the first wheezing episode (P<0.05). The children with the second wheezing episode also had significantly higher positive rates of dust mites and mould than those with the first wheezing episode (P<0.05). CONCLUSIONS: Early HRV infection and inhaled allergen sensitization are closely associated with the development of wheezing in infants and young children at high risk of asthma.


Assuntos
Asma , Hipersensibilidade a Ovo , Alérgenos , Animais , Criança , Pré-Escolar , Humanos , Lactente , Pyroglyphidae , Sons Respiratórios
13.
J Med Chem ; 62(6): 3147-3162, 2019 03 28.
Artigo em Inglês | MEDLINE | ID: mdl-30827110

RESUMO

Homologous recombination repair (HRR), a crucial approach in DNA damage repair, is an attractive target in cancer therapy and drug design. The Bloom syndrome protein (BLM) is a 3'-5' DNA helicase that performs an important role in HRR regulation. However, limited studies about BLM inhibitors and their biological effects have been reported. Here, we identified a class of isaindigotone derivatives as novel BLM inhibitors by synthesis, screening, and evaluating. Among them, compound 29 was found as an effective BLM inhibitor with a high binding affinity and good inhibitory effect on BLM. Cellular evaluation indicated that 29 effectively disrupted the recruitment of BLM at DNA double-strand break sites, promoted an accumulation of RAD51, and regulated the HRR process. Meanwhile, 29 significantly induced DNA damage responses, as well as apoptosis and proliferation arrest in cancer cells. Our finding provides a potential anticancer strategy based on interfering with BLM via small molecules.


Assuntos
Alcaloides/farmacologia , DNA/metabolismo , Descoberta de Drogas , Inibidores Enzimáticos/farmacologia , Quinazolinas/farmacologia , RecQ Helicases/antagonistas & inibidores , Reparo de DNA por Recombinação , Alcaloides/química , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Quebras de DNA de Cadeia Dupla/efeitos dos fármacos , Inibidores Enzimáticos/química , Células HCT116 , Humanos , Quinazolinas/química , Rad51 Recombinase/metabolismo , RecQ Helicases/metabolismo
14.
World J Clin Cases ; 7(24): 4355-4365, 2019 Dec 26.
Artigo em Inglês | MEDLINE | ID: mdl-31911919

RESUMO

BACKGROUND: Multisystemic smooth muscle dysfunction syndrome (MSMDS) is a rare genetic disease worldwide. The main mutation is the actin alpha 2 (ACTA2) gene p.R179H. In this paper, we report a Chinese MSMDS patient and systematically review the previous literature. CASE SUMMARY: Here, we report a 9.6-month-old Chinese girl who was diagnosed with MSMDS based on her history and symptoms, such as recurrent cough, wheezing, and complications with congenital fixed dilated pupils. Chest high-resolution computed tomography revealed inhomogeneous lung transparency, obvious exudative lesions, and some lung fissures that were markedly thickened. Cranial magnetic resonance imaging excluded bleeding and infarction but showed abnormal signals in the centrum ovale majus and bilateral periventricular regions. Echocardiography only showed patent foramen ovale, and no patent ductus arteriosus, pulmonary artery dilatation, or pulmonary hypertension was found. Bronchoscopy indicated moderate bronchial malacia. These examinations in conjunction with the typical eye abnormality suggested a diagnosis of MSMDS, and sequencing of exon 6 of the ACTA2 gene demonstrated the heterozygous mutation c.536G>A, p.R179H. However, her parents' gene analyses were normal. CONCLUSION: MSMDS is a rare genetic disease mainly caused by the mutation of the ACTA2 gene p.R179H. Early genetic diagnosis should be performed for children presenting with congenital fixed dilated pupils and patent ductus arteriosus. During the process of diagnosis and treatment, clinicians should be on high alert for cerebrovascular, cardiovascular, and pulmonary complications.

15.
Sci Rep ; 8(1): 16287, 2018 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-30389975

RESUMO

Totally asymmetric simple exclusion process (namely, TASEP) is one of the most vital driven diffusive systems, which depicts stochastic dynamics of self-driven particles unidirectional updating along one-dimensional discrete lattices controlled by hard-core exclusions. Different with pre-existing results, driven diffusive system composed by multiple TASEPs with asymmetric heterogeneous interactions under two-dimensional periodic boundaries is investigated. By using detailed balance principle, particle configurations are extensively studied to obtain universal laws of characteristic order parameters of such stochastic dynamic system. By performing analytical analyses and Monte-Carlo simulations, local densities are found to be monotone increase with global density and spatially homogeneous to site locations. Oppositely, local currents are found to be non-monotonically increasing against global density and proportional to forward rate. Additionally, by calculating different cases of topologies, changing transition rates are found to have greater effects on particle configurations in adjacent subsystems. By intuitively comparing with pre-existing results, the improvement of our work also shows that introducing and considering totally heterogeneous interactions can improve the total current in such multiple TASEPs and optimize the overall transport of such driven-diffusive system. Our research will be helpful to understand microscopic dynamics and non-equilibrium dynamical behaviors of interacting particle systems.

