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1.
Chin J Integr Med ; 2020 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-33000415

RESUMO

OBJECTIVE: To observe the effects and safety of Tongyan Spray () on the range and time of hyoid motion in patients with ischemic post-stroke dysphagia. METHODS: Seventy-two patients with ischemic post-stroke dysphagia were selected and randomly assigned to a treatment group (36 cases) and a control group (36 cases) by a random number table from January 2013 to October 2014. All patients swallowed 4 kinds of barium meals with different traits respectively, and each patient underwent video fluoroscopy (VF) examination twice. In the treatment group, Tongyan Spray was sprayed to the pharynx on both sides and the middle part once respectively. The spray was applied 30 min before the second examination. Purified water at room temperature was used as placebo in the control group. The changes in the range and time of hyoid motion in both groups were observed before and after treatment. RESULTS: Six patients dropped out in each group, and 60 patients completed the study and were included in the final analysis. Significant improvement was observed in the range of superior hyoid excursion distance and the time of hyoid motion in the treatment group compared with the control group (P<0.05). There were no obvious adverse reactions observed in oral mucosa in both groups during the whole study. CONCLUSION: Tongyan Spray was an effective and safe medicine for improving swallowing function in patients with ischemic post-stroke dysphagia.

2.
Int J Mol Med ; 46(5): 1938, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33000183

RESUMO

Following the publication of this article, the authors have realized that grant number published in the 'Funding' section of their paper was written incorrectly: The grant number for the support the authors received from the Health Commission of Hubei Province Scientific Research Project should have been written as 'WJ2019F038' instead of 'WJ2009F038'. The authors apologize to the funders of their research project, and to the readership of the Journal for any inconvenience caused. [the original article was published in International Journal of Molecular Medicine 46: 849­858, 2020; DOI: 10.3892/ijmm.2020.4623].

3.
Theranostics ; 10(24): 11178-11196, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33042277

RESUMO

Selective modulation of metabotropic glutamate receptor 2 (mGlu2) represents a novel therapeutic approach for treating brain disorders, including schizophrenia, depression, Parkinson's disease (PD), Alzheimer's disease (AD), drug abuse and addiction. Imaging mGlu2 using positron emission tomography (PET) would allow for in vivo quantification under physiological and pathological conditions and facilitate drug discovery by enabling target engagement studies. In this paper, we aimed to develop a novel specific radioligand derived from negative allosteric modulators (NAMs) for PET imaging of mGlu2. Methods. A focused small molecule library of mGlu2 NAMs with tetrahydro naphthyridine scaffold was synthesized for pharmacology and physicochemical evaluation. GIRK dose-response assays and CNS panel binding selectivity assays were performed to study the affinity and selectivity of mGlu2 NAMs, among which compounds 14a and 14b were selected as PET ligand candidates. Autoradiography in SD rat brain sections was used to confirm the in vitro binding specificity and selectivity of [11C]14a and [11C]14b towards mGlu2. In vivo binding specificity was then studied by PET imaging. Whole body biodistribution study and radiometabolite analysis were conducted to demonstrate the pharmacokinetic properties of [11C]14b as most promising PET mGlu2 PET ligand. Results. mGlu2 NAMs 14a-14g were synthesized in 14%-20% yields in five steps. NAMs 14a and 14b were selected to be the most promising ligands due to their high affinity in GIRK dose-response assays. [11C]14a and [11C]14b displayed similar heterogeneous distribution by autoradiography, consistent with mGlu2 expression in the brain. While PET imaging study showed good brain permeability for both tracers, compound [11C]14b demonstrated superior binding specificity compared to [11C]14a. Further radiometabolite analysis of [11C]14b showed excellent stability in the brain. Conclusions. Compound 14b exhibited high affinity and excellent subtype selectivity, which was then evaluated by in vitro autoradiography and in vivo PET imaging study after labeling with carbon-11. Ligand [11C]14b, which we named [11C]MG2-1904, demonstrated high brain uptake and excellent in vitro/in vivo specific binding towards mGlu2 with high metabolic stability in the brain. As proof-of-concept, our preliminary work demonstrated a successful example of visualizing mGlu2 in vivo derived from NAMs, which represents a promising chemotype for further development and optimization aimed for clinical translation.

