Biomedical subjects

Motoyuki Nakamura

Publications and source records attributed to Motoyuki Nakamura.

At least 19 recordsLinked to original sources

PubMed2007

Efficacy of amiodarone for preventing the recurrence of symptomatic paroxysmal and persistent atrial fibrillation after cardioversion.

BACKGROUND: It has been previously reported that the efficacy of class I antiarrhythmics in preventing the recurrence of symptomatic paroxysmal and persistent atrial fibrillation (AF) is limited when AF lasts for 48 h or more. However, it is unclear whether the efficacy of amiodarone, a class III drug, is superior to class I antiarrhythmics in patients with long-lasting AF. METHOD AND RESULTS: The relationship between the duration of tachycardia and the efficacy of amiodarone in preventing recurrence of tachycardia was examined in 55 patients (37 men, 18 women, mean age 68+/-9 years) to whom amiodarone was administered after electrical or pharmacological cardioversion for paroxysmal and persistent AF. In 26 patients, paroxysmal and persistent AF ceased within 48 h after onset (Group A), and in the other 29 patients, it ceased after 48 h (Group B). Patient characteristics and actuarial recurrence-free rates were compared between the 2 groups. The mean follow-up period was 30+/-11 months. No statistically significant difference between the groups was found in patient characteristics. Actuarial recurrence-free rates in Group A and B at 1, 3, 6, 9, and 12 months were 100%, 81%, 69%, 62%, and 54%, and 93%, 79%, 66%, 52%, and 48%, respectively (p=NS at 12 months). The period of maintenance of sinus rhythm was 14.7+/-3.2 months in group A and 13.3+/-3.3 months in group B (mean+/-SE, p=NS). CONCLUSION: In the case of amiodarone, efficacy for maintaining sinus rhythm after cardioversion of AF was not biased by the duration of arrhythmia. This observation suggests amiodarone is effective in maintaining normal sinus rhythm after cardioversion, even in patients with long-lasting AF and electrical atrial remodeling.

Aged↗

PubMed2006

Elevated circulating levels of heat shock protein 70 are related to systemic inflammatory reaction through monocyte Toll signal in patients with heart failure after acute myocardial infarction.

BACKGROUND: Recent studies have shown that heat shock protein (HSP) 70 may serve as a "damage signal" to the immune system and could be the endogenous ligand for Toll-like receptor (TLR) 4 mediating synthesis of inflammatory cytokines. AIMS: To explore the relationship between circulating HSP70 levels and activation of monocyte TLR4 and myocardial damage after AMI. METHODS AND RESULTS: This study examined circulating HSP70 and monocyte TLR4 levels in 52 patients with AMI and 20 controls, and analyzed ex vivo inflammatory cytokine productions using HSP70-stimulated monocytes. Circulating HSP70 levels were higher in AMI patients on day 1 after onset than in controls and remained elevated in AMI patients 14 days after onset. HSP70 levels were positively correlated with monocyte TLR4, plasma interleukin-6 and tumor necrosis factor-alpha levels in AMI patients. HSP70 levels 14 days after onset were higher in AMI patients with heart failure (n=15) than in those without heart failure. In our in vitro study, HSP70-stimulated monocytes resulted in dose-dependent TLR4 expression and release of inflammatory cytokines. TLR4 antibody inhibited inflammatory cytokines release. CONCLUSIONS: Elevated circulating levels of HSP70 may be involved in TLR4 signal-mediated immune response and the progression of heart failure after AMI.

Acute Disease↗

PubMed2006

Effect of pre-myocardial infarction angina pectoris on post-myocardial infarction arrhythmias after reperfusion therapy.

