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1.
Chinese Journal of Biotechnology ; (12): 1202-1216, 2023.
Article in Chinese | WPRIM | ID: wpr-970433

ABSTRACT

Biodegradation of pyridine pollutant by microorganisms is one of the economical and effective methods to solve the environmental pollution of pyridine under high salinity conditions. To this end, screening of microorganisms with pyridine degradation capability and high salinity tolerance is an important prerequisite. In this paper, a salt-resistant pyridine degradation bacterium was isolated from the activated sludge of Shanxi coking wastewater treatment plant, and identified as a bacterium belonging to Rhodococcus on the basis of colony morphology and 16S rDNA gene phylogenetic analysis. Salt tolerance experiment showed that strain LV4 could grow and degrade pyridine with the initial concentration of 500 mg/L completely in 0%-6% saline environment. However, when the salinity was higher than 4%, strain LV4 grew slowly and the degradation time of pyridine by strain LV4 was significantly prolonged. Scanning electron microscopy showed that the cell division of strain LV4 became slower, and more granular extracellular polymeric substance (EPS) was induced to secrete in high salinity environment. When the salinity was not higher than 4%, strain LV4 responded to the high salinity environment mainly through increasing the protein content in EPS. The optimum conditions for pyridine degradation by strain LV4 at 4% salinity were 30 ℃, pH 7.0 and 120 r/min (DO 10.30 mg/L). Under these optimal conditions, strain LV4 could completely degrade pyridine with an initial concentration of 500 mg/L at a maximum rate of (29.10±0.18) mg/(L·h) after 12 h adaptation period, and the total organic carbon (TOC) removal efficiency reached 88.36%, indicating that stain LV4 has a good mineralization effect on pyridine. By analyzing the intermediate products in pyridine degradation process, it was speculated that strain LV4 achieved pyridine ring opening and degradation mainly through two metabolic pathways: pyridine-ring hydroxylation and pyridine-ring hydrogenation. The rapid degradation of pyridine by strain LV4 in high salinity environment indicates its application potential in the pollution control of high salinity pyridine environment.


Subject(s)
Rhodococcus/genetics , Phylogeny , Extracellular Polymeric Substance Matrix/metabolism , Sewage , Biodegradation, Environmental , Pyridines/metabolism
2.
Braz. J. Pharm. Sci. (Online) ; 58: e191026, 2022. tab, graf
Article in English | LILACS | ID: biblio-1384003

ABSTRACT

In this present study, 63 different 5-[4-methyl-2-(pyridin-3/4-yl)thiazole-5-yl]-4-substituted-3-substituted benzylthio-4H-1,2,4-triazole derivatives were synthesized, and evaluated for their in vitro antimicrobial activity against various human pathogenic microorganisms and antioxidant activity. The derivatives were synthesized in a multi-step synthesis procedure including triazole and thiazole ring closure reactions, respectively. The synthesized derivatives (A1-24; B1-39) were screened for their antibacterial, antifungal, and antioxidant activities compared to standard agents. The derivatives possessing 3-pyridyl moiety particularly exhibited relatively high antibacterial activity (MIC= < 3.09-500 µg/mL) against Gram-positive bacteria, and compounds possessing 4-pyridyl moiety showed remarkable antioxidant activity


Subject(s)
Pyridines/analysis , Thiazoles/analysis , Triazoles/analysis , Methods , Antioxidants , In Vitro Techniques/methods , Gram-Positive Bacteria/classification
3.
Article | IMSEAR | ID: sea-210749

ABSTRACT

The objective of the present study is the protection of secondary amine in the substituted pyrazole derivative withthe help of a green catalyst to facilitate the synthesis of anticancer compounds. Di-tert-butyl dicarbonate (Boc) hasbeen used as a protecting agent with various catalysts such as Polyethylene glycols-400, Dimethyl aminopyridine,and N, N-Diisopropyl ethylamine. In this study, five different synthetic methods have been applied, but success hasbeen achieved in only two. The very first method has been reported for the protection of secondary amine in pyrazole,associated with these catalysts. These synthetic methods had given a good yield and fewer side products, and it also agreen approach toward synthetic chemistry.

