• Biomolecules & Therapeutics
• /
• v.11 no.1
• /
• pp.41-50
• /
• 2003

General pharmacological properties of DA-8159, a new pyrazolopyrimidinone derivative were examined in laboratory animals to investigate its safety profile. The oral administration of DA-8159 (1, 5 or 30 mg/kg) in mice and rats had no effect on general behaviors and central nervous system of the animals in test systems, such as hexobarbital-induced sleeping time, motor coordination, normal body temperature, writhing syndromes induced by 0.75% acetic acid solution, chemo-shock produced by pentetrazole solution and rotar rod test. Anesthetized cats treated intravenously with DA-8159 (0.1, 0.3, 1, 3 or 10 mg/kg) showed transient and mild decrease in blood pressure. However, heart rate, respiration rate and tidal volume were not changed by intravenous DA-8159. In the isolated organs including ileum, heart (sinus rate of atria and contractility of papillary muscle), trachea of guinea pigs and phrenic nerve of rats, DA-8159 ($10^{-8}$ ∼$10^{-5}$ mg/L) did not elicit any effect or inhibitory action on the chemically or electrically stimulated contraction. DA-8159 did not influence gastric secretion, pH and total acid output in rats and intestinal propulsion in mice. The administration of DA-8159 in rats had no effect on the platelet aggregation induced by ADP in rabbit plasma, urinary volume and electrolyte ion ($Na^{+}$, $K^{+}$, $Cl^{-}$) excretion in rats. Prothrombin time (PT) of the rats showed a mild but significant increase after administration of DA-8159. Activated partial thromboplastin time (APTT), however, was not affected by DA-8159. These results indicate that DA-8159 does not exert any of serious pharmacological effects.

• Journal of Microbiology and Biotechnology
• /
• v.18 no.2
• /
• pp.338-342
• /
• 2008

This study was performed to screen and select Lactobacillus strains from chicken feces for probiotic use in animals. Of these strains, strain AU had the highest immunostimulatory effect. Therefore, strain A12 was characterized as a potential probiotic. Strain A12 was tentatively identified as Lactobacillus acidophilus A12, using the API 50 CHL kit based on a 99.9% homology. L. acidophilus A12 was highly resistant to artificial gastric juice (pH 2.5) and bile acid (oxgall). Based on results from the API ZYM kit, leucine arylamidase, crystine arylamidase, acid phosphatase, naphthol-AS-BI-phosphohydrolase, ${\alpha}$-galactosidase, ${\beta}$-galactosidase, ${\alpha}$-glucosidase, ${\beta}$-glucosidase, and N-acetyl-${\beta}$-glucosamidase were produced by strain A12. L. acidophilus A12 showed resistance to several antibiotics (nisin, gentamicin, and erythromycin). The amount of interleukin $(IL)-1{\alpha}$ in $20{\times}$ concentrated supernatant from L. acidophilus A12 was approximately 156pg/ml. With regard to antioxidant activity, L. acidophilus A12 supernatant showed 60.6% DPPH radical scavenging activity. These results demonstrate the potential use of L. acidophilus A12 as health-promoting probiotics.

• Journal of Microbiology and Biotechnology
• /
• v.29 no.11
• /
• pp.1729-1738
• /
• 2019

In sourdough fermentation, lactic acid bacteria perform important roles in the production of volatile and antimicrobial compounds, and exerting health-promoting effects. In this study, we report the probiotic properties and baking characteristics of Lactobacillus plantarum SPC-SNU 72-2 isolated from kimchi. This strain is safe to use in food fermentation as it does not carry genes for biogenic amine production (i.e., hdc, tdc, and ldc) and shows no β-hemolytic activity against red blood cells. The strain is also stable under simulated human gastrointestinal conditions, showing tolerance to gastric acid and bile salt, and adheres well to colonic epithelial cells. Additionally, this strain prevents pathogen growth and activates mouse peritoneal macrophages by inducing cytokines such as tumor necrosis factor-α, interleukin (IL)-6, and IL-12. Furthermore, the strain possesses good baking properties, providing rich aroma during dough fermentation and contributing to the enhancement of bread texture. Taken together, L. plantarum SPC-SNU 72-2 has the properties of a good starter strain based on the observation that it improves bread flavor and texture while also providing probiotic effects comparable with commercial strains.

