摘要
The interaction of the organic ligands with metal nanoparticle has a very important role for applications in catalysis, as well as other processes involving ligands that can activate or poison the surface of metal nanoparticles. Very little has been studied so far on the role of organic ligands used either in the preparation of nanoparticles for applications in catalysis or addition in the reaction to activate the catalyst. In this thesis, we have studied strategies for the synthesis of metal nanoparticles, their use as components for the preparation of supported catalysts and activation and deactivation processes involving the ligands used as stabilizers or purposely added to the reaction medium or support for stimulate new reactivity and selectivity in reactions of industrial interest, such as hydrogenation. Here, the concept of frustrated Lewis pairs (FLPs) has been expanded to surface-FLP analogous formed by combining gold nanoparticles (NPs) and Lewis bases, such as amines or phosphines, creating a new channel for the heterolytic cleavage of H2, and thereby performing selective hydrogenation reactions with gold. A first approach to improve the catalytic activity of gold nanoparticles was to analyze the effect of nitrogen-containing bases. The starting inactive gold nanoparticles became highly active for the selective hydrogenation of alkyne into cis-alkenes. The hydrogenation proceeded smoothly and fully selective using H2 as the hydrogen source and under relatively mild conditions (80 °C, 6 bar H2). Our studies also have revealed that the presence of capping ligands blocks the adsorption of the amine to the gold surface, avoiding the FLPs interface and thereby leading to low catalytic activity. When the capping ligands were removed from the catalyst surface and an amine ligand was added, the FLPs interface is recovered and an enhanced catalytic activity was observed. Furthermore, we have demonstrated the successful use of simple organophosphorus ligands to boost the catalytic activity of Au NPs for a range of important reduction reactions, namely, epoxides, N-oxides, sulfoxides, and alkynes. Furthermore, the choice of phosphorus-containing ligands resulted in a decrease in the amount necessary to reach high conversion and selectivity in comparison with our previous study with N-containing ligands. The ligand-to-metal ratio decreased from 100 (amine/Au) to 1 (phosphite/Au). The synthesis of gold nanoparticles supported on N-doped carbon supports was used as an alternative method for the synthesis of a heterogeneous active gold catalyst for selective hydrogenations. The main advantage with respect to previous studies was to avoid the addition of external ligands, in large excess, for the activation of gold surfaces via FLP, making the whole process environmentally and economically attractive
A interação dos ligantes orgânicos com nanopartículas de metal certamente tem um papel muito importante para aplicações em catálise, bem como outros processos envolvendo ligantes que podem ativar ou envenenar a superfície de nanopartículas metálicas. Até agora, muito pouco foi estudado sobre o papel dos ligantes orgânicos utilizados na preparação de nanopartículas para aplicações em catálise ou adição na reação para ativar o catalisador. Nesta tese, foram estudadas estratégias para a síntese de nanopartículas metálicas, seu uso como componentes para a preparação de catalisadores suportados e processos de ativação e desativação envolvendo ligantes empregados como estabilizantes ou propositalmente adicionados ao meio de reação ou suporte para estimular novas reatividades e seletividade em reações de interesse industrial, como reações de hidrogenação. Aqui, o conceito de pares de Lewis frustrados (FLPs) foi expandido para o seu análogo de superfície formado pela combinação de nanopartículas (NPs) de ouro e bases de Lewis, como aminas ou fosfinas, criando um novo canal para a clivagem heterolítica de H2 e, assim, realizando reações seletivas de hidrogenação com ouro. Uma primeira abordagem para melhorar a atividade catalítica das nanopartículas de ouro foi analisar o efeito de bases contendo nitrogênio. As nanopartículas de ouro inicialmente inativas tornaram-se altamente ativas para a hidrogenação seletiva de alquino em cis-alquenos. A hidrogenação prosseguiu foi factível e totalmente seletiva usando H2 como fonte de hidrogênio e sob condições relativamente amenas (80 °C, 6 bar de H2). Nossos estudos também revelaram que a presença de estabilizantes pode bloquear a adsorção da base na superfície do ouro, impedindo a formação da interface FLPs e, portanto, levando a baixa atividade catalítica. Quando os estabilizantes foram removidos da superfície do catalisador e um ligante foi adicionado, o FLPs é formado sendo a atividade catalítica aprimorada. Além disso, demonstramos o uso bem-sucedido de ligantes organofosforados atuando como ativadores de Au NPs em uma