Discovery of 4-(phenoxymethyl)-1H-1,2,3-triazole derivatives as novel xanthine oxidase inhibitors.

A series of 4-(phenoxymethyl)-1H-1,2,3-triazole derivatives were designed, synthesized, and evaluated for their xanthine oxidase (XO) inhibitory activities. Among these compounds, 9m emerged as the most effective XO inhibitor with an IC50 value of 0.70 µM, which was approximately 14-fold more potent than allopurinol. Additionally, compound 9m displayed favorable drug-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. We further explored the binding mode of 9m in complex with XO by molecular docking and molecular dynamics studies. In vivo hypouricemic studies also suggested that 9m could effectively lower the serum uric acid levels of rat. In summary, compound 9m could be a promising lead for further development of XO inhibitors.

[Ultrastructure observations on antennal sensilla of Heortia vitessoides the most serious pest of Aquilaria sinensis].

Heortia vitessoides is the most serious pest of Aquilaria sinensis,which is an economically important evergreen tree native to China and is the principal source of Chinese agarwood. In severe infestations,the insects completely eat up the leaves of A. sinensis,causing severe economic losses. In a more recent study,we found that the antennal sensilla of adult play important roles in the host location,mating and oviposition of H. vitessoides. Here,the external morphology of the antennal sensilla of H. vitessoides were examined using scanning electron microscopy. The result showed that the antennae of both sexes of H. vitessoides were filiform in shape,which consist of the scape,pedicel and about 64 segments of flagellomeres. Eight morphological sensilla types were recorded in both sexes,including sensilla trichodea,sensilla chaetica,sensilla basiconica,sensilla coeloconica,sensilla styloconica,sensilla auricillica,sensilla squamiformia and böhm bristle. Major differences were recorded in the distribution and quantity of different sensilla types in each segment of antenna. The sensillas are almost confined to the ventral and lateral surfaces rather than the back side of antennae. Antennal flagella contained the most sensilla while the scape and pedicel segments only contained böhm bristles and sensilla squamiformias. Sensilla trichodea Ⅲ were only found on male antennae. These results are discussed in relation to the possible roles of the sensilla types in the host location,mating and oviposition selection behavior of H. vitessoides.

[Spectroscopic Studies on the Host Plant Selection Mechanism of Trabala vishnou gigantina Yang (Lepidoptera: Lasiocampidae)].

Trabala vishnou gigantina Yang (Lepidoptera: Lasiocampidae) is a polyphagous forestry pest whose periodic breaking out results in great economic damage including total crop failure to forestry and fruit production in China. In this study, in order to improve the understanding of the host plant selection mechanism of T. vishnou gigantina larvae, locust, caragana, willow, poplar, apricot and sea-buckthorn were used as potential host plants for the test. Two-way choice experiment method was used to study the T. vishnou gigantina Yang feeding preferences of the six kinds of plants. Moreover, the chemical component and physical structure of six plants were analyzed with Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD). Among the six plants, T. vishnou gigantina larvae showed a strong preference for sea-buckthorn, followed by, apricot, willow, poplar, locust, and caragana. The FTIR analysis displayed that those six plants presented similar characteristic on absorption peak position, peak amount, and shape. The targets (1 154/1 733, 1 154/898) by FTIR showed that lipids and polysaccharide were major nutriments to affect the host plant selection of T. vishnou gigantina larvae. The XRD results showed that crystallinity index (CrI) also could affect the host plant selection of T. vishnou gigantina larvae. In this research, spectroscopy technology was firstly applied to the study of interactive relationship between insect and host, which would blaze a trail for intensive study of host plant selection mechanism of insect at molecular level.

New gall wasp species attacking chestnut trees: Dryocosmus zhuili n. sp. (Hymenoptera: Cynipidae) on Castanea henryi from southeastern China.

