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1.
J Asian Nat Prod Res ; 16(12): 1171-4, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25582432

ABSTRACT

Anti-inflammatory component (AIC) known as an important constituent of artificial musk exhibits bioactive effects on many pharmacological models. This study describes an immunochemical assay for the quality control of artificial musk in traditional Chinese medicine using an enzyme-linked immunosorbent assay. A polyclonal antibody against AIC was produced by rabbit. The method, at an effective measuring range of 3.13-200 ng/ml of AIC, 3 ng/ml limit of detection, and no cross-reaction with natural musk, successfully detected artificial musk in many traditional Chinese prescriptions containing artificial musk. The results demonstrated that a novel and reliable assay system for detection of artificial musk was generated.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Enzyme-Linked Immunosorbent Assay/methods , Fatty Acids, Monounsaturated , Medicine, Chinese Traditional , Animals , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/immunology , Fatty Acids, Monounsaturated/analysis , Fatty Acids, Monounsaturated/chemistry , Fatty Acids, Monounsaturated/pharmacology , Male , Molecular Structure , Rabbits
2.
J Asian Nat Prod Res ; 16(12): 1166-70, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25559500

ABSTRACT

In this letter, (R)-muscone and (S)-muscone were prepared by optical resolution of dl-muscone using N,N'-dibenzyl-l-tartaramide or N,N'-dibenzyl-d-tartaramide, according to the method reported by Kunihiko Takabe. But we separated the diastereomers using EtOH instead of MeOH in the recrystallization step to get the goal product with higher optical purity and yield. The regulatory effect of muscone and its enantiomer on the neural system showed that they could prolong mouse hypoxia tolerance and dose-dependently enhance mouse spinal cord stimulation induced by strychnine nitrate. (R)-muscone and (S)-muscone had a synergistic action on shortening sleep time induced by sodium pentobarbital in mice.


Subject(s)
Cycloparaffins/chemistry , Hippocampus/physiology , Nervous System/drug effects , Neurons/physiology , Animals , Cycloparaffins/pharmacology , Dose-Response Relationship, Drug , Hypoxia/metabolism , Mice , Molecular Structure , Phenobarbital/pharmacology , Stereoisomerism , Strychnine/pharmacology
3.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 36(6): 583-6, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25556727

ABSTRACT

OBJECTIVE: To identify the anti-inflammatory effects of artificial musk aqueous extract(AME)on lipopolysaccharide-stimulated cytokines secreted or released by RAW264.7 cells. METHODS: Cytokines including interleukin(IL)-6,IL-10,and tumor necrosis factor Α were determined using cytokine enzyme-linked immunosorbent assay kits. RESULT: Compared with model group,the levels of major cytokines such as tumor necrosis factor Α,IL-6,and IL-10 significantly decreased in different AME groups in a dose-dependent manner. CONCLUSION: In lipopolysaccharide-stimulated RAW264.7 macrophages,AME can remarkably inhibit the release of inflammatory cytokines and thus exerts its anti-inflammatory effects.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Fatty Acids, Monounsaturated/pharmacology , Inflammation Mediators/metabolism , Animals , Cell Line, Tumor , Cytokines/metabolism , Enzyme-Linked Immunosorbent Assay , Interleukin-6/metabolism , Lipopolysaccharides , Macrophages , Tumor Necrosis Factor-alpha/metabolism
4.
Talanta ; 80(5): 1868-72, 2010 Mar 15.
Article in English | MEDLINE | ID: mdl-20152425

ABSTRACT

An aptamer-based assay for thrombin with high specificity and sensitivity was presented. In the protocol, the aptamer for thrombin was immobilized on magnetic nanoparticle, and its complementary oligonucleotide was labeled with gold nanoparticles, then the aptamer was hybridized with the complementary oligonucleotide to form the duplex structure as a probe, this probe could be used for the specific recognition for thrombin. In the presence of thrombin, the aptamer prefer to form the G-quarter structure with thrombin, resulting in the dissociation of the duplex of the probe and the release of the gold labeled oligonucleotide. Upon this, we were able to detect thrombin through the detection of the electrochemical signal of gold nanoparticles. The strategy combines with the high specificity of aptamer and the excellent characteristics of nanoparticles. This assay is simple, rapid, sensitive and highly specific, it does not require labeling of thrombin, and it could be applied to detect thrombin in complex real sample. The method shows great potential in other protein analysis and in disease diagnosis.


