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1.
Water Res ; 204: 117583, 2021 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-34478995

RESUMO

UV-based water treatment processes have been reported to induce genotoxicity during the treatments of surface water, drinking water and artificial water with natural organic matters (NOMs), causing genotoxicity concerns for the drinking water safety. Nitrogenous disinfection byproducts (N-DBPs) were generally reported to be much more genotoxic than their non-nitrogenous analogues, and might be responsible for the genotoxicity in UV processes. Although nitrate-rich water was getting attention for the possibility of genotoxicity and N-DBPs during UV treatments, the impact mechanism of nitrate on the degradation of NOMs, the formation of N-DBPs and genotoxicity has not been explicated. Here simulation experiments of NOM degradation under medium-pressure (MP) UV and MP UV/H2O2 treatments were conducted to explore the effect of nitrate on the molecular characteristics of NOM, the nitrate-derived N-DBPs and the potential genotoxicity through non-targeted analysis and CALUX® reporter gene assays. The results showed that nitrate can accelerate the degradation of NOMs in the MP UV process but inhibit the degradation of NOMs in the MP UV/H2O2 process. During the degradation of NOMs, the molecular compositions varied by the effect of nitrate on oxygen atoms, molecule analogs, and saturation. A total of 105 and 374 nitrate-derived N-DBPs were identified in the MP UV and MP UV/H2O2 treatment, respectively. Most of these N-DBPs contain one nitrogen atom, and the representative features are nitro-, methoxy- (or hydroxyl-) and ester- groups on benzene. No genotoxicity was observed without nitrate spiking, whereas genotoxicity was induced after both MP UV and MP UV/H2O2 treatments when nitrate was spiked, which is worthy of attention for the drinking water safety management.

2.
Mol Med Rep ; 24(5)2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34490484

RESUMO

Naringin (Nar) is one of the natural glycosides extracted from pomelo and other citrus fruits. It has various pharmacological activities, including anti­inflammatory, antioxidant, anti­proliferative and anti­cancer. However, the underlying mechanisms by which Nar regulates apoptosis and autophagy in gastric cancer remain unclear. Thus, the present study aimed to assess the therapeutic effect of Nar and the underlying mechanisms. SNU­1 cell proliferation was determined using Cell Counting Kit­8 assay. Cell morphological changes were observed under a phase­contrast microscope. The changes in the cell cycle were determined using flow cytometry analysis and the changes in cell apoptosis were determined using flow cytometry, Hoechst 33258 and TUNEL staining. The protein levels pertaining to the PI3K/AKT pathway and cell apoptosis and autophagy were monitored using western blot analysis. The results demonstrated that Nar significantly inhibited SNU­1 cell growth and induced cell cycle arrest in the G0/G1 phase and cell apoptosis. Further mechanistic studies demonstrated that Nar blocked the PI3K/AKT pathway, activated cell autophagy and stimulated the expression of apoptosis­associated protein cleaved caspase 3 and Bax, but decreased the expression of Bcl­2. Preincubating SNU­1 cells with 3­methyladenine, a cell­autophagy inhibitor, significantly alleviated the effects of Nar in promoting cell apoptosis and cleaved caspase 3 expression. It was concluded that Nar promoted SNU­1 cell apoptosis via blocking the PI3K/AKT signaling pathway and activating cell autophagy.

