• Journal of Life Science
• /
• v.7 no.2
• /
• pp.127-133
• /
• 1997

The phytase(myo-inositol hexkisphosphate phosphohydrolase ; EC 3.1.3.8) activity was observed only in the homogenate of intestinal mucosa, though the activity of alkaline phisphatase was measurable in various organs. In addition, no protein bands were detected in any other organs on immunoblotting using the anti-90kDa phytase antiserum. Thses results suggest that phytase is specifically present in small intestinal mucosa, and that hydrolysis of phytic acid(inositol-hexakisphosphate) can be allotted for a physiological role of the intestine-specific enzyme. The activities of phytase was increased during development of rat. The 70kDa phytase appeared just after birth, but the 90kDa phytase was not observed until adult period, suggesting that the 90kDa phytase was synthesized in response to weanling.

• Korean Journal of Pharmacognosy
• /
• v.47 no.1
• /
• pp.29-37
• /
• 2016

Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and ${\alpha}$-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and ${\alpha}$-glucosidase with $IC_{50}$ value of $96.29{\pm}0.3$ and $264.71{\pm}14.87{\mu}g/mL$, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-${\beta}$-D-glucopyranoside and oleanolic acid-3-O-${\beta}$-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and ${\alpha}$-glucosidase over a range of concentrations ($12.5-50{\mu}M$). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited ${\alpha}$-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

• 한국유가공학회:학술대회논문집
• /
• 2007.09a
• /
• pp.39-47
• /
• 2007

Bone undergoes continuous remodeling throughout the life and bone health is governed by the balance of bone resorbing osteoclast and bone forming osteoblast. Bone resorption is reflected in tartrate resistant acid phosphatase, pyridinium cross link and collagen telopeptide, whereas bone formation activity can be expressed as bone specific alkaline phosphatase, osteocalcin and procollagen I extension peptide. Milk basic protein and lactoferrin have been reported as active proteins to modulating bone metabolism. In addition to these proteins, some bioactive milk peptides released during lactic fermentation may provide beneficial effect on bone metabolism. The effects of fermented products of Lactobacillus casei ATCC 393 on bone metabolism were investigated using a variety of biochemical markers in osteoblastic MC3T3-E1 cells and ovariectomized rats. Based on the results, the fermented products of Lactobacillus casei ATCC 393 played an functional role in bone metabolism by suppressing bone resorption and by increasing bone formation.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
• /
• v.28 no.3
• /
• pp.216-225
• /
• 2002

Hyaluronic acid (HA) is an almost essential component of extracellular matrices. Early in embryogenesis mesenchymal cells migrate, proliferate and differentiate, in part, because of the influence of HA. Since the features of embryogenesis are revisited during wound repair, including bone fracture repair, this study was initiated to evaluate whether HA has an effect on calcification and bone formation in an in vitro system of osteogenesis. Mouse calvaria Pre-osteoblast (MC3T3-E1) cells were cultured in ${\alpha}-MEM$ medium with microorganism-derivative hyaluronic acid that was produced by Strep. zooepidemicus which of molecular weight was 3 million units. The dosages were categorized in each 0.5, 1.0 and 2.0 mg/ml concentration experimental groups. After 2 and 4 days cultures in expeirmental and control groups, the tendency of cell proliferation, MTT assay, protein synthesis ability, collagen synthesis and alkaline phosphatase activity were analysed and bone nodule formation capacity were measured with Alizarin Red S stain after 29 days cultures. The cell proliferation was increased in time, especially the group of 0.5 and 1.0 mg/ml concentration of HA were showed prominent cell proliferation. After 2 and 4 days culture, experimental groups in general were greater cell activity in MTT assay. The protein synthesis was increased in all experimental groups compared to control group, especially most prominent in 1.0 mg/ml concentration group. The collagen synthesis capacity were increased in HA experimental groups, especially prominent in 1.0 mg/ml group and the activity of alkaline phosphatase were increased, especially also prominent in 1.0 mg/ml group, compared to control group. Above these, the activity of mouse carvarial pre-osteoblast cells was showed greater bone osteogenesis activity in all applied HA experimental group, especially group of 1.0 mg/ml concentration of HA.