It has not been concluded whether there is a relation between pre-myocardial infarction angina pectoris (pre-MIAP) and reperfusion arrhythmia, although pre-MIAP has been reported to have a beneficial effect in preserving left ventricular function. Moreover, factors that are associated with reperfusion arrhythmias in patients with acute myocardial infarction (AMI) who have been successfully reperfused by reperfusion therapy are unknown. This study examined the predictive factors of reperfusion arrhythmias in patients with AMI who underwent successful reperfusion. The Japanese Intervention Trial in Myocardial Infarction study is a prospective, randomized trial that compares the outcome in patients with AMI who undergo intracoronary thrombolysis or primary percutaneous conventional coronary balloon angioplasty. One hundred ten consecutive patients with AMI who had been successfully reperfused in this study were categorized into 2 groups according to whether or not patients showed reperfusion arrhythmias. Multivariate logistic regression analysis was performed using 11 clinical factors to clarify the determinants of reperfusion arrhythmia. Reperfusion arrhythmias developed in 65 of 110 patients (59%). Multivariate logistic regression analysis confirmed that inferior AMI and pre-MIAP were independently associated with reperfusion arrhythmia. The odds ratio that predicted reperfusion arrhythmias was 2.37 (p = 0.0056) for inferior AMI. In contrast, the odds ratio was minimal at 0.24 for pre-MIAP (p = 0.036). In conclusion, pre-MIAP suppresses reperfusion arrhythmias, and inferior AMI is an independent factor for reperfusion arrhythmias.

Angina Pectoris↗

PubMed2006

MR angiography and CT angiography of the artery of Adamkiewicz: state of the art.

It is very important to assess the artery of Adamkiewicz before repair of the thoracoabdominal or descending thoracic aorta. Several studies have demonstrated the feasibility and advantages of noninvasive assessment of the artery of Adamkiewicz with magnetic resonance (MR) angiography and multi-detector row computed tomographic (CT) angiography. Recent advances in MR angiography and CT angiography have led to changes in the detectability of this artery. In the present study, both MR angiography and CT angiography were performed without complications for preoperative evaluation of 30 patients who underwent repair of the thoracoabdominal or descending thoracic aorta. MR angiography provided detection rates as high as 93% and 80% with the morphologic "hairpin turn" criterion and the anatomic "continuity" criterion, respectively. Sixteen-detector row CT angiography provided detection rates as high as 83% and 60%, respectively. Use of both MR angiography and CT angiography provided higher detection rates of 97% and 90%, respectively. The collateral pathways were depicted in seven cases (23%). MR angiography is superior for depiction of the artery of Adamkiewicz, especially when it arises from the false lumen of a dissecting aneurysm. CT angiography has a wide field of view and allows depiction of significant collateral pathways associated with the internal thoracic artery and intercostal arteries.

Adult↗

PubMed2006

Anti-inflammatory activity of 4,4'-dihydroxy-alpha-truxillic acid.

The oral anti-inflammatory activity of 4,4'-dihydroxy-alpha-truxillic acid (1) was compared with that of two other nonsteroidal anti-inflammatory drugs, loxoprofen sodium (LOX) and diclofenac sodium (DIC). The activity of 1 against the inflammatory pain response induced by formalin was comparable to that of LOX, but weaker than that of DIC. In the monosodium urate (MSU)-induced acute inflammatory model, 1 showed stronger anti-inflammatory activity than both LOX and DIC. The ED50 value for 1 was 4.5 micromol/kg, while the values for LOX and DIC were 65 and 25 micromol/kg, respectively. Otherwise, the oral single-dose toxicity of 1 was investigated in both sexes of Sprague-Dawley rats administered once at a dose of 2000 mg/kg. 1 showed no death, clinical signs, changes in body weight or pathological findings related to the treatment. In addition, no mutagenicity was observed in the reverse mutation assay. Furthermore, 1 did not show any ulcerogenic activity at doses ranging from 30 to 300 mg/kg in rat. Thus, 1 might be considered to be an effective anti-inflammatory agent with no deleterious adverse effect.

Animals↗

PubMed2006

Antinociceptive activities of alpha-truxillic acid and beta-truxinic acid derivatives.

