DNA fingerprinting among members of the Chinese drug Pu Gong Ying(Taraxacum mongolicum Hand,-Mazz.)and six adulterants of Tu Gong Ying were demonstrated with random-primed polymerase chain reaction(PCR)including arbit...DNA fingerprinting among members of the Chinese drug Pu Gong Ying(Taraxacum mongolicum Hand,-Mazz.)and six adulterants of Tu Gong Ying were demonstrated with random-primed polymerase chain reaction(PCR)including arbitrarily primed polymerase chain reaction(AP-PCR)and random amplified polymorphic DNA(RAPD).Distinctive,reproducible genomic fingerprints from DNA from 7 species belonged to Compositae were generated with two long(20 and 24 mer)and one short(10 mer)randomly chosen primers.The Pu Gong Ying can be differentiated from six species of Tu Gong Ying according to the banding pattems of their amplified DNA on agarose gels.The results showed that AP-PCR and RAPD methods can be used for identifying Chinese drugs.Moreover,the Similarity Indexes of the genomic DNA fingerprints showed that Pu Gong Ying and its adulterants are unrelated.Therefore,AP-PCR and RAPD methods can be used for identifying Chinese drugs.展开更多
Near infrared(NIR)spectrum analysis technology has outstanding advantages such as rapid,nondestructive,pollution-free,and is widely used in food,pharmaceutical,petrochemical,agricultural products production and testin...Near infrared(NIR)spectrum analysis technology has outstanding advantages such as rapid,nondestructive,pollution-free,and is widely used in food,pharmaceutical,petrochemical,agricultural products production and testing industries.Convolutional neural network(CNN)is one of the most successful methods in big data analysis because of its powerful feature ex-traction and abstraction ability,and it is especially suitable for solving multi-classification problems.CNN-based transfer learning is a machine learning technique,which migrates para-meters of trained model to the new one to improve the performance.The transfer learning strategy can speed up the learning efficiency of the model instead of learning from scratch.In view of the difficulty in acquisition of drug NIR spectral data and high labeling cost,this paper proposes three simple but very effective transfer learning methods for multi-manufacturer identification of drugs based on one-dimensional CNN.Compared with the original CNN,the transfer learning method can achieve better classification performance with fewer NIR spectral data,which greatly reduces the dependence on labeled NIR spectral data.At the same time,this paper also compares and discusses three different transfer learning methods,and selects the most suitable transfer learning model for drug NIR spectral data analysis.Compared with the current popular methods,such as SVM,BP,AE and ELM,the proposed method achieves higher classification accuracy and scalability in multi-variety and multi-manufacturer NIR spectrum classification experiments.展开更多
A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors i...A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors is constructed with IBX mediated oxidation.Biological assay on five tumor cell lines indicates that four Michael acceptors,8a,11a,12a,14a,are with improved cytotoxicity(3-10 folds more potent than the parent compounds),which merit further investigations.Further thiol-sensitive assay of the active hit 8a revealed that it was an irreversible Michael acceptor.The results suggest that the strategy is not only effective and relatively high discovery rate(28%),but also resource saving.展开更多
Dihydroorotate dehydrogenase(DHODH)is a central enzyme of the de novo pyrimidine biosynthesis pathway and is a promising drug target for the treatment of cancer and autoimmune diseases.This study presents the identifi...Dihydroorotate dehydrogenase(DHODH)is a central enzyme of the de novo pyrimidine biosynthesis pathway and is a promising drug target for the treatment of cancer and autoimmune diseases.This study presents the identification of a potent DHODH inhibitor by proteomic profiling.Cell-based screening revealed that NPD723,which is reduced to H-006 in cells,strongly induces myeloid differentiation and inhibits cell growth in HL-60 cells.H-006 also suppressed the growth of various cancer cells.Proteomic profiling of NPD723-treated cells in ChemProteoBase showed that NPD723 was clustered with DHODH inhibitors.H-006 potently inhibited human DHODH activity in vitro,whereas NPD723 was approximately 400 times less active than H-006.H-006-induced cell death was rescued by the addition of the DHODH product orotic acid.Moreover,metabolome analysis revealed that H-006 treatment promotes marked accumulation of the DHODH substrate dihydroorotic acid.These results suggest that NPD723 is reduced in cells to its active metabolite H-006,which then targets DHODH and suppresses cancer cell growth.Thus,H-006-related drugs represent a potentially powerful treatment for cancer and other diseases.展开更多
Affinity core-shell magnetic nanoparticles (MNPs) were prepared for identifying the target proteins of drugs in the cell lysate when used in combination with nano-high-performance liquid chromatography tandem mass s...Affinity core-shell magnetic nanoparticles (MNPs) were prepared for identifying the target proteins of drugs in the cell lysate when used in combination with nano-high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS)-based shotgun proteomic analysis. A number of new potential targets of cyclosporine A (CsA) could be identified, owing to the high efficacy of the affinity MNPs in drug target identification. To the best of our knowledge, this is the first time to reveal such an abundant target spectrum of CsA.展开更多
