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
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
Basidial fungi have long been known as sources of antitumor compounds such as polysaccharides.Studies conducted by scientists from different countries demonstrate that polysaccharides and other fungal compounds(protei...Basidial fungi have long been known as sources of antitumor compounds such as polysaccharides.Studies conducted by scientists from different countries demonstrate that polysaccharides and other fungal compounds(proteins,glycoproteins,terpenoids,melanins,nucleosides,etc.)exhibit antiviral activity against many viruses pathogenic for humans.The review presents data on the studied antiviral activities of higher basidial fungi against herpes,West Nile,influenza,human immunodeficiency and hepatitis viruses as well as orthopoxviruses including variola virus.Many species of basidial fungi and various classes of biologically active compounds obtained from them are capable of effectively inhibiting the development of viruses in cells and animals while possessing low toxicity.Biologically active compounds from the same fungal species can exhibit antiviral effects against different pathogens.Effective strains isolated from wild mushrooms in culture represent promising objects for the development of biotechnological drugs,including ones possessing antiviral activity.The data on antitumor and antiviral activities of compounds from the same fungal species indicate the correlation of these properties.In this connection,preparations of basidial fungi may have prophylactic value in preventing cancers of viral etiology.展开更多
Chrysanthemum is rich in active compounds such as flavonoids and phenolic acids,and its dried head flowers are commonly used for tea and medicinal purposes.However,the genetic determinism underlying chrysanthemum acti...Chrysanthemum is rich in active compounds such as flavonoids and phenolic acids,and its dried head flowers are commonly used for tea and medicinal purposes.However,the genetic determinism underlying chrysanthemum active compounds remains elusive.In this study,we evaluated a panel of 137 chrysanthemum accessions for total flavonoids,chlorogenic acid,luteolin,and isochlorogenic acid A across two consecutive years.The four active compounds exhibited considerable variation,with a coefficient of variation ranging from 44.96%to 76.30%.Significant differences were observed in genotype and environments,and the broad-sense heritability was estimated at 0.5e0.63 for all examined traits.Significant pair-wise correlation was found between the four active compounds.Several accessions showing the highest active compounds were figured out for breeding use by integrating the membership function and hierarchical cluster analysis methods.Based on the 327042 high-quality SNPs,a genome-wide association study(GWAS)captured 59 significant SNPs for the four active compounds,of which 24 elite alleles exhibited pyramiding effects.A total of 18 potential candidate genes were mined,among which evm.model.scaffold_1149.273(QUA1)has one linkage disequilibrium(LD)block corresponding to Hap4 with the highest luteolin content.The findings are beneficial to understanding the genetic basis of the active compounds and provide parental materials and valuable markers for the genetic improvement of active compounds in chrysanthemums.展开更多
Pharmaceutically active compounds(PhACs)are widely used in medical treatments but pose risks to ecosystems and human health when present in the environment.Understanding their fate in nature is complex and influenced ...Pharmaceutically active compounds(PhACs)are widely used in medical treatments but pose risks to ecosystems and human health when present in the environment.Understanding their fate in nature is complex and influenced by various factors.Phototransformation,where PhACs change chemically upon light exposure,offers the potential for reducing their environmental levels.Studying this process is crucial for understanding risks,developing safe disposal strategies,and innovating removal methods to mitigate adverse effects.This review delves into the major factors influencing the transformation of PhACs under natural conditions.It provides a comprehensive analysis of the mechanisms involved in the photochemical activity of PhACs,shedding light on their behavior upon exposure to sunlight.Special attention is given to delineating the differences in the phototransformation processes among 13 major pharmaceutical classes.By examining the various factors influencing PhAC transformation and eluci-dating their mechanisms,this review aims to contribute to a deeper understanding of the fate of pharmaceuticals in the environment.Such insights are invaluable for developing effective strategies to mitigate the risks posed by PhAC contamination and safeguarding environmental and human health.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
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
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
