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Presented herein is a novel synthesis of unsymmetrical 3,3-diaryl oxindoles and 4,4-diaryl isoquinolinediones through the cascade reactions of 2-phenoxy-1H-benzo[d]imidazoles with diazo oxindoles or diazo homophthalimides.

Rh(III)-catalyzed C-H activation of N-phenoxyacetamides and chemodivergent coupling to alkylidenecyclopropanes (ACPs) have been accomplished. With the assistance of the ring strain of ACPs, the coupling can be transannulative or nonannulative, delivering 3-ethylidenedihydrobenzofurans or dienes, respectively, under different reaction conditions, and the selectivity is mainly solvent-controlled. All of the reactions proceeded under mild conditions with a good substrate scope and excellent chemo- and diastereoselectivity.

cis-8-Methoxy-1,3-diazaspiro[4.5]decane-2,4-dione, the key intermediate in the synthesis of spirotetramat, was synthesized by catalytic hydrogenation, oxidation, and Bucherer–Bergs reaction with 4-methoxycyclohexan-1-one as raw material. Spirotetramat was obtained in an overall yield of 20.4% by a multi-step reaction sequence including hydrolysis, esterification, acylation, intramolecular condensation, and O-acylation. The advantages of the proposed method are mild conditions, simple operation, and good to excellent yields in each step.

Bruton's tyrosine kinase (BTK) inhibitors suppressing the aberrant activation of BTK have led to a paradigm shift in the therapy of B-cell malignancies. However, there is an urgent need to discover more selective covalent BTK inhibitors owing to the off-target adverse effects of the approved inhibitor, ibrutinib. Herein, we disclose the discovery and preliminary activity studies of novel BTK inhibitors carrying 1-amino-1

Rh(III)-catalyzed C-H activation of

Background. Kinesio tape (KT) may be useful for the treatment of delayed onset muscle soreness (DOMS), but there has been no systematic review assessing their efficacy. Objectives. We conducted a systematic review and meta-analysis to evaluate the efficacy of KT on DOMS. Methods. We searched seven databases for randomized controlled trials (RCTs) and crossover randomized trials of KT in DOMS, from the earliest date available to December 31, 2019. The primary outcome was muscle soreness. The secondary outcome was muscle strength and serum creatine kinase (CK) level. The risk of bias was evaluated based on the Cochrane criteria. Data were analyzed using RevMan version 5.3.0 software. P values < 0.05 were considered statistically significant. Systematic review registration number is CRD42020157052. Results. Eight trials (six RCTs and two crossover randomized trials) with 289 participants were included. KT use significantly reduced muscle soreness at 48 h (mean difference (MD): -0.67, 95% confidence interval (CI): -1.10 to 0.24, P = 0.002 ) and 72 h postexercise (MD: -0.81, 95% CI: -1.45 to -0.17, P = 0.01 ) but not at 24 h. KT use improved muscle strength at 72 h postexercise (standardized mean difference: 0.35, 95% CI: 0.02 to 0.69, P = 0.04 ) but not at 24 or 48 h. However, the serum CK level at 24, 48, and 72 h postexercise was not better in the KT group relative to the control group. Conclusions. Current evidence suggests that KT might help to alleviate DOMS after strenuous exercise to improve muscle strength. Thus, using KT on the skin for more than 48 hours postexercise, but not for 24 h, appears more effective at relieving pain and improving muscle strength.

Background To investigate the effects of low-intensity exercise on aerobic exercise capacity and autophagy of skeletal muscle in rats after myocardial infarction (MI) and its possible mechanisms. Methods Thirty male Sprague Dawley rats, weighing 180–200 g, were randomly divided into sham, MI, and MI with exercise training (MI + Ex) groups. MI was induced by ligation of the left anterior descending artery. One week after surgery, low-intensity exercise training was carried out on a treadmill 5 days per week for 4 weeks. Results Infarct size of MI and MI + Ex groups was 30.8 ± 5.5% and 27.6 ± 5.0% of left ventricle, respectively (P > 0.05). Heart weight and heart to body weight ratio in the MI group were significantly higher than those in the sham group (P < 0.01), and were lowered by exercise training (P < 0.01). The maximal exercise distance and duration in the MI group were lower than those in the sham group (P < 0.01), but were significantly increased by exercise training (P < 0.05). Autophagosome of the gastrocnemius was not detectable in the sham group, scattered in the MI group but clustered in the MI + Ex group. Microtubule-associated protein light chain 3 (LC3-I/II) and Beclin-1 protein levels in the gastrocnemius were similar between MI and sham groups, but were significantly higher in the MI + Ex group (P < 0.05). Conclusions Low-intensity exercise improves exercise capacity in rats after MI. The effect is associated with enhanced autophagy of the skeletal muscle.

