Three well-preserved fossil species ofParandrexis longicornis Lu, Shih & Ren sp. nov., P. agilis Lu, Shih & Ren sp. nov. and P. oblongis Lu, Shih & Ren sp. nov. are described and illustrated from the late Middle Ju...Three well-preserved fossil species ofParandrexis longicornis Lu, Shih & Ren sp. nov., P. agilis Lu, Shih & Ren sp. nov. and P. oblongis Lu, Shih & Ren sp. nov. are described and illustrated from the late Middle Jurassic Jiulongshan Formation of Daohugou in Inner Mongolia Autonomous Region, China. These new species are distinguished from other described species of Parandrexis by body size, head dimension (ratio of length to width), pronotum shape, and antennal characters. Based on new morphological data, we emend the generic diagnosis. These findings support the sexual size dimorphism of parandrexids and suggest a gymnosperm sap feeding habit by Parandrexis.展开更多
A strain isolated from the fruiting body of a fungus parasitized on Elaphomyces was identified as Cordyceps ophioglossoides based on the morphological characteristics and the analysis of ITS-5.8s rDNA sequence. The op...A strain isolated from the fruiting body of a fungus parasitized on Elaphomyces was identified as Cordyceps ophioglossoides based on the morphological characteristics and the analysis of ITS-5.8s rDNA sequence. The optimal medium, composition (g·L^-1), containing sucrose 66.0, yeast powder 10.0, silkworm chrysalises digest 30.0, MgSO4· 7H2O 0.4, and KH2PO4 0.4, Was found using fractional factorial design ancl a central composite design, and the optimization of cultural conditions obtained a result of seed age 6 days, inoculum size 6% (by volume), initial pH 5.6, temperature 24℃, shaking speed 160 ·'min^-1 by one-factor-at-a-time method. The maximum biomass reached about 20.2 g·L^-1 after 90 hours culture under the optimal conditions. Elementary nharmaeclogical actlwtties showed that mycelia of C. ophioglossoides L2 from submerged culture promoted Uterus growth in estrogen- depleted mice. In the 15-litre scale-up fermentation, the mycelial biomass was around 19.1 g·L^-1, indicating a promising prospect for this biotechnoloagy and the potency to develoo its medical value.展开更多
As the most widely used plasticizers in the world, phthalate esters (PAEs) are potential endocrine disruption compounds (EDCs). In the present study, the toxicity of dimethyl phthalate (DMP), diethyl phthalate ...As the most widely used plasticizers in the world, phthalate esters (PAEs) are potential endocrine disruption compounds (EDCs). In the present study, the toxicity of dimethyl phthalate (DMP), diethyl phthalate (DEP), dibutyl phthalate (DBP), di (2-ethylhexyl) phthalate (DEHP) on embryogenesis and larvae development of the marine univalve Haliotis diversicolor supertexta was examined in laboratory. The results show that the malformation of embryos appeared during the experiment, such as embryos died or lysed, small transparent flocculent rings studded on the periphery of the embryo, and the larvae could failed to hatch. In embryo toxic test, embryos incubated at the highest concentration of DMR DEP and DBP solutions showed significantly high abnormal rate compared with the control, while DEHP solutions displayed no significant difference. In larval toxic test, in all concentrations of DMP, DEP and DBP solutions, larval settlement rates were low significantly than that of the control. Similarly, DEHP solutions show nearly no effect on the larval settlement. The order of toxicity on embryos and larvae is DBP〉DEP〉DMP〉DEHE Being a simple and easy stimulation to indoor spawn, sensitive to environmental factors, and short culture time, the embryos of H. diversicolor supertexta can be used to indicate toxicity of the PAEs.展开更多
A quantitative structure–activity relationship(QSAR) was performed to analyze antimalarial activities against the D10 strains of Plasmodium falciparum of triazole-linked chalcone and dienone hybrid derivatives using ...A quantitative structure–activity relationship(QSAR) was performed to analyze antimalarial activities against the D10 strains of Plasmodium falciparum of triazole-linked chalcone and dienone hybrid derivatives using partial least squares regression coupled with stepwise forward–backward variable selection method. QSAR analyses were performed on the available IC50 D10 strains of Plasmodium falciparum data based on theoretical molecular descriptors. The QSAR model developed gave good predictive correlation coefficient(r2) of 0.8994, significant cross validated correlation coefficient(q2) of 0.7689, r2 for external test set)(2predr of 0.8256, coefficient of correlation of predicted data set)(2sepred,r of 0.3276. The model shows that antimalarial activity is greatly affected by donor and electron-withdrawing substituents. The study implicates that chalcone and dienone rings should have strong donor and electron-withdrawing substituents as they increase the activity of chalcone. Results show that the predictive ability of the model is satisfactory, and it can be used for designing similar group of antimalarial compounds. The findings derived from this analysis along with other molecular modeling studies will be helpful in designing of the new potent antimalarial activity of clinical utility.展开更多
A neutral metalloprotease was purified from the cultured mycelia of Laccocephalum mylittae,an effective medicinal fungus widely used in anthelmintic therapy.The protease was purified to homogeneity with 31.85-fold pur...A neutral metalloprotease was purified from the cultured mycelia of Laccocephalum mylittae,an effective medicinal fungus widely used in anthelmintic therapy.The protease was purified to homogeneity with 31.85-fold purification and a final yield of 21.76%.The subunit molecular weight of the protease is about 40000 estimated by sodium dodecyl sulfate polyacrylamide gel electrophoresis(SDS-PAGE).The optimum reaction pH and temperature are 7.5 and 50oC,respectively.The protease activity is largely enhanced by Ca2 +,but highly inhibited by tetrasodium ethylenediaminetetraacetate(EDTA),a metal-chelator,suggesting that the enzyme is a metalloprotease.The Michaelis-Menten constan Km and Vmax value for casein substrate are 6.09 mg·ml -1and 21.32μg·min -1·ml -1, respectively.In vitro anthelmintic tests of the protease exhibit distinct lethal effects on the third stage larvae(L3)of Ascaris suum.Scanning electron microscopy and SDS-PAGE analysis indicates that the proteolysis of larvae proteins caused by this protease may relate to the anthelmintic activity of L.mylittae.展开更多