4.
Artigo em Inglês | MEDLINE | ID: mdl-33047298

RESUMO

INTRODUCTION: Patients with atopic dermatitis (AD) have a greater risk of conjunctivitis and other ocular surface disorders than the general population. We evaluated the burden of ocular surface disorders and related symptoms prior to treatment initiation in adults with moderate-to-severe AD. METHODS: Patients were enrolled in a randomized, placebo-controlled, double-blinded, phase 3 trial of dupilumab administered with concomitant topical corticosteroids. At the beginning of the screening period, all enrolled patients completed a survey of ocular disorder diagnoses received in the past year; at baseline, patients completed a survey of frequency and severity of ocular symptoms (discomfort, itching, redness, and tearing) experienced in the past month. RESULTS: A total of 712 of 740 patients enrolled in the trial provided responses to the survey. At screening, 286 of 740 patients (38.6%) reported having at least one ocular disorder in the past year. At baseline, 499 of 712 respondents (70.1%) reported having at least one symptom within the past month. Of these patients, 4.4%, 6.0%, 5.5%, and 4.4%, respectively, reported having discomfort, itching, redness, and tearing all of the time. Mild discomfort, itching, redness, and tearing were reported by 26.1%, 33.7%, 30.8%, and 31.6% of patients, respectively, while 7.3%, 7.7%, 6.2%, and 4.2%, reported severe discomfort, itching, redness, and tearing, respectively. CONCLUSIONS: These data demonstrate a high burden of ocular surface disorders and related symptoms in a population of adults with moderate-to-severe AD. Dermatologists should be aware of increased incidence of these disorders in AD and query their patients for signs and symptoms of eye disease. CLINICALTRIALS. GOV REGISTRATION NUMBER: NCT02260986.

5.
Zootaxa ; 4808(3): zootaxa.4808.3.3, 2020 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-33055962

RESUMO

Three species of the family Perlodidae are newly reported or confirmed for China, Isoperla asiatica Rauser from Arxan, Inner Mongolia Autonomous Region, Isoperla eximia Zapekina-Dulkeit from Changbai Mountain, Jilin Province, and Mesoperlina capnoptera (McLachlan, 1886) from Xinjiang Uygur Autonomous Region. Based on new material, additional taxonomic notes and images of another perlodid stonefly, Rauserodes epiproctalis (Zwick, 1997) is provided.

6.
J Inorg Biochem ; 213: 111260, 2020 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-33039746

RESUMO

Two copper complexes, Cu1 (CuL1Cl2, L1 = 2-(6,7-dimethoxyisoquinolin-1-yl) aniline) and Cu2 (CuL2Cl2, L2 = 2-(6-methoxyisoquinolin-1-yl) aniline), were synthesized and characterized. These complexes exhibited high cytotoxic activity toward different cancer cell lines, including the A549 lung cancer cell line, and low cytotoxicity toward normal human cells. Mechanistic studies have shown that these complexes induce bimodal death of cancer cells through apoptosis and autophagy, including the activation of apoptotic and autophagic cell signaling pathways. In addition, Cu1 and Cu2 interacted with calf thymus DNA (ct-DNA) via an intercalative binding mode. The different biological behaviors of these copper complexes could be attributed to the presence of electron-donating methoxy groups on the ligands. Cu1 and Cu2 effectively inhibited tumor growth in a xenografted mouse model bearing A549 cells but exhibited lower in vivo toxicity than cisplatin. Thus, Cu1 and Cu2 can be developed as potential anticancer agents.

7.
Nat Commun ; 11(1): 5211, 2020 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-33060583

RESUMO

Chromatin-associated RNA (caRNA) has been proposed as a type of epigenomic modifier. Here, we test whether environmental stress can induce cellular dysfunction through modulating RNA-chromatin interactions. We induce endothelial cell (EC) dysfunction with high glucose and TNFα (H + T), that mimic the common stress in diabetes mellitus. We characterize the H + T-induced changes in gene expression by single cell (sc)RNA-seq, DNA interactions by Hi-C, and RNA-chromatin interactions by iMARGI. H + T induce inter-chromosomal RNA-chromatin interactions, particularly among the super enhancers. To test the causal relationship between H + T-induced RNA-chromatin interactions and the expression of EC dysfunction-related genes, we suppress the LINC00607 RNA. This suppression attenuates the expression of SERPINE1, a critical pro-inflammatory and pro-fibrotic gene. Furthermore, the changes of the co-expression gene network between diabetic and healthy donor-derived ECs corroborate the H + T-induced RNA-chromatin interactions. Taken together, caRNA-mediated dysregulation of gene expression modulates EC dysfunction, a crucial mechanism underlying numerous diseases.