16.
Huan Jing Ke Xue ; 39(8): 3927-3936, 2018 Aug 08.
Artigo em Chinês | MEDLINE | ID: mdl-29998703

RESUMO

Marine microalgae, Platymonas helgolondica var. tsingtaoensis, were used as experimental subjects to study the acute toxic effects of graphene oxide (GO) and dibutyl phthalate (DBP), both individually and together. The growth of algae cells, production of photosynthetic pigments, cell permeability, and oxidative stress were investigated. The effects of GO on the algal toxicity of DBP were evaluated. The results showed that low concentrations of GO (0.1-10 mg·L-1) had no significant effect on algae density and chlorophyll production of Platymonas helgolondica var. tsingtaoensis (P<0.05). However, the algae cell permeability increased significantly with GO concentration (P<0.05) and reached 2.2 times that of the control group at 10 mg·L-1. The EC50, 96 h value of DBP for Platymonas helgolondica var. tsingtaoensis was (11.14±0. 80) mg·L-1, which, in terms of toxicity, was much higher than that of GO (EC50, 96 h>100 mg·L-1). At a GO concentration of 1 mg·L-1, the EC50, 96 h value of DBP decreased to (4.93±2.14) mg·L-1, showing that low concentrations of GO enhanced the algae toxicity of DBP. When 1 mg·L-1 of GO was added, low concentrations of DBP (0.1-2 mg·L-1) did not have any significant effect on algae density, chlorophyll production, cell permeability, ROS, and SOD. However, the inhibitory effects of high concentrations of DPB (4 mg·L-1) on algae density and chlorophyll production were enhanced by GO, thereby increasing the average ROS and SOD in algae cells by 21% and 7%, respectively. SEM images showed that GO was the primary factor responsible for increasing the coverage and packing of, and the aggregation effect on, algae cells, which could be the reasons for the increased toxicity of DBP. The results of our study can provide data to reveal the risk of novel carbon nanomaterial pollutants to marine organisms.


Assuntos
Clorófitas/efeitos dos fármacos , Dibutilftalato/toxicidade , Grafite/toxicidade , Nanopartículas/toxicidade , Clorofila/química , Óxidos
17.
Zhongguo Zhong Yao Za Zhi ; 43(12): 2570-2574, 2018 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-29950077

RESUMO

The present research aimed to establish an associated two-dimensional fingerprint of Huanglian between characteristic chemical composition and antioxidant activity, which was applied to on-line screen the active constituents. In this study, the HPLC-ABTS-DAD-Q-TOF/MS method, which can simultaneously identify individual components and rapidly screen for antioxidant compounds, was used to screen and identify antioxidant components in Huanglian. Fourteen compositions were discovered, and eight of them displayed antioxidant activity. The antioxidant activity of different ingredients was evaluated by antioxidant efficiency. The data showed that 2, 3, 4-trihydroxy phenylpropionic acid, chlorogenic acid, ferulic acid, cularine, 3-O-feruloylquinic acid and feruloyltyramine showed stronger antioxidant activity than that of alkaloids. These experimental data can provide data support for the basic research of the antioxidant ingredients of Huanglian.


Assuntos
Antioxidantes/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Cromatografia Líquida de Alta Pressão
18.
J Pharm Biomed Anal ; 156: 278-283, 2018 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-29730337

RESUMO

Yudanshen, the genuine medicinal materials of Danshen (Salvia miltiorrhiza), is a well-known traditional Chinese medicine (TCM) used to treat cardiovascular and cerebrovascular diseases. Although its pharmacological and antioxidative activities have been well-documented, there is little research on the hydroxyl radical (OH) scavenging capacity of Yudanshen. In this study, we established multiple on-line high-performance liquid chromatography- chemiluminescence detector-diode-quadrupole-time of flight mass spectrometry (HPLC-CL-DAD-Q-TOF/MS) methods to rapidly screen and identify the OH scavengers in Yudanshen simultaneously. The chromatographic and potency fingerprints revealed seventeen peaks that showed the inhibition of OH. Fourteen of them were identified as danshensu, protocatechuic aldehyde, caffeic acid, ferulic acid, salvianolic acid F, salvianolic acid H/L, salvianolic acid G, salvianolic acid D, salvianolic acid E, rosmarinic acid, salvianolic acid B, isosalvianolic acid B, salvianolic acid A, and salvianolic acid C. This study explores the OH scavenging activities of Yudanshen, and provides novel and powerful multiple on-line methods in the field of TCM for rapid screening and identification of OH scavengers.


