Structure activity relationship of ar-turmerone analogues

For the analysis of structure activity relationship of ar-turmerone analogues, the compounds containing the various substituents on the phenyl ring and 1(or 2)-naphthyl group in the place of phenyl of ar-turmerone were prepared and tested their cytotoxicity against HL-60, K-562, and L1210 leukemia cellsin vitro. The substituents at para position are methoxy, phenoxy, methyl, trifluoromethyl, fluoro, and chloro. Atmeta position methoxy, methyl, trifluoromethyl, or chloro groups and atortho position methoxy or chloro group were introduced. Against HL-60 and K-562 cells, ED₅₀ values of the analogues are ranged from 0.8 to 30.0 μg/ml. Against L1210 cell, these are located more than 20.0 μg/ml. However, 5-carboethoxy-2-methyl-6-(1-naphthyl)-2-octen-4-one (5n) possesses ED50 valuses 0.8, 2.1, 6.5 μg/ml against HL-60, K-562, L1210 cells, respectively. The electronic nature of the subsituents on phenyl ring of ar-turmerone dose not affect the biological activity. Therefore the flat structure of aromatic portion of ar-turmerone analogues is the more important factor for their activity rather than its electronic nature. The potentiation of the cytotoxicity with the enlargement of aromatic ring region also supports the importance of the plane structure of this area. The restriction of the single bond rotation between C-6 and aromatic ring through the introduction of substituents at theortho position of phenyl ring and the increment of size of alkyl group at C-6 position enhances the activity. Therefore the effective conformation should be the one having the orthogonal arrangement between the aromatic ring and the side chain.     

c-Fos basal immunoreactivity decreases in rat spinal cord during normal ageing

The pattern of distribution in rat spinal cord and changing pattern during normal ageing of c-Fos expression were investigated by immunohistochemical staining in male Sprague-Dawley rats at the age of 1 week, 5 months and 2 years. c-Fos immunoreactivity was observed diffusely in gray matters in neonatal rats, preferentially located in deep dorsal horn and around central canal. Compared with those of neonatal rats, these cells decreased prominently in adult rats. In aged rats, immunoreactive cells were not seen in any segments. c-Fos immunoreactivity in spinal cord may be related to stress response, functional differentiation, and in part, neuronal death with target dependence. In conclusion, we demonstrated for the first time that c-Fos expression patterns change during normal ageing.     

Replantation of avulsed scalps and secondary aesthetic correction

Five patients with avulsed scalps were treated with replantation between 1992 and 1998. All patients were women age 20 to 36 years. The percentage of the avulsed scalp ranged from 50% to 100% of the whole scalp. The vessels chosen for anastomosis were the superficial temporal artery, occipital artery, and superficial temporal vein. A vein graft harvested from the cephalic vein of the forearm was performed on the venous and arterial sides in 1 patient. Two patients experienced complete survival of the replanted scalp. Three patients showed 40%, 50%, and 80% survival areas, with the remaining defects resurfaced as split-thickness skin grafts. Six months later, the scar areas in the last 3 patients were reconstructed with an expansion of the normal or replanted scalp. The follow-up period ranged from 1 to 7 years. In 4 patients a partial return of sensation in the replanted scalp and motor function of the frontalis muscle were observed. All patients were satisfied with the aesthetic results of their surgery.     

Melatonin improves insulin resistance and hepatic steatosis through attenuation of alpha‐2‐HS‐glycoprotein

Melatonin plays an important role in regulating circadian rhythms. It also acts as a potent antioxidant and regulates glucose and lipid metabolism, although the exact action mechanism is not clear. The α2‐HS‐glycoprotein gene (AHSG) and its protein, fetuin‐A (FETUA), are one of the hepatokines and are known to be associated with insulin resistance and type 2 diabetes. The aim of this study was to determine whether melatonin improves hepatic insulin resistance and hepatic steatosis in a FETUA‐dependent manner. In HepG2 cells treated with 300 μmol/L of palmitic acid, phosphorylated AKT expression decreased, and FETUA expression increased, but this effect was inhibited by treatment with 10 μmol/L of melatonin. However, melatonin did not improve insulin resistance in FETUA‐overexpressing cells, indicating that improvement in insulin resistance by melatonin was dependent on downregulation of FETUA. Moreover, melatonin decreased palmitic acid‐induced ER stress markers, CHOP, Bip, ATF‐6, XBP‐1, ATF‐4, and PERK. In addition, in the high‐fat diet (HFD) mice, oral treatment with 100 mg/kg/day melatonin for 10 weeks reduced body weight gain to one‐third of that of the HFD group and hepatic steatosis. Insulin sensitivity and glucose intolerance improved with the upregulation of muscle p‐AKT protein expression. FETUA expression and ER stress markers in the liver and serum of HFD mice were decreased by melatonin treatment. In conclusion, melatonin can improve hepatic insulin resistance and hepatic steatosis through reduction in ER stress and the resultant AHSG expression.     

Assessment of masticatory function in patients with non‐sagittal occlusal discrepancies

Non‐sagittal occlusal discrepancies such as posterior cross‐bite and anterior openbite are common types of malocclusion, but studies on masticatory function related to those malocclusions have been scarce. The aim of this study was to quantify the masticatory performance in patients with non‐sagittal discrepancies compared to those with normal occlusion, using both objective and subjective measures. Maximum bite force and contact area using Dental Prescale^® system as a static objective assessment, Mixing Ability Index (MAI) as a dynamic objective evaluation and food intake ability (FIA) as a subjective assessment were analysed from 21 people in normal occlusion (Group N) and 64 patients with posterior cross‐bite (Group C), anterior openbite (Group O) or both (Group B). The differences of the maximum bite force, the contact area, the MAI and the FIA were compared, and their correlations were figured out. The non‐sagittal malocclusion groups showed lower values in the maximum bite force, the contact area, the MAI and the FIA compared to those in the normal group (P < 0·0001). Compared to Group N, Groups C, O and B showed 61·5%, 42·1% and 40·1% of the maximum bite force, and 84%, 84% and 76% of hard food FIA, respectively. However, there were no significant differences among Groups C, O and B. The MAI showed higher correlation with the FIA (r = 0·38, P < 0·01), than with the maximum bite force and the contact area (both r = 0·24, P < 0·5). These results revealed that masticatory function in patients with non‐sagittal discrepancies is significantly reduced both objectively and subjectively.     

A Case of Acquired Idiopathic Pterygium Inversum Unguis

Pterygium inversum unguis (PIU) is a rare nail abnormality in which the distal nail bed adheres to the ventral surface of the nail plate, with obliteration of the distal groove. Because of the rarity of this condition, its exact origin is unknown. This disorder can be either congenital or acquired, with or without a family history. The acquired forms may be idiopathic or secondary to systemic connective tissue diseases or other causes such as stroke, neurofibromatosis, leprosy, or the use of nail fortifiers. We present an unusual case of acquired idiopathic PIU of the 10 fingernails in a 22-year-old man.