4.
Article | IMSEAR | ID: sea-210739

ABSTRACT

A series of pyrazolines and pyridines bearing benzofuran moiety (M1–M10) were synthesized for evaluation of theirin vitro cytotoxicity against MCF-7 and HepG2 cell lines. Furthermore, in silico drug-likeness study was carried out.The result of the cytotoxicity of M1–M10 showed that some compounds displayed cytotoxic activity against MCF-7and HepG2 cells. An assessment of in silico drug-likeness study of M1–M10 illustrates that some compounds showedan agreement to the Lipinski, Ghose, Veber, Egan, and Muegge rules with orally bioavailable.

5.
Journal of Jilin University(Medicine Edition) ; (6): 45-49, 2020.
Article in Chinese | WPRIM | ID: wpr-841579

ABSTRACT

Objective: To investigate the effect of silencing sirtuin 3 (Sirt3) on the apoptosis of human ovarian cancer SKOV3 cells induced by resveratrol (Res), and to explore its mechanism of promoting apoptosis. Methods: The human ovarian cancer SKOC3 cells were cultured with different concentrations 0, 2. 5, 5. 0, 10.0, 20.0, 40.0 and 80.0 mg · L-1) of Res for 24 h. The survival rate of cells was measured by MTT assay. The SKOV3 cells were randomly divided into control group, Sirt3 inhibitory 3-1H-1, 2, 3-triazol-4-yl) pyridine 3-TYP group, Res group and 3-TYP+Res group. After 24 h of culture, the inhibitory rates of proliferation of the cells in various groups were detected by MTT assay; the nuclei were stained with Hoechst 33342, and the morphorgy nucleus was observed by laser confocal microscope; reactive oxygen species (ROS) probe was used to detect the intracellular ROS levels; Western blotting method was used to detect the expression levels of Sirt3, Bax, Bcl-2 and cleaved caspase-3 proteins in the cells in various groups. Results: The results of MTT assay showed that the survival rates of SKOV3 cells were significantly decreased with the increase of concentration of Res, and the median inhibitory concentration (IC50) was 42. 73 mg · L-1. Compared with control group, the inhibitory rates of proliferation of cells in Res group and 3-TYP+Res group were significantly decreased (P0.05); the protein expression levels of Sirt3 and Bcl-2 proteins in Res group were significantly decreased (P< 0.05), and the expression levels of Bax and cleaved caspase-3 proteins were significantly increased (P<0.05). Compared with Res group, the expression levels of Bax and cleaved caspase-3 proteins in 3-TYP + Res group were significantly increased (P<0.05), and the expression levels of Bcl-2 and Sirt3 proteins in 3-TYP+Res group were significantly decreased (P<0.05). Conclusion: Res can induce the apoptosis of SKOV3 cells, and the inhibition of Sirt3 expression by 3-TYP can enhance the effect of Res.

6.
Acta Pharmaceutica Sinica ; (12): 489-494, 2020.
Article in Chinese | WPRIM | ID: wpr-815843

ABSTRACT

The ethyl acetate fraction of 80% ethanol extract from Bidens parviflora Willd.was isolated and purified by silica, polyamide, Sephadex LH-20 and HPLC. A total of eleven compounds were isolated and identified by physicochemical properties and spectral data as (2S)-11E-tetradecene-3,5,7,9-tetrayne-1,2,13-triol (1), pyridine-4-formyl-O-β-D-glucopyranoside (2), maritimein (3), trichocarpine (4), okanin-4-methyl ether-3′-O-β-D-glucopyranoside (5), okanin-4-methyl ether-4′-O-β-D-(6″-acetyl)-glucopyranoside (6), (Z)-6-O-(4″-acetyl-6″-O-p-coumaroyl-β-D-glucopyranosyl)-6,7,3′,4′-tetrahydroxyaurone (7), quercetin-3-O-α-L-arabinoside (8), hyperoside (9), (3S)-(6E,12E)-tetradecadiene-8,10-diyne-1,14-diol-3-O-β-D-glucopyranoside (10), bipinnata polyacetyloside B (11). Compounds 1 and 2 are new compounds, compounds 4 and 8 were isolated from the genus Bidens for the first time, compounds 5-7, 10 and 11 were isolated from this plant for the first time.

