• Biomolecules & Therapeutics
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• v.22 no.3
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• pp.260-266
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• 2014

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin $E_2$ in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

• Korean journal of applied entomology
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• v.17 no.4 s.37
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• pp.193-199
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• 1978

Five parents and their 10 $F_1$ crosses of maize (Zea mays L.) were tested by means of diallel analysis for the inheritance of peroxidase activity following Puccinia sorghi rust infection. Peroxidase activity was measured at day zero and at 2 days and 8 days after inoculation. Peroxidase activity was increased significantly by P. sorghi infection in all 15 genotypes after 8 days, but not after 2 days. Highly significant differences in peroxidase activity were detected among the 15 genotypes. The highly genera] resistant inbred, CM105, and its hybrids showed exceptionally high peroxidase activity in both healthy and infected plants. However, another highly resistant inbred, Oh545, showed exceptionally low peroxidase activity. Significant general combining ability (GCA) and specific combining ability (SCA) means quares were detected for peroxidase activity independent of disease. GCA mean spuares, however, were consistently a major contiribution to the inheritance of peroxidase activity in the infected plants whereas SCA men square contributions were minor. Rust resistant maize plants controlling mongenic dominant $Rp_1^d$gene showed stronger peroxidase reroxidase responses than their susceptible counterparts in the gel electrophoresis and densiometric tracings. The increased peroxidase activity occurred in both major leaf peroxidases, $Px_3\;and\; Px_7$.

• Journal of Veterinary Clinics
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• v.26 no.4
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• pp.324-330
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• 2009

This study was performed to determine the effectiveness of poloxamer/sodium alginate mixture(PX/SA) barriers on prevention of post-operative peritoneal adhesion in dogs. Fifteen mongrel dogs were divided into three experimental groups: non-treated group, 2% Sodium Carboxymethylcellulose (SCMC) treated group and PX/SA treated group. In order to induce adhesions, the anti-mesenteric serosa of the ileum was exteriorized and then abraded in a standard manner by scraping with a scalpel blade to create homogeneous petechial hemorrhagic surface over a 1 ${\times}$ 1 cm area. Solution of SCMC was allowed to spread across the intraperitoneal organs through a catheter using a syringe. PX/SA was simply coated over the abraded tissues. On day before and day 1, 4, 7, and 14 after operation, venous blood specimens were collected for measurement of RBC, total WBC and fibrinogen. The adhesions were blindly assessed 3 weeks later by using a computerized tensiometer. The RBC, total WBC and fibrinogen values of three groups showed no statistical significances. The mean tensile strength(gram force, gf) of formed adhesions on day 21 after surgery was 173.05${\pm}$113.48 in the non-treated group, 111.42 ${\pm}$ 38.25 in the SCMC group, and 69.00 ${\pm}$ 45.07 in the PX/SA group. The tensile strength values for adhesion seperation in PX/SA group was lower than those in SCMC group(p < 0.05) and significantly lower than those in the non-treated group(p < 0.05). Our data suggested that PX/SA should be effective on reducing peritoneal adhesion formation in dogs compared with SCMC. PX/SA may be applicable to preventing post-operative intraperitoneal adhesion in dogs.

• Proceedings of the Korean Society for Applied Microbiology Conference
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• 2000.04a
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• pp.208-213
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• 2000

Penicillium fellutanum produces a phosphorylated, choline-containing extracellular peptido-polysaccharide, peptidophosphogalactomannan (pPxGM) (8). The $\^$13/C-methyl labeled pPxGM ([methyl-$\^$13/C]pPxGM) was prepared from the cultures supplemented with L-[methyl-$\^$13/C]methionine or [2-$\^$13/C]glycine and was used as a probe to monitor the fate of phosphocholine in this polymer. Addition of purified [methyl-$\^$l3/C]pPxGM to growing cultures in low phosphate medium resulted in the disappearance of [methyl-$\^$13/C]phosphocholine and -N,N'-dimethyl-phosphoethanolamine from the added [methyl-$\^$13/C]pPxGM. Two $\^$l3/C-methyl-enriched cytoplasmic solutes, choline-O-sulfate and glycine betaine, were found in mycelial extracts, suggesting that phosphocholine-containing extracellular pPxGM of P.fellutanum is a precursor of intracellular choline-O-sulfate and glycine betaine and thus of phosphatydilcholine (l0). $\^$13/C-Methyl-labeled cells grown in 3 M NaCl-containing medium showed 2.6- and 22-fold more accumulation of $\^$13/C-methyl labeled choline-O-sulfate and glycine betaine, respectively, originated from the extracellular [$\^$13/C-methyl]pPxGM than those grown without added NaCl. The results suggest that, in addition to glycerol and erythritol, glycine betaine and choline-O-sulfate and thus choline are also osmoprotectants and hence that pPxGM is involved in osmotolerance of this fungus (11). Taken collectively, the $\^$l3/C- and $\^$31/P-NMR analyses of cytosolic solute pools and structural modulation of extracellular pPxGM corresponding to environmental stimuli in P. fellutanum, provided evidence that pPxGM is involved in cellular choline metabolism, osmotolerance, and recycling of metabolites.

