首页> 外国专利> KS 513 a novel compound KS 513 isolated from the extract of Pseudolysimachion rotundum var. subintegrum and the composition comprising the same as an active ingredient for preventing or treating allergy disease inflammatory disease asthma or chronic obstructive pulmonary disease

KS 513 a novel compound KS 513 isolated from the extract of Pseudolysimachion rotundum var. subintegrum and the composition comprising the same as an active ingredient for preventing or treating allergy disease inflammatory disease asthma or chronic obstructive pulmonary disease

机译:KS 513是一种新的化合物KS 513,从圆形假单胞菌提取物中提取。亚整合体和包含其的组合物作为预防或治疗变态反应性疾病炎性疾病哮喘或慢性阻塞性肺疾病的活性成分

摘要

The present invention relates to a novel compound isolated from an acidic extract of Pseudomonas sp., An extract of (3R, 5S, 5aS, 6R, 7S, 8R, 8aS) -8-chloro-8a-hydroxy- (3R, 5S, 5aS, 6R, 7S, 6S, 6S, 6R, 6S) 8R, 8aS) -8-chloro-8a-hydroxy-5- (2-hydroxy acetoxy) hexahydro-1H-3,6-methanocyclopenta [e] [1,3] dioxepin-7-yl 3,4-dihydroxybenzoate} Inflammatory, asthma or chronic obstructive pulmonary disease, which comprises, as an active ingredient, an anti-inflammatory agent (KS-513) as an active ingredient. Test of cell viability in RAW264.7 cells (Experimental Example 1) for the compounds according to the present invention; Effects of iNOS and COX-2, the precursor inflammatory mediator genes that induce gene expression in RAW 264.7 cells treated with LPS, and IL-1β, IL-6, and TNF-α mRNA expression levels of precursor inflammation-mediated cytokine genes Experiment (Experimental Example 2); Inhibition experiment on protein expression and NO production concentration of enzyme gene iNOS associated with NO production (Experimental Example 3); Inhibition experiment on the protein expression and PGE 2 production concentration of the precursor inflammatory mediator gene COX-2 (Experimental Example 4); Inhibition of production of NO and PGE 2 induced by LPS in RAW 264.7 cells, inhibition of iNOS and COX-2 protein by RAE 264.7 cells, inhibition of proinflammatory cytokines TNF-α, IL-1β and IL- And the expression of the gene and suppresses the secretion amount of TNF-α, IL-1β and IL-6, which are proinflammatory mediators of the proinflammatory cytokines, and the composition is used for the prevention and treatment of inflammation, asthma or chronic obstructive pulmonary disease A pharmaceutical composition, a health functional food or a health supplement.
机译:本发明涉及从假单胞菌属(Pseudomonas sp。)的酸性提取物中分离的新型化合物,所述提取物是(3R,5S,5aS,6R,7S,8R,8aS)-8-氯-8a-羟基-(3R,5S, 5aS,6R,7S,6S,6S,6R,6S)8R,8aS)-8-氯-8a-羟基-5-(2-羟基乙酰氧基)六氢-1H-3,6-甲基环戊[e] [1, [3] 3,4-二羟基苯甲酸酯-7-二氧杂pin-7-基炎性,哮喘或慢性阻塞性肺疾病,其包含作为有效成分的消炎剂(KS-513)作为有效成分。测试本发明化合物在RAW264.7细胞中的细胞生存力(实验实施例1); iNOS和COX-2的作用,诱导LPS处理的RAW 264.7细胞中基因表达的前体炎症介质基因,以及前体炎症介导的细胞因子基因的IL-1β,IL-6和TNF-αmRNA表达水平实验(实验例2);与NO产生相关的酶基因iNOS的蛋白质表达和NO产生浓度的抑制实验(实验例3);对前体炎症介质基因COX-2的蛋白表达和PGE 2 产生浓度的抑制实验(实验例4); LPS诱导的RAW 264.7细胞NO和PGE 2 的产生抑制,RAE 264.7细胞抑制iNOS和COX-2蛋白,抑制促炎细胞因子TNF-α,IL-1β和IL-并且该基因的表达并抑制作为促炎细胞因子的促炎介质的TNF-α,IL-1β和IL-6的分泌量,并且该组合物用于预防和治疗炎症,哮喘或慢性阻塞性疾病。肺部疾病药物组合物,保健食品或保健品。

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