Copper-Catalyzed [3 + 2] Annulation of O-Acyl Oximes with 4-Sulfonamidophenols for the Synthesis of 5-Sulfonamidoindoles and 2-Amido-5-sulfonamidobenzofuran-3(2H)-ones.

A copper-catalyzed [3 + 2] annulation of O-acyl oximes with 4-sulfonamidophenols is developed. The advantage of this method lies in the concurrent double activation of two substrates to form nucleophilic enamines and electrophilic quinone monoimines. The substituent on the α-carbon of O-acyl oxime determines two different reaction pathways, thereby leading to the selective generation of 5-sulfonamidoindoles and 2-amido-5-sulfonamidobenzofuran-3(2H)-ones.

Anxiolytic-like effect of α-asarone in mice.

The effects of α-asarone in four assays predictive of anxiolytic activity in male mice were studied, with diazepam as a positive anxiolytic control. The use of the elevated plus-maze test revealed that diazepam (2 mg/kg) or α-asarone (3.5 mg/kg) increased the percentage of entries into open arms and of the time spent on open arms. In the light/dark transition test, as with 2 mg/kg diazepam, 7 mg/kg α-asarone increased the time spent in the light area and the number of transitions between the two compartments. In the novel food consumption test, α-asarone (3.5, 7 and 14 mg/kg) caused significant increases in food intake during 5 min as well as diazepam (0.5 mg/kg). In the marble burying test, α-asarone also produced a significant inhibition of marble burying at doses of 14 and 28 mg/kg, as did diazepam (5 mg/kg). Thus, these findings indicated that α-asarone exhibited an anxiolytic-like effect. Further studies will be required to assess the generality of the present findings to other species and behavioral paradigms.

The analysis of the characteristics of imported COVID-19 cases from January to April in 2020: a cross-sectional study.

Background: Since the first case reported in December 2019, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused an outbreak of coronavirus disease 2019 (COVID-19) worldwide. The global case count continued to rise and the WHO declared a Public Health Emergency of International Concern (PHEIC), causing a growing risk of imported COVID-19 infection. This study aimed to provide descriptive and quantitative epidemiological characteristics of imported COVID-19 cases in China. Methods: This cross-sectional study examined all imported COVID-19 cases in Mainland China from 22 January to 21 April 2020. Ratios, Median and percentile were used for descriptive analysis. Spearman's correlation analysis was performed between daily new imported cases in Mainland China and the country of origin. The chi-square test was used to evaluate the difference between home quarantine and compulsory centralized quarantine on native transmission. Results: A total of 1,610 cases of COVID-19 were imported from 49 countries to 27 provincial administrative regions in China; 79.8% were from European countries and the United States of America (the USA). Before 29 March 2020, the imported cases were mainly from the USA (27.7%) and United Kingdom (UK; 42.6%). After 29 March 2020, the daily newly imported cases from Russia rapidly grew. After 12 April 2020, the number of daily newly imported cases gradually decreased and remained at a low level (12±7 cases per day). Airport entry was encouraged, and ground border crossing was limited. Among the 1,610 cases, 54.0% were in the asymptomatic incubation period on arrival in Mainland China. Conclusions: The transmissions by imported COVID-19 were gradually and effectively curbed in Mainland China, despite a disproportionally high number of cases worldwide. Entry screening measures must be implemented universally to all inbound travelers at a point of entry or targeted to specific travel routes or to specific travelers. Compulsory centralized quarantine should be recommended in the prevention of the imported COVID-19 epidemic.

Speckle-Free SAR Image Ship Detection.

Ship detection is one of important applications for synthetic aperture radar (SAR). Speckle effects usually make SAR image understanding difficult and speckle reduction becomes a necessary pre-processing step for majority SAR applications. This work examines different speckle reduction methods on SAR ship detection performances. It is found out that the influences of different speckle filters are significant which can be positive or negative. However, how to select a suitable combination of speckle filters and ship detectors is lack of theoretical basis and is also data-orientated. To overcome this limitation, a speckle-free SAR ship detection approach is proposed. A similar pixel number (SPN) indicator which can effectively identify salient target is derived, during the similar pixel selection procedure with the context covariance matrix (CCM) similarity test. The underlying principle lies in that ship and sea clutter candidates show different properties of homogeneity within a moving window and the SPN indicator can clearly reflect their differences. The sensitivity and efficiency of the SPN indicator is examined and demonstrated. Then, a speckle-free SAR ship detection approach is established based on the SPN indicator. The detection flowchart is also given. Experimental and comparison studies are carried out with three kinds of spaceborne SAR datasets in terms of different polarizations. The proposed method achieves the best SAR ship detection performances with the highest figures of merits (FoM) of 97.14%, 90.32% and 93.75% for the used Radarsat-2, GaoFen-3 and Sentinel-1 datasets, accordingly.

