• The Korean Journal of Pharmacology
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• v.27 no.2
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• pp.145-153
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• 1991

Human neutrophil cathepsin-G, which has been known as one of the active enzymes causing inflammatory diseases, was purified by two steps procedure involving one size exclusion (Ultorogel AcA54) and one ion exchange (CM-Sephadex) chromatography. Purified HNCGs were cross-reacted with Anti-HNCathepsin-G antibodies which were radised in rabbits and purified by cathepsin-G labeled Sepharose 4B affinity chromatography. HNCGs were effectively inhibited by NSAIDs including phenylbutazone, sulindac, oxyphenbutazone, salicylic acid and salicyluric acid. $IC_{50}_s$ of these drugs for inhibition of Cathepsin G were 0.3-0.8 mM. Other NSAIDs including aspirin showed little or no inhibition effect on the activity of Cathepsin G. These results strongly indicated that NSAIDs which showed inhibition effect on the activity of HNCGs possibly be at least a part of mechanism of action which might be related to direct inhibition of cathepsin G at the tissue destruction sites beside of their known mechanism of action as an anticyclo-oxygenase in treatment of inflammatory diseases. Lipid soluble component of Korean Red Ginseng which was known as an anti-inflammatory agent inhibited HNCGs strongly, but no other fractions did inhibited HNCGs. Antibiotics including novobiosin and rifamycin showed some inhibition effect on HNCGs, i. e.., $IC_{50}$ of these drugs were 2.6 mM and 1.5 mM respectively, and other antibiotics including penicillin G showed no or negligible inhibition effect on the activity of HNCGs. However. tetracyclines inhibited HNCGs very effectively at the concentration of therapeutic range. The inhibition effect of the activity of HNCGs by tetracycline are not related to the N-dimethyl radical on the 4 position of the tetracycline molecule. Furthermore, N-dedimethylated tetracyclines may have beneficial effect for long term treatment of chronic inflammatory diseases without developing any drug resistance to microorganisms.

• Tuberculosis and Respiratory Diseases
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• v.52 no.6
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• pp.590-596
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• 2002

Background : Lung cancer is the leading cause of malignant pleural effusions, which is currently most commonly treated using pleurodesis via bedside thoracostomy. Several agents had been used for the treatment of pleural sclerosis, but with differing efficacies and associated side effects. Our purpose with this study was to compare the efficacy, side effects and disease free survival times of patients being treated with OK-432 and doxycycline sclerotherapy in lung cancer induced malignant pleureal effusions. Materials and Methods : 79 patients who underwent pleurodesis with OK-432 and doxycycline, between Jan.1994 and Aug. 2001, were retrospectively reviewed. Response 30 days following pleurodesis were determined from chest radiographs, with the disease free survival time being evaluated according to the response. Results : The success rates, 30 day followint pleurodesis, with OK-432 and doxycycline 83 and 87%, respectively (p=0.677). With regard to the side effects, fever was more common when OK-432 was used (59%, p=0.001), and pain was more common with doxycycline use (73%, p=0.008). There was no significant difference in disease free survival times between OK-432 (13.6 Months) and doxycycline (11.6 Months) (p=0.532). Conclusion : with the use of OK-432, for pleurodesis, was as effective as doxycycline, can be considered as an alternative treatment for malignant effusion in patients with lung cancer.

• Tuberculosis and Respiratory Diseases
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• v.60 no.4
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• pp.404-411
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• 2006

Purpose : Multidrug-resistant tuberculosis (MDR-TB) is an emerging threat to human beings. However, there is little data on the current status of MDR-TB in Korea. This study investigated the current status of MDR-TB in Korea using a survey of all the data from drug susceptibility tests (DST) performed across the country over the last three years. Method : The DST results between Jan. 2000 and Dec. 2002 from 7 laboratories, which were in charge of all antituberculous DSTs across the country as of March 2002, were collected and analyzed to determine the actual number of drug-resistant or MDR-TB patients, annual trend, degree and pattern of resistance against anti-TB drugs, etc. Results : Six laboratories used the absolute concentration method for DST and one used the proportional method. 59, 940 tests had been performed over the 3 year study period. The number of DST performed annually was 18,071, 19,950, and 21,919 in 2000-2002, respectively. The number of resistant tuberculosis patients (resistant against at least one anti-TB drug) had increased by 16.9% from 6,338 in 2000 to 7,409 in 2002. The rate of resistant tuberculosis among all DST results was 35.1% in 2000, 34.5% in 2001, and 33.8% in 2002. The number of MDR-TB patients (resistant against at least both isoniazid and rifampin) showed an increasing trend (14.5%) from 3,708 in 2000 to 4,245 in 2002. Conclusion : Approximately 4,000 MDR-TB cases are newly identified by DST annually and the number is showing an increasing trend. This study suggests that in order to cope with the current MDR-TB situation, the DST methods will need to be standardized and more aggressive measures will be required.

