苦楝化学成分及抗糖尿病活性研究

Chemical Constituents from Melia azedarach and Their Anti-diabetes Activities

为研究苦楝皮的化学成分及其抗糖尿病活性，采用正相、反相及Sephadex LH-20凝胶柱色谱等方法分离纯化化合物，通过波谱数据和理化性质分别鉴定为12β，20（S）-dihydroxydammar-24-en-3one（1），dammarendiol Ⅱ3-0-caffeate（2），24-methylenecyclosnenone（3），meliavolin（4），3，20-diacetyl-11-methoxy-1-tigloylmeliacarpinin（5），methyl3-formyl-2，4-dihydroxy-6．methylbenzoate（6），usnicacid（7），epi-catechin（8）。其中化合物1～3，6，7均为首次从该植物中分离得到。采用酶偶联、液闪接近测定等技术测试化合物2～5体外抗糖尿病活性。研究结果表明，受试化合物2～5均未表现出GK、SIRTl体外激动活性和DPPIV抑制活性，但化合物2对人11β-HSD1具有显著的抑制作用（IC50=94．15nmol／L）。

The chemical constituents from the barks of Melia azedarach were isolated by silica gel, reverse phase silica gel and Sephadex LH-20 column chromatography, and their anti-diabetes activities were subsequently evaluated. Eight compounds were obtained and elucidated as 12β,20 （S）-dihydroxydammar-24-en-3-one （1）, dammarendiol II 3-O-caf- feate（2） ,24-methylenecycloartenone（3 ）, meliav.olin （4） ,3,20-diacetyl-11-methoxy- 1-tigloylmeliacarpinin （5）, methyl 3-formyl-2,4-dihydroxy-6-methyl benzoate （6）, usnic acid （7） and epi-catechln （8） based on their spectra and physio- chemical characteristics. Among these, compounds 1-3,6, and 7 were isolated from this species for the first time. All the tested compounds 2-5 were inactive against GK, SIRT1 and DPPIV, but compounds 2 showed significant inhibitory activi- ty against human 11β-HSD1 with IC50 value of 94.15 nmol/L.