p-Menthane type monoterpene derivatives were identified as bio-based compounds with high herbicidal activities. In order to search novel p-menthane type monoterpene derivatives in good performance, a series of novel c...p-Menthane type monoterpene derivatives were identified as bio-based compounds with high herbicidal activities. In order to search novel p-menthane type monoterpene derivatives in good performance, a series of novel cis-p-menthane type Schiff base derivatives were designed and synthesized. All target products were easily available novel compounds and characterized by FT-IR,^1H NMR,^13 C NMR and ESI＋-MS. Their pre-emergence herbicidal activities against annual ryegrass were evaluated. The bioassays indicated that most of the target compounds displayed excellent herbicidal activities in pre-emergence treatment.展开更多
An activated carbon pore-expanding technique was achieved through innovative reactivation by CO_2/microwave.The original and modified activated carbons were characterized by nitrogen adsorption–desorption,scanning el...An activated carbon pore-expanding technique was achieved through innovative reactivation by CO_2/microwave.The original and modified activated carbons were characterized by nitrogen adsorption–desorption,scanning electron microscopy,transmission electron microcopy,and Fourier transform infrared spectroscopy.The mesopore volume increased from 0.122 cm^3·g^(-1) to 0.270 cm^3·g^(-1),and a hierarchical pore structure was formed.A gradual decrease in the phenolic hydroxyl and carboxyl groups on the surface of activated carbon enhanced the surface inertia of granular activated carbon(GAC).The toluene desorption rate of the modified sample increased by 8.81% compared with that of the original GAC.Adsorption isotherm fittings revealed that the Langmuir model was applicable for the original and modified activated carbons.The isosteric adsorption heat of toluene on the activated carbon decreased by approximately 50%,which endowed the modified sample with excellent stability in application.The modified samples showed an enhanced desorption performance of toluene,thereby opening a way to extend the cycle life and improve the economic performance of carbon adsorbent in practical engineering applications.展开更多
According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects...According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects on leaching rate of alumina have been investigated. The results showed that the fly ash can be activated effectively and the leaching rate of alumina can be improved to more than 92% through this method. The best process parameters were the ratio of raw materials,i. e. the material weight ratio of fly ash,calcium carbonate and sodium carbonate was 1. 0∶1. 2∶0. 9. The activating temperature was 850℃-900℃,activating time was 3 h. This process has a potential application prospect and improves the value of comprehensive utilization of fly ash.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
Objective To summarize the uric acid-lowering effects and mechanisms of Chinese medicines with medicine-food homology,aiming to provide novel perspectives for the devel-opment of new anti-hyperuricemia(HUA)drugs.Metho...Objective To summarize the uric acid-lowering effects and mechanisms of Chinese medicines with medicine-food homology,aiming to provide novel perspectives for the devel-opment of new anti-hyperuricemia(HUA)drugs.Methods Papers on the research of HUA prevention and treatment with medicine-food ho-mology from December 15,2002 to August 10,2024 were screened and collected through Chi-na National Knowledge Infrastructure(CNKI),PubMed,ScienceDirect,and Google Scholar.Subsequently,the impact of these medications and their extracts,as well as the active com-pounds on HUA were assessed.Results A total of 148 relevant papers were collected,including 43 kinds of Chinese medicines and 61 active compounds,all of which have anti-HUA activity.Among them,41 kinds of Chinese medicines could inhibit the activity of xanthine oxidase,thus leading to the inhibition of uric acid production;and 22 kinds of Chinese medicines could facilitate uric acid excretion,while 15 kinds of Chinese medicines could reduce the inflammation levels in the body and promoting renal protection.Notably,polyphenols and flavonoids are the key active components for the uric acid-lowering effects.Conclusion This study systematically summarized and analyzed the uric acid-lowering ef-fects and mechanisms of Chinese medicines with medicine-food homology,laying a founda-tion for their development as HUA agents.展开更多
Oral diseases include periodontal and oral tumors.Current treatment methods rely largely on surgical interventions and mechanical cleaning,with a lack of targeted pharmacological therapies.Regardless,natural active co...Oral diseases include periodontal and oral tumors.Current treatment methods rely largely on surgical interventions and mechanical cleaning,with a lack of targeted pharmacological therapies.Regardless,natural active compounds have now become a new focus of research for the treatment of oral diseases owing to their low toxicity,favorable biocompatibility,and multi-target effects.This review summarizes the research progress regarding the role and application potential of natural active compounds,such as berberine and curcumin,in the prevention and treatment of oral diseases.展开更多