3.
Dalton Trans ; 2021 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-34518853

RESUMO

Three mononuclear, dinuclear and one-dimensional dysprosium(III) complexes based on 3-azotriazolyl-2,6-dihydroxybenzoic acid (H4ATB) of [Dy(H3ATB)3]·3H2O (1), [Dy2(H2ATB)2(H2DHB)2(H2O)4]·2CH3CN·5H2O (2), and [Dy2(H2ATB)2(DCB)(DMF)2(H2O)2]·4DMF (3) were synthesized and structurally characterized by X-ray single crystal diffraction (H3DHB = 2,6-dihydroxybenzoic acid, H2DCB = 1,4-dicarboxybenzene). Complex 1 was used as a precursor to synthesize complexes 2 and 3, and 2 was further used to synthesize 3. Complex 1 is a mononuclear complex, in which the Dy(III) ion is in a nine-coordinated structure surrounded by three tridentate chelate H3ATB- ligands. Complex 2 displays a dinuclear structure bridged by two µ2 carboxyl groups of two H2DHB- ligands and two µ1,1-O atoms from the phenolic hydroxyl groups of two H2ATB2- ligands. Complex 3 shows a one-dimensional structure formed by two bridging DCB2- ligands. The magnetic measurements were performed on three complexes 1-3, and they showed different magnetic behavior. Complex 1 shows a field-induced slow magnetic relaxation. Complexes 2 and 3 display distinct slow magnetic relaxation under zero dc field with energy barriers (Ueff) of 26(2) cm-1 and 11(1) cm-1, respectively. The magnetic behavior of three complexes 1-3 was investigated by ab initio calculations.

4.
J Nat Prod ; 2021 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-34519213

RESUMO

The soil bacterium Streptomyces pactum ATCC 27456 produces a number of polyketide natural products. Among them is NFAT-133, an inhibitor of the nuclear factor of activated T cells (NFAT) that suppresses interleukin-2 (IL-2) expression and T cell proliferation. Biosynthetic gene inactivation in the ATCC 27456 strain revealed the ability of this strain to produce other polyketide compounds including analogues of NFAT-133. Consequently, seven new derivatives of NFAT-133, TM-129-TM-135, together with a known compound, panowamycin A, were isolated from the culture broth of S. pactum ATCC 27456 ΔptmTDQ. Their chemical structures were elucidated on the basis of their HRESIMS, 1D and 2D NMR spectroscopy, and ECD calculation and spectral data. NFAT-133, TM-132, TM-135, and panowamycin A showed no antibacterial activity or cytotoxicity, but weakly reduced the production of LPS-induced nitric oxide in RAW264.7 cells in a dose-dependent manner. A revised chemical structure of panowamycin A and proposed modes of formation of the new NFAT-133 analogues are also presented.

5.
Chem Asian J ; 2021 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-34519415

RESUMO

The properties of high stability, periodic porosity, and tunable nature of ordered mesoporous polymers make these materials ideal catalytic nanoreactors. However, the application of them in organocatalysis have been rarely explored. We report herein for the first time the incorporation of a versatile organocatalyst, 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO), into the pores of an FDU-type mesoporous polymer via pore surface engineering strategy. The resulting FDU-15-TEMPO possesses high ordered mesoporous organic framework and enhanced stability, and shows excellent catalytic activity in the selective oxidation of alcohols and aerobic oxidative synthesis of 2-substituted benzoxazoles, benzimidazoles and benzothiazoles. Moreover, the catalyst can be easily recovered and reused for up to 7 consecutive cycles.