[Objective] The aim was to study characters of pollen grains of tetraploid lines and diploid control line of Chrysanthemum cinerariifolium (Trev.) Vis.,morphological characters,fertility of pollen grain and germinatio...[Objective] The aim was to study characters of pollen grains of tetraploid lines and diploid control line of Chrysanthemum cinerariifolium (Trev.) Vis.,morphological characters,fertility of pollen grain and germination percentage of seeds. [Method] Pollen grains were prepared by sulphuric acid-acetyl oxide decomposition method. The lengths of polar axis and equatorial axis of pollen grains were determined with general optical microscope. The morphology of pollen grains was observed with SEM (scanning electron microscope) and the typical visual fields of 2 500× (or 2 000×),7 000× were taken pictures. [Result] Comparing with the diploid control line,the pollen grains of five tetraploid lines which were tested were different from the diploid line in morphology,sculpture,etc.. 4 of the 5 tested samples were significant larger than the diploid line in size and one was similar to the diploid line. [Conclusion] This research provided references for breeding tetraploid improved varieties of Chrysanthemum cinerariifolium (Trev.) Vis. with good fertility and high germination percentage.展开更多
Artificially induced tetraploid Pacific oyster, Crassostrea gigas Thunberg, produces more aneuploid gametes than nor- mal diploid one, although they showed a comparable fecundity to diploidy. The meiotic chromosome co...Artificially induced tetraploid Pacific oyster, Crassostrea gigas Thunberg, produces more aneuploid gametes than nor- mal diploid one, although they showed a comparable fecundity to diploidy. The meiotic chromosome configuration of 3 tetraploid and 1 tetraploid/triploid mosaic males were analyzed through direct chromosome observation. A majority of metaphase I spermato- cytes contained both bivalents and quadrivalents. The chromosome configuration of these males was characterized by preferential formation of bivalents to quadrivalents. Bivalents appeared in all spermatocytes and consisted of 86% of all chromosome aggregates. In comparison, quadrivalents occurred in 91% spermatocytes and consisted of only 12.6% of all chromosome aggregates. The mean bivalent frequency per spermatocyte varied between 14.4 and 17.2; while that of quadrivalents varied between 2.2 and 2.7. Most quadrivalents were tandemly chained (58%) or circled (39%). The total number of chromosome aggregates per spermatocyte ranged from 13 to 20 with an average of 17.6; while 18 (16 bivalents and 2 quadrivalents) was the most frequent. Univalents and trivalents appeared in very low frequency. Aneuploid (hypotetraploid) spermatocytes were observed in a low frequency. The chromosome con- figuration of in the mosaic individual was similar to that of tetraploid individuals. The percentage of triploid spermatocytes (2%) of the mosaic individual was significantly lower (2"2 =30, P〈 0.01) than that of triploid cells (46%) in its somatic tissue.展开更多
Nutrition management is the most important for high yield production but it may affect the response of rice plants to pest and diseases due to the change of microclimate under rice plant canopy. The knowledge of nutri...Nutrition management is the most important for high yield production but it may affect the response of rice plants to pest and diseases due to the change of microclimate under rice plant canopy. The knowledge of nutrition management and its relation with pest and diseases are basis for setting up a high yield production system. Most of the pest and disease control procedures used by farmers can be considered as soil fertility management and these nutrition practices can have impact on the physiological susceptibility of crop plants to pest and diseases by affecting the plant resistance. Silicon content of plants is particularly effective against pest and diseases in rice and certain rice genotypes are more efficient accumulators of silicon, thus making them more resistant. In the absence of natural heritable resistance in rice varieties, resistance could be induced by altemate strategies to suppress certain pest and pathogens. Hence experiments were carried out in two stages during kharif 2010 and 2011 to assess the concentration of silicon in the index leaves of rice plant utilizing 133 varieties in four locations. The silica content of promising varieties ranged from 1.50% to 3.20%, 1.60% to 3.15%, 1.49% to 3.20% and 1.55% to 3.06% with a mean values of 2.50%, 2.48%, 2.51% and 2.43% at Jagtial, Warangal, Rajendranagar and Rudrur centres of Telangana region and not much variation in mean silica content in index leaves at different places. The overall yield from four locations ranged from 2,653 kg/ha to 6,860 kg/ha with a mean of 5,624 kg/ha. The yields recorded at Jagtial, Warangal, Rajendranagar and Rudrur centres ranged from 2,886 to 7,198, 2,653 to 6,831, 2,653 to 6,860 and 4,399 to 5,950 kg/ha, respectively. The lowest mean yield 5,069 kg/ha was noticed at Rudrur and the highest yield 5,940 kg/ha was found at Warangal. The variations in yields might be due to genotypic variations and also due to variations in climatic conditions of different locations.展开更多