8.
J Inorg Biochem ; 212: 111208, 2020 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-33065383

RESUMO

Two new copper(II) complexes, 9-PMAH-Cu (1) and 9-FPMAH-Cu (2), of anthrahydrazone were synthesized and structurally characterized, in which 9-FPMAH (9-(4'-trifluoromethyl)-pyrimidine anthrahydrazone) is the 4'-CF3 derivative of 9-PMAH (9-pyrimidine anthrahydrazone). Both complexes 1 and 2 showed similar intercalative binding modes towards DNA and might compete with the typical DNA intercalator, GelRed, in the same binding site. They could also act as topoisomerase (type I) suppressor to effectively inhibit its activity, in which complex 1 was more effective than 2. The in vitro antitumor screening indicated that complex 1 displayed much higher antiproliferative ability than 2 and cisplatin towards all the tested tumor cell lines. On the other hand, complex 1 also showed high cytotoxicity against human normal liver cell line HL-7702, suggesting it is a potential high cytotoxic antitumor candidate. While it was also suggested that the loss of activity of complex 2 might be due to the presence of 4'-CF3 on the pyrimidine ring. Studies on the cellular level showed that complex 1 could arrest the cell cycle of the most sensitive T-24 cells at G2/M phase and induced cell apoptosis. Complex 1 further showed a significant suppression on the tumor growth on the T-24 tumor xenograft mouse model, but not reduced the body weight. Especially, complex 1 could retain its coordination state in H2O even in the presence of HSA. The results suggests that complex 1 is of enough safety to be considered as a promising anticancer candidate by combining the bioactive Cu(II) and the anthrahydrazone pharmacophore.

9.
Metabolomics ; 16(11): 115, 2020 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-33067714

RESUMO

INTRODUCTION: Diabetes mellitus is a serious metabolic disorder causing multiple organ damage in human. However, the lipidomic profiles in different organs and their associations are rarely studied in either diabetic patients or animals. OBJECTIVES: To evaluate and compare the characteristics of lipid species in serum and multiple tissues in a diabetic mouse model. METHODS: Semi-quantitative profiling analyses of intact and oxidized lipids were performed in serum and multiple tissues from a diabetic mouse model fed a high fat diet and treated with streptozotocin by using LC/HRMS and MS/MS. The total content of each lipid class, and the tissue-specific lipid species in all tissue samples were determined and compared by multivariate analyses. RESULTS: The diabetic mouse model displayed characteristic differences in serum and multiple organs: the brain and heart showed the largest reduction in cardiolipin, while the kidney had more alterations in triacylglycerol. Interestingly, the lipidomic differences also existed between different regions of the same organ: cardiolipin species with highly polyunsaturated fatty acyls decreased only in atrium but not in ventricle, while renal cortex showed longer fatty acyl chains for both increased and decreased triacylglycerol species than renal medulla. Importantly, diabetes caused an accumulation of lipid hydroperoxides, suggesting that oxidative stress was induced in all organs except for the brain during the development of diabetes. CONCLUSIONS: These findings provided novel insight into the organ-specific relationship between diabetes and lipid metabolism, which might be useful for evaluating not only diabetic tissue injury but also the effectiveness of diabetic treatments.

10.
Mol Cell Neurosci ; 108: 103552, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32918999

RESUMO

Quiescent stem cells have been found in multiple adult organs, and activation of these stem cells is critical to the restoration of damaged tissues in response to injury or stress. Existing evidence suggests that extrinsic cues from the extracellular matrix or supporting cells of various stem cell niches may interact with intrinsic components to initiate stem cell differentiation, but the molecular and cellular mechanisms regulating their activation are not fully understood. In the present study, we find that olfactory horizontal basal cells (HBCs) are stimulated by neural glial-related cell adhesion molecules (NrCAMs). NrCAM activation requires matrix metalloproteases (MMPs) and epidermal growth factor receptors (EGFRs). Inhibiting MMP activity or EGFR activation not only blocks HBC proliferation in the cultured olfactory organoids, but also severely suppresses HBC proliferation in the olfactory epithelium following methimazole-induced injury, resulting in a delay of olfactory mucosa reconstitution and functional recovery of the injured mice. Both NrCAMs and EGFR are expressed by the HBCs and their expression increases upon injury. Our data indicate that MMP-mediated cleavage of NrCAMs serves as an autocrine or paracrine signal that activates EGFRs on HBCs to trigger HBC proliferation and differentiation to reconstruct the entire olfactory epithelium following injury.