A new gall wasp species, Dryocosmus zhuili Liu et Zhu, is herein described from the southeastern Fujian province of China. The new species induces galls on trees of Henry's chestnut, Castanea henryi, which is also a native host for the notorious Oriental chestnut gall wasp (OCGW, Dryocosmus kuriphilus Yasumatsu). D. zhuili overlaps with OCGW in emergence time and induces galls morphologically similar to that of OCGW on similar plant parts. In a previous study, we reported considerable divergence between mtDNA CO1 (mitochondrial DNA Cytochrome c oxidase subunit I) sequences of these wasps and the true OCGW wasps and suggested the existence of a cryptic species. Herein, we confirm the identity of the new species based on morphological and biological differences and provide a formal description. Although the new species is relatively easily separated from OCGW on basis of morphology, field identification involving the two species can still be problematic because of their small body size, highly similar gall morphology, and other life history traits. We further discussed the potential of the new species to be a pest for the chestnut industry and the consequences of accidental introduction of this species into nonnative areas, especially with regard to the bisexual reproduction mode of the new species in contrast to the parthenogenetic reproduction mode of OCGW.

[Features of Clinical Register of Chinese Medicine and Pharmacy Based on ClinicalTrials.gov. (USA)].

In recent 10 years, clinical trials of Chinese medicine and pharmacy (cMP) at clinicalTrials.gov.(USA) are gradually increasing. In order to analyze features of CMP clinical register, ClinicalTrials.gov register database were comprehensively retrieved in this study. Included clinical trials were input one item after another using EXCEL. A final of 348 CMP clinical trials were included. Results showed that China occupied the first place in CMP clinical register, followed by USA. CMP clinical trials, sponsored mainly by colleges/universities and hospitals, mostly covered interventional studies on evaluating safety/effectiveness of CMP. The proportions of studies, sponsored by mainland China and companies, recruitment trials and multi-center clinical trials in interventional trials were increasing. The proportions of studies sponsored by Hong Kong and Taiwan, research completed trials, unclear research status, phase III clinical trials, and published research trials in interventional trials were decreasing. Published ratios of CMP clinical trials were quite low. There were more missing types and higher proportions in trial register information.

[The necessity and feasibility of establishing technical specifications for registry of Chinese medicine clinical study].

International clinical trials register is one of the global measures to realize transparency in clinical trials and also one of a powerful measure to improve the quality of clinical trials. Many scholars studying the quality of TCM clinical trials find that they are poor in quality and lack transparency. Furthermore, they find that TCM clinical trial registry has many problems. We must base on the successful experiences of WHO and international clinical trial registry to establish technical specifications for registry of traditional Chinese medicine clinical study of their own. Then, it can effectively improve the overall level of TCM clinical studies. We have suggested some concrete and feasible measures to establish technical specifications for registry of traditional Chinese medicine clinical study of their own based on the problems of TCM clinical trial registry.

Ultrastructure of antennal sensilla in Hydrotaea armipes (Fallén) (Diptera: Muscidae): new evidence for taxonomy of the genus Hydrotaea.

The morphology and ultrastructure of the antennal sensilla of male Hydrotaea (Hydrotaea) armipes (Fallén) are examined via scanning electron microscopy in order to highlight the importance of antennal sensilla as a source of morphological characters for taxonomy and phylogeny of Hydrotaea. Antennal scape and pedicel have only one type of sensilla, the sharp-tipped chaetic sensilla, whereas antennal funiculus possesses several types of sensilla, including trichoid sensilla, two subtypes of basiconic sensilla, coeloconic sensilla and clavate sensilla. These results are compared with previously published studies on other fly species, especially on H. (H.) irritans (Fallén) and H. (Ophyra) chalcogaster (Wiedemann), and there are possible uniquely derived characters or diagnostic characters examined on antennal pedicel and antennal funiculus, which suggests either affinities and divergence between species at subgenus level. Thus, new morphological evidence is provided, which might help to develop the much disputed taxonomy of genus Hydrotaea Robineau-Desvoidy in future.

New artificial diet for continuous rearing of the bean pod borer, Maruca vitrata.

