Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 26
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Steroids ; 151: 108465, 2019 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-31351940

RESUMO

The incorporation of the heterocycles into the steroid nucleus has been recognized as a useful strategy to develop new steroidal agents for disease treatment. Representative examples are abiraterone and galeterone, which are presently used in clinic for the treatment of advanced prostate cancers. Herein we have developed the first Al2O3/KF-promoted pfitzinger reactions for the synthesis of new steroidal quinolines. These new steroidal quinolines showed moderate to good antiproliferative activity against several human lung cancer cells. Of these compounds, compound 2f exhibited the best potency toward the tested three lung cancer cells with IC50 values <10 µM. Mechanistic studies showed that compound 2f concentration-dependently inhibited colony formation, morphological changes, apoptosis, and migration of A549 cells. To conclude, compound 2f could be used as a hit compound for developing steroid-based anti-lung cancer agents.

2.
J Biol Chem ; 294(38): 13915-13927, 2019 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-31350334

RESUMO

Replication protein A (RPA) is the major eukaryotic ssDNA-binding protein and has essential roles in genome maintenance. RPA binds to ssDNA through multiple modes, and recent studies have suggested that the RPA-ssDNA interaction is dynamic. However, how RPA alternates between different binding modes and modifies ssDNA structures in this dynamic interaction remains unknown. Here, we used single-molecule FRET to systematically investigate the interaction between human RPA and ssDNA. We show that RPA can adopt different types of binding complexes with ssDNAs of different lengths, leading to the straightening or bending of the ssDNAs, depending on both the length and structure of the ssDNA substrate and the RPA concentration. Importantly, we noted that some of the complexes are highly dynamic, whereas others appear relatively static. On the basis of the above observations, we propose a model explaining how RPA dynamically engages with ssDNA. Of note, fluorescence anisotropy indicated that RPA can also associate with RNA but with a lower binding affinity than with ssDNA. At the single-molecule level, we observed that RPA is undergoing rapid and repetitive associations with and dissociation from the RNA. This study may provide new insights into the rich dynamics of RPA binding to ssDNA and RNA.

3.
Zhongguo Zhong Yao Za Zhi ; 44(3): 574-581, 2019 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-30989925

RESUMO

The Chinese medicine is mostly derived from plants or animals, highly polymorphic, with dynamic components which are reflected by the characteristic peaks and fingerprint peaks in chromatographic fingerprints. The chromatopharmacokinetics method for determined components is not applicable due to dynamic changes of chromatopharmacokinetics. Based on the preliminary study, dynamic pharmacokinetics mathematical model for multiple components in Chinese medicine was set up and verified by Buyang Huanwu Decoction as the model drug, applying the principle of the total quantum statistical moment(TQSM), superimposing or subtracting the relevant statistical parameters in blood samples and blank samples. This provided a new method for the chromatopharmacokinetic study of Chinese medicine. HPLC was used to determine the TQSM parameters in blood and blank sample fingerprints of Buyang Huanwu Decoction at each point, and the overall TQSM parameters of drug-containing blood sample and blank samples were obtained with addition calculation of TQSM; while the initial TQSM of the pure drug can be obtained with subtraction calculation. The metabolic and absorption equilibrium constants were calculated iteratively to a steady state using the estimated metabolic equilibrium constants, then the metabolic chromatopharmacokinetic parameters in rats were obtained: VUC_T 1.262×10~8 mAu·s, MRT_T 37.48 h, VRT_T 9.016×10~2 h~2, CL_T 25.79 mL·h~(-1)·kg~(-1), Vs 1.586×10~2 mL·kg~(-1), t_(T,0.5) 6.15 h, respectively. This suggested that 95% of the compounds in whole recipe were metabolized and secreted from the body after 0-96.33 h. The experiment verified that the established mathematical model and the total quantum moment statistics parameters can represent the dose-time relationship of Buyang Huanwu Decoction, which can be used to study on in vivo metabolism dynamics for Chinese medicine.


Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Animais , Cromatografia Líquida de Alta Pressão , Ratos
4.
Data Brief ; 20: 805-811, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30211279

RESUMO

This data article contains descriptive and experimental data on the construction, expression, and simple characterization of AG11-843 and AG11-1581. AG1 is an important member of the DUF1220 protein family. It׳s hard to get the recombinant protein because of its DNA sequence. The DNA sequence were optimized by proper design, cloned by overlap PCR and constructed into expression vector. AG11-843 and AG11-1581.were over expressed in Escherichia coli, purified and analyzed by dynamic light scattering and gel filtration analysis. An effective technique is provided to construct and express proteins with complicated sequences.

5.
Protein Expr Purif ; 152: 71-76, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29870801

RESUMO

AG1, a member of the DUF1220 protein family, exhibits the most extreme human lineage-specific copy number expansion of any protein-coding sequence in the genome. These variations in copy number have been linked to both brain evolution among primates and brain size in humans. Unfortunately, our current understanding of the structure and function of these proteins is limited because current cloning and expression techniques fail to consistently produce recombinant protein for in vitro studies. The present work describes a method for amino acid and DNA sequence optimization and synthesis, recombinant protein expression and analysis of two AG1 fragments, AG11-843 and AG11-1581. It was first necessary to modify the nucleotide sequence, while holding the GC content at 52.9%. The genes were then sectionally synthesized by overlap PCR. The resulting segments were cloned into the pET-15 b-sumo expression vector and subsequently transformed into BL21 (DE3) cells. After inducing their expression, the AG11-843 and AG11-1581 proteins were isolated and purified. Furthermore, using dynamic light scattering and gel filtration analysis, AG11-843 and AG11-1581 were shown to be present in tetrameric and dimeric forms in solution. To our knowledge, this is the first study to synthesize and express fragments of the DUF1220 protein family for in vitro analysis. Taken together, the proven utility and versatility of this method indicate that it can be used as an effective technique to construct and express other proteins with complicated sequences, thus providing the means to study their function and structure in vitro.

6.
Phytomedicine ; 45: 68-75, 2018 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-29699843

RESUMO

BACKGROUND: Nowadays, to research and formulate an efficiency extraction system for Chinese herbal medicine, scientists have always been facing a great challenge for quality management, so that the transitivity of Q-markers in quantitative analysis of TCM was proposed by Prof. Liu recently. In order to improve the quality of extraction from raw medicinal materials for clinical preparations, a series of integrated mathematic models for transitivity of Q-markers in quantitative analysis of TCM were established. Buyanghuanwu decoction (BYHWD) was a commonly TCMs prescription, which was used to prevent and treat the ischemic heart and brain diseases. In this paper, we selected BYHWD as an extraction experimental subject to study the quantitative transitivity of TCM. STUDY DESIGN: Based on theory of Fick's Rule and Noyes-Whitney equation, novel kinetic models were established for extraction of active components. Meanwhile, fitting out kinetic equations of extracted models and then calculating the inherent parameters in material piece and Q-marker quantitative transfer coefficients, which were considered as indexes to evaluate transitivity of Q-markers in quantitative analysis of the extraction process of BYHWD. METHODS: HPLC was applied to screen and analyze the potential Q-markers in the extraction process. Fick's Rule and Noyes-Whitney equation were adopted for mathematically modeling extraction process. Kinetic parameters were fitted and calculated by the Statistical Program for Social Sciences 20.0 software. The transferable efficiency was described and evaluated by potential Q-markers transfer trajectory via transitivity availability AUC, extraction ratio P, and decomposition ratio D respectively. The Q-marker was identified with AUC, P, D. RESULTS: Astragaloside IV, laetrile, paeoniflorin, and ferulic acid were studied as potential Q-markers from BYHWD. The relative technologic parameters were presented by mathematic models, which could adequately illustrate the inherent properties of raw materials preparation and affection of Q-markers transitivity in equilibrium processing. AUC, P, D for potential Q-markers of AST-IV, laetrile, paeoniflorin, and FA were obtained, with the results of 289.9 mAu s, 46.24%, 22.35%; 1730 mAu s, 84.48%, 1.963%; 5600 mAu s, 70.22%, 0.4752%; 7810 mAu s, 24.29%, 4.235%, respectively. CONCLUSION: The results showed that the suitable Q-markers were laetrile and paeoniflorin in our study, which exhibited acceptable traceability and transitivity in the extraction process of TCMs. Therefore, these novel mathematic models might be developed as a new standard to control TCMs quality process from raw medicinal materials to product manufacturing.


