Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl(1→6)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-15β-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at 100 µM. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and π-π stacking interactions which could explain the compound potency to inhibit AChE and BChE.
Acetylcholinesterase ; Alzheimer Disease ; Butyrylcholinesterase ; Cholinesterases ; Hydrogen ; In Vitro Techniques ; Neurodegenerative Diseases

Cholinesterase (ChE) is one of the most ubiquitous enzymes and in addition to its well characterized catalytic function, the morphogenetic involvement of ChE has also been demonstrated in neuronal tissues and in non-neuronal tissues such as bone and cartilage. We have previously reported that during mouse tooth development, acetylcholinesterase (AChE) activity is dynamically localized in the dental epithelium and its derivatives whereas butyrylcholinesterase (BuChE) activity is localized in the dental follicles. To test the functional conservation of ChE in tooth morphogenesis among different species, we performed cholinesterase histochemistry following the use of specific inhibitors of developing molar and incisors in the hamster from embryonic day 11 (E11) to postnatal day 1 (P1). In the developing molar in hamster, the localization of ChE activity was found to be very similar to that of the mouse. At the bud stage, no ChE activity was found in the tooth buds, but was first detectable in the dental epithelium and dental follicles at the cap and bell stages. AChE activity was found to be principally localized in the dental epithelium whereas BuChE activity was observed in the dental follicle. In contrast to the ChE activity in the molars, BuChE activity was specifically observed in the secretory ameloblasts of the incisors, whilst no AChE activity was found in the dental epithelium of incisors. The subtype and localization of ChE activity in the dental epithelium of the incisor thus differed from those of the molar in hamster. In addition, these patterns also differed from the ChE activity in the mouse incisor. These results strongly suggest that ChE may play roles in the differentiation of the dental epithelium and dental follicle in hamster, and that morphogenetic subtypes of ChE may be variable among species and tooth types.
Acetylcholinesterase ; Ameloblasts ; Animals ; Butyrylcholinesterase ; Cartilage ; Cholinesterases ; Cricetinae ; Dental Sac ; Epithelium ; Incisor ; Mice ; Molar ; Morphogenesis ; Neurons ; Tooth ; Tooth Germ

22 patients with proved urogenital malignancies was done to determine the value of bone scanning versus roentgenographic skeletal survey in assessing the degree of metastatic involvement with serum phosphatase level. Findings on bone scans were positive in 11 patients and in 6 patients of these patients results of radiologic of radiologic skeletal survey were negative. Of these 11 patients with positive scanning, 3 patients showed elevation of serum acid phosphatase and 4 other patients showed elevation of serum alkaline phosphatase. And of the others with negative scanning, 1 patient showed elevation of acid phosphatase and elevation of alkaline phosphatase in 3 other patients.
Acid Phosphatase ; Alkaline Phosphatase ; Diagnosis ; Humans ; Neoplasm Metastasis*

22 patients with proved urogenital malignancies was done to determine the value of bone scanning versus roentgenographic skeletal survey in assessing the degree of metastatic involvement with serum phosphatase level. Findings on bone scans were positive in 11 patients and in 6 patients of these patients results of radiologic of radiologic skeletal survey were negative. Of these 11 patients with positive scanning, 3 patients showed elevation of serum acid phosphatase and 4 other patients showed elevation of serum alkaline phosphatase. And of the others with negative scanning, 1 patient showed elevation of acid phosphatase and elevation of alkaline phosphatase in 3 other patients.
Acid Phosphatase ; Alkaline Phosphatase ; Diagnosis ; Humans ; Neoplasm Metastasis*

The effect of orthodontic force on the collagenase and phosphatase activities of the adjacent alveolar bone was evaluated. Maxillary canines of male cats were treated orthodontically with closed coil spring so as to exert about 80g force. Sixteen cats were equally divided into one control group and seven experimental groups (12 hrs, 24 hrs, 36 hrs, 2 days, 3 days, 5 days and 7 days after orthodontic treatment). After sacrificing all animals on experimental intervals, collagenase, acid phosphatase (ACP) and alkaline phosphatase (ALP) activities were determined in the pressure and tension sides of alveolar bones. ACP activities increased in both the pressure and tension sides, but significantly increased in the pressure side continuously. ALP activities increased in the tension side at early stage (1-2 days after treatment), but changed small amount in the pressure side. Collagenase activities increased in the pressure side, especially at late stage (5-7 days after treatment). These results suggest that (1) orthodontic force increases the ACP, ALP and collagenase activities generally and (2) activities of ACP and collagenase increase in the pressure side, but that of ALP in the tension side and (3) activities of ACP and ALP increase at early stage, but that of collagenase at late stage after orthodontic treatment. Therefore it is shown that there are time differences in the formation and destruction of organic and inorganic components in the bone metabolism of alveolus with application of the orthodontic forces.
Acid Phosphatase ; Alkaline Phosphatase ; Animals ; Cats ; Collagenases ; Humans ; Male ; Metabolism

