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The amino acid derivative reactivity assay (ADRA) is an in chemico alternative assay for skin sensitization listed in OECD test guideline 442C. ADRA evaluates the reactivity of sensitizers to proteins, which is key event 1 in the skin sensitization adverse outcome pathway. Although the current key event 1 evaluation method is a simple assay that evaluates nucleophile and test chemical reactivity, mixtures of unknown molecular weights cannot be evaluated because a constant molar ratio between the nucleophile and test chemical is necessary. In addition, because the nucleophile is quantified by HPLC, the frequency of co-eluting the test chemical and nucleophile increases when measuring multi-component mixtures. To solve these issues, test conditions have been developed using a 0.5 mg/mL test chemical solution and fluorescence-based detection. Since the practicality of these methods has not been substantiated, a validation test to confirm reproducibility was conducted in this study. The 10 proficiency substances listed in the ADRA guidelines were tested three times at five different laboratories. The results of both within- and between-laboratory reproducibility were 100%, and the results of ultraviolet- and fluorescence-based measurements were also consistent. In addition to the proficiency substances, a new positive control, squaric acid diethyl ester, was tested three times at the five laboratories. The results showed high reproducibility with N-(2-(1-naphthyl)acetyl)-l-cysteine depletion of 37%-52% and α-N-(2-(1-naphthyl)acetyl)-l-lysine depletion of 99%-100%. Thus, high reproducibility was confirmed in both evaluations of the 0.5 mg/mL test chemical and the fluorescence-based measurements, validating the practicability of these methods.

Swim bladder tumors were detected in three out of 28 wavy medakas aged about 2 years old, all of which displayed abnormal swimming patterns caused by their spinal curvature. The tumors were located in the dorsal abdominal cavity. The swim bladder lumen was not detected in the region where it was originally assumed to be located, and that region was replaced with adipose tissue. The tumors were non-invasive, expansile, and encapsulated solid masses composed of a homogenous population of well-differentiated, densely packed, gas glandular epithelium-like cells. The tumor masses were connected to the rete mirabile, but the tumor cells did not infiltrate into them. Histopathologically, these tumors were diagnosed as adenomas originating from the gas glandular epithelium of the swim bladder. Spontaneous swim bladder tumors are rare in medaka, with an incidence of 0.02%; however, in the present study of wavy medaka, the incidence was much higher (10.7%). The long-term physical effects on the gas gland caused by swim bladder deformation considered to be a secondary effect of the spinal curvature may be an important factor in the proliferation of the gas glandular epithelium in the wavy medaka, resulting in the higher incidence of swim bladder tumors.

It is extremely rare to have multiple spontaneous proliferative lesions in young adult rats. Here, we report the occurrence of different proliferative lesions in multiple tissues of a 7-week-old female rat in a 1-week repeated toxicity study. Grossly, multiple white patches and nodules in the bilateral kidneys, femoral and subcutaneous masses, and a nodule in the liver were observed. Renal lesions were diagnosed as renal mesenchymal tumors. One of the femoral subcutaneous masses was diagnosed as an adenolipoma consisting of mammary epithelial cells and mature adipocytes. The other femoral and abdominal subcutaneous masses were diagnosed as lipomas consisting of mature adipocytes. The liver nodule was diagnosed as non-regenerative hepatocellular hyperplasia, which was characterized by the proliferation of slightly hypertrophic hepatocytes. In the cauda equina, the growth of enlarged Schwann cells around the axon was observed, and this lesion was diagnosed as a neuroma.