7.
Article | IMSEAR | ID: sea-210595

ABSTRACT

Given the increasing role of P90 Ribosomal S6 Kinase 2 (RSK2) as an anticancer drug target, we performed3D-Quantitative structure–activity relationship, including comparative molecular field analysis (CoMFA) andcomparative molecular similarity indices analysis (CoMSIA) on difluorophenol pyridine derivatives as the inhibitorof RSK2. CoMFA model with q2 of 0.597 and R2 of 0.993, while CoMSIA model with q2 of 0.563 and R2 of 0.993,were obtained. The predictive ability of both models was assured using a test set compound with R2pred values of 0.996each. Using the validated models, novel compound was proposed and its interaction with RSK2 was investigatedemploying molecular docking and molecular dynamics simulation of 50 ns. Furthermore, molecular-mechanicsPoisson–Boltzmann surface area calculation was performed. The result showed that the newly designed compoundhas a comparable binding free energy with the known RSK2 inhibitor, indicating its potential as a new RSK2 inhibitor.

8.
Braz. J. Pharm. Sci. (Online) ; 54(4): e00153, 2018. tab, graf
Article in English | LILACS | ID: biblio-1001583

ABSTRACT

Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities


Subject(s)
Pyridines/analysis , Pyrimidines/agonists , Pyrroles , Thiophenes/analysis , Coumarins/analysis , Antipyretics , Analgesics/classification
9.
Chinese Traditional and Herbal Drugs ; (24): 5125-5129, 2017.
Article in Chinese | WPRIM | ID: wpr-852312

ABSTRACT

Objective: To optimize the sulfated modification conditions of Rhodiola sachalinensis polysaccharide (RSP) and improve the anti-oxidant activity of RSP. Methods: RSP were sulfated by chlorosulfonic acid-pyridine method, and the optimal conditions for the sulfated modification were determined by single factor experiments. The physical and chemical properties of RSP and sulfated RSP (S-RSP) were analyzed by infrared spectroscopy (IR) and scanning electron microscopy (SEM). The relation between substituting degree (DS) of S-RSP and anti-oxidative activity of polysaccharide was investigated by testing the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging ability of RSP and S-RSP. Results: When the volume ratio of chlorosulfonic acid to pyridine was 1∶4, the reaction time was 2 h and the reaction temperature was 60 ℃, the maximum sulfur content of S-RSP was 18.83% and the DS was the highest for 2.38. Moreover, the anti-oxidant activity of RSP was enhanced by the sulfated modification, and there was a certain positive proportional relationship between DS and DPPH free radical scavenging ability of S-RSP. Conclusion: The volume ratio of chlorosulfonic acid to pyridine affects the DS of S-RSP, and the sulfated modification can increase the anti-oxidant capacity of RSP by changing its polarity.

10.
Article in English | IMSEAR | ID: sea-168495

ABSTRACT

Green Chemistry is defined as environmentally benign chemistry. The revolution in green chemistry provides enormous scopes for discovery and even application for new synthetic approaches. An efficient and general method has been described for the formation of imidazo[1,2-a]pyridine from 2-amino pyridine with substituted α- haloketones in the presence of water and acidic additives in efficient yields.

11.
Arq. bras. cardiol ; 104(3): 185-194, 03/2015. tab, graf
Article in English | LILACS | ID: lil-742788

ABSTRACT

Background: Ruthenium (Ru) tetraamines are being increasingly used as nitric oxide (NO) carriers. In this context, pharmacological studies have become highly relevant to better understand the mechanism of action involved. Objective: To evaluate the vascular response of the tetraamines trans-[RuII(NH3)4(Py)(NO)]3+, trans-[RuII(Cl)(NO) (cyclan)](PF6)2, and trans-[RuII(NH3)4(4-acPy)(NO)]3+. Methods: Aortic rings were contracted with noradrenaline (10−6 M). After voltage stabilization, a single concentration (10−6 M) of the compounds was added to the assay medium. The responses were recorded during 120 min. Vascular integrity was assessed functionally using acetylcholine at 10−6 M and sodium nitroprusside at 10−6 M as well as by histological examination. Results: Histological analysis confirmed the presence or absence of endothelial cells in those tissues. All tetraamine complexes altered the contractile response induced by norepinephrine, resulting in increased tone followed by relaxation. In rings with endothelium, the inhibition of endothelial NO caused a reduction of the contractile effect caused by pyridine NO. No significant responses were observed in rings with endothelium after treatment with cyclan NO. In contrast, in rings without endothelium, the inhibition of guanylate cyclase significantly reduced the contractile response caused by the pyridine NO and cyclan NO complexes, and both complexes caused a relaxing effect. Conclusion: The results indicate that the vascular effect of the evaluated complexes involved a decrease in the vascular tone induced by norepinephrine (10−6 M) at the end of the incubation period in aortic rings with and without endothelium, indicating the slow release of NO from these complexes and suggesting that the ligands promoted chemical stability to the molecule. Moreover, we demonstrated that the association of Ru with NO is more stable when the ligands pyridine and cyclan ...