In order to reconstruct the paleoproductivity evolution history of the West Philippine Sea during the last 700 ka, the vertical gradient of Δδ13C in dissolved inorganic carbon Δδ13C between those of foraminifera P...In order to reconstruct the paleoproductivity evolution history of the West Philippine Sea during the last 700 ka, the vertical gradient of Δδ13C in dissolved inorganic carbon Δδ13C between those of foraminifera Pulleniatina obliquiloculata and Cibicidoides wuellerstorfi) and planktonic foraminiferal assemblages were analysed in piston Core MD06-3047 retrieved from the Benham Rise (east of the Luzon Island). Paleoproductivity evolution in the West Philippine Sea during the last 700 ka is closely related to glacial-interglacial cycles and precession-controlled insolation. Controlling factors ofpaleoproductivity could have been both thermocline fluctuations related with ENSO-Iike processes and eolian input associated with East Asian winter monsoon, and the former could have been the primary factor. A higher productivity and a shallower thermocline coeval with the occurrence of low CO2 concentrations in the EPICA Dome C ice core might indicate that biological export production in the low-latitude could act as a significant sink in the global carbon cycle, and modify atmospheric CO2 concentrations. Spectral analysis further reveals that the paleoproductivity is mainly controlled by thermocline fluctuations subjected to ENSO processes responding to processional variability of insolation. High coherences in eccentricity, obliquity and precession periods fiuther revealing the close link between thermocline fluctuations, paleoproductivity and atmospheric CO2 levels.展开更多
The effeclt of condensed tannins from Leucaena leucocephala (Lam.) and sodium lauryl sulfate (SLS) addition to basal diets of corn silage on nematode eggs and protozoa interaction in the rumen within Thai native x...The effeclt of condensed tannins from Leucaena leucocephala (Lam.) and sodium lauryl sulfate (SLS) addition to basal diets of corn silage on nematode eggs and protozoa interaction in the rumen within Thai native x Anglo-Nubian male goats was studied. Goats (n = 24 male; BW = 30 + 2) were randomly considered toward treatment position into randomized complete block design (RCBD). The treatments were: 1) Basal (B; 1.0-1.2 kg/head/day, corn silage), 2) B + SLS 8 g/head/day) 3) B + 40g Leucaena/head/day (1.0% condensed tannins), and 4) B + 40g Leucaena/head/day (1.0% condensed tannins) with SLS 4 g/head/day). These studies indicate that the action of 1.0% condensed tannins by Leucaena with 8 g SLS has the effect of increasing C3 (P 〈 0.05). The opposite effect was observed for C2 which decreased (P 〈 0.05). Both intestinal nematode eggs and protozoa in the rumen were reduced highly significantly (P 〈 0.01). Bacteria population was raised (P 〈 0.01). Nevertheless, all of these treatments did not affect intake, productive performances and blood urea nitrogen.展开更多
A light and temperature dual responsive copolymer,poly(7-(4-vinylbenzy-loxyl)-4-methylcoumarin-co-N vinyl caprolactam-co-tri(ethylene glycol)methyl ether methacrylate)(PVNM),was grafted on the surface of dopamine base...A light and temperature dual responsive copolymer,poly(7-(4-vinylbenzy-loxyl)-4-methylcoumarin-co-N vinyl caprolactam-co-tri(ethylene glycol)methyl ether methacrylate)(PVNM),was grafted on the surface of dopamine based mesoporous silica nanoparticles(MSNs).The resulting polymer brush,MSNs-g-PVNM,was characterized by FT-IR,TEM,TGA and XPS.The dual responsive behaviors of MSNs-g-PVNM were systematically studied.With imidacloprid as the model guest pesticide,the loading percentage and loading efficiency of the polymer brush were determined as 9.2%and 40.6%,respectively.The release efficiency of imidacloprid in MSNs-g-PVNM was the lowest value of 5.4%at 20℃ and 365 nm,and it reached the highest value of 52.4%at 50℃ and 254 nm.The loss percentage of imidacloprid on the leaves contained imidacloprid-loaded MSNs-g-PVNM(8.4%)was much less than that contained only imidacloprid(25.2%)after three rinses.It was confirmed that the release process of imidacloprid was well regulated through changing external conditions such as light and temperature.展开更多
Objective Sulfanilamide,sulfadiazine,and dapsone were the first sulfonamides to be used to treat malaria by disrupting the folate biosynthesis process,which is essential for parasite survival.Therefore,we aimed to syn...Objective Sulfanilamide,sulfadiazine,and dapsone were the first sulfonamides to be used to treat malaria by disrupting the folate biosynthesis process,which is essential for parasite survival.Therefore,we aimed to synthesize novel N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives through a rational drug design approach.Methods All compounds were synthesized by the conventional method,and the products were characterized by spectral analysis(1 H NMR and mass spectrometry).The progression of the reaction was monitored using thin-layer chromatography(TLC).All the derivatives were analyzed for their effective binding mode in the allosteric site of the plasmodium cysteine protease falcipain-2.Antibacterial and antifungal activities were determined using the broth dilution method.Results S6(N-(2-thiazol-4 yl)-acetyl-aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S9(N-(1 H-benzo[d]imidazol-2-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed five hydrogen bonds;S8(N-(2-1 H-imidazol-2 yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S10(N-(1 H-benzo[d]imidazol-5-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed four hydrogen bonds with the allosteric site of the enzyme.Considering the docking scores and formation of hydrogen bonds with the target enzyme,the novel derivatives were processed for wet lab synthesis.All the newly synthesized derivatives were subjected to in vitro antimalarial,antifungal,and antibacterial activities.All the derivatives exhibited sufficient sensitivity to the Plasmodium falciparum strain compared to the standards.Moreover,compounds S9 and S10 showed the most potent dual antimicrobial and antimalarial activities.They also exhibited powerful molecular interactions in molecular docking studies.Conclusion Based on the above results,it was concluded that N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives have excellent biological potential to act as antimalarial,antifungal,and antibacterial agents.展开更多