We performed a medaka bioassay for the carcinogenicity of methylazoxymethaol acetate (MAM-Ac) to examine the sequential histological changes in the liver from 3 days after exposure until tumor development. The medaka were exposed to MAM-Ac at a concentration of 2 ppm for 24 hours, and were necropsied at 3, 7, 10, 14, 21, 28, 35, 42, 49, 60, and 91 days after exposure. MAM-Ac induced four cases of hepatocellular adenoma and one case of hepatocellular carcinoma in 8 fish after 60 or 91 days of exposure. Histological changes in the liver until tumor development were divided into three phases. In the cytotoxic phase (1-10 days), MAM-Ac-exposed hepatocytes showed vacuolar degeneration and underwent necrosis and apoptosis, resulting in multiple foci of hepatocyte loss. In the repopulation phase (14-35 days), the areas of hepatocyte loss were filled with hepatic cysts and the remaining hepatocytes were surrounded by hepatic stellate-like cells (or spindle cells) and gradually disappeared. In the proliferation phase (42-91 days), the original hepatic parenchyma was regenerated and progressively replaced by regenerative hyperplastic nodules and/or liver neoplasms. The medaka retained a strong hepatocyte regenerative ability in response to liver injury. It is considered that this ability promotes the proliferation of initiated hepatocytes in multistep carcinogenesis and influences the development of liver tumor over a short period in medaka.

Amino acid derivative reactivity assay (ADRA) for skin sensitization was adopted as an alternative method in the 2019 OECD Guideline for the Testing of Chemicals (OECD TG 442C). The molar ratio of the nucleophilic reagent to the test chemicals in the reaction solution was set to 1:50. Imamura et al. reported that changing this molar ratio from 1:50 to 1:200 reduced in false negatives and improved prediction accuracy. Hence, a ring study using ADRA with 4 mM of a test chemical solution (ADRA, 4 mM) was conducted at five different laboratories to verify within- and between-laboratory reproducibilities (WLR and BLR, respectively). In this study, we investigated the WLR and BLR using 14 test chemicals grouped into three classes: (1) eight proficiency substances, (2) four test chemicals that showed false negatives in the ADRA with 1 mM test chemical solution (ADRA, 1 mM), but correctly positive in ADRA (4 mM), and (3) current positive control (phenylacetaldehyde) and a new additional positive control (squaric acid diethyl ester). The results showed 100% reproducibility and 100% accuracy for skin sensitization. Hence, it is clear that the ADRA (4 mM) is an excellent test method in contrast to the currently used ADRA (1 mM). We plan to resubmit the ADRA (4 mM) test method to the OECD Test Guideline Group in the near future so that OECD TG 442C could be revised for the convenience and benefit of many ADRA users.

We investigated the morphological effects of testosterone on placental development in a rat model of polycystic ovarian syndrome (PCOS). Testosterone propionate (TP), which was subcutaneously administered to pregnant rats with 5 mg/animal from gestation day (GD) 14 to GD 18, induced a maternal weight reduction without mortality or clinical signs from GD 19 onwards. A decrease in fetal and placental weight, an increase in intrauterine growth retardation (IUGR) rates, and histological changes in the placenta were observed on GD 21 but not on GD15 or 17. Histopathologically, on GD 21, the trophoblast septa thickened, and the maternal sinusoids were narrowed in the labyrinth zone, resulting in a small placenta. Additionally, the placental weight, thickness, and histological morphology in the labyrinth zone on GD 21 in the TP-treated group were nearly identical to those on GD 17 in the control and TP-treated groups. Therefore, it was assumed that the testosterone-induced small placenta was induced in association with the developmental inhibition of the fetal part of the placentas from GD 17 onwards.

Recently, intratracheal instillation has been focused on as a simple, low-cost alternative to the inhalation method. In this study, intratracheal instillation of sulfuric acid, a typical acidic compound, was performed to compare the acute toxicity of acidic compounds that could cause damage to the respiratory system between intratracheal instillation and inhalation. Sulfuric acid was administered to male rats at doses of 0.7, 2, 7, 20, and 60 mg/kg by dividing the total dose into four doses. General condition and body weight were examined up to 14 days after administration, and macropathological and histopathological examinations were performed. The half-lethal dose was then estimated. All animals administered 20 and 60 mg/kg sulfuric acid and one animal administered 2 mg/kg sulfuric acid died within 4 h after administration. No abnormalities were observed in other animals. At 20 and 60 mg/kg, multiple red foci or diffuse red areas were macroscopically observed in the lungs. In these lesions, histopathologically, clefts between the mucosal epithelium and basement membrane and necrosis of the alveolar epithelium were observed. Deaths in these groups may have resulted from lung injury. No notable changes were observed in other animals. Therefore, the half-lethal dose of sulfuric acid by intratracheal instillation was estimated as 7-20 mg/kg. The acute toxicity by intratracheal instillation was evaluated with two-fold sensitivity since the exposure at the half-lethal sulfuric acid concentration in inhalation studies was calculated as 43.2 mg/kg.