Subject(s)
Aptamers, Nucleotide/metabolism , Biosensing Techniques/methods , Gold/chemistry , Magnetics , Nanoparticles/chemistry , Thrombin/analysis , Aptamers, Nucleotide/chemistry , Biosensing Techniques/economics , Microscopy, Electron, Scanning , Sensitivity and Specificity , Temperature , Thrombin/metabolism
5.
Yao Xue Xue Bao ; 45(12): 1503-8, 2010 Dec.
Article in Chinese | MEDLINE | ID: mdl-21351489

ABSTRACT

The aim of the present study is to investigate the effects of Vam3 which is one of the dihydroxystilbene compounds on expressions of ICAM-1 in the lungs of OVA-induced asthmatic mice and the mechanisms of anti-airway inflammation. Balb/c mice were challenged with OVA inhalation. Lung tissues were stained with Mayer's hematoxylin and eosin for histopathologic examination. The expression of ICAM-1 in the lungs of mice was analyzed by Western blotting and immunohistochemistry method. The NF-kappaB activities were detected by NF-kappaB-luc reporter genetic transient transfection method. The activities of MMP-9 induced by LPS, TNF-alpha and PMA in THP-1 cells were determined by gelatin zymography method. The results showed that Vam3 could inhibit the expression of ICAM-1 in the OVA-induced mouse model. In addition, Vam3 could significantly suppress the activities of NF-kappaB in A549 cells and MMP-9 in THP-1 cells induced by LPS, TNF-alpha and PMA. These results suggested that Vam3 could alleviate the asthmatic inflammation by decreasing ICAM-1 expression in asthmatic mice, down regulating NF-kappaB and MMP-9 activities. Compound Vam3 showed inhibitory effects on inflammatory signal pathways involved in asthma.


Subject(s)
Asthma/metabolism , Benzofurans/pharmacology , Intercellular Adhesion Molecule-1/metabolism , Matrix Metalloproteinase 9/metabolism , NF-kappa B/metabolism , Stilbenes/pharmacology , Animals , Anti-Asthmatic Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Asthma/chemically induced , Cell Line, Tumor , Humans , Inflammation/metabolism , Leukemia, Myeloid/metabolism , Leukemia, Myeloid/pathology , Lung/metabolism , Lung/pathology , Lung Neoplasms/metabolism , Lung Neoplasms/pathology , Male , Mice , Mice, Inbred BALB C , Ovalbumin
7.
Yao Xue Xue Bao ; 41(4): 346-51, 2006 Apr.
Article in Chinese | MEDLINE | ID: mdl-16856481

ABSTRACT

AIM: A series of new 1,4-pentadien-3-one derivatives were synthesized to search for new Eight novel hydroxylated non-steroidal anti-inflammatory drugs (NSAIDs) with potent activity. METHODS: E,E-1-(3'-indolyl)-5-( substituted phenyl)-1,4-pentadien-3-one derivatives were synthesized by means of aldol condensation and characterized by 1H NMR, ESI-MS and element analysis. Their anti-inflammatory activity in vitro were evaluated. RESULTS: Preliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity. CONCLUSION: Compounds 4d and 4e exhibited potent anti-inflammatory activity and their anti-inflammatory activity was comparable to resveratrol, and were worthy of further study.