11.
Small ; : e2003724, 2020 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-32985107

RESUMO

Potassium ion hybrid capacitors (PIHCs) are of particular interest benefiting from high energy/power densities. However, challenges lie in the kinetic mismatch between battery-type anode and capacitive-type cathode, as well as the difficulty in achieving optimized charge/mass balance. These significantly sacrifice the electrochemical performance of PIHCs. Here, strategies including charge/mass balance pursuance, electrolyte optimization, and tailored electrode design, are employed, together, to address these challenges. The key parameters determining the energy storage properties of PIHCs are identified. Specifically, i) the good kinetic match between anode and cathode translates into the very small variation of cathode/anode mass ratio at various rates. This sets general rules for the pursuance of charge balance, and to maximize the electrochemical performance of hybrid devices. ii) A potassium bis(fluoroslufonyl)imide (KFSI)-based electrolyte promotes better electrode kinetics and allows for the formation of more stable and intact solid electrolyte interphase layer, with respect to potassium hexafluorophosphate (KPF6 )-based electrolyte. And iii) hierarchically porous N/O codoped carbon nanosheets (NOCSs) with enlarged interlayer spacing, disordered structure, and abundant pyridinic-N functional groups are advantageous in terms of high electronic/ionic transport dynamics and structural stability. All these together, contribute to the high energy/power density of the activated carbon//NOCSs PIHCs (113.4 Wh kg-1 , at 17,000 W Kg-1 ).

12.
Artigo em Inglês | MEDLINE | ID: mdl-32985128

RESUMO

OBJECTIVE: This study examined the extent to which maternal immune activity during pregnancy is associated with childhood adiposity, and if so, whether associations at birth differ from those in infancy and childhood. Sex-specific associations were also examined. METHODS: Participants were 1,366 singleton pregnancies from the Collaborative Perinatal Project (1959-1966). Interleukin-1ß (IL-1ß), IL-6, TNF-α, IL-8, and IL-10 in maternal sera were assayed repeatedly during pregnancy. Children's BMI was calculated repeatedly from birth through age 8 and derived age- and sex-normalized BMI z scores (BMIz). Linear mixed models were used to estimate the cumulative concentration of each cytokine in the second and third trimesters and then related this concentration to child BMIz. RESULTS: Children exposed to higher IL-1ß, IL-6, IL-8, and IL-10 concentrations had lower BMIz at birth but higher BMIz during childhood. Higher concentrations of IL-8 and IL-1ß were also associated with higher BMIz during infancy (B per log increase in IL-8 = 0.04; 95% CI: 0.02 to 0.07; B per log increase in IL-1ß = 0.03; 95% CI: 0.001 to 0.06). The associations between TNF-α and BMIz were in opposing directions in boys (B = -0.13; 95% CI: -0.31 to 0.04) and girls (B = 0.14; 95% CI: 0.02 to 0.26) during childhood. CONCLUSIONS: Maternal prenatal inflammation contributes to the age- and sex-specific programming of obesity risk in childhood.

13.
Artigo em Inglês | MEDLINE | ID: mdl-32900435

RESUMO

Peiai 64S (PA64S) is a photoperiod- and thermo sensitive genic male sterile (PTGMS) rice line that has been widely applied in two-line hybrid rice breeding. The male fertility mechanism of PTGMS has always been the research focus. We obtained fertile PA64S (F) and sterile fertile PA64S (S) plants at 21℃ and 28℃, respectively. Here, we analyzed the development of anthers and pollen grains of PA64S (S) and found that the degradation of tapetum and sporopollenin accumulation of pollen exine was abnormal. The content of lipid components in PA64S (F) and PA64S (S) were different by LC-MS, among which sterols, (O-acyl) ω-hydroxy fatty acids, ceramide, and other lipid components were upregulated in PA64S (F). The results of transcriptome showed that many significantly different genes were enriched in the lipid metabolism pathways. Additionally, lipid synthesis and transport genes were downregulated in PA64S (S). In summary, the differences of the PA64S fertility under different temperatures were analyzed through multi-levels comparison. These results suggest that lipid synthesis and transport during PA64S anther development affects the lipid accumulation of pollen exine, and ultimately affected fertility. The differences in lipids content may also be a factor affecting PA64S pollen fertility.

