Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (7): 1860-1863.DOI: 10.6023/cjoc201701002 Previous Articles     Next Articles

Notes

大别山五针松松针中二萜成分及其蛋白酪氨酸磷酸酶1B抑制活性研究

李明, 胡长玲, 韩晗, 熊娟, 胡金锋   

  1. 复旦大学药学院 天然药物化学教研室 上海 201203
  • 收稿日期:2017-01-04 修回日期:2017-02-19 发布日期:2017-03-08
  • 通讯作者: 胡金锋 E-mail:jfhu@fudan.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21472021,81273401,81202420)、教育部高等学校博士学科点(博导类)基金(Nos.20120071110049,20120071120049)和国家重点基础研究发展规划(973计划,No.2013CB530700)资助项目.

Diterpenoids from the Needles of the Endangered Plant Pinus dabeshanensis and Their Protein Tyrosine Phosphatase 1B Inhibitory Effects

Li Ming, Hu Changlin, Han Han, Xiong Juan, Hu Jinfeng   

  1. Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203
  • Received:2017-01-04 Revised:2017-02-19 Published:2017-03-08
  • Contact: 10.6023/cjoc201701002 E-mail:jfhu@fudan.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.21472021,81273401,81202420),the Ph.D.Programs Foundation of Ministry of Education of China (Nos.20120071110049,20120071120049),and the National Basic Research Program of China (973 Program,No.2013CB530700).

One new, dabeshanensin L (1), and nine known diterpenoids with diverse structures were isolated from the 90% MeOH extract of the needles (30 g dried mass-limited samples) of Pinus dabeshanensis, an endangered conifer listed in the China Plant Red Data Book (CPRDB). The new structure was established by detailed analysis of its spectroscopic data (IR, 1D/2D NMR, HRMS). Among the isolates, isopimara-7-en-18-oic acid (4), trans-abienol (6), and lambertianic acid (8) showed significant inhibitory activities against the human protein tyrosine phosphatase 1B (PTP1B) enzyme, a key target for the treatment of type-Ⅱ diabetes and obesity, with IC50 values ranging from 14.6 to 37.7 μmol/L.

Key words: endangered plant, Pinus dabeshanensis, diterpenoids, dabeshanensin L, PTP1B inhibition