Subject(s)
Alkadienes/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Indoles/chemical synthesis , Macrophages, Peritoneal/metabolism , Tumor Necrosis Factor-alpha/metabolism , Alkadienes/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Indoles/pharmacology , Macrophages, Peritoneal/cytology , Male , Mice
9.
Acta Pharmacol Sin ; 27(6): 735-40, 2006 Jun.
Article in English | MEDLINE | ID: mdl-16723093

ABSTRACT

AIM: To explore the anti-inflammatory effects of amurensin H on asthma-like reaction induced by allergen in sensitized mice. METHODS: BALB/c mice were sensitized by ovalbumin (OVA, ip) on d 0 and d 14 and challenged with 1% OVA on d 18 to 22. Mice developed airway eosinophilia, mucus hypersecretion, and elevation in cytokine levels. Mice were administered amurensin H orally at the doses of 49, 70, or 100 mg/kg once every day from d 15 to the last day. Bronchoalveolar lavage fluid (BALF) were collected at 24 h and 48 h after the last OVA challenge. Levels of tumor necrosis factor-alpha (TNF-alpha), interleukin 4 (IL-4), interleukin 5 (IL-5), and interleukin 13 (IL-13) in BALF were measured using ELISA method. Differential cell counts of macrophages, lymphocytes, neutrophils and eosinophils were performed in 200 cells per slide (one slide per animal). Lung tissue sections of 6-mum thickness were stained with Mayer's hematoxylin and eosin for assessment of cell infiltration, mucus production, and tissue damage. RESULTS: Oral administration of amurensin H significantly inhibited OVA-induced increases in total cell counts, eosinophil counts, and TNF- alpha, IL-4, IL-5 and IL-13 levels in BALF. In addition, amuresin H dramatically decreased OVA-induced lung tissue damage and mucus production. CONCLUSION: Amurensin H may have therapeutic potential for the treatment of allergic airway inflammation.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Asthma/drug therapy , Benzofurans/pharmacology , Stilbenes/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Asthma/chemically induced , Asthma/metabolism , Benzofurans/isolation & purification , Cytokines/metabolism , Interleukin-13/metabolism , Interleukin-4/metabolism , Interleukin-5/metabolism , Lung/pathology , Male , Mice , Mice, Inbred BALB C , Molecular Structure , Ovalbumin , Plants, Medicinal/chemistry , Stilbenes/isolation & purification , Tumor Necrosis Factor-alpha/metabolism , Vitis/chemistry
10.
Yao Xue Xue Bao ; 40(6): 513-7, 2005 Jun.
Article in Chinese | MEDLINE | ID: mdl-16144315

ABSTRACT

AIM: To investigate the regulatory effects of various anti-inflammatory drugs on both endogenous and TNFalpha-induced NF-kappaB activation as well as the relative biological activity. METHODS: HEK293 cells were cultured in 96-well plate and 6-well plate, treated with meloxicam, indomethacin, dexamethasone and hydrocortisone, without or with 10 ng.mL(-1) TNFalpha for 24 hours. Then cell proliferation was measured by MTT and cell apoptosis was analyzed by pI stain-flow cytometry. HEK293/ kappaB-luc cells transfected stably with pElam-kappaB-luc vector, were cultured in 96-well plate and treated as above. Equal amounts of cell lysates were tested for luciferase activity which represents NF-kappaB activation. RESULTS: Endogenous NF-kappaB activation was present in HEK293 cells and its level can be increased about 2 times by 10 ng.mL(-1) TNFalpha-induction. Dexamethasone (1 x 10(-8) mol.L(-1)) and meloxicam (1 x 10(-7) - 1 x 10(-6) mol.L(-1)) can decrease both endogenous and TNFalpha-induced NF-kappaB activation. Hydrocortisone (1 x 10(-9) mol.L(-1)) increases endogenous NF-kappaB activation but decreases TNFalpha-induced one significantly. No influence of indomethacin on endogenous NF-kappaB activation was observed. However, its influence on TNFalpha-induced NF-kappaB activation is needed for further study. Cell apoptosis was observed after treatment with TNFalpha and 1 x 10(-8), 1 x 10(-6) mol.L(-1) dexamethasone and 1 x 10(-7) mol.L(-1) indomethacin, or only with dexamethasone. No significant effect of these anti-inflammatory drugs on cell proliferation was observed. CONCLUSION: Various anti-inflammatory drugs differ in their ability to regulate NF-kappaB activation in HEK293 cells, which indicates that NF-kappaB activation might be a potential useful target to study mechanism and for drug screening.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Apoptosis/drug effects , Kidney/cytology , NF-kappa B/metabolism , Cell Line , Cell Proliferation/drug effects , Dexamethasone/pharmacology , Embryo, Mammalian , Humans , Hydrocortisone/pharmacology , Indomethacin/pharmacology , Kidney/metabolism , Meloxicam , Thiazines/pharmacology , Thiazoles/pharmacology
11.
J Med Chem ; 48(16): 5112-22, 2005 Aug 11.
Article in English | MEDLINE | ID: mdl-16078831