Genetic map construction and QTL analysis of leaf-related traits in soybean under monoculture and relay intercropping.

Soybean (Glycine max L.) is an important food and oil crop widely planted by intercropping in southwest China. The shade caused by intercropping changes plant growth traits, such as soybean leaf and dry mass, thereby reducing yields. To improve the yield and elucidate the genetic mechanism of the leaf-related traits in intercropped soybeans, we measured the F6:7-8 recombinant inbred lines (RILs) derived from the cross of 'Nandou 12' and 'Jiuyuehuang' for six leaf-related traits under monoculture and relay intercropping in 2015 and 2016. We found 6366 single-nucleotide polymorphisms (SNPs) markers that covered the whole genome of soybean distributed in 20 linkage groups, which spanned 2818.67 cM with an average interval of 0.44 cM between adjacent markers. Nineteen quantitative trait loci (QTLs) were detected in two environments in 2 years. Three candidate genes associated to leaf-related traits were found according to gene expression and GO enrichment analyses. These results revealed the susceptibility of leaf phenotype to shading and helped elucidate the mechanisms that control leaf-related traits.

Value of radiographic esophageal imaging in determining an optimal atrial septal puncture site for percutaneous balloon mitral valvuloplasty.

OBJECTIVE: To investigate the value of radiographic esophageal imaging in facilitating transseptal catheterization in patients undergoing percutaneous balloon mitral valvuloplasty. SUBJECTS AND METHODS: A total of 468 patients were randomized into either the study group (n = 234), in which radiographic esophageal imaging by the oral administration of a contrast media took place, or the control group (n = 234), in which the Ross technique was used. Of the 468 patients, 203 were males and 265 were females. The average ages of the study and control groups were 53 +/- 16 and 51 +/- 17 years, respectively. The patients had severe left atrial enlargement, as measured using 2-dimensional echocardiography. RESULTS: In the study group, the left atrial impression on the esophagus was clearly seen, and was used to identify the puncture site on the right atrial side for the passage of the transseptal catheter. In the control group, the left atrial silhouette was not clearly shown by fluoroscopy in 112 patients (47.5%). The success rate of transseptal catheterization in the study group was higher than in the control group (99.6 vs. 45.7%, p = 0.0001). There were no complications in the study group, but pericardial tamponade occurred in 1 patient in the control group. CONCLUSION: Radiographic esophageal imaging facilitates the identification of an optimal atrial transseptal puncture site, and improves the success rate of transseptal catheterization in patients undergoing percutaneous balloon mitral valvuloplasty.

[Expression of human insulin in lactic acid bacteria and its oral administration in non-obese diabetic mice].

Type 1 diabetes mellitus (T1DM) is an auto-immune disease while oral administrating its autoantigens could be a treatment of T1DM. To express human insulin gene (ins) in lactic acid bacteria (LAB) for oral vaccine, ins gene was replaced by LAB bias codon and an 8-amino-acid-residue linker peptide forming a beta-turn was designed to link insulin chain A and B. After synthesized by primer annealing method, the whole ins gene was fused with signal peptide sequence SP(Usp45), subcloned into a LAB secretory expressive vector pSW501 and then introduced to Lactococcus lactis (L. lactis) MG1363 and Lactobacillus casei (Lb. casei ) ATCC27092 respectively. Western blot showed that the expression product (SP(Usp45)-INS protein) targeted mainly at the cell wall while little was found in cytoplasm or supernatant. The highest expression level emerged in exponential phase when the optical density at 600nm of the culture was 0.4. The culture of the recombinant strain Lb. casei/pSW501 was administered to non-obese diabetic (NOD) mice orally. ELISA and Western blot results showed that the recombinant strain could induce SP(Usp45)-INS-specific antibodies and raise IL-4 level (38.583 +/- 2.083 pg/mL, P < 0.05) in the mice' s sera. Expression of insulin in the food-grade vehicle LAB could induce oral immune tolerance in NOD mice and protect it from pancreas injury, suggesting it might be a new way to the treatment of T1DM.