série de importantes reações de redução, como, epóxidos, N-óxidos, sulfóxidos e alquinos. Além disso, a escolha do ligante fosforado resultou em uma diminuição na quantidade necessária para alcançar alta conversão mantendo a seletividade inalterada. A relação ligante/metal diminuiu de 100/1 (amina/Au) para 1/1 (fosfito/Au). A síntese de nanopartículas de ouro suportadas em carbono dopado com nitrogênio foi utilizada como método alternativo para a síntese de um catalisador heterogêneo de ouro ativo para hidrogenações seletivas. A principal vantagem em relação aos estudos anteriores foi evitar a adição de ligantes externos, em grande excesso, para a ativação de superfícies de ouro via FLP, tornando todo o processo ambiental e economicamente atraente
Subject(s)
Catalysis , Catalyzer , Lewis Bases/antagonists & inhibitors , Gold/agonists , Ligands , Carbon/agonists , Health Strategies , Alkenes/classification , Metal Nanoparticles , Occupational Groups摘要
Study the suitability of organic film for salvianolic acid in the ultrafiltration process of Danshen Dizhuye. UPLC was used to analyze the migration of nine phenolic active ingredients in Danshen Dizhuye during ultrafiltration of PES hollow fiber membrane and PS hollow fiber membrane. The structural composition of multi-components was analyzed by three different batches of Danshen Dizhuye before and after ultrafiltration of the two membranes. The results showed that 9 phenolic active ingredients in Danshen Dizhuye did not change significantly after ultrafiltration through PES membrane. However, after ultrafiltration through PS membrane, the content of sodium danshensu, protocatechualdehyde, caffeic acid, 3-hydroxy-4-methoxycinnamic acid and rosmarinic acid in Danshen Dizhuye did not change significantly, while salvianolic acid D, salvianolic acid B and lithospermic acid decreased by about 20%, and the content of salvianolic acid A decreased significantly. The final content in equilibrium was only about 20% of the original solution. Therefore, an in-depth study on the migration particularity of salvianolic acid A in ultrafiltration membrane was the focuse. The results showed that the loss of salvianolic acid A was caused by both membranes during ultrafiltration, and salvianolic acid A was lost more in PS membrane. When the membrane was washed and regenerated, it was found that salvianolic acid A was detected in the ethanol washing solution, but not in the washing liquid, indicating that the loss of salvianolic acid A during the ultrafiltration was mainly adsorptive action. The results suggested that the migration of phenolic active ingredients in Danshen Dizhuye during the membrane ultrafiltration process did not completely follow the molecular weight passing rule of the membrane pore size. At the same time, it may be affected by factors, such as the structure of the membrane material, and the interaction between the membrane structure and the structure of components, and exhibit different migration behaviors during the ultrafiltration of the membrane.
Subject(s)
Alkenes/chemistry , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/chemistry , Polyphenols/chemistry , Salvia miltiorrhiza/chemistry , Ultrafiltration摘要
The purpose of this study was to investigate the feasibility of the salvianolic acids reference extract for quality control for Salvia miltiorrhiza and salvianolic acids for injection. An Agilent ZORBAX SB-C18( 4. 6 mm×250 mm,5 μm) column was used with mobile phase consisting of 0. 1% formic acid-water and 0. 1% formic acid-acetonitrile in gradient elution procedure. The column temperature was 30 ℃; the flow rate was 1 m L·min-1; and the detection wavelength was 288 nm. The content of rosmarinic acid,lithospermic acid and salvianolic acid B in S. miltiorrhiza was determined by using the salvianolic acids reference extract as control substance. The content of caffeic acid,salvianolic acid E,rosmarinic acid,lithospermic acid,salvianolic acid B,and salvianolic acid Y in the salvianolic acids for injection was also determined. The linear relationship between chemicals was good( r>0. 998 9),and the injection precision RSD was 0. 30%-0. 90%. The sexual RSD is between 1. 4% and 3. 0%,and the RSD of the reproducibility of the extract is between 2. 1% and 5. 2%. The recovery rate of the three components in S. miltiorrhiza was 96. 80%-99. 20%,and the recovery rate of the six components in salvianolic acids for injection was 88. 90%-107. 5%. The solution of S. miltiorrhiza and salvianolic acids for injection were stable within 48 h. A total of 8 batches of S. miltiorrhiza and injection were determined by the reference extract,and the difference was smaller than that measured by the monomer control. This study preliminarily verified that the salvianolic acids reference extract can be used as a substitute for the monomer control for the quality control of S. miltiorrhiza and salvianolic acids for injection.
