• Journal of Pharmaceutical Investigation
• /
• v.27 no.2
• /
• pp.119-123
• /
• 1997

The physicochemical and structural properties of new capsaicin derivative, DA-5018, were examined. The reference standard of this compound was obtained by the recrystallization. A method for the determination of the dissociation constant of the compound is described. pH-solubility and distribution coefficient were determined by chromatographic method. Fundamental properties on thermal behaviors were investigated by TG, DTA and DSC. Structural analysis based on spectroscopic method coincided with the chemical structure of DA-5018. Approximate dissociation constant of the compound determined by UV spectral method was 9.35. Solubilities and partition coefficients in various pH buffer solution appeared pH-dependency. No crystal transition or further transition was found in the thermal analysis. This compound showed good stability, but pH 13 buffer and acetone made some degradative products.

• The Korean Journal of Pesticide Science
• /
• v.4 no.3
• /
• pp.27-33
• /
• 2000

N-Dimethoxyphosphinothionyl carbofuran, PSC, has a high insecticidal activity and low mammalian toxicity. Ten N-phosphinothionyl carbofuran derivatives were synthesized and their insecticidal activities were determined against brown plant hopper (Nilaparvata lugens), green peach aphid (Myzus persicae), diamondback moth (Plutella xylostella), and two-spotted spider mite (Tetranychus urticae). Green peach aphid, diamondback mea and brown plant hopper were controlled over 90% by application of 125 ppm, 125 ppm, and 63 ppm, respectively, of carbosulfan. Two hundred and fifty ppm of newly synthesized compounds could control most of brown plant hopper and diamondback moth. Especially, insecticidal activities of compound 10 against brown plant hopper, diamondback moth, and green peach aphid were similar to those of carbosulfan. Our results show that the newly synthesized derivatives of NV-phosphinothionyl carbofuran have a similar insecticidal activity to carbosulfan.

• Korean journal of applied entomology
• /
• v.61 no.2
• /
• pp.299-305
• /
• 2022

We investigated the occurrence and damage information of 9 species (7 families) of insect pests in two places of rucola (Eruca sativa Mill.) cultivated houses in Gyeonggi Province from 2019 to 2021, and selected five insecticides that could efficiently control the beet armyworm, Spodoptera exigua. Five insecticides (spineram SC, fluxametamide EC, chlorantraniliprole WG, cyantraniliprole DC, and emamectin benzoate EC) showed high control effects over 95% against 3^rd instar larvae of S. exigua at the two places of rucola cultivation, and there was no phytotoxicity at double dose of concentration.

• Journal of The Korean Ophthalmological Society
• /
• v.59 no.11
• /
• pp.1039-1048
• /
• 2018

Purpose: To evaluate the effects of anti-vascular endothelial growth factor (VEGF) treatment on the healthcare-related finances of patients with age-related macular degeneration. Methods: Changes in health care financing due to newly introduced benefit standards were predicted over the coming 5-year period (2018-2022). We also analyzed the financial impact of scenarios in which agents similar to anti-VEGF, such as the over-licensed drug bevacizumab, were introduced. For this purpose, the future number of patients receiving anti-VEGF treatments was estimated for various scenarios based on National Health Insurance Corporation claims data followed by an estimate of the financial burden. Results: In the case of age-related macular degeneration, the current standard of care (14 times in a lifetime) was maintained in scenario 1. In 2018, the insurance budget for the coming 5-year period was estimated at approximately 440.3 billion won. The insurance cost for that period was estimated at approximately 560.1 billion won under the revised standard of December 2017 (scenario 2). For scenarios wherein, after 2020, similar treatments (scenario 3) and bevacizumab (scenario 4) were introduced, the estimated health insurance costs were 521 billion won and 419.7 billion won, respectively. Conclusions: Health insurance costs are projected to increase substantially due to the elimination of the 14 time pay standard; however, the actual budget will only moderately increase, due to new limitations of visual acuity ${\leq}0.1$ or in case of scarring/atrophic lesions. Clinically similar agents and bevacizumab could be considered as alternatives to anti-VEGF treatment for age-related macular degeneration.

• The Korean Journal of Pesticide Science
• /
• v.14 no.3
• /
• pp.199-208
• /
• 2010

Phenylformamidine derivatives are well known as insecticides for their specific activity against the insects. It has now been established that they show insecticidal activity as agonists on the octopamine receptor. In order to get a highly active compound we have intensively exploited fluorine substituted-aromatic formamidines possessing N-dialkylaminosulfeny group. Up to now, there are several candidates we found: N-(dialkylamino)sulfenyl-N-methyl-N'-(4-fluoro-2-methylphenyl)formamidines. The miticidal activity of Compound 29 show five-fold higher than Amitraz.

