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

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

从濒危植物大别山五针松(Pinus dabeshanensis)松针(干重仅30 g)的90%甲醇提取物中分离得到10个二萜类化合物,其中新化合物dabeshanensin L(1)的结构是通过运用1D/2D NMR等波谱手段进行确证的.体外活性测试结果表明化合物isopimara-7-en-18-oic acid(4)、trans-abienol(6)和lambertianic acid(8)对蛋白酪氨酸磷酸酶1B(PTP1B)有显著的抑制作用,其IC_(50)值在14.6~37.7μmol/L之间.

One new, dabeshanensin L（1）, and nine known diterpenoids with diverse structures were isolated from the 90% Me OH 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.