ABSTRACT

N(2)-[alpha-O-benzyl-N-(acetylmuramyl)-L-alanyl-D-isoglutaminyl]-N(6)-trans-(m-nitrocinnamoyl)-L-lysine (muramyl dipeptide C, or MDP-C) has been synthesized as a novel, nonspecific immunomodulator. The present study shows that MDP-C induces strong cytolytic activity by macrophages on P388 leukemia cells and cytotoxic activity by cytotoxic T lymphocytes (CTLs) on P815 mastocytoma cells. Our results also indicate that MDP-C is an effective stimulator for production of interleukin-2 and interleukin-12 by murine bone marrow derived dendritic cells (BMDCs) and production of interferon-gamma by CTLs. Additionally, MDP-C increases the expression levels of several surface molecules, including CD11c, MHC class I, and intercellular adhesion molecule-1 in BMDCs. Moreover, MDP-C remarkably enhances the immune system's responsiveness to hepatitis B surface antigen (HBsAg) in hepatitis B virus transgenic mice for both antibody production and specific HBsAg T-cell responses ex vivo. Our results indicate that MDP-C is an apyrogenic, nonallergenic, and low-toxicity immunostimulator with great potential for diagnostic, immunotherapeutic, and prophylactic applications in diseases such as hepatitis B and cancers.


Subject(s)
Acetylmuramyl-Alanyl-Isoglutamine/analogs & derivatives , Adjuvants, Immunologic/chemical synthesis , Hepatitis B Surface Antigens/immunology , Acetylmuramyl-Alanyl-Isoglutamine/adverse effects , Acetylmuramyl-Alanyl-Isoglutamine/chemical synthesis , Acetylmuramyl-Alanyl-Isoglutamine/pharmacology , Adjuvants, Immunologic/adverse effects , Adjuvants, Immunologic/pharmacology , Animals , Antibody Formation , Bone Marrow Cells/drug effects , Bone Marrow Cells/metabolism , CD11c Antigen/biosynthesis , Cell Line, Tumor , Cytotoxicity, Immunologic , Dendritic Cells/drug effects , Dendritic Cells/metabolism , Hepatitis B/immunology , Hepatitis B Vaccines/immunology , Histocompatibility Antigens Class I/biosynthesis , In Vitro Techniques , Intercellular Adhesion Molecule-1/biosynthesis , Interleukin-12/biosynthesis , Interleukin-2/biosynthesis , Macrophages/drug effects , Macrophages/immunology , Male , Mice , Mice, Inbred C57BL , Mice, Transgenic , Rabbits , Rats , Rats, Wistar , T-Lymphocytes, Cytotoxic/drug effects , T-Lymphocytes, Cytotoxic/immunology , Toxicity Tests, Acute
13.
Yao Xue Xue Bao ; 40(4): 332-6, 2005 Apr.
Article in English | MEDLINE | ID: mdl-16011261

ABSTRACT

AIM: To study the effects of ginsenoside-Ro on cell proliferation and cytokine production in murine splenocytes. METHODS: The effect of ginsenoside-Ro on murine splenocytes proliferation was studied using [3H] thymidine incorporation assay. Effects of ginsenoside-Ro on the production of cytokines interleukin-2 (IL-2), interferon-gamma (IFN-gamma) and interleukin-4 (IL-4) from murine splenocytes were detected by ELISA method. Effects of ginsenoside-Ro on mRNA level of Th1 cytokine IFN-gamma and Th2 cytokine IL-4 were evaluated by reverse transcription polymerase chain reaction (RT-PCR) analysis. RESULTS: Ginsenoside-Ro showed no mitogenic effect on unstimulated murine splenocytes. It enhanced the proliferation of Con A-induced murine splenocytes and the production of IL-2 at concentrations of 1-10 micromol x L(-1). Moreover, ginsenoside-Ro increased the production and expression of Th2 cytokine IL-4 and decreased the production and expression of Th1 cytokine IFN-gamma in Con A-induced murine splenocytes at concentrations of 2-10 micromol x L(-1). CONCLUSION: Ginsenoside-Ro showed immunomodulatory effects by regulating the production and expression of Th1/Th2 cytokines in murine splenocytes.


