Antiallergic Activity of 6-Deoxy-2-O-methyl-6-(N-hexadecanoyl)amino-L-ascorbic Acid

Allergy is an excessive immune response to a specific antigen. Type I allergies, such as hay fever and food allergies, have increased significantly in recent years and have become a worldwide problem. We previously reported that an ascorbic acid derivative having palmitoyl and glucosyl groups, 2-O-α-D-glucopyranosyl-6-O-hexadecanoyl-L-ascorbic acid (6-sPalm-AA-2G), showed inhibitory effects on degranulation in vitro and on the passive cutaneous anaphylaxis (PCA) reaction in mice. In this study, several palmitoyl derivatives of ascorbic acid were synthesized and a structure–activity relationship study was performed to discover more potent ascorbic acid derivatives with degranulation inhibitory activity. 6-Deoxy-2-O-methyl-6-(N-hexadecanoyl)amino-L-ascorbic acid (2-Me-6-N-Palm-AA), in which a methyl group was introduced into the hydroxyl group at the C-2 position of ascorbic acid and in which the hydroxyl group at the C-6 position was substituted with an N-palmitoyl group, exhibited much higher inhibitory activity for degranulation in vitro than did 6-sPalm-AA-2G. 2-Me-6-N-Palm-AA strongly inhibit the PCA reaction in mice at lower doses than those of 6-sPalm-AA-2G. These findings suggest that 2-Me-6-N-Palm-AA may be a promising therapeutic candidate for allergic diseases

An epidemiological study on anemia among institutionalized people with intellectual and/or motor disability with special reference to its frequency, severity and predictors

BACKGROUND: To examine the type, frequency, severity, and predictors of anemia and its relationship with co-morbid conditions among institutionalized people with intellectual and/or motor disability. METHODS: We conducted a cross-sectional study at a public facility for people with intellectual and/or motor disability in Ibaraki prefecture, Japan. Health checkup data obtained in 2001 from 477 people with intellectual disability (male: 286, average age 40.6 ± 12.3; female: 191, average age 45.1 ± 11.6) were retrospectively reviewed. RESULTS: The prevalence of anemia among male participants was higher than in female participants for each disability category (intellectual disability, 41.1%, 4.2%; cerebral palsy, 37.5%, 4.8%; Down's syndrome, 15.0%, 0%; severe motor and intellectual disabilities, 61.9%, 16.7%). Most participants with anemia (93.8 – 100%) showed a normocytic normochromic anemia pattern. Multivariate analysis revealed that factors related to an increase in frequency included sex (male), low body mass index (BMI), use of anticonvulsants or major tranquilizers, and a high zinc sulfate turbidity test (ZTT) value. No clinically diagnosed co-morbid condition was found to be related to the presence of anemia. CONCLUSION: A high frequency of mild normocytic normochromic anemia in institutionalized people with intellectual and/or motor disability was observed, particularly among males. Medications and chronic inflammation may increase the risk of anemia

Antiallergic Activity of 6-Deoxy-2-O-methyl-6-(N-hexadecanoyl)amino-l-ascorbic Acid

Allergy is an excessive immune response to a specific antigen. Type I allergies, such as hay fever and food allergies, have increased significantly in recent years and have become a worldwide problem. We previously reported that an ascorbic acid derivative having palmitoyl and glucosyl groups, 2-O-α-d-glucopyranosyl-6-O-hexadecanoyl-l-ascorbic acid (6-sPalm-AA-2G), showed inhibitory effects on degranulation in vitro and on the passive cutaneous anaphylaxis (PCA) reaction in mice. In this study, several palmitoyl derivatives of ascorbic acid were synthesized and a structure–activity relationship study was performed to discover more potent ascorbic acid derivatives with degranulation inhibitory activity. 6-Deoxy-2-O-methyl-6-(N-hexadecanoyl)amino-l-ascorbic acid (2-Me-6-N-Palm-AA), in which a methyl group was introduced into the hydroxyl group at the C-2 position of ascorbic acid and in which the hydroxyl group at the C-6 position was substituted with an N-palmitoyl group, exhibited much higher inhibitory activity for degranulation in vitro than did 6-sPalm-AA-2G. 2-Me-6-N-Palm-AA strongly inhibit the PCA reaction in mice at lower doses than those of 6-sPalm-AA-2G. These findings suggest that 2-Me-6-N-Palm-AA may be a promising therapeutic candidate for allergic diseases

