丹顶草中抑制蛋白酪氨酸磷酸酯酶1B活性的三萜类化合物研究

doi:10.5246/jcps.2012.02.023

丹顶草中抑制蛋白酪氨酸磷酸酯酶1B活性的三萜类化合物研究

崔龙^*, 李志, 孙亚楠, 张南, 金永镐

1. 北华大学药学院, 吉林吉林市 132013
2. 中国石油吉林石化公司, 吉林吉林市 132021
3. 忠南大学药学院, 大韩民国大田直辖市, 305-764

收稿日期:2011-09-26 修回日期:2011-12-01 出版日期:2012-03-15 发布日期:2012-03-15
通讯作者: 崔龙*

Inhibition of protein tyrosine phosphatase 1B activity by triterpenes isolated from Aceriphyllum rossii

Long Cui^*, Zhi Li, Ya-Nan Sun, Nan Zhang, Young-Ho Kim

1. College of Pharmacy, Beihua University, Jilin 132013, China
2. China Petroleum Jilin Petrochemical Co., Ltd., Jilin 132021, China
3. College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea

Received:2011-09-26 Revised:2011-12-01 Online:2012-03-15 Published:2012-03-15
Contact: Long Cui*

摘要/Abstract

摘要： 利用生物活性导向分离方法, 从丹顶草提取物中筛选出有效抑制蛋白酪氨酸磷酸酯酶1B (PTP1B) 活性的四个三萜类化合物, 通过文献比较分别鉴定为aceriphyllic acid C (1), aceriphyllic acid D (2), aceriphyllic acid E (3)和aceriphyllic acid F (4)。所得化合物1-4有效抑制PTP1B活性的IC₅₀值范围在 (2.1±1.5) μmol/L到 (11.2±2.5) μmol/L之内。化合物1和2的动力学分析结果显示齐墩果烷型三萜类化合物以混合形式抑制PTP1B活性。

关键词: 丹顶草, 蛋白酪氨酸磷酸酯酶1B, 三萜类化合物, 生物活性导向分离

Abstract: An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B (PTP1B) inhibition. Bioassay guided fractionation resulted in the isolation of PTP1B inhibitory activity of triterpenes (1-4). These four compounds were identified as aceriphyllic acid C (1), aceriphyllic acid D (2), aceriphyllic acid E (3) and aceriphyllic acid F (4). The isolated 1-4 compounds inhibited PTP1B with IC₅₀ values ranged from (2.1±1.5) μmol/L to (11.2±2.5) μmol/L. Kinetic analysis of PTP1B inhibition by aceriphyllic acid C (1) and aceriphyllic acid D (2) suggested that oleanane-type triterpenes inhibited PTP1B activity in a mixed-type manner.

Key words: Aceriphyllum rossii, Protein tyrosine phosphatase 1B, Triterpenes, Bioassay guided

中图分类号:

R962

Supporting:

Foundation items: The Scientific Research Foundation for the Returned Overseas Chinese Scholars (Grant No. 20091590), State Education Ministry and Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules (Yanbian University), Ministry of Education, China (Grant No. 201003).
^*Corresponding author. Tel.: 86-432-64608281

崔龙^*, 李志, 孙亚楠, 张南, 金永镐. 丹顶草中抑制蛋白酪氨酸磷酸酯酶1B活性的三萜类化合物研究[J]. , DOI: 10.5246/jcps.2012.02.023.

Long Cui^*, Zhi Li, Ya-Nan Sun, Nan Zhang, Young-Ho Kim. Inhibition of protein tyrosine phosphatase 1B activity by triterpenes isolated from Aceriphyllum rossii [J]. , DOI: 10.5246/jcps.2012.02.023.