More than 50% of the world population is infected with Helicobacter pylori (H. pylori). The bacterium highly links to peptic ulcer diseases and duodenal ulcer, which was classified as a group I ...More than 50% of the world population is infected with Helicobacter pylori (H. pylori). The bacterium highly links to peptic ulcer diseases and duodenal ulcer, which was classified as a group I carcinogen in 1994 by the WHO. The pathogenesis of H. pylori is contributed by its virulence factors including urease, flagella, vacuolating cytotoxin A (VacA), cytotoxin-associated gene antigen (Cag A), and others. Of those virulence factors, VacA and CagA play the key roles. Infection with H. pylori vacA-positive strains can lead to vacuolation and apoptosis, whereas infection with cagA-positive strains might result in severe gastric inflammation and gastric cancer. Numerous medicinal plants have been reported for their anti-H. pylori activity, and the relevant active compounds including polyphenols, flavonoids, quinones, coumarins, terpenoids, and alkaloids have been studied. The anti-H. pylori action mechanisms, including inhibition of enzymatic (urease, DNA gyrase, dihydrofolate reductase, N-acetyltransferase, and myeloperoxidase) and adhesive activities, high redox potential, and hydrophilic/hydrophobic natures of compounds, have also been discussed in detail. H. pylori-induced gastric inflammation may progress to superficial gastritis, atrophic gastritis, and finally gastric cancer. Many natural products have anti-H. pylori-induced inflammation activity and the relevant mechanisms include suppression of nuclear factor-κB and mitogen-activated protein kinase pathway activation and inhibition of oxidative stress. Anti-H. pylori induced gastric inflammatory effects of plant products, including quercetin, apigenin, carotenoids-rich algae, tea product, garlic extract, apple peel polyphenol, and finger-root extract, have been documented. In conclusion, many medicinal plant products possess anti-H. pylori activity as well as an anti-H. pylori-induced gastric inflammatory effect. Those plant products have showed great potential as pharmaceutical candidates for H. pylori eradication and H. pylori induced related gastric disease prevention.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
Widely distributed in plants,ent-kaurane diterpenoids could reduce the incidence of inflammatory.The most important active ingredient of Isodon serra(Maxim.)Hara is ent-kaurane diterpenoids,which contribute to the ant...Widely distributed in plants,ent-kaurane diterpenoids could reduce the incidence of inflammatory.The most important active ingredient of Isodon serra(Maxim.)Hara is ent-kaurane diterpenoids,which contribute to the anti-inflammatory pharmacological effects of Isodon serra.However,the ingredients,the active compounds,drug targets,inflammatory targets and exact molecular mechanism of Isodon serra in treating inflammatory are still unclear.The purpose of this study was to use the method of network pharmacological analysis to find the active compounds in Isodon serra.These active compounds match the library of ent-kaurane diterpenoids compounds we established,and we find all the eligible ent-kaurane diterpenoids compounds.Isodon serra related and anti-inflammatory targets were found and then combined to get intersection,which represented potential anti-inflammatory targets of active compounds in Isodon serra.Moreover,anti-inflammatory targets and active compounds targets protein-protein interaction network were merged to get the protein-protein interaction network intersection and core genes in anti-inflammatory target protein-protein interaction network.For the anti-inflammatory targets of Isodon serra,Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway analysis were executed to confirm gene functions of Isodon serra in antagonizing inflammation.Finally,TCMSP analysis identified 10 active compounds out of 48 ent-kaurane.The pathway analysis showed enrichment for different pathways like AGE-RAGE signaling pathway in diabetic complications,small cell lung cancer and human cytomegalovirus infection,which were all connected to inflammatory.On the whole,the proposed method clearly identified the ent-kaurane diterpenoids of Isodon serra and the results gave the active compounds of Isodon serra for the first time.The combining use of the qualitative analysis of traditional Chinese medicine(TCM)and network pharmacological methods could discover potential drug targets and reveal the biological process of TCM,which would open up a new approach in the study of TCM in future.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