[Preparation of kangfuxin colon targeting micro-pellets].

OBJECTIVE: To prepare coated micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting delivery system, to make them go to colon, then release, educe partial effect. METHOD: We eploy pan-pill to prepare simple pellets, and prepare tunicatus pellets with fluidized bed coating. We investigated the preparation and parameter of pellets, so, we bolting the best shaping and tunicatus artwork. RESULT: The ingredients for preparing the micro-pellets are 125% starch +2% CMC-Na, and add 30% ethanol to be binder, pellets were coated with Eudragit S100 to prepare ph-dependent and pectin-HPMC to prepare enzyme-dependent colon targeting micro-pellets. CONCLUSION: We get two micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting.

[In vivo/in vitro evaluation of Kangfuxin colon targeting capsules].

OBJECTIVE: To evaluate the release in fixed position of pH-dependent and enzyme-dependent Kangfuxin colon targeting capsules in vivo and in vitro. METHOD: The dissolution was tested in vitro and X-ray radiography was used for the evaluation in vivo. RESULT: After two hours pH-dependent colon targeting in man-made colon fluid, medicine release in fixed position on the whole, colon loc-release. Add enzyme into man-made colon, when enzyme-dependent colon targeting in it, then medicine release quickly, mainly release in fixed position; The conveying time in vivo of pH-dependent and enzyme-dependent capsules have big individuality difference. In the experiment, disintegration is stabilize among individuales, between 2.0-3.5 hours. CONCLUSION: Kangfuxin colon targeting capsules of two principles all release in fixed position to achieve the goal.

Effects of taurine on rat behaviors in three anxiety models.

In our previous studies using an elevated plus-maze test in mice, taurine was shown to present an anxiolytic-like effect after single and repeated administration. The aim of the present study was to investigate the anxiolytic and behavioral effects of taurine on rats in the open field, hole-board, and social interaction test compared to the positive control diazepam. Taurine (14, 42, and 126 mg/kg, i.p.) was administered 30 min before the tests. In the social interaction and hole-board tests, taurine (42 mg/kg) significantly increased social interaction time and the number and duration of head-dipping. In the open field test, taurine (126 mg/kg, i.p.) presented anxiolytic-like effects by increasing the number of center entries, time spent in the central area and the anti-thigmotactic score while having no effect on the locomotor activity. Results from these experiments suggest that taurine produces an anxiolytic-like effect in these animal models and may act as a modulator or anti-anxiety agent in the central nervous system.

Anxiolytic-like effect of asiaticoside in mice.

The putative anxiolytic activity of asiaticoside was examined in male mice by using a number of experimental paradigms of anxiety, with diazepam being as a positive anxiolytic control. In the elevated plus-maze test, diazepam (1 and 2 mg/kg) or asiaticoside (5 or 10 mg/kg) increased the percentage of entries into open arms and of time spent on open arms. In the light/dark test, as with 1 mg/kg diazepam, asiaticoside (10 and 20 mg/kg) increased the time spent in the light area and the movement in the light area without altering the total locomotor activity of the animals. In the hole-board test, asiaticoside at 10 mg/kg significantly increased head-dipping counts and duration as well as diazepam (0.3 mg/kg). Thus, these findings indicated that asiaticoside exhibited an anxiolytic-like effect. Further studies will be required to assess the generality of present findings to other species and behavioural paradigms.

Behavioral effects of sinomenine in murine models of anxiety.

The present study was designed to investigate the putative anxiolytic-like effect of sinomenine in three experimental models of anxiety in male rats and mice. Use of the elevated plus-maze test revealed that sinomenine (20 and 40 mg/kg, p.o.) increased the percentage of open arm entries and diazepam (2 mg/kg, p.o.) increased the percentage of open arm entries, the percentage of time spent on open arms and total arm entries in mice. In the light/dark transition test, sinomenine (20 and 40 mg/kg, p.o.) increased time spent in the light area and diazepam (2 mg/kg, p.o.) increased time spent in the light area and the overall movements in mice. In the social interaction test, the sinomenine-treated animals significantly increased social interaction time in low light unfamiliar (7 mg/kg, p.o.) and high light unfamiliar conditions (7 and 14 mg/kg, p.o.) as well as diazepam (3 mg/kg, p.o.). Sinomenine (28 mg/kg, p.o.) can also decrease squares entered in rats in social interaction test under low light unfamiliar condition. In the open-field test, sinomenine (160 mg/kg) decreased squares entered in mice. Thus, these findings indicated that sinomenine exhibited anxiolytic-like effect.