6.
Neurochem Int ; : 105180, 2021 Sep 09.
Artigo em Inglês | MEDLINE | ID: mdl-34509561

RESUMO

The identity of the mechanism that controls aggressive behavior in rodents is unclear. Serotonin (5-HT) and GABA are associated with aggressive behavior in rodents. However, the regulatory relationship between these chemicals in the different brain regions of rats has not been fully defined. This study aimed to clarify the role of GABABR1 in DRN-mediated GABA to regulate 5-HT expression in multiple brain regions in male rats with high and low aggressive behavior. Rat models of highly and less aggressive behavior were established through social isolation plus resident intruder. On this basis, GABA content in the DRN and 5-HT contents in the PFC, hypothalamus, hippocampus and DRN were detected using ELISA. Co-expression of 5-HT and GB1 in the DRN was detected by immunofluorescence and immunoelectron microscopy at the tissue and subcellular levels, respectively. GB1-specific agonist baclofen and GB1-specific inhibitor CGP35348 were injected into the DRN by stereotaxic injection. Changes in 5-HT levels in the PFC, hypothalamus and hippocampus were detected afterward. After modeling, rats with highly aggressive behavior exhibited higher aggressive behavior scores, shorter latencies of aggression, and higher total distances in the open field test than rats with less aggressive behavior. The contents of 5-HT in the PFC, hypothalamus and hippocampus of rats with high and low aggressive behavior (no difference between the two groups) were significantly decreased, but the change in GABA content in the DRN was the opposite. GB1 granules could be found on synaptic membranes containing 5-HT granules, which indicated that 5-HT neurons in the DRN co-expressed with GB1, which also occurred in double immunofluorescence results. At the same time, we found that the expression of GB1 in the DRN of rats with high and low aggressive behavior was significantly increased, and the expression of GB1 in the DRN of rats with low aggressive behavior was significantly higher than that in rats with high aggressive behavior. Nevertheless, the expression of 5-HT in DRN was opposite in these two groups. After microinjection of baclofen into the DRN, the 5-HT contents in the PFC, hypothalamus and hippocampus of rats in each group decreased significantly. In contrast, the 5-HT contents in the PFC, hypothalamus and hippocampus of rats in each group increased significantly after injection with CGP35348. The significant increase in GABA in the DRN combined with the significant increase in GB1 in the DRN further mediated the synaptic inhibition effect, which reduced the 5-HT level of 5-HT neurons in the DRN, resulting in a significant decrease in 5-HT levels in the PFC, hypothalamus and hippocampus. Therefore, GB1-mediated GABA regulation of 5-HT levels in the PFC, hypothalamus and hippocampus is one of the mechanisms of highly and less aggressive behavior originating in the DRN. The increased GB1 level in the DRN of LA-behavior rats exhibited a greater degree of change than in the HA-group rats, which indicated that differently decreased 5-HT levels in the DRN may be the internal mechanisms of high and low aggression behaviors.

7.
Pharmazie ; 76(9): 422-427, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34481532

RESUMO

MicroRNAs are emerging as important endogenous regulators of gene function and they are playing an important role in the occurrence and development of cancer. They are also regarded as robust biomarkers of cancer diagnosis and prognosis. Hepatocellular carcinoma (HCC) is a common and complex human malignancy with high mortality and morbidity in the world. MicroRNA-122 (miR-122) is a liver-specific microRNA and is closely associated with HCC metastasis, which makes miR-122 a promising target for drug design and development. In this study, we performed a cell-based screening method for discovering miR-122 activators and found that oleanolic acid (OA), a natural pentacyclic triterpene, specifically increased miR-122 expression in a concentration-dependent manner. Two HCC cell lines (HepG2 and Sk-hep-1 cells) were used to evaluate the effect of OA on cell migration and invasion abilities. The results indicated that OA attenuated the migration and invasion abilities of HCC cells by upregulating miR-122 expression. In addition, OA increased the expression of E-cadherin and decreased the expression of ß-catenin, N-cadherin and vimentin. After knocking down miR-122 with miR-122 inhibitor, we found that the effect of OA on these epithelial-to-mesenchymal transition (EMT) related molecules was significantly weakened, indicating OA exhibited anti-EMT effect by increasing the expression of miR-122. These finding may help to better understand the molecular mechanism of OA's anti-metastasis activity.