Trumpet shell, Charonia sauliae, is an endangered and valuable species, but its artificial propagation protocol has not been successfully established. To estimate the possibility of cryopreservation for larvae of C. s...Trumpet shell, Charonia sauliae, is an endangered and valuable species, but its artificial propagation protocol has not been successfully established. To estimate the possibility of cryopreservation for larvae of C. sauliae, which is a potential preparation for its artificial reproduction and further research, in this study a protocoi for the cryopreservation of veliger larvae of trumpet shell was optimized. Through a two-step cryopreservation procedure, four kinds of cryoprotectants (ethylene glycol, 1, 2-propanediol, dimethyl sulfoxide and glycerol) were employed at three concentrations (1.0, 1.5 and 2.0molL^-1) respectively and survival rates of larvae were determined after a storage of lh. The larvae frozen with these four cryoprotectants after 1 h storage were cultured, and then survival rates were determined at 24, 72 and 120 h after thawing. Dimethyl sulfoxide at a concentration of 1.5 molL^-1 showed the best protective effect in all experiments (p〈0.05). And survival rates of larvae frozen with dimethyl sulfoxide were determined after 1, 7 and 15 d of storage. The survival rates of larvae frozen with 1.5 molL^-1 dimethyl sulfoxide after 1 h, 1 d, 7 d and 15 d of storage were 80.77% ±7.51%, 80.34%±11.28%, 83.10%±9.14% and 77.23%±6.22% respectively. No significant differences in survival rates of larvae frozen with dimethyl sulfoxide were observed after various storage periods (p〉0.05).展开更多
Transfer functions between the benthic foraminiferal fauna of seventy-one sediment surface-samples retrieved from the South Yellow Sea inner shelf and the environmental factors, including the summer bottom-water salin...Transfer functions between the benthic foraminiferal fauna of seventy-one sediment surface-samples retrieved from the South Yellow Sea inner shelf and the environmental factors, including the summer bottom-water salinity(Ss), the summer bottom-water temperature(Ts) and the winter bottom-water temperature(Tw) have been developed utilizing weighted averaging partial least square regression(WA-PLS). Subsequently, the transfer functions have been applied to a late Holocene piston core SY01 from the South Yellow Sea inner shelf, established the variation curves of the Ss, Ts, and Tw during the last 3.9 cal. ka. The Ss and Ts showed a nearly synchronous trend to the published stalagmite δ18O curve from the Jiuxian Cave, meaning they could be used as reliable indicators for the summer monsoon. Similarly, the Tw could be used as an indicator for the winter monsoon for its synchronous change to the insensitive grain size variation of the core ZY-2 retrieved from the Central Yellow Sea mud area. These results suggest that transfer functions based on benthic foraminiferal fauna can be a potentially useful tool in palaeoceanographic and palaeoenvironmental research along the Chinese seaboard.展开更多
To search for novel 2-arylpyrroles with unique biological activities,a series of novel 2-arylpyrrole derivatives were designed and synthesized,and their structures were characterized by 1 H and 13 C NMR spectroscopy,M...To search for novel 2-arylpyrroles with unique biological activities,a series of novel 2-arylpyrrole derivatives were designed and synthesized,and their structures were characterized by 1 H and 13 C NMR spectroscopy,MS spectrometry,and elemental analysis.Their insecticidal activities against Lepidopteran pests (e.g.Mythimna separata) and acaricidal activities against mites (e.g.Tetranychus urticae) were evaluated.The results of bioassays indicate that some of these title compounds exhibited excellent insecticidal and acaricidal activities.For example,4-bromo-1-((chloromethoxy)methyl)-2-(4-chloro phenyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile (6a),4-bromo-2-(4-chlorophenyl)-1-((2-fluoroethoxy)-methyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile (6d) showed insecticidal activity against Mythimna separata and 4-bromo-2-(4-chlorophenyl)1-((isopropoxymethoxy)methyl)-5-(trifluoro methyl)pyrrole-3-carbonitrile (7d) showed acaricidal activity against Tetranychus urticae.They were more effective than Chlorfenapyr,which has been the only commercialized member of a new class of chemicals of 2-arylpyrroles.展开更多
基金supported by the National Basic Research Program of China (973 Program) (2012CB821906)the National Natural Science Foundation of China (31230065,41272006)+1 种基金Great Wall Scholar and KEY project of the Beijing Municipal Commission of Education (KZ201310028033)Program for Changjiang Scholars and Innovative Research Team in University (IRT13081)
文摘Three well-preserved fossil species ofParandrexis longicornis Lu, Shih & Ren sp. nov., P. agilis Lu, Shih & Ren sp. nov. and P. oblongis Lu, Shih & Ren sp. nov. are described and illustrated from the late Middle Jurassic Jiulongshan Formation of Daohugou in Inner Mongolia Autonomous Region, China. These new species are distinguished from other described species of Parandrexis by body size, head dimension (ratio of length to width), pronotum shape, and antennal characters. Based on new morphological data, we emend the generic diagnosis. These findings support the sexual size dimorphism of parandrexids and suggest a gymnosperm sap feeding habit by Parandrexis.