The bean pod borer, Maruca vitrata Fabricius (Lepidoptera: Crambidae), is a serious pantropical pest of grain legumes. A suitable artificial diet is desirable for producing uniform insects for commercial purposes or research. Three previously described artificial diets, 1 newly-developed artificial diet, and cowpea (Vigna unguiculata (L.) Walp. (Fabales: Fabaceae)), the natural hostplant of M. vitrata, were used for rearing M. vitrata, and the life parameters were examined. The results indicated that insects completed a full life cycle only when the larvae were fed cowpea or the diet reported by Onyango and Ochieng'-Odero ( 1993 ), called the "D-OO diet." However, the rearing efficiency (i.e., larval and pupal survival, longevity of adults, and fecundity) on the D-OO diet was inferior to the rearing efficiency on cowpea. Subsequently, a new artificial diet was formulated based on soybean powder, Glycine max (L.) Merr. (Fabales: Fabaceae), and wheat germ, Triticum aestivum L. (Poales: Poaceae). The egg production, egg hatching, larval developmental duration, and pupal survival of the M. vitrata reared on the new artificial diet were found to be significantly improved relative to the D-OO diet, but were not significantly better than on the host-plant cowpea. The optimum rearing density was 15-25 larvae per box. There were no significant changes in reproductive potential after 8 successive generations of rearing on the new diet. These results indicated that the newly developed diet could serve as a viable alternative to cowpea plant for continuous rearing of M. vitrata.

Female sex pheromone blends and male response of the legume pod borer, Maruca vitrata (Lepidoptera: Crambidae), in two populations of mainland China.

The legume pod borer, Maruca vitrata (Lepidoptera: Crambidae; syn. M. testulalis), is a serious pantropical insect pest of grain legumes. Comparative studies of M. vitrata female sex pheromone components in two different geographic populations in China, Wuhan and Huazhou, confirmed that (E,E)-10,12-hexadecadienal (E10,E12-16:Ald) and (E)-10-hexadecenal (E10-16:Ald) were present in variable ratios in all pheromone gland extracts of both populations. (E,E)-10,12-hexadecadienol (E10,E12-16:OH) was always detected in minor amounts using polar DB-WAX columns, but was never detected using medium-polar DB-17 columns for the two populations. E10-16:OH was not found in any of the M. vitrata sex pheromone gland extracts. The average ratios of E10-16:Ald, E10,E12-16:Ald, and E10,E12-16:OH in the pheromone gland extracts of populations from Wuhan and Huazhou were 79.5:100:12.1 and 10.3:100:0.7, respectively. Electrophysiological testing suggested that E10,E12-16:Ald elicited the highest male electroantennography (EAG) response, followed by E10,E12-16:OH and E10-16:Ald. Field-trapping tests with single synthetic sex pheromone lures showed that E10,E12-16:OH alone could not attract males, whereas E10,E12-16:Ald or E10-16:Ald alone attracted few males. Wuhan and Huazhou males were most attracted by lures containing E10-16:Ald + E10,E12-16:Ald + E10,E12-16:OH in doses of (80 + 100 + 10) microg and (10 + 100 + 10) microg, respectively, per vial. Males could discriminate between the blends that were most attractive to their own geographic population and those that were most attractive to the reference population. Our findings suggest that geographic variation exists in the sex pheromone system of M. vitrata in China. The results are discussed with regard to the mechanisms underlying the sex pheromone variation.

[Pharmacovigilance of parenterally administered salvianolate based on analysis of spontaneous reporting system data].

Spontaneous reporting system (SRS) is currently a basic method to monitor and find adverse drug reactions (ADR) signals used worldwide. This method can promptly and effectively discover ADR signals and is of great significance to effectively prevent and avoid ADRs. Parenterally administered salvianolate has the functions of activating blood circulation and removing stasis. It is mainly used in the treatment of stable angina pectoris. As the drug is widely used clinically and ADRs are increasingly reported promptly, ADR information in the national ADR monitoring center's SRS database has also increased. How to quickly and effectively identify suspicious ADRs is a major concern. This study uses BCPNN and PRR to detect early warning signals. S739 ADR case reports were identified. There were 106 types, 1 310 events, and 24 serious ADR cases ( 3.25% of 739 case reports) There wre no deaths. The ten most frequent ADRs were: rash, dizziness, itch, headache, chills and breath, nausea, palpitation, anaphylactic reaction and hot. The drugs early warning signs were dizziness, headache, nausea, itchiness and rash estimated using PRR. Early warning signs based on BCPNN were dizziness and headache. The ADRs of dizziness and headache are early warning signals associated with the nervous system.

