• Advances in Traditional Medicine
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• v.9 no.3
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• pp.238-244
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• 2009

Gymnosporia rothiana (walp) Lawson (celastraceae), commonly known as Maytenus rothiana, is used in Indian folk medicine as an antiulcerogenic agent. However, there have been no scientific reports regarding its antiulcer activity. Therefore, this study was intended to evaluate the antiulcer property of petroleum ether, chloroform, and methanolic extract of leaves of Gymnosporia rothiana at different dose levels in ethanol induced and indomethacin induced gastric ulcer models. It was observed that oral administration of all the extract of Gymnosporia rothiana produces significant reduction in ulcer lesion index as well as increase in volume and pH of gastric content in both experimental models, being petroleum ether extract the most effective at dose of 250 mg/kg; it significantly reduced gastric lesion index (70.06%), in comparison to omeprazole (71.20%) and methanolic extract at a dose of 500 mg/kg (67.22%). Increased gastric mucosal defense mechanism by petroleum ether extract is probably due to its high levels of terpenoids like $\beta$ amyrin, lupeol acetate. The present results clearly shows antiulcer effect of Gymnosporia rothiana against various irritants has been mainly due to cytoprotective effect mediated through prostaglandin and partly due to free radical scavenging activity.

• Journal of the Korean Chemical Society
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• v.57 no.2
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• pp.234-240
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• 2013

The synthesis of title compounds were accomplished by synthetic sequence shown in Scheme 1. Chalcones on cyclocondensation with thiourea in ethanol and potassium hydroxide under reflux yielded the respective dihydropyramidin-2(1H)-thiones. Each of the dihydropyrimidin thiones was, then subjected to the Mannich condensation in alkaline medium using three different secondary amines, viz., dimethylamine, diethylamine and morpholine to obtain a new series of S-Mannich bases. All the synthesised compounds ($C_1-C_{15}$) were evaluated for their antiulcer and antibacterial activities. Compounds $C_4$, $C_5$, $C_6$, $C_{14}$ and $C_{15}$ exhibited relatively more potent antiulcer activity but not comparable to the standard; Omeprazole, while $C_1$, $C_2$, $C_3$ and $C_{13}$ were moderate in activity at 100 mg/kg p.o. All the compounds ($C_1-C_{15}$) showed mild to moderate activity against both Gram-positive (S.aureus, L.delbrueckii) and Gram-negative (P.vulgaris, E.coli) bacteria. Amongst the compounds tested, only $C_6$, $C_9$, $C_{12}$ and $C_{15}$ were found to be potent.

• Korean Journal of Clinical Pharmacy
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• v.10 no.2
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• pp.57-61
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• 2000

Gastrointestinal (GI) medications have been administered to many patients without any gastrointestinal diseases. The objectives of this study were to evaluate use of GI drugs and assess related factors. Medical records of 600 outpatients were reviewed from January 1997 to December 1997 at A Hospital, Kyunggi-do, Korea. Fifty patients every month among all outpatients were randomly selected up to total 600 patients. Surgical patients, visitors for regular health examination and inpatients were excluded. GI symptoms included nausea, vomiting, diarrhea, dyspepsia, constipation, heartburn, dysphagia and abdominal pain. The prescribed gastrointestinal drugs were antacids. $H_2$-antagonist, sucralfate, cisapride, omeprazole, laxatives, digestive enzymes and antidiarrheal agents. Patients without GI symptoms were 348 out of 600 outpatients who were screened. Two hundred and eighty two of 348 patients $(81\%)$ were given GI drugs though they did not have any GI symptoms. There were no differences in regard to sex and age of patients. Most of medical departments prescribed gastrointestinal drugs for these patients. The most frequently prescribed drugs were in order of digestive enzyme, antacids and $H_2$-antagonists. In view of economic aspects, patients paid 12.28 percents of total cost per prescription for unnecessary medicines. The medical practice of prescribing GI drugs should be assessed to define appropriate subgroups to have benefits with prophylactic administration and to reduce adverse effects caused by drug interactions. Pharmacists would have a significant role to promote rational drug therapy.

