In the present study,the variation patterns of leaf shape in different populations of individual Semiliquidambar cathayensis plants were analyzed to investigate the relationship among leaf shape variation,photosynthet...In the present study,the variation patterns of leaf shape in different populations of individual Semiliquidambar cathayensis plants were analyzed to investigate the relationship among leaf shape variation,photosynthetic properties,and active compounds to understand the genetic characteristics of S.cathayensis and screen elite germplasms.The leaf shape of 18 offspring from three natural S.cathayensis populations was analyzed to investigate the level of diversity and variation patterns of leaf shape.Furthermore,photosynthetic pigment content,physiological parameters of photosynthesis,and the active compounds in leaves of different shapes were determined.Statistical analysis showed that the leaf shape variation in S.cathayensis indicated a high level of genetic diversity among and within the populations.Cluster analysis showed that the three natural populations formed two clusters,one whose offspring was dominated by entire leaves and another characterized by palmately trifoliate leaves.The differences in photosynthetic characteristics and active compounds of leaves of three different shapes were comprehensively evaluated using principal component analysis.Two principal components with a cumulative contribution rate of 92.768%were extracted,of which the highest comprehensive score was for asymmetrically lobed leaves.The leaf shape in different S.cathayensis germplasms exhibited distinct patterns,and there were some correlations between the photosynthetic properties and active compounds in leaves of different shapes.Thus,the leaf shape can be used to predict active compound content,and in turn,select varieties based on that purpose;it also provides a simple and effective method to classify S.cathayensis germplasms.展开更多
The occurrence,fate,and environmental risk of 40 pharmaceutically active compounds(PhACs)from surface waters and sediments were comprehensively investigated in the Beijiang River,Xijiang River,and Maozhou River of the...The occurrence,fate,and environmental risk of 40 pharmaceutically active compounds(PhACs)from surface waters and sediments were comprehensively investigated in the Beijiang River,Xijiang River,and Maozhou River of the Pearl River basin,South China.Salicylic acid and diclofenac(antiinflammatory drugs),gemfibrozil(a lipid regulator),carbamazepine(an antiepileptic drug),diazepam(a psychoactive drug),and 2-methyl-4-chloro-phenoxyacetic acid(MCPA,a pesticide)were the most ubiquitous compounds in the studied region.The average concentrations of detected PhACs in surface waters and sediments ranged from 0.17 to 19.1 ng/L and 0.10 to 10.4 ng/g,respectively.Meanwhile,PhACs concentration in surface waters and sediments varied greatly among and within the Beijiang River,Xijiang River,and Maozhou River.The largest annual flux of PhACs of the Xijiang River and Beijiang River was more than 11000 kg per annum,whereas only 25.7 kg/a in the Maozhou River.In addition,the estimated emissions of PhACs in the Beijiang River,Xijiang River,and Maozhou River ranged respectively from 0.28 to 4.22 kg/a,0.12 to 6.72 kg/a,and 6.66 to 91.0 kg/a,and the backestimated usage varied with a range from 12.0 to 293 kg/a,6.79 to 944 kg/a,368 to 17459 kg/a.Moreover,the emissions of PhACs showed a close relationship with the gross domestic product(GDP)of each city along the Pearl River.The environmental risk assessment suggested that diazepam and ibuprofen had a moderate risk in this region.展开更多
OBJECTIVE:To detect the effects of active compounds of Caodoukou(Semen Alpinia Katsumadai)(ACAK)on the proliferation,migration and invasion of pancreatic cancer,and explain the possible molecular mechanism of ACAK int...OBJECTIVE:To detect the effects of active compounds of Caodoukou(Semen Alpinia Katsumadai)(ACAK)on the proliferation,migration and invasion of pancreatic cancer,and explain the possible molecular mechanism of ACAK interacting with these processes.Methods:Cell counting kit-8 method,cell scratch repair experiment,Transwell migration and invasion experiment,immunohistochemistry,western blot assay and real-time polymerase chain reaction experiment were used to evaluate the effect of ACAK on the proliferation,migration and invasion of pancreatic cancer cells.The levels of active molecules involved in the phosphoinosmde-3-kinase(PI3K)/Akt/the mammalian target of rapamycin(m TOR)signal transduction were detected by Western blot assay.In addition,the function of ACAK in vivo was evaluated by xenotransplantation tumor model in nude mice.Results:The inhibitory effect of ACAK on the proliferation of pancreatic cancer cells showed certain time-dose dependence.The results of scratch repair test,Transwell test,Western blotting and real time polymerase chain reaction assay showed that ACAK could inhibit the migration and invasion of pancreatic cancer cells in vitro.In addition,the regulatory effect of ACAK on epithelialmesenchymal transition(EMT)is partly attributed to PI3K/Akt/mT OR signaling pathway.The experimental results in vivo showed that ACAK regulated the development of pancreatic cancer.Conclusions:ACAK can partly inhibit the activity of EMT and matrix metallopeptidases by down-regulating the downstream proteins of PI3K/Akt/mTOR signal pathway,thus inhibiting the ability of migration and invasion of pancreatic cancer.展开更多
Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran der...Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran derivatives, respectively were studied.展开更多
Mono-substituted heterocyclic ketene aminals are formed by the reaction of 1-methyl-2-methylthio-imidazoline with active methylene compounds containinq an acetyl or benzoyl group by the elimination of both a methylthi...Mono-substituted heterocyclic ketene aminals are formed by the reaction of 1-methyl-2-methylthio-imidazoline with active methylene compounds containinq an acetyl or benzoyl group by the elimination of both a methylthio and an acyl group.This is resulted by the secondary reactio of the produced methanethiol to attack the more active carbonyl group.展开更多
Eriochrome black T and Nitrosulfophenol S were advocated as the chemical models of carcinogenic non-aminoazo compounds. The main products of their oxidative cleavage in horseradish peroxidase/H2O2 system was identifie...Eriochrome black T and Nitrosulfophenol S were advocated as the chemical models of carcinogenic non-aminoazo compounds. The main products of their oxidative cleavage in horseradish peroxidase/H2O2 system was identified as the benezenediazonium ion, the ultimate carcinogens, which could bind to DNA. The reaction conditions were investigated preliminarily. Some inhibitors and inducers of the reaction were discovered.展开更多
Diabetes mellitus(DM)is characterized by persistently elevated blood glucose concentration that lead to multisystem complications.There are about 400 medicinal plants cited to have a beneficial effect on DM.We must ch...Diabetes mellitus(DM)is characterized by persistently elevated blood glucose concentration that lead to multisystem complications.There are about 400 medicinal plants cited to have a beneficial effect on DM.We must choose products wisely based on data derived from scientific studies.However,a major obstacle in the amalgamation of herbal medicine in modern medical practices is the lack of clinical data on its safety,efficacy and drug interaction.Trials of these herbal products often underreport the side effects and other crucial intervention steps deviating from the standards set by Consolidated Standards of Reporting Trials.Due to a lack of knowledge of the active compounds present in most herbal medicines,product standardization is difficult.Cost-effectiveness is another issue that needs to be kept in mind.In this mini-review,we focus on the antihyperglycemic effect of herbal products that are commonly used,along with the concerns stated above.展开更多
The composite exciter and the CaO to Na_(2)SO_(4) dosing ratios are known to have a strong impact on the mechanical strength offly-ash concrete.In the present study a hybrid approach relying on experiments and a machi...The composite exciter and the CaO to Na_(2)SO_(4) dosing ratios are known to have a strong impact on the mechanical strength offly-ash concrete.In the present study a hybrid approach relying on experiments and a machine-learn-ing technique has been used to tackle this problem.The tests have shown that the optimal admixture of CaO and Na_(2)SO_(4) alone is 8%.The best 3D mechanical strength offly-ash concrete is achieved at 8%of the compound activator;If the 28-day mechanical strength is considered,then,the best performances are obtained at 4%of the compound activator.Moreover,the 3D mechanical strength offly-ash concrete is better when the dosing ratio of CaO to Na_(2)SO_(4) in the compound activator is 1:1;the maximum strength offly-ash concrete at 28-day can be achieved for a 1:1 ratio of CaO to Na_(2)SO_(4) by considering a 4%compound activator.In this case,the compressive andflexural strengths are 260 MPa and 53.6 MPa,respectively;the mechanical strength offly-ash concrete at 28-day can be improved by a 4:1 ratio of CaO to Na_(2)SO_(4) by considering 8%and 12%compound excitants.It is shown that the predictions based on the aforementioned machine-learning approach are accurate and reliable.展开更多
Drying tea flowers into a high-quality product is important to its commodity value.In the present work,a combination of microwave-assisted drying and air drying(MAD-AD)was applied in the processing of fresh tea flower...Drying tea flowers into a high-quality product is important to its commodity value.In the present work,a combination of microwave-assisted drying and air drying(MAD-AD)was applied in the processing of fresh tea flowers and its effects on flavor quality,active nutraceutical compounds,and antioxidant capacities were studied.The results showed that compared to air drying and freeze drying tea flowers,the MAD-AD tea flowers had higher amounts of active compounds such as catechins,flavonol glycosides,and triterpenoid saponins,and possessed high antioxidant activities.Moreover,this drying method improved the tea flowers'color and preserved a more floral fragrance.This combined method could be of interest as an industrial method for drying tea flowers with the benefit of reduced processing time,more reserved active compounds and high quality of products.展开更多
