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1.
Bioorg Med Chem Lett ; 27(14): 3060-3064, 2017 07 15.
Article in English | MEDLINE | ID: mdl-28551100

ABSTRACT

Sialidases are key virulence factors that remove sialic acid from host cell surface glycans, thus unmasking receptors to facilitate bacterial adherence and colonization. In this study, we report the isolation and characterization of novel inhibitors of the Streptococcus pneumoniae sialidases NanA, NanB, and NanC from Myristica fragrans seeds. Of the isolated compounds (1-12), malabaricone C showed the most pneumococcal sialidases inhibition (IC50 of 0.3µM for NanA, 3.6µM for NanB, and 2.9µM for NanC). These results suggested that malabaricone C and neolignans could be potential agents for combating S. pneumoniae infection agents.


Subject(s)
Enzyme Inhibitors/pharmacology , Lignans/pharmacology , Myristica/chemistry , Neuraminidase/antagonists & inhibitors , Plant Extracts/pharmacology , Enzyme Activation/drug effects , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Inhibitory Concentration 50 , Kinetics , Lignans/chemistry , Lignans/isolation & purification , Myristica/metabolism , Neuraminidase/metabolism , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Protein Isoforms/antagonists & inhibitors , Protein Isoforms/metabolism , Resorcinols/chemical synthesis , Resorcinols/isolation & purification , Resorcinols/pharmacology , Seeds/chemistry , Seeds/metabolism , Streptococcus pneumoniae/drug effects , Streptococcus pneumoniae/enzymology
2.
Gut and Liver ; : 49-57, 2014.
Article in English | WPRIM | ID: wpr-36653

ABSTRACT

BACKGROUND/AIMS: The major compounds of Cochinchina momordica seed extract (SK-MS10) include momordica saponins. We report that the gastroprotective effect of SK-MS10 in an ethanol-induced gastric damage rat model is mediated by suppressing proinflammatory cytokines and downregulating cytosolic phospholipase A2 (cPLA2), 5-lipoxygenase (5-LOX), and the activation of calcitonin gene-related peptide. In this study, we evaluated the gastroprotective effects of SK-MS10 in the nonsteroidal anti-inflammatory drug (NSAID)-induced gastric damage rat model. METHODS: The pretreatment effect of SK-MS10 was evaluated in the NSAID-induced gastric damage rat model using aspirin, indomethacin, and diclofenac in 7-week-old rats. Gastric damage was evaluated based on the gross ulcer index by gastroenterologists, and the damage area (%) was measured using the MetaMorph 7.0 video image analysis system. Myeloperoxidase (MPO) was measured by enzyme-linked immunosorbent assay, and Western blotting was used to analyze the levels of cyclooxygenase (COX)-1, COX-2, cPLA2, and 5-LOX. RESULTS: All NSAIDs induced gastric damage based on the gross ulcer index and damage area (p<0.05). Gastric damage was significantly attenuated by SK-MS10 pretreatment compared with NSAID treatment alone (p<0.05). The SK-MS10 pretreatment group exhibited lower MPO levels than the diclofenac group. The expression of cPLA2 and 5-LOX was decreased by SK-MS10 pretreatment in each of the three NSAID treatment groups. CONCLUSIONS: SK-MS10 exhibited a gastroprotective effect against NSAID-induced acute gastric damage in rats. However, its protective mechanism may be different across the three types of NSAID-induced gastric damage models in rats.


Subject(s)
Animals , Male , Rats , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Arachidonate 5-Lipoxygenase/drug effects , Calcitonin Gene-Related Peptide/drug effects , Cyclooxygenase 1/drug effects , Cyclooxygenase 2/drug effects , Disease Models, Animal , Gastric Mucosa/chemistry , Group IV Phospholipases A2/drug effects , Momordica/chemistry , Peroxidase/drug effects , Plant Extracts/pharmacology , Rats, Sprague-Dawley , Seeds/chemistry , Stomach Ulcer/chemically induced , Treatment Outcome
3.
Article in English | WPRIM | ID: wpr-206183

ABSTRACT

In this study, we produced iron-fortified yeast (Saccharomyces cerevisiae) producing Sus scrofa ferritin heavy-chain to provide iron supplementation in anemic piglets. We determined whether iron-ferritin accumulated in recombinant yeasts could improve iron deficiency in mice. C57BL/6 male mice exposed to Fe-deficient diet for 2 weeks were given a single dose of ferrous ammonium sulfate (FAS), ferritin-producing recombinant yeast (APO), or APO reacted with iron (Fe2+) (FER). The bioavailability of recombinant yeasts was examined by measuring body weight gain, hemoglobin concentration and hematocrit value 1 week later. In addition, ferritin protein levels were evaluated by western blot analysis and iron stores in tissues were measured by inductively coupled plasma spectrometer. We found that anemic mice treated with FER exhibited increased levels of ferritin heavy-chain in spleen and liver. Consistently, this treatment restored the iron concentration in these tissues. In addition, this treatment significantly increased hemoglobin value and the hematocrit ratio. Furthermore, FER treatment significantly enhanced body weight gain. These results suggest that the iron-fortified recombinant yeast strain is bioavailable.