• Journal of Veterinary Clinics
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• v.40 no.5
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• pp.341-348
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• 2023

An 11-year-old neutered male domestic short-haired cat presented with neurological symptoms that developed over a three-month period. These included mental dullness, vocalization, ataxia, and visual impairment. The patient was diagnosed with a primary intracranial tumor at a local animal hospital. After the first diagnosis, the cat was administered hydroxyurea, prednisolone, omeprazole, and gabapentin for 3 months. After the initiation of medical treatment, the patient's clinical symptoms did not improve and the size of the tumor was static on the second magnetic resonance imaging (MRI). The dosage of hydroxyurea and prednisolone was increased for two weeks. The patient's clinical signs improved, and subsequently, a craniotomy was performed. The clinical signs completely resolved six days after surgery. Adjuvant chemotherapy with hydroxyurea was continuously administered after the craniotomy. The patient demonstrated a good clinical status during the nine-month follow-up period. Neoadjuvant chemotherapy has not yet been reported for meningiomas in cats. Further clinical trials with longer follow-up periods and larger patient cohorts will be required to confirm the effectiveness of neoadjuvant chemotherapy with hydroxyurea in feline meningioma.

• Journal of Veterinary Clinics
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• v.31 no.3
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• pp.220-222
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• 2014

A 14 year-old Shih-tzu was referred to the Veterinary Medical Teaching Hospital of Chungnam National University with a history of foreign body ingestion and vomiting. The vomitus contained ketoprofen plaster, which is used for orthopedic analgesia in humans. Supportive care and gastrointestinal (GI) protective agents were administered, including famotidine, misoprostol, sucralfate, omeprazole, and fluid therapy. However, the clinical signs worsened, and anemia, melena, leukocytosis, and azotemia developed. The patient was diagnosed with GI hemorrhage and underwent a whole blood transfusion followed by barium sulfate administration. After administering barium sulfate as a GI protectant, the clinical signs improved, and the patient was discharged.

• The Journal of Korean Medicine
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• v.32 no.6
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• pp.74-84
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• 2011

Objectives: Palmul-tang (hachimotsu-to in Japanese and bawu-tang in Chinese) is a mixture of eight herbs. It is traditionally used for the treatment of anemia, anorexia, general weakness, and female infertility in China, Japan, and Korea. In this study, we investigated the protective effects of Palmul-tang water extract (PTE) against ethanol-induced acute gastric injury in rats. Material and Methods: Acute gastric lesions were induced by intragastric administration of 5mL/kg body weight of absolute ethanol to each rat. Control group rats were given PBS orally and the ethanol group (EtOH group) received absolute ethanol (5mL/kg) by oral gavage. The positive control group and the PTE group were given oral doses of omeprazole (50mg/kg) or PTE (400mg/kg), respectively, 2 h prior to the administration of absolute ethanol. The stomach of each animal was excised and examined for gastric mucosal lesions. To confirm the protective effects of PTE, we evaluated the degree of lipid peroxidation, the level of reduced glutathione (GSH), and the activities of the antioxidant enzymes catalase, glutathione-S-transferase, glutathione peroxidase, and glutathione reductase in the stomach. Results: PTE reduced ethanol-induced hemorrhage and hyperemia in the gastric mucosa. PTE reduced the increase in lipid peroxidation associated with ethanol-induced acute gastric lesions and increased mucosal GSH content and the activities of antioxidant enzymes. Conclusion: These results indicate that PTE protects gastric mucosa against ethanol-induced acute gastric injury by increasing antioxidant status. We suggest that PTE could be developed as an effective drug for the treatment of acute gastric injury.

• Toxicological Research
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• v.17
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• pp.145-155
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• 2001