BACKGROUND A comprehensive literature search shows that Sanqi and Huangjing(SQHJ)can improve diabetes treatment in vivo and in vitro,respectively.However,the combined effects of SQHJ on diabetes mellitus(DM)are still ...BACKGROUND A comprehensive literature search shows that Sanqi and Huangjing(SQHJ)can improve diabetes treatment in vivo and in vitro,respectively.However,the combined effects of SQHJ on diabetes mellitus(DM)are still unclear.AIM To explore the potential mechanism of Panax notoginseng(Sanqi in Chinese)and Polygonati Rhizoma(Huangjing in Chinese)for the treatment of DM using network pharmacology.METHODS The active components of SQHJ and targets were predicted and screened by network pharmacology through oral bioavailability and drug-likeness filtration using the Traditional Chinese Medicine Systems Pharmacology Analysis Platform database.The potential targets for the treatment of DM were identified according to the DisGeNET database.A comparative analysis was performed to investigate the overlapping genes between active component targets and DM treatmentrelated targets.We constructed networks of the active component-target and target pathways of SQHJ using Cytoscape software and then analyzed the gene functions.Using the STRING database to perform an interaction analysis among overlapping genes and a topological analysis,the interactions between potential targets were identified.Gene Ontology(GO)function analyses and Kyoto Encyclopedia of Genes and Genomes enrichment analyses were conducted in DAVID.RESULTS We screened 18 active components from 157 SQHJ components,187 potential targets for active components and 115 overlapping genes for active components and DM.The network pharmacology analysis revealed that quercetin,beta-sitosterol,baicalein,etc.were the major active components.The mechanism underlying the SQHJ intervention effects in DM may involve nine core targets(TP53,AKT1,CASP3,TNF,interleukin-6,PTGS2,MMP9,JUN,and MAPK1).The screening and enrichment analysis revealed that the treatment of DM using SQHJ primarily involved 16 GO enriched terms and 13 related pathways.CONCLUSION SQHJ treatment for DM targets TP53,AKT1,CASP3,and TNF and participates in pathways in leishmaniasis and cancer.展开更多
Activated methylene compound such as dimethyl malonate reacted readily with benzylic alcohols in the presence of ferric chloride/silica gel mixture (FeCl3/SiO2) under microwave irradiation to produce benzylic deriva...Activated methylene compound such as dimethyl malonate reacted readily with benzylic alcohols in the presence of ferric chloride/silica gel mixture (FeCl3/SiO2) under microwave irradiation to produce benzylic derivative of dimethyl malonate in high yields in solvent-free condition. 2009 Mohammad Reza Shushizadeh. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
A protocol for the Knoevenagel condensation of aromatic aldehydes with methylene compounds catalyzed by task specifed ionic liquid 1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium lactate under solvent-free conditions has bee...A protocol for the Knoevenagel condensation of aromatic aldehydes with methylene compounds catalyzed by task specifed ionic liquid 1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium lactate under solvent-free conditions has been developed. The reactions proceed at ambient temperature and the work-up procedures are very simple. Good to excellent yields could be obtained. The ionic liuid could be simply prepared and recycled efficiently.展开更多
A catalyst-free, facile and efficient Michael addition reaction of active methylene compounds as well as nitromethane with chalcones catalyzed by guanidinium lactate ionic liquid was done. A series of chalcones, nitro...A catalyst-free, facile and efficient Michael addition reaction of active methylene compounds as well as nitromethane with chalcones catalyzed by guanidinium lactate ionic liquid was done. A series of chalcones, nitromethane, and active methylene compounds were converted smoothly to the corresponding products in high yields. The simple procedure, very mild conditions, high yields, and reuse of the IL without any loss of catalytic activity make this protocol considerably attractive for academic researches and practical applications.展开更多
A simple and efficient Knoevenagel condensation between a b-unsaturated aldehydes and active methylene compounds is reported.Notably,this condensation can be catalyzed by PPL(lipase from porcine pancreas) with satis...A simple and efficient Knoevenagel condensation between a b-unsaturated aldehydes and active methylene compounds is reported.Notably,this condensation can be catalyzed by PPL(lipase from porcine pancreas) with satisfied yields(49%–92%).Moreover,PPL induces moderate Z/E selectivity in the Knoevenagel condensation.展开更多
The title compound 2-((2-fluorobenzyl)thio)-5-(pyridin-4-yl)-1,3,4-oxadiazole(C_(14)H_(10)FN_3OS) was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It ...The title compound 2-((2-fluorobenzyl)thio)-5-(pyridin-4-yl)-1,3,4-oxadiazole(C_(14)H_(10)FN_3OS) was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It crystallizes in the monoclinic system,space group P21/n with a = 11.541(16),b = 8.226(12),c = 13.683(19) ?,β = 94.872(17)o,V = 1294(3) ?~3,Z = 4 and R = 0.0648 for 2198 observed reflections with I 〉 2σ(I). The preliminary biological test shows that the title compound has good activity against Pythium ultimum with inhibitory to be 100%.展开更多