The morphological effects of β-naphthoflavone (β-NF) on placental development in pregnant rats were examined. β-NF, administered to pregnant rats intraperitoneally at 15 mg/kg bw from gestation day (GD) 9 to GD 14, had no effect on maternal body weight gain, mortality, or clinical sign. In the β-NF-exposed rats, intrauterine growth retardation (IUGR) rates increased on GDs 17 and 21, although there was no effect on fetal mortality rate, fetal or placental weight, or external fetal abnormality. Histopathologically, β-NF induced apoptosis and inhibition of cell proliferation of the trophoblastic septa in the labyrinth zone, resulting in its poor development. In the basal zone, β-NF induced spongiotrophoblast apoptosis and delayed glycogen islet regression, resulting in their cystic degeneration. β-NF-induced CYP1A1 expression was detected in the endothelial cells of the fetal capillaries in the labyrinth zone and in the endothelial cells of the spiral arteries in the metrial gland, but not in any trophoblasts. This indicates that CYP1A1 is inducible in the endothelial cells of the fetal capillaries in the labyrinth zone, and that these cells have an important role in metabolizing CYP1A1 inducers crossing the placental barrier.

Aims Oxaliplatin (l-OHP) is a key drug in therapeutic regimens for metastatic or advanced-stage colorectal cancer, but causes peripheral neuropathy as a dose-limiting adverse effect. It is reported that this peripheral neuropathy results from l-OHP accumulation in dorsal root ganglion (DRG) neurons, and that one of the transporters responsible for the accumulation in DRG neurons is organic cation transporter novel (OCTN) 1. Here, we examined whether co-administration of ergothioneine, a substrate/inhibitor of OCTN1, with l-OHP could prevent this peripheral neuropathy. Main methods l-OHP (4 mg/kg, i.p., twice/week, for 6 weeks) and ergothioneine or l -carnitine (1.5 or 15 mg/kg, i.v., twice per l-OHP administration) were administered to rats, and tissue/cellular platinum concentrations and peripheral neuropathy were determined. Expression of transporters in DRG neuronal cells was evaluated by real-time PCR and immunocytochemistry. Key findings On administration of l-OHP to rats, it accumulated in DRG neurons and their mitochondria, while negligible accumulation was found in Schwann cells. Expression of OCTN1 was observed in DRG neurons, especially in small- and medium-sized ones, which are responsible for the nociceptive response. In rats repeatedly administered l-OHP, co-administration of ergothioneine (15 mg/kg), but not l -carnitine, a substrate/inhibitor of OCTN2, decreased l-OHP accumulation in DRGs and development of the mechanical allodynia. Significance These results indicated that l-OHP-induced peripheral neuropathy was ameliorated by co-administration of ergothioneine, at least in part, via a decrease in its accumulation in DRG neurons. Plant diets contain ergothioneine, and thus their consumption might offer relief to patients suffering from l-OHP-induced peripheral neuropathy.