Subject(s)
Animals , Humans , Male , Mice , Ammonium Sulfate , Anemia , Biological Availability , Blotting, Western , Body Weight , Diet , Ferritins , Ferrous Compounds , Hematocrit , Hemoglobins , Iron , Liver , Plasma , Quaternary Ammonium Compounds , Saccharomyces , Saccharomyces cerevisiae , Spleen , Sprains and Strains , Sus scrofa , Yeasts
4.
Article in Korean | WPRIM | ID: wpr-59555

ABSTRACT

Recently, intra-Muscular Stimulation (IMS) therapy is being increasingly used for musculoskeletal pain. This procedure is generally regarded as a safe procedure for the general public. Some cases of iatrogenic pneumothorax caused by acupuncture have been reported in the medical literature. However, a case of an IMS therapy associated pneumothorax has not reported. We experienced two cases of iatrogenic pneumothorax after IMS therapy. A 62 year-old man received IMS therapy on the right shoulder due to posterior neck pain. After IMS therapy, acute dyspnea and chest discomfort developed. The other patient was a 74 year-old woman who also received IMS therapy. This patient experienced a nonproductive cough and acute dyspnea after the treatment. As the popularity of this form of alternative medicine increases, we might expect to see more cases of iatrogenic pneumothorax. Physicians should be aware of the adverse events associated with IMS therapy.


Subject(s)
Aged , Female , Humans , Middle Aged , Acupuncture , Complementary Therapies , Cough , Dyspnea , Musculoskeletal Pain , Neck Pain , Pneumothorax , Shoulder , Thorax
5.
Article in Korean | WPRIM | ID: wpr-57771

ABSTRACT

Pseudohypoaldosteronism (PHA) type l is a rare neonatal disease characterized by salt wasting, dehydration, hyperkalemia and metabolic acidosis. It is unresponsive to mineralocorticoid treatment with elevated aldosterone concentration. The three different modes of inheritance has been described. The autosomal dominant form has a mild clinical course and gradually improves with age. In this form, resistance to aldosterone seems to be restricted to the kidney. The autosomal recessive form displays generalized aldosterone resistance including kidney, colon, lung, sweat and salivary gland system. This form is more severe and requires life-long supplement with high-dose salt. The sporadic form is mild and resembles the autosomal dominant form. In this paper, we describe a male patient diagnosed as PHA type l at the age of 19 months. He presented with recurrent vomiting, diaphoresis accompanying hyponatremia, hyperkalemia, metabolic acidosis, elevated plasma renin activity and aldosterone level. Ultimately he has improved with treatment by oral sodium bicarbonate.


Subject(s)
Humans , Male , Acidosis , Aldosterone , Colon , Dehydration , Hyperkalemia , Hyponatremia , Kidney , Lung , Plasma , Pseudohypoaldosteronism , Renin , Salivary Glands , Sodium Bicarbonate , Sweat , Vomiting , Wills
6.
Korean Journal of Medicine ; : 607-615, 2007.
Article in Korean | WPRIM | ID: wpr-17397