Our recent study demonstrated that the dimeric structure of alpha-truxillic acid derivatives played an important role in the expression of their anti-inflammatory activities. In the present report, to investigate the correlation between the structure and anti-inflammatory activity, alpha-truxillic acid (1) and its derivatives (2-6), beta-truxinic acid (7) and its derivatives (8-10) were prepared, and their activities were evaluated in the formalin test. All compounds showed only weak or no activities against the neurogenic pain response, but demonstrated significant activities against the inflammatory pain response induced by formalin. The highest anti-inflammatory activities were observed for alpha-truxillic acid (1) and its derivative 4,4'-dihydroxy-alpha-truxillic acid (2). In addition, alpha-truxillic acid (1) and its derivative, alpha-truxillic acid bis(p-nitrophenyl)ester (5), showed higher anti-inflammatory activities than beta-truxinic acid (7) and the corresponding derivative (10). Furthermore, free carboxylic acids (1, 2) showed higher activities than their dimethyl esters (3, 4) and bis(p-nitrophenyl)ester (5). These results confirmed that the alpha-formation of dimeric structure and the free carboxylic acid were also important for the expression of anti-inflammatory activities. Otherwise, 4,4'-dichloro-beta-truxinic acid (8) had higher activity than its parent compound 7; furthermore, 1,3-dibenzoyl-2,4-di(4-chlorophenyl)cyclobutane (6) also showed strong anti-inflammatory activity. These results suggested that substituents in the phenyl groups were also important for the expression of anti-inflammatory activity. In order to gain information about their activity intensity, the anti-inflammatory activities of 2 and 4,4'-dichlorolated derivatives (6, 8) were compared with that of indomethacin (a nonsteroidal anti-inflammatory drug) in the formalin test. As a result, compounds 2, 6 and 8 showed stronger anti-inflammatory activities than indomethacin. These results suggested that alpha-truxillic acid and beta-truxinic acid derivatives might be developed into a new type of anti-inflammatory drug.

Analgesics↗

PubMed2006

Randomized crossover study of the long-term effects of pilsicainide and cibenzoline in preventing recurrence of symptomatic paroxysmal atrial fibrillation: influence of the duration of arrhythmia before therapy.

BACKGROUND: There is little information on the selection of antiarrhythmic agents for long-term prevention of paroxysmal atrial fibrillation (PAF). In the present study the preventive effects of pilsicainide (Pil) and cibenzoline (Cib) were compared in patients with PAF that was defibrillated at <48 h or >or=48 h after onset. METHODS AND RESULTS: A total of 60 patients (45 men, 15 women, mean age 66+/-10 years) were divided into 2 groups: Group I consisted of 22 patients in whom atrial fibrillation (AF) lasted for <48 h before cardioversion and Group II consisted of 38 patients in whom AF lasted for >or=48 h. A randomized, crossover protocol of treatment with Pil (150 mg/day) and Cib (300 mg/day) was used. Mean follow-up was 35+/-18 months. In Group I, the mean duration of maintenance of sinus rhythm was 12.3+/-2.9 months in patients treated with Pil, compared with 12.9+/-2.5 months in those givem Cib (p=NS between 2 groups). Actuarial event-free rates at 1, 3, 6, 12 months were 82%, 68%, 59% and 41%, respectively, in patients treated with Pil, and 91%, 77%, 68% and 50%, respectively, in those givenh Cib (p=NS between 2 groups). In Group II, the mean duration of maintenance of sinus rhythm was 1.6+/-0.5 months in patients treated with Pil, compared with 5.9+/-1.7 months in those given Cib (p<0.01). Actuarial event-free rates at 1, 3, 6, 12 months were 45%, 18%, 8% and 3%, respectively, in patients treated with Pil, and 63%, 45%, 29% and 16%, respectively, in those given Cib (p<0.05, at 12 months). CONCLUSIONS: Prolonged tachycardia (>or=48 h) in patients with PAF seems to cause electrical remodeling. Cib, a multichannel blocker, is considered to be more effective in preventing the recurrence of PAF in the electrically remodeled atria than Pil, a pure sodium-channel blocker.

Adult↗

PubMed2005

The association of C-reactive protein levels with carotid intima-media complex thickness and plaque formation in the general population.