Objective To investigate and predict the molecular targets and mechanism of Huanglian Jiedu Decoction(黄连解毒汤,HLJDD)in the treatment of Corona Virus Disease 2019(COV-ID-19)through network pharmacology and molecular...Objective To investigate and predict the molecular targets and mechanism of Huanglian Jiedu Decoction(黄连解毒汤,HLJDD)in the treatment of Corona Virus Disease 2019(COV-ID-19)through network pharmacology and molecular docking analysis.Methods The chemical constituents and action targets of HLJDD were retrieved on Tradi-tional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP),SymMap v2,Encyclopedia of Traditional Chinese Medicine(ETCM),a High-throughput Ex-periment-and Reference-guided Database of Traditional Chinese Medicine(HERB),and Tra-ditional Chinese Medicine Integrated Database(TCMID).UniProt and GeneCards were used to query the target genes that corresponding to the active compounds,and then a compound-target network was constructed using Cytoscape 3.7.2.Gene Ontology(GO)database was used to annotate GO functions.Kyoto Encyclopedia of Genes and Genomes(KEGG)was used to predict the possible mechanisms of active compounds.The Database for Annotation,Visu-alization and Integrated Discovery(DAVID)was used to analysis the tissue enrichment.The main active compounds in HLJDD are molecularly docked with their corresponding related targets.Results Seventy-six compounds were screened and 458 corresponding targets in the network were obtained.Gene annotation showed that the targets were involved mainly in 1953 biolo-gical processes.884 signaling pathways was enriched,involving signaling by interleukins,cy-tokine signaling in immune system,generic transcription pathway,and RNA polymerase II transcription.The targets mainly distributed in the lung,liver,and placenta,involving a vari-ety of immune cells,such as T cells and B cells.The molecular docking results showed that core compounds such as wogonin,berberine,and baicalein had high affinity with tumor nec-rosis factor(TNF),insulin(INS),and tumor protein 53(TP53).Conclusion The active compounds in HLJDD may have a therapeutic effect on COVID-19 through regulating multiple signal pathways by targeting genes such as vascular endothelial growth factor A(VEGFA),INS,interleukin-6(IL-6),TNF,caspase-3,TP53,and mitogen-activ-ated protein kinase 3(MAPK3).展开更多
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.
文摘Basidial fungi have long been known as sources of antitumor compounds such as polysaccharides.Studies conducted by scientists from different countries demonstrate that polysaccharides and other fungal compounds(proteins,glycoproteins,terpenoids,melanins,nucleosides,etc.)exhibit antiviral activity against many viruses pathogenic for humans.The review presents data on the studied antiviral activities of higher basidial fungi against herpes,West Nile,influenza,human immunodeficiency and hepatitis viruses as well as orthopoxviruses including variola virus.Many species of basidial fungi and various classes of biologically active compounds obtained from them are capable of effectively inhibiting the development of viruses in cells and animals while possessing low toxicity.Biologically active compounds from the same fungal species can exhibit antiviral effects against different pathogens.Effective strains isolated from wild mushrooms in culture represent promising objects for the development of biotechnological drugs,including ones possessing antiviral activity.The data on antitumor and antiviral activities of compounds from the same fungal species indicate the correlation of these properties.In this connection,preparations of basidial fungi may have prophylactic value in preventing cancers of viral etiology.
基金supported by the National Key Research and Development Program of China(2022YFD1200504)the National Natural Science Foundation of China(32171857)+2 种基金China Agriculture Research System(CARS-23-A18)The“JBGS”Project of Seed Industry Revitalization in Jiangsu Province(JBGS[2021]094)the Priority Academic Program Development of Jiangsu Higher Education Institutions.
文摘Chrysanthemum is rich in active compounds such as flavonoids and phenolic acids,and its dried head flowers are commonly used for tea and medicinal purposes.However,the genetic determinism underlying chrysanthemum active compounds remains elusive.In this study,we evaluated a panel of 137 chrysanthemum accessions for total flavonoids,chlorogenic acid,luteolin,and isochlorogenic acid A across two consecutive years.The four active compounds exhibited considerable variation,with a coefficient of variation ranging from 44.96%to 76.30%.Significant differences were observed in genotype and environments,and the broad-sense heritability was estimated at 0.5e0.63 for all examined traits.Significant pair-wise correlation was found between the four active compounds.Several accessions showing the highest active compounds were figured out for breeding use by integrating the membership function and hierarchical cluster analysis methods.Based on the 327042 high-quality SNPs,a genome-wide association study(GWAS)captured 59 significant SNPs for the four active compounds,of which 24 elite alleles exhibited pyramiding effects.A total of 18 potential candidate genes were mined,among which evm.model.scaffold_1149.273(QUA1)has one linkage disequilibrium(LD)block corresponding to Hap4 with the highest luteolin content.The findings are beneficial to understanding the genetic basis of the active compounds and provide parental materials and valuable markers for the genetic improvement of active compounds in chrysanthemums.