This paper proposes an aerial robot that can land on and cling to a steel structure using electric permanent magnets to be- have as a vibration sensor probe for use in vibration-based structural health monitoring. In the last decade, structural health monitoring techniques have been studied intensively to tackle with serious social issues that most of the infrastructures in advanced countries are being deteriorated. In the typical concept of the structural health monitoring, vibration sensors like accelerometers are installed in the structure to continuously collect the dynamical response of the operating structure to find a symptom of the structural damage. It is unreasonable, however, to permanently deploy the sensors to numerous infrastructures because most of the infrastructures except for those of primary importance do not need continuous measurement and evaluation. In this study, the aerial robot plays a role of a mobile detachable sensor unit. The design guidelines of the aerial robot that performs the vibration measurement from the analysis model of the robot is shown. Experiments to evaluate the frequency response function of the acceleration measured by the robot with respect to the acceleration at the point where the robot adheres are carried out. And the experimental results show that the prototype robot can measure the acceleration of the host structure accurately up to 150 Hz.

Eltrombopag (ELT), an orally available thrombopoietin receptor agonist, is a substrate of organic anion transporting polypeptide 1B1 (OATP1B1), and coadministration of ELT increases the plasma concentration of rosuvastatin in humans. Since the pharmacokinetic mechanism(s) of the interaction is unknown, the present study aimed to clarify the drug interaction potential of ELT at transporters. The OATP1B1-mediated uptake of ELT was inhibited by several therapeutic agents used to treat lifestyle diseases. Among them, rosuvastatin was a potent inhibitor with an IC(50) of 0.05 µM, which corresponds to one-seventh of the calculated maximum unbound rosuvastatin concentration at the inlet to the liver. Nevertheless, a simulation study using a physiologically based pharmacokinetic model predicted that the effect of rosuvastatin on the pharmacokinetic profile of ELT in vivo would be minimal. On the other hand, ELT potently inhibited uptake of rosuvastatin by OATP1B1 and human hepatocytes, with an IC(50) of 0.1 µM. However, the results of the simulation study indicated that inhibition of OATP1B1 by ELT can only partially explain the clinically observed interaction with rosuvastatin. ELT also inhibited transcellular transport of rosuvastatin in MDCKII cells stably expressing breast cancer resistance protein (BCRP), and was found to be a substrate of BCRP. The interaction of ELT with rosuvastatin can be almost quantitatively explained on the assumption that intestinal secretion of rosuvastatin is essentially completely inhibited by ELT. These results suggest that BCRP in small intestine may be the major target for interaction between ELT and rosuvastatin in humans.

When the quenching occurs in a superconducting coil, excessive joule heating in normal area may damage the coil. It is necessary to detect quenching in the coil as soon as possible and discharge the magnetic energy stored in the coil. Therefore, we propose a superconducting coil protection system based on an active power method. The system is highly resistant to the noise and does not require cancel voltage taps, so it is useful for both AC and DC coils. We have presented the effectiveness of the system using some test coils cooled in LN 2 or LHe. However, we have not discussed the effectiveness of the proposed system for helium-free cryocooled magnets, in which a larger temperature rise occurs after quenching than in liquid-cooled magnets. In this paper, we verify the effectiveness and practicality of the proposed system through coil protection tests for a cryocooled Nb 3 Al LTS coil.

A convergent total synthesis of F1α antigen, a member of the tumor-associated O-linked mucin glycosyl amino acid, was tried by one-pot sequential glycosylation. Highly α-selective glycosylation of amino acid 7 with thioglycoside 6 was successfully carried out by combining trityl trifluoromethanesulfonate (TrOTf) and N-iodosuccimide (NIS) which gave glycosyl amino acid 21 in high yield (97%, α/β = 83⁄17). Next, the glycosylation of thioglycoside 4 with galactosyl phenyl carbonate 2 or fluoride 3 was tried by the promotion of trityl tetrakis(pentafluorophenyl)borate [TrB(C6F5)4] or trifluoromethanesulfonic acid (TfOH); protected F1α 25 was afforded in 80 or 89% overall yield, respectively, by the further addition of glycosyl amino acid 5 and NIS. The desired trisaccharide was obtained in high yield after removal of the protecting groups. Next, a convergent total synthesis of branched hepta-β-glucoside 30 having phytoalexin-elicitor activity was efficiently performed by way of two one-pot sequential glycosyl...