• The Korean Journal of Nuclear Medicine
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• v.38 no.2
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• pp.161-170
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• 2004

Molecular Nuclear Neuro-Imaging in "CNS" drug discovery and development tan be divided into four categories that are clearly inter-related.(1) Neuroreceptor mapping to examine the involvement of specific neurotransmitter system in CNS diseases, drug occupancy characteristics and perhaps examine mechanisms of action;(2) Structural and spectroscopic imaging to examine morphological changes and their consequences;(3) Metabolic mapping to provide evidence of central activity and "CNS fingerprinting" the neuroanatomy of drug effects;(4) Functional mapping to examing disease-drug interactions. In addition, targeted delivery of therapeutic agents could be achieved by modifying stem cells to release specific drugs at the site of transplantation('stem cell pharmacology'). Future exploitation of stem cell biology, including enhanced release of therapeutic factors through genetic stem cell engineering, might thus constitute promising pharmaceutical approaches to treating diseases of the nervous system. With continued improvements in instrumentation, identification of better imaging probes by innovative chemistry, molecular nuclear neuro-imaging promise to play increasingly important roles in disease diagnosis and therapy.

• Korean journal of applied entomology
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• v.15 no.2 s.27
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• pp.57-60
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• 1976

Experiments were carried out to determine the effectiveness of a new systemic fungicide EL-291 (5-Methyl-1, 2,4-triazolo (3,4-b) benzothiazole) for the control of rice blast disease in greenhouse and paddy field. The efficiency of EL-291 was much greater when applied before inoculation than when applied after inoculation. Kasugamin and Benlate were most effective as eradicants. For control of leaf blast, effectiveness of EL-291 was not significantly different than either Kasugamin or Benlate. However, EL-291 was considered more economical and reliable than either Kasugamin or Benlate. EL-291 required only a single foliar application or a transplant root soak, whereas two applications of the other fungicides were required. EL-191 was also more effective against panicle blast when applied only once, compared with two applications of Kasugamin or Benlate. The highest riceyields were obtained in plots treated with EL-29l.

• Parasites, Hosts and Diseases
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• v.24 no.1
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• pp.3-141
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• 1986

간흡충은 우리나라를 비롯하여 중국, 대만, 일본 및 월남등지에 널리 분포되어 있으며 1947년에 Stoll씨의 통계에 의하면 세계적으로 1,900만명이 넘는 감염자가 있다고 하였다. 현재 우리나라에서만 약 200만명의 간흡충 감염자가 있을 것으로 추산되고 있다. 간흡충은 McConnell이 1874년에 인도의 Calcutta에서 한 중국인의 간담도에서 본충을 처음 발견한 것이다. 이것을 Cobbold(1875)가 Distoma sinense라고 명명하였다가 후에 Looss (1907)가 Clonorchis sinensis라고 하였다. Kobayashi (1910)는 담수어가 간흡충감염의 중간숙주로 작용한다는 것을 처음으로 발견하였고 Muto (1918)에 의하여 왜우렁이가 제1중간숙주임을 발견함으로서 간흉충의 생활사가 확실해 졌다. Faust 및 Khaw (1927)에 의하여 중국에서 간흡충의 생물학 및 역학에 관한 광범한 연구업적이 발표된 이래 일본, 한국, 중국등 여러곳에서 많은 사람들에 의하여 연구되어 왔다. 그러나 적절한 치료방법이 없었고 또 민물고기를 생식하는 식습관과 위생시설의 미비등 여러가지 요인때문에 예방이 어려움에 직면하였다. 최근 다행히 새로이 개 발된 praziquantel이 간흡충중에 대하여 우수한 치료효과를 나타내고 집단치료에도 적합하다는 것이 증명됨으로서 간흡충증 예방과 관리에 큰 서광이 보이게 되었다. 따라서 간흉충증의 발생과 임상적 병증의 중요성을 좀 더 이해하기 위하여 간흡충체의 미세구조, 병인, 역학, 임상증상등 최근 알려진 새로운 지견과 우리나라에 있어서 간흡충증의 분포 및 유행지 형성 상황을 수학적으로 역학적 분석을 시도하였다. 그리고 과거 간흡충중의 화학치료에 관한 연구성적을 종합하여 화학요법제의 특성 빚 치료 적용여부에 대하여 논하였고 각약제의 시험관내 및 실험동물에 있어서의 살충효과와 임상시험에 있어서의 치료효과 및 부작용에 대하여 기술하였다. 그리고 새로 개발된 praziquantel의 간흡충에 대한 작용기전에 대하여도 논하였다. (중략)