• Korean Journal of Bronchoesophagology
• /
• v.9 no.1
• /
• pp.60-66
• /
• 2003

Although there is a wide range of diseases caused by gastric acid reflux and the number of cases is on the rise, it is difficult for the laryngologist to make the correct diagnosis. The treatment for laryngopharyngeal reflux can be grouped into 3 categories - changes in lifestyle, medication, and surgery. The medication used to treat laryngopharyngeal reflux are prokinetic agents and acid supressive agents such as antacids, H2 blockers, and PPIs(Proton pump inhibitor). Rabeprazole sodium($Pariet^{\circledR}$) is a newly developed agent belonging to the PPI group, but in contrast with the existing drugs such as omeprazole, lansoprazole, pantoprazole, has a low dependency on CYP2C19 during the metabolic cycle. Thus, it is known to have a quick but fixed antiacid effect and less individual differences. We analyzed 2166 patients from 32 hospitals who were prescribed $Pariet^{\circledR}$ from May, 2001 to April, 2002. The patients were divided into 4 groups according to the duration of treatment - Group 1: 1-14 days, Group 2: 15-28 days, group 3: 29-56 days, Group 4: more than 56 days. The cases were then analyzed for improvement of 8 symptoms(heart bum, regurgitation, chronic cough, hoarseness, globus sensation, chronic throat clearing, sore throat, and dysphagia), improvement on laryngoscope, usefulness to the doctor, and complication development. Of the total of 2116 patients, 1627(75.1%) cases showed at least 50% improvement of symptoms and the amount of improvement increased according to the duration of medical treatment. Most of the patients showed objective improvement on the laryngoscope, with 32.9% showing significant improvement and 38.7% showing moderate improvement. 37.6% of the doctors questioned replied that $Pariet^{\circledR}$ was very useful and 50.3% said it was useful, showing that most were satisfied with the treatment results. The complications known to develop after taking PPI are headache, nausea, diarrhea, abdominal pain, constipation, dizziness, fatigue, and of these, only a small percentage of the patients complained of mild headache. $Pariet^{\circledR}$ has shown to be a relatively safe and effective drug for the treatment of laryngopharyngeal reflux.

• YAKHAK HOEJI
• /
• v.38 no.2
• /
• pp.123-130
• /
• 1994

Physicochemical properties and hydrolysis kinetics of new some oral cephalosporins were examined in buttered solution and human plasma or rat liver homogenate. The test cephalosporins were 7-[(Z)-2-(2-aminothiazole-4-yl)-2- methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazinyl] thiocarbonylthhiomethyl-3-cephem-4-carboxylic acid (CEN1), 7-[(Z)-2-(2-aminoth iazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimidyl)piperazinyl]th iocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN2), pivaloyloxymethyl-7-[ (Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl)piperazi nyl]thiocarbonylthiomethy1-3-cephem-4-carboxylate (CEN1P), and pivaloyloxymethyl-7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[ 4-(2-pyrimidyl)piperazinyl]thiocarbonyl-thiomethyl-3-cephem-4-carboxylate (CEN2P). The partition coefficient(Ko/w) of CEN1P, CEN2P were higher than those of CEN1, CEN2. The calculated pKa values of CEN1, CEN2, CEN1P, and CEN2P were 7.09, 7.75, 4.92, and 5.39, respectively. The hydrolysis of CEN1P and CEN2P were not depend on the composition of pH of the test medium except weak alkaline buffered solution (pH 8.00). CEN1 and CEN2 were very stable in pH 6.80 and 8.00 buffer solutions. CEN1P and CEN2P were rapidly deesterified to CEN1 and CEN2 in human plasma and in rat liver homogenate. Half-lives$(t_{1/2})$ of CEN1 and CEN2 were 3.49 and 4.93 hr in human plasma, 1.47 and 1.26 hr in rat liver homogenate, respectively.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.42 no.7
• /
• pp.1157-1161
• /
• 2013

