[Case-control study on risk factors of recurrent aphthous ulcer].

PURPOSE: To evaluate the risk factors for the occurrence of recurrent aphthous ulcer (RAU) in Fuzhou city by case-control study. METHODS: A questionnaire survey of 113 patients with RAU and 102 non-RAU patients in the same hospital was made, including 58 items. Chi-square test and conditional logistic regression were used for monovariate and multivariate analysis respectively with SPSS23.0 software package. RESULTS: One-way Chi-square test showed that immigrants, genetic factors, gastrointestinal disorders, menstrual period, oral health status, anxiety were related factors for patients suffering from RAU. Conditional logistic regression analysis indicated that genetic factors as well as more dental calculus in the oral cavity were RAU risk factors. Tendency Chi-square test revealed that there was a negative correlation between the occurrence of RAU and vegetable intake, and a positive correlation with the amount of dental calculus and soft scale in the oral cavity. CONCLUSIONS: The occurrence of RAU is the result of combination of "multiple factors" in the digestive system, genetic system, immune system and oral microenvironment.

Novel selective cannabinoid CB(1) receptor antagonist MJ08 with potent in vivo bioactivity and inverse agonistic effects.

AIM: To characterize the biological profiles of MJ08, a novel selective CB(1) receptor antagonist. METHODS: Radioligand binding assays were performed using rat brain and spleen membrane preparations. CB(1) and CB(2) receptor redistribution and intracellular Ca(2+) ([Ca(2+)](i)) assays were performed with IN CELL Analyzer. Inverse agonism was studied using intracellular cAMP assays, and in guinea-pig ileum and mouse vas deferens smooth muscle preparations. In vivo pharmacologic profile was assessed in diet-induced obesity (DIO) mice. RESULTS: In radioligand binding assay, MJ08 selectively antagonized CB(1) receptor (IC(50)=99.9 nmol/L). In EGFP-CB(1)_U2OS cells, its IC(50) value against CB(1) receptor activation was 30.23 nmol/L (SR141716A: 32.16 nmol/L). WIN 55,212-2 (1 µmol/L) increased [Ca(2+)](i) in the primary cultured hippocampal neuronal cells and decreased cAMP accumulation in CHO-hCB(1) cells. MJ08 (10 nmol/L-10 µmol/L) blocked both the WIN 55,212-2-induced effects. Furthermore, MJ08 reversed the inhibition of electrically evoked twitches of mouse vas deferens by WIN 55,212-2 (pA(2)=10.29±1.05). MJ08 and SR141716A both showed an inverse agonism activity by markedly promoting the contraction force and frequency of guinea pig ileum muscle. MJ08 significantly increased the cAMP level in CHO-hCB(1) cells with an EC(50) value of 78.6 nmol/L, which was lower than the EC(50) value for SR141716A (159.2 nmol/L). Besides the more potent pharmacological effects of cannabinoid CB(1) receptor antagonism in DIO mice, such as reducing food intake, decreasing body weight, and ameliorating dyslipidemia, MJ08 (10 mg/kg) unexpectedly raised the fasted blood glucose in vivo. CONCLUSION: MJ08 is a novel, potent and selective CB(1) receptor antagonist/inverse agonist with potent bioactive responses in vitro and in vivo that may be useful for disclosure the versatile nature of CB(1) receptors.