Assuntos
Biomarcadores Farmacológicos/análise , Medicamentos de Ervas Chinesas/química , Modelos Teóricos , Amigdalina/análise , Fracionamento Químico , Cromatografia Líquida de Alta Pressão , Ácidos Cumáricos/análise , Medicamentos de Ervas Chinesas/análise , Glucosídeos/análise , Cinética , Monoterpenos/análise , Saponinas/análise , Triterpenos/análise
7.
Acta Crystallogr C Struct Chem ; 74(Pt 3): 381-385, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29504569

RESUMO

The nucleoside analogue entecavir {systematic name: 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-1,9-dihydro-6H-purin-6-one}, C12H15N5O3, is an antihepatitis B virus drug that has been approved in the US, EU and several countries worldwide. We report here the single-crystal structure of the anhydrous form and compare it with that of the previously reported monohydrate form [Jiang & Liu (2009). Acta Cryst. E65, o2232]. Hirshfeld surface analysis has been employed to understand and visualize the subtle packing differences between the two crystalline forms. The results show that, compared to the previously reported hydrated form, the anhydrous crystal has significantly different intermolecular interactions and packing patterns.


Assuntos
Guanina/análogos & derivados , Nucleosídeos/química , Cristalografia por Raios X , Guanina/química , Ligações de Hidrogênio
8.
Phytomedicine ; 45: 18-25, 2018 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-29555366

RESUMO

BACKGROUND: It is well-known that the public still have been facing on a severe issue about the inconsistency of quality and therapeutic efficacy of traditional medicines. Recently, Professor Chang-Xiao Liu has created a new promising concept for identifying relevant quality-markers (Q-marker) from herbs, their formulas and manufacturing products. Therefore, building up a new approach is necessary for us to bridge over quality to efficacy of pharmaceutical products. STUDY DESIGN: In this paper, five candidate Q-markers, astragaloside IV, paeonflorin, amygdalin, tetramethylpyrazine, ferulic acid in Buyanghuanwu injection (BYHWI) had been designed to carry out in rat by using single and polypharmacokinetic models for total quanta to ascertain adequate Q-marker. METHODS: The Q-marker transitivity in vivo was studied with polypharmacokinetic model and its similarity approach, which were modeled with TQSM principle. The Q-marker was ascertained with transitive similarity and bioavailability in polypharmacokinetics. Their concentrations in plasma sample of white rat were determined by RP-HPLC. Data analyses were used by the DAS software for singles and myself-written-program with EXCEL for multiples. RESULTS: In BYHWI, five candidate Q-marker pharmacokinetic profiles were singly fixed to two compartmental models in rat using classical compartmental analysis, but there were tremendous differences among which the candidate parameters were fluctuated from nearly 3552 folds to equivalency. The theoretical value of TQSM polypharmacokinetic parameters such as AUCT, MRTT, VRTT, CLT, VT over the mixure of five drugs were 110.8 ±â€¯51.91 mg min ml-1, 176.0 ±â€¯36.5 min, 39,921 ±â€¯4311 min2, 0.3116 ±â€¯0.02347 ml min-1 kg-1, 54.83 ±â€¯7.683 ml kg-1 respectively. The TQSM polypharmacokinetic parameters in astragaloside Ⅳ ordered by AUCT, MRTT, VRTT, CLT, VT were 110.8 ±â€¯51.91 mg min ml-1, 176.0 ±â€¯36.5 min, 39,921 ±â€¯4311 min2, 0.3116 ±â€¯0.02347 ml min-1 kg-1, 54.83 ±â€¯7.683 ml kg-1, respectively, which were closed to the theoretical values. TQSM similarity versus astragaloside Ⅳ was 0.9661. CONCLUSION: The results represented that the optimum Q-marker in BYHWI is astragaloside Ⅳ, whose transitivity in vivo similarity was close to the behavior of polypharmacokinetics with maximum bioavailability to the total quanta. It is feasible for Q-marker in CMMs to screen on the comparison of single pharmacokinetic behavior and bioavailability to the total quanta.