基金Supported by the Research Project of Science and Technology of Zhejiang Province, China (2005C23027), the National High Technology Research and Development Program of China (2007AA021506) and the Natural Science Foundation of Zhejiang Province (R207609). We would like to thank Dr. Birnie from New Zealand for his editing of this manuscript.
文摘A strain isolated from the fruiting body of a fungus parasitized on Elaphomyces was identified as Cordyceps ophioglossoides based on the morphological characteristics and the analysis of ITS-5.8s rDNA sequence. The optimal medium, composition (g·L^-1), containing sucrose 66.0, yeast powder 10.0, silkworm chrysalises digest 30.0, MgSO4· 7H2O 0.4, and KH2PO4 0.4, Was found using fractional factorial design ancl a central composite design, and the optimization of cultural conditions obtained a result of seed age 6 days, inoculum size 6% (by volume), initial pH 5.6, temperature 24℃, shaking speed 160 ·'min^-1 by one-factor-at-a-time method. The maximum biomass reached about 20.2 g·L^-1 after 90 hours culture under the optimal conditions. Elementary nharmaeclogical actlwtties showed that mycelia of C. ophioglossoides L2 from submerged culture promoted Uterus growth in estrogen- depleted mice. In the 15-litre scale-up fermentation, the mycelial biomass was around 19.1 g·L^-1, indicating a promising prospect for this biotechnoloagy and the potency to develoo its medical value.
基金Supported by National Natural Science Foundation of China (No. 40476057)
文摘As the most widely used plasticizers in the world, phthalate esters (PAEs) are potential endocrine disruption compounds (EDCs). In the present study, the toxicity of dimethyl phthalate (DMP), diethyl phthalate (DEP), dibutyl phthalate (DBP), di (2-ethylhexyl) phthalate (DEHP) on embryogenesis and larvae development of the marine univalve Haliotis diversicolor supertexta was examined in laboratory. The results show that the malformation of embryos appeared during the experiment, such as embryos died or lysed, small transparent flocculent rings studded on the periphery of the embryo, and the larvae could failed to hatch. In embryo toxic test, embryos incubated at the highest concentration of DMR DEP and DBP solutions showed significantly high abnormal rate compared with the control, while DEHP solutions displayed no significant difference. In larval toxic test, in all concentrations of DMP, DEP and DBP solutions, larval settlement rates were low significantly than that of the control. Similarly, DEHP solutions show nearly no effect on the larval settlement. The order of toxicity on embryos and larvae is DBP〉DEP〉DMP〉DEHE Being a simple and easy stimulation to indoor spawn, sensitive to environmental factors, and short culture time, the embryos of H. diversicolor supertexta can be used to indicate toxicity of the PAEs.
文摘A quantitative structure–activity relationship(QSAR) was performed to analyze antimalarial activities against the D10 strains of Plasmodium falciparum of triazole-linked chalcone and dienone hybrid derivatives using partial least squares regression coupled with stepwise forward–backward variable selection method. QSAR analyses were performed on the available IC50 D10 strains of Plasmodium falciparum data based on theoretical molecular descriptors. The QSAR model developed gave good predictive correlation coefficient(r2) of 0.8994, significant cross validated correlation coefficient(q2) of 0.7689, r2 for external test set)(2predr of 0.8256, coefficient of correlation of predicted data set)(2sepred,r of 0.3276. The model shows that antimalarial activity is greatly affected by donor and electron-withdrawing substituents. The study implicates that chalcone and dienone rings should have strong donor and electron-withdrawing substituents as they increase the activity of chalcone. Results show that the predictive ability of the model is satisfactory, and it can be used for designing similar group of antimalarial compounds. The findings derived from this analysis along with other molecular modeling studies will be helpful in designing of the new potent antimalarial activity of clinical utility.