A catalytic and stereoselective glycosylation of various glycosyl acceptors, such as methyl glycosides, thioglycosides, or a disarmed glycosyl fluoride, with benzyl-protected armed glycosyl fluoride was successfully carried out by using various protic acids in the presence of MS 5A. In the cases when trifluoromethanesulfonic acid (TfOH) or perchloric acid (HClO4) was used in diethyl ether (Et2O), α-glycosides were obtained as major products, while β-stereoselectivity was observed when tetrakis(pentafluorophenyl)boric acid [HB(C6F5)4] was used in a mixed solvent of trifluoromethylbenzene (BTF)–pivalonitrile (tBuCN) = 5 : 1. Stereoselectivity of this glycosylation was controlled by the properties of counter anions of the catalyst as well as by those of solvents. Also, one-pot trisaccharide synthesis was performed by successive addition of NIS and third-sugar to afford Glcα or β1–6Glcβ1–6Glc and Glcα or β1–6GlcNβ1–6Glc in excellent yields.

A catalytic and stereoselective glycosylation of several glycosyl acceptors with β-D-glycosyl fluoride was successfully performed in the presence of a catalytic amount of trityl tetrakis(pentafluorophenyl)borate (TrB(C6F5)4) or trifluoromethanesulfonic acid (TfOH). When TrB(C6F5)4 was used as a catalyst in the solvent pivalonitrile/(trifluoromethyl)benzene 1 : 5, the glycosylation proceeded smoothly to afford the glycosides in high yields with high β-D-stereoselectivities (see Table 3). Further, the glycosylation by the armed-disarmed strategy in the presence of this catalyst was established (see Table 4). Similarly, glycosylation catalyzed by the strong protic acid TfOH afforded the corresponding β-D-glycosides in good-to-excellent yields on treating β-D- glycosyl fluorides having a 2-O-benzoyl group with various glycosyl acceptors including thioglycosides (see Tables 6 and 7).

We report a case of a 40-years-old man diagnosed with osteopetrosis at the age of 11. Since 11 years old, he had sustained 11 long bone fractures and these previous fractures were all successfully treated conservatively. He also had osteomyelitis of the right mandible since he was 19 years old.In Janualy 1996, he had suffered a subtrochanteric fracture of the right femur after a minor contusion, and it was treated consevatively but bone union was not achieved. In October 1996, he was referred to our hospital for right thigh pain and severe anemia. Physical examination revealed anemia on the palpebral conjunctiva, syrinx of the right jaw, contracture of the right hip and bilateral coxa vara. Laboratory findings demonstrated severe anemia, and an elevated level of serum acid phosphatase. Skeletal roentgenograms showed the classic features of osteopetrosis; generalized osteosclerosis, bone within a bone appearance, sandwiched vertebrae, etc.He refused an operative treatment for the nonunited fracture, so we treated conservatively with a long leg brace. To date, the fracture has not united yet.

Use of solid film nanopore in which DNA is threaded through for efficient DNA sequencing devices has various practical issues concerned with nucleobase motion that should be controlled. Translocation rate and different orientation of nucleobases, stochastic motion of single-strand DNA through a nanopore introduce definite amount of noise into the signal defining interaction of nucleobase and nanopore. We propose to consider the single layer graphene nanopore as a two-way interaction scanning device. The interaction forces between pore and base are structure dependent, even within orientation and noise average over a base, and can be evaluated. The appropriate translocation rate of the base molecule provide a time-dependent function of interaction change inside of interaction interval of each individual base with graphene nanopore. In such case transient characteristics of the individual bases can be used for identification of the bases. The forces between bases and graphene nanopore of 1.5nm diameter are calculated as interaction characteristics of bases. Molecular dynamics method is used for the DNA base and graphene nanopore calculations with the MM2/MM3 potentials for the base and REBO graphene potential. Interaction potential between the bases and graphene are of the MM2/MM3 type although the possibility of the Van der Waals interaction only can also be considered. The noise of the force signal due to orientation of the bases in the pore is evaluated and base-dependent interaction recognition is considered relative to the magnitude of the AFM signal in the non-contact mode. The time-dependent in-plane for graphene transient force signal resolution for different bases is probed. Possibility of base identification by combination of transient in-plane force taken as orientation averaged signal is studied. Obtained results can simultaneously give additional information for the electronic transport calculations with possible transient base orientations relative to the edge of pore in graphene.