Cytochrome P4502C19 (CYP2C19) is one of human polymorphic xenobiotic-metabolizing enzymes. The enzyme has been reported to catalyze more than 70 substrates, involving more than 100 reactions. These include several classes of therapeutic agents (e.g. anti-microbial. cardiovascular, psycho-active, etc.), sex hormones and insecticides. Associations of the CYP2C19 genotype/phenotype with individual differences in drug efficacy (e.g. diazepam, omeprazole, proguanil) and toxicity (e.g. mephenytoin, barbiturates) have been documented by many investigators. At least 11 allelic variants of CYP2C19 gene were reported to date. Most of the mutant alleles found in the poor metabolizer (PM) led to the production of truncated and/or inactive proteins. Except for the exon 6, single-nucleotide mutations were reported in all nine exons of the gene. Genetic polymorphism of CYP2C19 shows marked interethnic variation with the population frequencies of PM phenotype ranging from 1∼2% up to more than 50%. The prevalence of CYP2C19 PM tends to be higher in Asian and certain Pacific Islanders than other race or ethnic specificity. Genotyping results of CYP2C19 also revealed that there are different proportions of individual mutant alleles among ethnic populations. This may, in part, explains the interethnic difference in the metabolism of certain drugs (i.e. diazepam), though they were from the same CYP2C19 phenotype. Recently, our research group has studied the genotype and phenotype of CYP2C19 and found that the PM frequency (7∼8%) in Thais is lower than other Asian populations. Molecular and clinical impacts of this finding warrant to further investigation.

• Microbiology and Biotechnology Letters
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• v.47 no.4
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• pp.536-545
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• 2019

Cytochrome P450 (P450 or CYP) is involved in the metabolism of endogenous and exogenous compounds in most organisms. P450s have great potential as biocatalysts in the pharmaceutical and fine chemical industries because they catalyze diverse oxidative reactions using a wide range of substrates. The high-cost nicotinamide cofactor, NADPH, is essential for P450 reactions. Glucose-6-phosphate dehydrogenase (G6PDH) has been commonly used in NADPH-generating systems (NGSs) to provide NADPH for P450 reactions. Currently, only two G6PDHs from Leuconostoc mesenteroides and Saccharomyces cerevisiae can be obtained commercially. To supply high-cost G6PDH cost-effectively, we cloned the cytosolic G6PDH gene of Solanum lycopersicum (tomato) with 6xHis tag, expressed it in Escherichia coli, and purified the recombinant G6PDH (His-G6PDH) using affinity chromatography. In addition, enzymatic properties of His-G6PDH were investigated, and the His-G6PDH-coupled NGS was optimized for P450 reactions. His-G6PDH supported CYP102A1-catalyzed hydroxylation of omeprazole and testosterone by NADPH generation. This result suggests that tomato His-G6PDH could be a cost-effective enzyme source for NGSs for P450-catalyzed reactions as well as other NADPH-requiring reactions.

• Journal of Microbiology and Biotechnology
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• v.21 no.5
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• pp.483-493
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• 2011

An acid phosphatase (HppA) activated by $NH_4Cl$ was purified 192- and 34-fold from the periplasmic and membrane fractions of Helicobacter pylori, respectively. SDS-polyacrylamide gel electrophoresis revealed that HppA from the latter appears to be several kilodaltons larger in molecular mass than from the former by about 24 kDa. Under acidic conditions (pH${\leq}$4.5), the enzyme activity was entirely dependent on the presence of certain mono- and/or divalent metal cations (e.g., $K^+$,$ NH_4{^+}$, and/or $Ni^{2+}$). In particular, $Ni^{2+}$ appeared to lower the enzyme's $K_m$ for the substrates, without changing $V_{max}$. The purified enzyme showed differential specificity against nucleotide substrates with pH; for example, the enzyme hydrolyzed adenosine nucleotides more rapidly at pH 5.5 than at pH 6.0, and vice versa for CTP or TTP. Analyses of the enzyme's N-terminal sequence and of an $HppA^-$ H. pylori mutant revealed that the purified enzyme is identical to rHppA, a cloned H. pylori class C acid phosphatase, and shown to be the sole bacterial 5'-nucleotidase uniquely activated by $NH_4Cl$. In contrast to wild type, $HppA^-$ H. pylori cells grew more slowly. Strikingly, they imported $Mg^{2+}$ at a markedly lowered rate, but assimilated urea rapidly, with a subsequent increase in extracellular pH. Moreover, mutant cells were much more sensitive to extracellular potassium ions, as well as to metronidazole, omeprazole, or thiophenol, with considerably lowered MIC values, than wild-type cells. From these data, we suggest that the role of the acid phosphatase HppA in H. pylori may extend beyond 5'-nucleotidase function to include cation-flux as well as pH regulation on the cell envelope.

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