Based on literature reviews and analysis of research reports on Pinellia ternata found locally and abroad in recent years,this article summarizes and arranges them.The research on Pinellia ternata mainly focuses on it...Based on literature reviews and analysis of research reports on Pinellia ternata found locally and abroad in recent years,this article summarizes and arranges them.The research on Pinellia ternata mainly focuses on its cultivation,tissue culture,and so on.There are only a few research on its active components and its regulation mechanism.The wild resources of Pinellia ternata are gradually decreasing,hence it is urgent to take effective measures to protect these wild resources as well as to establish germplasm resources bank and nursery.In order to meet the needs of the domestic market,it is necessary to investigate the distribution of wild Pinellia ternata resources,explore the best growing environment and conditions,artificially cultivate Pinellia ternata,as well as implement resource industrialization,sustainable development,and utilization.展开更多
[Objectives]This study was conducted to investigate the quality standard of Heracleum moellendorffii Hance.,so as to provide data support for the 2003 version of Quality Standards for Chinese Medicinal Materials and E...[Objectives]This study was conducted to investigate the quality standard of Heracleum moellendorffii Hance.,so as to provide data support for the 2003 version of Quality Standards for Chinese Medicinal Materials and Ethnic Medicinal Materials in Guizhou Province.[Methods]H.moellendorffii was subjected to character identification and microscopic identification.Referring to Chinese Pharmacopoeia,TCL thin-layer identification and extract determination were carried out on 10 batches of H.moellendorffii from 6 habitats in Guizhou.[Results]The characters and microscopic characteristics of H.moellendorffii were described in detail.The TLC thin-layer identification spots were clear,with strong specificity.The limit of the medicinal material extract was determined to be not less than 22.0%.[Conclusions]This study can provide data support for the quality evaluation and standard improvement of the medicinal material H.moellendorffii.展开更多
文摘DNA fingerprinting among members of the Chinese drug Pu Gong Ying(Taraxacum mongolicum Hand,-Mazz.)and six adulterants of Tu Gong Ying were demonstrated with random-primed polymerase chain reaction(PCR)including arbitrarily primed polymerase chain reaction(AP-PCR)and random amplified polymorphic DNA(RAPD).Distinctive,reproducible genomic fingerprints from DNA from 7 species belonged to Compositae were generated with two long(20 and 24 mer)and one short(10 mer)randomly chosen primers.The Pu Gong Ying can be differentiated from six species of Tu Gong Ying according to the banding pattems of their amplified DNA on agarose gels.The results showed that AP-PCR and RAPD methods can be used for identifying Chinese drugs.Moreover,the Similarity Indexes of the genomic DNA fingerprints showed that Pu Gong Ying and its adulterants are unrelated.Therefore,AP-PCR and RAPD methods can be used for identifying Chinese drugs.
基金supported by National Key R&D Program(Grant No.2018AAA0102600)National Natural Science Foundation of China(Grant No.61906050)+1 种基金Guangxi Technology,R&D,Program(Grant No.2018AD11018)Guangxi University Young and Middle-aged Teachers'Research Ability Improvement Project(Grant No.2020KY05034)
文摘Near infrared(NIR)spectrum analysis technology has outstanding advantages such as rapid,nondestructive,pollution-free,and is widely used in food,pharmaceutical,petrochemical,agricultural products production and testing industries.Convolutional neural network(CNN)is one of the most successful methods in big data analysis because of its powerful feature ex-traction and abstraction ability,and it is especially suitable for solving multi-classification problems.CNN-based transfer learning is a machine learning technique,which migrates para-meters of trained model to the new one to improve the performance.The transfer learning strategy can speed up the learning efficiency of the model instead of learning from scratch.In view of the difficulty in acquisition of drug NIR spectral data and high labeling cost,this paper proposes three simple but very effective transfer learning methods for multi-manufacturer identification of drugs based on one-dimensional CNN.Compared with the original CNN,the transfer learning method can achieve better classification performance with fewer NIR spectral data,which greatly reduces the dependence on labeled NIR spectral data.At the same time,this paper also compares and discusses three different transfer learning methods,and selects the most suitable transfer learning model for drug NIR spectral data analysis.Compared with the current popular methods,such as SVM,BP,AE and ELM,the proposed method achieves higher classification accuracy and scalability in multi-variety and multi-manufacturer NIR spectrum classification experiments.