The purpose of this work was to measure the changes in ${\gamma}$-aminobutyric acid (GABA) and polyphenolic content of two different rice varieties (Geunnun and Ilpum), as well as the antiproliferative activities of both germinated brown rice varieties in cancer cells. The contents of GABA in Geunnun and Ilpum, especially in the bran of Ilpum increased significantly after germination. The content of polyphenol in Geunnun also increased after germination, but the contents of flavonoid in both varieties decreased after germination. A significant increase in the antiproliferative activity of both varieties on human lung and gastric cancer cell line was observed after germination.

• Journal of the Korean Society of Laryngology, Phoniatrics and Logopedics
• /
• v.18 no.2
• /
• pp.96-101
• /
• 2007

Laryngopharyngeal reflux (LPR) is the retrograde movement of gastric contents into the larynx, pharynx, and upper aero-digestive tract. LPR differs from gastroesophageal reflux in that it is often not associated with heartburn and regurgitation symptoms. Otolaryngological manifestations of acid reflux include a wide range of pharyngeal and laryngeal symptoms. Belafsky et al. developed a useful self-administered tool, the reflux symptom index (RSI), for assessing the degree of LPR symptoms. Patients are asked to use a 0 to 5 point scale to grade the following symptoms: 1) hoarseness or voice problems; 2) throat clearing; 3) excess throat mucus or postnasal drip ; 4) difficulty swallowing; 5) coughing after eating or lying down; 6) breathing difficulties ; 7) troublesome or annoying cough; 8) sensation of something sticking or a lump in the throat; 9) heartburn, chest pain, indigestion or stomach acid coming up. A RSI score greater than 13 is considered abnormal. As there is no validated instrument to document the physical findings and severity of LPR, Belafsky et al. developed an eight-item clinical severity scale for judging laryngoscopic finding, the reflux finding score (RFS). They rated eight LPR-associated findings on a scale from 0 to 4 : subglottic edema, ventricular obliteration, erythema/hyperemia, vocal-fold edema, diffuse laryngeal edema, posterior commissure hypertrophy, granuloma/granulation tissue, and thick endolaryngeal mucus. A RFS score of greater than 7 was found to suggest LPR-associated laryngitis. Although both indices (RSI and RFS) are widely used, there is some controversy about their validity (sensitivity and specificity) and reliability (intra-rater and inter-rater) in LPR diagnosis and treatment. We discuss the validity and reliability of RSI and RFS with literature review.

• The Journal of Internal Korean Medicine
• /
• v.34 no.2
• /
• pp.165-177
• /
• 2013

Objectives : The object of this study was to observe the protective effects of 8 types of individual herbal components of Yijintang-gamibang, on the reflux esophagitis (RE) in rats as compared with omeprazole. Methods : Each 100 mg/kg individual herbal component was orally pretreated, at 1 hr before and 6 hrs after pylorus and forestomach ligation, the changes on the esophageal lesion areas, gastric volumes, acid and pepsin outputs, antioxidant effects, esophageal total hexose and sialic acid contents were observed with changes on the esophageal histopathology. The results were compared with an omeprazole 10 mg/kg treated group. Results : Pylorus and forestomach ligation-induced RE were inhibited by treatment of all 8 herbal components and omeprazole except for Pinella Rhizoma and Massa Meicata Fermentata, in order of Atractylodis Rhizoma, Citri Pericarpium, omeprazole, Glycyrrhizae Radix, Hordei Fructus Germiniatus, Holelen and Citri Pericarpium, as compared with RE control. Pinella Rhizoma and Massa Meicata Fermentata did not show any favorable protective effects against RE nor antioxidant effects in the present study. Conclusions : The main active herbal components showing favorable protective effects on RE of Yijintang-gamibang mediated by antioxidant effects, were Atractylodis Rhizoma, Citri Pericarpium, Glycyrrhizae Radix, Hordei Fructus Germiniatus, Holelen and Citri Pericarpium. Furthermore Atractylodis Rhizoma and Citri Pericarpium showed more favorable protective effects as compared with omeprazole, therefore, it is expected that Atractylodis Rhizoma and Citri Pericarpium have potential as new alternatives or safe therapeutics against RE.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.18 no.1
• /
• pp.187-193
• /
• 2004