Circular RNAs (circRNAs) act as a key role in mediating carcinogenesis. Nevertheless, the functions and mechanisms of circRNAs in osteosarcoma (OS) are still not fully understood. In the present study, we aim to investigate the functions of circ-XPO1 in OS and its potential mechanism underlying OS progression. CircRNA microarray indicated elevation of circ-XPO1 in OS specimens relative to normal samples. Elevation of circ-XPO1 and XPO1 mRNA was identified in OS tissue specimens and cells by qRT-PCR. In addition, enhanced expression of circ-XPO1 and XPO1 mRNA both correlated with poor prognosis for the patients with OS, as estimated by Kaplan-Meier analysis. Functionally, circ-XPO1 and XPO1 both facilitated the growth and invasion and decreased the apoptosis of OS cells. Moreover, we constructed the circ-XPO1-miRNAs-XPO1 3'-UTR interaction network and verified that circ-XPO1 could sponge miR-23a-3p, miR-23b-3p, miR-23c, and miR-130a-5p to regulate XPO1 expression. Furthermore, rescue assay indicated that the effect of circ-XPO1 on cell progression was partly relying on these miRNAs. Taken together, we found that circ-XPO1 regulated the expression of XPO1 through sponging miRNAs as a competing endogenous (ceRNA), providing the possibility that circ-XPO1 might play as a new therapeutic target for OS.

Background POH1, a member of the JAMM domain containing deubiquitinases, functions in malignant progression of certain types of cancer. However, the role of POH1 in prostate cancer (PCa) remains unclear. Methods We performed RNA interference against the JAMM members in PC3 cells and analyzed cell proliferation. POH1 knockdown was established to evaluate the effects of POH1 on cell growth in vitro and in vivo. RNA-sequencing was utilized to explore the molecular details underlying the biological function of POH1 in PCa. The expression of POH1 in PCa tissues was detected by immunohistochemistry. The POH1 inhibitor capzimin was evaluated to explore whether pharmacologically inhibiting POH1 significantly affected PCa cell proliferation alone or enhanced the inhibitory efficacy of docetaxel and androgen deprivation. Results Functional analyses identified POH1 as a JAMM deubiquitinase that is required for PCa proliferation. Importantly, expression of POH1 was higher in human PCa tissues (PCas) than that in normal prostate tissues, and a positive correlation was detected between elevated POH1 expression and higher pathological grades in PCas. In vivo experiments further demonstrated that depleting POH1 significantly suppressed the growth of PCa cell xenografts. POH1 deficiency profoundly inhibited the expression of a set of genes involving the cell cycle and caused G0/G1 phase arrest. Furthermore, the POH1 inhibitor capzimin phenotypically recapitulated the effects of POH1 knockdown and improved the efficacy of docetaxel and androgen deprivation in PCa cells. Conclusions POH1 was overexpressed in PCas and was correlated with pathological grades in human PCas. Inhibiting POH1 by gene silencing or pharmacological inhibition with capzimin suppressed PCa cell growth. Exploring the inhibition of POH1 in combination with other drugs may provide a strategy to benefit patients with PCa.

Determining the mechanisms underlying the spatial distribution of plant species is one of the central themes in biogeography and ecology. However, we are still far from gaining a full understanding of the autecological processes needed to unravel species distribution patterns. In the current study, by comparing seedling recruitment, seedling morphological performance and biomass allocation of two Haloxylon species, we try to identify the causes of the dune/interdune distribution pattern of these two species. Our results show the soil on the dune had less nu- trients but was less saline than that of the interdune; with prolonged summer drought, soil water availability was lower on the dune than on the interdune. Both species had higher densities of seedlings at every stage of recruit- ment in their native habitat than the adjacent habitat. The contrasting different adaptation to nutrients, salinity and soil water conditions in the seedling recruitment stage strongly determined the distribution patterns of the two spe- cies on the dune/interdune. Haloxylon persicum on the dunes had lower total dry biomass, shoot and root dry bio- mass, but allocated a higher percentage of its biomass to roots and possessed a higher specific root length and specific root area by phenotypic traits specialization than that of Haloxylon ammodendron on the interdune. All of these allowed H. persicum to be more adapted to water stress and nutrient shortage. The differences in morphology and allocation facilitated the ability of these two species to persist in their own environments.