Medicinal plants,as medicinal materials and important drug components,have been used in traditional and folk medicine for ages.However,being sessile organisms,they are seriously affected by extreme environmental condi...Medicinal plants,as medicinal materials and important drug components,have been used in traditional and folk medicine for ages.However,being sessile organisms,they are seriously affected by extreme environmental conditions and abiotic stresses such as salt,heavy metal,temperature,and water stresses.Medicinal plants usually produce specific secondary metabolites to survive such stresses,and these metabolites can often be used for treating human diseases.Recently,medicinal plants have been found to partner with endophytic fungi to form a long-term,stable,and win-win symbiotic relationship.Endophytic fungi can promote secondary metabolite accumulation in medicinal plants.The close relationship can improve host plant resistance to the abiotic stresses of soil salinity,drought,and extreme temperatures.Their symbiosis also sheds light on plant growth and active compound production.Here,we show that endophytic fungi can improve the host medicinal plant resistance to abiotic stress by regulating active compounds,reducing oxidative stress,and regulating the cell ion balance.We also identify the deficiencies and burning issues of available studies and present promising research topics for the future.This review provides guidance for endophytic fungi research to improve the ability of medicinal plants to resist abiotic stress.It also suggests ideas and methods for active compound accumulation in medicinal plants and medicinal material development during the response to abiotic stress.展开更多
Eight new complexes with the formula [PhC_2C(OH)R^2R^2]Co_2(CO)_6 were prepared from phenyl substituted propargylic alcohols and dicobalt octacarbonyl.The reactions of these propargylio alcohol complexes with active m...Eight new complexes with the formula [PhC_2C(OH)R^2R^2]Co_2(CO)_6 were prepared from phenyl substituted propargylic alcohols and dicobalt octacarbonyl.The reactions of these propargylio alcohol complexes with active methylene compounds,2,4-pentanedione or ethyl acetoacetate,in the presnce of an acid,HBF_4(40%)+P_2O_5(in excess)or BF_3·Et_2O,at room temperature in dichlorome- thane were investigated.From the 1-alkyl substituted tertiary propargylic alcohol complexes,three new conjugated ene-yne complexes produced by intramolecular dehydration reaction were isolated in high yields(82—95%).On the other hand,four new alkylated complexes were obtained with satisfactory yields(44—66%)from the secondary propargylic alcohol complexes.The influence of other acids,phosphorus pentoxide and polyphosphoric acid,on both dehydration reaction and alkylated reaction was also studied.展开更多
Palladium-catalyzed allylation of carbonucleophiles has been widely used for carbon-carbon bond formation.Among the allylic compounds studied,allylic acetates were mostwidely used as precursors of(π-allyl)palladium i...Palladium-catalyzed allylation of carbonucleophiles has been widely used for carbon-carbon bond formation.Among the allylic compounds studied,allylic acetates were mostwidely used as precursors of(π-allyl)palladium intermediates.However,bases such as NaHmust be used to generate anions in this reaction.Recently,research on carrying out the palla-展开更多
The chemical composition of Zanthoxylum bungeanum(Z bungeanum) essential oi1(39 batches) was analyzed by gas chromatography-mass spectrometry(GC-MS) analysis(23 ingredients), and the antitumor activity against...The chemical composition of Zanthoxylum bungeanum(Z bungeanum) essential oi1(39 batches) was analyzed by gas chromatography-mass spectrometry(GC-MS) analysis(23 ingredients), and the antitumor activity against HeLa cells was detected via the MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. Two composition-activity relationship(CAR) models, generalized regression neural network(GRNN) and support vector regression(SVR) were respectively used to calculate the mean impact value(MIV) so as to identify bioactive com- pounds. Among them 9 ingredients(peaks 4, 15, 7, 8, 13, 3, 16, 9 and 11) were selected due to their high absolute MIVs. All of them have been confirmed with potential antitumor activity by previous researches. The CAR model combined with MIV was expected to be a credible tool for the active compound identification from herbs.展开更多
To overcome the inconveniences related to its conventional obtainment of natural sweeteners and active compounds from Stevia rebaudiana Bertoni,methods involving application of technology,such as ultrasound assisted e...To overcome the inconveniences related to its conventional obtainment of natural sweeteners and active compounds from Stevia rebaudiana Bertoni,methods involving application of technology,such as ultrasound assisted extraction,microwave assisted extraction,extraction under pressurized conditions by means of pressurized liquid extraction,subcritical water extraction and supercritical fluid extraction have been investigated.In this review,these emerging techniques were analyzed and discussed,the process variables and operational strategies,their impacts on the extraction and their comparison against the conventional techniques were demonstrated.Simplicity and the possibility of operational automation,the use of less energy and solvents,in addition to the reduced complexity of the subsequent purification steps,make up viable alternatives suitable for a possible industrial application.These processes leverage the concept of green chemistry,but still suffer limitations related to acquisition and maintenance costs,in addition to the effects of the action of some of these technologies remaining unexplored.展开更多
基金funded by Changsha Natural Science Foundation(Grant No.kq2202356)Hunan Forestry Science and Technology Innovation Plan Project(Grant No.XLK202106-2).