Assuntos
Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacocinética , Amigdalina/sangue , Amigdalina/farmacocinética , Animais , Disponibilidade Biológica , Biomarcadores/sangue , Cromatografia Líquida de Alta Pressão/métodos , Ácidos Cumáricos/sangue , Ácidos Cumáricos/farmacocinética , Medicamentos de Ervas Chinesas/administração & dosagem , Glucosídeos/sangue , Glucosídeos/farmacocinética , Injeções , Monoterpenos/sangue , Monoterpenos/farmacocinética , Pirazinas/sangue , Pirazinas/farmacocinética , Ratos Wistar , Saponinas/sangue , Saponinas/farmacocinética , Triterpenos/sangue , Triterpenos/farmacocinética
9.
Curr Med Chem ; 25(19): 2233-2244, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29189121

RESUMO

BACKGROUND: Antibiotic resistance is one of the biggest threats to global health today, leading to higher medical costs and increased mortality. Because of the emergence and rapid spread of new resistance mechanisms globally, a growing number of infections are becoming harder to treat as the antibiotics used to treat them become less effective. Therefore, the development of new effective antimicrobial agents is still urgently needed. In last decades, a large number of structurally novel spirooxindoles have been synthesized mainly based on the ylide intermediates generated in situ and further assessed for their antimicrobial activity against different types of bacteria, leading to the discovery of some potent lead compounds with antimicrobial potentials. OBJECTIVE: The aim of this review to submarize recent advances on the synthesis, structure- activity relationship studies (SARs) and antimicrobial activity of spirooxindoles. METHODS: Peer-reviewed research work on spirooxindoles with antimicrobial activity were downloaded from bibliographic databases and analyzed based on their chemoptypes. RESULTS: 50 papers were retrieved from the literature databases, of which 20 papers described the synthesis and antimicrobial activity of spirooxindoles. CONCLUSION: This review highlights the importance of spirooxindoles as potential antimicrobial agents. The antimicrobial activity of spirooxindoles against different types of bacteria is less studied, mainly centering on primary antimicrobial assessment, some of these compounds have showed interesting antimicrobial activity. However, the current study is only limited to primary antimicrobial assessment, no detailed modes of action are investigated.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Indóis/farmacologia , Compostos de Espiro/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Indóis/síntese química , Indóis/química , Estrutura Molecular , Compostos de Espiro/síntese química , Compostos de Espiro/química , Relação Estrutura-Atividade
10.
Zhongguo Zhong Yao Za Zhi ; 42(12): 2420-2424, 2017 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-28822202

RESUMO

The effect of Chinese medicine (CM) compound prescription is the combined action results of single herbs based on the basic theory of Chinese medicine, and its function embodies the characteristics of multi components, multi targets and comprehensive effects. It is difficult to study the therapeutic material, establish quality standards or determine Q-marker, so we can't strictly monitor the quality of the whole process of CM. The identification of Q-marker has a profound influence on the whole process of the pharmaceutical engineering of CM. The scattered effect of CM multi-components is regarded as the integral action of the parent nucleus group by the metabolic rule of co-network compatibility and rainbow potential (CCRP). The rule can be used to communicate the individual components and macro components, to reveal the metabolism of CM in organism body and basic law of information exchange, thus revealing the action law of CM on human body. Through the systematic analysis of the Q-marker's guidance to the development of CM and its relationship with the metabolic rule of CCRP, we try to provide some ideas for the identification of Q-marker.


Assuntos
Biomarcadores , Medicamentos de Ervas Chinesas/normas , Prescrições de Medicamentos , Humanos , Medicina Tradicional Chinesa , Padrões de Referência
11.
J Biochem ; 162(3): 183-191, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28338731

RESUMO

Mutations in human BLM helicase give rise to the autosomal recessive Bloom syndrome, which shows high predisposition to types of malignant tumours. Though lots of biochemical and structural investigations have shed lights on the helicase core, structural investigations of the whole BLM protein are still limited due to its low stability and production. Here by comparing with the expression systems and functions of other BLM homologues, we developed the heterologous high-level expression and high-yield purification systems for Gallus gallus BLM (gBLM) in Escherichia coli. Subsequent DNA binding and unwinding determinations demonstrated that gBLM was a vigorous atypical DNA structure specific helicase, which not only showed high preference for the 3'-tailed DNA structures but also could efficiently unwind bubble DNA structures with blunt-ends, indicating its biological roles in processing DNA metabolism intermediates. Further comparative analysis between gBLM and gBLM Core revealed that the long N-terminal domain facilitated the binding affinity of forked and bubble DNA structures and it was also required for the DNA unwinding activities of gBLM. Thus, we present the first enzymatic characterization of gBLM and its N-terminal domain, providing a new model for probing the mechanism and structure of human BLM.