ABSTRACT

BACKGROUDN: In end-stage renal disease (ESRD) patients, cardiovascular disease (CVD) is a major cause of morbidity and mortality. These patients frequently have hyperhomocysteinemia, a putative risk factor for cardiovascular disease. Several studies suggest that lowering plasma homocysteine may improve endothelial dysfunction, a marker of atherothrombotic risk. Pulse wave velocity (PWV) is a useful diagnostic tool to access endothelial dysfunction, and is widely used screening test for atherosclerosis. METHODS: We measured fasting total plasma homocysteine (tHcy) in 84 hemodialysis patients and 21 peritoneal dialysis patients. Subjects were assigned to two groups. Group I (tHcy or =20 umol/L) consisted of 26 ESRD patients who have taken high dose folate (5 mg/day). For 15 Group I patients and 5 Group II patients, pulse wave doppler velocity (PWV) measurements were taken before and after 3 months of folate treatment. RESULTS: The mean tHcy concentration was higher in the ESRD patients (82 HD: 16.9+/-6.4 mol/L, 20 PD: 18.0+/-16.7 mol/L). The pulse wave velocity (PWV) was faster in ESRD patients-19 HD: Aorta (Ao)-PWV 8.98+/-1.4, lower extremities (LE)-PWV 10.15+/-1.3, upper extremities (UE)-PWV 8.80+/-0.8 (m/s); 8 PD: Ao-PWV 9.32+/-1.8, LE-PWV 10.64+/-1.4, UE-PWV 9.24+/-0.7 (m/s). The PWV increased in ESRD patients with coronary heart disease and who had a history of angioplasty because of thrombosis or stenosis of vascular access. There was a significant reduction in hyperhomocysteinemia after 3 months in the high dose folate supplement group as compared to the usual dose folate supplement group with a significant statistical difference between the two groups. (15 Group I patients: 13.9+/-4.9 mol/L->13.5+/-6.1 for 5 Group II patients: 34.3+/-27.5 mol/L->23.0+/-5.9 mol/L (p0.05, paired t-test). CONCLUSIONS: We assume that PWV and homocysteine concentration have some correlation and both studies are available as part of screening tests for atherosclerosis in ESRD. Although no significant interval change was detected for the PWV, this finding suggests that high-dose folate supplementation was helpful to minimize the risk of cardiovascular disease associated with hyperhomocysteinemia in ESRD patients.


Subject(s)
Humans , Angioplasty , Aorta , Atherosclerosis , Blood Flow Velocity , Cardiovascular Diseases , Constriction, Pathologic , Coronary Disease , Fasting , Folic Acid , Homocysteine , Hyperhomocysteinemia , Kidney Failure, Chronic , Lower Extremity , Mass Screening , Mortality , Peritoneal Dialysis , Plasma , Pulse Wave Analysis , Renal Dialysis , Risk Factors , Thrombosis , Upper Extremity
7.
Immune Network ; : 19-24, 2002.
Article in Korean | WPRIM | ID: wpr-213058

ABSTRACT

BACKGROUND: Salvia miltiorrhiza (SM), a traditional oriental medicine, has been reported to have anti-tumor properties, but its exact mechanism remains to be elucidated. In this study, we investigated several of the molecular events that occur in human breast carcinoma MCF-7 cells and human pulmonary adenocarcinoma A549 cells. METHODS: For this purpose, we evaluated the growth-inhibitory effect of SM in association with the expressions of p53, p21, cyclin D1, and pRb, which are known to be involved in cell cycle arrest. The extent of thymidine incorporation was also examined to assess G1/S phase cell cycle arrest in both cells by 3H-thymidine incorporation. RESULTS: Our results show that SM inhibits the growth and the proliferation of MCF-7 and A549 cells. Furthermore, we also observed increased expression of p21 via a p53-dependent pathway in both cell lines after treating with SM. In addition, treatment with SM for 24 hours caused the suppression of hyperphosphorylated retinoblastoma protein (pRb) expression and the dephosphorylation of pRb. CONCLUSION: These findings suggest that the growth inhibitory and the anti-proliferation effects of SM on MCF-7 cells and A549 cells are mediated via the decreased expression and dephosphorylation of pRB by p21 up-regulation in a p53-dependent manner. To the best of our knowledge, this study is the first to report upon the molecular mechanisms involved in SM-induced tumor cell growth inhibition.


Subject(s)
Humans , Adenocarcinoma , Breast Neoplasms , Cell Cycle Checkpoints , Cell Line , Cyclin D1 , MCF-7 Cells , Medicine, East Asian Traditional , Retinoblastoma Protein , Salvia miltiorrhiza , Salvia , Thymidine , Up-Regulation
8.
Article in Korean | WPRIM | ID: wpr-115337

