Design, Synthesis, and Biological Activity of Novel Aromatic Amide Derivatives Containing Sulfide and Sulfone Substructures

In recent years,the damage caused by soil nematodes has become increasingly serious;however,the varieties and structures of the nematicides available on the market are deficient.Fluopyram,a succinate dehydrogenase inhibitor(SDHI)fungicide developed by Bayer AG in Germany,has been widely used in the prevention and control of soil nematodes due to its high efficiency and novel mechanism of action.In this paper,two series of novel target compounds were designed and synthesized with nematicidal and fungicidal fluopyram as the molecular skeleton in order to introduce sulfide and sulfone substructures.The structures were identified and characterized by 1H nuclear magnetic resonance(NMR),13C NMR,and high-resolution mass spectrometer(HRMS).The bioassays revealed that most of the compounds showed excellent nematicidal activities at 200 lgmL-1 in comparison with fluopyram,while the nematode mortality rate dropped sharply at 100μg·mL-1,except for compounds I-11 and II-6.In terms of fungicidal activity,compound I-9 was discovered to have an excellent inhibitory rate,and a molecular docking simulation was performed that can provide important guidance for the design and exploration of efficient fungicidal lead compounds.

Effects of bark beetle pheromones on the attraction of Monochamus alternatus to pine volatiles

We evaluated the attraction ofMonochamus alternatus Hope （Coleoptera： Cerambycidae）, Dryocoetes luteus Blandford and Orthotomicus erosus Wollaston （Coleoptera： Curculionidae： Scolytinae） to multiple-funnel traps baited with the pine volatiles, ethanol and （＋）-α-pinene and the bark beetle pheromones, ipsenol and ipsdienol. M. alternatus were attracted to traps baited with ethanol and （＋）-α-pinene but not those baited with ipsdienol and ipsenol. Ipsdienol and ipsenol decreased catches ofM. alternatus in traps baited with ethanol and （＋）-α-pinene. Traps baited with either binary combinations of ethanol and （＋）-α-pinene or ipsdienol and ipsenol were attractive to D. luteus and O. erosus. The addition of ipsenol and ipsdienol to traps baited with ethanol and （＋）-α-pinene synergized attraction of O. erosus but not D. luteus .

Phytolith carbon sequestration in bamboos of different ecotypes:a case study in China

Occlusion of carbon(C) within phytoliths(Phyt OC) is becoming one of the most promising terrestrial C sequestration mechanisms. This study explored the production of Phyt OC within 35 bamboo species belonging to three ecotypes using methods of microwave digestion. The aim of this study is to explore the present and potential C sequestration rate within phytoliths of bamboo species from three ecotypes. Phyt OC content in bamboos of three ecotypes ranges from 0.07 % to 0.42 %. The mean Phyt OC production flux decreases as: clustered bamboo(0.050 ±0.016 t CO2ha-1a-1) & mixed bamboo(0.049 ± 0.016 t CO2ha-1a-1) [ scattered bamboo(0.038 ± 0.020 t CO2ha-1a-1). The phytolith carbon sequestration in Chinese bamboo is estimated to be 0.293 ± 0.127 Tg(1 Tg =1012g) CO2a-1; approximately 75 %, 3 %, and 22 % of which is contributed from scattered, mixed and clustered bamboo, respectively. Taking the Phyt OC production flux of 0.18 ± 0.12 t CO2ha-1a-1and current annual area increasing rate of 3 %, global bamboo phytoliths wouldsequester 11.9 ± 7.9 Tg CO2a-1by 2050. Consequently,bamboo forests have significant potential to mitigate the increasing concentration of atmospheric CO2 by maximizing Phyt OC production flux and expanding bamboos.

Design, Synthesis and Biological Activity of N-Sulfonyl Aromatic Amide Derivatives

Fifteen novel N-sulfonyl aromatic amide derivatives were designed and synthesized, and the structures were characterized by 1H-and 13C-NMR, EA and HRMS. The crystal structures of compounds I-8 and I-9 were obtained from X-ray diffraction: I-8 is of triclinic system, Mr = 372.35, space group P2_(1/n) with a = 7.9151(10), b = 8.5637(11), c = 12.2022(15) A, β = 86.865(2)o, V = 807.09(18) A^(3), Z = 2, F(000) = 384, D_(c) = 1.532 g/cm^(3), the final R = 0.0408 and wR = 0.1068 for 2836 unique reflections with 2435 observed ones(I > 2σ(I)). I-9 belongs to triclinic system, M_r = 407.39, space group P2_1/n, with a = 8.4911(8), b = 8.6053(9), c = 14.5808(15) A, β = 77.1190(10)o, V = 995.44(17)A^(3), Z = 2, F(000) = 416, D_(c) = 1.359 g/cm^(3), the final R = 0.0567 and wR = 0.1779 for 3475 unique reflections with 2392 observed ones(I > 2σ(I)). The preliminary bioassay results indicated that the target compounds showed weak nematicidal activity, while compound I-5 displayed good fungicidal activity against Colletotrichum capsici with the inhibition rate of 61.7%.