8.
Eur J Surg Oncol ; 2021 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-34483031

RESUMO

BACKGROUND: Microsatellite instability, programmed death-ligand 1 and tumor-infiltrating leukocytes are prognostic biomarkers in colorectal cancer but unknown toward familial adenomatous polyposis. AIM: To investigate the prognostic and clinicopathological roles of microsatellite instability, programmed death-ligand 1 and tumor-infiltrating leukocytes in familial adenomatous polyposis. METHODS: Clinical data and paraffin embedded tissues from 45 familial adenomatous polyposis patients were collected. Microsatellite instability was detected by immunohistochemistry and polymerase chain reaction. Programmed death-ligand 1 was detected by immunohistochemistry. Tumor-infiltrating leukocytes comprising CD8+ T cells, M1 and M2 tumor associated macrophages, CD56bright and CD56dim natural killer cells were analyzed using multiple fluorescence immunohistochemistry. RESULTS: Microsatellite instability high was noted in 6 samples but not associated with overall survival or progression-free survival. Programmed death-ligand 1 is negative on tumor cells but positive on tumor-infiltrating leukocytes, and positive programmed death-ligand 1 expression on tumor-infiltrating leucocytes is associated with overall survival. Low CD56bright natural killer cell infiltration was associated with longer progression-free survival and was an independent prognostic factor in FAP. CONCLUSION: For familial adenomatous polyposis, microsatellite instability high can be found but has no correlation with prognosis; programmed death-ligand 1 on tumor-infiltrating leukocytes is related with overall survival; CD56bright natural killer cell is an independent prognostic factor associating with longer progression-free survival.

9.
Zhongguo Zhong Yao Za Zhi ; 46(12): 2912-2922, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34467681

RESUMO

The dried fruit body of Phylloporia ribis(Hymenochaetaceae), which prefers to live on the stumps of Lonicera japonica(Caprifoliaceae), has a variety of activities, whereas its pharmacodynamic material basis is not completely clear and there are few reports on its quality control and evaluation. In this study, an UPLC-Q-TOF-MS method was used to analyze the nucleosides and nucleobases in P. ribis and a HPLC method was established for simultaneous determination of 10 nucleosides and nucleobases. MS and MS/MS data were acquired in positive ion mode. Based on the data comparison of the sample and the reference substance, the literature data and the compound databases of ChemSpider and PubChem, 18 nucleosides and nucleobases were identified qualitatively from the water extract of P. ribis for the first time. After optimization, the HPLC was performed using a Welch Ultimate AQ C_(18) column(4.6 mm×250 mm, 5 µm) by gradient elution with acetonitrile and water as mobile phase, the flow rate of 1.0 mL·min~(-1), the detection wavelength of 260 nm, and the column temperature of 30 ℃. Through the investigation of the extraction method, solvent and time, it was determined that the test solution should be obtained by cold water extraction for 18 h. At the present HPLC conditions, 10 components of uracil, cytidine, hypoxanthine, uridine, thymine, inosine, guanosine, 2'-deoxyinosine, 2'-deoxyguanosine and thymidine could be well separated(R > 1.5) and showed good linearity(r > 0.999 9) in the concentration ranges of 0.247-24.7, 0.283-28.3, 0.273-27.3, 0.256-25.6, 0.257-25.7, 0.318-31.8, 0.245-24.5, 0.267-26.7, 0.250-25.0 and 0.267-26.7 mg·L~(-1), respectively. The average reco-veries of 10 components were 95.78%-104.5%, and the RSDs were 2.2%-5.2%(n=6). The contents of 10 nucleosides and nucleobases in different samples of P. ribis varied greatly, which were 0.021-0.122, 0.004-0.029, 0.014-0.226, 0.009-0.442, 0.003-0.014, 0.002-0.146, 0.007-0.098, 0-0.054, 0.005-0.069, 0.004-0.081 and 0.072-1.28 mg·g~(-1) for uracil, cytidine, hypoxanthine, uridine, thymine, inosine, guanosine, 2'-deoxyinosine, 2'-deoxyguanosine, thymidine and total 10 components, respectively. These results demonstrated that the components had significant differences in the internal quality, and good quality control was needed to ensure the medical efficacy. This study provides a scientific basis for the discovery of pharmacodynamic ingredients, quality control and evaluation of P. ribis.