Fundamento: As tetra-aminas de rutênio cada vez mais se destacam como carreadoras da molécula de óxido nítrico. Desse modo, estudos farmacológicos tornam-se altamente relevantes, afim de melhor compreender o mecanismo de ação envolvido. Objetivo: Avaliar a resposta vascular das tetra-aminas trans-[RuII(NH3)4(Py)(NO)]3+, trans-[RuII(Cl)(NO)(Cyclan)](PF6)2 e trans-[RuII(NH3)4(4-acPy)(NO)]3+. Métodos: Anéis de aorta foram pré-contraídos com noradrenalina (10-6M). Após estabilização da tensão, concentração única (10-6M) dos compostos foi adicionada ao banho de incubação. As respostas foram registradas ao longo de 120 minutos. A integridade vascular foi avaliada funcionalmente (acetilcolina 10-6M; nitroprussiato de sódio 10-6M) e histologicamente Resultados: A análise histológica confirmou a presença ou não de células endoteliais nos tecidos analisados. Todos os complexos alteraram a resposta contrátil induzida pela noradrenalina, resultando em aumento de tônus seguido de efeito relaxante. Em anéis com endotélio, a inibição do óxido nítrico endotelial causou redução do efeito contrátil da piridina óxido nítrico. Não foram observadas respostas significativas em anéis com endotélio referente ao composto cyclan óxido nítrico. Por outro lado, em anéis sem endotélio, a inibição da guanilato ciclase reduziu significativamente a resposta contrátil dos complexos piridina óxido nítrico e cyclan óxido nítrico, levando ambos os compostos a um efeito relaxante. Conclusão: Os resultados obtidos demonstram que o efeito vascular dos complexos avaliados apresentaram diminuição no tônus vascular induzido pela noradrenalina (10-6M) ao final do tempo de incubação, em anéis com e sem endotélio, indicando liberação lenta da molécula de óxido nítrico do composto estudado e sugerindo que os ligantes causaram estabilidade química à molécula. Demonstramos que a ligação rutênio óxido nítrico é mais estável quando utilizamos os ligantes piridina e cyclan para a formulação ...


Subject(s)
Animals , Humans , Mice , Apoptosis/physiology , MicroRNAs/physiology , Endothelial Cells/physiology , MicroRNAs/antagonists & inhibitors , MicroRNAs/metabolism , Molecular Targeted Therapy/methods , Neoplasms/physiopathology , Ribonuclease III/deficiency , Ribonuclease III/physiology , Up-Regulation , Vascular Endothelial Growth Factor A/physiology
12.
Endocrinology and Metabolism ; : 98-104, 2015.
Article in English | WPRIM | ID: wpr-150112

ABSTRACT

BACKGROUND: Autism spectrum disorder (ASD) encompasses a range of disorders that are characterized by social and communication deficits and repetitive behaviors. This study evaluated the effect of methyl-6-(phenylethynyl)-pyridine (MPEP), an antagonist of the mGluR5 metabotropic glutamate receptor, on memory enhancement in the BTBR T+tf/J (BTBR) mouse strain, which has been recognized as a model of ASD. METHODS: The pharmacological effects of MPEP on memory and motor coordination were assessed using the Morris water maze and rotarod tests in BTBR and C57BL/6J (B6) mice. Furthermore, we performed morphological analyses of cerebellar foliation in BTBR and B6 mice using hematoxylin and eosin staining. RESULTS: MPEP-treated BTBR mice exhibited improved learning and memory in the Morris water maze test. MPEP administration also improved motor coordination in the rotarod test. However, no significant difference was observed regarding the numbers of Purkinje cells in the cerebella of BTBR versus normal B6 mice. CONCLUSION: This study suggests that the mGluR5 antagonist MPEP has the potential to ameliorate learning and memory dysfunction and impaired motor coordination in BTBR mice. These results further suggest that the BTBR mouse model may be useful in pharmacological studies investigating drugs that could potentially alleviate cognitive dysfunction in ASD.