The inhibition mechanism of the uptake of lamivudine via human organic anion transporter 1 by Stellera chamaejasme L. extracts

Stellera chamaejasme L.is a traditional Chinese medicine with a long history to treat stubborn skin ulcer,and it also has antiviral and antitumor effects.Neochamaejasmine B(NCB),Neochamaejasmine A(NCA)and Chamaechromone(CMC)are the major components in dried roots of Stellera chamaejasme L..Our studies suggested that NCB,NCA and CMC are inhibitors of Organic anion transporter 1(OAT1).OAT1 is encoded by solute carrier family 22 member 6 gene(SLC22 A6)in humans and plays a critical role in the organic anion drug uptake and excretion in the kidney.Lamivudine is the typical substrate of OAT1 and is frequently used in combination with other antiviral drugs in clinical antiviral treatments.The aim of this study is to investigate the interaction and its mechanism between these bi-flavone components in Stellera chamaejasme L.and lamivudine via OAT1 both in vitro and in vivo.In vitro,the uptake studies in Madin-Darby canine kidney(MDCK)cells overexpressing OAT1 suggested that NCB inhibited the uptake of 6-CFL and lamivudine.Similar results were obtained for NCA and CMC.NCB was a noncompetitive and competitive inhibitor interaction with OAT1.IC50 values of NCB,NCA and CMC for inhibiting OAT1-mediated lamivudine transport were 2.46,8.35 and 0.61μmol·L^–1,respectively.In vivo,the pharmacokinetic results of lamivudine in rats showed that the mean area under the plasma concentration-time curve(AUC0-∞)and maximal plasma concentration(Cmax)of lamivudine after co-administration is increased 2.94-fold and 1.87-fold,respectively,compared to lamivudine administration alone.The results of interactions between lamivudine and these bi-flavone components in Stellera chamaejasme L.extracts via OAT1 in vivo are consistent with studies in vitro.The inhibition of OAT1-mediated uptake of lamivudine by NCB,NCA and CMC is the possible mechanism for Stellera chamaejasme L.extracts improving the oral bioavailability of lamivudine in rats.

The effects of biodiversity gradient on plant mass and metabolism of individual submerged macrophytes

Background:The effects of biodiversity on community function and services are frequently studied in the history of ecology,while the response of individual species to biodiversity remains great elusive.In this study,we determined the biodiversity effects on community productivity as well as species level plant mass and carbon(C)and nitrogen(N)metabolism of eight submerged plants.These macrophytes in Lake Erhai were selected and planted in a water depth of one meter along a diversity gradient of 1,2,4 or 8 species.Then,the community productivity or species level plant mass,soluble protein,free amino acid and soluble carbohydrate were correlated to species richness to determine the biodiversity effects on community and single species.Results:The results showed that the community level biomass was positively correlated to plant species richness although the species level plant mass of individual species responded differently to the overall plant species richness.Namely,only one plant mass positively correlated to species richness and the others decreased or showed no significant correlation with the increase of species richness.The soluble proteins of most macrophytes were positively correlated to species richness;however,both the free amino acid and soluble carbohydrate of the plants were negatively or not significantly correlated to species richness.Conclusions:These results indicated that the selection effects might dominate in our aquatic communities and the negative impacts of biodiversity on C and N metabolism of the macrophytes increased with the increase of species richness,which might result from the strong competition among the studied species.The biodiversity effects on the plant mass,and C and N metabolism of individual submerged species were first reported in this study,while more such field and control experiments deserve further research.

Social-ecological transformations of Inner Mongolia:a sustainability perspective

Introduction:Sustainability requires the reconciling of human needs with the healthy natural ecosystem,which should be achieved within the grand course of industrialization and modernization.Systematic transitions on demography,economy,technology,and institutions are required,while different civilizations may take their respective paths.In this study,we analyze the social-ecological transitions of Inner Mongolia Autonomous Region of China during the past century,focusing on major changes in its environmental,demographic,and socioeconomic conditions.Results:A two-level social-ecological system analysis framework was proposed,and four stages of transition were identified:traditional nomadism,primitive industrial civilization,collectivization era,and economic reform/opendoor policy era.Our analysis showed that Inner Mongolia has made great achievements in its socioeconomic domains but is faced with numerous challenging environmental problems.Overconsumption of resources and failure to curtail ecological degradation may lead to a trap of unsustainability.Conclusions:However,the slowing-down population growth,improvements of the economic structure,and many new sustainability initiatives and strong support from the central government together give hope for a sustainable future of the region.