Anxiolytic-like effect of paeonol in mice.

The present study in mice compared the putative anxiolytic-like effect of paeonol, a phenolic component from the root bark of Paeonia moutan, with the benzodiazepine diazepam in the elevated plus maze and the light/dark box-test. The comparison was also with regard to locomotor activity (open-field test) and myorelaxant potential (inclined plane test). As with 2 mg/kg diazepam, paeonol (at 17.5 mg/kg) increased the percentage of time spent on open arms in the elevated plus maze and increased the time spent in the light area of the light/dark box (at 8.75 and 17.5 mg/kg). Since paeonol, in contrast to diazepam, had no effect on either the number of squares entered in the open-field test or in the inclined plane test, its side-effect profile is considered as superior to the benzodiazepine.

The effects of angelica essential oil in social interaction and hole-board tests.

In our previous studies, we have demonstrated the anxiolytic effects of angelica essential oil in three anxiety models using mice. This study aimed to characterize the similar behavior effects of angelica essential oil in the social interaction test of anxiety and the hole-board test of exploration and locomotor activity in rats. These results indicate that angelica essential oil possessed a wide range of anxiolytic properties. In the social interaction test, angelica essential oil decreased aggressive behaviors at the doses of 21 and 42 mg/kg, while the doses of 21 and 42 mg/kg significantly increased social interaction time of the high light, unfamiliar test condition and 21 mg/kg could also prolong social interaction time of the high light, familiar test condition. In the hole-board test, angelica essential oil at 10.5 mg/kg significantly increased head-dipping counts and duration. Thus, our findings suggest the potential usefulness of angelica essential oil against various types of anxiety-related disorders and social failure.

Anxiolytic-like effect of succinic acid in mice.

The putative anxiolytic activity of succinic acid was examined in male mice by using a number of experimental paradigms of anxiety and compared with that of the known anxiolytic compound diazepam. Use of the elevated plus-maze test revealed that diazepam (1.0, 2.0 and 4.0 mg/kg, PO) or succinic acid (3.0 or 6.0 mg/kg, PO) increased the percentage of entries into open arms and of time spent on open arms. In novel food consumption test, succinic acid (3.0, 6.0, and 12.0 mg/kg, IP) caused significant increases in food intake during 5 min when compared with the vehicle. In the stress-induced hyperthermia test, 40 min after drug administration rectal temperature was measured, succinic acid at dose of 1.5 mg/kg, inhibited stress-induced hyperthermia. Thus, these findings indicated that, in contrast with diazepam, succinic acid exhibits anxiolytic-like effect.

Possible anxiolytic effects of taurine in the mouse elevated plus-maze.

The effects of taurine, an inhibitory amino acid, on the behavior of male mice were examined in the elevated plus-maze test of anxiety. Acute taurine treatment (60 mg/kg, PO) significantly increased the percentage of time spent in the open arms. Moreover, when taurine was administered daily for seven days and the plus-maze test was conducted 40 minutes after the last administration, a significant increase of the percentage of time in the open arms was observed even at dose of 2.5 mg/kg, however the open arm entries and the total entries were unaffected at any dose tested. In order to get a comprehensive profile of drug action, detailed behavioral analyses were further exerted. Single administration of 60 mg/kg taurine can significantly reduce the total rears. The results suggest that taurine have some anxiolytic-like properties, although its effects seem more limited and are not consistent with those presented by classic anxiolytics, such as diazepam.

The effects of angelica essential oil in three murine tests of anxiety.

The effects of angelica essential oil in three assays predictive of anxiolytic activity in male mice were studied, with diazepam as a positive anxiolytic control. In the elevated plus-maze test, compared to the positive control diazepam, angelica essential oil (30.0 mg/kg, PO) had a modest anxiolytic-like effect (increased the percentage of open-arm time and reduced the percent protected head dips). In the light/dark test, angelica essential oil (30.0 mg/kg) prolonged the time spent in the light area without altering the locomotor activity of the animals. In the stress-induced hyperthermia test, 60 and 70 min after drug administration, rectal temperature was measured twice, angelica essential oil at the dose of 30.0 mg/kg inhibited stress-induced hyperthermia. Thus, these findings indicate that angelica essential oil, as does diazepam, exhibits an anxiolytic-like effect. Further studies will be required to assess the generality of the present findings to other species and behavioural paradigms.