During studies for identification of biologically active components from natural sources, a new polyoxygenated xanthone mangostanol was isolated from the fruit hull of Garcinia mangostana , along with known xanthones, α-mangostin, γ-mangostin, gartanin, 8-deoxygartnin, 5,9-dihydroxy-2,2-dimethyl-8-methoxy-7-(3-methylbut-2-enyl)-2 H ,6 H -pyrano[3,2- b ]xanthen-6-one, garcinone E and 2-(γ,γ-dimethylallyl)-1,7-dihydroxy-3-methoxyxanthone and epicatechin. Spectroscopic analysis mainly by 1D and 2D NMR spectroscopy, established the structure of mangostanol {3,5,9-trihydroxy-2,2-dimethyl-8-methoxy-7-(3-methylbut-2-enyl)-2 H ,6 H -3,4-dihydropyrano[3,2- b ]xanthen-6-one} Mangostanol, and α- and γ-mangostin show moderate inhibitory effects on cAMP phosphodiesterase.

A bi-functional oxygen catalyst for use in the positive electrode of metal hydride (MH)/air secondary batteries needs a low overpotential for both oxygen reduction reaction (ORR) and oxygen evolution reaction (OER) in alkaline solutions, and a pyrochlore-type oxide catalyst, Bi2Ir2O7-z, is being developed by our group [1]. The catalyst’s activity for the oxygen reactions is normally evaluated with the positive electrode comprising the catalyst loaded on the conductive material, e.g., carbon powder, in which it is difficult to eliminate the influence of the conductive material on the catalytic activity. Another issue on the measurements with the positive electrode is that the specific activity of the catalyst is also difficult to determine, because it strongly depends on how the catalyst is loaded on the surface of the conductive material. These seem to be still the issues even when a flat surface of glassy carbon disk is used as the conductive substrate, which is popular as the method to investigate the oxygen reactions with a rotating-disk electrode (RDE). In this paper, we introduce a novel method to evaluate the catalytic activity of Bi2Ir2O7-z particles for the oxygen reactions with RDE using a titanium disk as the conductive material. The preparation procedure of Bi2Ir2O7-z nano-particles on the disk and the results obtained in different concentrations of KOH solutions are presented. Bi2Ir2O7-z particles were prepared by co-precipitation method which was carried out by the calcination of the precipitates obtained by adding excess NaOH solutions into the metal salt solution containing Bi(III) and Ir(IV). The obtained particles were loaded on a titanium disk by dropping the solution prepared by dispersing Bi2Ir2O7-z particles in distilled water under ultrasonic agitation. No binder and no ion exchange resin were used for the preparation. The oxide loaded titanium disk was analyzed by SEM and used as the working electrode for oxygen reduction and evolution. The concentration of KOH solutions was changed from 0.1 mol/L to 6 mol/L at 25 oC. The SEM results showed that Bi2Ir2O7-z particles were spread uniformly on the titanium disk and were the same size as those before loading, as shown in Fig. 1, and the ultrasonic agitation time was important to make the uniform distribution of the particles. The oxygen reduction current was measured in the solutions under N2 or O2 atmospheres, and the net current for oxygen reduction was obtained by subtracting the current under in N2 from that under O2. The titanium disk showed no current for oxygen reduction in both atmospheres. Therefore, the obtained current with the catalyst loaded titanium disk was given with no catalytic effect by titanium disk. The measurements were performed to evaluate the onset potential for oxygen reduction and evolution, the Tafel slope, the diffusion-limited current at different amounts of the catalyst. The effects of the KOH concentration on the polarization measurements were also investigated. The detailed results are presented in the paper. The authors acknowledge “Advanced Low Carbon Technology Research and Development Program (ALCA)” of Japan Science and Technology Agency (JST). References [1] C. Baba, K. Kawaguchi, and M. Morimitsu, Electrochemistry, 83, 855 (2015). Figure 1

