目的 研究苦楝Melia azedarach皮的化学成分及其抗糖尿病活性。方法 运用正相、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鉴定结构，并测试所得化合物体外对葡萄糖激酶（GK）、组蛋白去乙酰化酶SIRT1激动活性和二肽基肽酶IV（DPPIV）、11β-羟基类固醇脱氢酶（11β-HSD）的抑制活性。结果 从苦楝皮甲醇提取物中分离得到6个三萜和3个甾体化合物，分别鉴定为meliastatin 3（1）、苦楝酸（2）、苦楝萜酮内酯（3）、sendanolactone（4）、南岭楝酮B（5）、20, 24-环甘遂烷-7(8)-烯-16β, 21α, 25-三羟基-3-酮（6）、3β-羟基-5, 8-环氧麦角甾-6, 22-二烯（7）、2β, 3β, 4β-三羟基-孕甾-16-酮（8）、3β-羟基-孕甾-5, 17 (20)-二烯-16-酮（9）。化合物2对人11β-HSD1的IC₅₀值为54.15 nmol/L。结论 化合物6～9为首次从该植物中分离得到，受试化合物1～4均未表现出GK、SIRT1体外激动活性和DPPIV抑制活性，但化合物2对人11β-HSD具有良好的选择性。

Objective To investigate the chemical constituents from the barks of Melia azedarach and their antidiabetes activities. Methods The constituents were isolated and purified by silica gel, reverse phase silica gel, and Sephadex LH-20 column chromatography, and their structures were identified by spectra and physiochemical characteristic analysis. The agonist activities of the isolated triterpenoids against glucokinase (GK) and SIRT1, and the inhibitory activity against dipeptidyl peptidasesIV (DPPIV), and 11β-hydroxysteroid dehydrogenase (11β-HSD) were tested in vitro. Results Six triterpenoids and three sterols were obtained from MeOH extract in the barks of M. azedarach and were elucidated as meliastatin 3 (1), kulonic acid (2), kulactone (3), sendanolactone (4), dubione B (5), 20, 24-cyclotirucalla-7(8)-en-16β, 21α, 25-trihydroxy-3-one (6), 3β- hydroxy-5, 8-epidioxy-ergosta-6, 22-diene (7), 2β, 3β, 4β-trihydroxy-pregn-16-one (8), and 3β-hydroxy-pregn-5, 17 (20)-dien-16-one (9). Compound 2 showed the inhibitory activity against 11β-HSD1 with the IC₅₀ value of 54.15 nmol/L. Conclusion Compounds 6—9 are obtained from this species for the first time. The tested compounds 1—4 are inactive against GK, SIRT1, and DPPIV, but compound 2 shows high selectivity against human 11β-HSD.

国家自然科学基金资助项目（81360477）；“973”计划前期研究专项（2011CB512005）；国家重点实验室培育基地——广西壮族自治区药用资源化学与药物分子工程重点实验室基金（CMEMR2012-B05）；2012年度广西高等学校优秀人才资助计划