Inhibitory effects of glycyrrhetinic Acid on DNA polymerase and inflammatory activities.
Inhibitory effects of glycyrrhetinic Acid on DNA polymerase and inflammatory activities.
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DOI：
10.1155/2012/650514
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
Yoshida M
中科院分区：
文献类型：
--
作者：
Ishida T;Mizushina Y;Yagi S;Irino Y;Nishiumi S;Miki I;Kondo Y;Mizuno S;Yoshida H;Azuma T;Yoshida M
我们研究了三种甘草素衍生物，如甘草素（化合物1）、甘草酸二钾（化合物2）和甘草次酸（化合物3）对哺乳动物pol活性的抑制作用。在这些衍生物中，化合物3是分别属于pols的B、A、Y和X家族的哺乳动物pols α、β、κ和λ的最强抑制剂，而化合物1和2显示中等抑制。在测试的这些衍生物中，化合物3在使用小鼠巨噬细胞RAW 264.7和源自小鼠的腹膜巨噬细胞的细胞培养系统中显示出对由脂多糖（LPS）诱导的肿瘤坏死因子-α（TNF-α）产生的最强抑制。此外，发现化合物3抑制核因子-κB（NF-κB）在工程化人胚肾（HEK）293细胞中的作用。此外，化合物3引起比化合物1和2更大的12-O-十四酰基佛波醇-13-乙酸酯-（TPA-）诱导的小鼠耳中急性炎症的减少。总之，本研究已经鉴定了化合物3，其是化合物1和2的糖苷配基，作为基于哺乳动物pol抑制的有希望的抗炎候选物。
We investigated the inhibitory effect of three glycyrrhizin derivatives, such as Glycyrrhizin (compound 1), dipotassium glycyrrhizate (compound 2) and glycyrrhetinic acid (compound 3), on the activity of mammalian pols. Among these derivatives, compound 3 was the strongest inhibitor of mammalian pols α, β, κ, and λ, which belong to the B, A, Y, and X families of pols, respectively, whereas compounds 1 and 2 showed moderate inhibition. Among the these derivatives tested, compound 3 displayed strongest suppression of the production of tumor necrosis factor-α (TNF-α) induced by lipopolysaccharide (LPS) in a cell-culture system using mouse macrophages RAW264.7 and peritoneal macrophages derived from mice. Moreover, compound 3 was found to inhibit the action of nuclear factor-κB (NF-κB) in engineered human embryonic kidney (HEK) 293 cells. In addition, compound 3 caused greater reduction of 12-O-tetradecanoylphorbol-13-acetate-(TPA-) induced acute inflammation in mouse ear than compounds 1 and 2. In conclusion, this study has identified compound 3, which is the aglycone of compounds 1 and 2, as a promising anti-inflammatory candidate based on mammalian pol inhibition.
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影响因子：
2.8
作者：
Lin, G;Nnane, IP;Cheng, TY
通讯作者：
Cheng, TY
影响因子：
5
作者：
Medeiros, Rodrigo;Otuki, Michel F.;Calixto, Joao B.
通讯作者：
Calixto, Joao B.
影响因子：
4.8
作者：
García-Díaz, M;Bebenek, K;Blanco, L
通讯作者：
Blanco, L
影响因子：
5.6
作者：
García-Díaz, M;Domínguez, O;Blanco, L
通讯作者：
Blanco, L
DOI：
10.1016/0167-4781(96)00121-2
发表时间：
1996-09-11
期刊：
BIOCHIMICA ET BIOPHYSICA ACTA-GENE STRUCTURE AND EXPRESSION
影响因子：
--
作者：
Mizushina, Y;Tanaka, N;Sakaguchi, K
通讯作者：
Sakaguchi, K