Subject(s)
Cell Proliferation/drug effects , Ginsenosides/pharmacology , Interferon-gamma/biosynthesis , Interleukin-4/biosynthesis , Spleen/metabolism , Animals , Ginsenosides/isolation & purification , Interferon-gamma/genetics , Interleukin-2/metabolism , Interleukin-4/genetics , Male , Mice , Mice, Inbred BALB C , Panax/chemistry , Plants, Medicinal/chemistry , RNA, Messenger/biosynthesis , RNA, Messenger/genetics , Spleen/cytology
15.
Planta Med ; 71(3): 202-7, 2005 Mar.
Article in English | MEDLINE | ID: mdl-15770538

ABSTRACT

Seven protopanaxatriol-type ginsenosides and their aglycones including PPT, PT, -Re, -Rg (1), -F (1), -Rh (1), 20(R)-Rh (1) which are closely related in structure were studied for their effects on type 1 and type 2 cytokines production from murine splenocytes and their related mechanisms were examined. The results indicate that PPT, PT and ginsenoside-Re show hardly any or weak effects on concanavalin A (Con A)-induced production of IFN-gamma and IL-4. Ginsenoside-Rh (1) and 20(R)-Rh (1) induce a Con A-induced type 1 cytokine pattern by increasing the production of interleukin-12 (IL-12), the expression of IFN-gamma, T-bet and enhancing NF-kappaB DNA binding activity. In contrast ginsenosides-Rg (1) and -F (1) cause a Con A-induced type 2 cytokines response by increasing the expression of IL-4, GATA-3 and enhancing NF-kappaB DNA binding activity. Thus, these protopanaxatriol-type ginsenosides have different immunomodulatory effects, which might explain the complex immunomodulatory effect of Panax ginseng.


Subject(s)
Cytokines/drug effects , Panax , Phytotherapy , Sapogenins/pharmacology , Triterpenes/pharmacology , Animals , Cytokines/genetics , Cytokines/metabolism , DNA Primers , DNA-Binding Proteins/drug effects , DNA-Binding Proteins/metabolism , Dose-Response Relationship, Drug , GATA3 Transcription Factor , Ginsenosides/administration & dosage , Ginsenosides/pharmacology , Ginsenosides/therapeutic use , Interferon-gamma/drug effects , Interferon-gamma/metabolism , Interleukin-12/metabolism , Interleukin-4/metabolism , Male , Mice , Mice, Inbred BALB C , Mice, Inbred C57BL , NF-kappa B/drug effects , NF-kappa B/metabolism , RNA, Messenger/analysis , Reverse Transcriptase Polymerase Chain Reaction , Sapogenins/administration & dosage , Sapogenins/therapeutic use , Spleen/cytology , T-Box Domain Proteins , Trans-Activators/drug effects , Trans-Activators/metabolism , Transcription Factors/drug effects , Transcription Factors/metabolism , Triterpenes/administration & dosage , Triterpenes/therapeutic use
16.
Wei Sheng Yan Jiu ; 34(6): 710-2, 2005 Nov.
Article in Chinese | MEDLINE | ID: mdl-16535842