A new sesquiterpenoid, 11-hydroxy-valenc-1(10),3(4)-dien-2-one (3), two chemically synthesized but first isolate from nature, 3-oxocedran-8β-ol (1) and valenc-1(10),3(4),11(12)-trien-2-one (2) along with four known compounds, sugiol (4), (+)-nootkatone (5), 11-hydroxy-valenc-1(10)-en-2-one (6), and clovandiol (7), were isolated from the heartwood of Juniperus chinensis. All chemical structures were elucidated using extensive spectroscopic analysis including 1D and 2D NMR spectroscopy. Valenc-1(10),3(4),11(12)-trien-2-one (2) exhibited significant inhibitory activity against butyrylcholinesterase with an IC₅₀ value of 68.45 µM.
Acetylcholinesterase ; Butyrylcholinesterase ; Juniperus ; Magnetic Resonance Spectroscopy

By using the hyperchem program, authors calculated quantitatively the change about the charge and stereo structure of molecules along various stages of the reaction of non-specific esterase (ANAE); Simultaneously, the changes of torsion, angle, energy, bond length were showed. That is evident to prove correlatively the kinetic mechanism of the electrophin substitute reaction. From the above calculations, the factors that affect to the optimum process for a highest effect of ANAE cytochemistry can be deduced
Lymphocytes ; Esterases

The nuclear bone scan is a highly sensitive means of detecting skeletal metastases in patients with prostatic cancer. The results of bone scan with technetium 99m-labeled methylene diphosphonate in 61 patients with biopsy-proven primary prostatic cancer demonstrated bone metastases in 60.7% of cases. The addition of bone scanning to radiographic survey increased the detection rate of bone metastasis by 45.2% and only 1 patient had abnormal roentgenograms but normal scans, a yield of 5.3% false-negative scans. Of those with proved bone metastases by bone scan with radiography, 44.4% had no bone pain, 55.6% had normal acid phosphatase level and 3l.2% had normal alkaline phosphatase levels. Of those without bone metastases by bone scan with radiography, 4.3% had bone pain, 9.1% had elevated acid phosphatase levels and 9.1% had elevated alkaline phosphatase levels.
Acid Phosphatase ; Alkaline Phosphatase ; Humans ; Neoplasm Metastasis* ; Prostatic Neoplasms* ; Radiography ; Technetium

The histochemical study, especially the demonstration of alkaline phosphatase and acid phosphatase was carried out in order to differentiate ascarides of human and pigs. The experimental material were obtained from naturally contaminated men and pigs. As the histochemical staining methods the Gomori's was applied for acid phosphatase and Takeuchi and Takami's for alkaline phosphatase. The results obtained were summerized as follows : In the pig's ascarides, alkaline phosphatase was richly found in the subcuticular tissue, lateral line, median line, strial zone and epithelial cells of the intestine, epithelial cell and basal membrane of the ovary, the same part of the uterus and also in eggs. Acid phosphatase in the pig's ascarides were distributed in the same part as alkaline phosphatase. It, however, was darker brown in the soft tissue of the lateral line, epithelium of excretory canal, median bundle, whole zone of the intestine and intestinal contents. In the human ascarides, the alkaline phosphatase was distributed in the testes and the parts where the acid phosphatase was found in the pig ascarides. The acid phosphatase in the human ascarides was demonstrated in the subcuticular tissue, soft tissue of lateral line, epithelium of excretory cells, strial zone, transparent zone, granular zone and epithelial zone of esophagus and intestine, ovary, ova in the uterus, epithelial cell and basal membrane of the uterus and in testes. In the pig's ascarides, the area of distribution of alkaline phosphatase was restricted, but that of acid phosphatase was wider. In human ascarides, the area of distribution of alkaline phosphatase and acid phosphatase was not significantly different, but in some part showed slight difference. Above mentioned finding suggest that the distribution of phosphatase could be utilized for the differentiation of ascarides of human and pig.
parasitology-helminth-nematode-Ascaris lumbricoides ; Ascaris suum ; histochemistry ; differentiation ; alkaline phosphatase ; acid phosphatase ; animal ; human ; pig

Effects of several cytokines(IL -1beta, TNFalpha, and IFNgamma) have been examined on fetal rat osteoblast-like cells. To investigate whether cytokines play direct causal roles in production of lysosomal enzyme, fetal rat osteoblast-like cells were treated with IL-1beta, TNFalpha, and IFNgamma, respectively or combined. And acid phosphatase was determined by biochemical method. Alkaline phosphatase was assayed to determine the effects of IL-1beta, TNFalpha, and IFNgamma on the expression of this enzyme. And also experiment of calcified nodule formation was performed to assess the effects of cytokines on the bone-forming activity of osteoblast-like cells in vitro. Acid phosphatase activity was significantly increased by the addition of IL-1beta and TNFalpha, whereas decreased by IFNgamma, However, no significant changes in alkaline phosphatase activity was observed when the osteoblast-like cells were treated with IL-1beta and TNFalpha. Interestingly, IFNalpha showed stimulatory effect on alkaline phosphatase activity. The number of calcified nodules was decreased by treatment of cultures with 1ng/ml IL -lbeta, 20ng/ml TNFalpha, and 500 u/ml IFNgamma continuously for 21 days, while considerable number of calcified nodules were formed in control group of osteoblast-like cell in culture for 21 days. These results seem to suggest that cytokines may play crucial roles in bone remodeling through the direct action on the osteoblast-like cell.
Acid Phosphatase ; Alkaline Phosphatase ; Animals ; Bone Remodeling ; Cytokines* ; Interleukin-1beta ; Rats* ; Tumor Necrosis Factor-alpha