ABSTRACT

BACKGROUND: The effects of the inhibitor of nitric oxide synthase (NOS) in cerebral ischemia have been debated. Recently, it has been suggested that it depends on the amount of the inhibitor used. Therefore, this study was carried out to evaluate the effects of the NOS in the acute ischemia-reperfusion of the cat model using variable amounts of the inhibitor. METHODS: Nineteen cats were divided into 3 groups: group 1 (n = 6), 10 mg/kg of N-nitro-L-arginine methyl ester (L-NAME); group 2 (n = 7), 0.5 mg/kg; group 3 (n = 6), control group. Incomplete global cerebral ischemia was induced by ligation of both carotid arteries with arterial hypotension (-40 mmHg) for 30 minutes followed by 3 hours of reperfusion. The NOS inhibitor (L-NAME), was injected intraperitoneally 5 minutes before reperfusion. 31P and 1H MR spectroscopy were performed. A series of spectra was acquired in the time intervals before ligation, during ischemia, and after reperfusion. RESULTS: Phosphocreatine/inorganic phosphate (PCr/Pi) ratios for group 1 were significantly lower than for groups 2 and 3 (P < 0.05), and there was no significant difference between groups 2 and 3. Lactate/N-acetyl aspartate (Lac/NAA) and lactate/creatine (Lac/Cr) ratios at 180 minutes after reperfusion were higher for group 1 than for groups 2 and 3 (P < 0.05). There were no significant differences in pH and lactate/choline (Lac/Cho) ratios among the 3 groups. CONCLUSIONS: It is demonstrated that the effect of the NOS inhibitor is dosage dependent. A high dose (10 mg/kg) of L-NAME seems to have an adverse effect on recovery of the ischemia, but a low dose (0.5 mg/kg) seems to have no effect.


Subject(s)
Animals , Cats , Aspartic Acid , Brain Ischemia , Brain , Carotid Arteries , Energy Metabolism , Hydrogen-Ion Concentration , Hypotension , Ischemia , Ligation , Magnetic Resonance Spectroscopy , NG-Nitroarginine Methyl Ester , Nitric Oxide Synthase , Nitric Oxide , Reperfusion
9.
Article in Korean | WPRIM | ID: wpr-178752

ABSTRACT

The delayed adjustable strabismus surgery may be desirable because the angle of strabismus can be changed after the strabismus surgery. We have studied the effect of 2% cyclosporin A on the delayed adjustable strabismus surgery in rabbits. Two percent cyclosporin A was soaked for 5 minutes for group 4 and 10 minutes for group 5 between the conjunctiva and sclera during the adjustable strabismus surgery on the eyes of New Zealand white rabbits. The eyes in group 1 received only adjustable strabismus surgery, and those in group 2 and 3 received the surgery including 5 minutes and 10 minutes soaking with castor oil, respectively. We evaluated the time of adjustability and measured the traction force and length during adjustment after the adjustable strabismus surgery. We could adjust in all of the 6 eyes in group 4 and 5 two weeks after the surgery. At 1 week, the traction forces were 30.7+/-14.0 (mean+/-SD), 42.0+/-39.6, 31.7+/-7.5, 24.0+/-7.5, and 21.8+/-6.0 gm in group 1, 2, 3, 4, and 5, respectively. The forces in group 4 and 5 were not significantly different from those in group 1, 2, and 3. At 2 weeks, the degrees of adhesion between the conjunctiva and superior rectus muscle, and those between the muscle and sclera were significantly lower in group 4 and 5 than those in group 1, 2, and 3. These results suggest that 2% cyclosporin A soaking is useful to obtain the better results due to the delayed adjustment by decreasing the adhesion around the muscle (J KoreanOphthalmol Soc 41:2115~2123, 2000).


Subject(s)
Rabbits , Castor Oil , Conjunctiva , Cyclosporine , Sclera , Strabismus , Traction
10.
Article in Korean | WPRIM | ID: wpr-121018

ABSTRACT

Developmental glaucoma is essentially a surgical disease, with goniotomy or trabeculotomy recommended as a primary surgical procedure. Although the success rates of both procedure are similar, trabeculotomy can be performed in eyes of with a hazy cornea, whereas a clear cornea is necessary to perform a goniotomy. To inspect the clinical results after primary trabeculotomy and find out the factors that have an influence on the outcome of surgery, we reviewed 40 consecutive eyes of 26 patients with developmental glaucoma who had underwent trabeculotomy as a primary surgical procedure. Preoperative intraocular pressure (IOP), corneal diameter, C/D ratio was compared to postoperative values and the cumulative success probability was calculated, with defining the success as the case where the IOP has been maintained equal to or less than 21mmHg after surgery without no enlargement in corneal diameter or progression of cupping of the optic disc. IOP was reduced by 18.7% after surgery and this change was statistically significant (p<0.01). However, there were no significant changes from the preoperative value in corneal diameter and C/D ratio. The cumulative success probability were 82.3% and 49.0% at 6 month and 1 year, respectively. Corneal opacity seemed to influence the outcome adversely with the 1 year cumulative success rate of 90.0% in the cases without corneal opacity and 37.6% in the cases with corneal opacity (p<0.05), whereas the type of glaucoma, age at the time of surgery, corneal opacity, preoperative IOP, corneal diameter, and C/D ratio appeared to make no differences on the outcome. In conclusion, trabeculotomy reduced the IOP effectively, but the success rate was significantly lower in eyes with corneal opacity. Therefore, investigations to find a better surgical treatment modality for the developmental glaucoma with corneal opacity will be needed.