• Molecules and Cells
• /
• v.44 no.10
• /
• pp.710-722
• /
• 2021

Hypoxia, or low oxygen tension, is a hallmark of the tumor microenvironment. The hypoxia-inducible factor-1α (HIF-1α) subunit plays a critical role in the adaptive cellular response of hypoxic tumor cells to low oxygen tension by activating gene-expression programs that control cancer cell metabolism, angiogenesis, and therapy resistance. Phosphorylation is involved in the stabilization and regulation of HIF-1α transcriptional activity. HIF-1α is activated by several factors, including the mitogen-activated protein kinase (MAPK) superfamily. MAPK phosphatase 3 (MKP-3) is a cytoplasmic dual-specificity phosphatase specific for extracellular signal-regulated kinase 1/2 (Erk1/2). Recent evidence indicates that hypoxia increases the endogenous levels of both MKP-3 mRNA and protein. However, its role in the response of cells to hypoxia is poorly understood. Herein, we demonstrated that small-interfering RNA (siRNA)-mediated knockdown of MKP-3 enhanced HIF-1α (not HIF-2α) levels. Conversely, MKP-3 overexpression suppressed HIF-1α (not HIF-2α) levels, as well as the expression levels of hypoxia-responsive genes (LDHA, CA9, GLUT-1, and VEGF), in hypoxic colon cancer cells. These findings indicated that MKP-3, induced by HIF-1α in hypoxia, negatively regulates HIF-1α protein levels and hypoxia-responsive genes. However, we also found that long-term hypoxia (>12 h) induced proteasomal degradation of MKP-3 in a lactic acid-dependent manner. Taken together, MKP-3 expression is modulated by the hypoxic conditions prevailing in colon cancer, and plays a role in cellular adaptation to tumor hypoxia and tumor progression. Thus, MKP-3 may serve as a potential therapeutic target for colon cancer treatment.

• KOREAN JOURNAL OF CROP SCIENCE
• /
• v.30 no.4
• /
• pp.405-411
• /
• 1985

The buffer soluble proteins were extracted from six cultivars of barley grains and analyzed by various electrophoresis; 7.5% polyacrylamide slab gel, 2-30% polyacrylamide porosity gradient tube gel, isoelectric focusing (pH4-9) and starch gel electrophoresis. The proteins, esterase, acid phosphatase, malate dehydrogenase, glutamate dehydrogenase and leucine aminopeptidase were investigated to find out the best method to differentiate barley cultivars. The result were that protein and esterase bands in 2-30% polyacrylamide porosity gradient tube gel electrophoresis and protein bands in 7.5% polyacrylamide slab gel electrophoresis showed typical varietal differences. Therefore, those methods were suitable for differentiation of barley cultivars. It was difficult to differentiate the cultivars by the other methodes and patterns of the other enzymes.

• The korean journal of orthodontics
• /
• v.24 no.1 s.44
• /
• pp.17-35
• /
• 1994

Vanadium is an essential trace element but has not been identified with a specific biogical role. To study the direct effects of vanadium on osteoblast, we incubated murin osteoblast-like (MC3T3-El) cells with various corcentration of vanadium oxide & sodium orthovanadate. This study was designed to investigate the effect of vanadium on DNA synthesis, alkaline phosphatase (ALP) activity, cAMP formation responsive to parathormone(PTH) and type I $\alpha$ 2 collagen ribonucleic acid (mRNA) level in murin osteoblast-like (MC3T3-El) cells. The cells were cultured in $\alpha-minimal$ essential medium$(\alpha-MEM)$ supplemented with $10\%$ fetal bovine serum (FBS) and then changed to $0.1\%$ FBS with various concenoation of vanadium oxide & sodium orthovanadate. Quiescent cultured MC3T3-El cells incubated for 24 hours with 2,5,10,15,20 ${\mu}M$ vanadium oxide incorporated $[^3H]Thymidine;$ every concentration showed increases in $[^3H]Thymidine$ incorporations dose dependant manner, the greatest response occurred at $20{\mu}M$. Quiescent cultured MC3T3-E1 cells incubated for 3days with 2,5,10,15,20 ${\mu}M$ vanadium oxide, for 2days with sodium orthovanadate and alkaline phosphatase was assayed with disodium phenyl phosphate as substrate. Vanadium oxide increased the alkaline phosphatase content in MC3T3-El cells at $2{\mu}M\;&\;6{\mu}M$ ; the greatest response occurred at $2{\mu}M$. But decreased at other content sodium orthovanadate increased alkaline phosphatase content in MC3T3-El cells at all concenoation ; the greatest response occurred at $4{\mu}M$. Quiescent cultured MC3T3-El cells incubated for 3days with $5,10{\mu}M$ vanadium oxide , with $5,8{\mu}M$ sodium orthovanadate and cAMP formation was measured by Radioimmunoassay(RIA). Vanadium oxide & sodium orthovanadate showed the tendency of inhibitory effects on cAMP responsiveness to PTH in MC3T3-El cells. Quiescent cultured MC3T3-El cells incubated for 24hours with $10,20{\mu}M$ vanadium oxide, with $5,10{\mu}M$ sodium orthovanadate and Type I $\alpha$ 2 collagen ribonucleic acid (mRNA) expression was studied by Nothern blot analysis. Northern blot analysis of vanadium oxide treated cells showed decreasing effects 0& sodium orthovanadate revealed increasing effects in type I $\alpha$ 2 collagen ribonucleic acid (mRNA) level.

