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We succeeded in the electrical polarization of β-tricalcium phosphate (β-TCP) granules and performed an unprecedented attempt to implant them into maxillary bone defects in canines to confirm their ability to facilitate new bone formation. Two holes were drilled into each maxilla half of a canine and filled with electrically polarized and nonpolarized β-TCP granules (grouping assignment was decided randomly). The implanted specimens were dissected en bloc and used for microcomputed tomography (μCT) observations and histological analyses 4 and 8 weeks after the operation. New bone ingrowth in the bone hole progressed over time from the superficial layer of the cortex toward the inner cancellous bone. The percentage area of new bone in the bone hole, as measured by μCT in the sagittal plane, was significantly larger after 4 and 8 weeks, and that measured by H&E-stained specimens in the transverse plane after 4 weeks was significantly larger in the polarized group than in the nonpolarized group. In addition to the structural stability and chemical characteristics of the β-TCP granules, electrical stimulation bears influence not indirectly but directly on osteogenic and vessel cells, which might work cooperatively for the early initiation of the bone formation process.

Objective The present study aimed to evaluate the histological outcome of tunnel β-TCP blocks grafting in extraction sockets missing the buccal bone wall, after 6 months of healing. Background Tunnel β-tricalcium phosphate (β-TCP) blocks made of randomly organized tunnel-shaped β-TCP ceramics appeared promising for alveolar ridge preservation in tooth extraction sockets missing the buccal bone, in a previous study in dogs, with a 2-month healing time. Methods In six beagle dogs, the maxillary first premolars were extracted and the buccal bone was surgically removed to create bone defects of 4 mm (mesio-distal) × 5 mm (apico-coronal) × 4 mm (bucco-palatal). Thus, extraction sockets missing the buccal bone plate were grated with tunnel β-TCP blocks (test) or left empty for spontaneous healing (control). Histology/histomorphometry was performed after 6 months of healing. Results The horizontal bucco-palatal width of the alveolar ridge was significantly greater at test sites than at control sites. The amount of mineralized tissue was greater at test sites (57.8% ± 11.1%) than at control sites (28.9% ± 8.5%), while the amount of connective tissue was significantly greater at control sites (41.7% ± 6.4%) than at test sites (19.6% ± 9.2%). No significant difference was found between sites in terms of basic multicellular units and bone marrow. Residual β-TCP at test sites was 5.8% ± 3.2%. Conclusion Grafting with tunnel β-TCP block significantly limited the resorption of the alveolar ridge at extraction sockets missing the buccal bone compared with sites left to heal spontaneously, even after 6-month follow-up.

Various bone graft products are commercially available worldwide. However, there is no clear consensus regarding the appropriate bone graft products in different clinical situations. This review is intended to summarize bone graft products, especially alloplastic bone substitutes that are available in multiple countries. It also provides dental clinicians with detailed and accurate information concerning these products. Furthermore, it discusses the prospects of alloplastic bone substitutes based on an analysis of the current market status, as well as a comparison of trends among countries. In this review, we focus on alloplastic bone substitutes approved in the United States, Japan, and Korea for use in periodontal and bone regeneration. According to the Food and Drug Administration database, 87 alloplastic bone graft products have been approved in the United States since 1996. According to the Pharmaceuticals and Medical Devices Agency database, 10 alloplastic bone graft products have been approved in Japan since 2004. According to the Ministry of Health and Welfare database, 36 alloplastic bone graft products have been approved in Korea since 1980. The approved products are mainly hydroxyapatite, β-tricalcium phosphate, and biphasic calcium phosphate. The formulations of the products differed among countries. The development of new alloplastic bone products has been remarkable. In the near future, alloplastic bone substitutes with safety and standardized quality may be the first choice instead of autologous bone; they may offer new osteoconductive and osteoinductive products with easier handling form and an adequate resorption rate, which can be used with growth factors and/or cell transplantation. Careful selection of alloplastic bone graft products is necessary to achieve predictable outcomes according to each clinical situation.