文摘In the present study,the variation patterns of leaf shape in different populations of individual Semiliquidambar cathayensis plants were analyzed to investigate the relationship among leaf shape variation,photosynthetic properties,and active compounds to understand the genetic characteristics of S.cathayensis and screen elite germplasms.The leaf shape of 18 offspring from three natural S.cathayensis populations was analyzed to investigate the level of diversity and variation patterns of leaf shape.Furthermore,photosynthetic pigment content,physiological parameters of photosynthesis,and the active compounds in leaves of different shapes were determined.Statistical analysis showed that the leaf shape variation in S.cathayensis indicated a high level of genetic diversity among and within the populations.Cluster analysis showed that the three natural populations formed two clusters,one whose offspring was dominated by entire leaves and another characterized by palmately trifoliate leaves.The differences in photosynthetic characteristics and active compounds of leaves of three different shapes were comprehensively evaluated using principal component analysis.Two principal components with a cumulative contribution rate of 92.768%were extracted,of which the highest comprehensive score was for asymmetrically lobed leaves.The leaf shape in different S.cathayensis germplasms exhibited distinct patterns,and there were some correlations between the photosynthetic properties and active compounds in leaves of different shapes.Thus,the leaf shape can be used to predict active compound content,and in turn,select varieties based on that purpose;it also provides a simple and effective method to classify S.cathayensis germplasms.
基金This work was financially supported by the National Natural Science Foundation of China(Nos.41877358 and U1701242)the Pearl River Talent Plan of Guangdong Province(No.2017GC010244)the Key R&D projects of Guangxi(No.2018AB36018).
文摘The occurrence,fate,and environmental risk of 40 pharmaceutically active compounds(PhACs)from surface waters and sediments were comprehensively investigated in the Beijiang River,Xijiang River,and Maozhou River of the Pearl River basin,South China.Salicylic acid and diclofenac(antiinflammatory drugs),gemfibrozil(a lipid regulator),carbamazepine(an antiepileptic drug),diazepam(a psychoactive drug),and 2-methyl-4-chloro-phenoxyacetic acid(MCPA,a pesticide)were the most ubiquitous compounds in the studied region.The average concentrations of detected PhACs in surface waters and sediments ranged from 0.17 to 19.1 ng/L and 0.10 to 10.4 ng/g,respectively.Meanwhile,PhACs concentration in surface waters and sediments varied greatly among and within the Beijiang River,Xijiang River,and Maozhou River.The largest annual flux of PhACs of the Xijiang River and Beijiang River was more than 11000 kg per annum,whereas only 25.7 kg/a in the Maozhou River.In addition,the estimated emissions of PhACs in the Beijiang River,Xijiang River,and Maozhou River ranged respectively from 0.28 to 4.22 kg/a,0.12 to 6.72 kg/a,and 6.66 to 91.0 kg/a,and the backestimated usage varied with a range from 12.0 to 293 kg/a,6.79 to 944 kg/a,368 to 17459 kg/a.Moreover,the emissions of PhACs showed a close relationship with the gross domestic product(GDP)of each city along the Pearl River.The environmental risk assessment suggested that diazepam and ibuprofen had a moderate risk in this region.