基金Supported by the National High Technology Research and Development Program of China(2007AA021506) the Natural Science Foundation of Zhejiang Province(R207609)
文摘A neutral metalloprotease was purified from the cultured mycelia of Laccocephalum mylittae,an effective medicinal fungus widely used in anthelmintic therapy.The protease was purified to homogeneity with 31.85-fold purification and a final yield of 21.76%.The subunit molecular weight of the protease is about 40000 estimated by sodium dodecyl sulfate polyacrylamide gel electrophoresis(SDS-PAGE).The optimum reaction pH and temperature are 7.5 and 50oC,respectively.The protease activity is largely enhanced by Ca2 +,but highly inhibited by tetrasodium ethylenediaminetetraacetate(EDTA),a metal-chelator,suggesting that the enzyme is a metalloprotease.The Michaelis-Menten constan Km and Vmax value for casein substrate are 6.09 mg·ml -1and 21.32μg·min -1·ml -1, respectively.In vitro anthelmintic tests of the protease exhibit distinct lethal effects on the third stage larvae(L3)of Ascaris suum.Scanning electron microscopy and SDS-PAGE analysis indicates that the proteolysis of larvae proteins caused by this protease may relate to the anthelmintic activity of L.mylittae.
基金Supported by the Fundamental Research Funds for the Central Universities (SWJTU09BR221)~~
文摘[Objective] The aim was to study characters of pollen grains of tetraploid lines and diploid control line of Chrysanthemum cinerariifolium (Trev.) Vis.,morphological characters,fertility of pollen grain and germination percentage of seeds. [Method] Pollen grains were prepared by sulphuric acid-acetyl oxide decomposition method. The lengths of polar axis and equatorial axis of pollen grains were determined with general optical microscope. The morphology of pollen grains was observed with SEM (scanning electron microscope) and the typical visual fields of 2 500× (or 2 000×),7 000× were taken pictures. [Result] Comparing with the diploid control line,the pollen grains of five tetraploid lines which were tested were different from the diploid line in morphology,sculpture,etc.. 4 of the 5 tested samples were significant larger than the diploid line in size and one was similar to the diploid line. [Conclusion] This research provided references for breeding tetraploid improved varieties of Chrysanthemum cinerariifolium (Trev.) Vis. with good fertility and high germination percentage.
文摘Artificially induced tetraploid Pacific oyster, Crassostrea gigas Thunberg, produces more aneuploid gametes than nor- mal diploid one, although they showed a comparable fecundity to diploidy. The meiotic chromosome configuration of 3 tetraploid and 1 tetraploid/triploid mosaic males were analyzed through direct chromosome observation. A majority of metaphase I spermato- cytes contained both bivalents and quadrivalents. The chromosome configuration of these males was characterized by preferential formation of bivalents to quadrivalents. Bivalents appeared in all spermatocytes and consisted of 86% of all chromosome aggregates. In comparison, quadrivalents occurred in 91% spermatocytes and consisted of only 12.6% of all chromosome aggregates. The mean bivalent frequency per spermatocyte varied between 14.4 and 17.2; while that of quadrivalents varied between 2.2 and 2.7. Most quadrivalents were tandemly chained (58%) or circled (39%). The total number of chromosome aggregates per spermatocyte ranged from 13 to 20 with an average of 17.6; while 18 (16 bivalents and 2 quadrivalents) was the most frequent. Univalents and trivalents appeared in very low frequency. Aneuploid (hypotetraploid) spermatocytes were observed in a low frequency. The chromosome con- figuration of in the mosaic individual was similar to that of tetraploid individuals. The percentage of triploid spermatocytes (2%) of the mosaic individual was significantly lower (2"2 =30, P〈 0.01) than that of triploid cells (46%) in its somatic tissue.
文摘Nutrition management is the most important for high yield production but it may affect the response of rice plants to pest and diseases due to the change of microclimate under rice plant canopy. The knowledge of nutrition management and its relation with pest and diseases are basis for setting up a high yield production system. Most of the pest and disease control procedures used by farmers can be considered as soil fertility management and these nutrition practices can have impact on the physiological susceptibility of crop plants to pest and diseases by affecting the plant resistance. Silicon content of plants is particularly effective against pest and diseases in rice and certain rice genotypes are more efficient accumulators of silicon, thus making them more resistant. In the absence of natural heritable resistance in rice varieties, resistance could be induced by altemate strategies to suppress certain pest and pathogens. Hence experiments were carried out in two stages during kharif 2010 and 2011 to assess the concentration of silicon in the index leaves of rice plant utilizing 133 varieties in four locations. The silica content of promising varieties ranged from 1.50% to 3.20%, 1.60% to 3.15%, 1.49% to 3.20% and 1.55% to 3.06% with a mean values of 2.50%, 2.48%, 2.51% and 2.43% at Jagtial, Warangal, Rajendranagar and Rudrur centres of Telangana region and not much variation in mean silica content in index leaves at different places. The overall yield from four locations ranged from 2,653 kg/ha to 6,860 kg/ha with a mean of 5,624 kg/ha. The yields recorded at Jagtial, Warangal, Rajendranagar and Rudrur centres ranged from 2,886 to 7,198, 2,653 to 6,831, 2,653 to 6,860 and 4,399 to 5,950 kg/ha, respectively. The lowest mean yield 5,069 kg/ha was noticed at Rudrur and the highest yield 5,940 kg/ha was found at Warangal. The variations in yields might be due to genotypic variations and also due to variations in climatic conditions of different locations.