BACKGROUND AND PURPOSE: An inflammatory response has been associated with the development of atherosclerosis. Our aim was to clarify which atherosclerotic changes (intima-media complex thickness [IMT] increase, plaque formation, and arterial dilatation) are associated with C-reactive protein (CRP) levels and to determine whether there are any gender differences. METHODS: Carotid ultrasound and measurement of high-sensitivity CRP (hs-CRP) levels were performed in 2056 subjects selected from a general population (mean age 58.3 years; 1290 men). RESULTS: In both genders, IMT significantly increased with increasing hs-CRP quartile (P<0.001), but this relationship disappeared after adjustment for age and other traditional cardiovascular risk factors. In men, but not women, carotid luminal diameter significantly increased with increasing hs-CRP levels (P<0.05), but again, this relationship disappeared with adjustment for age and other risk factors. However, in men, but not women, plaque score increased significantly with increasing hs-CRP quartile (P<0.01), even after adjustment for age and other traditional risk factors. CONCLUSIONS: CRP level was closely associated with early atherosclerotic changes represented by carotid plaque formation. However, the IMT increase was strongly associated with aging and other traditional cardiovascular risk factors rather than CRP level. In the general population, CRP may serve as a complementary and quantitative marker for atherosclerotic plaque formation in men but not women.

Adult↗

PubMed2005

Activated toll-like receptor 4 in monocytes is associated with heart failure after acute myocardial infarction.

Peripheral monocytosis may affect the development of heart failure (HF) after acute myocardial infarction (AMI). Activated toll-like receptor (TLR) 4 in monocytes plays an important role in the synthesis of proinflammatory cytokines. We examined TLR4 expression in monocytes, which may be a possible source of proinflammatory cytokines in AMI. Sixty-five patients with AMI and 20 healthy subjects (HS) were studied. Monocytes were isolated from peripheral blood on days 1 and 14 after the onset of AMI. TLR4 levels in monocytes were measured using real-time RT-PCR and flow cytometry. Generation capacity was evaluated by TLR4 levels and cytokine concentrations in the culture medium with lipopolysaccharide (LPS) stimulation. On day 1 after onset, baseline levels of TLR4 and plasma proinflammatory cytokines, notably IL-6 and TNF-alpha, were higher in AMI patients than in HS. These levels remained elevated in AMI patients 14 days after onset. Generation capacities of TLR4 and proinflammatory cytokines (IL-2, IL-6, IL-8, IL-10, GM-CSF and TNF-alpha) were increased in AMI patients compared to HS. LPS-stimulated TLR4 levels were positively correlated with IL-6 and TNF-alpha levels in AMI patients. Baseline TLR4 levels and plasma proinflammatory cytokine (IL-6, GM-CSF and TNF-alpha) levels were higher in AMI patients with HF (n = 22) than in those without HF. Generation capacities of TLR4 and proinflammatory cytokines (IL-6, GM-CSF and TNF-alpha) were greater in AMI patients with HF than in those without HF. Activation of TLR4 through a myocytic inflammatory reaction is associated with HF after AMI. These observations suggest that TLR4 signaling in monocytes may play a role in the development of HF after AMI.

Aged↗

PubMed2005

Association between serum C-reactive protein levels and pulse wave velocity: a population-based cross-sectional study in a general population.

Arterial stiffness as determined by aortic pulse wave velocity (PWV) has been shown to predict cardiovascular events in high-risk subjects such as those with hypertension or end-stage renal disease. Although it is suspected that low-grade inflammation as represented by increased C-reactive protein (CRP) plays an important role in the progression of atherosclerosis, it is not yet known whether serum CRP levels are associated with PWV. To examine the relationship between brachial-ankle PWV (baPWV) and serum CRP levels, several cardiovascular risk factors including these two markers (baPWV and CRP) were measured in 870 participants (mean age 59 years) randomly selected from a general population. Age, male gender, systolic blood pressure, heart rate, diabetes, and serum CRP levels increased with the quartiles divided by baPWV (all, p<0.01). By multiple regression analysis, age (p<0.001), systolic blood pressure (p<0.001), heart rate (p<0.001), body mass index (p<0.001), and CRP (p<0.01) were significant and independent predictors for baPWV. In conclusion, this cross sectional study has demonstrated in the general population that the arterial stiffness marker baPWV was independently correlated with serum CRP levels after adjustment for other established cardiovascular risks factors. This result suggests that baPWV may be a surrogate marker for atherosclerotic vascular damages including an inflammatory component.