基金Financial support from the project No.30-PCF-23-24 dated January 25,2023,subject:BR18574143“Development and implementation of groundwater purification technology and provision of drinking water to the population and animals of an agricultural enterprise”financed by Ministry of Science and Higher Education of the Republic of Kazakhstan and partial funding from RUSA and SPARC are gratefully acknowledged.
文摘Pharmaceutically active compounds(PhACs)are widely used in medical treatments but pose risks to ecosystems and human health when present in the environment.Understanding their fate in nature is complex and influenced by various factors.Phototransformation,where PhACs change chemically upon light exposure,offers the potential for reducing their environmental levels.Studying this process is crucial for understanding risks,developing safe disposal strategies,and innovating removal methods to mitigate adverse effects.This review delves into the major factors influencing the transformation of PhACs under natural conditions.It provides a comprehensive analysis of the mechanisms involved in the photochemical activity of PhACs,shedding light on their behavior upon exposure to sunlight.Special attention is given to delineating the differences in the phototransformation processes among 13 major pharmaceutical classes.By examining the various factors influencing PhAC transformation and eluci-dating their mechanisms,this review aims to contribute to a deeper understanding of the fate of pharmaceuticals in the environment.Such insights are invaluable for developing effective strategies to mitigate the risks posed by PhAC contamination and safeguarding environmental and human health.
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.
基金funded by the Key Projects in the National Science&Technology Pillar Program during the Twelfth Five-year Plan Period(No.2015BAD15B04)the National Natural Science Foundation of China(No.31600466)the Fundamental Research Funds for Jiangsu Key Laboratory of Biomass Energy and Material(No.JSBEM-S-201605)
文摘p-Menthane type monoterpene derivatives were identified as bio-based compounds with high herbicidal activities. In order to search novel p-menthane type monoterpene derivatives in good performance, a series of novel cis-p-menthane type Schiff base derivatives were designed and synthesized. All target products were easily available novel compounds and characterized by FT-IR,^1H NMR,^13 C NMR and ESI＋-MS. Their pre-emergence herbicidal activities against annual ryegrass were evaluated. The bioassays indicated that most of the target compounds displayed excellent herbicidal activities in pre-emergence treatment.
基金Supported by the National Natural Science Foundation of China(21506194,21676255)the Natural Science Foundation of Zhejiang Province(Y16B070025)the Commission of Science and Technology of Zhejiang Province(2013C03021,2017C33106)
文摘An activated carbon pore-expanding technique was achieved through innovative reactivation by CO_2/microwave.The original and modified activated carbons were characterized by nitrogen adsorption–desorption,scanning electron microscopy,transmission electron microcopy,and Fourier transform infrared spectroscopy.The mesopore volume increased from 0.122 cm^3·g^(-1) to 0.270 cm^3·g^(-1),and a hierarchical pore structure was formed.A gradual decrease in the phenolic hydroxyl and carboxyl groups on the surface of activated carbon enhanced the surface inertia of granular activated carbon(GAC).The toluene desorption rate of the modified sample increased by 8.81% compared with that of the original GAC.Adsorption isotherm fittings revealed that the Langmuir model was applicable for the original and modified activated carbons.The isosteric adsorption heat of toluene on the activated carbon decreased by approximately 50%,which endowed the modified sample with excellent stability in application.The modified samples showed an enhanced desorption performance of toluene,thereby opening a way to extend the cycle life and improve the economic performance of carbon adsorbent in practical engineering applications.
文摘According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects on leaching rate of alumina have been investigated. The results showed that the fly ash can be activated effectively and the leaching rate of alumina can be improved to more than 92% through this method. The best process parameters were the ratio of raw materials,i. e. the material weight ratio of fly ash,calcium carbonate and sodium carbonate was 1. 0∶1. 2∶0. 9. The activating temperature was 850℃-900℃,activating time was 3 h. This process has a potential application prospect and improves the value of comprehensive utilization of fly ash.