Subject(s)
Alkenes/analysis , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/standards , Polyphenols/analysis , Quality Control , Reproducibility of Results , Salvia miltiorrhiza/chemistry摘要
Postmenopausal women, who have reduced circulating estrogen levels, are more prone to develop obesity and related metabolic diseases than premenopausal women. The absence of safe and effective treatments for postmenopausal obesity has changed the focus to natural products as alternative remedies. Total salvianolic acids (TSA) are the major water-soluble ingredients of Danshen. Salvianolic acid (SA) is the major constituent of the TSA. Salvianolic acids, including TSA and SA, are widely used in traditional Chinese medicine. In the present study, ovariectomized rats and LO2 cells were used to study the effects of salvianolic acids on body weight gain and hepatic steatosis. Salvianolic acids reduced ovariectomy (OVX)-induced body weight gain, attenuated the expressions of hepatic lipogenic genes, such as sterol regulatory element binding protein (SREBP)1, fatty acid synthase (FAS), and stearoyl-CoA desaturase (SCD)1, and decreased the liver triglyceride (TG) and total cholesterol (TC). For the molecular mechanisms, OVX and high glucose-induced phosphorylation of signal transducer and activator of transcription (STAT)-3 was inhibited by salvianolic acids treatment. In LO2 cells, inhibition of STAT-3 by siRNA attenuated the increased expression of SREBP1 and TG induced by high glucose. Salvianolic acids reduced the upregulation of SREBP1 and TG induced by high glucose in LO2 cells. In conclusion, these findings illustrated that salvianolic acids markedly alleviated the lipid metabolism disorders and protected against the postmenopausal obesity. The underlying mechanism was probably associated with the regulation of STAT-3 signaling.
Subject(s)
Animals , Female , Humans , Rats , Alkenes , Drugs, Chinese Herbal , Lipid Metabolism , Liver , Metabolism , Obesity , Drug Therapy , Genetics , Metabolism , Ovariectomy , Polyphenols , Postmenopause , Genetics , Metabolism , STAT3 Transcription Factor , Genetics , Metabolism , Salvia miltiorrhiza , Chemistry , Signal Transduction , Sterol Regulatory Element Binding Protein 1 , Genetics , Metabolism , Triglycerides , Metabolism摘要
Postmenopausal women, who have reduced circulating estrogen levels, are more prone to develop obesity and related metabolic diseases than premenopausal women. The absence of safe and effective treatments for postmenopausal obesity has changed the focus to natural products as alternative remedies. Total salvianolic acids (TSA) are the major water-soluble ingredients of Danshen. Salvianolic acid (SA) is the major constituent of the TSA. Salvianolic acids, including TSA and SA, are widely used in traditional Chinese medicine. In the present study, ovariectomized rats and LO2 cells were used to study the effects of salvianolic acids on body weight gain and hepatic steatosis. Salvianolic acids reduced ovariectomy (OVX)-induced body weight gain, attenuated the expressions of hepatic lipogenic genes, such as sterol regulatory element binding protein (SREBP)1, fatty acid synthase (FAS), and stearoyl-CoA desaturase (SCD)1, and decreased the liver triglyceride (TG) and total cholesterol (TC). For the molecular mechanisms, OVX and high glucose-induced phosphorylation of signal transducer and activator of transcription (STAT)-3 was inhibited by salvianolic acids treatment. In LO2 cells, inhibition of STAT-3 by siRNA attenuated the increased expression of SREBP1 and TG induced by high glucose. Salvianolic acids reduced the upregulation of SREBP1 and TG induced by high glucose in LO2 cells. In conclusion, these findings illustrated that salvianolic acids markedly alleviated the lipid metabolism disorders and protected against the postmenopausal obesity. The underlying mechanism was probably associated with the regulation of STAT-3 signaling.