Eltrombopag (ELT) is a novel thrombopoietin receptor agonist for the treatment of idiopathic thrombocytopenic purpura. Previous reports indicate that ELT is mainly eliminated in the liver, although its pharmacokinetic profile has not yet been clarified in detail. The purpose of the present study is to investigate the overall elimination mechanism of ELT. After intravenous administration of ELT to rats, approximately 40% of unchanged ELT was excreted into the bile in 72 h, whereas less than 0.02% of the dose was excreted in urine, indicating that liver is the major elimination organ for ELT. The total clearance was much lower than the hepatic blood flow rate and comparable with hepatic uptake clearance obtained from integration plot analysis. Coadministration of rifampicin, an organic anion transporter inhibitor, reduced both total clearance and hepatic uptake clearance of ELT. These results suggest that hepatic uptake is the rate-limiting process in the overall elimination of ELT. To further characterize the uptake mechanism, uptake of ELT by freshly isolated mouse hepatocytes was examined. The ELT uptake showed concentration and energy dependence and was inhibited by various compounds, including not only organic anions but also organic cations. Hepatic uptake clearance in vivo was reduced by coadministration of an organic cation, tetrapentylammonium. Finally, uptake of ELT was observed in human embryonic kidney 293 cells transfected with human hepatic transporters organic anion-transporting polypeptide (OATP) 1B1 and OATP2B1 and organic cation transporter OCT1. These results suggest that multiple transporters, including organic anion transporters and organic cation transporters, are involved in hepatic ELT uptake.

Fracture of the distal end of the radius is one of the most common fractures, and if comminuted it is difficult to treat with only cast immobilization. Therefore, sometimes it has to be treated with external fixation or open reduction and internal fixation. We reported two cases with Hoffmann external fixation. The first case was an old fracture, the other fresh and communited in the distal end of the radius. According to the point system by Saito, the results were fair and good. Both patients are almost satisfied with their return to the work force, and they can work as before.*Authors Note:In this last sentence the meaning needs to be made clearer.Are the patients almost able to return to work, or do you mean they are satisfied with the functional recovery of their arm?

A new efficient method for the catalytic stereoselective synthesis of various α-L-fucosides by using an easily available and stable glycosyl donor, 2,3,4-tri-O-benzyl-L-fucopyranosyl methoxyacetate, is established. Also, trimethylsilyl trifluoroacetate and lithium perchlorate are found to be effective additives in the synthesis of Fucα1-3GlcNAc and Fucα1-4GlcNAc linkages.

During studies for identification of biologically active components from natural sources, a new polyoxygenated xanthone mangostanol was isolated from the fruit hull of Garcinia mangostana , along with known xanthones, α-mangostin, γ-mangostin, gartanin, 8-deoxygartnin, 5,9-dihydroxy-2,2-dimethyl-8-methoxy-7-(3-methylbut-2-enyl)-2 H ,6 H -pyrano[3,2- b ]xanthen-6-one, garcinone E and 2-(γ,γ-dimethylallyl)-1,7-dihydroxy-3-methoxyxanthone and epicatechin. Spectroscopic analysis mainly by 1D and 2D NMR spectroscopy, established the structure of mangostanol {3,5,9-trihydroxy-2,2-dimethyl-8-methoxy-7-(3-methylbut-2-enyl)-2 H ,6 H -3,4-dihydropyrano[3,2- b ]xanthen-6-one} Mangostanol, and α- and γ-mangostin show moderate inhibitory effects on cAMP phosphodiesterase.

The anomerization reactions of several β-D-glucopyranosides proceed smoothly in the coexistence of MgBr2·OEt2 and a catalytic amount of titanium(IV)halides to afford the corresponding α-D-glucopyranosides. The desired alkyl α-glucosides and α-anomer of disaccharides such as Glcα1-6Glc were obtained in high yields with high stereoselectivities.