Assuntos
RecQ Helicases/isolamento & purificação , RecQ Helicases/metabolismo , Animais , Galinhas
12.
Chem Biol Drug Des ; 89(5): 806-814, 2017 05.
Artigo em Inglês | MEDLINE | ID: mdl-27862991

RESUMO

Previous studies have demonstrated that miRNAs play an important role in tumor development and progression. The role of miR-320d has been studied in several cancers except for glioma. The aim of the study was to investigate the expression levels, biological function, and mechanism of miR-320d in glioma. The expression levels of miR-320d were detected in glioma tissues and cell lines (U87 and U251) by RT-qPCR. Cell proliferation, colony formation, apoptosis, cell cycle, and transwell assays were performed in glioma cell lines transfected with miR-320d mimics or controls to evaluate the effects of miR-320d in vitro. The expression levels of invasive-related proteins were determined by Western blot analysis. Results showed that the expression of miR-320d was significantly decreased in glioma tissues and cell lines. Overexpression of miR-320d could significantly suppress cell growth, migration and invasion, and induced cell apoptosis as well as cell cycle at G0/G1 arrest in U87 and U251 cell lines. Additionally, expression levels of MMP-2, MMP-9, N-cadherin, and integrin-ß1 reduced, while E-cadherin increased in miR-320d mimic group. Overall, this study is the first to demonstrate that miR-320d may serve as an independent prognostic factor, indicating that miR-320d is a biomarker for prognosis and therapy in glioma.


Assuntos
Neoplasias Encefálicas/genética , Glioma/genética , MicroRNAs/metabolismo , Adulto , Antagomirs/metabolismo , Apoptose , Neoplasias Encefálicas/mortalidade , Neoplasias Encefálicas/patologia , Caderinas/genética , Caderinas/isolamento & purificação , Pontos de Checagem do Ciclo Celular , Linhagem Celular Tumoral , Movimento Celular , Proliferação de Células , Regulação para Baixo , Feminino , Glioma/mortalidade , Glioma/patologia , Humanos , Estimativa de Kaplan-Meier , Masculino , Metaloproteinase 2 da Matriz/genética , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/genética , Metaloproteinase 9 da Matriz/metabolismo , MicroRNAs/antagonistas & inibidores , MicroRNAs/genética , Pessoa de Meia-Idade , Análise Multivariada , Prognóstico , Modelos de Riscos Proporcionais
13.
Zhongguo Zhong Yao Za Zhi ; 41(2): 345-349, 2016 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28861984

RESUMO

The (anaphylactoid) hypersensibility mechanism of ″imprinting templates″ characteristics of traditional Chinese medicine (TCM) injection supramolecules was clarified to lay the foundation to build safety evaluation method. Based on the previous publication on special impact of Chinese medicine theories on supramolcular chemistry, combined with the natural origination of (anaphylactoid) hypersensitized special rules as well as the sensitization phenomenon of cordate houttuynia injection, the impact of the structure characteristics of ″imprinting templates″ in TCM injection supramolecules on its (anaphylactoid) hypersensibility was clarified. In Chinese medicine injections, the supramolecular structures can independently be generated, showing overall apparent (anaphylactoid) hypersensibility nature, and their structure characteristics were dependent on the strength. In addition, (anaphylactoid) hypersensitive critical supramolecular structure was present. When it was administrated by ″injection″, it's structure was not easy to be destroyed, often showing apparent immunogenicity, whereas if it was administrated by ″oral″, the structure would be destroyed by the gastrointestinal tract, showing weaker or no apparent immunogenicity. Therefore, there are differences in (anaphylactoid) hypersensibility between ″injection″ and ″oral″ administration of TCM. TCM injections would produce the supramolecules between ″molecular society″ by independent reaction of supramolecular ″imprinting template″ (chemical determinants), showing apparent immune process of recognition, copying, and storage. Single molecule is a special example for this. The screening of anaphylactoid (sensitinogen) includes the single ingredients and their forming supramolecules for TCM injection. This is the unique feature for safety evaluation of Chinese medicine injection.