Subject(s)
Animals , Female , Humans , Rats , Alkenes , Drugs, Chinese Herbal , Lipid Metabolism , Liver , Metabolism , Obesity , Drug Therapy , Genetics , Metabolism , Ovariectomy , Polyphenols , Postmenopause , Genetics , Metabolism , STAT3 Transcription Factor , Genetics , Metabolism , Salvia miltiorrhiza , Chemistry , Signal Transduction , Sterol Regulatory Element Binding Protein 1 , Genetics , Metabolism , Triglycerides , Metabolism摘要
Lippia sidoides Cham is a typical herb species of Northeast Brazil with widespread use in folk medicine. The major constituents of the essential oil of L. sidoides (EOLs) are thymol, p-cymene, myrcene, and caryophyllene. Several studies have shown that the EOLs and its constituents have pharmacological effects, including antibacterial, anti-inflammatory, antioxidant and neuroprotective activity. Therefore, this work aimed to investigate the effects of the EOLs and their main constituents on rat sciatic nerve excitability. The sciatic nerves of adult Wistar rats were dissected and mounted in a moist chamber. Nerves were stimulated by square wave pulses, with an amplitude of 40 V, duration of 100 μs to 0.2 Hz. Both EOLs and thymol inhibited compound action potential (CAP) in a concentration-dependent manner. Half maximal inhibitory concentration for CAP peak-to-peak amplitude blockade were 67.85 and 40 µg/mL for EOLs and thymol, respectively. CAP peak-to-peak amplitude was significantly reduced by concentrations ≥60 µg/mL for EOLs and ≥30 µg/mL for thymol. EOLs and thymol in the concentration of 60 µg/mL significantly increased chronaxie and rheobase. The conduction velocities of 1st and 2nd CAP components were also concentration-dependently reduced by EOLs and thymol in the range of 30-100 µg/mL. Differently from EOLs and thymol, p-cymene, myrcene and caryophyllene did not reduce CAP in the higher concentrations of 10 mM. These data demonstrated that EOLs and thymol inhibited neuronal excitability and were promising agents for the development of new drugs for therapeutic use.
Subject(s)
Animals , Male , Female , Alkenes/pharmacology , Lippia/chemistry , Monoterpenes/pharmacology , Oils, Volatile/pharmacology , Sciatic Nerve/drug effects , Sesquiterpenes/pharmacology , Thymol/pharmacology , Action Potentials/drug effects , Action Potentials/physiology , Nerve Block/methods , Neural Conduction/drug effects , Oils, Volatile/chemistry , Rats, Wistar , Reproducibility of Results , Sciatic Nerve/physiology , Time Factors摘要
Periodontal ligament mesenchymal stem cells (PDLMSCs) are an important alternative source of adult stem cells and may be applied for periodontal tissue regeneration, neuroregenerative medicine, and heart valve tissue engineering. However, little is known about the impact of bacterial toxins on the biological properties of PDLSMSCs, including self-renewal, differentiation, and synthesis of extracellular matrix. Objective : This study investigated whether proliferation, expression of pro-inflammatory cytokines, and osteogenic differentiation of CD105-enriched PDL progenitor cell populations (PDL-CD105+ cells) would be affected by exposure to bacterial lipopolysaccharide from Escherichia coli (EcLPS). Material and Methods : Toll-like receptor 4 (TLR4) expression was assessed in PDL-CD105+ cells by the immunostaining technique and confirmed using Western blotting assay. Afterwards, these cells were exposed to EcLPS, and the following assays were carried out: (i) cell viability using MTS; (ii) expression of the interleukin-1 beta (IL-1β), interleukin-6 (IL-6), interleukin-8 (IL-8), and tumor necrosis factor alpha (TNF-α) genes; (iii) osteoblast differentiation assessed by mineralization in vitro, and by mRNA levels of run-related transcription factor-2 (RUNX2), alkaline phosphatase (ALP) and osteocalcin (OCN) determined by quantitative PCR. Results : PDL-CD105+ cells were identified as positive for TLR4. EcLPS did not affect cell viability, but induced a significant increase of transcripts for IL-6 and IL-8. Under osteogenic condition, PDL-CD105+ cells exposed to EcLPS presented an increase of mineralized matrix deposition and higher RUNX2 and ALP mRNA levels when compared to the control group. Conclusions : These results provide evidence that CD105-enriched PDL progenitor cells are able to adapt to continuous Escherichia coli endotoxin challenge, leading to an upregulation of osteogenic activities. .