Adult↗

PubMed2005

B-type natriuretic peptide testing for structural heart disease screening: a general population-based study.

BACKGROUND: Several types of structural heart disease are important precursors for congestive heart failure or cardioembolic stroke. We have previously demonstrated that plasma B-type natriuretic peptide (BNP) measurement is useful for detection of structural heart disease in a multiphasic health screening setting. To extend our hypothesis to the general population, the utility of BNP testing for identifying structural heart disease was assessed in a general population and in subgroups divided by sex, age, and presence/absence of risk factors. METHODS AND RESULTS: This cross-sectional cohort study measured plasma BNP concentrations in 993 randomly selected community-dwelling adults (mean age 58 years). All subjects underwent plasma BNP measurement and transthoracic echocardiography. Using prejudged criteria, 41 subjects were diagnosed to have some form of structural heart disease (mild left ventricular systolic dysfunction in 11, valvular heart disease in 9, hypertensive heart disease in 3, hypertrophic cardiomyopathy in 2, ischemic heart disease in 2, lone atrial fibrillation in 14). The utility of BNP testing was evaluated by receiver operating characteristic (ROC) analysis and by cost analysis for detection of 1 case within each subgroup of the cohort. Overall, the sensitivity and specificity of BNP testing for identification of structural heart disease were 61% and 92%, respectively. The area under the ROC curve was 0.77 (95% CI; 0.74-0.79). When sex-specific ROC analyses were performed, sensitivity and specificity were 61% and 91% in men, and 50% and 95% in women, respectively. Although the performance of BNP testing on the basis of these figures might be suboptimal, efficacy was improved in subgroups with a high prevalence of heart disease (>8%) such as the cohort aged > or =65 years (men, area under ROC curve = 0.88; cost <US $1400: women, area under ROC curve = 0.83; cost <US $3000) as well as the cohort having cardiovascular risk factors such as hypertension or diabetes (men, area under ROC curve = 0.85; cost <US $1700: women, area under ROC curve = 0.83; cost <US $3100). CONCLUSION: The present results suggest that BNP testing for structural heart disease screening in community-based populations is useful for cohorts with a high prevalence of heart disease. However, its efficacy is reduced in cohorts with a low prevalence rate.

Adult↗

PubMed2005

C-reactive protein co-expresses with tumor necrosis factor-alpha in the myocardium in human dilated cardiomyopathy.

BACKGROUND: C-reactive protein (CRP) has recently been reported to be present in cardiac tissue and to stimulate the production of proinflammatory cytokines. Cardiac expression of tumor necrosis factor-alpha (TNF-alpha) plays an important role in the pathogenesis of dilated cardiomyopathy (DCM). AIMS: To determine whether CRP co-expresses with TNF-alpha in the myocardium and to examine its association with clinical features in patients with DCM. METHODS AND RESULTS: Endomyocardial biopsy tissues were obtained from 41 DCM patients and 16 controls by right ventricular endomyocardial biopsy. Levels of CRP and TNF-alpha mRNA were measured by real-time RT-PCR. Immunohistochemistry and in situ hybridization were performed to identify the cellular sources of CRP and TNF-alpha. Both CRP and TNF-alpha mRNA were expressed in myocardium obtained from DCM patients, but not in controls. A positive correlation was found between CRP and TNF-alpha levels. CRP/TNF-alpha double staining was found to be colocalized in the cardiomyocytes of DCM patients. Both forms of mRNA were also expressed in cardiomyocytes. Both CRP and TNF-alpha mRNA levels were negatively correlated with systolic function and positively correlated with left ventricular volume in DCM patients. These mRNA levels were lower in DCM patients treated with a combination of spironolactone and either angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin II type 1 receptor blockers (ARBs) than in patients not treated with these drugs. CONCLUSION: Cardiac expression of CRP with TNF-alpha may function as a proinflammatory mediator in DCM and may be related to the clinical severity of DCM. Expression of both of these proteins was decreased in DCM patients receiving spironolactone and either ACEIs or ARBs.

