• Applied Biological Chemistry
• /
• v.41 no.6
• /
• pp.477-482
• /
• 1998

In order to discover new Leukotriene $D_4$ antagonists, Quantitative Structure-Activity Relationships (QSAR) were applied based on the known data. A series of chalcone derivatives were selected for the training set. A candidate was predicted using QSAR and synthesized, and its biological activity was tested.

• Journal of Applied Biological Chemistry
• /
• v.44 no.1
• /
• pp.35-38
• /
• 2001

• 한국생물공학회:학술대회논문집
• /
• 2005.10a
• /
• pp.960-960
• /
• 2005

• Journal of Integrative Natural Science
• /
• v.9 no.4
• /
• pp.228-233
• /
• 2016

Cysteinyl leukotrienes are inflammatory mediators having important role in pathophysiological conditions such as asthma and allergic rhinitis. CysLT1 receptor mediates most of the disease regulatory actions of the CysLTs and it is been implicated in a number of inflammatory conditions including gastrointestinal and cardiovascular diseases. Hence in the present study, molecular docking of CysLT1 was performed with its potent and orally efficacious antagonist CP-199330 and CP-199331. The aim of this study was to compare the interaction of CP-199330 and CP-199331 with known drugs such as Zafirlukast, Pranlukast and Montelukast which had already showed clinical efficacy in the treatment of asthma. The residues such as TYR83, GLN274, LYS311 and SER313 were found to interact with both the antagonist and the known drugs. Also, we noticed the docking scores and interaction of the antagonists were comparable with the known drugs. Hence these antagonists could serve as better drugs for the treatment of allergy.

• Journal of Applied Biological Chemistry
• /
• v.48 no.2
• /
• pp.97-100
• /
• 2005

Chiral dienophile 5 was synthesized from D-glucose by consecutive diisopropylidenation, partial deprotection, diol cleavage, and Wittig reactions. Under thermal conditions, asymmetric Diels-Alder reaction between chiral dienophile and cyclopentadiene gave four possible chiral norbornenes stereoisomers whose absolute configurations were determined through CADD and NMR.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2001.11a
• /
• pp.23-31
• /
• 2001

MBST at 4hr and SST at 3hr after oral administration remarkably inhibited histamine release from rat mast cells in a dose-dependent manner. MBST treated GPs failed to show biphasic phenomena which indicated to reduce nasal volume as leukotriene antagonists. Both groups of patients who took MBST and SST for 1 week or 2weeks showed significant decreased symptom severity index(SSI) from treatment week 2(p<0.05). The percent volume change after challenge of the antigen was decreased in patients took the extracts for tweets. We abstained longer suppression of the symptom than antihistamine.

• Clinical and Experimental Pediatrics
• /
• v.48 no.7
• /
• pp.766-771
• /
• 2005

Purpose : Cysteinyl leukotrienes are important inflammatory mediators in the pathogenesis of asthma; therefore interruption of cysteinyl leukotrienes by leukotriene receptor antagonists improves clinical symptoms in the management of patients with mild to moderate asthma. We evaluated whether clinical response to montelukast, a leukotriene receptor antagonist, in childhood asthma was predicted by genotypes of leukotriene $C_4$ synthase($LTC_4S$) promoter gene polymorphism. Methods : An 8-week prospective, open trial of montelukast was carried out in 161 children with mild to moderate asthma. Genotyping of $LTC_4S$ gene polymorphism was determined by restriction fragment length polymorphism. Results : The distribution of the $LTC_4S$ genotypes AA, AC, and CC was 70.8 percent, 23.6 percent, and 5.6 percent, respectively in asthma group and 74.0 percent, 22.6 percent, and 3.4 percent, respectively in control group. A statistically significant difference in the distribution of $LTC_4S$ genotype was not observed between the asthma and the control groups, and there was no significant difference between the $LTC_4S$ genotype and asthma severity. The responders to montelukast were significantly prevalent in the mild asthma group(P<0.05). There was no significant difference in the distribution of the responders compared to non-responders within genotype in the total asthma group or the moderate asthma group. However, the responsiveness for montelukast was significant difference within genotype for both AA and AC/CC in the mild asthma group : The AA genotype was more included in the responder group(P<0.05). Conclusion : In the mild persistent asthma group, the A allele of $LTC_4S$ polymorphism may be regarded as a predictable factor for clinical response to montelukast. However, LTC4S polymorphism was not significantly associated with the clinical response to montelukast in asthmatic children.

