In vitro antimicrobial activities of 1-methoxyficifolinol, licorisoflavan A, and 6,8-diprenylgenistein against Streptococcus mutans.

The objective of the study was to investigate the antimicrobial effects of purified single compounds from ethanol-extracted licorice root on Streptococcus mutans. The crude licorice root extract (CLE) was obtained from Glycyrrhiza uralensis, which was subjected to column chromatography to separate compounds. Purified compounds were identified by mass spectrometry and nuclear magnetic resonance. Antimicrobial activities of purified compounds from CLE were evaluated by determining the minimum inhibitory concentration and by performing time-kill kinetics. The inhibitory effects of the compounds on biofilm development were evaluated using crystal violet assay and confocal microscopy. Cell toxicity of substances to normal human gingival fibroblast (NHGF) cells was tested using a methyl thiazolyl tetrazolium assay. Chlorhexidine digluconate (CHX) was used in the control group. Three antimicrobial flavonoids, 1-methoxyficifolinol, licorisoflavan A, and 6,8-diprenylgenistein, were isolated from the CLE. We found that the three flavonoids and CHX had bactericidal effects on S. mutans UA159 at the concentration of ≥4 and ≥1 µg/ml, respectively. The purified compounds completely inhibited biofilm development of S. mutans UA159 at concentrations over 4 µg/ml, which was equivalent to 2 µg/ml of CHX. Confocal analysis showed that biofilms were sparsely scattered in the presence of over 4 µg/ml of the purified compounds. However, the three compounds purified from CLE showed less cytotoxic effects on NHGF cells than CHX at these biofilm-inhibitory concentrations. Our results suggest that purified flavonoids from CLE can be useful in developing oral hygiene products, such as gargling solutions and dentifrices for preventing dental caries.

[Preparation and characterization of vincristine sulfate-loaded PLGA microspheres].

OBJECTIVE: To prepare the vincristine sulfate (VCR) microspheres by W/O/O solvent evaparation method and evaluate the effect of zinc carbonate (ZnCO3) on the morphology and release kinetics of the microspheres. METHODS: Degradation kinetic of VCR was tested in PBS of four different pH values at 37TC to select the optimal incubation medium for in vitro release. Microspheres were made with or without Zn-CO3 (w/w 5% and 10%) in the polymeric phase. The properties and in vitro release profiles of the microspheres were examed. RESULTS: ZnCO3 increased the stability of VCR in the PLGA microspheres. During the 36 days of in vitro release, the accumulative release of VCR from the microspheres reached > 70% when added with ZnCO3, and was (54.2 +/- 1.1)% when no ZnCO3 was added. 10% ZnCO3 showed superior effect than 5% ZnCO3 in the stabilization of microspheres. CONCLUSIONS: Adding ZnCO3 is essential during the preparation of PLGA microspheres. It can remarkably improve the stability of drugs in the acid microenvironment inside PL-GA microspheres and decrease the VCR degradation during incubation.