Angiotensin II Type 1 Receptor Blockers↗

PubMed2005

Myocardial osteopontin expression is associated with collagen fibrillogenesis in human dilated cardiomyopathy.

BACKGROUND: Osteopontin (OPN), an extracellular matrix (ECM) protein, plays an important role in myocardial remodeling by promoting collagen synthesis and accumulation in experimental animal models. AIMS: We hypothesized that OPN could be expressed in myocardial tissues and contribute to collagen accumulation and myocardial dysfunction in human dilated cardiomyopathy (DCM). METHODS AND RESULTS: Endomyocardial biopsy tissues were obtained from 51 patients with DCM and 15 controls by right ventricular endomyocardial biopsy. OPN, collagen types I (Col I) and III (Col III) mRNA levels were measured by real-time reverse transcriptase polymerase chain reaction (RT-PCR). The cellular source of OPN was analyzed using immunohistochemistry and in situ hybridization. Myocardial collagen volume fraction (CVF) was determined by digital planimetry. OPN, Col I and Col III mRNA levels were higher in DCM patients than in controls (P<0.01). OPN mRNA levels were positively correlated with Col I levels and CVF in DCM patients (OPN vs. Col I: r=0.60, P<0.01; OPN vs. CVF: r=0.52, P<0.001). Immunostaining of OPN was present in cardiomyocytes from DCM patients. In situ hybridization identified cardiomyocytes as the major source of OPN mRNA transcription in DCM patients. OPN and Col I mRNA levels were highly expressed in the DCM subgroup with large left ventricular (LV) end-systolic diameter (LVESD > or = 54.5 mm) or low LV ejection fraction (LVEF < 29.5%). There was a weak positive correlation between OPN mRNA levels and LV end-systolic diameter (r=0.39, P<0.01). Levels of OPN mRNA were also negatively correlated with LV ejection fraction (r=-0.43, P<0.01). CONCLUSIONS: These results suggest that OPN may play a pivotal role in the development of Col-I-induced cardiac fibrosis and dysfunction in human DCM.

Cardiomyopathy, Dilated↗

PubMed2005

CRP levels are elevated in smokers but unrelated to the number of cigarettes and are decreased by long-term smoking cessation in male smokers.

BACKGROUND: It is not clear whether there is a dose-response relationship between the number of cigarettes smoked per day and CRP level and whether there is a relationship between the length of smoking cessation and CRP level. METHODS: Geometric mean levels of CRP were compared in smoking status groups for 1926 men aged 40 to 69 years using analysis of covariance. RESULTS: After adjusting for several confounding factors, geometric mean levels of CRP (mg/L) were significantly different among the three smoking status groups (0.41 in non-smokers, 0.57 in current smokers, 0.48 in past smokers, P < 0.05). A linear trend was not found in the relationship between CRP level and number of cigarettes smoked per day. The mean CRP level in the long cessation (> or =5 years) group was significantly lower than that in the short cessation (<5 years) group (0.45 vs. 0.58, P < 0.05) and similar to that in the non-smokers group (0.45 vs. 0.41, NS). CONCLUSIONS: CRP levels in current smokers are elevated but unrelated to the number of cigarettes smoked per day. In past smokers, long-term smoking cessation may contribute to the reduction in risk of development of cardiovascular diseases through inflammatory mechanisms.

Adult↗

PubMed2005

Activated tumour necrosis factor-alpha shedding process is associated with in-hospital complication in patients with acute myocardial infarction.