Assuntos
Hipersensibilidade a Drogas/etiologia , Medicamentos de Ervas Chinesas/efeitos adversos , Medicamentos de Ervas Chinesas/síntese química , Hipersensibilidade a Drogas/imunologia , Medicamentos de Ervas Chinesas/administração & dosagem , Humanos , Injeções , Medicina Tradicional Chinesa , Impressão Molecular
14.
Zhongguo Zhong Yao Za Zhi ; 41(6): 1040-1045, 2016 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-28875667

RESUMO

The study focused on the in vitro release of Buyanghuanwu (BYHW) elementary osmotic pump sustained release tablets. Its band similarity was calculated by the total quantum statistical moment. Meanwhile, in vitro release characteristics were analyzed to discuss the existence of supramolecular imprinting templates. The results show that the same imprint templates may exist in different structures of traditional Chinese medicine(TCM)'s multi-components. The BYHW sustained release tablets prepared by elementary osmotic pump can meet the objectives of "overall control, synchronous release". However, the supramolecular imprinting templates in TCM compound prescriptions should be further explored, the overall and synchronous release of different components was controlled through imprinting templates, so as to seek the more suitable sustained release preparation technology for multiple components of TCM, and make it in line with the characteristics of TCM.


Assuntos
Preparações de Ação Retardada/química , Medicamentos de Ervas Chinesas/química , Química Farmacêutica , Impressão Molecular , Solubilidade , Comprimidos/química
15.
Zhongguo Zhong Yao Za Zhi ; 41(6): 1152-1160, 2016 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-28875686

RESUMO

More and more disputes have happened to confront us continuously since the separation of Japanese(wild) honeysuckle flower in Chinese Pharmacopoeia in 2005. The state pharmacopeia committee decided to separate Japanese(wild) honeysuckle flower into two species for japanese(wild) honeysuckle flower, but didn't define their the convincing reasons still did not provide to us as a result that two medicines are not described the differences in natural properties, efficiency and indication, usage and dosage, as well as not given a resolving methodand specific solution. It was known for us that in the history of traditional Chinese medicine(TCM), the phenomenenphenomena of the "one drug from multi-species" and "one species for multi-drug" are very ordinary thingswere ubiquitous. Whether separation of the drug species are separated shall be decided to by clinical efficiency. Through Chinese pharmacopoeia (2015 edition) issue of Chinese Pharmacopoeia the 2015 issue of the Chinese Pharmacopoeia, we still cannot find a scientific solution for the dispute of for Japanese (wild) honeysuckle flower, perhaps because of insufficient reorganization of TCM clinical medication regularities, such as "treatment of different diseases with same drug", " treatment of the same disease with different drugs" and "treatment of the same syndrome with multi-prescriptions", and "one prescription treating multiple syndromes"; lack of in-depth analysis for multi-component TCM compounds and autonomisation of "supermolecular template" for organs and meridians; less attention to the advance of efficacy and safety evaluation technologies for multi-component TCM compounds; impacts from the medication mode of "one ingredient-one composition-one effect"; as well as insufficient research methods for bioequivalent evaluation in preclinic and clinic studies . The dispute for species combination or separation for Japanese(wild) honeysuckle flower was apparently caused by regional economy, drug biological equivalent of efficacy and safety, but arising from clinical principles for systematical syndrome treatment with TCM, or concepts in the treatment of diseases with TCM or western medicines. This paper focused on current studies on Japanese(wild) honeysuckle flower in the combination with TCM clinical medication regularities, such as "treatment of different diseases with same drug", "treatment of the same disease with different drugs" and "treatment of the same syndrome with multi-prescriptions", and "one prescription treating multiple syndromes", expounded the specific pharmacological regularity of "heterogeneous equivalence" of Japanese (wild) honeysuckle flower, and put forward methods for studying bioequivalence of Japanese(wild) honeysuckle flower, in order to solve the combination and separation of Japanese(wild) honeysuckle flower and lay a foundation for promoting the development of Chinese herbal medicine industry.