• The Korean Society of Law and Medicine
• /
• v.19 no.1
• /
• pp.3-20
• /
• 2018

Pharmacopunture is a new combined method of acupunture and oriental drugs. Recently, this method is widely used to treat traffic accident patients in oriental medicine. However, there is no evidences of treatment, no information of effects and side-effects of this method, and no information of drugs used. In South Korea, western medicine and oriental medicine are regulated differently. When a new technology is invented in the area of western medicine, that method should pass several stages of clinical trials. After that processes, that method can be done as a medical practice. However, in the area of oriental medicine, there is no process like that. According to in South Korea, medical practice without license are composed of two behaviors. First type is that medical practice is done by a person who has no medical license. Second type is that medical practice is done by a person who has a medical license but the area of the license is different. Because of this reason, the distinction between the western medical practices and the oriental medical practices is very important. Medical practices are protected by license mainly because they can harm human life or body. When we invented new medical practice and try to practice it to the patients, we should consider the risk of that method whether it is western medical practice or oriental medical practice. It is not clear that the pharmcopunture which has been done is satisfied the standard of medical treatment.

• Tuberculosis and Respiratory Diseases
• /
• v.49 no.6
• /
• pp.691-702
• /
• 2000

Background : Acute lung injury (ALI) is a commonly encountered respiratory disease and its prognosis is poor when the treatment is not provided promptly and properly. However no specific pharmacologic treatment is currently available for ALI, although recently several supportive drugs have been under scrutiny. We studied anti-inflammatory effects of pentoxifylline (PF), a methylated xanthine, and ONO-5046, a synthetic neutrophil elastase inhibitor on lipopolysaccharide (LPS)-induced ALI in vitro. Methods : To establish an in vitro model of LPS-induced ALI, primary rat alveolar macrophages and peripheral neutrophils in various ratios (1:0, 5:1, 1:1, 1:5, 0:1) were co-cultured with transformed rat alveolar epithelial cells (L2 cell line) or vascular endothelial cells (IP2-E4 cell line) under LPS stimulation. Each experiment was divided into five groups-control, LPS, LPS+PF, LPS+ONO, and LPS+PF+ONO. We compared LPS-induced superoxide anion productions from primary rat alveolar macrophages and peripheral neutrophils in various ratios, and the resultant cytotoxicity on L2 cells or IP2-E4 cells between groups. In addition we also compared the productions of tumor necrosis factor (TNF)-$\alpha$ interleukin (IL)-$1{\beta}$, monocyte chemotactic protein(MCP)-1, IL-6, and IL-10 as well as mRNA expressions of TNF-$\alpha$ inducible nitric oxide synthetase(iNOS), and MCP-1 from LPS-stimulated primary rat alveolar macrophages between groups. Results : (1) PF and ONO-5046 in each or both showed a trend to suppress LPS-induced superoxide anion productions from primary rat alveolar macrophages and peripheral neutrophils regardless of their ratio, except for the LPS+PF+ONO group with the 1:5 ratio, although statistical significance was limited to a few selected experimental conditions. (2) PF and ONO-5046 in each or both showed a trend to prevent IP2-E4 cells from LPS-induced cytotoxicity by primary rat alveolar macrophages and peripheral neutrophils regardless their ratio, although statistical significance was limited to a few selected experimental conditions. the effects of PF and/or ONO-5046 on LPS-induced L2 cell cytotoxicity varied according to experimental conditions. (3) PF showed a trend to inhibit LPS-induced productions of INF-$\alpha$ MCP-1, and IL-10 from primary rat alveolar macrophages. ONO-5046 alone didnot affect the LPS-induced productions of proinflammatory cytokines from primary rat alveolar macrophages but the combination of PF and ONO-5046 showed a trend to suppress LPS-induced productions of INF-$\alpha$ and IL-10 PF and ONO-5046 in each or both showed a trend to increase LPS-induced IL-$\beta$ and IL-6 productions from primary rat alveolar macrophages. (4) PF and ONO-5046 in each or both showed a trend to attenuate LPS-induced mRNA expressions of TNF-$\alpha$ and MCP-1 from primary rat alveolar macrophages but at the same time showed a trend increase iNOS mRNA expression. Conclusion : These results suggest that PF and ONO-5046 may play a role in attenuating inflammation in LPS-induced ALI and that further study is needed to use these drugs as a new supportive therapeutic strategy for ALI.

