• Journal of Pharmacopuncture
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• v.20 no.1
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• pp.45-51
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• 2017

Objectives: This study aimed to evaluate the hypoglycemic effects of an ethanol extract of Cassia abbreviata (ECA) bark and the possible mechanisms of its action in diabetic albino rats. Methods: ECA was prepared by soaking the powdered plant material in 70% ethanol. It was filtered and made solvent-free by evaporation on a rotary evaporator. Type 2 diabetes was induced in albino rats by injecting 35 mg/kg body weight (bw) of streptozotocin after having fed the rats a high-fat diet for 2 weeks. Diabetic rats were divided into ECA-150, ECA-300 and Metformin (MET)-180 groups, where the numbers are the doses in mg.kg.bw administered to the groups. Normal (NC) and diabetic (DC) controls were given distilled water. The animals had their fasting blood glucose levels and body weights determined every 7 days for 21 days. Oral glucose tolerance tests (OGTTs) were carried out in all animals at the beginning and the end of the experiment. Liver and kidney samples were harvested for glucose 6 phosphatase (G6Pase) and hexokinase activity analyses. Small intestines and diaphragms from normal rats were used for ${\alpha}-glucosidase$ and glucose uptake studies against the extract. Results: Two doses, 150 and 300 mg/kg bw, significantly reduced the fasting blood glucose levels in diabetic rats and helped them maintain normal body weights. The glucose level in DC rats significantly increased while their body weights decreased. The 150 mg/kg bw dose significantly increased hexokinase and decreased G6Pase activities in the liver and the kidneys. ECA inhibited ${\alpha}-glucosidase$ activity and promoted glucose uptake in the rats' hemi-diaphragms. Conclusion: This study revealed that ECA normalized blood glucose levels and body weights in type 2 diabetic rats. The normalization of the glucose levels may possibly be due to inhibition of ${\alpha}-glucosidase$, decreased G6Pase activity, increased hexokinase activity and improved glucose uptake by muscle tissues.

• Molecules and Cells
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• v.26 no.4
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• pp.380-386
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• 2008

During embryonic and cancer development, the Hedgehog family of proteins, including Sonic Hedgehog, play an important role by relieving the inhibition of Smo by Ptc, thus activating the Smo signaling cascade. Recently, a purine compound, purmorphamine, has been reported to target the Hedgehog signaling pathway by interacting with Smo. Interestingly, both Sonic Hedgehog and purmorphamine were found to promote the osteogenic differentiation of mouse chondroprogenitor cells. However, there is insufficient information as to how the activation of this seemingly unrelated signaling pathway, either by Sonic Hedgehog or purmorphamine, contributes to osteogenesis. Using alkaline phosphatase assays, we screened 125 purmorphamine derivatives from the Korea Chemical Bank for effects on the differentiation of preosteoblast C2C12 cells. Here, we report that two purine derivatives modulate ALP activity as well as the expression of genes whose expression is known or suggested to be involved in osteogenesis.

• The Journal of Korean Obstetrics and Gynecology
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• v.27 no.1
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• pp.17-27
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• 2014

Objectives: This study was conducted to evaluate the inhibitory effect of polygoni cuspidati radix (PCR) extract on osteoclast differentiation. Methods: MTT-assay was performed to estimate cytotoxicity of PCR extract in BMMs stimulated with RANKL. Tartrate resistant acid phosphatase (TRAP) staining, TRAP activity and RT-PCR were performed to know the inhibitory effect on osteoclast differentiation. actin ring formation were analysed to observe the effect of PCR extract. Results: PCR decreased the number of TRAP positive cells and TRAP activities in BMMs stimulated with RANKL and M-CSF. PCR restrained the formation of actin ring. PCR down regulated the induction of NFATc1, c-Fos, TRAP and OSCAR by RANKL. PCR inhibited NF-${\kappa}B$ activity by inducing degradation of $I{\kappa}B{\alpha}$. Conclusions: We suggest that PCR Extracts can be an effective therapeutic agent on osteoclast differentiation caused by diseases such as osteoporosis.

• Biomedical Science Letters
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• v.27 no.4
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• pp.223-230
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• 2021