Several 2-deoxy-α-D-glucopyranosides are stereoselectively synthesized in high yields by glycosylation of various alcoholic nucleophiles with 3,4,6-tri-O-benzyl-2-deoxy-glucopyranose using a catalytic amount of trityl tetrakis(pentafluorophenyl)borate.

A catalytic and stereoselective glycosylation of glycosyl fluorides with several glucosides is successfully performed by using a catalytic amount of trityl tetrakis(pentafluorophenyl)borate.

The trityl tetrakis(pentafluorophenyl)borate [TrB(C6F5)4] catalyzed stereoselective synthesis of various disaccharides was successfully carried out by treating a new 2-O-acyl-protected glycosyl donor, 3,4,6-tri-O-benzyl-2-O-p-toluoyl-β-D-glucopyranosyl phenylcarbonate, with several glycosyl acceptors, thioglycosides, affording the corresponding disaccharides in high yields.

New highly effective promoter system for the glycosylation of thioglycoside, the combined use of stoichiometric amount of either N-iodosuccinimide or N-bromosuccinimide and a catalytic amount of TrB(C6F5)4, was developed and was successfully applied to the one-pot sequential synthesis of trisaccharides. In the first glycosylation step, 3,4,6-tri-O-benzyl-2-O-p-toluoyl-β-D-glucopyranosyl phenylcarbonate was treated with thioglycosides in the presence of a catalytic amount of TrB(C6F5)4 alone, and the following glycosylation with methyl α-D-glycosides was carried out by further addition of either N-iodosuccinimide or N-bromosuccinimide to the initially resulted reaction mixture to afford the corresponding trisaccharides in one-pot manner.

A catalytic and stereoselective glycosylation of various glycosyl acceptors, such as methyl glycosides, thioglycosides, or a disarmed glycosyl fluoride, with benzyl-protected armed glycosyl fluoride was successfully carried out by using various protic acids in the presence of MS 5A. In the cases when trifluoromethanesulfonic acid (TfOH) or perchloric acid (HClO4) was used in diethyl ether (Et2O), α-glycosides were obtained as major products, while β-stereoselectivity was observed when tetrakis(pentafluorophenyl)boric acid [HB(C6F5)4] was used in a mixed solvent of trifluoromethylbenzene (BTF)–pivalonitrile (tBuCN) = 5 : 1. Stereoselectivity of this glycosylation was controlled by the properties of counter anions of the catalyst as well as by those of solvents. Also, one-pot trisaccharide synthesis was performed by successive addition of NIS and third-sugar to afford Glcα or β1–6Glcβ1–6Glc and Glcα or β1–6GlcNβ1–6Glc in excellent yields.

The case is a 60-year-old woman who had complained of right coxalgia. At the first time, there was no fracture on roentgenograms of the hip. Significantly elevated erythrocyte sedimentation rate (ESR) level was found. After a month, the pathological fracture of the right femoral neck was fonud. The case was diagnosed as the multiple myeloma by open biopsy. And then the operation of endoprosthesis was performed. It is difficult to diagonose multiple myeloma without apparent fracture, but it is useful to examine bone scintgraphy and blood test.

A sixteen-ear-old boy came to our hospital complaining of the prominence of bony mass with audible and palpable grating localized at the medial side of the right scapula. Regular anteroposterior and tangential view of the scapula showed a bony mass on the sixth rib. At operation, there was an inflamed bursa containing bloody fluid between the scap ula and the sixth rib. The tumor was removed from the right sixth rib. Histological examination showed it to be an osteochondroma.Snapping scapula (scapulothoracic syndrome) is a relatively common clincal condition. It may be attributed to two underlying causes: (1) changes in the interposed soft tissues, the muscles, and the bursae between the scapula and the chest wall and (2) changes in the congruence between anterior scapular surface and underlying chest wall.The snapping scapula of this case was due to the projection of an exostosis of the right sixth rib and the inflamed bursae between the scapula and exostosis.