Clinical effect of a dentifrice containing three kinds of bactericidal ingredients on periodontal disease: a pilot study in patients undergoing supportive periodontal therapy.

OBJECTIVE: This study aimed to evaluate clinically the effect of a novel dentifrice containing three kinds of bactericidal ingredients on periodontal disease. RESULTS: This was a single-arm, prospective clinical study that enrolled patients with periodontitis undergoing supportive periodontal therapy. Periodontal examination, microbiological testing of saliva samples, and evaluation of inflammatory markers (IL-1ß, IL-6, IL-8, TNF-α) in gingival crevicular fluid were performed. After 4 weeks of the use of test dentifrice, these parameters were re-evaluated. The use of dentifrice was also subjectively evaluated by clinicians and participants. Among 30 participants, there were significant improvements in the periodontal and microbiological parameters, and the level of interleukin-1ß in the gingival crevicular fluid, following the use of the test dentifrice. In clinicians' subjective evaluation of the overall usefulness of the dentifrice, 'mild' and 'moderate' improvement accounted for 83% of the total responses. In the participants' subjective evaluation, the majority indicated their experience of the use as favorable. Within the limitations of this study, it is suggested that the progression of periodontal disease during the supportive periodontal therapy can be prevented by the use of the test dentifrice. Trial registration UMIN Clinical Trials Registry (UMIN-CTR) 000023175. Date of formal registration: July 14, 2016 ( https://upload.umin.ac.jp/cgi-open-bin/ctr/ctr_view.cgi?recptno=R000026716 ).

Effect of enzymatically modified isoquercitrin in spontaneously hypertensive rats.

Enzymatically modified isoquercitrin (EMIQ) is a water-soluble glycoside of quercetin produced from rutin by enzymatic treatment. We investigated the anti-hypertensive effect of orally administered EMIQ in spontaneously hypertensive rats (SHR). The systolic blood pressure (SBP) in SHR administered EMIQ at a dose of 3 and 26 mg/kg/d was significantly lower than that in the control group on d 22, 36 and 50 of administration. The effect of EMIQ (26 mg/kg/d) was higher than equimolar administration of quercetin. Diltiazem administered as a positive control also suppressed the increase in SBP. and the effect was stronger than that of EMIQ. In the control group, the mean values of mean blood pressure (MBP) and diastolic blood pressure (DBP) were increased after the start of administration. Although diltiazem suppressed the increase in MBP, no significant changes were observed in the EMIQ groups. Compared with the control group, EMIQ groups showed the incidental changes of MBP and heart rate on day 22 of administration only. These results indicate that EMIQ suppressed the increase in SBP in SHR dose-dependently, and was more effective than the aglycone quercetin. It was also speculated that EMIQ showed higher anti-hypertensive effect than quercetin due to the high bioavailability, and the mechanism of SBP suppression is possibly through the improvement of endothelial NO production. In conclusion, our results suggest that EMIQ shows possibility as a naturally-derived safe food material which has an antihypertensive effect.

Effects of uptake of flavonoids on oxidative stress induced by hydrogen peroxide in human intestinal Caco-2 cells.

The relation between the uptake of flavonoids and the response of human colon adenocarcinoma Caco-2 cells exposed to oxidative stress induced by hydrogen peroxide (H(2)O(2)) was examined. Flavonoid aglycones were incorporated into Caco-2 cells in a concentration- and time-dependent manner, but neither glycosides nor unstable myricetin were incorporated into the cells. The incorporated flavonoids reduced the reactive oxygen species (ROS) induced by H(2)O(2) in the cells in proportion to the amount incorporated and the radical scavenging activity of flavonoids. But, flavonoids with high radical scavenging activity also generated H(2)O(2). The activity decreasing intracellular ROS was inversely related to the H(2)O(2) scavenging activity of flavonoids. Therefore, the decrease in the amount of intracellular ROS induced by H(2)O(2) was not directly due to the scavenging of H(2)O(2), but rather to the scavenging of ROS generated from H(2)O(2). These results suggest that strong antioxidative flavonoids have both a cytoprotective effect owing to the scavenging of ROS and cytotoxic effect caused by the generation of H(2)O(2).

Transepithelial permeability of myricitrin and its degradation by simulated digestion in human intestinal Caco-2 cell monolayer.

Myricitrin permeated the human intestinal Caco-2 cell monolayer via the paracellular pathway in a time- and concentration-dependent manner. Myricitrin was not conjugated by Caco-2 cells. Myricitrin was degraded by simulated intestinal digestion, but permeability did not change significantly.

Myricitrin degraded by simulated digestion inhibits oxidation of human low-density lipoprotein.

The inhibitory effects of myricitrin on the oxidation of human low-density lipoprotein were investigated before and after its degradation by simulated digestion. Myricitrin strongly inhibited the low-density lipoprotein oxidation induced by either 2,2'-azobis (2-amidinopropane) dihydrochloride or CuSO4 in a concentration-dependent manner. Myricitrin was very stable under an acidic condition (pH 1.8) corresponding to the gastric environment, but it was easily degraded under an alkaline condition (pH 8.5) corresponding to the intestinal environment. However, degraded myricitrin also had a strong inhibitory effect on the oxidative degradation of alpha-tocopherol, cholesterol and apolipoprotein B-100 in low-density lipoprotein. Our study revealed that myricitrin was degraded into many components under a mildly alkaline condition, but the degraded myricitrin still retained the free radical-scavenging and copper-chelating activities toward low-density lipoprotein.