Subject(s)
Alkenes/metabolism , /chemistry , Staphylococcaceae/enzymology , Catalysis , Enzyme Stability , Industrial Microbiology , Osmolar Concentration摘要
Taxa-4(5),11(12)-diene is the precursor for paclitaxel biosynthesis. The diterpenoid paclitaxel (marketed as Taxol), a plant secondary metabolite isolated from yew, is an effective drug widely used in the treatment of numerous cancers. However, further application of taxol has been restricted due to its low yield in plants and the difficulties in extraction. To increase the intact isoprene flux, we constructed the fusion gene plasmid pBgGGTS and individual cassette plasmid pBgGGgTS to enhance the expression levels of geranylgeranyl diphosphate synthase gene (ggpps) and a taxadiene synthase gene (ts) in Coprinopsis cinerea. These two plasmids were separately transformed into C. cinerea LT2 strain, resulting in several putative transformants. Putative transformants were determined by PCR technique, indicating that 5 out of 13 putative transformants transformed by pBgGGTS and 6 out of 13 putative transformants transformed by pBgGGgTS, respectively. Additionally, the Southern blotting analysis of these 10 transformants confirmed that both ggpps and ts gene were stably integrated into the genome of C. cinerea. Crude extracts from each of the transformants were analyzed. There is no difference in the mycelium extracts among the wild-type LT2 and two types of transformants. However, analysis of culture filtrates indicated that an additional GC peak was found at the retention time of 16.762 min which was absent in the wild type control. The mass fragmentation pattern of this peak had the same diagnostic ions with taxa-4(5),11(12)-diene. According to peak area, the amounts of taxa-4(5),11(12)-diene in each fermented broth were 44 ng/L (transformed with pBgGGgTS) and 30 ng/L (transformed with pBgGGTS), respectively. In conclusion, co-expression of the ggpps and ts gene could increase the taxadiene production in C. cinerea.
Subject(s)
Agaricales , Metabolism , Alkenes , Metabolism , Diterpenes , Metabolism , Farnesyltranstransferase , Genetics , Metabolism , Genetic Engineering , Isomerases , Genetics , Metabolism , Paclitaxel , Plasmids摘要
The chemical constituents of Taxus chinensis var. mairei cell cultures were investigated by chromatographic methods, including silica gel column chromatography, Sephadex LH-20 and preparative HPLC. Thirteen compounds were isolated from the 80% ethanol extract of cultured cells and their structures were elucidated by spectral data and physicochemical properties, which were identified as 2α,4α,7β,9α,10β-pentaacetoxy-14β-hydroxytax-11-ene (1), 2α,4α,7β,9α,10β-pentaacetoxytax-11-ene (2), 1β-deoxybaccatin VI (3), 2α-acetoxytaxusin (4), taxuyunnanine C (5), yunnanxane (6), 2α,5α,10β-triacetoxy-14β-propionyloxy-4 (20), 11-taxadiene (7), 2α,5α,10β-triacetoxy-14β-isobutyryloxy-4 (20), 11-taxadiene (8), 2α,5α,10β-triacetoxy-14β-(2'-methyl)butyryloxy-4 (20), 11-taxadiene (9), 13-dehydroxylbaccatin III (10), 13-dehydroxy-10-deacetylbaccatin III (11), paclitaxel (12) and (13) β-sitosterol. Among them, compound 1 is a new compound, and compounds 2, 4, 10 and 11 are isolated from the cell culture of Taxus chinensis var. mairei for the first time.
Subject(s)
Alkenes , Cell Culture Techniques , Cells, Cultured , Diterpenes , Molecular Structure , Paclitaxel , Sitosterols , Taxoids , Taxus , Chemistry摘要
The purpose of this research was to prepare total salvianolic acids-phytosome-HA coprecipitate to improve drug dissolution and its micromeritic properties. Firstly, the coprecipitate was prepared by solvent method and in vitro dissolution of tripterine was performed with the salvianolic acid B and danshensu as criteria. At the same time, the micromeritic properties was characterizated, the structure of samples was characterized by TEM, DSC, XRD and FTIR. Results showed that when the ratio of drug to HA was 1:2, it had a better dissolution, the accumulative drug-release percent in vitro at 60 min was over 90%. At the same time, it has good liquidity and low moisture absorption. Its micromeritic properties have improved. It is proved that the drug still existed amorphously by microstructure analysis. The preparation process is simple and feasible, it has practical value.
Subject(s)
Alkenes , Chemistry , Chemical Precipitation , Chemistry, Pharmaceutical , Methods , Durapatite , Chemistry , Phospholipids , Chemistry , Polyphenols , Chemistry , Time Factors摘要
To prepare salvianolic acid phospholipid compound. With the compound of salvianolic acids and soybean phospholipid as the index, mono-factor experiment and orthogonal design experiment were conducted to screen its technical parameters. According to the results, the optimal preparation conditions of salvianolic acid phospholipid compound were that THF were taken as the reaction solvent, the concentration time was 3 h, the reactant concentration was 5 g x L(-1), the mass ratio of salvianolic acids and phospholipid was 1: 1.5, and the reaction temperature was 40 degrees C. The oil/water partition coefficient of the prepared salvianolic acid phospholipid compound significant increased in water and buffers with different pH values. The results of phase analysis such as DSC, XRD and FTIR indicated that salvianolic acids existed in phospholipid in an amorphous state.