基金Sichuan Science and Technology program:Study on the Molecular Mechanism and Reversal Strategy of Drug Resistance in“T+A”Therapy for Liver Cancer,No.2022YSF0625)Joint Project from Luzhou city and Southwest Medical University:Study on Preparation and Anti-colon Cancer Activity of PEG-PLGA Nanoparticles from Active Fraction of Clove,No.20ykdhz0008)Grants from National Natural Science Foundation of China:Study on the Interaction between Granulin A and ENO1 and Its Molecular Mechanism of Inhibiting Tumor Growth and Metastasis(No.81773776)。
文摘OBJECTIVE:To detect the effects of active compounds of Caodoukou(Semen Alpinia Katsumadai)(ACAK)on the proliferation,migration and invasion of pancreatic cancer,and explain the possible molecular mechanism of ACAK interacting with these processes.Methods:Cell counting kit-8 method,cell scratch repair experiment,Transwell migration and invasion experiment,immunohistochemistry,western blot assay and real-time polymerase chain reaction experiment were used to evaluate the effect of ACAK on the proliferation,migration and invasion of pancreatic cancer cells.The levels of active molecules involved in the phosphoinosmde-3-kinase(PI3K)/Akt/the mammalian target of rapamycin(m TOR)signal transduction were detected by Western blot assay.In addition,the function of ACAK in vivo was evaluated by xenotransplantation tumor model in nude mice.Results:The inhibitory effect of ACAK on the proliferation of pancreatic cancer cells showed certain time-dose dependence.The results of scratch repair test,Transwell test,Western blotting and real time polymerase chain reaction assay showed that ACAK could inhibit the migration and invasion of pancreatic cancer cells in vitro.In addition,the regulatory effect of ACAK on epithelialmesenchymal transition(EMT)is partly attributed to PI3K/Akt/mT OR signaling pathway.The experimental results in vivo showed that ACAK regulated the development of pancreatic cancer.Conclusions:ACAK can partly inhibit the activity of EMT and matrix metallopeptidases by down-regulating the downstream proteins of PI3K/Akt/mTOR signal pathway,thus inhibiting the ability of migration and invasion of pancreatic cancer.
基金the National Natural Science Foundation of China (No.20676123) for financial support.
文摘Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran derivatives, respectively were studied.
文摘Mono-substituted heterocyclic ketene aminals are formed by the reaction of 1-methyl-2-methylthio-imidazoline with active methylene compounds containinq an acetyl or benzoyl group by the elimination of both a methylthio and an acyl group.This is resulted by the secondary reactio of the produced methanethiol to attack the more active carbonyl group.
文摘Eriochrome black T and Nitrosulfophenol S were advocated as the chemical models of carcinogenic non-aminoazo compounds. The main products of their oxidative cleavage in horseradish peroxidase/H2O2 system was identified as the benezenediazonium ion, the ultimate carcinogens, which could bind to DNA. The reaction conditions were investigated preliminarily. Some inhibitors and inducers of the reaction were discovered.
文摘Diabetes mellitus(DM)is characterized by persistently elevated blood glucose concentration that lead to multisystem complications.There are about 400 medicinal plants cited to have a beneficial effect on DM.We must choose products wisely based on data derived from scientific studies.However,a major obstacle in the amalgamation of herbal medicine in modern medical practices is the lack of clinical data on its safety,efficacy and drug interaction.Trials of these herbal products often underreport the side effects and other crucial intervention steps deviating from the standards set by Consolidated Standards of Reporting Trials.Due to a lack of knowledge of the active compounds present in most herbal medicines,product standardization is difficult.Cost-effectiveness is another issue that needs to be kept in mind.In this mini-review,we focus on the antihyperglycemic effect of herbal products that are commonly used,along with the concerns stated above.
基金supported by the Scientific Research Fund Project of Yunnan Education Department(Grant Numbers 2023J1974 and 2023J1976)the Yunnan University Professional Degree Graduate Student Practical Innovation Fund Project(Grant Number ZC-22222374)also supported by the Yunnan Provincial Education Department Fund(Grant No.2022Y286).
文摘The composite exciter and the CaO to Na_(2)SO_(4) dosing ratios are known to have a strong impact on the mechanical strength offly-ash concrete.In the present study a hybrid approach relying on experiments and a machine-learn-ing technique has been used to tackle this problem.The tests have shown that the optimal admixture of CaO and Na_(2)SO_(4) alone is 8%.The best 3D mechanical strength offly-ash concrete is achieved at 8%of the compound activator;If the 28-day mechanical strength is considered,then,the best performances are obtained at 4%of the compound activator.Moreover,the 3D mechanical strength offly-ash concrete is better when the dosing ratio of CaO to Na_(2)SO_(4) in the compound activator is 1:1;the maximum strength offly-ash concrete at 28-day can be achieved for a 1:1 ratio of CaO to Na_(2)SO_(4) by considering a 4%compound activator.In this case,the compressive andflexural strengths are 260 MPa and 53.6 MPa,respectively;the mechanical strength offly-ash concrete at 28-day can be improved by a 4:1 ratio of CaO to Na_(2)SO_(4) by considering 8%and 12%compound excitants.It is shown that the predictions based on the aforementioned machine-learning approach are accurate and reliable.
基金the Natural Science Foundation of Zhejiang Province(LY16C200004)the Key Research and Development Projects in Zhejiang Province industrialization Model Projects on Exploring Functional Components and Related Products from Tea Flowers and Fruits(2018C02012),China.