Subject(s)
Humans , Cornea , Corneal Opacity , Glaucoma , Intraocular Pressure , Trabeculectomy
11.
Article in Korean | WPRIM | ID: wpr-32174

ABSTRACT

PURPOSE: This study was designed to evaluate early parenchymal changes of acute cerebral ischemia / infarct by using T2-weighted, diffusion-weighted, and calculated apparent diffusion coefficient (ADC) MR imaging. MATERIALS AND METHODS: The brain MR images were successfully obtained 30, 60, 90, 120, 150 and 180 minutes after intraarterial administration of Lipiodol (0.4 - 0.6 ml) into the common carotid artery in 10 of 11 cats (91%). T2-and diffusion-weighted images and ADC were analyzed and compared with histopathologic findings. RESULTS: High signal intensity on T2-weighted and diffusion-weighted images was found in one cerebral hemisphere 30 minutes after Lipiodol injection, which tended to increase with time until 3 hours. Subcortical white matter showed higher signal intensity than cortical gray matter since 30 minutes after embolization. ADC images showed decreased signal intensity in the embolized hemisphere, which tended to decrease until 3 hours. Microscopic findings of the area corresponding to the abnormal signal intensity on MR images revealed varying degrees of edema in the gray and white matters involved. CONCLUSION: It is suggested that Lipiodol can be used as a good embolic agent causing early ischemic changes in experimental models. In addition to T2-weighted images, diffusion-weighted and ADC images can provide the further informations in the evaluation of the early parenchymal changes of cerebral infarct.


Subject(s)
Animals , Cats , Brain , Brain Ischemia , Carotid Artery, Common , Cerebrum , Diffusion , Edema , Ethiodized Oil , Magnetic Resonance Imaging , Models, Theoretical
12.
Article in Korean | WPRIM | ID: wpr-192998

ABSTRACT

In vivo 31P NMR spectra were obtained in eight infant brain at 4.7T. Each phosphorus metabolite and its ratio were analyzed to evaluate the brain damage and maturity, and compared with the reported data obtained at the lower field strength. Measurement of T1 relaxation time at 4.7T was done in an infant and a cat brain in vivo. PCr/Pi and PCr/β-ATP ratio were used as a marker of brain damage. PME/PDE revealed higher values than those of the reported data obtained at the lower field strength and the difference was partly attributed to the long T1 relaxation time of PME rather than the brain immaturity. Although the resolution of the spectrum was improved at 4.7T, a long repetition time is recommended to minimize T1difference of phosphorus metabolites of brain at 4.7T.


Subject(s)
Animals , Cats , Humans , Infant , Brain , Magnetic Resonance Spectroscopy , Phosphorus , Relaxation
14.
Article in Korean | WPRIM | ID: wpr-92022

ABSTRACT

The authors observed the anesthetic effects of an intravenous drip of ketamine hydrochloride supplemented with diazepam and nitrous oxide on the cardiovascular system and the psychotomimetic reaction in 38 relarively healthy patients who underwent abdominal surgery at Chonbuk National Hospital from May to Sept., 1985. The results were compared with those obtained from patients anesthetized with halothanenitrous oxide-oxygen. 1) The rate of intravenous drip of ketamine was 1mg/kg/hr, which adequately maintained the level of surgical anesthesia. The total amount of pancuronium required for satisfactory skeletal muscle relaxation was 40% more in the ketamine group than in the halothane group. 2) Following ketamine anesthesia, systolic pressure revealed a transient increase immediately after induction, and about 4minutes after the commencement of surgery it thereafter returned to the preinduction level and remained stable during the operation this is in contrast with halothane anesthesia in which the systolic pressure decreased and remained below the level of preinduction after a transient increase immediately after induction. 3) The difference in diastolic pressure between ketamine and halothane anesthesia was significant(p0.05). 5) Contrary to halothane anesthesia, anticholinergic premedication could not completely prevent endotracheal secretion following ketamine anesthesia. 6) Premedication with diazepam could not completely relieve psychotomimetic reactions including convulsion and hallucination after ketamine anesthesia.


Subject(s)
Humans , Anesthesia , Anesthetics , Blood Pressure , Cardiovascular System , Diazepam , Hallucinations , Halothane , Heart Rate , Infusions, Intravenous , Ketamine , Muscle, Skeletal , Nitrous Oxide , Pancuronium , Premedication , Relaxation , Seizures
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