Subject(s)
Alkenes , Chemistry , Metabolism , Chemical Phenomena , Chemistry, Pharmaceutical , Methods , Intestinal Absorption , Phospholipids , Chemistry , Polyphenols , Chemistry , Metabolism , Glycine max , Chemistry , Temperature摘要
In order to study the inherent difference among terpenes producing yeasts from the point of metabolomics, we selected taxadiene producing yeasts as the model system. The changes of cellular metabolites during fermentation log phase of artificial functional yeasts were determined using metabolomics methods. The results represented that compared to W303-1A as a blank control, the metabolites in glycolysis, tricarboxylic acid cycle (TCA) cycle and several amino acids were influenced. And due to the changes of metabolites, the growth of cells was inhibited to a certain extent. Among the metabolites identified, citric acid content in taxadiene producing yeasts changed the most, the decreasing amplitude reached 90% or more. Therefore, citric acid can be a marker metabolite for the future study of artificial functional yeasts. The metabolomics analysis of taxadiene producing yeasts can provide more information in further studies on optimization of terpenes production in heterologous chassis.
Subject(s)
Alkenes , Metabolism , Amino Acids , Metabolism , Citric Acid , Citric Acid Cycle , Diterpenes , Metabolism , Fermentation , Glycolysis , Metabolome , Metabolomics , Yeasts , Metabolism摘要
AIM@#To investigate the different effects of salvianolic acid and notoginseng triterpenes on proliferation, angiogenesis and expression of vascular endothelial growth factor in EA-hy926 cells in vitro.@*METHODS@#EA-hy926 cells were cultured in vitro. Salvianolic acid and notoginseng triterpenes at concentrations of 0.4, 0.8 and 1.2 mg·L(-1) were used to culture EA-hy926 cells. EA-hy926 cells in a blank control group were grown in culture solution only. Viability of cells was assessed by CCK-8, and after treated for 12 h, capillary-like structures were examined. After 24 h culture, the expression of VEGF was detected by real-time PCR.@*RESULTS@#Salvianolic acid at 0.4, 0.8 mg·L(-1), the same as notoginseng triterpenes, increased VEGF content in EA-hy926 cells. Expression of VEGF protein in the salvianolic acid at 1.2 mg·L(-1) group, was up-regulated as compared with notoginseng triterpenes group (P < 0.05).@*CONCLUSION@#Salvianolic acid and notoginseng triterpenes can promote EA-hy926 cell proliferation, angiogenesis and expression of VEGF protein. This analysis also provided evidence that salvianolic acid had the better effects as compared with notoginseng triterpenes.
Subject(s)
Humans , Alkenes , Pharmacology , Cell Line, Tumor , Cell Proliferation , Coronary Stenosis , Drug Therapy , Genetics , Metabolism , Drugs, Chinese Herbal , Pharmacology , Endothelial Cells , Metabolism , Neovascularization, Pathologic , Drug Therapy , Genetics , Metabolism , Panax notoginseng , Chemistry , Polyphenols , Pharmacology , Triterpenes , Pharmacology , Vascular Endothelial Growth Factor A , Genetics , Metabolism摘要
<p><b>OBJECTIVE</b>To explore the mechanism of protective effects of salvianolic acids and Panax notoginseng saponins and their combination on cardiomyocytes suffered with hypoxia-reoxygenation (HR) injury.</p><p><b>METHOD</b>HR-injured H9c2 cell was employed as cellular model to evaluate cardioprotective effects of salvianolic acids, P. notoginseng saponins and their combination. The viability of cells was determined by MT assay, while the leakage of lactate dehydrogenase (LDH) was also determined. Apoptosis of cells was monitored by staining with Hoechst 33342 fluorescent, and was further evaluated by flow cytometry. Immunoblot analysis of apoptosis-related proteins Bcl-2, Bax and Caspase-3 was performed. Moreover, content of Na+, K(+)-ATPase, Ca2+, Mg2(+)-ATPase, and ATP were analyzed.</p><p><b>RESULT</b>Salvianolic acids (0.05-0.5 mg x L(-1)) and P. notoginseng saponins (5-50 mg x L(-1)) have synergistic protective effects on cardiomyocytes with hypoxia-reoxygenation injury in a dose-dependent manner. Both salvianolic acids and P. notoginseng saponins can reduce hypoxia and reoxygenation-induced myocardial apoptosis and improve the energy metabolism in cardiomyocytes. Moreover, the combined use of salvianolic acids and P. notoginseng saponins exerts synergistic effects.</p><p><b>CONCLUSION</b>Salvianolic acids compatibility with P. notogiriseng saponins can protect cardiomyocytes during hypoxia and reoxygenation injury by inhibiting apoptosis and improving energy metabolism.</p>