The binding mode and mechanism of dysprosium–naproxen complex (Dy–NAP) with calf thymus deoxyribonucleic acid (ctDNA) were studied using UV–vis and fluorescence spectra in physiological buffer (pH 7.4). The results showed that more than one type of quenching process occurred and the binding mode between Dy–NAP with ctDNA might be intercalation. In addition, ionic strength, iodide quenching and fluorescence polarization experiments corroborated the intercalation binding mode between Dy–NAP and ctDNA. The calculated thermodynamic parameters Δ G , Δ H and Δ S at different temperature demonstrated that hydrophobic interaction force played a major role in the binding process.

Previous studies by our group have indicated that exercise intervention can ameliorate endothelial dysfunction, which is an early pathophysiological change of prediabetes mellitus. The present study aimed to test the hypothesis that nitric oxide synthases (NOSs), which are expressed in blood vessel endothelium, contribute to the mitigation of vascular endothelium-dependent dysfunction by aerobic exercise in prediabetes mellitus. A prediabetic rat model was established by feeding the rats an additional high-energy diet, and was confirmed by testing blood glucose levels, the area-under-the-curve for the blood glucose tests (P

Fluorescence spectroscopy in combination with UV absorption spectroscopy was carried out to investigate the interaction between the neodymium–naproxen complex (Nd–NAP) and calf thymus DNA (ctDNA). The experimental results showed that Nd–NAP intercalated with the ctDNA base pairs. Analysis of fluorescence quenching data of Nd–NAP by ctDNA at different temperatures using a Stern–Volmer equation revealed that dynamic and static quenching occurred simultaneously. The binding constants and the number of binding sites at 293 and 310 K were obtained as 2.904 × 104 L mol−1, 1.172 and 2.432 × 104 L mol−1, 1.143, respectively. The thermodynamic parameters ΔG, ΔH, and ΔS calculated at different temperatures indicated that hydrogen bonding and van der Waals force were the main binding forces. © 2012 Wiley Periodicals, Inc. J Biochem Mol Toxicol 26:193–198, 2012; View this article online at wileyonlinelibrary.com. DOI 10.1002/jbt.21401

Hydraulic resistance components and water relations were studied on Haloxyolon ammoden- dron, a small xeric tree, growing at sites significantly differed in soil texture. Soil water content, leaf water potential (ψl), xylem water potential (ψx), root water potential (ψroot), leaf transpiration rate (TR) and stomatal conductance (gs) were measured at the two sites during the growing season of 2005 and 2006. Leaf spe- cific hydraulic resistance (Rplant) during the whole growing season, hydraulic resistance of plants (Rp), shoots (Rshoot) and roots (Rroot) in the August of both years were calculated and expressed on leaf area basis. The results showed the proportion of the hydraulic resistance of the aerial part (Rshoot) to the Rp was the same to the proportion of the hydraulic resistance of the soil part (Rroot) to the Rp, indicating that both parts were equivalent important to plant water hydraulic system from soil to leaf. Positive significant corre- lations were found between Rp and Rroot, suggesting that root hydraulics resistance was a major determi- nant of plant hydraulic resistance (Rp) and transpiration rate. The integrated effect of stomatal control, hy- draulic regulation and morphology adjustment enabled plants at heavy soil site surviving the extreme water deficit period.

The phase transition behavior of totally synthetic bilayer-forming amphiphiles, CnAzoCmN+Br−,with various chain lengths of the spacer (m) and tail (n) parts, has been investigated by the differential scanning calorimetry, X-ray diffraction, and absorption spectroscopic methods. The compounds which have the relationship of m − n = 2 showed similar aggregation states, the so-called H-aggregation state. However, there are some structural differences between the odd and the even number compounds in the hydrophilic region. These structural differences made big differences in the transition temperatures (Tc), enthalpy (ΔH) and entropy (ΔS) at Tc between the odd and even number compounds. On the other hand, the CnAzoC5N+Br− (n = 6 ∼ 12) showed very similar molecular aggregation states, the so-called J-aggregation state. Their transition temperatures showed no such tendency. They had similar values of about 130°C. However, very small odd-even effects of the ΔH and ΔS at Tc were observed. These were attri...

