Michinori Kubo

Absolute stereostructures of novel norcadinane- and trinoreudesmane-type sesquiterpenes with nitric oxide production inhibitory activity from Alpinia oxyphylla

Novel 14-norcadinane-type sesquiterpenes, oxyphyllenodiols A and B, and 11,12,13-trinoreudesmane-type sesquiterpenes, oxyphyllenones A and B, were isolated from the methanolic extract of kernels of Alpinia oxyphylla. The absolute stereostructures of these norsesquiterpenes were determined on the basis of physicochemical and chemical evidence. In addition, oxyphyllenodiol A and oxyphyllenone A were found to inhibit the NO production in lipopolysaccharide-activated macrophages.

Antipruritic and antinociceptive effects of Chenopodium album L. in mice

The ethanolic extract from the fruits of Chenopodium album L. (FCAL), orally administered at doses of 100-400 mg/kg, dose-dependently inhibited scratching behavior induced by 5-HT (10 micro g per mouse, s.c.) or compound 48/80 (50 micro g per mouse, s.c.) in mice. But it failed to affect hind paw swelling induced by 5-HT or compound 48/80 in mice at doses of 100 and 200 mg/kg and only showed a relatively weak inhibition on the swelling at a higher dose of 400 mg/kg. In addition, FCAL (200 and 400 mg/kg) significantly attenuated the writhing responses induced by an intraperitoneal injection of acetic acid and the inflammatory pain response induced by an intraplantar injection of formalin in mice. At a dose of 400 mg/kg, it also inhibited the neurogenic pain response of formalin test. In conclusion, FCAL possesses antipruritic and antinociceptive activities and the antinociceptive effects are not secondary to anti-inflammatory effects. The findings support evidence for the clinical use of FCAL to treat cutaneous pruritus.

Serum concentrations of carboxyterminal propeptide of type 1 procollagen and tissue inhibitor of metalloproteinase 1 in patients with dermatomyositis

Abstract Serum levels of carboxyterminal propeptide of type I procollagen (PICP) and aminoterminal propeptide of type I procollagen (PINP) have been used as indices of collagen synthesis in patients with various fibrotic diseases during the active stages. One of the suggested contributory factors to the development of tissue fibrosis is a decrease in collagenase activity, which may be related to levels of serum tissue inhibitors of metalloproteinases-1 (TIMP-1). In this study, the serum levels of PICP and PINP in 20 patients with dermatomyositis and 29 control subjects and of TIMP-1 in 29 patients with dermatomyositis and 29 control subjects were measured using an enzyme-linked immunosorbent assay (ELISA) or a radioimmunoassay (RIA). We found that the mean PICP level in patients with dermatomyositis was significantly higher than that in normal controls (mean ± SD 326 ± 76 ng/ml vs 135 ± 88 ng/ml; P < 0.001). In 60% of dermatomyositis patients, the serum PICP level was elevated (more than 311 ng/ml, i.e. 2 × SD above the mean control value). Elevated serum PICP levels were correlated with the incidence of elevated serum creatine kinase levels in patients with dermatomyositis. The serum concentration of PINP was not elevated in comparison with that of the normal control subjects (mean ± SD 36 ± 30 ng/ml vs 63 ± 34 ng/ ml). The mean TIMP-1 level in the patients with dermatomyositis was also significantly higher than in the normal control subjects (mean ± SD 438 ± 328 ng/ml vs 163 ± 63 ng/ml; P < 0.001). In 59% of dermatomyositis patients, the mean serum TIMP-1 level was elevated (more than 289 ng/ml, i.e. 2 × SD above the mean control value). Serum PICP and TIMP-1 levels might be useful for detecting disease activity or severity in dermatomyositis.

Histochemistry : IX. Distribution of saikosaponins in bupleurum falcatum root

Abstract The root of Bupleurum falcatum cultivated in Japan was examined by histological and chemical means in order to clarify the distribution of saikosaponins in the various kinds of tissues and parts of the root. By means of qualitative thin-layer chromatographic—densitometric and quantitative high-performance liquid chromatographic analyses, saikosaponins, bioactive principles in the root, were found to be abundant in the outer phloem layer, especially the pericycle and its neighbouring parenchyma cells in the root. It was also found that the highest level of saikosaponins was detected in thinner root hairs and that the level decreased towards the thicker root head.

Tandem Beckmann and Huisgen–White rearrangement of the9-azabicyclo[3.3.1]nonan-3-one system. Part 2.1 The secondmode of the rearrangement leading to 6-(prop-1-enyl)piperidin-2-ylaceticacid, a versatile intermediate for the syntheses of piperidine alkaloids(+)-pinidine and (+)-monomorine I

The second mode of the Huisgen–White rearrangement of the bicyclic lactam, (-)-2-ethyl-4-oxo-3,10-diazabicyclo[4.3.1]decane (-)-13, leading to cis-[6-(prop-1-enyl)piperidin-2-yl]acetic acid (-)-9a under alkaline conditions is described. A reasonable reaction mechanism accounting for the preferable formation of the (E)-propenyl isomer (E)-9a is presented. Conversions of the olefinic acid 9a into two piperidine alkaloids (+)-pinidine (+)-10 and (-)-dihydropinidine (-)-21, and (-)-cis-2-formyl-6-methylpiperidine (-)-22, a key synthetic intermediate for an ants’ trail pheromone (+)-monomorine I (+)-11, are also described.

Renal Changes of Streptozotocin-Induced Diabetic Rats Fed a Low-Zinc Diet

The changes in kidneys of streptozotocin (STZ)-induced diabetic rats fed a low-zinc (LZ) diet were observed. Calcium deposits were detected in the LZ-diabetic groups from the 2nd to the 8th week. The deposits were mainly detected in the corticomedullary junction, and found in the tubular lumina and epithelial cytoplasm and interstitium. Tubular morphological changes, including luminary distension, epithelial flattening, and paleness of cytoplasm and nuclei, were observed near the calcium deposits in the LZ-diabetic group over the 2nd week. Moreover, at the 8th week, wedge-shaped vasogenic lesions were found on the surface of the renal cortex in the LZ-diabetic group. No changes were detected in the control for the LZ or in the diabetic group fed a standard (SC) diet. When STZ was administered, plasma glucose level in groups fed LZ or SC diet increased in the 1st week, and over the 2nd week, glucose level was maintained at more than 400 mg/dL. Glucose level of the LZ-diabetic group did not differ from that of the SC-diabetic group. However, urinary N-acetyl-beta-D-glucosaminidase activity of the LZ-diabetic group at the 8th week was significantly higher than that of the SC-diabetic group. These findings suggested that low-zinc diet hastens renal damages in diabetic rats.

Trace elements (Cu, Fe, Zn) in several tissues of CCl4-induced chronic hepatitis rats

Liver injury induced by CCl/sub 4/ inhalation is used as 2 model of chronic hepatitis. The authors used rats, induced CCl/sub 4/ inhalation and measured their hydroxyproline contents as the index of chronic liver fibrosis. They examined the relationship between changes in homeostasis and levels of trace elements in various tissues.