• Journal of Pharmaceutical Investigation
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• v.39 no.5
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• pp.359-366
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• 2009

In this study, paclitaxel-loaded lipid nanosuspension (PxLN) was prepared and the in vivo profiles after intravenous administration in rats were investigated. We compared the manufacturing processes depending on the temperature: PxLN-H for a hot homogenization process and PxLN-C for solidification of lipid-drug mixtures by liquid nitrogen. Both formulations showed submicron size distribution and the similar drug loading efficiency of about 70%. In vitro release of PxLNs and Taxol$^{(R)}$ performed by a dialysis diffusion method showed similar pattern for PxLN-H and Taxol$^{(R)}$, but the reduced release profile for PxLN-C. PxLN or Taxol$^{(R)}$ was intravenously administered to the rats at a dose of 5 mg/kg as paclitaxel. The drug in blood samples were assayed by the HPLC/MS/MS method. The AUC$_t$ of PxLN-H was 3.4-fold greater than that of Taxol$^{(R)}$. PxLN-H gave higher biodistribution in all tissues than did Taxol$^{(R)}$. In addition, it maintained the higher drug concentration for 12 h. This lipid nanosuspension might be a promising candidate for an alternative formulation for the parenteral delivery of poorly water-soluble paclitaxel.

• Preventive Nutrition and Food Science
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• v.9 no.4
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• pp.367-373
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• 2004

The prevalence of type-2 diabetes increases remarkably in post-menopausal women, possibly because insulin secretion fails to compensate for the insulin resistance induced in various tissues by estrogen insufficiency. However, this has not been fully defined. Therefore, the present study investigated whether an ovariectomy (OVX) would increase insulin resistance and decrease the $\beta$-cell function and mass in female rats with and without a $90\%$ pancreatectomy (Px). Female rats aged 15 weeks were divided into four groups: 1) OVX + Px, 2) SOVX (sham operation of OVX) + Px, 3) OVX + SPx (sham operation of Px), and 4) SOVX + SPx, and given a $30\%$ fat diet for 8 weeks. At the end of the experimental period, the islet function and insulin resistance were determined using a hyperglycemic clamp and a euglycemic hyperinsulinemic clamp, respectively. The OVX only increased the body weight in the SPx rats, which was partially related to the food intake. Yet, the OVX did increase the peripheral insulin resistance, while the Px increased this resistance further. The OVX and Px both exacerbated the islet function, as measured by the insulin secretion pattern, while delaying and decreasing the first-phase insulin secretion. The OVX only decreased the proliferation of $\beta$-cells in the Px rats, while increasing apoptosis in both the Px and SPx rats. As a result, the OVX decreased the $\beta$-cell mass in the Px rats, but increased the mass in the SPx rats. In conclusion, an OVX was found to accelerate the development and progression of diabetes by increasing the insulin resistance and decreasing the $\beta$-cell mass. Therefore, menopause can be a risk factor for type-2 diabetes, mainly due to a deceased proliferation of $\beta$-cells.

• Korean Journal of Food Science and Technology
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• v.33 no.5
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• pp.619-625
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• 2001

We determined whether the supplementation of Polygonatum Odoratum (Mill) Druce (POD) extract had a good effect on insulin resistance in peripheral tissues of 90% pancreatectomized (Px) and sham-operated (Sham) male Sprague Dawley rats. Px and Sham rats were divided into two groups; one group daily consumed 0.3 g of POD extracts per 1 ㎏ body weight for two months, and the other group had a placebo. All rats freely consumed a 40% fat diet. At the end of the experiment, a euglycemic hyperinsulinemic (EH) clamp was performed in a fasting, awake, and unstressed state to determine insulin resistance. At EH clamp, body weights were higher in Sham rats than Px rats, and serum glucose levels of baseline were affected by diabetic status and POD administration. Serum insulin concentrations were higher in Sham rats than Px rats, and POD administration decreased them in Sham rats compared to P. Glucose disposal rates in peripheral tissues increased with POD in both Px (n=10) and Sham (n=10) rats. But glycogen deposits in soleus muscle increased with POD administration in Px and Sham rats, and total glycogen synthase activity and fraction velocity were higher in POD groups. Triglyceride contents in quadriceps muscles decreased with POD in Px rats. In conclusions, POD improves insulin resistance by enhancing glucose utilization with increasing glycogen deposit and decreasing triglyceride contents in muscles.