Assuntos
Nucleosídeos , Espectrometria de Massas em Tandem , Basidiomycota , Cromatografia Líquida de Alta Pressão , Guanosina
10.
Zhongguo Zhong Yao Za Zhi ; 46(12): 2889-2899, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34467710

RESUMO

Sophorae Flavescentis Radix,derived from the root of Sophora flavescens in the Leguminosae family,has been widely used in the medicine,agriculture,animal husbandry,and daily chemical industry. A pharmacophore model-based method for rapid discovery of tyrosinase inhibitors( TIs) from S. flavescens was established by molecular docking under Lipinski rules,and verified by enzyme assays. Briefly,the chemical constituent database of S. flavescens( CDSF) was established based on the previous papers. Theoptimal pharmacophore model( OPM) was constructed by DS 2019 on the basis of known active TIs. Eighty-three hits predominated by flavonoids having higher fitting scores with OPM than the positive control were screened out,and subjected to molecular docking based on the three-dimensional structure of tyrosinase crystal protein. The potential TIs such as kurarinone and nor-kurarinone were rapidly discovered from the compounds with higher docking scores than the positive control under the Lipinski rules. The results were verified by the in vitro enzyme assays. The inhibition activities of tyrosinase from non-medicinal parts of S. flavescens were also tested to explore the relationship between the inhibition activity and chemical compositions. This study is expected to provide data support for the comprehensive application and development of S. flavescens and also a new method for the rapid discovery of active substances or functional constituents in the complex systems.


Assuntos
Sophora , Animais , Flavonoides , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Extratos Vegetais/farmacologia , Raízes de Plantas
11.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4034-4039, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467712

RESUMO

As anti-aging ingredients, ß-nicotinamide mononucleotide(NMN) and nicotinamide adenine dinucleotide(NAD~+) have attracted worldwide attention in recent years. After oral administration, NMN can be converted into NAD~+ in vivo and the latter is the actual ingredient which exerts anti-aging effect. In order to explore the "rejuvenating and anti-aging" effect of Dendrobium officinale, which was firstly recorded in Shennong's Herbal Classic of Materia Medica, this study established the quantitative method of UPLC-MS/MS for simultaneous determination of NMN and NAD~+ in D. officinale and the congeneric species for the first time, and 34 batches of samples were detected. UPLC conditions are as follows: ACQUITY UPLC HSS T3 column(2.1 mm × 100 mm, 1.8 µm), gradient elution with acetonitrile-0.1% formic acid in water at the flow rate of 0.3 mL·min~(-1), and column temperature of 40 ℃. MS conditions were scanned electrospray ionization source and multiple reaction monitoring mode. The method was verified by systematic methodology. The mean recoveries of NMN and NAD~+ were 77.58% and 80.70%, respectively, with RSD of 3.6% and 4.3%, separately. All results showed that the content of NMN was higher in D. officinale than in the other congeneric species. Particularly, the content in fresh D. officinale stems was as high as 0.931 9 µg·g~(-1). NAD~+ was only found in D. officinale and the content was three times higher than that of NMN. This may be the reason that D. officinale topped the "nine famous anti-aging herbs". In addition, processing method influences the content of NMN and NAD~+ in Dendrobium. Specifically, the content of NMN and NAD~+ was in the order of fresh Dendrobium stems > dried Dendrobium stem segments > spiral or spring-like dried Dendrobium stems.


Assuntos
Dendrobium , Mononucleotídeo de Nicotinamida , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , NAD , Espectrometria de Massas em Tandem
12.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4040-4050, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467713