Assuntos
Medicamentos de Ervas Chinesas/química , Lonicera/química , Flores/química , Humanos , Impressão Molecular , Estrutura Molecular , Prescrições
16.
Zhongguo Zhong Yao Za Zhi ; 41(18): 3496-3500, 2016 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-28925138

RESUMO

To analyze the research status of traditional Chinese medicine (TCM) processing and key scientific issues to be resolved by using characteristic of TCM biological supramolecules and reaction theories of 'Qi chromatography' to human being, and then put forward the solution countermeasures. Based on the previous explications of theories of the Chinese medicine with supramolecular chemistry as 'Qi chromatograpy', biological supramolecular chemistry theory was used to explain the root of the problem in TCM processing and form the countermeasures for supramolecular chemistry research in the processing of TCM decoction pieces. TCM is a huge complex biological supramolecular body, so the processing of TCM is in view of the processing of huge complex biological supramolecular body. In nature, it is a TCM pharmaceutical technology with chemical changes of the subject and object of biological supramolecular body with or without auxiliary materials, under the condition of high temperature and high humidity. Supramolecular chemistry was throughout the processing of TCM, so the use of supramolecular technology was appropriate in research. TCM decoction pieces were the product of subject and object molecular changes after supramolecular chemistry reaction, with changes in physical and chemical properties of the subject and object molecules, such as bound water overflow, chemical bond rupture, dehydration, carbonization, and reaction with auxiliary materials. Changes in drug property and drug efficacy after processing depended on the degree of subject and object "imprinting template" change, which can be measured by 'Qi chromatography' function of supermolecular imprinting template in human body. In this paper, the research ideas, methods, variety attribution, processing principle, quality standard and clinical application were analyzed to find out the sticking point of the problems, and form the countermeasures with supramolecular chemistry as the core. The processing of TCM is a chemical technology of biological supramolecular body based on the function of supermolecular 'imprinting template' (medical element) of human meridian-viscera, and its reaction products (decoction pieces) showed determinacy when used alone and compatibility when used together, which may constitute a compatible drug delivery system of TCM in clinical application.


Assuntos
Medicamentos de Ervas Chinesas/química , Química Farmacêutica , Humanos , Medicina Tradicional Chinesa , Meridianos
17.
Zhongguo Zhong Yao Za Zhi ; 41(24): 4675-4679, 2016 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-28936855

RESUMO

Controlled sustained-release preparation (CSRP) is a definitely important source of innovative medicines, however, its further researches and development are limited due to the complexity of Chinese medicine (CM) compositions, and a series of unclear key problems like the apparent properties from physical and chemical aspects. Combined with the CM characteristics of the multiple components and synergistic effect, a series of bottleneck problems in the preparation of CSRP were analyzed. Then the mechanism and influences of supermolecular chemical theory in the CSRP about the multiple-components overall-control were explored under the guideline of "overall control, synchronous dissolution" in CSRP, based on the previous explications about supramolecular chemistry theories and with the application of single component precision controlling technologies. The supermolecular mechanism of multi-component overall control and synchronous release of the CSRP was investigated, providing an useful academic reference for the research and development of the CSRP and laying the theoretical and technical foundation for the manufacturing process of CSRP.


Assuntos
Química Farmacêutica , Preparações de Ação Retardada/química , Medicina Tradicional Chinesa , Medicamentos de Ervas Chinesas
18.
Nucleic Acids Res ; 43(18): 8942-54, 2015 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-26384418