• Journal of Life Science
• /
• v.26 no.7
• /
• pp.835-846
• /
• 2016

Chemo-resistance is the biggest issue of effective cancer therapy. ABCG2 is highly correlated with multi-drug resistance, and represent a typical phenotype of multiple cancer stem-like cells. Accumulating evidence recently reported that oncolytic viruses represent a new strategy for multiple aggressive cancers and drug resistant cancers including cancer stem cell-like cells and ABCG2 expressing cells. In this study, we generated an evolutionally engineered vaccinia virus, SLJ-496, for drug-resistant cancer therapy. We first showed that SLJ-496 treatment enhanced tumor affinity using cytopathic effect assay, plaque assay, as well as cell viability assay. Next, we clearly demonstrated that in vitro SLJ-496 treatment represents significant cytotoxic effect in multiple cancers including colorectal cancer cells (HT-29, HCT-116, HCT-8), gastric cancer cells (AGS, NCI-N87, MKN-28), Hepatocellular carcinoma cells (SNU-449, SNU-423, SNU-475, HepG2), as well as mesothelioma cell (NCI-H226, NCI-H28, MSTO-221h). Highly ABCG2 expressing HT-29 cells represent cancer stem like phenotype including stem cell marker expression, and self-renewal bioactivities. Interestingly, we demonstrated that in vitro treatment of SLJ-496 showed significant cytotoxicity effect, as well as viral replication capacity in ABCG2 overexpressing cell. In addition, we also demonstrated the cytotoxic effect of SLJ-496 in Adriamycin-resistant cell lines, SNU-620 and ADR-300. Taken together, these findings provide us a pivotal clue that cancer therapy using SLJ-496 vaccinia virus might be new therapeutic strategy to overcome ABCG2 expressing cancer stem-like cell and multiple chemo-resistance cancer cells.

• Tuberculosis and Respiratory Diseases
• /
• v.64 no.1
• /
• pp.8-14
• /
• 2008

Background: Acinetobacter infections are difficult to treat as they often exhibit multiple resistance to the antibiotics that are currently available for the treatment of pneumonia. Colistin is active against gram-negative bacteria, including the multiple drug resistant (MDR) Acinetobacter species. However, intravenous administration of colistin was abandoned because of its nephrotoxicity and neurotoxicity. The aims of this study were to examine the efficacy and safety of colistin administered by aerosol in the treatment of pneumonia caused by MDR Acinetobacter baumannii. Methods: We retrospectively reviewed the medical records of patients admitted to the intensive care unit (ICU) from Dec. 2006 to Aug. 2007 who had been diagnosed as suffering from pneumonia due to MDR Acinetobacter baumannii and had been treated with nebulized colistin. Results: 31 patients received aerosolized colistin. The average duration of the treatment was $14{\pm}7$ days and the daily dose of ranged from 225 mg to 300 mg. All patients received concomitant intravenous antimicrobial agents. The average length of the stay in the ICU was $34{\pm}21$ days and in the hospital $58{\pm}52$ days. The overall microbiological eradication was observed in 25 patients (80.6%). 14 of these (56%) were cured, and 11 (44%) were infected with other microorganisms. The overall crude mortality of the ICU was 48%. Nephrotoxicity and significant bronchial constriction did not occur in any patient during neublized colistin treatment. Conclusion: Nebulized colistin may be a safe and effective option in the treatment of pneumonia due to MDR Acinetobacter baumannii. Its role in therapy warrants further investigation in comparative studies.

• Tuberculosis and Respiratory Diseases
• /
• v.48 no.2
• /
• pp.191-202
• /
• 2000

Background: Bronchial asthma is characterized by airway hyperresponsiveness(BHR) and inflammation. The cyclooxygenase(COX) is believed to be one of the important enzymes in these inflammatory reactions. Recently, the COX was divided into two isoforms, COX1 and COX2. COX2 is induced by lipopolysaccharide and some cytokines at the inflammation site. Prostaglandin E2(PGE2), produced from COX2, may affect airway inflammation. The purpose of this study is to evaluate the effect of COX2 inhibitor on COX2 expression, plasma PGE2, airway resistance and histologic finding in an animal asthma model. Methods : Sprague-Dawley rats were divided into 3 groups. The normal control group did not receive any treatment, but the asthma control group was sensitized by ovalbumin but not treated with the COX2 inhibitor(nimesulide, Mesulid$^{(R)}$). The treatment group was sensitized and treated with nimesulide. Specific airway resistance(sRaw) before and after nimesulide ingestion was investigated. The PGE2 level in the plasma was examined and COX2 immunogold-silver stain on lung tissue was performed. Results: sRaw and eosionophilic infiltration on airway, which increased in the asthma control group, was compared to normal control(p=0.014). However, there was no difference in eosinophilic infiltration between asthma control and treatment groups(p=0.408) and no difference in COX2 expression on bronchiolar epithelium among the three groups. Plasma PGE2 levels were not statically different among the three groups. Conclusion: The role of COX2 in the allergen-induced BHR was not significant The effect of nimesulide was not observed on BHR, COX2 expression, and plasma PGE2 level. Therefore, COX2 may not be a major substance of allergic asthma.