Subject(s)
Animals , Child , Mice , Autism Spectrum Disorder , Eosine Yellowish-(YS) , Hematoxylin , Learning , Maze Learning , Memory , Memory, Short-Term , Purkinje Cells , Receptors, Metabotropic Glutamate , Rotarod Performance Test
13.
Article in English | IMSEAR | ID: sea-163239

ABSTRACT

The aim of this study was to analyze the relationship between electronic structure and anti Bovine Viral Diarrhea Virus activity in a series of imidazo[1,2-a] pyrrolo [2,3-c]pyridine derivatives. The electronic structure and the local atomic reactivity indices were obtained with density functional theory at the B3LYP/6-31G (d,p) level. A statistically significant equation (n=15, R=0.90, R2=0.82, adj R2=0.77, F(3,11)=16.60 (p<0.0002), outliers>2σ=0, SD=0.29) relating the variation of the antiviral activity with the variation of the electrondonor and electron-acceptor properties of three atoms was obtained. The variation of antiviral potency is orbital-controlled. A partial antiviral pharmacophore is proposed.

14.
Article in English | IMSEAR | ID: sea-151924

ABSTRACT

Nine N-pyridine Schiff bases (1-9) that were synthesized by reacting different ortho-, meta- and ortho-metasubstituted salicylaldehyde and 3,5-substituted aminopyridine were evaluated for their antimicrobial activity. The acute in vivo toxicity and genotoxic activity of these compounds were also tested. All of the compounds exhibited antimicrobial activity against Gram-positive (Bacillus cereus, Listeria monocytogenes, Staphylococcus aureus and S. epidermidis) and Gram-negative bacteria (Citrobacter freundii, Enterobacter aerogenes, Escherichia coli, Proteus vulgaris and Salmonella typhimurium) and against yeasts (Candida albicans, C. glabrata, C. utilis, Pichia membranafaciens and Rhodotorula rubra). The minimum inhibitory concentrations (MICs) of the compounds ranged from 0.95 to 1000 μg/ml. For the yeasts tested, the MICs ranged from 0.97 to 250 μg/ml. Compounds 1-6, which were substituted with CH3, NO2, Br and Cl, showed especially significant inhibitory activity against C. albicans, and the MICs of these compounds ranged from 0.97 to 7.81 μg/ml. An in vivo brine shrimp (Artemia salina) acute toxicity assay was used to determine the LD50 values of the test compounds. The LD50 (24 h) values of these compounds ranged from 31.64 to 94.9 μg/ml. Additionally, according to umu-test results, none of the tested compounds showed a genotoxic effect over a range from 10 to 5000 μg/ml.

15.
Chinese Pharmaceutical Journal ; (24): 904-908, 2013.
Article in Chinese | WPRIM | ID: wpr-860369

ABSTRACT

OBJECTIVE: To establish an LC-MS/MS method for simultaneous determination of blonanserin and its metabolite blonanserin C in the plasma of healthy volunteers. METHODS: After adding saturated aqueous solution of sodium bicarbonate as the basification reagent, blonanserin and blonanserin C were extracted from plasma by ethyl acetate-dichloromethane (4;1). Then blonanserin and blonanserin C were determined by LC-MS/MS using blonanserin B and blonanserin D as internal standards respectively. Separation was carried on an Agilent Eclipse plus C18 column(4.6 mm×150 mm, 5 μm)with a mobie phase of acetonitrile-0.005 mol·L-1 ammonium formate aqueous solution containing 0.1% formic acid (87;13) at the flow rate of 0.5 mL·min-1. The column temperature was set at 40°C. ESI source was applied and operated in positive ion mode. Quantitative determination was performed using selective reaction monitoring (SRM) at m/z 368.2→297.2 for blonanserin, m/z 396.3→297.2 for blonanserin B, m/z 340.2→297.1 for blonanserin C and m/z 356.2→313.3 for blonanserin D. RESULTS: Blonanserin and blonanserin C showed good linearity in the range of 10-2000 ng·L-1(r2=0.997). The extraction recoveries for blonanserin and blonanserin C were more than 93.5% and 74.5% respectively, while the intra-day and inter-day RSDs were lower than 9.0% and 16.4% respectively. CONCLUSION: The method is simple, rapid, accurate and sensitivie for simultaneous determination of blonanserin and blonanserin C in human plasma, which can be applied to the clinical pharmacokinetic study and therapeutic drug monitoring of blonanserin.

16.
Article in English | IMSEAR | ID: sea-161549

ABSTRACT

2,4,5-triphenylimidazoles/1-(2-Methyl)-3-(2-hydroxyphenyl)imidazo[1,5- a]pyridine could be obtained in excellent yields by the one-pot three-component condensation of benzil/2-acetyl pyridine, aldehyde and ammonium acetate in the presence of catalytic amount of the inexpensive, readily available NaH2PO4 under solvent-free condition. The mixture was ground together in a mortar with a pestle at room temperature for short reaction time and easy operation under solvent free condition.