Assuntos
Avaliação Pré-Clínica de Medicamentos/métodos , Medicamentos de Ervas Chinesas/química , Depuradores de Radicais Livres/análise , Salvia miltiorrhiza/química , Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/métodos , Contaminação de Medicamentos/prevenção & controle , Avaliação Pré-Clínica de Medicamentos/instrumentação , Depuradores de Radicais Livres/química , Radical Hidroxila/metabolismo , Medições Luminescentes/instrumentação , Medições Luminescentes/métodos , Espectrometria de Massas/instrumentação , Espectrometria de Massas/métodos
19.
Anticancer Drugs ; 29(6): 491-502, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29683800

RESUMO

The main aim of this study was to establish a novel paclitaxel (PTX)-resistant human gastric carcinoma cell line and to investigate its biological significance. A cell line, MGC803/PTX, was established by gradually increasing PTX density on the basis of MGC803 over a period of 10 months. In addition, a pair of resistant cell lines (SW620 and SW620/PTX) were added to further explain the resistant mechanism of PTX. The drug resistance index and stability of MGC803/PTX cells were detected using the Cell Counting Kit-8 method. The morphological features were observed using inverted microscopy. Apoptosis was measured by flow cytometry (FCM) and Hoechst 33258 fluorescence staining. The distribution of the cell cycle was determined by FCM, and protein expressions of P-gp, Bcl-2, Bax, and PARP were detected by western blot analysis. When characterizing the resistance in vitro, we found that MGC803/PTX cells were 10.3-fold more resistant to PTX compared with MGC803 cells. In addition, MGC803/PTX cells showed cross-resistance to 5-fluorouracil and adriamycin. FCM and Hoechst 33258 fluorescence staining indicated that MGC803/PTX cells had a significantly lower percentage of apoptotic cells after treatment with PTX compared with MGC803 cells. Other differences between parental cells and resistant cells included morphology, proliferation rate, doubling time, cell cycle distribution, and colony-formation rate. Western blot analysis indicated that P-gp, Bcl-2, and PARP protein were more abundant in MGC803/PTX and SW620/PTX cells compared with MGC803 and SW620 cells, whereas Bax protein levels were lower in resistant cells. Furthermore, MGC803/PTX cells showed obvious resistance to PTX in vivo. To our knowledge, this is the first report on the establishment of a PTX-resistant MGC803 cell line, which is an important tool to explore the resistance of anticancer drugs and to overcome tumor drug resistance.


Assuntos
Linhagem Celular Tumoral , Paclitaxel/farmacologia , Neoplasias Gástricas/tratamento farmacológico , Neoplasias Gástricas/patologia , Animais , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Apoptose/fisiologia , Processos de Crescimento Celular/efeitos dos fármacos , Processos de Crescimento Celular/fisiologia , Resistencia a Medicamentos Antineoplásicos , Feminino , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Fenótipo , Distribuição Aleatória , Ensaios Antitumorais Modelo de Xenoenxerto
20.
J Med Chem ; 61(8): 3436-3453, 2018 04 26.
Artigo em Inglês | MEDLINE | ID: mdl-29618208

RESUMO

Telomeric G-quadruplex targeting and telomere maintenance interference are emerging as attractive strategies for anticancer therapies. Here, a novel molecular scaffold is explored for telomeric G-quadruplex targeting. A series of novel schizocommunin derivatives was designed and synthesized as potential telomeric G-quadruplex ligands. The interaction of telomeric G-quadruplex DNA with the derivatives was explored by biophysical assay. The cytotoxicity of the derivatives toward cancer cell lines was evaluated by the methyl thiazolyl tetrazolium (MTT) assay. Among the derivatives, compound 16 showed great stabilization ability toward telomeric G-quadruplex DNA and good cytotoxicity toward cancer cell lines. Further cellular experiments indicated that 16 could induce the formation of telomeric G-quadruplex in cells, triggering a DNA damage response at the telomere and causing telomere dysfunction. These effects ultimately provoked p53-mediated cell cycle arrest and apoptosis, and suppressed tumor growth in a mouse xenograft model. Our work provides a novel scaffold for the development of telomeric G-quadruplex ligands.


Assuntos
Antineoplásicos/farmacologia , Dano ao DNA , DNA/genética , Indóis/farmacologia , Telômero/metabolismo , Animais , Antineoplásicos/síntese química , Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Descoberta de Drogas , Feminino , Quadruplex G , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Humanos , Indóis/síntese química , Indóis/uso terapêutico , Ligantes , Camundongos Endogâmicos BALB C , Telomerase/antagonistas & inibidores , Telômero/genética , Encurtamento do Telômero , Proteínas de Ligação a Telômeros/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Ensaios Antitumorais Modelo de Xenoenxerto
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