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.
基金National Key R&D Program of China(2021YFD 1600301 and 2021YFD1600105)Hunan Provincial Key Research and Development Project(2023NK2041).
文摘Objective To summarize the uric acid-lowering effects and mechanisms of Chinese medicines with medicine-food homology,aiming to provide novel perspectives for the devel-opment of new anti-hyperuricemia(HUA)drugs.Methods Papers on the research of HUA prevention and treatment with medicine-food ho-mology from December 15,2002 to August 10,2024 were screened and collected through Chi-na National Knowledge Infrastructure(CNKI),PubMed,ScienceDirect,and Google Scholar.Subsequently,the impact of these medications and their extracts,as well as the active com-pounds on HUA were assessed.Results A total of 148 relevant papers were collected,including 43 kinds of Chinese medicines and 61 active compounds,all of which have anti-HUA activity.Among them,41 kinds of Chinese medicines could inhibit the activity of xanthine oxidase,thus leading to the inhibition of uric acid production;and 22 kinds of Chinese medicines could facilitate uric acid excretion,while 15 kinds of Chinese medicines could reduce the inflammation levels in the body and promoting renal protection.Notably,polyphenols and flavonoids are the key active components for the uric acid-lowering effects.Conclusion This study systematically summarized and analyzed the uric acid-lowering ef-fects and mechanisms of Chinese medicines with medicine-food homology,laying a founda-tion for their development as HUA agents.
基金supported by grants from the Jiangsu Province Capability Improvement Project through Science,Technology and Education-Jiangsu Provincial Research Hospital Cultivation Unit(YJXYYJSDW4)Jiangsu Provincial Medical Innovation Center(CXZX202227).
文摘Oral diseases include periodontal and oral tumors.Current treatment methods rely largely on surgical interventions and mechanical cleaning,with a lack of targeted pharmacological therapies.Regardless,natural active compounds have now become a new focus of research for the treatment of oral diseases owing to their low toxicity,favorable biocompatibility,and multi-target effects.This review summarizes the research progress regarding the role and application potential of natural active compounds,such as berberine and curcumin,in the prevention and treatment of oral diseases.
文摘More than 50% of the world population is infected with Helicobacter pylori (H. pylori). The bacterium highly links to peptic ulcer diseases and duodenal ulcer, which was classified as a group I carcinogen in 1994 by the WHO. The pathogenesis of H. pylori is contributed by its virulence factors including urease, flagella, vacuolating cytotoxin A (VacA), cytotoxin-associated gene antigen (Cag A), and others. Of those virulence factors, VacA and CagA play the key roles. Infection with H. pylori vacA-positive strains can lead to vacuolation and apoptosis, whereas infection with cagA-positive strains might result in severe gastric inflammation and gastric cancer. Numerous medicinal plants have been reported for their anti-H. pylori activity, and the relevant active compounds including polyphenols, flavonoids, quinones, coumarins, terpenoids, and alkaloids have been studied. The anti-H. pylori action mechanisms, including inhibition of enzymatic (urease, DNA gyrase, dihydrofolate reductase, N-acetyltransferase, and myeloperoxidase) and adhesive activities, high redox potential, and hydrophilic/hydrophobic natures of compounds, have also been discussed in detail. H. pylori-induced gastric inflammation may progress to superficial gastritis, atrophic gastritis, and finally gastric cancer. Many natural products have anti-H. pylori-induced inflammation activity and the relevant mechanisms include suppression of nuclear factor-κB and mitogen-activated protein kinase pathway activation and inhibition of oxidative stress. Anti-H. pylori induced gastric inflammatory effects of plant products, including quercetin, apigenin, carotenoids-rich algae, tea product, garlic extract, apple peel polyphenol, and finger-root extract, have been documented. In conclusion, many medicinal plant products possess anti-H. pylori activity as well as an anti-H. pylori-induced gastric inflammatory effect. Those plant products have showed great potential as pharmaceutical candidates for H. pylori eradication and H. pylori induced related gastric disease prevention.