文摘Drying tea flowers into a high-quality product is important to its commodity value.In the present work,a combination of microwave-assisted drying and air drying(MAD-AD)was applied in the processing of fresh tea flowers and its effects on flavor quality,active nutraceutical compounds,and antioxidant capacities were studied.The results showed that compared to air drying and freeze drying tea flowers,the MAD-AD tea flowers had higher amounts of active compounds such as catechins,flavonol glycosides,and triterpenoid saponins,and possessed high antioxidant activities.Moreover,this drying method improved the tea flowers'color and preserved a more floral fragrance.This combined method could be of interest as an industrial method for drying tea flowers with the benefit of reduced processing time,more reserved active compounds and high quality of products.
基金Supported by the Central Government guides local S&T Program of Hebei Province,No.216Z2501GScientific Research Project of Hebei Provincial Market Supervision Administration,No.2021YJ11.
文摘BACKGROUND A comprehensive literature search shows that Sanqi and Huangjing(SQHJ)can improve diabetes treatment in vivo and in vitro,respectively.However,the combined effects of SQHJ on diabetes mellitus(DM)are still unclear.AIM To explore the potential mechanism of Panax notoginseng(Sanqi in Chinese)and Polygonati Rhizoma(Huangjing in Chinese)for the treatment of DM using network pharmacology.METHODS The active components of SQHJ and targets were predicted and screened by network pharmacology through oral bioavailability and drug-likeness filtration using the Traditional Chinese Medicine Systems Pharmacology Analysis Platform database.The potential targets for the treatment of DM were identified according to the DisGeNET database.A comparative analysis was performed to investigate the overlapping genes between active component targets and DM treatmentrelated targets.We constructed networks of the active component-target and target pathways of SQHJ using Cytoscape software and then analyzed the gene functions.Using the STRING database to perform an interaction analysis among overlapping genes and a topological analysis,the interactions between potential targets were identified.Gene Ontology(GO)function analyses and Kyoto Encyclopedia of Genes and Genomes enrichment analyses were conducted in DAVID.RESULTS We screened 18 active components from 157 SQHJ components,187 potential targets for active components and 115 overlapping genes for active components and DM.The network pharmacology analysis revealed that quercetin,beta-sitosterol,baicalein,etc.were the major active components.The mechanism underlying the SQHJ intervention effects in DM may involve nine core targets(TP53,AKT1,CASP3,TNF,interleukin-6,PTGS2,MMP9,JUN,and MAPK1).The screening and enrichment analysis revealed that the treatment of DM using SQHJ primarily involved 16 GO enriched terms and 13 related pathways.CONCLUSION SQHJ treatment for DM targets TP53,AKT1,CASP3,and TNF and participates in pathways in leishmaniasis and cancer.
基金Science and Research University for financial support of this work
文摘Activated methylene compound such as dimethyl malonate reacted readily with benzylic alcohols in the presence of ferric chloride/silica gel mixture (FeCl3/SiO2) under microwave irradiation to produce benzylic derivative of dimethyl malonate in high yields in solvent-free condition. 2009 Mohammad Reza Shushizadeh. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
基金Supported by the National Natural Science Foundation of China(No.20776127)the National Key Technology Research and Development Program of China(No.2007BAI34B07)
文摘A protocol for the Knoevenagel condensation of aromatic aldehydes with methylene compounds catalyzed by task specifed ionic liquid 1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium lactate under solvent-free conditions has been developed. The reactions proceed at ambient temperature and the work-up procedures are very simple. Good to excellent yields could be obtained. The ionic liuid could be simply prepared and recycled efficiently.
文摘A catalyst-free, facile and efficient Michael addition reaction of active methylene compounds as well as nitromethane with chalcones catalyzed by guanidinium lactate ionic liquid was done. A series of chalcones, nitromethane, and active methylene compounds were converted smoothly to the corresponding products in high yields. The simple procedure, very mild conditions, high yields, and reuse of the IL without any loss of catalytic activity make this protocol considerably attractive for academic researches and practical applications.
基金the financial support from the National Natural Science Foundation of China (Nos. 21172093, 31070708, and 21072075)the Natural Science Foundation of Jilin Province of China (Nos. 201115039 and 20140101141JC)the Scientific Research Fund of Jilin University (No. 450060326007)
文摘A simple and efficient Knoevenagel condensation between a b-unsaturated aldehydes and active methylene compounds is reported.Notably,this condensation can be catalyzed by PPL(lipase from porcine pancreas) with satisfied yields(49%–92%).Moreover,PPL induces moderate Z/E selectivity in the Knoevenagel condensation.
基金funded by the Natural Science Foundation of Zhejiang Province(No.LY16C140007)the program of Science and Technology of Jiangsu Province(BY2014108-14)
文摘The title compound 2-((2-fluorobenzyl)thio)-5-(pyridin-4-yl)-1,3,4-oxadiazole(C_(14)H_(10)FN_3OS) was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It crystallizes in the monoclinic system,space group P21/n with a = 11.541(16),b = 8.226(12),c = 13.683(19) ?,β = 94.872(17)o,V = 1294(3) ?~3,Z = 4 and R = 0.0648 for 2198 observed reflections with I 〉 2σ(I). The preliminary biological test shows that the title compound has good activity against Pythium ultimum with inhibitory to be 100%.