[Anti-emetic effect of ethanol extract from "Wuzhuyu broth"].

OBJECTIVE: To investigate the anti-emetic effect of ethanol extract from "WuZhuYu broth" and its mechanism. METHOD: Three experiments were carried out test which extract has anti-emetic activity, such as CuSO4-induced pigeon's emetic response, gastric emptying in mice and ACh-induced or 5-HT-induced contraction in vitro gastric muscle in rats. Meanwhile, effect of anti-emetic extract on concentration-response curve to ACh, 5-HT, histamine was investigated. RESULT: 50% ethanol extract and 70% ethanol extract were identified as having significantly stronger anti-emetic activities with little side effect, which showed the significant effect on concentration-response curve to ACh, 5-HT, histamine. CONCLUSION: 50% ethanol extract and 70% ethanol extract contain more anti-emetic fractions, more anti-emetic fractions can be gained at the concentrations of 50% and 70% ethanol; the mechanism of anti-emetic effect is related to its antagonism to the receptors of ACh, 5-HT, histamine.

Effect of intracoronary tirofiban in patients undergoing percutaneous coronary intervention for acute coronary syndrome.

BACKGROUND: To investigate the efficacy of intracoronary tirofiban during primary percutaneous coronary intervention (PCI) for patients with acute coronary syndrome (ACS). METHODS AND RESULTS: The 118 patients aged 70 years and above (average age 75+/-2) were divided into study (n = 58, intracoronary bolus tirofiban) and control (n = 57, intravenous tirofiban) groups. The culprit vessels were targeted with primary PCI in all patients. Compared with the control group, the study group showed better Thrombolysis In Myocardial Infarction (TIMI) flow grades and TIMI myocardial perfusion grades (TMPG) immediately after PCI (p = 0.016 and 0.026, respectively). The 14-day composite major adverse cardiac events rate was lower in the study group (3.5% vs 17.5%, p = 0.030), but was similar between the 2 groups at 30 days following PCI (7.0% vs 1.7%, p = 0.350). The left ventricular ejection fraction in the study group was higher than in the control group 30 days following PCI (67.4+/-6.2% vs 60.7+/-4.6%, p = 0.033). The 14-day bleeding complication (p = 0.201) and platelet reduction rates (p = 0.984) were similar between the 2 groups. CONCLUSION: In patients with ACS undergoing primary PCI, intracoronary bolus administration of tirofiban is superior to intravenous bolus injection for improving coronary flow, myocardial perfusion and short-term clinical outcomes.

Identification of some benproperine metabolites in humans and investigation of their antitussive effect.

AIM: To identify 4 unknown metabolites of benproperine (BPP, 1) in human urine after a po dose, and to investigate the antitussive effect of monohydroxylate metabolites. METHODS: The putative metabolite references were prepared using chemical synthesis. Their structures were identified using 1H and 13C nuclear magnetic resonance, and mass spectrometry. The metabolites in human urine were separated and assayed using liquid chromatography-ion trap mass spectrometry (LC/MS/MS), and further confirmed by comparison of their mass spectra and chromatographic retention times with those of synthesized reference substances. The antitussive effects of metabolites were evaluated on coughs induced by 7.5% citric acid in conscious guinea pigs. RESULTS: 1-[1-Methyl-2-[2-(phenylmethyl)phenoxy]-ethyl]-4-piperidinol (2), 1-[1-methyl-2-[2-(phenylmethyl)phenoxy] ethyl]-3-piperidinol (3) and their glucuronides 4 and 5 were obtained from chemical synthesis. Four urinary metabolites in human urine showed peaks with the same chromatographic retention times and mass spectra in LC/MS/MS as synthetic substances 2, 3, 4 and 5. Phosphates of compounds 2 and 3 prolonged the latency of cough and reduced the number of coughs during the 3 min test using citric acid, but did not reduce the number of coughs during the 5 min immediately after the test in conscious guinea pigs. CONCLUSION: Compounds 2, 3, 4, and 5 were identified as the metabolites of BPP in human urine. Among them, compounds 2 and 3 are inactive in the antitussive effect.