14.
Cancer Control ; 27(1): 1073274820960467, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32938231

RESUMO

Patients with lung cancer are presumed to be at high risk from COVID-19 infection due to underlying malignancy. A total of 31 COVID-19 patients with pre-diagnosed lung cancer and 186 age and sex matched COVID-19 patients without cancer in 6 hospitals in Wuhan, China were identified in our study. There was a significantly higher level of IL-6 in lung cancer group showed by multifactorial analysis. The restricted mean survival time in 10, 20, and 53 days in COVID-19 patients with lung cancer were ealier than non-cancer COVID-19 patients in the same observation time (all P values < 0.05). Our results indicated that pre-diagnosed lung cancer was associated with higher morbidity and mortality in COVID-19 patients.


Assuntos
Betacoronavirus , Infecções por Coronavirus/epidemiologia , Neoplasias Pulmonares/complicações , Pandemias , Pneumonia Viral/epidemiologia , China/epidemiologia , Infecções por Coronavirus/complicações , Feminino , Hospitalização/tendências , Humanos , Neoplasias Pulmonares/epidemiologia , Masculino , Pessoa de Meia-Idade , Pneumonia Viral/complicações , Estudos Retrospectivos , Fatores de Risco , Taxa de Sobrevida/tendências
15.
Int J Mol Med ; 46(5): 1816-1826, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32901853

RESUMO

The aim of the present study was to identify natural compounds that bear significant anti­tumor activity. Thus, the effects of 63 small molecules that were isolated from traditional Chinese medicinal herbs on A549 human non­small cell lung cancer (NSCLC) and MCF­7 breast cancer cells were examined. It was found that ursolic acid (UA), a natural pentacyclic triterpenoid, exerted significant inhibitory effect on these cells. Further experiments revealed that UA inhibited the proliferation of various lung cancer cells, including the NSCLC cells, H460, H1975, A549, H1299 and H520, the human small cell lung cancer (SCLC) cells, H82 and H446, and murine Lewis lung carcinoma (LLC) cells. UA induced the apoptosis and autophagy of NSCLC cells. The inhibition of the mammalian target of rapamycin (mTOR) signaling pathway, but not the activation of the extracellular signal­regulated kinase 1/2 (ERK1/2) signaling pathway contributed to the UA­induced autophagy of NSCLC cells. Moreover, the inhibition of autophagy by chloroquine (CQ) or siRNA for autophagy­related gene 5 (ATG5) enhanced the UA­induced inhibition of cell proliferation and promotion of apoptosis, indicating that UA­induced autophagy is a pro­survival mechanism in NSCLC cells. On the whole, these findings suggest that combination treatment with autophagy inhibitors may be a novel strategy with which enhance the antitumor activity of UA in lung cancer.

16.
Sensors (Basel) ; 20(17)2020 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-32867293

RESUMO

Accurately sensing the surrounding 3D scene is indispensable for drones or robots to execute path planning and navigation. In this paper, a novel monocular depth estimation method was proposed that primarily utilizes a lighter-weight Convolutional Neural Network (CNN) structure for coarse depth prediction and then refines the coarse depth images by combining surface normal guidance. Specifically, the coarse depth prediction network is designed as pre-trained encoder-decoder architecture for describing the 3D structure. When it comes to surface normal estimation, the deep learning network was designed as a two-stream encoder-decoder structure, which hierarchically merges red-green-blue-depth (RGB-D) images for capturing more accurate geometric boundaries. Relying on fewer network parameters and simpler learning structure, better detailed depth maps are produced than the existing states. Moreover, 3D point cloud maps reconstructed from depth prediction images confirm that our framework can be conveniently adopted as components of a monocular simultaneous localization and mapping (SLAM) paradigm.