基金supported by National Natural Science Foundation of China(No.82003896,81673528)Natural Science Foundation of Zhejiang Province(No.LQ21H280003)+1 种基金Young Innovative Talents Project of Zhejiang Medical Health Science and Technology(No.2022RC052)Talent Projects of Zhejiang Chinese Medical University(No.2021ZR09).
文摘Medicinal plants,as medicinal materials and important drug components,have been used in traditional and folk medicine for ages.However,being sessile organisms,they are seriously affected by extreme environmental conditions and abiotic stresses such as salt,heavy metal,temperature,and water stresses.Medicinal plants usually produce specific secondary metabolites to survive such stresses,and these metabolites can often be used for treating human diseases.Recently,medicinal plants have been found to partner with endophytic fungi to form a long-term,stable,and win-win symbiotic relationship.Endophytic fungi can promote secondary metabolite accumulation in medicinal plants.The close relationship can improve host plant resistance to the abiotic stresses of soil salinity,drought,and extreme temperatures.Their symbiosis also sheds light on plant growth and active compound production.Here,we show that endophytic fungi can improve the host medicinal plant resistance to abiotic stress by regulating active compounds,reducing oxidative stress,and regulating the cell ion balance.We also identify the deficiencies and burning issues of available studies and present promising research topics for the future.This review provides guidance for endophytic fungi research to improve the ability of medicinal plants to resist abiotic stress.It also suggests ideas and methods for active compound accumulation in medicinal plants and medicinal material development during the response to abiotic stress.
基金Work supported by the National Natural Science Foundation of China.
文摘Eight new complexes with the formula [PhC_2C(OH)R^2R^2]Co_2(CO)_6 were prepared from phenyl substituted propargylic alcohols and dicobalt octacarbonyl.The reactions of these propargylio alcohol complexes with active methylene compounds,2,4-pentanedione or ethyl acetoacetate,in the presnce of an acid,HBF_4(40%)+P_2O_5(in excess)or BF_3·Et_2O,at room temperature in dichlorome- thane were investigated.From the 1-alkyl substituted tertiary propargylic alcohol complexes,three new conjugated ene-yne complexes produced by intramolecular dehydration reaction were isolated in high yields(82—95%).On the other hand,four new alkylated complexes were obtained with satisfactory yields(44—66%)from the secondary propargylic alcohol complexes.The influence of other acids,phosphorus pentoxide and polyphosphoric acid,on both dehydration reaction and alkylated reaction was also studied.
文摘Palladium-catalyzed allylation of carbonucleophiles has been widely used for carbon-carbon bond formation.Among the allylic compounds studied,allylic acetates were mostwidely used as precursors of(π-allyl)palladium intermediates.However,bases such as NaHmust be used to generate anions in this reaction.Recently,research on carrying out the palla-
基金the National Natural Science Foundation of China
文摘The chemical composition of Zanthoxylum bungeanum(Z bungeanum) essential oi1(39 batches) was analyzed by gas chromatography-mass spectrometry(GC-MS) analysis(23 ingredients), and the antitumor activity against HeLa cells was detected via the MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. Two composition-activity relationship(CAR) models, generalized regression neural network(GRNN) and support vector regression(SVR) were respectively used to calculate the mean impact value(MIV) so as to identify bioactive com- pounds. Among them 9 ingredients(peaks 4, 15, 7, 8, 13, 3, 16, 9 and 11) were selected due to their high absolute MIVs. All of them have been confirmed with potential antitumor activity by previous researches. The CAR model combined with MIV was expected to be a credible tool for the active compound identification from herbs.
基金The authors would like to thank the Coordenaç˜ao de Aperfeiçoamento de Pessoal de Nível Superior(CAPES,process number 88882.449245/2019-01),for the financial support.
文摘To overcome the inconveniences related to its conventional obtainment of natural sweeteners and active compounds from Stevia rebaudiana Bertoni,methods involving application of technology,such as ultrasound assisted extraction,microwave assisted extraction,extraction under pressurized conditions by means of pressurized liquid extraction,subcritical water extraction and supercritical fluid extraction have been investigated.In this review,these emerging techniques were analyzed and discussed,the process variables and operational strategies,their impacts on the extraction and their comparison against the conventional techniques were demonstrated.Simplicity and the possibility of operational automation,the use of less energy and solvents,in addition to the reduced complexity of the subsequent purification steps,make up viable alternatives suitable for a possible industrial application.These processes leverage the concept of green chemistry,but still suffer limitations related to acquisition and maintenance costs,in addition to the effects of the action of some of these technologies remaining unexplored.