基金Supported by the National Natural Science Foundation of China(Nos.41230959,41076030,40906038,41106042,41006032)the Pilot Project of the Knowledge Innovation Program of Chinese Academy of Sciences(No.KZCX2-YW-221)the Foundation of Key Laboratory of Marine Geology and Environment of Chinese Academy of Sciences(No.MGE2011KG01)
文摘In order to reconstruct the paleoproductivity evolution history of the West Philippine Sea during the last 700 ka, the vertical gradient of Δδ13C in dissolved inorganic carbon Δδ13C between those of foraminifera Pulleniatina obliquiloculata and Cibicidoides wuellerstorfi) and planktonic foraminiferal assemblages were analysed in piston Core MD06-3047 retrieved from the Benham Rise (east of the Luzon Island). Paleoproductivity evolution in the West Philippine Sea during the last 700 ka is closely related to glacial-interglacial cycles and precession-controlled insolation. Controlling factors ofpaleoproductivity could have been both thermocline fluctuations related with ENSO-Iike processes and eolian input associated with East Asian winter monsoon, and the former could have been the primary factor. A higher productivity and a shallower thermocline coeval with the occurrence of low CO2 concentrations in the EPICA Dome C ice core might indicate that biological export production in the low-latitude could act as a significant sink in the global carbon cycle, and modify atmospheric CO2 concentrations. Spectral analysis further reveals that the paleoproductivity is mainly controlled by thermocline fluctuations subjected to ENSO processes responding to processional variability of insolation. High coherences in eccentricity, obliquity and precession periods fiuther revealing the close link between thermocline fluctuations, paleoproductivity and atmospheric CO2 levels.
文摘The effeclt of condensed tannins from Leucaena leucocephala (Lam.) and sodium lauryl sulfate (SLS) addition to basal diets of corn silage on nematode eggs and protozoa interaction in the rumen within Thai native x Anglo-Nubian male goats was studied. Goats (n = 24 male; BW = 30 + 2) were randomly considered toward treatment position into randomized complete block design (RCBD). The treatments were: 1) Basal (B; 1.0-1.2 kg/head/day, corn silage), 2) B + SLS 8 g/head/day) 3) B + 40g Leucaena/head/day (1.0% condensed tannins), and 4) B + 40g Leucaena/head/day (1.0% condensed tannins) with SLS 4 g/head/day). These studies indicate that the action of 1.0% condensed tannins by Leucaena with 8 g SLS has the effect of increasing C3 (P 〈 0.05). The opposite effect was observed for C2 which decreased (P 〈 0.05). Both intestinal nematode eggs and protozoa in the rumen were reduced highly significantly (P 〈 0.01). Bacteria population was raised (P 〈 0.01). Nevertheless, all of these treatments did not affect intake, productive performances and blood urea nitrogen.
基金Project(21376271)supported by the National Natural Science Foundation of ChinaProject(2016TP1007)supported by the Hunan Provincial Science and Technology Plan Project,ChinaProjects(201810533078,S2020105330395)supported by the Undergraduates Innovative Training Foundation of Central South University,China。
文摘A light and temperature dual responsive copolymer,poly(7-(4-vinylbenzy-loxyl)-4-methylcoumarin-co-N vinyl caprolactam-co-tri(ethylene glycol)methyl ether methacrylate)(PVNM),was grafted on the surface of dopamine based mesoporous silica nanoparticles(MSNs).The resulting polymer brush,MSNs-g-PVNM,was characterized by FT-IR,TEM,TGA and XPS.The dual responsive behaviors of MSNs-g-PVNM were systematically studied.With imidacloprid as the model guest pesticide,the loading percentage and loading efficiency of the polymer brush were determined as 9.2%and 40.6%,respectively.The release efficiency of imidacloprid in MSNs-g-PVNM was the lowest value of 5.4%at 20℃ and 365 nm,and it reached the highest value of 52.4%at 50℃ and 254 nm.The loss percentage of imidacloprid on the leaves contained imidacloprid-loaded MSNs-g-PVNM(8.4%)was much less than that contained only imidacloprid(25.2%)after three rinses.It was confirmed that the release process of imidacloprid was well regulated through changing external conditions such as light and temperature.
