从中华青荚叶中分离得到的甘草素和异甘草素对黄嘌呤氧化酶的抑制作用。
Inhibition of xanthine oxidase by liquiritigenin and isoliquiritigenin isolated from Sinofranchetia chinensis.
作者信息
Kong L D, Zhang Y, Pan X, Tan R X, Cheng C H
机构信息
State Key Laboratory of Pharmaceutical Biotechnology, Institute of Pharmaceutical Biology and Phytochemistry, Nanjing University, China.
出版信息
Cell Mol Life Sci. 2000 Mar;57(3):500-5. doi: 10.1007/PL00000710.
The methanol extract of the stem of Sinofranchetia inhibited the activity of xanthine oxidase in vitro. Bioassay-guided purification led to the isolation ofliquiritigenin and isoliquiritigenin as the main xanthine oxidase inhibitors. This inhibition of enzyme activity was found to be dose dependent, with an IC50 value of approximately 49.3 microM for liquiritigenin and 55.8 microM for isoliquiritigenin. Lineweaver-Burk transformation of the inhibition data indicated that the inhibition was of a mixed type for both liquiritigenin and isoliquiritigenin. For liquiritigenin, the Ki and K(I) were determined to be 14.0 microM and 151.6 microM, respectively. For isoliquiritigenin, the Ki and K(I) were determined to be 17.4 microM and 81.9 microM, respectively. These results suggest that these natural products could be used to treat conditions where the inhibition of xanthine oxidase is warranted.
猫儿屎茎的甲醇提取物在体外抑制黄嘌呤氧化酶的活性。通过生物活性导向的纯化方法，分离得到了甘草素和异甘草素作为主要的黄嘌呤氧化酶抑制剂。发现这种酶活性抑制具有剂量依赖性，甘草素的IC50值约为49.3微摩尔，异甘草素的IC50值约为55.8微摩尔。对抑制数据进行Lineweaver - Burk转换表明，甘草素和异甘草素的抑制作用均为混合型。对于甘草素，Ki和K(I)分别测定为14.0微摩尔和151.6微摩尔。对于异甘草素，Ki和K(I)分别测定为17.4微摩尔和81.9微摩尔。这些结果表明，这些天然产物可用于治疗有必要抑制黄嘌呤氧化酶的病症。
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