The fruit of Actinidia arguta (AA) has been used mainly for the treatment of skin diseases, diuresis, diabetes mellitus and osteoporosis in Korean traditional medicine. It is known that AA (hardy kiwi) fruit extract has an effect on 2-chloro-1,3,5-trinitrobenzene-induced atopic dermatitis-like skin ...
The fruit of Actinidia arguta (AA) has been used mainly for the treatment of skin diseases, diuresis, diabetes mellitus and osteoporosis in Korean traditional medicine. It is known that AA (hardy kiwi) fruit extract has an effect on 2-chloro-1,3,5-trinitrobenzene-induced atopic dermatitis-like skin lesions in NC/Nga mice. Mode of action for it is associated with the modulation of biphasic Th1/Th2 cytokines. Furthermore, DA9102 containing AA is a herbal medicine currently under phase II clinical trial for atopic dermatitis in Korea. However, no active principles of AA on the decrease of Th2 cytokines including IL-4 and IL-10 have been identified. In this study, bioactivity-guided fractionation of an alcohol extract from the dried fruits of AA using ELISA assay for IL-4 production led to the isolation of $\alpha$-linolenic acid (I), linoleic acid (II), ethyl linolenate (III), ethyl linoleate (IV) and ethyl stearate (V) as the major active components. These compounds showed the down-regulatory effects of IL-4 production in A23187-stimulated RBL-2H3 cells without cytotoxicity.
The fruit of Actinidia arguta (AA) has been used mainly for the treatment of skin diseases, diuresis, diabetes mellitus and osteoporosis in Korean traditional medicine. It is known that AA (hardy kiwi) fruit extract has an effect on 2-chloro-1,3,5-trinitrobenzene-induced atopic dermatitis-like skin lesions in NC/Nga mice. Mode of action for it is associated with the modulation of biphasic Th1/Th2 cytokines. Furthermore, DA9102 containing AA is a herbal medicine currently under phase II clinical trial for atopic dermatitis in Korea. However, no active principles of AA on the decrease of Th2 cytokines including IL-4 and IL-10 have been identified. In this study, bioactivity-guided fractionation of an alcohol extract from the dried fruits of AA using ELISA assay for IL-4 production led to the isolation of $\alpha$-linolenic acid (I), linoleic acid (II), ethyl linolenate (III), ethyl linoleate (IV) and ethyl stearate (V) as the major active components. These compounds showed the down-regulatory effects of IL-4 production in A23187-stimulated RBL-2H3 cells without cytotoxicity.
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문제 정의
Although AA has high inhibitory effects on allergic diseases, the active compounds causing these effects have not been identified. The aim of the present study was to isolate components with anti-allergic activities from AA and elucidate their structures. Moreover, the deduction of these active compounds will be meaningful as candidates for regulatory reagents of atopic diseases.
This study focuses on the isolation and elucidation of compounds with IL-4 inhibitory activities from AA using an activity guided isolation method. The extract of A.
제안 방법
After 12 hours, the cultured media were taken to determine the level of IL-4 by ELISA (R&D systems, Minneapolis, MN, USA).
Activity tests were performed by ELISA assay to examine the down-regulatory effects on IL-4 production in the RBL-2H3 mast cell line. Structures of the compounds isolated were elucidated using EI-MS, 1H-NMR and 13C-NMR and confirmed by comparison of all spectroscopic data with literature values. All isolated compounds were determined to the series of fatty acids through spectral analyses.
대상 데이터
; Fisher Scientific, Schwerte, Germany) used for instrumental analysis were guaranteed grade reagent. Minimum Essential Medium (MEM), fetal bovine serum (FBS) and penicillin-streptomycin (PS) were purchased from Gibco-BRL (Grand Island, NY, USA). A23187 and dexamethasone were purchased from Sigma (St.
RBL-2H3 cells, which are from the mast cell line, were used for bioassay. RBL-2H3 cells were purchased from American Type Culture Collection (ATCC, Rockville, MD, USA). RBL2H3 cells were maintained in monolayer culture in Minimum Essential Medium (MEM, Gibco-BRL, Grand Island, NY, USA) supplemented with 15% (v/v) fetal bovine serum (FBS, GibcoBRL, Grand Island, NY, U.
RBL-2H3 cells were pre-treated with test samples at concentration that did not affect cell viability and then stimulated with A23187 for 12 hrs. Test samples were evaluated for suppression of the production of IL-4 in the concentration range without cell toxicity in A23187-simulated RBL-2H3 cells.
데이터처리
Statistical analysis was performed using one-way analysis of variance (ANOVA) followed by Student’s t-test.
성능/효과
In conclusion, the present results demonstrate that various compounds, such as linoleic acid, α-linolenic acid, ethyl linoleate, ethyl linolenate and ethyl stearate isolated from AA fruits, have potential as IL-4 production inhibitor.
In this study, according to the results of the down-regulatory effects on IL-4 production in RBL-2H3 cell, five compounds isolated had significant inhibitory activities. The results of the present study suggest that linolenic acid ethyl ester, linoleic acid ethyl ester, stearic acid ethyl ester, linolenic acid and linoleic acid, the five active compounds isolated from AA, are potent inhibitors of A23187-induced IL-4 production in RBL2H3 cells. These findings increase the importance of AA as a natural product and the five fatty acids as components for the suppression of IL-4 production correlated with an attack of allergic diseases.
참고문헌 (34)
Abbas, A. K., Murphy, K. M. and Sher, A. (1991) Functional diversity of
Bomford. R. (1981) The adjuvant activity of fatty acid esters. The role
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