• The Korean Journal of Physiology
• /
• v.7 no.1
• /
• pp.1-11
• /
• 1973

To study the effects of Korean ginseng on mice visceral alkaline phosphatase activity and inorganic phosphate phosphorus level in the blood, the experimental groups of male and female mice were injected subcutaneously with 0.01 ml or 0.02 ml of Tyrode solution per 10 g of body weight daily, and 0. 1 mg or 0.2 mg of alcohol extract of ginseng which was diluted with Tyrode solution. After groups of mice were treated for 7 days or 14 days, the alkaline phosphatase activity in the jejunum, kidney and liver homogenate and serum were determined with sodium ${\beta}-glycerophophosphate$ as substrate, and quantified the content of inorganic phosphate phosphorus in the blood of above mice. 1. Alkaline phosphatase activity in the jejunum, kidney, liver and serum of male mice for the 7 day treatment with ginseng extract (0.1 mg/10 g) was increased by 15.28%, 12.86%, lg.05% and 11.70% respectively, compared with Tyrode solution group. 2. Alkaline phosphatase activity in the jejunum, kidney, liver and serum of female mice for the 7 day treatment with ginseng extract (0.2 mg/10 g) was increased 3.46%, 6.94%, 20.37% and 4.05 % respectively. 3. Alkaline phosphatase activity in the jejunum, kidney, liver and serum of male mice for the 14 day treatment with ginseng extract(0.1 mg/10 g) was increased·15.92%, 19.76f, 10.16% and -1.63 % respectively. 4. Alkaline phosphatase activity in the jejunum, kidney, liver and serum of female mice for the 14 day treatment with ginseng extract(0.2 mg/10 g) was increased 18.89%, 24.55%, 16.97% and 27.59% respectively. 5. Increasing activity of the enzyme in the liver of both male and female mice for the 7 day treatment was declined to some extent at the 14 day treatment, on the other hand, increasing activity of the enzyme in the jejunum, kidney and serum of mice for the 7 day treatment was more promoted at the 14 day treatment. 6. The 7 day and 14 day treatment with ginseng extract increased 20.20% and 20.96% of inorganic phosphate phosphorus in male blood, 22.38% and 17.57f in female blood respectively. In accordance with the results mutual relationships of ginseng, internal secretion, nucleic acid and alkaline phosphatase activity were disscussed.

• The korean journal of orthodontics
• /
• v.25 no.6 s.53
• /
• pp.697-704
• /
• 1995

Chicken calvarial bone is known to contain various cell types, but their exact composition is unknown. By characterizing the chicken calvarial bone biochemically, it can be used to study biochemical, histochemical actions of bone cells in general. Calvaria of 18-day-old white leg horn embryo was aseptically dissected and bone cell populations were isolated by sequential enzymatic digestion. Histochemical study for osteoclast-like bone cell. population was performed with tartrate resistant acid phosphatase(TRAP) stain and for osteoblast-like bone cell population, alkaline phosphatase(ALP) stain was performed. Biochemical study for osteoblast-like bone cell population was performed using alkaline phosphatase(ALP) assay. Following conclusions were obtained from this study. 1. TRAP positive multi and mononuclear cells were mostly observed in group I and II, indicating that osteoclast-like bone cell population is mostly found in these groups. 2. All the cultured groups showed almost equal ALP activities and were positive for ALP stain, indicating that osteoblast-like bone cell population is evenly dispersed in all culture groups. 3. Experimental group treated with $1,25(OH)_{2}D_3$ showed increase in ALP activity in contrast to the control group, confirming previous studies that $1,25(OH)_{2}D_3$ increases ALP activities in in vitro bone cultures. 4. Results from von Kossa's stain indicated that in vitro bone formation had occured after 3 weeks of culture with beta-glycero phosphate.

• Journal of Radiopharmaceuticals and Molecular Probes
• /
• v.7 no.1
• /
• pp.33-40
• /
• 2021

Recently, antibody-drug conjugates (ADCs) are used to deliver efficient cytotoxic payloads selectively in cancer cells. In the designing of an ADC, the antibody is connected to a toxic payload via a covalent linker, which helps to solubilizes the typical hydrophobic payload as well as stabilizes the linkage over circulation. The development of the linkers for the antibody drug conjugate is still in demand. Initially, the acid, disulfide, and cathepsin-sensitive ADCs attracted considerable attention for the delivery of a potent cytotoxic payload but suffer from instability in human and mouse plasma with a short half-life. In addition, It also suffer from a solubility issue that induces aggregation, which is the major problem in their development. ADCs associated with sulfatase and phosphatase cleavable linker are highly soluble due to the anionic nature of sulfate and phosphate groups. The ADCs also showed high stability in human and mouse plasma. Therefore, to overcome these limitations, sulfatase and phosphatase cleavable linkers were developed. This review focuses on the recently reported advantages of sulfatase and phosphatase cleavable linkers for ADCs.