[Expert consensus post-marketing evaluation scheme to detect immunotoxicity of Chinese medicine in clinical populations (draft version for comments)].

Through consensus, establish a post-marketing scheme and the technical processes to evaluate Chinese medicine's immunotoxicity on a population, as well as its beneficial influences on the immune system. Provide regulations on the collection, storage and transportation of serum samples. This article applies to the post-marketing scientific evaluation of the immunotoxicity of parenterally administered, and for other ways of taking Chinese medicine.

[Explore dengzhan xixin injection effecting on outcome of coronary heart disease based on propensity score].

Records of 2 325 patients with CHD were extracted from 20 hostpial information systems, who were divided into two groups, one group has 768 patients using Dengzhan Xixin, the other group has 1 557 patients without using Dengzhan Xixin. Using generalized boosted models (GBM) with propensity scores to balance confounding factors and using three Logistic regressions to analysis the cure rates of coronary heart disease. The results is that 72 knowing confounding factors between two groups, such as: age, admission condition, dying days, regression coefficients of three Logistic regressions were negative (P < 0.05), statistically, the result of using Dengzhan Xixin injection to cure coronary heart disease is significantly higher than do not using Dengzhan Xixin injection. Propensity score could be a good method to balance confounding factors in a retrospective data analysis. However it is not a prospective research, the information from this study should be carefully referred to.

Phase-controlled photon blockade in optomechanical systems.

The manipulation of photons is a key technology for obtaining optical quantum information. In this study, we present a phase-modulated optomechanical system comprising two coupled cavity resonators and illustrate the phase-controlled photon blockade in the system. The coupling phase of the cavities reveals the interference of photons and introduces an unconventional photon-blockade effect. We also study the influence of the energy level fineness on the photon blockade and resonant frequency of the mechanical mode. Numerical simulations demonstrate that photon blockade can occur over a wide range of system parameters. These results have several implications for understanding the role of the state phase in quantum cavity optomechanics and provide a promising method for the realization of optomechanical quantum devices using photon blockade.

(E)-2-styrylanthracene-9,10-dione derivatives as novel fluorescent probes: synthesis, photophysical properties and application in mitochondria imaging.

Our previous work firstly reported that (E)-2-styrylanthracene-9,10-dione is a novel fluorescent core (EK01) with the ability of specific mitochondria imaging. In this effort, we mainly focused our attention on the structure-photophysical property relationship and application in cells imaging of this new fluorescent chemotype. A series of the structural derivatives (TZ series) were designed and synthesized by introducing some substituents onto the 2-styryl moiety. The structure-photophysical property relationship analysis suggested that TZ03 is an excellent fluorescent molecular building block with the property of fluorescent "turn-on" effect after the modification of acylation, and TZ07 is an excellent fluorescent dye with a series of advantages such as high fluorescence intensity (Fmax = 4049.0 in CH2Cl2, 25.80 µM), moderate molar extinction coefficients (3.77 × 103-5.93 × 103 mol-1∙L∙cm-1), strong fluorescence quantum yield (Φmax = 0.739 in CH2Cl2), large Stokes shift (99.0 nm-161.8 nm) and well biological tolerance. As a classical D-π-A structure, the ICT characteristic of TZ07 was analyzed through spectroscopy verification and DFT calculations. Furthermore, optimized compound TZ07 was successfully applied in the living cells imaging with the excellent selectivity to mitochondria in a green fluorescent form. It was also suggested that the mechanism of TZ07 targeting mitochondria is independent of mitochondrial membrane potential, but probably related to the mitochondrial complex I. These findings may provide some insights into the development of novel mitochondria-targeted fluorescent probes.

Identification and field evaluation of pear fruit volatiles attractive to the oriental fruit moth, Cydia molesta.