Background and objective It is well known that recombinant human fibroblast growth factor-2 (rhFGF-2) signaling plays an important role in tissue repair and regeneration. rhFGF-2 strongly binds to acidic gelatin via ionic linkages and is gradually released upon gelatin decomposition. On the other hand, the linkage between rhFGF-2 and basic gelatin is so weak that most rhFGF-2 is rapidly released from basic gelatin by simple desorption. Gelatin/β-tricalcium phosphate (β-TCP) sponges, which comprise 50 wt% gelatin and 50 wt% β-TCP in a cross-linked structure, can release rhFGF-2 gradually owing to their electrical features. In a previous study, we reported that new bone height in the test group using rhFGF-2 with acidic gelatin/β-TCP sponges was significantly greater than that in the control group using acidic gelatin/β-TCP sponges alone in a ridge augmentation model in dogs. However, whether these results depend on controlled release by the gelatin/β-TCP sponges remains controversial. In this study, we evaluated the effects of controlled release by comparing acidic and basic gelatin/β-TCP sponges with different isoelectric points (IEP) on ridge augmentation in dogs. Materials and methods Twelve weeks after extraction of the maxillary second and third incisors of six dogs, critically sized saddle-type defects (8 mm length × 4 mm depth) were surgically created bilaterally 2 mm from the mesial side of the canine. Acidic gelatin/β-TCP sponges (IEP 5.0) soaked with 0.3% rhFGF-2 were applied to the defect in the acidic group, whereas basic gelatin/β-TCP sponges (IEP 9.0) soaked with 0.3% rhFGF-2 were applied to the defect in the basic group. Twelve weeks after surgery, biopsy specimens were obtained and subjected to microcomputed tomography (micro-CT) and histological analyses. Results New bone area detected by micro-CT analysis was significantly smaller in the basic group than in the acidic group. New bone height calculated by histologic sections was significantly lower in the basic group than in the acidic group. The total tissue height was lower in the basic group than in the acidic group. However, the differences between both sites were not significant. Conclusions These findings suggest that in ridge augmentation of saddle-type defects, controlled release of rhFGF-2 induces notably more alveolar bone formation than does short-term application of rhFGF-2.

We have developed a new route for synthesizing mercapto C-nucleoside possessing a phenyl thiol group, using organometallic reagents. Duplexes incorporating redox-active nucleobase analogues display a high melting temperature under oxidation condition. Originally, we had anticipated the production of mercapto C-nucleoside using a Friedel–Crafts coupling reaction via bis(toluoyl) protected ribose and tert -butyl phenyl sulfide in the presence of Lewis acid. However, an undesired coupling compound was formed by cleavage of the S - tert -butyl group of S - tert -butyl phenyl sulfide by Lewis acids (BF 3 Et 2 O, SnCl 4 ). The highly stereoselective synthesis of mercapto C-nucleoside was, however, achieved by the addition of p -( tert -butyl)thiophenyllithium to a disiloxane-protected 2-deoxyribonolactone. This route showed moderately good yield at all steps. The tert -butyl moiety coupled to the sulfur atom at the phenyl group was converted to a 2-nitrophenylsulfenyl (Nps) group, and the Nps group was easily cleaved by ethanethiol to afford the desired compound and its disulfide dimer.

A series of five new fluorescent deoxynojirimycin (DNJ) conjugates were synthesized and evaluated for their inhibitory effect (IC50) on several α- and β-glucosidases. Three of the conjugates showed enhanced activity. The two synthetic conjugates, DNJ-CF31 and DNJ-Me 2, exhibited improved α-glucosidase inhibitory effects compared to DNJ and miglitol. Interestingly, conjugates 1 and 2 showed strong inhibition of almond-derived β-glucosidase, in contrast to the inhibition tendencies of other inhibitors. Conjugate 5 strongly inhibited rat intestinal maltase, even at 0.10μM. A docking study indicated that all five conjugates bind to the active site of α-glucosidase (PDB: 3L4V, derived from Homo sapiens). The DNJ portion of the conjugate fits into the cavity of the enzyme, and the fluorescent part locates randomly on the outside surface. Thus, it is likely that these conjugates can specifically recognize intestinal cells, specifically the α-glucosidase on cell membranes.