RESUMO

ScPif1 DNA helicase is the prototypical member of a 5'-to-3' helicase superfamily conserved from bacteria to human and plays various roles in the maintenance of genomic homeostasis. While many studies have been performed with eukaryotic Pif1 helicases, including yeast and human Pif1 proteins, the potential functions and biochemical properties of prokaryotic Pif1 helicases remain largely unknown. Here, we report the expression, purification and biochemical analysis of Pif1 helicase from Bacteroides sp. 3_1_23 (BsPif1). BsPif1 binds to a large panel of DNA substrates and, in particular, efficiently unwinds partial duplex DNAs with 5'-overhang, fork-like substrates, D-loop and flap-like substrates, suggesting that BsPif1 may act at stalled DNA replication forks and enhance Okazaki fragment maturation. Like its eukaryotic homologues, BsPif1 resolves R-loop structures and unwinds DNA-RNA hybrids. Furthermore, BsPif1 efficiently unfolds G-quadruplexes and disrupts nucleoprotein complexes. Altogether, these results highlight that prokaryotic Pif1 helicases may resolve common issues that arise during DNA transactions. Interestingly, we found that BsPif1 is different from yeast Pif1, but resembles more human Pif1 with regard to substrate specificity, helicase activity and mode of action. These findings are discussed in the context of the possible functions of prokaryotic Pif1 helicases in vivo.


Assuntos
Proteínas de Bactérias/metabolismo , Bacteroides/enzimologia , DNA Helicases/metabolismo , DNA/metabolismo , Proteínas de Bactérias/química , Proteínas de Bactérias/isolamento & purificação , DNA/química , DNA Helicases/química , DNA Helicases/isolamento & purificação , Quadruplex G , Especificidade por Substrato
19.
Zhongguo Zhong Yao Za Zhi ; 40(8): 1624-9, 2015 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-26281611

RESUMO

In this paper, based on the special influence of supramolecular chemistry on the basic theory of Chinese medicines ( CM) , the authors further analyzed the history of meridian tropism and natural origins of CM organisms and explained CM ingredients and the universal regularity of the automatic action of the supramolecular "imprinting templates" hole channel structure. After entering human bodies, CMs, as the aggregation of supramolecular "imprinting templates" , automatically seek supramolecular subjects that are matched with their "imprinting templates" in human meridians and organs for the purpose of self-recognition, self-organization, self-assembly and self-replication, so as to generate specific efficacy in meridians and organs, which is reflected as the meridian tropism phenomena at macro level. This regularity can be studied by in vitro and in vivo experimental studies. In vitro methods are mostly supra molecular structure analysis and kinetic and thermodynamic parameter calculation; Whereas in vivo methods are dominated by the analysis on object component distribution, chromatopharmacodynamic parameters and network chromatopharmacodynamic parameters; Particularly, the acupoint-medicine method can simplify to study the supramolecular subject-object relations. Consequently, CM's'meridian tropism reveals the universal regularity for interactions of macromolecular and micromolecular "imprinting templates" of subjects and objects in natural organisms. As the first barrier for the material base of the CM theory and breakthrough in the modernization of the basic CM theory, meridian tropism plays an important role in studies on basic theories of the basic CM theory.


Assuntos
Medicamentos de Ervas Chinesas/química , Meridianos , Pontos de Acupuntura , Tratamento Farmacológico , Humanos , Medicina Tradicional Chinesa
20.
Zhongguo Zhong Yao Za Zhi ; 40(2): 240-4, 2015 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-26080552

RESUMO

The solubility parameter determination of astrageloside from Buyang Huanwu decoction with inverse gas chromatography (IGC) method evaluation was investigated in this paper. Di-n-octyl phthalate Kwai alternative sample was used to carry out methodological study. The accuracy of the measured correlation coefficient was 0.992 1. Experimental precision measured by IGC experiments showed that the results were accurate and reliable. The sample was uniformly coated on the surface of an inert carrier and N2 gas was carrier gas, a variety of polar solvents such as isopropanol, toluene, acetone, chloroform, cyclohexane as probes. TCD detector temperature was 150 degrees C, gas room temperature was 120 degrees C. Similar headspace method was used whichever over 1 µL gas into the GC measurement, Retention time t(R), t(0) and all the parameters of air and probes molecules within the column were tested. Astragaloside solubility parameter was (21.02 ± 2.4) [J x cm(-3)] ½, literature value was 19.24 [J x cm(-3)] ½, and relevant coefficient was 0.984 5. IGC method is effective and accurate to measure ingredients solubility parameter.


Assuntos
Cromatografia Gasosa/métodos , Medicamentos de Ervas Chinesas/análise , Saponinas/química , Solubilidade
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA