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Urinary enzyme activities (N-acetyl-beta-D-glucosaminidase [NAG], alkaline phosphatase [ALP], leucine aminopeptidase [LAP], gamma-glutamyl transpeptidase [gamma-GTP]) were investigated to determine their clinical significance in diabetic nephropathy. There were correlations among ALP, LAP, and gamma-GTP, though no correlation existed between NAG and the other three enzymes. Activities of NAG isozymes (both A and B) were higher than in normal controls. It has been reported that NAG isozyme A might be associated with glomerular diseases, and isozyme B might be associated with proximal tubular damage. The results of our study suggest that NAG reflects lysosomal dysfunction of both glomerular and proximal tubular epithelial cells, which may be caused by poor glycemic control, and that ALP, LAP, and gamma-GTP reflect brush border damage of proximal tubules, which may be caused by diabetic nephropathy.

Thirteen hundred and nineteen children aged 3 years living in Higashi-ku of Fukuoka City were examined for dental caries. To their mothers were given questionnaires concerning feeding methods, between-meal eating habits, using period of feeding bottles, use of feeding bottles at bedtime, kinds of between-meal snacks, drinking of acidophilus beverages, and so on. The percentage of the children with carious teeth was 75.5 and the mean deft was 4.5, and these were both samaller than the percentage of children with caious teeth and the mean deft of the whole nation, respectively. The percent of children with carious teeth was significantly larger in the following groups: breast-fed children, children using feeding bottles for more than 24 months, children using feeding bottles often at bedtime, children eating between meals irregularly, and children drinking acidophilus beverages every day or 2-3 times per week. The groups that took between-meal snacks irregularly had the largest percentage of children with carious teeth (83.5%) and the largest mean deft (5.5) throughout this study. Regarding the use of feeding bottles at bedtime, and between-meal eating habits including drinking of acidophilus beverages, breast-fed children did not have so strong a tendency toward dental caries as mixedand bottle-fed children. This study indicated that some circumstances such as breast feeding, long-term use of feeding bottles, frequent use of feeding bottles at bedtime, and irregular eating between-meal snacks might be harmful to the dental health of 3-year-old children.

福岡市博多保健所において昭和50年度から同54年度までの間に実施された3歳児歯科健診時の各種資料を基に, 同期間における3歳児健診受診状況ならびにう蝕罹患状況の推移, さらには, 保育環境および保健所の実施した母子保健活動とう蝕罹患状況との関連を検討した。健診受診率およびf歯率ほこの期間毎年有意に増加し, う蝕罹患者率および一人平均df歯数は有意に減少した。なお, う蝕罹患型別罹患者率については有意な増減は認められなかった。昭和54年度においては, 被健診児が第1子である方が第2子以下よりう蝕罹患者率が有意に低率であり, また, f歯串は保育園非就園児が就園児より, そして祖父母と同居している方が核家族より有意に高率であった。また, 同保健所管内で保健所が行なう母子保健活動の度合は異なった地区別のう蝕罹患状況の変化を昭和50年と54年について比較すると, う蝕罹患者率および一人平均df歯数はそれぞれ母子保健が推進された地区においてより高い改善傾向がみられた。

Erythrosine, eosine Y, rose bengal, mercurochrome, methylene blue, azure A and azure B accelerated the photodecomposition of pyridoxine and pyridoxamine at pH 5–9, but fluorescein and acid red did not. The photodecomposition of pyridoxine in the presence of erythrosine was greatest at pH 9·0, The singlet oxygen generated by light-excited dyes played a role as a mediator in the decomposition of pyridoxine but the degradation products of erythrosine had no effect. The photodecomposition of pyridoxine and pyridoxamine in the presence of dyes was depressed by aminopyrine, sulpyrine and tryptophan. Pyridoxine 3, 4′-dioctanoate was stable in the presence of erythrosine.

The pharmacokinetics of sulfaguanidine in rats was studied after its intravenous or oral administration. In adult rats, its elimination from plasma, after intravenous administration of 2.5 or 25 mg/kg doses, could be described by a two-compartment open model, while its plasma concentration after oral administration of 25 mg/kg doses, agreed with the one- or two-compartment open model. Neonatal rats displayed a lower elimination of sulfaguanidine than adult rats. Comparison of the drug's gastrointestinal absorption showed that the maximum plasma concentration after oral administration was significantly higher for neonatal than for adult rats. However, there was no significant difference between the times required to reach maximum plasma concentrations. The area under the plasma concentration-time curve at 0-infinity h was significantly higher for neonatal than for adult rats. The absolute bioavailability (57.86%) in neonatal rats was approximately five times that (12.76%) in adult rats. Thus, sulfaguanidine was poorly absorbed by adult rats, but was efficiently absorbed by immature gastrointestines of neonatal rats.

alpha 4-O-Benzoyl-pyridoxine (PN-4'MB) and alpha 5-O-benzoyl-pyridoxine (PN-5'MB) were hydrolyzed in 10% aqueous solution of acetone at pH 1-4. They were hydrolyzed obeying apparent first-order kinetics. In the pH range of 1-7, PN-4'MB was hydrolyzed 10 times faster than PN-5'-MB. At pH 7-12, an interconversion between the two derivatives was observed. They were bactericidal against Escherichia coli and Bacillus subtilis and prevented severe convulsions induced in mouse by 4'-methoxypyridoxine, a potent antagonist of vitamin B6. PN-4'MB was hydrolyzed with the homogenate of rat liver more easily than PN-5'MB. The metabolite of PN-MBs in man was identified as 4'-pyridoxic acid, i.e., a principal metabolite of PN, using high-performance liquid chromatography. The amount of urinary excretion of 4'-pyridoxic acid in 10 hr after oral administration of PN-4'MB or PN-5'MB was as large as that of PN.

Diabetes mellitus is one of the common diseases which often involve thrombi formation in major and microcirculation. Although these thrombi might be caused by a hypercoagulable and hypofibrinolytic state in this disease, precise mechanism is not get clearly understood.In this study, we measured Fibrinopeptide A (FPA) and Fibrinopeptide Bβ15-42 using radioimmunoassay in patients with diabetes mellitus. In the plasma of diabetic patients, FPA and FPBβ15-42 were elevated, although fibrinogen, FDP, α2-PI and ATIII levels remained the same. Fasting blood sugar levels did not correlate to plasma FPA and FPBβ15-42. Fibrinogen levels in patients with diabetic nephropathy (Group I) were statistically higher than those in patients without nephropathy (Group II). Urinary FPA, FPBβ15-42 and FDP levels in group I were higher than those in group II. Urinary FPA had an inverse relationship to 24 hours creatinine clearance. After administration of heparin to patients with high urinary FPA and FDP excretion, we observed a remarkable reduction of urinary FPA and FDP levels but no changes in urinary protein, plasma FPA and serum FDP. These data suggest that (1) blood sugar per se does not cause activation of the coagulation system, (2) intrarenal coagulation is involved in group I, but not in group II, (3) the measurement of urinary FPA can be a potential value in determining intrarenal coagulation in patients with diabetic nephropathy.

4'-Substituted pyridoxine analogues (4'-PN analogues), which were potent antagonists of vitamin B6, induced severe convulsions in mouse which could be prevented by vitamin B6. To elucidate the mechanism of the convulsive action, the effect of 4'-PN analogues on partially purified pyridoxal kinase (PL-kinase) from mouse brain was studied. 4'-Methoxypyridoxine (4'-MPN), 4'-ethoxypyridoxine (4'-EPN), 4'-propoxypyridoxine (4'-PPN) and 4'-isopropoxypyridoxine (4'-isoPPN) were found to powerful inhibitors of PL-kinase and competed with pyridoxal (PL). There was a good relationship between mouse convulsions and inhibitory activities of PL-kinase. We also studied whether 4'-MPN, 4'-EPN, 4'-PPN and 4'-isoPPN were used as substrates of PL-kinase. High-performance liquid chromatography was used to separate 4'-PN 5'-phosphate analogues and ADP which were formed in the enzyme reaction, and to measure them quantitatively. The results showed that 4'-MPN, 4'-EPN, 4'-PPN and 4'-isoPPN were also phosphorylated by PL-kinase like 4'-deoxypyridoxine.

The intestinal absorption of pyridoxal 5'-phosphate (PLP) at physiological levels (10(-7) -10(-6) M) was studied in comparison with that of pyridoxal (PL) in rat, using in vitro everted sac and an intestinal preparation that permitted continuous in situ collection of mesenteric venous blood. After PLP administration (10(-6) -10(-3) M) in situ, larger amounts of PLP were found in the mesenteric venous plasma than after PL administration at the same dose. The amount of PLP found in the mesenteric venous plasma was dependent on its dose at lower concentrations up to 10(-4) M but became independent at higher concentrations. After PL administration at various doses, the amount of PL found in the mesenteric venous blood increased linearly with the dose. When various concentrations of PLP were added to the mucosal side, under the in vitro condition with protection from alkaline phosphate hydrolysis, PLP was detected in the serosal side and the extent of PLP transport was dependent on the initial concentration of PLP in the mucosal side. When various concentrations of PL were added to the mucosal side, the extent of PL transport was independent of the initial concentration of PL in the mucosal side. In rat pretreated with actinomycin D, PLP transport in vitro was inhibited but not that of PL. N2-induced anoxia and pyridoxamine 5'-phosphate and anion transport inhibitor (4,4'-diisothiocyanostilben-2,2'-disulfonic acid disodium salt) showed no effect on PLP transport. These results suggest that PLP can be absorbed in the phosphorylated form and imply the presence of a saturable process for direct absorption of PLP itself and a diffusive process for PL absorption. In addition, the result of the in vivo neonatal experiment suggests that the neonatal intestine also can transport PLP in phosphorylated form.