ABSTRACT

OBJECTIVE: In order to study the effects of different levels of zinc nutrition status on the immune function of mice spleen lymphocytes. METHODS: The experiment included two periods: zinc depleted period and repletion period. In the depleted period, mice were divided into 3 dose groups: zinc deficient group (ZD, 5.2mg/kg), zinc pair-fed group (PZ) and normal zinc group (NZ, 25.6 mg/kg). In the repletion period, mice were divided into 3 dose groups: ZD group, DZ-NZ group and PZ-NZ group. It was measured some biomarkers of immunity to assess the zinc nutritional status, including lymphocytes amount, lymphocytes proliferation index and IL-2 activity. RESULTS: The lymphocytes counts of ZD group spleen showed significant decline at seventy days fed zinc deficiency diets. The counts of ZD-NZ group were increased after 22 days of taking normal zinc diet. Zinc deficiency could suppressed the proliferation of the spleen lymphocytes. The spleen lymphocytes proliferation of the ZD-NZ group showed a moderate but non-significant increase compared with the ZD group. Zinc deficiency could decrease IL-2 production. The production of IL-2 of ZD group was lower than those of ZP (P < 0.05), IL-2 production increased following zinc supplement. CONCLUSION: It is found that zinc status can affect the immune function. Production of IL-2 in spleen lymphocyte is affected evidently by zinc.


Subject(s)
Lymphocytes/immunology , Spleen/immunology , Zinc/administration & dosage , Zinc/pharmacology , Animals , Cell Proliferation/drug effects , Interleukin-2/biosynthesis , Lymphocytes/cytology , Male , Mice , Mice, Inbred C57BL , Spleen/cytology
17.
Acta Pharmacol Sin ; 25(12): 1671-6, 2004 Dec.
Article in English | MEDLINE | ID: mdl-15569414

ABSTRACT

AIM: To investigate the immunoenhancing activity of ginsenoside-F3 in murine spleen cells and explore its mechanism. METHODS: The enhancing effect of ginsenoside-F3 on murine spleen cell proliferation was studied using [3H]thymidine incorporation assay. Effects of ginsenoside-F3 on the production of type 1 cytokines IL-2, IFN-gamma, and type 2 cytokines IL-4 and IL-10 from murine spleen cells were detected by ELISA method. Effects of ginsenoside-F3 on mRNA level of cytokines IL-4, IFN-gamma, and transcription factors T-bet and GATA-3 were evaluated by RT-PCR analysis. Effect of ginsenoside-F3 on NF-kappaB DNA binding activity in murine spleen cells was investigated by electrophoretic mobility shift assays (EMSA). RESULTS: Ginsenoside-F3 at 0.1-100 micromol/L not only promoted the murine spleen cell proliferation, but also increased the production of IL-2 and IFN-gamma, while decreased the production of IL-4 and IL-10 from murine spleen cells with the maximal effect at 10 micromol/L. RT-PCR analysis displayed that ginsenoside-F3 enhanced the IFN-gamma and T-bet gene expression and decreased IL-4 and GATA-3 gene expression. EMSA experiment showed that ginsenoside-F3 10 micromol/L enhanced the NF-kappaB DNA binding activity induced by ConA in murine spleen cells. CONCLUSION: Ginsenoside-F3 has immunoenhancing activity by regulating production and gene expression of type 1 cytokines and type 2 cytokines in murine spleen cells.


Subject(s)
Cell Proliferation/drug effects , Cytokines/biosynthesis , Ginsenosides/pharmacology , Panax , Spleen/immunology , Animals , Cell Separation , Cytokines/genetics , Ginsenosides/isolation & purification , Male , Mice , Mice, Inbred BALB C , Panax/chemistry , Plant Leaves/chemistry , Plants, Medicinal/chemistry , Sapogenins/isolation & purification , Sapogenins/pharmacology , Spleen/cytology , Triterpenes/isolation & purification , Triterpenes/pharmacology
18.
Acta Pharmacol Sin ; 25(7): 927-31, 2004 Jul.
Article in English | MEDLINE | ID: mdl-15210067