Plant volatiles play a key role in host plant location of phytophagous insects. Cydia molesta is an important pest of pear fruit late in the growing season. We identified and quantified volatiles from immature and mature fruits of six pear varieties by using gas chromatography-mass spectrometry (GC-MS). Attractiveness of synthetic blends to adults based on gas chromatography-electroantennogram detection (GC-EAD) activity was investigated in both field and laboratory. Consistent electroantennographic activity was obtained for 12 compounds from headspace collections of the mature fruits of the six pear varieties. Qualitative and quantitative differences were found among six odor profiles. Among the six mixtures, the mixture of 1-hexanol, nonanal, ethyl butanoate, butyl acetate, ethyl hexanoate, hexyl acetate, hexyl butanoate, and farnesene (different isomers) with a 1:1:100:70:7:5:1:4 ratio from the variety Jimi and the mixture of nonanal, ethyl butanoate, 3-methylbutyl acetate, ethyl hexanoate, hexyl acetate, and farnesene with a 1:100:1:32:1:2 ratio from the variety Huangjin were highly attractive to both sexes in the field. However, male captures were much higher than those of females. Further wind tunnel tests proved that both sexes exhibited upwind flight to the lures, but only males landed on the source. Our finding indicates that mixtures mimicking Jimi and Huangjin volatiles attract both females and males of C. molesta, and these host volatiles may be involved in mate finding behavior.

[Analysis of volatile compounds of inflorescence by GC-MS from Cistanche deserticola].

OBJECTIVE: To study the volatile compounds from inflorescence of Cistanche deserticola and provide basis for its utilization and seed breeding. METHODS: The volatile compounds were collected by dynamic headspace adsorption and analyzed by gas chromatography-mass spectrometry (GC-MS). RESULTS: Forty volatile components were identified in inflorescence of Cistanche deserticola from squaring period to full-bloom period. The main components in buds of Cistanche deserticola were hydrocarbons and green leaf volatiles in squaring period. Some components were characteristic in buds and disappeared or decreased in flowers. The relative contents of some components gradually increased with the buds blooming. And some components only emerged in flowers of Cistanche deserticola. The higher content of esters and aromatics were found in flowers, which were significantly increased in comparison with the volatile compounds from buds. CONCLUSION: The volatile compounds from inflorescence of Cistanche deserticola were complex, consisting of various compositions and significantly different with buds blooming.

Peach volatile emission and attractiveness of different host plant volatiles blends to Cydia molesta in adjacent peach and pear orchards.

The oriental fruit moth (OFM), Cydia (= Grapholitha) molesta, is a highly damaging pest; peaches are its primary host, and pears serve as post-peach secondary hosts during the late season in China. We collected volatiles from detached peach shoots and fruits, and identified them with gas chromatography-mass spectrometry (GC-MS). Antennally active compounds were identified by gas chromatography-electroantennogram detection (GC-EAD), and these were further tested in the laboratory and field. We detected consistent electroantennographic activity was for ten compounds. Significantly more C. molesta females were caught with a mixture of female EAD-active compounds identified from the detached matured peach fruits (nonanal, butyl acetate, 3-methylbutyl acetate, hexyl acetate, (Z)-3-hexenyl acetate, linalool and farnesene) than other mixtures mimicking the volatile profile from detached matured fruits or shoots. We identified a new GC-EAD active mixture from intact peach shoots composed of nonanal, (Z)-3-hexenyl acetate, (E)-ß-ocimene, and 6-methyl-5-hepten-2-one. In the field test, the background odour of orchards could affect trap catches, and two peach-derived blends together with two previously known pear-derived blends were proven to be able to monitor the seasonal OFM population dispersal in adjacent orchards. These host plant blends will be effective for further designing candidate attractants for season-long C. molesta population dynamic monitoring.

Sample Preparation Method of Scanning and Transmission Electron Microscope for the Appendages of Woodboring Beetle.

This report described sample preparation methods that scanning and transmission electron microscope observations, demonstrated by preparing appendages of the woodboring beetle, Chlorophorus caragana Xie & Wang (2012), for both types of electron microscopy. The scanning electron microscopy (SEM) sample preparation protocol was based on sample chemical fixation, dehydration in a series of ethanol baths, drying, and sputter-coating. By adding Tween 20 (Polyoxyethylene sorbitan laurate) to the fixative and the wash solution, the insect body surface of woodboring beetle was washed more cleanly in SEM. This study's transmission electron microscopy (TEM) sample preparation involved a series of steps including fixation, ethanol dehydration, embedding in resin, positioning using fluorescence microscopy, sectioning, and staining. Fixative with Tween 20 enabled penetrate the insect body wall of woodboring beetle more easily than it would had been without Tween 20, and subsequently better fixed tissues and organs in the body, thus yielded clear transmission electron microscope observations of insect sensilla ultrastructures. The next step of this preparation was determining the positions of insect sensilla in the sample embedded in the resin block by using fluorescence microscopy to increase the precision of target sensilla positioning. This improved slicing accuracy.

Effect of Xuefu Zhuyu Capsule () on Angiogenesis in Hindlimb Ischemic Rats.

OBJECTIVE: To investigate the effect and mechanism of Xuefu Zhuyu Capsule (, XZC) on pro-angiogenesis in the hindlimb ischemic model rats. METHODS: A total of 100 Sprague Dawley rats were randomly divided into a model group, a regular-dose XZC group (0.48 g•kg-1•d-1) and a high-dose XZC group (0.96 g•kg-1•d-1) using random number table method. The model of hindlimb ischemic rats were made through femoral artery embolization with Bletilla microsphere agent. XZC were given on the first day after embolization surgery and lasted 5 days. Finally 72 models were obtained with 12 in each group for each time point. The lower ischemic limb was amputated on the third day after embolization surgery. Histopathological characters and the number of blood vessels of granulation tissues were observed at 36 and 48 h after amputation, respectively. The main genes were obtained from microarray analysis and were validated using real-time quantitative polymerase chain reaction. RESULTS: The vascular number of granulation tissues at both 36 and 48 h were characterized by new and fresh vessels. The number of angiogenesis in the high-dose XZC group at 36 and 48 h was greater compared with that in the regular-dose XZC and model groups (P<0.01), and high-dose XZC at 36 h increased more vessels than that at 48 h (P<0.01). Consequently, granulation tissues from the high-dose XZC group at 36 h were chosen for microarray analysis. In all, 2,085 differentially expressed genes (DEGs) were detected and 25 DEGs were determined to be directly related to angiogenesis. Four biological process terms were found including angiogenesis, regulation of angiogenesis, positive regulation of angiogenesis, and positive regulation of vascular endothelial growth factor receptor signaling pathway (P<0.05). Microarray analysis also showed 49 pathways including 11 pathways related to angiogenesis. CONCLUSION: XZC promoted angiogenesis moderately and the mechanism involved multiple DEGs and multiple pathways.

[Electrophysiological and behavioral responses of gall midge, Jaapiella sp. to volatiles of host plant Lycium barbarum]. / 枸杞红瘿蚊对寄主植物挥发物的电生理和行为反应.

Plant-derived volatiles are important for guiding herbivorous insects to their host plants. Jaapiella sp. (Diptera: Cecidomyiidae) is the most serious pest of Lycium barbarum. The young flower buds of L. barbarum are attractive to females of Jaapiella sp. for oviposition in the field. In this study, we compared response of Jaapiella sp. to volatiles from flower buds of L. barbarum at different stages, and clarified the crucial semiochemicals attracting Jaapiella sp. to lay eggs. Volatiles from young and mature flower buds were collected using SPME, and then identified and quantified by gas chromatography-mass spectrometry (GC-MS). Both electrophysiological and behavior experiments were conducted to measure the attraction of eight synthetic compounds to females and screen the crucial components based on gas chromatography-electroantennogram detection (GC-EAD) and Y-tube bioassays, respectively. Results showed that qualitative and quantitative diffe-rences between two odor profiles. Consistent electroantennographic response was observed for eight compounds from headspace collections, of which five synthetic compounds (3-carene, camphene, terpinolene, d-limonene, and (+)-pinene) were essential for significant preference or avoidance. Our results indicated that these compounds from L. barbarum flower buds could be effective candidates as oviposition attractant or repellents of Jaapiella sp., which would be helpful in the exploitation of new control agent to Jaapiella sp. in the field.