Tumor necrosis factor alpha (TNF-α) is a principal regulator of inflammation and immunity. The proinflammatory properties of TNF-α can be attributed to its ability to activate the enzyme cytosolic phospholipase A₂ (cPLA₂), which generates potent inflammatory lipid mediators, eicosanoids. L-glutamine (Gln) plays physiologically important roles in various metabolic processes. We have reported that Gln has a potent anti-inflammatory activity via rapid upregulation of mitogen-activated protein kinases (MAPKs) phosphatase (MKP)-1, which preferentially dephosphorylates the key proinflammatory enzymes, p38 MAPK and cytosolic phospholipase A₂ (cPLA₂). In this study, we have investigated whether Gln could inhibit TNF-α-induced cPLA₂ activation. Gln inhibited TNF-α-induced increases in cPLA₂ phosphorylation in the lungs and blood levels of the cPLA₂ metabolites, leukotrine B4 (LTB4) (lipoxygenase metabolite) and prostaglandin E2 (PGE2) (cyclooxygenase metabolite). TNF-α increased p38 and cPLA₂ phosphorylation and blood levels of LTB4 and PGE2, which were blocked by the p38 inhibitor SB202190. Gln inhibited TNF-α-induced p38 and cPLA₂ phosphorylation and production of the cPLA₂ metabolites. Such inhibitory activity of Gln was no longer observed in MKP-1 small interfering RNA-pretreated animals. Our data indicate that Gln inhibited TNF-α-induced cPLA₂ phosphorylation through MKP-1 induction/p38 inhibition, and suggest that the utility of Gln in inflammatory diseases in which TNF-α plays a major role in their pathogenesis.

• Korean Journal of Organic Agriculture
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• v.30 no.3
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• pp.409-422
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• 2022

Southern blight caused by Sclerotium rolfsii is a serious soilborne disease in economically important crops including pepper. In this study, we conducted a selection of antagonistic bacterial strains and organic materials to biologically control the disease. Out of 39 strains isolated from soils at Jinju in Korea, strain JJ2-01 showed the highest mycelial growth inhibition; garlic oil among various organic materials significantly reduced disease incidence and severity. When a combination of strain JJ2-01 and garlic oil, or each was drenched into the pepper plants, combined treatment and garlic oil significantly suppressed the disease development, however, acid phosphatase activity in garlic oil-treated plants decreased. In the case of combined treatment, the soil activities did not affect by treatment, while soil urease activity was significantly increased by the combined treatment. Therefore, given soil quality and health for sustainable agriculture, the combination of strain JJ2-01 and garlic acid was an effective application for environmental-friendly control of Southern blight in pepper plants.

• Journal of Periodontal and Implant Science
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• v.33 no.4
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• pp.585-597
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• 2003

Porphyromonas gingivalis has been implicated as an important periodontophathic bacterium in the etiology and progression of periodontal diseases. It has been reported that P.gingivalis may mediate periodontal destruction not only directly through its virulence factors, but also indirectly by including complex host mediated inflammatory reponses. The purpose of this study was t o evaluate the effects of P.gingivalis on the bone formation and resorption by osteoblasts. For this purpose, after determining the concentration below which sonicated P.gingivalis extracts (SPEs) have no cytotoxicity on mouse calvarial primary osteoblastic (POB) cells, we investigated the effects of SPEs on the alkaline phosphatase (ALP) activity, matrix metalloproteinase (MMP) expression (MMP-2, -9, 13), and prostaglandin $E_2$ ($PGE_2$) release in POB cells by treatment with SPEs below that concentration. The results were as follows; 1. SPEs showed no cytotoxic effect on POB cells up to a concentration of 1 ${\mu}m$/ml. 2. The treatment with SPEs reduced ALP activity in a dose-dependent manner in POB cells, In addition, when we investigated the effect of SPEs (1 ${\mu}m$/ml) on ALP activity for different exposure periods, statistically significant inhibition of ALP activity was shown at 2 days of exposure, and further significant inhibition occurred by extending the periods of exposure. 3. The treatment with SPEs stimulated the gene expression of MMP-9 in POB cells. 4. The pre-treatment with SPEs increased the amount of $PGE_2$ released in POB cells. In summary, the present study shows that P.gingivalis could inhibit osteogenesis and stimulate bone resorption not only by reducing ALP activity but also by increasing MMP-9 mRNA expression in osteoblasts, possibly through an endogenous $PGE_2$ pathway. In addition, our results suggest that if P.gingivalis affects osteoblasts in early differentiation stage, such effects by P. gingivalis could be irreversible.

• Applied Biological Chemistry
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• v.51 no.3
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• pp.171-176
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• 2008

The comparative molecular similarity indices analysis (CoMSIA) models between 3${\beta}$-Hydroxy-12-oleanen-28-oic acid (1-30) analogues as substrate molecule and their inhibitory activities ($pI_{50}$) against protein tyrosine phosphatase (PTP)-1B were derived and discussed quantitatively. Listing in order, the CoMFA>CoMSIA${\geq}$HQSAR>2D-QSAR model, these QSAR models had the better statistical values. The optimized CoMSIA F1 model at grid 3.0${\AA}$ had the best predictability and fitness ($q^2$=0.754 and $r^2$=0.976) by field fit alignment. The order of contribution ratio (%) of CoMSIA fields concerning the inhibitory activities was a H-bond acceptor (48.9%), steric field (25.8%) and hydrophobic field (25.4%), respectively. Therefore, the inhibitory activities of substrate molecules against PTP-1B were dependent upon H-bond acceptor field (A) of $R_4$-group. From the analytical results of CoMSIA contour maps, oleanolic acid derivatives will have better inhibition activities if $R_1$ group has H-bond acceptor disfavor, $R_3$group has steric disfavor and $R_4$ group has steric, hydrophobic, H-bond favor.