17.
Cell Biochem Funct ; 2020 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-32881051

RESUMO

Thyroid cancer is the most common endocrine carcinoma, with papillary thyroid carcinoma (PTC) accounting for 80%-90% of thyroid cancers. Accumulating studies reported that mitochondria plays an important role in the regulation of cell proliferation. ALDH5A1, may function as an oncogene or tumour suppressor in various human cancers, and the role of ALDH5A1 in PTC is still unclear. The aim of this study was to investigate the clinical significance of ALDH5A1 expression and its functions in PTC. In this present study, we studied ALDH5A1 expression on primary papillary thyroid carcinoma (PTC) in The Cancer Genome Atlas (TCGA) database. Results showed that the levels of ALDH5A1 were found positively correlated with tumour stage, metastasis, lymph node stage, and higher levels of ALDH5A1 demonstrated poor disease-free survival (DFS). Immunohistochemistry (IHC) revealed that significantly higher expression of ALDH5A1 was found in PTC tissues. On the other hand, knockdown of ALDH5A1 significantly inhibited PTC cell proliferation, migration and invasion detection found the migration and invasion of cells also were hindered when ALDH5A1 level was reduced. The knockdown of ALDH5A1 inhibited the expression of Vimentin and promoted the expression of E-cadherin. In brief, knockdown of ALDH5A1may act as a novel molecular target for the prevention and treatment of PTC. SIGNIFICANCE OF THE STUDY: The present study focused on the role and the potential mechanism of ALDH5A1 in papillary thyroid carcinoma. We demonstrated that reduced expression of ALDH5A1 might inhibit the progression of TC by inhibiting cell proliferation, migration and invasion and reversing epithelial-mesenchymal transition (EMT). The findings ensured the interaction relation between ALDH5A1 and EMT in PTC, providing a novel biological marker for PTC and enriching the potential strategies for TC treatment.

18.
J Am Chem Soc ; 142(38): 16471-16478, 2020 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-32909749

RESUMO

Here we report the first two-dimensional (2D) supramolecular polymer, which has varying structure and function arising from the perturbation of noncovalent metal···metal interactions in response to acid-base stimuli. This 2D assembly possesses a positively charged, honeycomb-like nanostructure consisting of trinuclear alkynylplatinum(II) terpyridine complexes appended with acid-sensitive dimethylamino groups. Upon addition of acids and bases, reversible switching mediated by protonation and deprotonation of dimethylamino and dimethylammonium moieties intrinsically alters the positive charge density of the constituent cationic units, which causes interior cavities to adaptively adjust their size, accompanied by drastic photoluminescence changes. When water molecules pass through the membranes obtained from 2D supramolecular polymers, the permeating flux can also be tuned by the pH values of the buffer media. This work paves the way toward supramolecularly engineered 2D smart materials with stimuli-responsive properties.

19.
Water Sci Technol ; 82(2): 207-226, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32941164

RESUMO

Biological creatures with unique surface wettability have long served as a source of inspiration for scientists and engineers. More specifically, certain beetle species in the Namib Desert have evolved to collect water from fog on their backs by way of wettability patterns, which attracted an ongoing interest in biomimetic studies. Bioinspired materials exhibiting extreme wetting properties, such as superhydrophilic and superhydrophobic surfaces, have attracted considerable attention because of their potential use in various applications. Combining these two extreme states of superhydrophilicity and superhydrophobicity on the same surface in precise two-dimensional micropatterns opens exciting new functionalities and possibilities for a wide variety of applications. In this review we briefly describe the water-harvesting mechanisms of a genus of Namib Desert beetle, Stenocarpa, consisting of the theory of wetting and transporting. Then we describe the methods for fabricating superhydrophilic-superhydrophobic patterns and highlight some of the newer and emerging applications of these patterned substrates that are currently being explored. Finally, we provide conclusions and outlook concerning the future development of bioinspired surfaces of patterned wettability.


Assuntos
Materiais Biomiméticos , Besouros , Animais , Interações Hidrofóbicas e Hidrofílicas , Propriedades de Superfície , Água
20.
J Med Chem ; 2020 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-32960052

RESUMO

Metabotropic glutamate receptor 2 (mGlu2) is a known target for treating several central nervous system (CNS) disorders. To develop a viable positron emission tomography (PET) ligand for mGlu2, we identified new candidates 5a-i that are potent negative allosteric modulators (NAMs) of mGlu2. Among these candidates, 4-(2-fluoro-4-methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (5i, also named as [11C]MG2-1812) exhibited high potency, high subtype selectivity, and favorable lipophilicity. Compound 5i was labeled with positron-emitting carbon-11 (11C) to obtain [11C]5i in high radiochemical yield and high molar activity by O-[11C]methylation of the phenol precursor 12 with [11C]CH3I. In vitro autoradiography with [11C]5i showed heterogeneous radioactive accumulation in the brain tissue sections, ranked in the order: cortex > striatum > hippocampus > cerebellum ≫ thalamus > pons. PET study of [11C]5i indicated in vivo specific binding of mGlu2 in the rat brain. Based on the [11C]5i scaffold, further optimization for new candidates is underway to identify a more suitable ligand for imaging mGlu2.

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