• YAKHAK HOEJI
• /
• v.56 no.2
• /
• pp.126-135
• /
• 2012

Purpose: To develop therapeutic duplication criteria for the drugs used for respiratory diseases. Method: Therapeutic duplication was defined as "more than 2 drug ingredient-usage in which each has the same therapeutic effect and combination therapy does not confer additional therapeutic benefit". Respiratory system drugs approved in Korea were examined for the study. The WHO's Anatomical Therapeutic Chemical Classification System was used for grouping of the corresponding drug ingredients. The principles and recommendations on combination usage or multiple drug regimens were reviewed by using the clinical practice guidelines, textbooks, product labelings, and clinical articles. Clinical expert group consultation was performed and expert opinions were incorporated into the final criteria. Results: Nine hundred sixty two drug products with Korean Food and Drug Administration classification codes of 141, 149, 222, and 229 were evaluated, of which 87 active ingredients were composed. The drug ingredients were classified into 12 groups (antihistamines, oral nasal decongestants, leukotriene receptor antagonists, inhaled anticholinergics, inhaled corticosteroids, oral ${\beta}2$-agonists, long-acting ${\beta}2$-agonists, short-acting ${\beta}2$-agonists, xanthines, antiallergics, mucolytics and cough suppressants). The use of more than 2 drug ingredients including the same group was therapeutic duplication, and thus combination should be recommended not to be used. Conclusion: Twelve drug groups were identified as therapeutic duplication criteria. Combination therapy within each group should not be used otherwise therapeutic benefits outweigh potential risks.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.24 no.3
• /
• pp.134-145
• /
• 1998

Facial hyperpigmentation in women, which is considered to be a serious cosmetic disability and a cause of mental distress, requires proper management. Melanocyte dendricity is a crucial factor affecting epidermal pigmentation. We found that BQ-788, the endothelin-B (ETB) receptor antagonist, blocks the formation of multi-dendricity which is induced by cocultured keratinocytes. Melanocytes in vivo show numerous dendrites which are in close contact with multiple keratinocytes, forming the epidermal-melanin unit. While melanocytes transfer their melanosomes into the neighboring keratinocytes via dendrites, keratinocytes secrete many growth factors and cytokines that influence viability, morphology, and melanin formation of melanocytes. Endothelin-1 (ET-1), prostaglandin E2(PGE2), and leukotriene-C4 (LT-C4) have been suggested as the candidates for increasing dendricity. Other reports suggested that ET-1 has stimulatory effects on proliferation and melanin formation of melanocytes in vitro. In the present study, using type-specific ET receptor antagonists, we observed how the morphology of melanocytes could be modulated in a coculture system. In addition, the roles of ET-1 for morphology and proliferation on melanocytes were evaluated in different culture media. We suggest that ET-1 increases dendricity and proliferation of melanocytes, and that its dendrite-inducing effect and mitogenic effect are regulated independently.

• Tuberculosis and Respiratory Diseases
• /
• v.85 no.1
• /
• pp.11-17
• /
• 2022

Background: In asthma, consistent control of chronic airway inflammation is crucial, and the use of asthma-controller medication has been emphasized. Our purpose in this study is to compare the incidence of acute exacerbation and healthcare costs related to the use of asthma-controller medication. Methods: By using data collected by the National Health Insurance Review and Assessment Service, we compared one-year clinical outcomes and medical costs from July 2014 to June 2015 (follow-up period) between two groups of patients with asthma who received different prescriptions for recommended asthma-controller medication (inhaled corticosteroids or leukotriene receptor antagonists) at least once from July 2013 to June 2014 (assessment period). Results: There were 51,757 patients who satisfied our inclusion criteria. Among them, 13,702 patients (26.5%) were prescribed a recommended asthma-controller medication during the assessment period. In patients using a recommended asthma-controller medication, the frequency of acute exacerbations decreased in the follow-up period, from 2.7% to 1.1%. The total medical costs of the controller group decreased during the follow-up period compared to the assessment period, from $3,772,692 to $1,985,475. Only 50.9% of patients in the controller group used healthcare services in the follow-up period, and the use of asthma-controller medication decreased in the follow-up period. Conclusion: Overall, patients using a recommended asthma-controller medication showed decreased acute exacerbation and reduced total healthcare cost by half.