• Journal of Korean Traditional Oncology
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• v.15 no.1
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• pp.119-128
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• 2010

항암치료는 현재 암환자의 주요한 치료임에도 불구하고 항암제내성과 같은 문제점을 가지고 있다. 약물내성은 다양한 기전에 의해 발생하는데 수송단백질의 과발현, 비독성화발현, 손상유전자의 복구, 세포사멸신호의 변화, STAT-3와 NF-${\kappa}B$의 발현 등이 포함된다. 암세포는 저산소환경에서 발생하며 일반세포에 비해 무산소해당에 상대적 의존도가 높고 이는 암세포의 성장과 전이를 촉진하는 인자가 된다. 항암제가 효과를 내기 위해서는 산소가 필요한데 저산소환경은 이를 방해하며 또한 유전자의 불안정화로 인해 약물내성이 유도된다. NF-${\kappa}B$는 주요 전사인자 중 하나로서 각종 염증과 암에서 지속적으로 활성화되며 암세포의 변화, 증식, 침윤, 전이에 관여한다. 환경적 스트레스 등과 대부분의 항암약제들이 NF-${\kappa}B$를 활성화시키며 임상적으로도 암환자의 생존과 연관된 중요한 예후인자이다. NF-${\kappa}B$의 발현은 항암제로 인한 암세포의 자멸을 회피하게 만들고 수송단백질을 활성화시켜 항암제내성을 유도한다. 강황, 적포도, 고추, 건칠 등 다양한 천연물에서 NF-${\kappa}B$를 억제시키는 효능이 발견되었으며 이는 항암제내성을 억제시키고 항암제의 효과를 증대시킨다. 저산소환경의 개선과 NF-${\kappa}B$의 억제는 상호연관성을 가지고 있으며 항암제내성의 개선뿐만 아니라 암치료제 개발의 새로운 연구목표가 될 수 있다.

• Journal of Pharmaceutical Investigation
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• v.34 no.1
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• pp.1-14
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• 2004

A promising approach to the development of a new single-step vaccine, which would eliminate the requirement for multiple injections, involves the encapsulation of antigens into microspheres. Biodegradable poly(lactide-co-glycolide) (PLGA) microspheres gave us a bright insight for controling antigen release in a pulsatile fashion, thereby mimicking two or tree boosting injections. However, in spite of the above merits, the level of immunization induced by a single-shot vaccination is often lower tan two doses of alum-adsorbed antigen. Therefore, optima modification of the microsphere is essential for the development of single-step vaccines. In the review, we discuss the stability of antigen in microsphere, safety and non-toxic in human and encapsulation technology. Also, we attempted to outline relevant physicochemical properties on the immunogenicity of microsphere vaccine and attainment of pulsatile release pater by combination of different microsphere, as well as to analyze immunological data associated with antigen delivery by microsphere. Although a lot of variables are related to the optimized microsphere formulation, we could conclude that judicious choice of proper polymer type, adjustment of particles size, and appropriate immunization protocol along with a suitable adjuvant might be a crucial factor for the generation of long-lasting immune response from a single-step vaccine formulation employing PLGA microsphere.

• The Korean Journal of Pesticide Science
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• v.3 no.3
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• pp.1-5
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• 1999

Novel O-quinolinylamidoxime derivatives were prepared by replacement of the carboxylic group at the 8 position of quinclorac with various amidoximes. In the flooded paddy conditions, most of the compounds show good herbicidal activity at a rate of 1 kg/ha. Some of them showed excellent herbicidal activity at a rate of 60 g/ha against barnyardgrass (Echinochloa aryicola) with good selectivity on rice. Under the two-leaf stage of barnyardgrass, most of O-quinolinylamidoximes showed good herbicidal activity, expecially compound 3c which showed excellent herbicidal activity barnyardgrass at a rate of 125 g/ha with good rice seletivity.

• Applied Biological Chemistry
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• v.45 no.2
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• pp.114-118
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• 2002

Phenalamides $A_1{\sim}A_3$ were reisolated as cytotoxic substances from culture broth of Myxococcus stipitatus JW111. The producing strain was isolated from the marine sediment collected off the shore of Geomun Island, Korea. The active principles were extracted from cell mass with acetone and successively purified by silica gel column chromatography, Sephadex LH-20 column chromatography, and finally recycling prep. HPLC. These compounds demonstrated significant cytotoxicity against certain human cancer cells, having $IC_50$ values ranging from 0.23 to 0.50 ${\mu}g/ml$. Moreover, they also inhibited the growth of adriamycin-resistant HCT/ADM human cancer cell line as well as its parent sensitive cell line.