RESUMO

In recent years, the establishment of the commercial grade of Yinpian [traditional Chinese medicine(TCM) pieces for decoction] in the TCM industry has been hotly disputed. In this article, Sophorae Flavescentis Radix(SFR) was selected as a representative example to investigated. Through systematic comparison and analysis, the different grades of SFR slices were traced, verified and evaluated. According to the current published local grade standards of SFR slices, the results showed that the first-class of SFR slices were mostly derived from the wild medicinal materials, the second-class were mostly originated from the cultivated materials in 3-4 years, and the third-class products were from a small number of lateral roots and short-growing years or harsh habitat of wild medicinal materials. On the basis of identifying the sources of different grades of SFR slices, the contents of the active components, including matrine, oxymatrine, oxysophocarpine, sophoridine, N-methyl-cytisine, sophocarpine, were quantitatively determined in typical samples, it was found that the grades were inversely proportional to the contents of active ingredients. In order to ensure the universality of the conclusion, the contents of different grades of commercial SFR slices were determined, and the conclusion was verified as "the commercial grades of SFR slices were inversely linked to their contents of active ingredients". This phenomenon is common in the determination of the commercial grade of Yinpian of radix and rhizome. Therefore, we propose that the method or standard of the commercial grade of Yinpian of radix and rhizome based on the size of Yinpian maybe not proper. Whether and how to classify Yinpian commercial grade is not only a multi-disciplinary issue, especially in combination with clinical efficacy, but also a big problem need to consider the production, commercial circulation and other processes link of quality risk and quality assurance, and should be treated with great caution.


Assuntos
Medicamentos de Ervas Chinesas , Sophora , Medicina Tradicional Chinesa , Raízes de Plantas , Rizoma
13.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4051-4060, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467714

RESUMO

This research established the HPLC methods for the determination of perillaketone, perillaldehyde, caffeic acid, scutellarin, and rosmarinic acid in 33 batches of Perillae Folium. Kromasil C_(18)(4.6 × 250 mm, 5 µm) chromatographic column was used, and the mobile phase for determination of the perillaketone and perillaldehyde was methanol-water(55∶45) solution, at a flow rate of 1.0 mL·min~(-1), with the column temperature at 30 ℃. The mobile phase for the determination of caffeic acid, scutellarin and rosmarinic acid was methanol(A)-0.2% phosphoric acid aqueous solution(B) with gradient elution(0-20 min, 25%-30% A; 20-60 min, 30%-43% A). The flow rate was 1.0 mL·min~(-1) and the column temperature was set at 30 ℃. The results showed that the established method can achieve good separation of the five components in samples, with a good linear relationship and high accuracy, indicating that the methods can be used for the determination of Perillae Folium. The results showed that all samples contained five components. And the content of rosmarinic acid(0.04%-1.57%) > scutellarin(0.03%-0.77%) > perillaldehyde(0.02%-0.66%) > perillaketone(0.03%-0.30%) > caffeic acid(0.006%-0.07%). Thirty-three Batches of Perillae Folium can be grouped into 5 categories. There are certain content rules and region specificities under different clusters. Perillaketone, perillaldehyde, and rosmarinic acid can be used as the main markers to evaluate the quality of Perillae Folium.


Assuntos
Medicamentos de Ervas Chinesas , Folhas de Planta , Cromatografia Líquida de Alta Pressão , Extratos Vegetais
14.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4117-4123, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467722

RESUMO

This study aims to explore the relationship of DNA methylation with the contents of the index components as well as the growth and development of Pogostemon cablin. The demethylation reagent 5-azacytidine(5-azaC) was used to treat the tissue culture seedlings of patchouliol-type P. cablin. High performance liquid chromatography was employed to evaluate the changes of DNA methy-lation in P. cablin, and GC-MS to detect the contents of index components in P.cablin. The agronomic characters of P.cablin were measured using the common methods. The results showcased that DNA methylation of P.cablin was significantly reduced by 5-azaC in a concentration-dependent manner. Thirty days after treatment with 5-azaC at different concentrations, the content of patchouli alcohol changed slightly; compared with that in the control group, the content of pogostone in 50 µmol·L~(-1) and 100 µmol·L~(-1) 5-azaC groups was significantly up-regulated. The 100 µmol·L~(-1) 5-azaC group had the largest differences in contents of pogostone and patchouli alcohol compared with the control group, followed by the 50 µmol·L~(-1) 5-azaC group. Ninety days after disinhibition, the content of pogostone in the treatment group was significantly increased and the content of patchouli alcohol was significantly decreased. In addition, 5-azaC significantly inhibited the growth and development of P.cablin in a dose-dependent manner. These results indicate that DNA methylation regulates the biosynthesis of the index components in patchouliol-type P.cablin and proper demethylation can directly promote the synthesis of pogostone and indirectly affect the accumulation of patchouli alcohol.