TACE [TNF-alpha (tumour necrosis factor-alpha)-converting enzyme] plays an essential role in the shedding of TNF-alpha, which could affect the outcome of AMI (acute myocardial infarction). To investigate the clinical significance of the TACE-TNF-alpha system in AMI, we examined TACE-mediated TNF-alpha synthesis in PBMCs (peripheral blood mononuclear cells), which are a possible source of TNF-alpha in AMI. Forty-one patients with AMI and 15 healthy subjects (HS) were enrolled in the present study. PBMCs were isolated from peripheral blood on day 1 and 14 after the onset of AMI. TACE and TNF-alpha mRNA levels and intracellular median fluorescence intensity were measured by real-time RT (reverse transcriptase)-PCR and flow cytometry respectively. TACE-mediated TNF-alpha production was evaluated in cultured PBMCs with PMA, which is known to activate TACE. Spontaneous TACE and TNF-alpha levels were higher in AMI patients than in HS (P<0.001). TACE and TNF-alpha levels in PMA-stimulated PMBCs were markedly increased in AMI patients compared with HS (P<0.001). There was a positive correlation between TACE and TNF-alpha levels in AMI. Although spontaneous and stimulated levels of TACE and TNF-alpha decreased 14 days after the onset of AMI, levels in AMI patients were higher than in HS. In AMI patients with in-hospital complications (n=15; pump failure in ten, recurrent myocardial infarction in one, malignant ventricular arrhythmia in three and cardiac death in one), spontaneous and stimulated levels of TACE and TNF-alpha were higher than in patients without complications (P<0.01). These levels were higher in AMI patients with in-hospital complications 14 days after onset. These results demonstrate that TACE-mediated TNF-alpha maturation in PBMCs may play an important role in poor outcomes from AMI, suggesting that TACE may be a potential target for the inhibition of cellular TNF-alpha production in AMI.

ADAM Proteins↗

PubMed2005

Anti-inflammatory activities of alpha-truxillic acid derivatives and their monomer components.

The anti-inflammatory activities of alpha-truxillic acid (1) and 4,4'-dihydroxy-alpha-truxillic acid (2) as well as their monomer components (E)-cinnamic acid (3) and (E)-p-coumaric acid (4) were evaluated in the formalin test. alpha-Truxillic acid (1) and its derivative 4,4'-dihydroxy-alpha-truxillic acid (2) exhibited significant activity against inflammatory pain response, while their monomer components (E)-cinnamic acid (3) and (E)-p-coumaric acid (4) did not show any activity against either neurogenic or inflammatory pain responses induced by formalin in mice. These results suggested that the dimeric structure might play an important role for the expression of anti-inflammatory activity. Furthermore, in order to gain information on their potencies, their anti-inflammatory activities were compared with that of incarvillateine (5) which contains the same dimeric structure and showed more potent antinociceptive activity than morphine in the formalin test. The activities of alpha-truxillic acid (1) and 4,4'-dihydroxy-alpha-truxillic acid (2) at the dose of 40 mg/kg against inflammatory pain response were equal to that of incarvillateine at doses of 20 mg/kg.

Animals↗

PubMed2005

Pharmacological study on the novel antinociceptive agent, a novel monoterpene alkaloid from Incarvillea sinensis.

To determine the antinociceptive mechanism of incarvillateine (INCA), the opiate antagonists nor-binaltorphimine (nor-BNI), beta-funaltrexamine (beta-FNA) and naltrindole (NTI) were pretreated prior to its injection in a formalin test. The antinociceptive effect of INCA was antagonized by nor-BNI (kappa-receptor antagonist) and beta-FNA (mu-receptor antagonist), while NTI (delta-receptor antagonist) did not influence its effect. Furthermore, the antinociceptive effect of INCA was blocked by theophylline (THEO), an adenosine-receptor antagonist. These results suggested that the antinociceptive effect arose from the activation of mu-, kappa-receptors and adenosine-receptor.

Alkaloids↗

PubMed2005

A monoterpene alkaloid from incarvillea sinensis.

A novel monoterpene alkaloid, named incarvillateine E, possessing three moles of incarvilline moieties, has been obtained from the aerial parts of Incarvillea sinensis LAM. (Bignoniaceae). On the basis of spectroscopic evidence, the structure of incarvillateine E has been characterized.

Alkaloids↗