Neurite Outgrowth-Promoting Compounds from the Petals of Paeonia lactiflora in PC12 Cells

Isorhamnetin-3-O-glucoside and astragalin, flavonol glucosides, were isolated from the petals of Paeonia lactiflora as neurite outgrowth-promoting compounds. Isoquercitrin, formed by demethylating the B ring of isorhamnetin-3-O-glucoside or by adding a hydroxyl group to the B ring of astragalin, was evaluated for neurite outgrowth-promoting activity and was compared with the activities of isorhamnetin-3-O-glucoside and astragalin. The activities of isorhamnetin, kaempferol, and quercetin, aglycones corresponding to isorhamnetin-3-O-glucoside, astragalin, and isoquercitrin, respectively, were also evaluated. Isorhamnetin-3-O-glucoside and astragalin showed much stronger neurite outgrowth-promoting activities than the activities of the other tested flavonoids. They exhibited relatively weak anti-oxidant activities and moderate AChE inhibitory activities compared to the activities of the other tested flavonoids. Isorhamnetin-3-O-glucoside and astragalin promoted morphological neurite outgrowth and the expression of neurofilaments induced by NGF in PC12 cells. Isorhamnetin-3-O-glucoside and astragalin might be candidate compounds as neural differentiation agents in peripheral nerves and functional food ingredients preventing cognitive decline

Continuous measurements of bronchial exposure induced by radon decay products during inharation

The deposition of radon decay products is not equal in each of the respiratory regions and as the presence of radon has been linked with an increase in lung cancer risk, it is important to calculate the deposition of radon decay products in each of the respiratory regions. Recently, many studies on the deposition of radon in respiratory regions have been simulated using wire screens. The systems and equipment used in those studies are not suitable for field measurements as their dimensions are relatively massive, nor can they measure continuously. We developed a continuous bronchial dosimeter (CBD) which is suitable for field measurements. It was designed with specifications that allow it to be remain compact. The CBD simulates the deposition of radon decay products in the different respiratory regions by the use of a combination of wire screens. Deposition in the simulated regions of the lung can be continuously estimated in various environments. The ratio of activities deposited in a simulated nasal cavity (N) and tracheobronchial (TB) regions was calculated from the results of simultaneous measurements using CBD-R (reference), CBD-N (nasal), and CBD-TB (tracheobronchial) measurement units. After aerosols were injected into the radon chamber, the ratio of N and TB depositions decreased. This results indicate that the CBD gave a good response to changes in the environment. It was found that the ratio of N and TB deposition also varied with time in each actual environment

Reassessment of the radiocesium resuspension flux from contaminated ground surfaces in East Japan

Resuspension of 137Cs from the contaminated ground surface to the atmosphere is essential for understanding the environmental behaviors of 137Cs and estimating external and inhalation exposure of residents. Kajino et al. (2016) assessed the 137Cs resuspension flux from bare soil and forest ecosystems in East Japan in 2013 using a numerical simulation constrained by surface air concentration measurements. However, the simulation was found to underestimate the observed deposition amounts by two orders of magnitude. The reason for this underestimation is that the simulation assumed that resuspended 137Cs is carried by submicron aerosols, which have low deposition rates. Based on the observational indications that soil dust and bioaerosols are the major carriers of resuspended 137Cs, a new simulation is performed with higher deposition rates constrained by both surface concentrations and deposition amounts. In the new estimation, the areal total annual resuspension of 137Cs in 2013 is 25.7 TBq, which is equivalent to 0.96 % of the initial deposition (2.68 PBq). Due to the rapid deposition rates, the annual redeposition amount is also large at 10.6 TBq, approximately 40 % of the resuspended 137Cs. The resuspension rate through the atmosphere (0.96 % y−1) seems slow, but it (2.6 × 10−5 d−1) may not be negligibly small compared to the actual decreasing trend of the ambient gamma dose rate obtained in Fukushima Prefecture after the radioactive decay of 137Cs plus 134Cs in 2013 is subtracted (1.0–7.9 × 10−4 d−1): Resuspension can account for 1–10 % of the decreasing rate due to decontamination and natural decay through land surface processes. The current simulation underestimated the 137Cs deposition in Fukushima city in winter by more than an order of magnitude, indicating the presence of additional resuspension sources. The site of Fukushima city is surrounded by major roads. Heavy traffic on wet and muddy roads after snow removal operations could generate superlarge (approximately 100 µm in diameter) road dust or road salt particles, which is not included in the model but might contribute to the observed 137Cs at the site