• Applied Biological Chemistry
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• v.29 no.3
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• pp.294-303
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• 1986

The effects of insecticides on biochemical precesses in soil were studied by determining the effects of the chemical structure of each insecticides on enzyme activities, pesticide residue and total number of bacteria revealed when soil treated with urea was incubated at $28{\pm}1^{\circ}$ for 56 days. The inhibition effects of insectides on enzyme activites in soil decreased in the order: dithiophosphoric acid > thiophosphhoric acid > phosphoric acid > carbamate insecticides for urease and phosphatase, thiophosphoric acid > dithiophosphoric acid > phosphoric acid > carbamate insecticides for L-glutaminase and protease. The inhibition effects of organophophorus insecticides on enzyme activities in soil were maintained longer than those of carbamate insecticides. Carbamate insecticides increased the activities of protease and L-glutaminase at 56 days. When insecticides were treated in soil together with urea, the degradation of insecticides was accelerated. By treatment of insecticides, the total number of bacteria was decreased at the early stage of treatment but thereafter increased according to phosphoric acid and carbamate insecticides.

• The korean journal of orthodontics
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• v.29 no.1 s.72
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• pp.95-106
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• 1999

This study was performed to examine the effect of bisphosphonate, an inhibitor of bone resorption, on the formation of osteoclast and bone resorption during experimental tooth movement. Whether bisphosphonate has a cytotoxicity in high dose was also examined. Eighty-seven male Sprague-Dawley rats, weighing 260-350g, were classified into normal (no appliance + $0.9\%$ NaCl), control (appliance + $0.9\%$ NaCl) and four bisphosphonate-treated (appliance + 0.8, 4, 20 or 100mg/kg) groups. The maxillary left first molar was moved mesially with the tipping movement using 50-70g of force. Bisphosphonate(etidronate disodium) was injected intraperitoneally with a dose of 0.8, 4, 20, or 100 mg/kg simultaneously with the application or the orthodontic force. They were killed at day 1, 3, or 7 after the application or the orthodontic force. The activities of serum acid phosphatase and lactate dehydrogenase (LDH) were assayed, and osteoclasts and the degree of bone resorption were examined histologically. The results obtained were as follows: 1. Acid phosphatase activities were significantly higher in the appliance groups, both control and bisphosphonate-treated (4, 20, and 100 mg/kg) groups, at days 1 and 3 than these in normal. At day 1, bisphosphonate-treated(4, 20mg/kg) groups showed even higher acid phosphatase than control. However, at day 7, no significant difference was noted between the control and bisphosphonate-treated groups. 2. LDH activities in the 4, 20mg/kg bisphosphonate-treated groups were increased during the experimental Periods examined, but there were no significant differences in the 0.8, 100mg/kg bisphosphonate-treated groups. 3. There was no bone resolution at day 1, but severe bone resorption was observed at days 3 and 7 in the control. Bone resorption was reduced by bisphosphonate-treatment at day 3. Bone resolution observed at day 7 was similar between the control and bisphosphonate-treated groups. 4. Few osteoclasts were observed at the alveolar bone in the control and bisphosphonate-treated groups at day 1. At day 3, numerous osteoclasts were shown in the control, the degree of which was reduced in bisphosphonate-treated groups. These results suggest that the inhibition of the osteoclast formation was not the mechanism of bone resorption by the bisphosphonate-treatment during experimenal tooth movement. There was no distinct cytotoxicity with a high dose of bisphosphonate. And the drug should be administrated repeatedly to maintain the inhibitory effect of bone resolution.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.11 no.9
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• pp.3358-3365
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• 2010

This study was carried out to investigate the effect of Sorbus commixta (SC), Geranium thunbergii (GT) and their mixture (SC:GT=1:1, MIX) on inhibition of bone loss and chondral defect. To examine their activities, we measured the alkaline phosphatase (ALP) activity in human osteoblast-like MG-63 cells and performed tartrate-resistant acid phosphate (TRAP) staining in osteoclast differentiated from Raw264.7 cells. To investigate the influence on chondrocyte differentiation, we performed alcian-blue staining in chondrocyte differentiated from ATDC5 cells. All of SC, GT and MIX did not increase ALP activity in MG-63 cells. However, SC and mixture (SC:GT=1:1, MIX) significantly inhibited osteoclastic differentiation. And they also induced chondrocyte differentiation. These results suggest that SC and GT may have a potential for the treatment of bone loss and chondral defect by suppression of osteoclast differentiation and stimulation of chondrocyte differentiation. Therefore, clarification of their mechanisms and active components will be needed.