Subject(s)
Animals , Rats , Alkenes , Pharmacology , Apoptosis , Cell Hypoxia , Cell Line , Drug Synergism , Myocytes, Cardiac , Cell Biology , Metabolism , Oxygen , Metabolism , Panax notoginseng , Chemistry , Polyphenols , Pharmacology , Saponins , Pharmacology摘要
<p><b>OBJECTIVE</b>To study the application of degrading multi-enzymes from Ganoderma lucidum in extracting effective constituents from fibrous roots of Salvia miltiorrhiza.</p><p><b>METHOD</b>Effective constituents were extracted from fibrous roots by degrading multi-enzymes of wood fiber. The enzymatic parameters were optimized by the orthogonal design.</p><p><b>RESULT</b>The extraction efficiencies of total tanshinones and total salvianolic acids in the extracts of fibrous roots of S. miltiorrhiza was obtained using optimum enzymolysis process reached 11.923%, 12.465%, respectively, which were 62.794%, 56.086% more than that by conventional non-enzymatic hydrolysis.</p><p><b>CONCLUSION</b>Degrading multi-enzymes of wood fiber can be used to fully extract effective constituents from fibrous roots of S. miltiorrhiza, which provides a new approach for recycling wastes of traditional Chinese medicines.</p>
Subject(s)
Alkenes , Metabolism , Abietanes , Metabolism , Drugs, Chinese Herbal , Metabolism , Hydrogen-Ion Concentration , Plant Roots , Chemistry , Polyphenols , Metabolism , Reishi , Salvia miltiorrhiza , Chemistry , Temperature , Wood摘要
Research on medicinal model organism is one of the core technologies to promote the modernization of traditional Chinese medicine (TCM). The research progress of Salvia miltiorrhiza as medicinal model plant is summarized in this paper. The genome of S. miltiorrhiza is small and its life cycle is short, as well as this plant can be stably genetically transformed. Because S. miltiorrhiza possesses the important medicinal and economic values, recently the transcriptome and genome of S. miltiorrhiza have been significantly recovered. The research prospect of S. miltiorrhiza as medicinal model plant in TCM was discussed, including biosynthesis of active components and their genetic regulation, relationship between quality of TCM and ecological environments, and selective breeding of good quality lines. Furthermore, as medicinal model plant, the construction of mutant library for S. miltiorrhiza, the genome map with high quality, and the functional genome should be investigated. Accompanying modern investigation of life sciences, the platform for medicinal model plant, S. miltiorrhiza, will be promoted to be established. It is important to develop the ethnopharmacology and new drugs around the world.
Subject(s)
Alkenes , Chromosome Mapping , Abietanes , Genetics , Ethnopharmacology , Genome, Plant , Medicine, Chinese Traditional , Plants, Medicinal , Genetics , Metabolism , Polyphenols , Genetics , Salvia miltiorrhiza , Genetics , Metabolism , Transcriptome摘要
The objective of the present study was to establish a method based on principal component analysis (PCA) for the study of transdermal delivery of multiple components in Chinese medicine, and to choose the best penetration enhancers for the active fraction of Xiangfusiwu decoction (BW) with this method. Improved Franz diffusion cells with isolated rat abdomen skins were carried out to experiment on the transdermal delivery of six active components, including ferulic acid, paeoniflorin, albiflorin, protopine, tetrahydropalmatine and tetrahydrocolumbamine. The concentrations of these components were determined by LC-MS/MS, then the total factor scores of the concentrations at different times were calculated using PCA and were employed instead of the concentrations to compute the cumulative amounts and steady fluxes, the latter of which were considered as the indexes for optimizing penetration enhancers. The results showed that compared to the control group, the steady fluxes of the other groups increased significantly and furthermore, 4% azone with 1% propylene glycol manifested the best effect. The six components could penetrate through skin well under the action of penetration enhancers. The method established in this study has been proved to be suitable for the study of transdermal delivery of multiple components, and it provided a scientific basis for preparation research of Xiangfusiwu decoction and moreover, it could be a reference for Chinese medicine research.