Assuntos
Pogostemon , Azacitidina , Metilação de DNA , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis , Pogostemon/genética
15.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4230-4237, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467737

RESUMO

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


Assuntos
Medicamentos de Ervas Chinesas , Dispepsia , Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Dispepsia/tratamento farmacológico , Humanos , Hiperplasia/tratamento farmacológico , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular
16.
Adv Mater ; : e2104867, 2021 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-34477263

RESUMO

While metal-halide perovskite light-emitting diodes (PeLEDs) hold the potential for a new generation of display and lighting technology, their slow operation speed and response time limit their application scope. Here, high-speed PeLEDs driven by nanosecond electrical pulses with a rise time of 1.2 ns are reported with a maximum radiance of approximately 480 kW sr-1  m-2 at 8.3 kA cm-2 , and an external quantum efficiency (EQE) of 1% at approximately 10 kA cm-2 , through improved device configuration designs and material considerations. Enabled by the fast operation of PeLEDs, the temporal response provides access to transient charge carrier dynamics under electrical excitation, revealing several new electroluminescence quenching pathways. Finally, integrated distributed feedback (DFB) gratings are explored, which facilitate more directional light emission with a maximum radiance of approximately 1200 kW sr-1  m-2 at 8.5 kA cm-2 , a more than two-fold enhancement to forward radiation output.

17.
Zhongguo Zhong Yao Za Zhi ; 46(15): 3877-3885, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34472263

RESUMO

Twenty-six compounds, including sixteen meroterpenoids(1-16), a triterpenoid(17), four terpenoid derivatives(18-21), and five aromatic compounds(22-26), were isolated from the leaves of Psidium guajava. Their structures were identified by spectroscopic analyses including NMR and MS. Compounds 21-26 were obtained from plants of Psidium for the first time. Based on the structure,(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24 a), an α-glucosidase inhibitor recently isolated from Paramignya trimera, should be revised as compound 24. Meroterpenoids 1-16 were evaluated for their antitumor and antifungal activities. Meroterpenoids psiguajadial D(4), guapsidial A(5), 4,5-diepipsidial A(7), guadial A(14), and guadial B(15) showed cytotoxicities against five human tumor cell lines(HL-60, A-549, SMMC-7721, MCF-7, and SW-480), among which 5 was the most effective with an IC_(50) of 3.21-9.94 µmol·L~(-1).


Assuntos
Psidium , Antifúngicos/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Extratos Vegetais , Folhas de Planta , Terpenos
18.
Zhen Ci Yan Jiu ; 46(8): 684-9, 2021 Aug 25.
Artigo em Chinês | MEDLINE | ID: mdl-34472754

RESUMO

OBJECTIVE: To observe the effect of transcutaneous electric acupoints stimulation (TEAS) on vascular endothelial function and inflammatory factors after percutaneous coronary intervention (PCI) in patients. METHODS: A total of 94 patients with coronary heart disease and undergoing PCI were randomized into a TEAS group and a sham-TEAS group, 47 cases in each one. In the TEAS group, TEAS started at unilateral Neiguan (PC6) and Ximen (PC4) 30 min before PCI till the end of PCI. In the sham-TEAS group, the procedure and persistent time were same as the TEAS group, but no electric stimulation was performed. Before treatment and at 8 h and 24 h after PCI, the levels of serum endothelin-1 (ET-1), von Willebrand factor (vWF), nitric oxide (NO), blood flow dependent diastolic function (FMD), interleukin-6 (IL-6), inteleukin-10 (IL-10), matrix metalloproteinase-9 (MMP-9) and high-sensitivity C-reactive protein (hs-CRP) were detected in the patients successively. RESULTS: Compared with the levels before PCI, the levels of ET-1 and vWF were all increased at 8 h and 24 h after PCI in the two groups (P<0.05) and the levels in the TEAS group were remarkably lower than those in the sham-TEAS group (P<0.05). Compared with the levels before PCI, the levels of NO and FMD at 8 h and 24 h after PCI were all reduced in the two groups (P<0.05) and the levels in the TEAS group were higher obviously than those in the sham-TEAS group (P<0.05). Compared with the levels before PCI, the levels of hs-CRP, MMP-9, IL-6 and IL-10 were all increased at 8 h and 24 h after PCI in the two groups (P<0.05); Compared with the sham-TEAS group, the levels of hs-CRP, MMP-9 and IL-6 were reduced and the level of IL-10 was increased at 8 h and 24 h after PCI in the TEAS group (P<0.05). CONCLUSION: TEAS effectively improves the vascular endothelial function and reduces serum inflammatory factors after PCI.