基金We thanked the National Natural Science Foundation of China(No.90813004,U0932602,20802083 and 973 Program No.2009CB522303 and No.2011CB915503)the State Key Laboratory of Phytochemistry and Plant Resources in West China(P2010-ZZ18)for financial support.
文摘A potential strategy for drug lead identification and in-active natural products re-discovery is elaborated.Starting from fifteen structurally diverse natural products,a focused library featured by Michael acceptors is constructed with IBX mediated oxidation.Biological assay on five tumor cell lines indicates that four Michael acceptors,8a,11a,12a,14a,are with improved cytotoxicity(3-10 folds more potent than the parent compounds),which merit further investigations.Further thiol-sensitive assay of the active hit 8a revealed that it was an irreversible Michael acceptor.The results suggest that the strategy is not only effective and relatively high discovery rate(28%),but also resource saving.
基金supported by AMED Grants(Nos.JP16cm0106112 and JP16cm0106002)JSPS KAKENHI Grants(Nos.JP17H06412,18H05503,JP19K05744,JP20K05857,JP20H05620,JP21H04720,JP22H04922,and JP22K05363).
文摘Dihydroorotate dehydrogenase(DHODH)is a central enzyme of the de novo pyrimidine biosynthesis pathway and is a promising drug target for the treatment of cancer and autoimmune diseases.This study presents the identification of a potent DHODH inhibitor by proteomic profiling.Cell-based screening revealed that NPD723,which is reduced to H-006 in cells,strongly induces myeloid differentiation and inhibits cell growth in HL-60 cells.H-006 also suppressed the growth of various cancer cells.Proteomic profiling of NPD723-treated cells in ChemProteoBase showed that NPD723 was clustered with DHODH inhibitors.H-006 potently inhibited human DHODH activity in vitro,whereas NPD723 was approximately 400 times less active than H-006.H-006-induced cell death was rescued by the addition of the DHODH product orotic acid.Moreover,metabolome analysis revealed that H-006 treatment promotes marked accumulation of the DHODH substrate dihydroorotic acid.These results suggest that NPD723 is reduced in cells to its active metabolite H-006,which then targets DHODH and suppresses cancer cell growth.Thus,H-006-related drugs represent a potentially powerful treatment for cancer and other diseases.
基金the National Natural Science Foundations of China,the National Key Laboratory of Organic Biochemistry Opening Foundations
文摘Affinity core-shell magnetic nanoparticles (MNPs) were prepared for identifying the target proteins of drugs in the cell lysate when used in combination with nano-high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS)-based shotgun proteomic analysis. A number of new potential targets of cyclosporine A (CsA) could be identified, owing to the high efficacy of the affinity MNPs in drug target identification. To the best of our knowledge, this is the first time to reveal such an abundant target spectrum of CsA.
基金Supported by Ankang Science and Technology Bureau,Shaanxi Province(2018ak03-ll)National Traditional Chinese Medicine Characteristic Technology Inheritor(t20194828003).
文摘Based on literature reviews and analysis of research reports on Pinellia ternata found locally and abroad in recent years,this article summarizes and arranges them.The research on Pinellia ternata mainly focuses on its cultivation,tissue culture,and so on.There are only a few research on its active components and its regulation mechanism.The wild resources of Pinellia ternata are gradually decreasing,hence it is urgent to take effective measures to protect these wild resources as well as to establish germplasm resources bank and nursery.In order to meet the needs of the domestic market,it is necessary to investigate the distribution of wild Pinellia ternata resources,explore the best growing environment and conditions,artificially cultivate Pinellia ternata,as well as implement resource industrialization,sustainable development,and utilization.
基金Science and Technology Innovation Platform Construction Project of Anshun City(ASKP[2017]03).
文摘[Objectives]This study was conducted to investigate the quality standard of Heracleum moellendorffii Hance.,so as to provide data support for the 2003 version of Quality Standards for Chinese Medicinal Materials and Ethnic Medicinal Materials in Guizhou Province.[Methods]H.moellendorffii was subjected to character identification and microscopic identification.Referring to Chinese Pharmacopoeia,TCL thin-layer identification and extract determination were carried out on 10 batches of H.moellendorffii from 6 habitats in Guizhou.[Results]The characters and microscopic characteristics of H.moellendorffii were described in detail.The TLC thin-layer identification spots were clear,with strong specificity.The limit of the medicinal material extract was determined to be not less than 22.0%.[Conclusions]This study can provide data support for the quality evaluation and standard improvement of the medicinal material H.moellendorffii.