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Hebei Administration of Traditional Chinese Medicine(Grant No.2021133)the Natural Science Foundation of Hebei Province of China(Grant No.H2019206562)the Key Projects of Hebei Education Department(Grant No.ZD2017244)。
文摘Widely distributed in plants,ent-kaurane diterpenoids could reduce the incidence of inflammatory.The most important active ingredient of Isodon serra(Maxim.)Hara is ent-kaurane diterpenoids,which contribute to the anti-inflammatory pharmacological effects of Isodon serra.However,the ingredients,the active compounds,drug targets,inflammatory targets and exact molecular mechanism of Isodon serra in treating inflammatory are still unclear.The purpose of this study was to use the method of network pharmacological analysis to find the active compounds in Isodon serra.These active compounds match the library of ent-kaurane diterpenoids compounds we established,and we find all the eligible ent-kaurane diterpenoids compounds.Isodon serra related and anti-inflammatory targets were found and then combined to get intersection,which represented potential anti-inflammatory targets of active compounds in Isodon serra.Moreover,anti-inflammatory targets and active compounds targets protein-protein interaction network were merged to get the protein-protein interaction network intersection and core genes in anti-inflammatory target protein-protein interaction network.For the anti-inflammatory targets of Isodon serra,Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway analysis were executed to confirm gene functions of Isodon serra in antagonizing inflammation.Finally,TCMSP analysis identified 10 active compounds out of 48 ent-kaurane.The pathway analysis showed enrichment for different pathways like AGE-RAGE signaling pathway in diabetic complications,small cell lung cancer and human cytomegalovirus infection,which were all connected to inflammatory.On the whole,the proposed method clearly identified the ent-kaurane diterpenoids of Isodon serra and the results gave the active compounds of Isodon serra for the first time.The combining use of the qualitative analysis of traditional Chinese medicine(TCM)and network pharmacological methods could discover potential drug targets and reveal the biological process of TCM,which would open up a new approach in the study of TCM in future.
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National Natural Science Foundation of China(81973670)Natural Science Foundation of Hunan Province(2018JJ2297)+2 种基金Key Program of Scientific Research Fund of Hunan Provincial Education Department(19A370)Domestic First-class Cultivation Discipline Integrated Traditional Chinese and Western Medicine Discipline Project of Hunan Province(2021ZXYJH10)College Student Innovation and Entrepreneurship Training Program of Hunan Province(S201910541046).
文摘Objective To investigate and predict the molecular targets and mechanism of Huanglian Jiedu Decoction(黄连解毒汤,HLJDD)in the treatment of Corona Virus Disease 2019(COV-ID-19)through network pharmacology and molecular docking analysis.Methods The chemical constituents and action targets of HLJDD were retrieved on Tradi-tional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP),SymMap v2,Encyclopedia of Traditional Chinese Medicine(ETCM),a High-throughput Ex-periment-and Reference-guided Database of Traditional Chinese Medicine(HERB),and Tra-ditional Chinese Medicine Integrated Database(TCMID).UniProt and GeneCards were used to query the target genes that corresponding to the active compounds,and then a compound-target network was constructed using Cytoscape 3.7.2.Gene Ontology(GO)database was used to annotate GO functions.Kyoto Encyclopedia of Genes and Genomes(KEGG)was used to predict the possible mechanisms of active compounds.The Database for Annotation,Visu-alization and Integrated Discovery(DAVID)was used to analysis the tissue enrichment.The main active compounds in HLJDD are molecularly docked with their corresponding related targets.Results Seventy-six compounds were screened and 458 corresponding targets in the network were obtained.Gene annotation showed that the targets were involved mainly in 1953 biolo-gical processes.884 signaling pathways was enriched,involving signaling by interleukins,cy-tokine signaling in immune system,generic transcription pathway,and RNA polymerase II transcription.The targets mainly distributed in the lung,liver,and placenta,involving a vari-ety of immune cells,such as T cells and B cells.The molecular docking results showed that core compounds such as wogonin,berberine,and baicalein had high affinity with tumor nec-rosis factor(TNF),insulin(INS),and tumor protein 53(TP53).Conclusion The active compounds in HLJDD may have a therapeutic effect on COVID-19 through regulating multiple signal pathways by targeting genes such as vascular endothelial growth factor A(VEGFA),INS,interleukin-6(IL-6),TNF,caspase-3,TP53,and mitogen-activ-ated protein kinase 3(MAPK3).