Subject(s)
Animals , Male , Rats , Administration, Cutaneous , Alkenes , Pharmacology , Azepines , Pharmacology , Benzophenanthridines , Pharmacokinetics , Berberine Alkaloids , Pharmacokinetics , Bridged-Ring Compounds , Pharmacokinetics , Coumaric Acids , Pharmacokinetics , Drug Combinations , Drug Synergism , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Glucosides , Pharmacokinetics , In Vitro Techniques , Monoterpenes , Pharmacokinetics , Permeability , Plants, Medicinal , Chemistry , Principal Component Analysis , Rats, Sprague-Dawley , Skin Absorption摘要
The synthetic biology matures to promote the heterologous biosynthesis of the well-known drug paclitaxel that is one of the most important and active chemotherapeutic agents for the first-line clinical treatment of cancer. This review focuses on the construction and regulation of the biosynthetic pathway of paclitaxel intermediates in both Escherichia coli and Saccharomyces cerevisiae. In particular, the review also features the early efforts to design and overproduce taxadiene and the bottleneck of scale fermentation for producing the intermediates.
Subject(s)
Alkenes , Chemistry , Metabolism , Antineoplastic Agents, Phytogenic , Chemistry , Metabolism , Biosynthetic Pathways , Diterpenes , Chemistry , Metabolism , Escherichia coli , Metabolism , Fermentation , Metabolic Engineering , Paclitaxel , Chemistry , Metabolism , Prodrugs , Saccharomyces cerevisiae , Metabolism , Synthetic Biology摘要
<p><b>OBJECTIVE</b>To study the plasma protein binding rate of isopropylidene-shikimic acid.</p><p><b>METHOD</b>The ultrafiltration was employed to determine the plasma protein binding rate of isopropylidene-shikimic acid. The plasma concentrations of isopropylidene-shikimic acid were measured by HPLC.</p><p><b>RESULT</b>The plasma protein binding rate of isopropylidene-shikimic acid with dog plasma at the concentration of 0.3, 0.15 g x L(-1) and 0.5 mg x L(-1) were (4.36 +/- 0.02)%, (4.12 +/- 0.19)% and (2.23 +/- 0.59)%, respectively. While the plasma protein binding rate of isopropylidene-shikimic acid with normal human plasma at the above concentrations were (11.23 +/- 0.01)%, (10.06 +/- 0.69)% and (9.72 +/- 0.59)%, respectively.</p><p><b>CONCLUSION</b>The binding rate of isopropylidene-shikimic acid with plasma protein is low.</p>
Subject(s)
Animals , Dogs , Humans , Alkenes , Chemistry , Blood Proteins , Metabolism , Chromatography, High Pressure Liquid , Protein Binding , Shikimic Acid , Chemistry , Metabolism , Species Specificity摘要
OBJECTIVE: Deficits in olfactory function are common features in neurodegenerative and neuropsychiatric disorders. Olfactory processing is related to dopamine metabolism and orbitofrontal cortex functioning, both known to be involved in the neurobiology of ADHD. Some investigations suggested alterations in olfactory processing (identification and detection threshold) in patients with ADHD. Despite increasing knowledge, controversy about this topic still exists regarding children with ADHD. This study was conducted to help elucidate some of this controversy. METHODS: 50 participants (8-15 years, mean=10.70+/-1.77) with ADHD were compared to 50 controls. The two groups were well matched for age, gender and Mean School Scores (MSS). We assessed odor identification and threshold through a smell test composed of two tests of identification and detection threshold. Odor detection threshold was assessed with the odorant phenyl ethyl alcohol solved in propylene glycol using a single staircase method. Odor identification was assessed with chemical essences of five common odorants. RESULTS: The mean Sensory Identification Score for children with ADHD and the control groups were 3.76 (1.06) and 4.46 (0.76), respectively (p<0.001). The mean for Sensory Threshold Score for ADHD and control group was 6.4 (3.35) and 9.75 (2.16), respectively (p<0.001). CONCLUSION: This study replicated altered olfactory performance in ADHD. Substantial olfactory deficits across the two domains of identification and detection threshold are observed in children with ADHD. These deficits do not seem to be a result of olfactory task difficulty and are not influenced by age, gender and MSS. Further studies are required to investigate whether olfactory function can be used as a biological marker for early diagnosis, treatment and prognosis of ADHD.