基金funding support from the National Natural Science Foundation of China(No.82074251)the Hunan Natural Science Foundation of China(No.2018JJ2413)the Hunan Provincial Health and Health Commission Project(No.c2018032)。
文摘Objective Sulfanilamide,sulfadiazine,and dapsone were the first sulfonamides to be used to treat malaria by disrupting the folate biosynthesis process,which is essential for parasite survival.Therefore,we aimed to synthesize novel N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives through a rational drug design approach.Methods All compounds were synthesized by the conventional method,and the products were characterized by spectral analysis(1 H NMR and mass spectrometry).The progression of the reaction was monitored using thin-layer chromatography(TLC).All the derivatives were analyzed for their effective binding mode in the allosteric site of the plasmodium cysteine protease falcipain-2.Antibacterial and antifungal activities were determined using the broth dilution method.Results S6(N-(2-thiazol-4 yl)-acetyl-aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S9(N-(1 H-benzo[d]imidazol-2-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed five hydrogen bonds;S8(N-(2-1 H-imidazol-2 yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide and S10(N-(1 H-benzo[d]imidazol-5-yl)aminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide formed four hydrogen bonds with the allosteric site of the enzyme.Considering the docking scores and formation of hydrogen bonds with the target enzyme,the novel derivatives were processed for wet lab synthesis.All the newly synthesized derivatives were subjected to in vitro antimalarial,antifungal,and antibacterial activities.All the derivatives exhibited sufficient sensitivity to the Plasmodium falciparum strain compared to the standards.Moreover,compounds S9 and S10 showed the most potent dual antimicrobial and antimalarial activities.They also exhibited powerful molecular interactions in molecular docking studies.Conclusion Based on the above results,it was concluded that N-(2-arylaminophenyl)-2,3-diphenylquinoxaline-6-sulfonamide derivatives have excellent biological potential to act as antimalarial,antifungal,and antibacterial agents.
文摘Trumpet shell, Charonia sauliae, is an endangered and valuable species, but its artificial propagation protocol has not been successfully established. To estimate the possibility of cryopreservation for larvae of C. sauliae, which is a potential preparation for its artificial reproduction and further research, in this study a protocoi for the cryopreservation of veliger larvae of trumpet shell was optimized. Through a two-step cryopreservation procedure, four kinds of cryoprotectants (ethylene glycol, 1, 2-propanediol, dimethyl sulfoxide and glycerol) were employed at three concentrations (1.0, 1.5 and 2.0molL^-1) respectively and survival rates of larvae were determined after a storage of lh. The larvae frozen with these four cryoprotectants after 1 h storage were cultured, and then survival rates were determined at 24, 72 and 120 h after thawing. Dimethyl sulfoxide at a concentration of 1.5 molL^-1 showed the best protective effect in all experiments (p〈0.05). And survival rates of larvae frozen with dimethyl sulfoxide were determined after 1, 7 and 15 d of storage. The survival rates of larvae frozen with 1.5 molL^-1 dimethyl sulfoxide after 1 h, 1 d, 7 d and 15 d of storage were 80.77% ±7.51%, 80.34%±11.28%, 83.10%±9.14% and 77.23%±6.22% respectively. No significant differences in survival rates of larvae frozen with dimethyl sulfoxide were observed after various storage periods (p〉0.05).
基金supported by the National Natural Science Foundation of China(Grant Nos.41006021,41176132)the Western Pacific Ocean System Project(Grant No.XDA11030104)
文摘Transfer functions between the benthic foraminiferal fauna of seventy-one sediment surface-samples retrieved from the South Yellow Sea inner shelf and the environmental factors, including the summer bottom-water salinity(Ss), the summer bottom-water temperature(Ts) and the winter bottom-water temperature(Tw) have been developed utilizing weighted averaging partial least square regression(WA-PLS). Subsequently, the transfer functions have been applied to a late Holocene piston core SY01 from the South Yellow Sea inner shelf, established the variation curves of the Ss, Ts, and Tw during the last 3.9 cal. ka. The Ss and Ts showed a nearly synchronous trend to the published stalagmite δ18O curve from the Jiuxian Cave, meaning they could be used as reliable indicators for the summer monsoon. Similarly, the Tw could be used as an indicator for the winter monsoon for its synchronous change to the insensitive grain size variation of the core ZY-2 retrieved from the Central Yellow Sea mud area. These results suggest that transfer functions based on benthic foraminiferal fauna can be a potentially useful tool in palaeoceanographic and palaeoenvironmental research along the Chinese seaboard.
基金supported by the National Basic Research Program of China(973 Program,2010CB126104)National Twelfth-five Key Project of China(2011BAE06B01-03)+2 种基金National Natural Science Foundation of China(21272062)the Hunan Provincial Natural Science Foundation (11JJ2006,11JJ3022 and 10JJ3053)Science Plan of Hunan Province (2010FJ2003)
文摘To search for novel 2-arylpyrroles with unique biological activities,a series of novel 2-arylpyrrole derivatives were designed and synthesized,and their structures were characterized by 1 H and 13 C NMR spectroscopy,MS spectrometry,and elemental analysis.Their insecticidal activities against Lepidopteran pests (e.g.Mythimna separata) and acaricidal activities against mites (e.g.Tetranychus urticae) were evaluated.The results of bioassays indicate that some of these title compounds exhibited excellent insecticidal and acaricidal activities.For example,4-bromo-1-((chloromethoxy)methyl)-2-(4-chloro phenyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile (6a),4-bromo-2-(4-chlorophenyl)-1-((2-fluoroethoxy)-methyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile (6d) showed insecticidal activity against Mythimna separata and 4-bromo-2-(4-chlorophenyl)1-((isopropoxymethoxy)methyl)-5-(trifluoro methyl)pyrrole-3-carbonitrile (7d) showed acaricidal activity against Tetranychus urticae.They were more effective than Chlorfenapyr,which has been the only commercialized member of a new class of chemicals of 2-arylpyrroles.