A totally synthetic azobenzene-containing amphiphile C32H52N3O3Br (C6AzoC10N+Br−) was crystallized from its solution in trichloromethane and ethanol. The crystal is triclinic with space group P\bar1; Z=2; a=24.317(5), b=8.632(1), and c=8.043(2) A; and α=91.41(2), β=80.62(2), and γ=99.01(1)°. The structure was solved by the direct method and refined by the full-matrix least-squares method: R=0.038 for 4305 observed reflections (2θ

The molecular and packing structures of H-aggregates of azobenzene-containing amphiphiles, C6AzoC8N+Br− and C8AzoC10N + Br−, have been determined by X-ray single crystal analyses. Both crystals belong to the monoclinic system with the space group P21 and Z = 2. The unit cell dimensions of the former crystal are a = 34.04(7), b = 7.468(2), c = 5.967(1) A, β = 94.67(3)˚. Those of the latter are a = 38.81(2), b = 7.451(1), c = 5.936(1) A, β = 97.56(3)˚. Molecular and crystal structures of these two compounds are quite similar. Molecules are packed laterally to form a monolayer structure. Therefore, two hydrophobic chains are arranged in the antiparallel fashion and interdigitated mutually. Contrary to the expectation for the H-aggregates, a fairly large inclination angle (ca. 65˚) was observed between the planes of the neighboring azobenzene chromophores.

A series of novel 4-azaindolyl-indolyl-maleimides were synthesized and evaluated for their GSK-3beta inhibitory activity. Most compounds exhibited high potency to GSK-3beta. Among them, compound 7c was the most promising GSK-3beta inhibitor. Preliminary structure-activity relationships were discussed based on the experimental data obtained and showed that different substituents on the indole ring and side chains at 1-position of indole had varying degrees of influence on the GSK-3beta inhibitory potency. In a cell-based functional assay, compounds 7c and 15a significantly reduced Abeta-induced Tau hyperphosphorylation by inhibiting GSK-3beta.

The Taihu Lake region in southern Jiangsu is one of the regions with flourishing economy and the highest level of urbanization due to favourable natural conditions and socio-economic foundation. However, there emerge a seriers of urban ecological problems on continuous stretch of cities and towns, a vague division of urban functions, ground subsidence, serious pollution of atmosphere and waters arising from dense population, irrational distribution of industry, backwardeness of municipal engineering facilities, and inexperienced scientific management of water resources. In order to improve the urban eco-environment in this lake region, we should work out an overall regional eco-environmental programme, perfect the urban economic set-up from the reqirements of urban material circulations and energy exchanges, and finally put into practice the urban functional regionalism, so that the Taihu Lake region in southern Jiangsu has not only a higher economic benefit, but also a beautiful and comfortable eco-environment.

Xiamen is an important coastal harbour and tourist city. Since the establishment of the Xiamen Special Economic Zone in 1980, great changes of developments in economy and urban construction have taken place. The comprehensive development is most important to Xiamen’s future. Xiamen has favorable geographical location, high level of economy opening to the outside world and close relation with Xiamen- Zhangzhou-Guanzhou economic area. The Xiamen Special Economic Zone should play the role of central city in the south Fujian Province.

Totally synthetic azobenzene-containing amphiphiles C10AzoC5N+Br− and C8AzoC5N+Br− (C31H50N3O3Br and C29H46N3O3Br respectively) were crystallized from their solutions by the solvent-evaporation method. Both crystals are triclinic, with the space group of P\bar1 and Z=2. The unit cell dimensions of the former crystal are a=3.233(5), b=0.854(2), c=0.608(1) nm, α=106.96(8), β=86.6(1), and γ=88.3(1)°. Those of the latter crystal are a=3.0098(6), b=0.8553(2), c=0.6084(1) nm, α=72.99(1), β=92.57(2), and γ=95.64(2)°. The crystal structure of C10AzoC5N+B− was solved by the direct method and refined by the block-diagonal least-squares method: R=0.082 for 2927 observed reflections (2θ