17.
Chinese Traditional and Herbal Drugs ; (24): 257-261, 2011.
Article in Chinese | WPRIM | ID: wpr-855674

ABSTRACT

Objective: With swertiamarin as the substrate, biotransformation conditions of swertiamarin were optimized by Aspergillus niger. Methods: With productivity ratio of EHPO {(2)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c] pyridine-1-one} and transformation ratio of swertiamarin as indexes, training time, carbon resource, nitrogen resource, metal ions, phosphate, growth factor (yeast extract paste), inoculum size, substrate concentration, initial pH value, and tempuraure were evaluated to optimize the biotransformation of swertiamarin. Results: It confirmed the optimization cultivating condition that glucose concentration was 10 g/L, peptone concentration was 5 g/L, yeast extract paste was 5 g/L, KH2PO4 concentration was 5 g/L, MgSO4 and CaCl2 concentration was 1 g/L, initial pH value was 6.0, inoculum size was 0.5%, substrate concentration was 1 mg/mL, cultivation temperature was 28 °C, and cultivating time was 5 d. Conclusion: The biotransformation ratio for EHPO into swertiamarin biotransformed by A. niger could steadily be about 8%.

18.
Journal of International Pharmaceutical Research ; (6): 292-301, 2010.
Article in Chinese | WPRIM | ID: wpr-845942

ABSTRACT

Objective: To search for new compounds with better water-solubility and higher antianxiety activities. Methods: A series of 2-arylimidazo[1,2-a] pyridine-3-acetamide derivitives were designed and synthesized. The anxiolytic activities were evaluated by BZDR competitive binding assay in vitro and the elevated-plus maze test in mice, the structure-activity relationship (SAR) has been studied. Results and Conclusion: Twenty-eight new compounds have been synthesized. Their structures were confirmed by 1H NMR and MS. According to the results of BZDR affinity test, compounds I1, I 8, I10, I13, I19 showed as good affinity as the positive control (Ro5-4864). The corresponding inhibition was 87%, 89%, 85%, 89% and 76% respectively at the concentration of 100 nmol/L, while that of Ro5-4864 was 82%. I8 and I10, which display better water-solubility and better BZDR affinity in vitro, show significant antianxiety effects in vivo.

19.
Chinese Journal of Primary Medicine and Pharmacy ; (12): 1209-1210, 2009.
Article in Chinese | WPRIM | ID: wpr-393662

ABSTRACT

Objective To explore the effects and mechanism in patients with ulcerative colitis (UC) treated by Yin Yang equilibrated preparation. Method 82 patients with UC as treatment group and 35 health parsons as control group underwent the testing. The serum and mucosal of all testing persons were taken pre and post treatment to detect CD+4 CD+25 regulatory T cells(Tregs) by flow cytometry at the end of one month,treating with SASP and Yin Yang equilibrated preparation. Result Compared with normal control group,the proportion of CD+4 CD+25 Tregs was markedly decreased in PB and mucesal of group A and B(P <0.01). But it was significanfly increased in therapeutic groups of SASP and Yin Yang equilibrated preparation, and their CD+4 CD+25 Tregs in PB and mucosal were much more than the control group at the end of one month after treating with SASP and Yin Yang equilibrated preparation(P <0.01 or P< 0.05). Conclusion CD+4 CD+25 Tregs with strong immune suppression play a central role in the initia-tion and development of UC,and the Yin Yang equilibrated preparation might exert its therapeutic effects on UC by the regulation of number and function of CD+4 CD+25 Tregs.

20.
China Pharmacy ; (12)2005.
Article in Chinese | WPRIM | ID: wpr-529168

ABSTRACT

OBJECTIVE: To establish a CGC method for the determination of pyridine in Potassium Dehydroandrograpol-ide Succinate. METHODS: The determination was performed on HP-INNOWAX capillary with column temperature at 100℃. The FID detector was used and the carrier gas was nitrogen. RESULTS:The linear range of Pyridine was 2.46~39.3?g?mL-1 and the average recovery was 98.07%,RSD=4.00(n=9).Its detection limit was 0.2?g?mL-1.CONCLUSION: The method is accurate and rapid, and applicable for the determination of the residual level of Pyridine in Potassium dehydroandrograpolide succinate.

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