• Journal of Veterinary Clinics
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• v.26 no.6
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• pp.547-555
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• 2009

This study was performed to determine the minimum dose of Poloxamer/Sodium alginate (PX/SA) mixture on preventing intraperitoneal adhesions to evaluate organ toxicity. Twenty five healthy adult mongrel dogs (weighing 4.68${\pm}$1.67 kg) were divided into five experimental groups composed of five dogs respectively; negative control group (NC, non-treated), positive control group (PC, 2% carboxymethyl chitosan solution treated), and experiment 1 group (E1, 0.25 ml PX/SA mixture of abraded area), experiment 2 group (E2, 0.5 ml PX/SA mixture of abraded area), experiment 3 group (E3, 1.0 ml PX/SA mixture of abraded area). Venous blood specimens were collected from all experimental animals for hematologic and biochemical analysis: WBC, fibrinogen, AST, ALT, ALP, BUN and creatinine. The anti-adhesion effect was evaluated using a serosa abrasion model. The denuded ileum was coated with PX/SA mixture, carboxymethyl chitosan solution or neither. The tensile strength of the adhesion site was evaluated with a tensiometer. For histopathological examination, tissue samples of the liver and kidney were collected from all dogs. According to the results, the frequency and tensile strength values for adhesion separation in PX/SA group were significantly lower than those in negative control group (p < 0.05). In E2 group, the tensile strength was significantly decreased in consideration of PX/SA dose. The values of AST, ALT, ALP, BUN and creatinine of the control and the experimental groups showed no statistical differences. No obvious microscopic differences were noted among tissue sections obtained from all groups. The results suggest that PX/SA mixture may be effective on reducing peritoneal adhesion formation in dog and that 0.5 ml PX/SA mixture of abraded area is most effective dose. Moreover, PX/SA mixture was considered not to have toxicity for the liver and the kidney.

• Journal of Microbiology and Biotechnology
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• v.27 no.11
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• pp.1925-1931
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• 2017

Korean red pine (Pinus densiflora) bark extract, PineXol (PX), was investigated for its potential antioxidant and anti-inflammation effects in vitro. It was hypothesized that PX treatment ($25-150{\mu}g/ml$) would reduce the lipid synthesis in HepG2 hepatocytes as well as lipid accumulation in 3T3-L1 adipocytes. Hepatocytes' intracellular triglycerides and cholesterol were decreased in the PX $150{\mu}g/ml$ treatment group compared with the control (p < 0.05). Consequently, de novo lipogenic proteins (acetyl-CoA carboxylase 1, stearoyl-CoA desaturase 1, elongase of very long chain fatty acids 6, glycerol-3-phosphate acyltransferase 1, and sterol regulatory element-binding protein 1) were significantly decreased in hepatocytes by PX $150{\mu}g/ml$ treatment compared with the control (p < 0.05). In differentiated 3T3-L1 adipocytes, the lipid accumulation was significantly attenuated by all PX treatments (p < 0.01). Regulators of adipogenesis, including CCAAT-enhancer-binding proteins alpha, peroxisome proliferatoractivated receptor gamma, and perilipin, were decreased in PX $100{\mu}g/ml$ treatment compared with the control (p < 0.05). In conclusion, PX might have anti-obesity effects by blocking hepatic lipogenesis and by inhibiting adipogenesis in adipocytes.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.2
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• pp.221-224
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• 1997

Effects of melatonin on hepatic glutathione-peroxidase (GSH-Px) and glutathione-reductase (GSH-reductase) activities were studied in Sprague-Dawley (SD) rats administered i.p. (10 mg/kg body weight) with melatonin during 15 days. The activity of cytosolic GSH-reductase in the liver was not changed by melatonin. However, melatonin injection increased significantly the activity of liver cytosolic GSH-Px activity compared with those in saline-treated rats. At the same time, plasma GSH-Px was also increased significantly in melatonin-treated rats. Since GSH-Px, a major antioxidative enzyme, removes $H_2O_2$ and lipid peroxides which are formed during lipid peroxidation from cellular membrane, such elevation of heptatic GSH-Px activity may contribute to the improvement of antioxidative effects under oxidative damage in the liver.