ABSTRACT

AIM: To investigate the inhibitory effect of imrecoxib, a synthetic compound of completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatory effect in vivo. METHODS: The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studied using whole cell assay with murine peritoneal macrophages induced by calcimycin and LPS. The inhibitory effects of imrecoxib on mRNA level of COX-1 and COX-2 in human macrophage cell line U937 were detected by reverse transcription polymerase chain reaction (RT-PCR) analysis. Effects of imrecoxib on acute and chronic inflammation were evaluated in rat carrageenan induced edema model and rat adjuvant-induced arthritis model, respectively. RESULTS: Imrecoxib was found to inhibit COX-1 and COX-2 with IC50 value of 115+/-28 nmol/L and 18+/-4 nmol/L, respectively. Imrecoxib was shown to selectively and dose-dependently inhibit COX-2 mRNA level. Imrecoxib effectively inhibited carrageenan-induced acute inflammation at the doses of 5, 10, and 20 mg/kg i.g. and adjuvant-induced chronic inflammation at the doses of 10 and 20 mg/kg/d i.g. CONCLUSION: Imrecoxib is a novel and moderately selective COX-2 inhibitor that possesses anti-inflammatory effect by inhibition of COX-2 mRNA expression.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cyclooxygenase Inhibitors/pharmacology , Isoenzymes/biosynthesis , Prostaglandin-Endoperoxide Synthases/biosynthesis , Pyrroles/pharmacology , Sulfides/pharmacology , Animals , Arthritis, Experimental/pathology , Cyclooxygenase 1 , Cyclooxygenase 2 , Cyclooxygenase 2 Inhibitors , Edema/pathology , Humans , Isoenzymes/antagonists & inhibitors , Isoenzymes/genetics , Male , Membrane Proteins , Mice , Mice, Inbred C57BL , Prostaglandin-Endoperoxide Synthases/genetics , Pyrroles/chemical synthesis , RNA, Messenger/genetics , Rats , Rats, Wistar , Sulfides/chemical synthesis , U937 Cells
19.
J Comb Chem ; 6(3): 431-6, 2004.
Article in English | MEDLINE | ID: mdl-15132605

ABSTRACT

A parallel solution-phase synthesis of 2-quinoxalinol analogues is described. The key step-simultaneous reductions of m-Ar(NO2)2 to m-Ar(NH2)2 was investigated extensively. We obtained preliminary pharmacological activity of those analogues for the inhibition of LPS-induced TNF-alpha release on mouse macrophage in vitro. Two compounds revealed inhibitory activity, with IC50 values of 0.40 microM (7-amino-6-[(3-methoxypropyl)amino]-3-methyl-2-quinoxalinol) and 2.2 microM (7-amino-6-[(3-butoxypropyl)amino]-3-methyl-2-quinoxalinol), respectively.


Subject(s)
Pharmaceutical Solutions , Tumor Necrosis Factor-alpha , Animals , Lipopolysaccharides , Macrophages , Mice , Solutions
20.
Acta Pharmacol Sin ; 24(11): 1167-71, 2003 Nov.
Article in English | MEDLINE | ID: mdl-14627504

ABSTRACT

AIM: To examine the inhibitory effect of resveratrol on matrix metalloroteinase-9 (MMP-9) and explore its mechanism. METHODS: MMP-9 activity was analyzed by gelatin zymography; MMP-9 protein was detected by Western blot; MMP-9 mRNA expression was investigated by RT-PCR. Activation of activator protein -1 (AP-1) was measured by electrophoretic mobility shift assay (EMSA). RESULTS: MMP-9 activity in U937 cells increased significantly after exposed to PMA at 10 nmol/L for 24 h without FCS (P<0.01). Resveratrol at 1 and 10 micromol/L showed significant inhibition on MMP-9 activity (P<0.05 and P<0.01, respectively). Western blot and RT-PCR experiments displayed that MMP-9 protein (P<0.01) and mRNA expression (P<0.01) increased significantly in PMA-treated U937 cells. Resveratrol at 1 and 10 micromol/L showed inhibitory effects on MMP-9 protein production and MMP-9 mRNA expression (P<0.05). The activation of AP-1 induced by PMA was also extensively inhibited by resveratrol at 0.1, 1, and 10 micromol/L. CONCLUSION: The inhibitory effect of resveratrol on MMP-9 activity may be partly through suppression of activation of nuclear transcription factor AP-1, and inhibition of MMP-9 mRNA expression and MMP-9 protein production.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Matrix Metalloproteinase 9/metabolism , Stilbenes/pharmacology , Transcription Factor AP-1/metabolism , Dexamethasone/pharmacology , Humans , Matrix Metalloproteinase 9/genetics , RNA, Messenger/genetics , Resveratrol , Transcription, Genetic , U937 Cells
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