Assuntos
Doença das Coronárias , Intervenção Coronária Percutânea , Estimulação Elétrica Nervosa Transcutânea , Pontos de Acupuntura , Proteína C-Reativa , Doença das Coronárias/terapia , Humanos , Intervenção Coronária Percutânea/efeitos adversos
19.
J Emerg Med ; 2021 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-34479750

RESUMO

BACKGROUND: Angioedema, a localized swelling of subcutaneous and submucosal tissues, may involve the upper airway. A subset of patients presenting for emergent evaluation of angioedema will require intubation. Little is known about airway management practices in patients with angioedema requiring intubation in the emergency department (ED). OBJECTIVE: To describe airway management practices in patients intubated for angioedema in the ED. METHODS: We analyzed data from the National Emergency Airway Registry. All patients with an intubation attempt for angioedema between January 1, 2016 and December 31, 2018 were included. We report univariate descriptive data as proportions with cluster-adjusted 95% confidence intervals. RESULTS: Of 19,071 patient encounters, intubation was performed for angioedema in 98 (0.5%). First-attempt success was achieved in 81%, with emergency physicians performing the procedure in 94% of encounters. The most common device used was a flexible endoscope (49%), and 42% of attempts were via a nasal route. Pharmacologic methods included sedation with paralysis (61%), topical anesthesia with or without sedation (13% and 13%, respectively), and sedation only (10%). Among 19 (19%) patients requiring additional attempts, intubation was achieved on second attempt in 10 (53%). The most common adverse events were hypotension (13%) and hypoxemia (12%). Cricothyrotomy occurred in 2 patients (2%). No deaths were observed. CONCLUSIONS: Angioedema was a rare indication for intubation in the ED setting. Emergency physicians achieved first-attempt success in 81% of encounters and used a broad range of intubation devices and methods, including flexible endoscopic techniques. Cricothyrotomy was rare, and no ED deaths were reported. © 2021 Elsevier Inc.

20.
Environ Microbiol ; 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34472190

RESUMO

Magnaporthe oryzae is an important plant pathogen that causes rice blast. Hse1 and Vps27 are components of ESCRT-0 involved in the multivesicular body (MVB) sorting pathway and biogenesis. To date, the biological functions of ESCRT-0 in M. oryzae have not been determined. In this study, we identified and characterized Hse1 and Vps27 in M. oryzae. Disruption of MoHse1 and MoVps27 caused pleiotropic defects in growth, conidiation, sexual development and pathogenicity, thereby resulting in loss of virulence in rice and barley leaves. Disruption of MoHse1 and MoVps27 triggered increased lipidation of MoAtg8 and degradation of GFP-MoAtg8, indicating that ESCRT-0 is involved in the regulation of autophagy. ESCRT-0 was determined to interact with coat protein complex II (COPII), a regulator functioning in homeostasis of the endoplasmic reticulum (ER homeostasis), and disruption of MoHse1 and MoVps27 also blocked activation of the unfolded protein response (UPR) and autophagy of the endoplasmic reticulum (ER-phagy). Overall, our results indicate that ESCRT-0 plays critical roles in regulating fungal development, virulence, autophagy and ER-phagy in M. oryzae.

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