Constipation is a common clinical problem that comprises of symptoms that include excessive straining, hard feces, feeling of incomplete evacuation and infrequent defecation. Although many conditions, such as metabolic problems, fiber deficiency, anorectal problem, an drug, can cause constipation. This study was examined the effects of Chilsun-Whan on intestinal mucosa and gastrointestinal transit time and plasma lipids in rats. Adult male rats were fed for weeks on diets containing no addition(basal diet group), 5% cellulose(cellulose group) and 2.5% . Chilsun-Whan group(Chilsun-Whan group). The results were as follows; 1. The fecal weght was significantly increased 2 times in Chilsun-Whan administrated group compare to basal diet group. 2. The gastrointestinal transit times was significantly decreased in Chilsun-Whan administrated group compare to basal diet. 3. Carmine red mixed with Chilsun-Whan, as a marker, was administered through a gastric tube for stomach or intracecally by a chronically implanted catheter for colon transit. Small intestinal transit and large intestinal transit time were significantly decreased in Chilsun-Whan administrated group compare to basal diet. 4. The height of jejunal villi was developed in Chilsun-Whan administrated group compare to basal diet The thickness of mucosa and muscle layer of colonic mucosa were significantly developed in Chilsun-Whan administrated group compare to basal diet group. 5. The change of goblet cell in colonic mucosa was increased acid mucin stained alcian blue in Chilsun-Whan administrated group compare to basal diet and cellulose group. 6. HDL-cholesterol of plasma lipid was increased in Chilsun-Whan administrated group compare to basal diet and cellulose groups. Theses results suggests that Chilsun-Whan may be used in prevention and treatment of constipation resulting in increase of fecal weight, decrease of gastrointestinal transit time. development of intestinal villi, intensify of stainability of acid mucin in colon.

• Macromolecular Research
• /
• v.17 no.9
• /
• pp.709-713
• /
• 2009

The aim of this study was to develop novel intestinal specific drug delivery systems with pH sensitive swelling and drug release properties. The carboxyl group of ibuprofen was converted to a vinyl ester group by reacting ibuprofen and vinyl acetate as an acylating agent in the presence of catalyst. The glucose-6-acrylate-1, 2, 3, 4-tetraacetate (GATA) monomer was prepared under mild conditions. Cubane-1, 4-dicarboxylic acid (CDA) linked to two 2-hydroxyethyl methacrylate (HEMA) group was used as the crosslinking agent (CA). Methacrylic-type polymeric prodrugs were synthesized by the free radical copolymerization of methacrylic acid, vinyl ester derivative of ibuprofen (VIP) and GATA in the presence of cubane cross linking agent. The structure of VIP was characterized and confirmed by FTIR, $^1H$ NMR and $^{13}C$ NMR spectroscopy. The composition of the cross-linked three-dimensional polymers was determined by FTIR spectroscopy. The hydrolysis of drug polymer conjugates was carried out in cel-lophane membrane dialysis bags, and the in vitro release profiles were established separately in enzyme-free simulated gastric and intestinal fluids (SGF, pH 1 and SIF, pH 7.4). The detection of a hydrolysis solution by UV spectroscopy at selected intervals showed that the drug can be released by hydrolysis of the ester bond between the drug and polymer backbone at a low rate. Drug release studies showed that increasing the MAA content in the copolymer enhances the rate of hydrolysis in SIP. These results suggest that these polymeric prodrugs can be useful for the release of ibuprofen in controlled release systems.