Herein, we describe β-selective coupling between a modified uracil and a deoxyribose to produce functionalized nucleosides catalyzed by thymidine phosphorylase derived from Escherichia coli. This enzyme mediates nucleobase-exchange reactions to convert unnatural nucleosides possessing a large functional group such as a fluorescent molecule, coumarin or pyrene, linked via an alkyl chain at the C5 position of uracil. 5-(Coumarin-7-oxyhex-5-yn)uracil (C4U) displayed 57.2% conversion at 40% DMSO concentration in 1.0 mM phosphate buffer pH 6.8 to transfer thymidine to an unnatural nucleoside with C4U as the base. In the case of using 5-(pyren-1-methyloxyhex-5-yn)uracil (P4U) as the substrate, TP also could catalyse the reaction to generate a product with a very large functional group at 50% DMSO concentration (21.6% conversion). We carried out docking simulations using MF myPrest for the modified uracil bound to the active site of TP. The uracil moiety of the substrate binds to the active site of TP, with the fluorescent moiety linked to the C5 position of the nucleobase located outside the surface of the enzyme. As a consequence, the bulky fluorescent moiety binding to uracil has little influence on the coupling reaction.

We investigated the antimicrobial activities of twelve derivatives of benzyl phenyl sulfide by using Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) values against 10 microbial strains. These derivatives of benzyl phenyl sulfides were synthesized by means of the nucleophilic coupling reaction at our laboratory. MIC testing revealed that all synthetic derivatives of benzyl and 4-methoxybenzyl phenyl sulfides had no effect against the tested microbial strains. However, the compounds of 4-nitrobenzyl phenyl sulfide showed antimicrobial activity against many of the tested strains. Above all, 4-nitrobenzyl 4-chlorophenyl sulfide 11 exhibited the strongest and widest ranging inhibitory effects among the twelve synthetic compounds. We researched the antimicrobial activities of the coupling materials of sulfide. As a result, it was considered important for the expression of antimicrobial activities that the sulfide had a 4-nitrobenzyl group and 4-chlorophenyl group in the same molecule as in the case of benzyl phenyl sulfide.

Here, we present the solution structure of a DNA duplex containing a disulfide base pair (S-DNA). The unnatural nucleoside "S" possessing a thiophenyl group as base was incorporated into a self-complementary singled-stranded oligonucleotide. Crosslinking of the disulfide base pair was analyzed by non-denaturing polyacrylamide gel electrophoresis. Under oxidizing conditions a high molecular weight band as 18 mer, corresponding to the double-stranded molecule (5'-GCGASTCGC: 3'-CGCTSAGCG), was found, whereas single-stranded self-complementary 9 mer oligonucleotide GCGASTCGC was detected in the presence of a reducing agent. These results suggest that the oligonucleotide is covalently linked by disulfide bonding under oxidizing conditions, which can be reversibly reduced to two thiol groups under reducing conditions. CD spectrum of S-DNA (CGASTCG) under oxidizing conditions suggested that the duplex had a right-handed double-stranded structure similar to that of natural DNA (B-form, CGATCG). NMR studies confirmed that this CGASTCG resembled natural B-DNA and that the two phenyl rings derived from the disulfide base pairing intercalated into the duplex. However, these two phenyl rings were not positioned in the same plane as the other base pairs. Specifically, NOEs suggest that although CGASTCG adopts a structure similar to B-type DNA, the S-DNA duplex is bent at the point of disulfide base pairing to face the major groove.